Singulair

montelukast sodium

Dosage Form: tablets, chewable tablets, oral granules
FULL PRESCRIBING INFORMATION

Indications and Usage for Singulair

Asthma

Singulair® is indicated for the prophylaxis and chronic treatment of asthma in adults and pediatric patients 12 months of age and older.

Exercise-Induced Bronchoconstriction

Singulair is indicated for prevention of exercise-induced bronchoconstriction (EIB) in patients 15 years of age and older.

Allergic Rhinitis

Singulair is indicated for the relief of symptoms of seasonal allergic rhinitis in patients 2 years of age and older and perennial allergic rhinitis in patients 6 months of age and older.

Singulair Dosage and Administration

Asthma

Singulair should be taken once daily in the evening. The following doses are recommended:

For adults and adolescents 15 years of age and older: one 10-mg tablet.

For pediatric patients 6 to 14 years of age: one 5-mg chewable tablet.

For pediatric patients 2 to 5 years of age: one 4-mg chewable tablet or one packet of 4-mg oral granules.

For pediatric patients 12 to 23 months of age: one packet of 4-mg oral granules.

Safety and effectiveness in pediatric patients less than 12 months of age with asthma have not been established.

There have been no clinical trials in patients with asthma to evaluate the relative efficacy of morning versus evening dosing. The pharmacokinetics of montelukast are similar whether dosed in the morning or evening. Efficacy has been demonstrated for asthma when montelukast was administered in the evening without regard to time of food ingestion.

Exercise-Induced Bronchoconstriction (EIB) in Patients 15 Years of Age and Older

For prevention of EIB, a single 10 mg dose of Singulair should be taken at least 2 hours before exercise. An additional dose of Singulair should not be taken within 24 hours of a previous dose. Patients already taking Singulair daily for another indication (including chronic asthma) should not take an additional dose to prevent EIB. All patients should have available for rescue a short-acting β-agonist. Safety and effectiveness in patients younger than 15 years of age have not been established. Daily administration of Singulair for the chronic treatment of asthma has not been established to prevent acute episodes of EIB.

Allergic Rhinitis

For allergic rhinitis, Singulair should be taken once daily. Efficacy was demonstrated for seasonal allergic rhinitis when montelukast was administered in the morning or the evening without regard to time of food ingestion. The time of administration may be individualized to suit patient needs.

The following doses for the treatment of symptoms of seasonal allergic rhinitis are recommended:

For adults and adolescents 15 years of age and older: one 10-mg tablet.

For pediatric patients 6 to 14 years of age: one 5-mg chewable tablet.

For pediatric patients 2 to 5 years of age: one 4-mg chewable tablet or one packet of 4-mg oral granules.

Safety and effectiveness in pediatric patients younger than 2 years of age with seasonal allergic rhinitis have not been established.

The following doses for the treatment of symptoms of perennial allergic rhinitis are recommended:

For adults and adolescents 15 years of age and older: one 10-mg tablet.

For pediatric patients 6 to 14 years of age: one 5-mg chewable tablet.

For pediatric patients 2 to 5 years of age: one 4-mg chewable tablet or one packet of 4-mg oral granules.

For pediatric patients 6 to 23 months of age: one packet of 4-mg oral granules.

Safety and effectiveness in pediatric patients younger than 6 months of age with perennial allergic rhinitis have not been established.

Asthma and Allergic Rhinitis

Patients with both asthma and allergic rhinitis should take only one Singulair dose daily in the evening.

Instructions for Administration of Oral Granules

Singulair 4-mg oral granules can be administered either directly in the mouth, dissolved in 1 teaspoonful (5 mL) of cold or room temperature baby formula or breast milk, or mixed with a spoonful of cold or room temperature soft foods; based on stability studies, only applesauce, carrots, rice, or ice cream should be used. The packet should not be opened until ready to use. After opening the packet, the full dose (with or without mixing with baby formula, breast milk, or food) must be administered within 15 minutes. If mixed with baby formula, breast milk, or food, Singulair oral granules must not be stored for future use. Discard any unused portion. Singulair oral granules are not intended to be dissolved in any liquid other than baby formula or breast milk for administration. However, liquids may be taken subsequent to administration. Singulair oral granules can be administered without regard to the time of meals.

Dosage Forms and Strengths

• Singulair 10-mg Film-Coated Tablets are beige, rounded square-shaped tablets, with code MRK 117 on one side and Singulair on the other.


• Singulair 5-mg Chewable Tablets are pink, round, bi-convex-shaped tablets, with code MRK 275 on one side and Singulair on the other.


• Singulair 4-mg Chewable Tablets are pink, oval, bi-convex-shaped tablets, with code MRK 711 on one side and Singulair on the other.


• Singulair 4-mg Oral Granules are white granules with 500 mg net weight, packed in a child-resistant foil packet.

Contraindications

Hypersensitivity to any component of this product.

Warnings and Precautions

Acute Asthma

Singulair is not indicated for use in the reversal of bronchospasm in acute asthma attacks, including status asthmaticus. Patients should be advised to have appropriate rescue medication available. Therapy with Singulair can be continued during acute exacerbations of asthma. Patients who have exacerbations of asthma after exercise should have available for rescue a short-acting inhaled β-agonist.

Concomitant Corticosteroid Use

While the dose of inhaled corticosteroid may be reduced gradually under medical supervision, Singulair should not be abruptly substituted for inhaled or oral corticosteroids.

Aspirin Sensitivity

Patients with known aspirin sensitivity should continue avoidance of aspirin or non-steroidal anti-inflammatory agents while taking Singulair. Although Singulair is effective in improving airway function in asthmatics with documented aspirin sensitivity, it has not been shown to truncate bronchoconstrictor response to aspirin and other non-steroidal anti-inflammatory drugs in aspirin-sensitive asthmatic patients [see Clinical Studies (14.1)].

Neuropsychiatric Events

Neuropsychiatric events have been reported in adult, adolescent, and pediatric patients taking Singulair. Post-marketing reports with Singulair use include agitation, aggressive behavior or hostility, anxiousness, depression, disorientation, dream abnormalities, hallucinations, insomnia, irritability, restlessness, somnambulism, suicidal thinking and behavior (including suicide), and tremor. The clinical details of some post-marketing reports involving Singulair appear consistent with a drug-induced effect.

Patients and prescribers should be alert for neuropsychiatric events. Patients should be instructed to notify their prescriber if these changes occur. Prescribers should carefully evaluate the risks and benefits of continuing treatment with Singulair if such events occur [see Adverse Reactions (6.2)].

Eosinophilic Conditions

Patients with asthma on therapy with Singulair may present with systemic eosinophilia, sometimes presenting with clinical features of vasculitis consistent with Churg-Strauss syndrome, a condition which is often treated with systemic corticosteroid therapy. These events usually, but not always, have been associated with the reduction of oral corticosteroid therapy. Physicians should be alert to eosinophilia, vasculitic rash, worsening pulmonary symptoms, cardiac complications, and/or neuropathy presenting in their patients. A causal association between Singulair and these underlying conditions has not been established [see Adverse Reactions (6.2)].

Phenylketonuria

Phenylketonuric patients should be informed that the 4-mg and 5-mg chewable tablets contain phenylalanine (a component of aspartame), 0.674 and 0.842 mg per 4-mg and 5-mg chewable tablet, respectively.

Adverse Reactions

Clinical Trials Experience

Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in clinical practice. In the following description of clinical trials experience, adverse reactions are listed regardless of causality assessment.

The most common adverse reactions (incidence ≥5% and greater than placebo; listed in descending order of frequency) in controlled clinical trials were: upper respiratory infection, fever, headache, pharyngitis, cough, abdominal pain, diarrhea, otitis media, influenza, rhinorrhea, sinusitis, otitis.

Adults and Adolescents 15 Years of Age and Older with Asthma

Singulair has been evaluated for safety in approximately 2950 adult and adolescent patients 15 years of age and older in clinical trials. In placebo-controlled clinical trials, the following adverse experiences reported with Singulair occurred in greater than or equal to 1% of patients and at an incidence greater than that in patients treated with placebo:

Table 1: Adverse Experiences Occurring in ≥1% of Patients with an Incidence Greater than that in Patients Treated with Placebo

	Singulair 10 mg/day (%) (n=1955)	Placebo (%) (n=1180)
* Number of patients tested (Singulair and placebo, respectively): ALT and AST, 1935, 1170; pyuria, 1924, 1159.
Body As A Whole     Pain, abdominal     Asthenia/fatigue     Fever     Trauma	2.9 1.8 1.5 1.0	2.5 1.2 0.9 0.8
Digestive System Disorders     Dyspepsia     Pain, dental     Gastroenteritis, infectious	2.1 1.7 1.5	1.1 1.0 0.5
Nervous System/Psychiatric     Headache     Dizziness	18.4 1.9	18.1 1.4
Respiratory System Disorders     Influenza     Cough     Congestion, nasal	4.2 2.7 1.6	3.9 2.4 1.3
Skin/Skin Appendages Disorder     Rash	1.6	1.2
Laboratory Adverse Experiences*     ALT increased     AST increased     Pyuria	2.1 1.6 1.0	2.0 1.2 0.9

The frequency of less common adverse events was comparable between Singulair and placebo.

The safety profile of Singulair, when administered as a single dose for prevention of EIB in adult and adolescent patients 15 years of age and older, was consistent with the safety profile previously described for Singulair.

Cumulatively, 569 patients were treated with Singulair for at least 6 months, 480 for one year, and 49 for two years in clinical trials. With prolonged treatment, the adverse experience profile did not significantly change.

Pediatric Patients 6 to 14 Years of Age with Asthma

Singulair has been evaluated for safety in 476 pediatric patients 6 to 14 years of age. Cumulatively, 289 pediatric patients were treated with Singulair for at least 6 months, and 241 for one year or longer in clinical trials. The safety profile of Singulair in the 8-week, double-blind, pediatric efficacy trial was generally similar to the adult safety profile. In pediatric patients 6 to 14 years of age receiving Singulair, the following events occurred with a frequency ≥2% and more frequently than in pediatric patients who received placebo: pharyngitis, influenza, fever, sinusitis, nausea, diarrhea, dyspepsia, otitis, viral infection, and laryngitis. The frequency of less common adverse events was comparable between Singulair and placebo. With prolonged treatment, the adverse experience profile did not significantly change.

In studies evaluating growth rate, the safety profile in these pediatric patients was consistent with the safety profile previously described for Singulair. In a 56-week, double-blind study evaluating growth rate in pediatric patients 6 to 8 years of age receiving Singulair, the following events not previously observed with the use of Singulair in this age group occurred with a frequency ≥2% and more frequently than in pediatric patients who received placebo: headache, rhinitis (infective), varicella, gastroenteritis, atopic dermatitis, acute bronchitis, tooth infection, skin infection, and myopia.

Pediatric Patients 2 to 5 Years of Age with Asthma

Singulair has been evaluated for safety in 573 pediatric patients 2 to 5 years of age in single- and multiple-dose studies. Cumulatively, 426 pediatric patients 2 to 5 years of age were treated with Singulair for at least 3 months, 230 for 6 months or longer, and 63 patients for one year or longer in clinical trials. In pediatric patients 2 to 5 years of age receiving Singulair, the following events occurred with a frequency ≥2% and more frequently than in pediatric patients who received placebo: fever, cough, abdominal pain, diarrhea, headache, rhinorrhea, sinusitis, otitis, influenza, rash, ear pain, gastroenteritis, eczema, urticaria, varicella, pneumonia, dermatitis, and conjunctivitis.

Pediatric Patients 6 to 23 Months of Age with Asthma

Safety and effectiveness in pediatric patients younger than 12 months of age with asthma have not been established.

Singulair has been evaluated for safety in 175 pediatric patients 6 to 23 months of age. The safety profile of Singulair in a 6-week, double-blind, placebo-controlled clinical study was generally similar to the safety profile in adults and pediatric patients 2 to 14 years of age. In pediatric patients 6 to 23 months of age receiving Singulair, the following events occurred with a frequency ≥2% and more frequently than in pediatric patients who received placebo: upper respiratory infection, wheezing; otitis media; pharyngitis, tonsillitis, cough; and rhinitis. The frequency of less common adverse events was comparable between Singulair and placebo.

Adults and Adolescents 15 Years of Age and Older with Seasonal Allergic Rhinitis

Singulair has been evaluated for safety in 2199 adult and adolescent patients 15 years of age and older in clinical trials. Singulair administered once daily in the morning or in the evening had a safety profile similar to that of placebo. In placebo-controlled clinical trials, the following event was reported with Singulair with a frequency ≥1% and at an incidence greater than placebo: upper respiratory infection, 1.9% of patients receiving Singulair vs. 1.5% of patients receiving placebo. In a 4-week, placebo-controlled clinical study, the safety profile was consistent with that observed in 2-week studies. The incidence of somnolence was similar to that of placebo in all studies.

Pediatric Patients 2 to 14 Years of Age with Seasonal Allergic Rhinitis

Singulair has been evaluated in 280 pediatric patients 2 to 14 years of age in a 2-week, multicenter, double-blind, placebo-controlled, parallel-group safety study. Singulair administered once daily in the evening had a safety profile similar to that of placebo. In this study, the following events occurred with a frequency ≥2% and at an incidence greater than placebo: headache, otitis media, pharyngitis, and upper respiratory infection.

Adults and Adolescents 15 Years of Age and Older with Perennial Allergic Rhinitis

Singulair has been evaluated for safety in 3357 adult and adolescent patients 15 years of age and older with perennial allergic rhinitis of whom 1632 received Singulair in two, 6-week, clinical studies. Singulair administered once daily had a safety profile consistent with that observed in patients with seasonal allergic rhinitis and similar to that of placebo. In these two studies, the following events were reported with Singulair with a frequency ≥1% and at an incidence greater than placebo: sinusitis, upper respiratory infection, sinus headache, cough, epistaxis, and increased ALT. The incidence of somnolence was similar to that of placebo.

Pediatric Patients 6 Months to 14 Years of Age with Perennial Allergic Rhinitis

The safety in patients 2 to 14 years of age with perennial allergic rhinitis is supported by the safety in patients 2 to 14 years of age with seasonal allergic rhinitis. The safety in patients 6 to 23 months of age is supported by data from pharmacokinetic and safety and efficacy studies in asthma in this pediatric population and from adult pharmacokinetic studies.

Post-Marketing Experience

The following adverse reactions have been identified during post-approval use of Singulair. Because these reactions are reported voluntarily from a population of uncertain size, it is not always possible to reliably estimate their frequency or establish a causal relationship to drug exposure.

Blood and lymphatic system disorders: increased bleeding tendency, thrombocytopenia.

Immune system disorders: hypersensitivity reactions including anaphylaxis, hepatic eosinophilic infiltration.

Psychiatric disorders: agitation including aggressive behavior or hostility, anxiousness, depression, disorientation, dream abnormalities, hallucinations, insomnia, irritability, restlessness, somnambulism, suicidal thinking and behavior (including suicide), tremor [see Warnings and Precautions (5.4)].

Nervous system disorders: drowsiness, paraesthesia/hypoesthesia, seizures.

Cardiac disorders: palpitations.

Respiratory, thoracic and mediastinal disorders: epistaxis.

Gastrointestinal disorders: diarrhea, dyspepsia, nausea, pancreatitis, vomiting.

Hepatobiliary disorders: Cases of cholestatic hepatitis, hepatocellular liver-injury, and mixed-pattern liver injury have been reported in patients treated with Singulair. Most of these occurred in combination with other confounding factors, such as use of other medications, or when Singulair was administered to patients who had underlying potential for liver disease such as alcohol use or other forms of hepatitis.

Skin and subcutaneous tissue disorders: angioedema, bruising, erythema multiforme, erythema nodosum, pruritus, urticaria.

Musculoskeletal and connective tissue disorders: arthralgia, myalgia including muscle cramps.

General disorders and administration site conditions: edema.

Patients with asthma on therapy with Singulair may present with systemic eosinophilia, sometimes presenting with clinical features of vasculitis consistent with Churg-Strauss syndrome, a condition which is often treated with systemic corticosteroid therapy. These events usually, but not always, have been associated with the reduction of oral corticosteroid therapy. Physicians should be alert to eosinophilia, vasculitic rash, worsening pulmonary symptoms, cardiac complications, and/or neuropathy presenting in their patients [see Warnings and Precautions (5.5)].

Drug Interactions

No dose adjustment is needed when Singulair is co-administered with theophylline, prednisone, prednisolone, oral contraceptives, terfenadine, digoxin, warfarin, thyroid hormones, sedative hypnotics, non-steroidal anti-inflammatory agents, benzodiazepines, decongestants, and Cytochrome P450 (CYP) enzyme inducers [see Clinical Pharmacology (12.3)].

USE IN SPECIFIC POPULATIONS

Pregnancy

Pregnancy Category B: There are no adequate and well-controlled studies in pregnant women. Because animal reproduction studies are not always predictive of human response, Singulair should be used during pregnancy only if clearly needed.

Teratogenic Effect: No teratogenicity was observed in rats and rabbits at doses approximately 100 and 110 times, respectively, the maximum recommended daily oral dose in adults based on AUCs [see Nonclinical Toxicology (13.2)].

During worldwide marketing experience, congenital limb defects have been rarely reported in the offspring of women being treated with Singulair during pregnancy. Most of these women were also taking other asthma medications during their pregnancy. A causal relationship between these events and Singulair has not been established.

Merck Sharp & Dohme Corp., a subsidiary of Merck & Co., Inc., maintains a registry to monitor the pregnancy outcomes of women exposed to Singulair while pregnant. Patients and healthcare providers are encouraged to report any prenatal exposure to Singulair by calling the Pregnancy Registry at 1-800-986-8999.

Nursing Mothers

Studies in rats have shown that montelukast is excreted in milk. It is not known if montelukast is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when Singulair is given to a nursing mother.

Pediatric Use

Safety and efficacy of Singulair have been established in adequate and well-controlled studies in pediatric patients with asthma 6 to 14 years of age. Safety and efficacy profiles in this age group are similar to those seen in adults [see Adverse Reactions (6.1), Clinical Pharmacology, Special Populations (12.3), and Clinical Studies (14.1)].

The efficacy of Singulair for the treatment of seasonal allergic rhinitis in pediatric patients 2 to 14 years of age and for the treatment of perennial allergic rhinitis in pediatric patients 6 months to 14 years of age is supported by extrapolation from the demonstrated efficacy in patients 15 years of age and older with allergic rhinitis as well as the assumption that the disease course, pathophysiology and the drug’s effect are substantially similar among these populations.

The safety of Singulair 4-mg chewable tablets in pediatric patients 2 to 5 years of age with asthma has been demonstrated by adequate and well-controlled data [see Adverse Reactions (6.1)]. Efficacy of Singulair in this age group is extrapolated from the demonstrated efficacy in patients 6 years of age and older with asthma and is based on similar pharmacokinetic data, as well as the assumption that the disease course, pathophysiology and the drug’s effect are substantially similar among these populations. Efficacy in this age group is supported by exploratory efficacy assessments from a large, well-controlled safety study conducted in patients 2 to 5 years of age.

The safety of Singulair 4-mg oral granules in pediatric patients 12 to 23 months of age with asthma has been demonstrated in an analysis of 172 pediatric patients, 124 of whom were treated with Singulair, in a 6-week, double-blind, placebo-controlled study [see Adverse Reactions (6.1)]. Efficacy of Singulair in this age group is extrapolated from the demonstrated efficacy in patients 6 years of age and older with asthma based on similar mean systemic exposure (AUC), and that the disease course, pathophysiology and the drug’s effect are substantially similar among these populations, supported by efficacy data from a safety trial in which efficacy was an exploratory assessment.

The safety of Singulair 4-mg and 5-mg chewable tablets in pediatric patients aged 2 to 14 years with allergic rhinitis is supported by data from studies conducted in pediatric patients aged 2 to 14 years with asthma. A safety study in pediatric patients 2 to 14 years of age with seasonal allergic rhinitis demonstrated a similar safety profile [see Adverse Reactions (6.1)]. The safety of Singulair 4-mg oral granules in pediatric patients as young as 6 months of age with perennial allergic rhinitis is supported by extrapolation from safety data obtained from studies conducted in pediatric patients 6 months to 23 months of age with asthma and from pharmacokinetic data comparing systemic exposures in patients 6 months to 23 months of age to systemic exposures in adults.

The safety and effectiveness in pediatric patients below the age of 12 months with asthma and 6 months with perennial allergic rhinitis have not been established. The safety and effectiveness in pediatric patients below the age of 15 years with exercise-induced bronchoconstriction have not been established.

Growth Rate in Pediatric Patients

A 56-week, multi-center, double-blind, randomized, active- and placebo-controlled parallel group study was conducted to assess the effect of Singulair on growth rate in 360 patients with mild asthma, aged 6 to 8 years. Treatment groups included Singulair 5 mg once daily, placebo, and beclomethasone dipropionate administered as 168 mcg twice daily with a spacer device. For each subject, a growth rate was defined as the slope of a linear regression line fit to the height measurements over 56 weeks. The primary comparison was the difference in growth rates between Singulair and placebo groups. Growth rates, expressed as least-squares (LS) mean (95% CI) in cm/year, for the Singulair, placebo, and beclomethasone treatment groups were 5.67 (5.46, 5.88), 5.64 (5.42, 5.86), and 4.86 (4.64, 5.08), respectively. The differences in growth rates, expressed as least-squares (LS) mean (95% CI) in cm/year, for Singulair minus placebo, beclomethasone minus placebo, and Singulair minus beclomethasone treatment groups were 0.03 (-0.26, 0.31), -0.78 (-1.06, -0.49); and 0.81 (0.53, 1.09), respectively. Growth rate (expressed as mean change in height over time) for each treatment group is shown in FIGURE 1.

Figure 1: Change in Height (cm) from Randomization Visit by Scheduled Week (Treatment Group Mean ± Standard Error* of the Mean)

Geriatric Use

Of the total number of subjects in clinical studies of montelukast, 3.5% were 65 years of age and over, and 0.4% were 75 years of age and over. No overall differences in safety or effectiveness were observed between these subjects and younger subjects, and other reported clinical experience has not identified differences in responses between the elderly and younger patients, but greater sensitivity of some older individuals cannot be ruled out. The pharmacokinetic profile and the oral bioavailability of a single 10-mg oral dose of montelukast are similar in elderly and younger adults. The plasma half-life of montelukast is slightly longer in the elderly. No dosage adjustment in the elderly is required.

Hepatic Insufficiency

No dosage adjustment is required in patients with mild-to-moderate hepatic insufficiency [see Clinical Pharmacology (12.3)].

Renal Insufficiency

No dosage adjustment is recommended in patients with renal insufficiency [see Clinical Pharmacology (12.3)].

Overdosage

No mortality occurred following single oral doses of montelukast up to 5000 mg/kg in mice (estimated exposure was approximately 335 and 210 times the AUC for adults and children, respectively, at the maximum recommended daily oral dose) and rats (estimated exposure was approximately 230 and 145 times the AUC for adults and children, respectively, at the maximum recommended daily oral dose).

No specific information is available on the treatment of overdosage with Singulair. In chronic asthma studies, montelukast has been administered at doses up to 200 mg/day to adult patients for 22 weeks and, in short-term studies, up to 900 mg/day to patients for approximately a week without clinically important adverse experiences. In the event of overdose, it is reasonable to employ the usual supportive measures; e.g., remove unabsorbed material from the gastrointestinal tract, employ clinical monitoring, and institute supportive therapy, if required.

There have been reports of acute overdosage in post-marketing experience and clinical studies with Singulair. These include reports in adults and children with a dose as high as 1000 mg. The clinical and laboratory findings observed were consistent with the safety profile in adults and pediatric patients. There were no adverse experiences in the majority of overdosage reports. The most frequently occurring adverse experiences were consistent with the safety profile of Singulair and included abdominal pain, somnolence, thirst, headache, vomiting and psychomotor hyperactivity.

It is not known whether montelukast is removed by peritoneal dialysis or hemodialysis.

Singulair Description

Montelukast sodium, the active ingredient in Singulair, is a selective and orally active leukotriene receptor antagonist that inhibits the cysteinyl leukotriene CysLT1 receptor.

Montelukast sodium is described chemically as [R - (E)] - 1 - [[[1 - [3 - [2 - (7 - chloro - 2 - quinolinyl)ethenyl]phenyl] - 3 - [2 - (1 - hydroxy - 1 - methylethyl)phenyl]propyl]thio]methyl]cyclopropaneacetic acid, monosodium salt.

The empirical formula is C35H35ClNNaO3S, and its molecular weight is 608.18. The structural formula is:

Montelukast sodium is a hygroscopic, optically active, white to off-white powder. Montelukast sodium is freely soluble in ethanol, methanol, and water and practically insoluble in acetonitrile.

Each 10-mg film-coated Singulair tablet contains 10.4 mg montelukast sodium, which is equivalent to 10 mg of montelukast, and the following inactive ingredients: microcrystalline cellulose, lactose monohydrate (89.3 mg), croscarmellose sodium, hydroxypropyl cellulose, and magnesium stearate. The film coating consists of: hydroxypropyl methylcellulose, hydroxypropyl cellulose, titanium dioxide, red ferric oxide, yellow ferric oxide, and carnauba wax.

Each 4-mg and 5-mg chewable Singulair tablet contains 4.2 and 5.2 mg montelukast sodium, respectively, which are equivalent to 4 and 5 mg of montelukast, respectively. Both chewable tablets contain the following inactive ingredients: mannitol, microcrystalline cellulose, hydroxypropyl cellulose, red ferric oxide, croscarmellose sodium, cherry flavor, aspartame, and magnesium stearate.

Each packet of Singulair 4-mg oral granules contains 4.2 mg montelukast sodium, which is equivalent to 4 mg of montelukast. The oral granule formulation contains the following inactive ingredients: mannitol, hydroxypropyl cellulose, and magnesium stearate.

Singulair - Clinical Pharmacology

Mechanism of Action

The cysteinyl leukotrienes (LTC4, LTD4, LTE4) are products of arachidonic acid metabolism and are released from various cells, including mast cells and eosinophils. These eicosanoids bind to cysteinyl leukotriene (CysLT) receptors. The CysLT type-1 (CysLT1) receptor is found in the human airway (including airway smooth muscle cells and airway macrophages) and on other pro-inflammatory cells (including eosinophils and certain myeloid stem cells). CysLTs have been correlated with the pathophysiology of asthma and allergic rhinitis. In asthma, leukotriene-mediated effects include airway edema, smooth muscle contraction, and altered cellular activity associated with the inflammatory process. In allergic rhinitis, CysLTs are released from the nasal mucosa after allergen exposure during both early- and late-phase reactions and are associated with symptoms of allergic rhinitis.

Montelukast is an orally active compound that binds with high affinity and selectivity to the CysLT1 receptor (in preference to other pharmacologically important airway receptors, such as the prostanoid, cholinergic, or β-adrenergic receptor). Montelukast inhibits physiologic actions of LTD4 at the CysLT1 receptor without any agonist activity.

Pharmacodynamics

Montelukast causes inhibition of airway cysteinyl leukotriene receptors as demonstrated by the ability to inhibit bronchoconstriction due to inhaled LTD4 in asthmatics. Doses as low as 5 mg cause substantial blockage of LTD4-induced bronchoconstriction. In a placebo-controlled, crossover study (n=12), Singulair inhibited early- and late-phase bronchoconstriction due to antigen challenge by 75% and 57%, respectively.

The effect of Singulair on eosinophils in the peripheral blood was examined in clinical trials. In patients with asthma aged 2 years and older who received Singulair, a decrease in mean peripheral blood eosinophil counts ranging from 9% to 15% was noted, compared with placebo, over the double-blind treatment periods. In patients with seasonal allergic rhinitis aged 15 years and older who received Singulair, a mean increase of 0.2% in peripheral blood eosinophil counts was noted, compared with a mean increase of 12.5% in placebo-treated patients, over the double-blind treatment periods; this reflects a mean difference of 12.3% in favor of Singulair. The relationship between these observations and the clinical benefits of montelukast noted in the clinical trials is not known [see Clinical Studies (14)].

Pharmacokinetics

Absorption

Montelukast is rapidly absorbed following oral administration. After administration of the 10-mg film-coated tablet to fasted adults, the mean peak montelukast plasma concentration (Cmax) is achieved in 3 to 4 hours (Tmax). The mean oral bioavailability is 64%. The oral bioavailability and Cmax are not influenced by a standard meal in the morning.

For the 5-mg chewable tablet, the mean Cmax is achieved in 2 to 2.5 hours after administration to adults in the fasted state. The mean oral bioavailability is 73% in the fasted state versus 63% when administered with a standard meal in the morning.

For the 4-mg chewable tablet, the mean Cmax is achieved 2 hours after administration in pediatric patients 2 to 5 years of age in the fasted state.

The 4-mg oral granule formulation is bioequivalent to the 4-mg chewable tablet when administered to adults in the fasted state. The co-administration of the oral granule formulation with applesauce did not have a clinically significant effect on the pharmacokinetics of montelukast. A high fat meal in the morning did not affect the AUC of montelukast oral granules; however, the meal decreased Cmax by 35% and prolonged Tmax from 2.3 ± 1.0 hours to 6.4 ± 2.9 hours.

The safety and efficacy of Singulair in patients with asthma were demonstrated in clinical trials in which the 10-mg film-coated tablet and 5-mg chewable tablet formulations were administered in the evening without regard to the time of food ingestion. The safety of Singulair in patients with asthma was also demonstrated in clinical trials in which the 4-mg chewable tablet and 4-mg oral granule formulations were administered in the evening without regard to the time of food ingestion. The safety and efficacy of Singulair in patients with seasonal allergic rhinitis were demonstrated in clinical trials in which the 10-mg film-coated tablet was administered in the morning or evening without regard to the time of food ingestion.

The comparative pharmacokinetics of montelukast when administered as two 5-mg chewable tablets versus one 10-mg film-coated tablet have not been evaluated.

Distribution

Montelukast is more than 99% bound to plasma proteins. The steady state volume of distribution of montelukast averages 8 to 11 liters. Studies in rats with radiolabeled montelukast indicate minimal distribution across the blood-brain barrier. In addition, concentrations of radiolabeled material at 24 hours postdose were minimal in all other tissues.

Metabolism

Montelukast is extensively metabolized. In studies with therapeutic doses, plasma concentrations of metabolites of montelukast are undetectable at steady state in adults and pediatric patients.

In vitro studies using human liver microsomes indicate that CYP3A4 and 2C9 are involved in the metabolism of montelukast. Clinical studies investigating the effect of known inhibitors of CYP3A4 (e.g., ketoconazole, erythromycin) or 2C9 (e.g., fluconazole) on montelukast pharmacokinetics have not been conducted. Based on further in vitro results in human liver microsomes, therapeutic plasma concentrations of montelukast do not inhibit CYP3A4, 2C9, 1A2, 2A6, 2C19, or 2D6 [see Drug Interactions (7) and Clinical Pharmacology, Drug-Drug Interactions (12.3)]. In vitro studies have shown that montelukast is a potent inhibitor of CYP2C8; however, data from a clinical drug-drug interaction study involving montelukast and rosiglitazone (a probe substrate representative of drugs primarily metabolized by CYP2C8) demonstrated that montelukast does not inhibit CYP2C8 in vivo, and therefore is not anticipated to alter the metabolism of drugs metabolized by this enzyme [see Drug Interactions (7) and Clinical Pharmacology, Drug-Drug Interactions (12.3)].

Elimination

The plasma clearance of montelukast averages 45 mL/min in healthy adults. Following an oral dose of radiolabeled montelukast, 86% of the radioactivity was recovered in 5-day fecal collections and <0.2% was recovered in urine. Coupled with estimates of montelukast oral bioavailability, this indicates that montelukast and its metabolites are excreted almost exclusively via the bile.

In several studies, the mean plasma half-life of montelukast ranged from 2.7 to 5.5 hours in healthy young adults. The pharmacokinetics of montelukast are nearly linear for oral doses up to 50 mg. During once-daily dosing with 10-mg montelukast, there is little accumulation of the parent drug in plasma (14%).

Special Populations

Hepatic Insufficiency: Patients with mild-to-moderate hepatic insufficiency and clinical evidence of cirrhosis had evidence of decreased metabolism of montelukast resulting in 41% (90% CI=7%, 85%) higher mean montelukast AUC following a single 10-mg dose. The elimination of montelukast was slightly prolonged compared with that in healthy subjects (mean half-life, 7.4 hours). No dosage adjustment is required in patients with mild-to-moderate hepatic insufficiency. The pharmacokinetics of Singulair in patients with more severe hepatic impairment or with hepatitis have not been evaluated.

Renal Insufficiency: Since montelukast and its metabolites are not excreted in the urine, the pharmacokinetics of montelukast were not evaluated in patients with renal insufficiency. No dosage adjustment is recommended in these patients.

Gender: The pharmacokinetics of montelukast are similar in males and females.

Race: Pharmacokinetic differences due to race have not been studied.

Adolescents and Pediatric Patients: Pharmacokinetic studies evaluated the systemic exposure of the 4-mg oral granule formulation in pediatric patients 6 to 23 months of age, the 4-mg chewable tablets in pediatric patients 2 to 5 years of age, the 5-mg chewable tablets in pediatric patients 6 to 14 years of age, and the 10-mg film-coated tablets in young adults and adolescents ≥15 years of age.

The plasma concentration profile of montelukast following administration of the 10-mg film-coated tablet is similar in adolescents ≥15 years of age and young adults. The 10-mg film-coated tablet is recommended for use in patients ≥15 years of age.

The mean systemic exposure of the 4-mg chewable tablet in pediatric patients 2 to 5 years of age and the 5-mg chewable tablets in pediatric patients 6 to 14 years of age is similar to the mean systemic exposure of the 10-mg film-coated tablet in adults. The 5-mg chewable tablet should be used in pediatric patients 6 to 14 years of age and the 4-mg chewable tablet should be used in pediatric patients 2 to 5 years of age.

In children 6 to 11 months of age, the systemic exposure to montelukast and the variability of plasma montelukast concentrations were higher than those observed in adults. Based on population analyses, the mean AUC (4296 ng•hr/mL [range 1200 to 7153]) was 60% higher and the mean Cmax (667 ng/mL [range 201 to 1058]) was 89% higher than those observed in adults (mean AUC 2689 ng•hr/mL [range 1521 to 4595]) and mean Cmax (353 ng/mL [range 180 to 548]). The systemic exposure in children 12 to 23 months of age was less variable, but was still higher than that observed in adults. The mean AUC (3574 ng•hr/mL [range 2229 to 5408]) was 33% higher and the mean Cmax (562 ng/mL [range 296 to 814]) was 60% higher than those observed in adults. Safety and tolerability of montelukast in a single-dose pharmacokinetic study in 26 children 6 to 23 months of age were similar to that of patients two years and above [see Adverse Reactions (6.1)]. The 4-mg oral granule formulation should be used for pediatric patients 12 to 23 months of age for the treatment of asthma, or for pediatric patients 6 to 23 months of age for the treatment of perennial allergic rhinitis. Since the 4-mg oral granule formulation is bioequivalent to the 4-mg chewable tablet, it can also be used as an alternative formulation to the 4-mg chewable tablet in pediatric patients 2 to 5 years of age.

Drug-Drug Interactions

Theophylline, Prednisone, and Prednisolone: Singulair has been administered with other therapies routinely used in the prophylaxis and chronic treatment of asthma with no apparent increase in adverse reactions. In drug-interaction studies, the recommended clinical dose of montelukast did not have clinically important effects on the pharmacokinetics of the following drugs: theophylline, prednisone, and prednisolone.

Montelukast at a dose of 10 mg once daily dosed to pharmacokinetic steady state, did not cause clinically significant changes in the kinetics of a single intravenous dose of theophylline [predominantly a cytochrome P450 (CYP) 1A2 substrate]. Montelukast at doses of ≥100 mg daily dosed to pharmacokinetic steady state, did not cause any clinically significant change in plasma profiles of prednisone or prednisolone following administration of either oral prednisone or intravenous prednisolone.

Oral Contraceptives, Terfenadine, Digoxin, and Warfarin: In drug interaction studies, the recommended clinical dose of montelukast did not have clinically important effects on the pharmacokinetics of the following drugs: oral contraceptives (norethindrone 1 mg/ethinyl estradiol 35 mcg), terfenadine, digoxin, and warfarin. Montelukast at doses of ≥100 mg daily dosed to pharmacokinetic steady state did not significantly alter the plasma concentrations of either component of an oral contraceptive containing norethindrone 1 mg/ethinyl estradiol 35 mcg. Montelukast at a dose of 10 mg once daily dosed to pharmacokinetic steady state did not change the plasma concentration profile of terfenadine (a substrate of CYP3A4) or fexofenadine, the carboxylated metabolite, and did not prolong the QTc interval following co-administration with terfenadine 60 mg twice daily; did not change the pharmacokinetic profile or urinary excretion of immunoreactive digoxin; did not change the pharmacokinetic profile of warfarin (primarily a substrate of CYP2C9, 3A4 and 1A2) or influence the effect of a single 30-mg oral dose of warfarin on prothrombin time or the International Normalized Ratio (INR).

Thyroid Hormones, Sedative Hypnotics, Non-Steroidal Anti-Inflammatory Agents, Benzodiazepines, and Decongestants: Although additional specific interaction studies were not performed, Singulair was used concomitantly with a wide range of commonly prescribed drugs in clinical studies without evidence of clinical adverse interactions. These medications included thyroid hormones, sedative hypnotics, non-steroidal anti-inflammatory agents, benzodiazepines, and decongestants.

Cytochrome P450 (CYP) Enzyme Inducers: Phenobarbital, which induces hepatic metabolism, decreased the area under the plasma concentration curve (AUC) of montelukast approximately 40% following a single 10-mg dose of montelukast. No dosage adjustment for Singulair is recommended. It is reasonable to employ appropriate clinical monitoring when potent CYP enzyme inducers, such as phenobarbital or rifampin,

Zinx

Generic Name: zinc supplement (Oral route, Parenteral route)

Commonly used brand name(s)

In the U.S.

• Galzin


• M2 Zinc 50


• Orazinc 110


• Orazinc 220


• Zinc-220


• Zinc Chelated


• Zn Plus Protein

In Canada

• Prostavan

Available Dosage Forms:

• Tablet


• Capsule


• Tablet, Extended Release

Uses For Zinx

Zinc supplements are used to prevent or treat zinc deficiency.

The body needs zinc for normal growth and health. For patients who are unable to get enough zinc in their regular diet or who have a need for more zinc, zinc supplements may be necessary. They are generally taken by mouth but some patients may have to receive them by injection.

Zinc supplements may be used for other conditions as determined by your health care professional.

Lack of zinc may lead to poor night vision and wound-healing, a decrease in sense of taste and smell, a reduced ability to fight infections, and poor development of reproductive organs.

• Acrodermatitis enteropathica (a lack of absorption of zinc from the intestine)


• Alcoholism


• Burns


• Type 2 diabetes mellitus


• Down's syndrome


• Eating disorders


• Intestine diseases


• Infections (continuing or chronic)


• Kidney disease


• Liver disease


• Pancreas disease


• Sickle cell disease


• Skin disorders


• Stomach removal


• Stress (continuing)


• Thalassemia


• Trauma (prolonged)

In addition, premature infants may need additional zinc.

Increased need for zinc should be determined by your health care professional.

Claims that zinc is effective in preventing vision loss in the elderly have not been proven. Zinc has not been proven effective in the treatment of porphyria.

Injectable zinc is given by or under the supervision of a health care professional. Other forms of zinc are available without a prescription.

Once a medicine or dietary supplement has been approved for marketing for a certain use, experience may show that it is also useful for other medical problems. Although this use is not included in product labeling, zinc supplements are used in certain patients with the following medical condition:

• Wilson's disease (a disease of too much copper in the body)

Importance of Diet

For good health, it is important that you eat a balanced and varied diet. Follow carefully any diet program your health care professional may recommend. For your specific dietary vitamin and/or mineral needs, ask your health care professional for a list of appropriate foods. If you think that you are not getting enough vitamins and/or minerals in your diet, you may choose to take a dietary supplement.

Zinc is found in various foods, including lean red meats, seafood (especially herring and oysters), peas, and beans. Zinc is also found in whole grains; however, large amounts of whole-grains have been found to decrease the amount of zinc that is absorbed. Additional zinc may be added to the diet through treated (galvanized) cookware. Foods stored in uncoated tin cans may cause less zinc to be available for absorption from food.

The daily amount of zinc needed is defined in several different ways.

• For U.S.—


• Recommended Dietary Allowances (RDAs) are the amount of vitamins and minerals needed to provide for adequate nutrition in most healthy persons. RDAs for a given nutrient may vary depending on a person's age, sex, and physical condition (e.g., pregnancy).


• Daily Values (DVs) are used on food and dietary supplement labels to indicate the percent of the recommended daily amount of each nutrient that a serving provides. DV replaces the previous designation of United States Recommended Daily Allowances (USRDAs).

• For Canada—


• Recommended Nutrient Intakes (RNIs) are used to determine the amounts of vitamins, minerals, and protein needed to provide adequate nutrition and lessen the risk of chronic disease.

Normal daily recommended intakes in milligrams (mg) for zinc are generally defined as follows:

Persons	U.S. (mg)	Canada (mg)
Infants and children birth to 3 years of age	5–10	2–4
Children 4 to 6 years of age	10	5
Children 7 to 10 years of age	10	7–9
Adolescent and adult males	15	9–12
Adolescent and adult females	12	9
Pregnant females	15	15
Breast-feeding females	16–19	15

Before Using Zinx

If you are taking a dietary supplement without a prescription, carefully read and follow any precautions on the label. For these supplements, the following should be considered:

Allergies

Tell your doctor if you have ever had any unusual or allergic reaction to medicines in this group or any other medicines. Also tell your health care professional if you have any other types of allergies, such as to foods dyes, preservatives, or animals. For non-prescription products, read the label or package ingredients carefully.

Pediatric

Problems in children have not been reported with intake of normal daily recommended amounts.

Geriatric

Problems in older adults have not been reported with intake of normal daily recommended amounts. There is some evidence that the elderly may be at risk of becoming deficient in zinc due to poor food selection, decreased absorption of zinc by the body, or medicines that decrease absorption of zinc or increase loss of zinc from the body.

Pregnancy

It is especially important that you are receiving enough vitamins and minerals when you become pregnant and that you continue to receive the right amount of vitamins and minerals throughout your pregnancy. The healthy growth and development of the fetus depend on a steady supply of nutrients from the mother. There is evidence that low blood levels of zinc may lead to problems in pregnancy or defects in the baby. However, taking large amounts of a dietary supplement in pregnancy may be harmful to the mother and/or fetus and should be avoided.

Breast Feeding

It is important that you receive the right amounts of vitamins and minerals so that your baby will also get the vitamins and minerals needed to grow properly. However, taking large amounts of a dietary supplement while breast-feeding may be harmful to the mother and/or baby and should be avoided.

Interactions with Medicines

Although certain medicines should not be used together at all, in other cases two different medicines may be used together even if an interaction might occur. In these cases, your doctor may want to change the dose, or other precautions may be necessary. When you are taking any of these dietary supplements, it is especially important that your healthcare professional know if you are taking any of the medicines listed below. The following interactions have been selected on the basis of their potential significance and are not necessarily all-inclusive.

Using dietary supplements in this class with any of the following medicines is usually not recommended, but may be required in some cases. If both medicines are prescribed together, your doctor may change the dose or how often you use one or both of the medicines.

• Amygdalin


• Deferoxamine


• Eltrombopag

Interactions with Food/Tobacco/Alcohol

Certain medicines should not be used at or around the time of eating food or eating certain types of food since interactions may occur. Using alcohol or tobacco with certain medicines may also cause interactions to occur. Discuss with your healthcare professional the use of your medicine with food, alcohol, or tobacco.

Other Medical Problems

The presence of other medical problems may affect the use of dietary supplements in this class. Make sure you tell your doctor if you have any other medical problems, especially:

• Copper deficiency—Zinc supplements may make this condition worse.

Proper Use of zinc supplement

This section provides information on the proper use of a number of products that contain zinc supplement. It may not be specific to Zinx. Please read with care.

Zinc supplements are most effective if they are taken at least 1 hour before or 2 hours after meals. However, if zinc supplements cause stomach upset, they may be taken with a meal. You should tell your health care professional if you are taking your zinc supplement with meals.

Dosing

The dose medicines in this class will be different for different patients. Follow your doctor's orders or the directions on the label. The following information includes only the average doses of these medicines. If your dose is different, do not change it unless your doctor tells you to do so.

The amount of medicine that you take depends on the strength of the medicine. Also, the number of doses you take each day, the time allowed between doses, and the length of time you take the medicine depend on the medical problem for which you are using the medicine.

• For oral dosage forms (capsules, lozenges, tablets, extended-release tablets):
  
  • To prevent deficiency, the amount taken by mouth is based on normal daily recommended intakes (Note that the normal daily recommended intakes are expressed as an actual amount of zinc. The dosage form [e.g., zinc gluconate, zinc sulfate] has a different strength):
    
    • For the U.S
    
    
    • Adult and teenage males—15 milligrams (mg) per day.
    
    
    • Adult and teenage females—12 mg per day.
    
    
    • Pregnant females—15 mg per day.
    
    
    • Breast-feeding females—16 to 19 mg per day.
    
    
    • Children 4 to 10 years of age—10 mg per day.
    
    
    • Children birth to 3 years of age—5 to 10 mg per day.
    
    
    • For Canada
    
    
    • Adult and teenage males—9 to 12 mg per day.
    
    
    • Adult and teenage females—9 mg per day.
    
    
    • Pregnant females—15 mg per day.
    
    
    • Breast-feeding females—15 mg per day.
    
    
    • Children 7 to 10 years of age—7 to 9 mg per day.
    
    
    • Children 4 to 6 years of age—5 mg per day.
    
    
    • Children birth to 3 years of age—2 to 4 mg per day.
    
    
  
  
  • To treat deficiency:
    
    • Adults, teenagers, and children—Treatment dose is determined by prescriber for each individual based on severity of deficiency.
    
    
  
  

Missed Dose

If you miss a dose of this medicine, take it as soon as possible. However, if it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule. Do not double doses.

If you miss taking zinc supplements for one or more days there is no cause for concern, since it takes some time for your body to become seriously low in zinc. However, if your health care professional has recommended that you take zinc, try to remember to take it as directed every day.

Storage

Keep out of the reach of children.

Store the medicine in a closed container at room temperature, away from heat, moisture, and direct light. Keep from freezing.

Do not keep outdated medicine or medicine no longer needed.

Precautions While Using Zinx

When zinc combines with certain foods it may not be absorbed into your body and it will do you no good. If you are taking zinc, the following foods should be avoided or taken 2 hours after you take zinc:

• Bran


• Fiber-containing foods


• Phosphorus-containing foods such as milk or poultry


• Whole-grain breads and cereals

Do not take zinc supplements and copper, iron, or phosphorus supplements at the same time. It is best to space doses of these products 2 hours apart, to get the full benefit from each dietary supplement.

Zinx Side Effects

Along with its needed effects, a dietary supplement may cause some unwanted effects. Although not all of these side effects may occur, if they do occur they may need medical attention.

Check with your doctor as soon as possible if any of the following side effects occur:

Rare - With large doses

• Chills


• continuing ulcers or sores in mouth or throat


• fever


• heartburn


• indigestion


• nausea


• sore throat


• unusual tiredness or weakness

Symptoms of overdose

• Chest pain


• dizziness


• fainting


• shortness of breath


• vomiting


• yellow eyes or skin

Other side effects not listed may also occur in some patients. If you notice any other effects, check with your healthcare professional.

Call your doctor for medical advice about side effects. You may report side effects to the FDA at 1-800-FDA-1088.

The information contained in the Thomson Reuters Micromedex products as delivered by Drugs.com is intended as an educational aid only. It is not intended as medical advice for individual conditions or treatment. It is not a substitute for a medical exam, nor does it replace the need for services provided by medical professionals. Talk to your doctor, nurse or pharmacist before taking any prescription or over the counter drugs (including any herbal medicines or supplements) or following any treatment or regimen. Only your doctor, nurse, or pharmacist can provide you with advice on what is safe and effective for you.

The use of the Thomson Reuters Healthcare products is at your sole risk. These products are provided "AS IS" and "as available" for use, without warranties of any kind, either express or implied. Thomson Reuters Healthcare and Drugs.com make no representation or warranty as to the accuracy, reliability, timeliness, usefulness or completeness of any of the information contained in the products. Additionally, THOMSON REUTERS HEALTHCARE MAKES NO REPRESENTATION OR WARRANTIES AS TO THE OPINIONS OR OTHER SERVICE OR DATA YOU MAY ACCESS, DOWNLOAD OR USE AS A RESULT OF USE OF THE THOMSON REUTERS HEALTHCARE PRODUCTS. ALL IMPLIED WARRANTIES OF MERCHANTABILITY AND FITNESS FOR A PARTICULAR PURPOSE OR USE ARE HEREBY EXCLUDED. Thomson Reuters Healthcare does not assume any responsibility or risk for your use of the Thomson Reuters Healthcare products.

Acetic Acid Solution

Pronunciation: a-SEE-tik
Generic Name: Acetic Acid
Brand Name: Generic only. No brands available.

Acetic Acid Solution is used for:

Preventing bladder infections from indwelling urinary catheters.

Acetic Acid Solution is an antibacterial solution. It works by lowering the pH in the bladder, which prevents certain bacteria from growing.

Do NOT use Acetic Acid Solution if:

• you are allergic to any ingredient in Acetic Acid Solution

Contact your doctor or health care provider right away if any of these apply to you.

Before using Acetic Acid Solution:

Some medical conditions may interact with Acetic Acid Solution. Tell your doctor or pharmacist if you have any medical conditions, especially if any of the following apply to you:

• if you are pregnant, planning to become pregnant, or are breast-feeding


• if you are taking any prescription or nonprescription medicine, herbal preparation, or dietary supplement


• if you have allergies to medicines, foods, or other substances


• if you have severe heart, lung, or kidney disease


• if you have lesions in the bladder

Some MEDICINES MAY INTERACT with Acetic Acid Solution. Because little, if any, of Acetic Acid Solution is absorbed into the blood, the risk of it interacting with another medicine is low.

This may not be a complete list of all interactions that may occur. Ask your health care provider if Acetic Acid Solution may interact with other medicines that you take. Check with your health care provider before you start, stop, or change the dose of any medicine.

How to use Acetic Acid Solution:

Use Acetic Acid Solution as directed by your doctor. Check the label on the medicine for exact dosing instructions.

• Acetic Acid Solution is usually administered at your doctor's office, hospital, or clinic. If you are using Acetic Acid Solution at home, carefully follow the procedures taught to you by your health care provider.


• If Acetic Acid Solution contains particles or is discolored, or if the vial is cracked or damaged in any way, do not use it.


• After opening, use Acetic Acid Solution promptly to prevent contamination. Do not save open containers of Acetic Acid Solution for later use.


• If you miss a dose of Acetic Acid Solution, contact your doctor right away.

Ask your health care provider any questions you may have about how to use Acetic Acid Solution.

Important safety information:

• Never inject Acetic Acid Solution into a vein.


• Acetic Acid Solution may be harmful if swallowed. If you or someone you know may have taken Acetic Acid Solution by mouth, contact your local poison control center or emergency room immediately.


• Before you have any medical or dental treatments, emergency care, or surgery, tell the doctor or dentist that you are using Acetic Acid Solution.


• PREGNANCY and BREAST-FEEDING: If you plan on becoming pregnant, discuss with your doctor the benefits and risks of using Acetic Acid Solution during pregnancy. It is unknown if Acetic Acid Solution is excreted in breast milk. If you are or will be breast-feeding while you are using Acetic Acid Solution, check with your doctor or pharmacist to discuss the risks to your baby.

Possible side effects of Acetic Acid Solution:

All medicines may cause side effects, but many people have no, or minor, side effects. Check with your doctor if any of these most COMMON side effects persist or become bothersome:

No common side effects.

Seek medical attention right away if any of these SEVERE side effects occur:

Severe allergic reactions (rash; hives; difficulty breathing; tightness in the chest; swelling of the mouth, face, lips, or tongue); blood in the urine; diarrhea; groin or bladder pain; headache; nausea; seizures; tremors; vomiting.

This is not a complete list of all side effects that may occur. If you have questions about side effects, contact your health care provider. Call your doctor for medical advice about side effects. To report side effects to the appropriate agency, please read the Guide to Reporting Problems to FDA.

If OVERDOSE is suspected:

Contact 1-800-222-1222 (the American Association of Poison Control Centers), your local poison control center, or emergency room immediately.

Proper storage of Acetic Acid Solution:

Store Acetic Acid Solution at room temperature at 77 degrees F (25 degrees C). Store away from heat, moisture, and light. Do not store in the bathroom. Keep Acetic Acid Solution out of the reach of children and pets.

General information:

• If you have any questions about Acetic Acid Solution, please talk with your doctor, pharmacist, or other health care provider.


• Acetic Acid Solution is to be used only by the patient for whom it is prescribed. Do not share it with other people.


• If your symptoms do not improve or if they become worse, check with your doctor.


• Check with your pharmacist about how to dispose of unused medicine.

This information is summary only. It does not contain all information about Acetic Acid Solution. If you have questions about the medicine you are taking or would like more information, check with your doctor, pharmacist, or other health care provider.

Issue Date: February 1, 2012

Database Edition 12.1.1.002

Copyright © 2012 Wolters Kluwer Health, Inc.

More Acetic Acid resources

• Acetic Acid Support Group
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Stanback Analgesic

Generic Name: aspirin (oral) (AS pir in)

Brand Names: Arthritis Pain, Aspergum Cherry, Aspergum Orginal, Aspir 81, Aspir-Low, Aspirin Lite Coat, Aspirin Litecoat, Aspirin Low Dose, Aspirin Low Strength, Bayer Aspirin, Bayer Aspirin Regimen, Bayer Aspirin Sugar Free, Bayer Aspirin with Calcium, Bayer Childrens Aspirin, Bayer Low Strength, Bayer Plus, Buffered Aspirin, Bufferin, Bufferin Arthritis Strength, Bufferin Extra Strength, Easprin, Ecotrin, Ecotrin Adult Low Strength, Ecotrin Maximum Strength, Fasprin, Genacote, Halfprin, Litecoat Aspirin, Norwich Aspirin, St. Joseph Aspirin, St. Joseph Aspirin Adult Chewable, St. Joseph Aspirin Adult EC, Stanback Analgesic, Tri-Buffered Aspirin, YSP Aspirin, Zorprin

What is aspirin?

Aspirin is in a group of drugs called salicylates (sa-LIS-il-ates). It works by reducing substances in the body that cause pain, fever, and inflammation.

Aspirin is used to treat mild to moderate pain, and also to reduce fever or inflammation. Aspirin is sometimes used to treat or prevent heart attacks, strokes, and chest pain (angina). Aspirin should be used for cardiovascular conditions only under the supervision of a doctor.

Aspirin may also be used for other purposes not listed in this medication guide.

What is the most important information I should know about aspirin?

There are many brands and forms of aspirin available and not all brands are listed on this leaflet.

Aspirin should not be given to a child or teenager who has a fever, especially if the child also has flu symptoms or chicken pox. Aspirin can cause a serious and sometimes fatal condition called Reye's syndrome in children.

Stop using this medication and call your doctor at once if you have any symptoms of bleeding in your stomach or intestines. Symptoms include black, bloody, or tarry stools, and coughing up blood or vomit that looks like coffee grounds.

Avoid drinking alcohol while you are taking aspirin. Alcohol may increase your risk of stomach bleeding.

Aspirin is sometimes used to treat or prevent heart attacks, strokes, and chest pain (angina). Aspirin should be used for cardiovascular conditions only under the supervision of a doctor.

What should I discuss with my healthcare provider before taking aspirin?

Aspirin should not be given to a child or teenager who has a fever, especially if the child also has flu symptoms or chicken pox. Aspirin can cause a serious and sometimes fatal condition called Reye's syndrome in children. Do not use this medication if you are allergic to aspirin, or if you have:

• 
  

  a recent history of stomach or intestinal bleeding;

  
  


• 
  

  a bleeding disorder such as hemophilia; or

  
  


• 
  

  an allergy to an NSAID (non-steroidal anti-inflammatory drug) such as Advil, Motrin, Aleve, Orudis, Indocin, Lodine, Voltaren, Toradol, Mobic, Relafen, Feldene, and others.

  
  

If you have any of these other conditions, you may need a dose adjustment or special tests to safely take aspirin:

• 
  

  asthma or seasonal allergies;

  
  


• 
  

  stomach ulcers;

  
  


• liver disease;


• kidney disease;


• 
  

  a bleeding or blood clotting disorder;

  
  


• 
  

  heart disease, high blood pressure, or congestive heart failure;

  
  


• 
  

  gout; or

  
  


• 
  

  nasal polyps.

  
  

If you are taking aspirin to prevent heart attack or stroke, avoid also taking ibuprofen (Advil, Motrin). Ibuprofen may make aspirin less effective in protecting your heart and blood vessels. If you must use both medications, take the ibuprofen at least 8 hours before or 30 minutes after you take the aspirin (non-enteric coated form). This medication may be harmful to an unborn baby's heart, and may also reduce birth weight or have other dangerous effects. Tell your doctor if you are pregnant or plan to become pregnant while you are taking aspirin. Aspirin can pass into breast milk and may harm a nursing baby. Do not use this medication without telling your doctor if you are breast-feeding a baby.

How should I take aspirin?

Use this medication exactly as directed on the label, or as it has been prescribed by your doctor. Do not use the medication in larger or smaller amounts, or use it for longer than recommended.

Take this medication with a full glass of water. Taking aspirin with food or milk can lessen stomach upset. Enteric-coated aspirin is specially formulated to be gentle on your stomach, but you may take it with food or milk if desired. Do not crush, chew, break, or open an enteric-coated or extended-release pill. Swallow the pill whole. The enteric-coated pill has a special coating to protect your stomach. Breaking the pill could damage this coating. The extended-release tablet is specially made to release medicine slowly in the body. Breaking this pill would cause too much of the drug to be released at one time.

The chewable tablet form of aspirin must be chewed before swallowing.

Keep the orally disintegrating tablet in its package until you are ready to take the medicine. Open the package and peel the back cover from the tablet. Using dry hands, place the tablet into your mouth. It will begin to dissolve right away, without water. Do not swallow the tablet whole. Allow it to dissolve in your mouth without chewing.

If you need to have any type of surgery, tell the surgeon ahead of time that you are taking aspirin. You may need to stop using the medicine for a short time.

Do not take this medication if you smell a strong vinegar odor in the aspirin bottle. The medicine may no longer be effective. Store aspirin at room temperature away from moisture and heat.

What happens if I miss a dose?

Since aspirin is often used as needed, you may not be on a dosing schedule. If you are using the medication regularly, take the missed dose as soon as you remember. If it is almost time for the next dose, skip the missed dose and wait until your next regularly scheduled dose. Do not use extra medicine to make up the missed dose.

What happens if I overdose?

Seek emergency medical attention if you think you have used too much of this medicine.

Overdose symptoms may include ringing in your ears, headache, nausea, vomiting, dizziness, confusion, hallucinations, rapid breathing, fever, seizure (convulsions), or coma.

What should I avoid while taking aspirin?

Do not use any other over-the-counter medication without first asking your doctor or pharmacist. Aspirin is contained in many medicines available over the counter. If you take certain products together you may accidentally take too much aspirin. Read the label of any other medicine you are using to see if it contains aspirin.

Avoid taking an NSAID (non-steroidal anti-inflammatory drug) while you are taking aspirin. NSAIDs include ibuprofen (Motrin, Advil), diclofenac (Voltaren), diflunisal (Dolobid), etodolac (Lodine), flurbiprofen (Ansaid), indomethacin (Indocin), ketoprofen (Orudis), ketorolac (Toradol), mefenamic acid (Ponstel), meloxicam (Mobic), nabumetone (Relafen), naproxen (Aleve, Naprosyn), piroxicam (Feldene), and others.

Avoid drinking alcohol while you are taking aspirin. Alcohol may increase your risk of stomach bleeding. Avoid taking ibuprofen (Advil, Motrin) if you are taking aspirin to prevent stroke or heart attack. Ibuprofen can make aspirin less effective in protecting your heart and blood vessels. If you must use both medications, take the ibuprofen at least 8 hours before or 30 minutes after you take the aspirin (non-enteric coated form).

Aspirin side effects

Get emergency medical help if you have any of these signs of an allergic reaction: hives; difficulty breathing; swelling of your face, lips, tongue, or throat. Stop using this medication and call your doctor at once if you have any of these serious side effects:

• 
  

  black, bloody, or tarry stools;

  
  


• 
  

  coughing up blood or vomit that looks like coffee grounds;

  
  


• 
  

  severe nausea, vomiting, or stomach pain;

  
  


• 
  

  fever lasting longer than 3 days;

  
  


• 
  

  swelling, or pain lasting longer than 10 days; or

  
  


• 
  

  hearing problems, ringing in your ears.

  
  

Less serious side effects may include:

• 
  

  upset stomach, heartburn;

  
  


• 
  

  drowsiness; or

  
  


• 
  

  headache.

  
  

This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

What other drugs will affect aspirin?

Tell your doctor if you are taking an antidepressant such as citalopram (Celexa), duloxetine (Cymbalta), escitalopram (Lexapro), fluoxetine (Prozac, Sarafem, Symbyax), fluvoxamine (Luvox), paroxetine (Paxil), sertraline (Zoloft), or venlafaxine (Effexor). Taking any of these drugs with aspirin may cause you to bruise or bleed easily.

Before taking aspirin, tell your doctor if you are using any of the following drugs:

• 
  

  a blood thinner such as warfarin (Coumadin); or

  
  


• 
  

  another salicylate such as choline salicylate and/or magnesium salicylate (Magan, Doan's, Bayer Select Backache Pain Formula, Mobidin, Arthropan, Trilisate, Tricosal), or salsalate (Disalcid).

  
  

This list is not complete and there may be other drugs that can interact with aspirin. Tell your doctor about all the prescription and over-the-counter medications you use. This includes vitamins, minerals, herbal products, and drugs prescribed by other doctors. Do not start using a new medication without telling your doctor.

More Stanback Analgesic resources

• Stanback Analgesic Side Effects (in more detail)
• Stanback Analgesic Use in Pregnancy & Breastfeeding
• Stanback Analgesic Drug Interactions
• Stanback Analgesic Support Group
• 0 Reviews for Stanback Analgesic - Add your own review/rating

• Aspirin Monograph (AHFS DI)


• Aspirin Prescribing Information (FDA)


• Aspirin MedFacts Consumer Leaflet (Wolters Kluwer)


• Bayer Low Strength Delayed-Release Tablets MedFacts Consumer Leaflet (Wolters Kluwer)


• Ecotrin Advanced Consumer (Micromedex) - Includes Dosage Information


• ZORprin Controlled-Release Tablets MedFacts Consumer Leaflet (Wolters Kluwer)

Compare Stanback Analgesic with other medications

• Angina
• Angina Pectoris Prophylaxis
• Ankylosing Spondylitis
• Antiphospholipid Syndrome
• Aseptic Necrosis
• Back Pain
• Fever
• Heart Attack
• Ischemic Stroke
• Ischemic Stroke, Prophylaxis
• Juvenile Rheumatoid Arthritis
• Kawasaki Disease
• Myocardial Infarction, Prophylaxis
• Niacin Flush
• Osteoarthritis
• Pain
• Prevention of Thromboembolism in Atrial Fibrillation
• Prosthetic Heart Valves
• Prosthetic Heart Valves, Mechanical Valves
• Revascularization Procedures, Prophylaxis
• Rheumatic Fever
• Rheumatoid Arthritis
• Sciatica
• Systemic Lupus Erythematosus
• Thromboembolic Stroke Prophylaxis
• Transient Ischemic Attack

Where can I get more information?

• Your pharmacist can provide more information about aspirin.

See also: Stanback Analgesic side effects (in more detail)

Carnitor

Generic Name: levocarnitine (Oral route, Intravenous route)

lee-voe-KAR-ni-teen

Commonly used brand name(s)

In the U.S.

• Carnitine


• Carnitor

Available Dosage Forms:

• Capsule


• Tablet


• Solution


• Wafer


• Powder

Therapeutic Class: Amino Acid Supplement

Uses For Carnitor

Levocarnitine is used to prevent and treat a lack of carnitine. It is used to prevent and treat this condition in patients with kidney disease on dialysis. It is given to people whose body cannot properly use carnitine from their diet. Lack of carnitine can lead to liver, heart, and muscle problems. Your doctor may treat lack of carnitine by prescribing levocarnitine for you.

Carnitine comes in two forms. Levocarnitine (L-carnitine) should not be confused with the D,L-carnitine form (labeled as “vitamin B T”'). Only the L-form of carnitine is used by the body to treat serious carnitine deficiency. The D,L-form does not help the body use fat and can actually interfere with and cause a lack of levocarnitine.

Certain levocarnitine products have been specifically approved by the U.S. Food and Drug Administration for medical use and are available only with your doctor's prescription.

Once a medicine has been approved for marketing for a certain use, experience may show that it is also useful for other medical problems. Although this use is not included in product labeling, levocarnitine is used in certain patients with the following medical condition:

• Carnitine deficiency that results from treatment with valproic acid

Before Using Carnitor

In deciding to use a medicine, the risks of taking the medicine must be weighed against the good it will do. This is a decision you and your doctor will make. For this medicine, the following should be considered:

Allergies

Tell your doctor if you have ever had any unusual or allergic reaction to this medicine or any other medicines. Also tell your health care professional if you have any other types of allergies, such as to foods, dyes, preservatives, or animals. For non-prescription products, read the label or package ingredients carefully.

Pediatric

Although there is no specific information comparing use of levocarnitine in children with use in other age groups, this dietary supplement is not expected to cause different side effects or problems in children than it does in adults.

Geriatric

There is no specific information comparing use of levocarnitine in the elderly with use in other age groups; however, this medicine is not expected to cause different side effects or problems in older people than it does in younger adults.

Pregnancy

	Pregnancy Category	Explanation
All Trimesters	B	Animal studies have revealed no evidence of harm to the fetus, however, there are no adequate studies in pregnant women OR animal studies have shown an adverse effect, but adequate studies in pregnant women have failed to demonstrate a risk to the fetus.

Breast Feeding

There are no adequate studies in women for determining infant risk when using this medication during breastfeeding. Weigh the potential benefits against the potential risks before taking this medication while breastfeeding.

Interactions with Medicines

Although certain medicines should not be used together at all, in other cases two different medicines may be used together even if an interaction might occur. In these cases, your doctor may want to change the dose, or other precautions may be necessary. When you are taking this medicine, it is especially important that your healthcare professional know if you are taking any of the medicines listed below. The following interactions have been selected on the basis of their potential significance and are not necessarily all-inclusive.

Using this medicine with any of the following medicines is usually not recommended, but may be required in some cases. If both medicines are prescribed together, your doctor may change the dose or how often you use one or both of the medicines.

• Acenocoumarol

Interactions with Food/Tobacco/Alcohol

Certain medicines should not be used at or around the time of eating food or eating certain types of food since interactions may occur. Using alcohol or tobacco with certain medicines may also cause interactions to occur. Discuss with your healthcare professional the use of your medicine with food, alcohol, or tobacco.

Other Medical Problems

The presence of other medical problems may affect the use of this medicine. Make sure you tell your doctor if you have any other medical problems, especially:

• Seizures—occur more often and are more severe in patients with a history of seizure activity


• Severe renal dysfunction—administration of high doses of oral levocarnitine for long periods of time may build up in the body of patients with severe kidney disease

Proper Use of levocarnitine

This section provides information on the proper use of a number of products that contain levocarnitine. It may not be specific to Carnitor. Please read with care.

Take levocarnitine with or just after meals. Also, if you are taking it in liquid form, drink it slowly. It will be less likely to upset your stomach if you take it this way. The liquid form may be taken alone or dissolved in drink or other liquid food.

This medicine is also less likely to cause unwanted effects when there is a constant amount in the blood. If you are taking more than one dose a day, take the doses at evenly spaced times throughout the day. Doses should be spaced at least 3 to 4 hours apart. If you need help in planning the best times to take your medicine, check with your health care professional.

Dosing

The dose of this medicine will be different for different patients. Follow your doctor's orders or the directions on the label. The following information includes only the average doses of this medicine. If your dose is different, do not change it unless your doctor tells you to do so.

The amount of medicine that you take depends on the strength of the medicine. Also, the number of doses you take each day, the time allowed between doses, and the length of time you take the medicine depend on the medical problem for which you are using the medicine.

Do NOT change brands or dosage forms of levocarnitine without first checking with your doctor. Different products may not work in the same way. If you refill your medicine and it looks different, check with your pharmacist.

• For oral dosage form (solution):
  
  • To prevent or treat carnitine deficiency:
    
    • Adults and teenagers—At first, 1 gram taken once a day with food. Your doctor may change the dose if needed.
    
    
    • Children—The dose is based on body weight and must be determined by your doctor. The usual dose at first is 50 mg per kg (22.7 mg per pound) of body weight a day, divided into smaller amounts with meals. Your doctor may change the dose if needed.
    
    
  
  


• For oral dosage form (tablets):
  
  • To prevent or treat carnitine deficiency:
    
    • Adults and teenagers—990 milligrams taken two or three times a day with meals.
    
    
    • Children—The dose is based on body weight and must be determined by your doctor. The usual dose at first is 50 mg per kg (22.7 mg per pound) of body weight a day, divided into smaller amounts with meals. Your doctor may change the dose if needed.
    
    
  
  


• For injection dosage form:
  
  • To treat carnitine deficiency:
    
    • Adults and children—The dose is based on body weight and must be determined by your doctor. The usual dose is 50 mg per kg (22.7 mg per pound) of body weight a day injected into a vein. Your doctor may change the dose if needed.
    
    
  
  
  • To prevent and treat carnitine deficiency in kidney disease patients on hemodialysis:
    
    • Adults and children—10 to 20 mg per kg of body weight a day, after dialysis. The dose may be reduced based on laboratory test results, after 3 to 4 weeks of therapy.
    
    
  
  

Missed Dose

If you miss a dose of this medicine, take it as soon as possible. However, if it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule. Do not double doses.

Taking doses too close together may increase stomach upset.

Storage

Store the medicine in a closed container at room temperature, away from heat, moisture, and direct light. Keep from freezing.

Keep out of the reach of children.

Do not keep outdated medicine or medicine no longer needed.

Precautions While Using Carnitor

Do not change brands or dosage forms of levocarnitine without first checking with your doctor. Different products may not work in the same way. If you refill your medicine and it looks different, check with your pharmacist.

Carnitor Side Effects

Along with its needed effects, a medicine may cause some unwanted effects. Although not all of these side effects may occur, if they do occur they may need medical attention.

Check with your doctor as soon as possible if any of the following side effects occur:

More common

• High blood pressure

Less common

• Fast heartbeat


• fever

Rare

• Seizures

Some side effects may occur that usually do not need medical attention. These side effects may go away during treatment as your body adjusts to the medicine. Also, your health care professional may be able to tell you about ways to prevent or reduce some of these side effects. Check with your health care professional if any of the following side effects continue or are bothersome or if you have any questions about them:

More common

• Abdominal or stomach cramps


• diarrhea


• headache


• nausea or vomiting

Less common

• Abdominal discomfort


• body odor


• depression


• dizziness


• impaired vision


• loss of appetite or weight


• swelling in hands, lower legs, and feet


• tingling sensation


• weakness

Other side effects not listed may also occur in some patients. If you notice any other effects, check with your healthcare professional.

Call your doctor for medical advice about side effects. You may report side effects to the FDA at 1-800-FDA-1088.

See also: Carnitor side effects (in more detail)

The information contained in the Thomson Reuters Micromedex products as delivered by Drugs.com is intended as an educational aid only. It is not intended as medical advice for individual conditions or treatment. It is not a substitute for a medical exam, nor does it replace the need for services provided by medical professionals. Talk to your doctor, nurse or pharmacist before taking any prescription or over the counter drugs (including any herbal medicines or supplements) or following any treatment or regimen. Only your doctor, nurse, or pharmacist can provide you with advice on what is safe and effective for you.

The use of the Thomson Reuters Healthcare products is at your sole risk. These products are provided "AS IS" and "as available" for use, without warranties of any kind, either express or implied. Thomson Reuters Healthcare and Drugs.com make no representation or warranty as to the accuracy, reliability, timeliness, usefulness or completeness of any of the information contained in the products. Additionally, THOMSON REUTERS HEALTHCARE MAKES NO REPRESENTATION OR WARRANTIES AS TO THE OPINIONS OR OTHER SERVICE OR DATA YOU MAY ACCESS, DOWNLOAD OR USE AS A RESULT OF USE OF THE THOMSON REUTERS HEALTHCARE PRODUCTS. ALL IMPLIED WARRANTIES OF MERCHANTABILITY AND FITNESS FOR A PARTICULAR PURPOSE OR USE ARE HEREBY EXCLUDED. Thomson Reuters Healthcare does not assume any responsibility or risk for your use of the Thomson Reuters Healthcare products.

More Carnitor resources

• Carnitor Side Effects (in more detail)
• Carnitor Use in Pregnancy & Breastfeeding
• Carnitor Support Group
• 0 Reviews for Carnitor - Add your own review/rating

• Carnitor Monograph (AHFS DI)


• Carnitor MedFacts Consumer Leaflet (Wolters Kluwer)

Compare Carnitor with other medications

• Carnitine Deficiency
• Peripheral Neuropathy

Solganal

Generic Name: gold compound (Oral route, Parenteral route)

Commonly used brand name(s)

In the U.S.

• Ridaura

Available Dosage Forms:

• Capsule

Uses For Solganal

The gold compounds are used in the treatment of rheumatoid arthritis. They may also be used for other conditions as determined by your doctor.

In addition to the helpful effects of this medicine in treating your medical problem, it has side effects that can be very serious. Before you take this medicine, you should discuss with your doctor the good that this medicine will do as well as the risks of using it.

Auranofin is available only with your doctor's prescription. The other gold compounds are given by your health care professional.

Schering-Plough discontinued aurothioglucose in May 2002.

Before Using Solganal

Allergies

Tell your doctor if you have ever had any unusual or allergic reaction to medicines in this group or any other medicines. Also tell your health care professional if you have any other types of allergies, such as to foods dyes, preservatives, or animals. For non-prescription products, read the label or package ingredients carefully.

Pediatric

Auranofin has been tested only in adult patients and there is no specific information about its use in children. However, gold sodium thiomalate have been tested in children and have not been shown to cause different side effects or problems than they do in adults.

Geriatric

These medicines have been tested and have not been shown to cause different side effects or problems in older people than they do in younger adults.

Pregnancy

Studies on birth defects with gold compounds have not been done in humans. However, studies in animals have shown that gold compounds may cause birth defects.

Breast Feeding

Gold sodium thiomalate pass into the breast milk and may cause unwanted effects in nursing babies. It is not known whether auranofin passes into the breast milk.

Interactions with Medicines

Although certain medicines should not be used together at all, in other cases two different medicines may be used together even if an interaction might occur. In these cases, your doctor may want to change the dose, or other precautions may be necessary. When you are taking any of these medicines, it is especially important that your healthcare professional know if you are taking any of the medicines listed below. The following interactions have been selected on the basis of their potential significance and are not necessarily all-inclusive.

Using medicines in this class with any of the following medicines is not recommended. Your doctor may decide not to treat you with a medication in this class or change some of the other medicines you take.

• Artemether


• Chloroquine


• Halofantrine


• Hydroxychloroquine


• Mefloquine


• Penicillamine


• Primaquine


• Proguanil


• Pyrimethamine


• Quinacrine


• Quinidine


• Quinine

Using medicines in this class with any of the following medicines is usually not recommended, but may be required in some cases. If both medicines are prescribed together, your doctor may change the dose or how often you use one or both of the medicines.

• Penicillamine

Interactions with Food/Tobacco/Alcohol

Certain medicines should not be used at or around the time of eating food or eating certain types of food since interactions may occur. Using alcohol or tobacco with certain medicines may also cause interactions to occur. Discuss with your healthcare professional the use of your medicine with food, alcohol, or tobacco.

Other Medical Problems

The presence of other medical problems may affect the use of medicines in this class. Make sure you tell your doctor if you have any other medical problems, especially:

• Blood or blood vessel disease or


• Colitis or


• Kidney disease (or history of) or


• Lupus erythematosus or


• Sjögren's syndrome or


• Skin disease—The chance of unwanted effects may be increased.

Proper Use of gold compound

This section provides information on the proper use of a number of products that contain gold compound. It may not be specific to Solganal. Please read with care.

In order for this medicine to work, it must be taken regularly as ordered by your doctor. Continue receiving the injections or taking auranofin even if you think the medicine is not working. You may not notice the effects of this medicine until after three to six months of regular use.

For patients taking auranofin:

• Do not take more of this medicine than ordered by your doctor. Taking too much auranofin may increase the chance of serious unwanted effects.

If you have any questions about this, check with your doctor.

Dosing

The dose medicines in this class will be different for different patients. Follow your doctor's orders or the directions on the label. The following information includes only the average doses of these medicines. If your dose is different, do not change it unless your doctor tells you to do so.

The amount of medicine that you take depends on the strength of the medicine. Also, the number of doses you take each day, the time allowed between doses, and the length of time you take the medicine depend on the medical problem for which you are using the medicine.

• For auranofin


• For oral dosage form (capsules):
  
  • For arthritis:
    
    • Adults—6 milligrams (mg) once a day or 3 mg twice a day. After six months, your doctor may increase the dose to 3 mg three times a day.
    
    
    • Children—Dose must be determined by your doctor.
    
    
  
  


• For injection dosage form:
  
  • For arthritis:
    
    • Adults and teenagers—10 milligrams (mg) for the first dose, then 25 mg once a week for the next two weeks, then 25 or 50 mg once a week. The medicine is injected into a muscle. After several months, the injections may be given less often (25 or 50 mg every two weeks for a while, then every three or four weeks).
    
    
    • Children 6 to 12 years of age—2.5 mg for the first dose, then 6.25 mg once a week for the next two weeks, then 12.5 mg once a week. The medicine is injected into a muscle. After several months, the injections may be given less often (6.25 or 12.5 mg every three or four weeks).
    
    
    • Children younger than 6 years of age—Dose must be determined by your doctor.
    
    
  
  

• For gold sodium thiomalate


• For injection dosage form:
  
  • For arthritis:
    
    • Adults and teenagers—10 milligrams (mg) for the first dose, then 25 mg a week later, then 25 or 50 mg once a week. The medicine is injected into a muscle. After several months, the injections may be given less often (25 or 50 mg every two weeks for a while, then every three or four weeks).
    
    
    • Children—10 mg for the first dose, then 1 mg per kilogram (about 0.45 mg per pound) of body weight, but not more than a total of 50 mg, once a week. The medicine is injected into a muscle. After several months, the same dose may be given less often (every two weeks for a while, then every three or four weeks).
    
    
  
  

Missed Dose

Call your doctor or pharmacist for instructions.

For patients taking auranofin: If you miss a dose of this medicine, and your dosing schedule is—

• One dose a day—Take the missed dose as soon as possible. However, if you do not remember until the next day, skip the missed dose and go back to your regular dosing schedule. Do not double doses.


• More than one dose a day—Take the missed dose as soon as possible. However, if it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule. Do not double doses.

Storage

Keep out of the reach of children.

Store the medicine in a closed container at room temperature, away from heat, moisture, and direct light. Keep from freezing.

Do not keep outdated medicine or medicine no longer needed.

Precautions While Using Solganal

Gold compounds may cause some people to become more sensitive to sunlight than they are normally. These people may break out in a rash after being in the sun, or a skin rash that is already present may become worse. To protect yourself, it is best to:

• Stay out of direct sunlight, especially between the hours of 10:00 a.m. and 3:00 p.m., if possible.


• Wear protective clothing.


• Ask your doctor if you may apply a sun block product. Products that have a skin protection factor (SPF) of at least 15 work best, but some patients may require a product with a higher SPF number, especially if they have a fair complexion.


• Do not use a sunlamp or tanning bed or booth.

If you have a severe reaction from the sun, check with your doctor.

For patients taking auranofin:

• Your doctor should check your progress at regular visits. Blood and urine tests may be needed to make certain that this medicine is not causing unwanted effects.

For patients receiving gold injections:

• Immediately following an injection of this medicine, side effects such as dizziness, feeling faint, flushing or redness of the face, nausea or vomiting, increased sweating, or unusual weakness may occur. These will usually go away after you lie down for a few minutes. If any of these effects continue or become worse, or if you notice any other effects within 10 minutes or so after receiving an injection, tell your health care professional right away.


• Joint pain may occur for 1 or 2 days after you receive an injection of this medicine. This effect usually disappears after the first few injections. However, if this continues or is bothersome, check with your doctor.

Solganal Side Effects

Gold compounds have been shown to cause tumors and cancer of the kidney when given to animals in large amounts for a long time. However, these effects have not been reported in humans receiving gold compounds for arthritis. If you have any questions about this, check with your doctor.

Along with its needed effects, a medicine may cause some unwanted effects. Although not all of these side effects may occur, if they do occur they may need medical attention.

Check with your doctor as soon as possible if any of the following side effects occur:

More common

• Irritation or soreness of tongue—less common with auranofin


• metallic taste—less common with auranofin


• redness, soreness, swelling, or bleeding of gums—rare with auranofin


• skin rash or itching


• ulcers, sores, or white spots on lips or in mouth or throat

Less common

• Bloody or cloudy urine


• hives

Rare

• Abdominal or stomach pain, cramping, or burning (severe)


• bloody or black, tarry stools


• confusion


• convulsions (seizures)


• coughing, hoarseness, difficulty in breathing, shortness of breath, tightness in chest, or wheezing


• dark urine


• decreased urination


• decreased vision


• difficulty in swallowing


• feeling of something in the eye


• fever


• hair loss


• hallucinations (hearing, seeing, or feeling things that are not there)


• irritation of nose, throat, or upper chest area, possibly with hoarseness or coughing


• irritation of vagina


• nausea, vomiting, or heartburn (severe and/or continuing)


• numbness, tingling, pain, or weakness, especially in the face, hands, arms, or feet


• pale stools


• painful or difficult urination


• pain in lower back, side, or lower abdomen (stomach) area


• pain, redness, itching, or tearing of eyes


• pinpoint red spots on skin


• problems with muscle coordination


• red, thickened, or scaly skin


• sore throat and fever with or without chills


• swelling of face, fingers, ankles, lower legs, or feet


• swellings (large) on face, eyelids, mouth, lips, and/or tongue


• swollen and/or painful glands


• unusual bleeding or bruising


• unusual tiredness or weakness


• vomiting of blood or material that looks like coffee grounds


• yellow eyes or skin

Some side effects may occur that usually do not need medical attention. These side effects may go away during treatment as your body adjusts to the medicine. Also, your health care professional may be able to tell you about ways to prevent or reduce some of these side effects. Check with your health care professional if any of the following side effects continue or are bothersome or if you have any questions about them:

More common with auranofin; rare with injections

• Abdominal or stomach cramps or pain (mild or moderate)


• bloated feeling, gas, or indigestion (mild or moderate)


• decrease or loss of appetite


• diarrhea or loose stools


• nausea or vomiting (mild or moderate)

Less common

• Constipation—with auranofin


• joint pain—with

Some patients receiving auranofin have noticed changes in the taste of certain foods. If you notice a metallic taste while receiving any gold compound, check with your doctor as soon as possible. If you notice any other taste changes while you are taking auranofin, it is not necessary to check with your doctor unless you find this effect especially bothersome.

Other side effects not listed may also occur in some patients. If you notice any other effects, check with your healthcare professional.

Call your doctor for medical advice about side effects. You may report side effects to the FDA at 1-800-FDA-1088.

The information contained in the Thomson Reuters Micromedex products as delivered by Drugs.com is intended as an educational aid only. It is not intended as medical advice for individual conditions or treatment. It is not a substitute for a medical exam, nor does it replace the need for services provided by medical professionals. Talk to your doctor, nurse or pharmacist before taking any prescription or over the counter drugs (including any herbal medicines or supplements) or following any treatment or regimen. Only your doctor, nurse, or pharmacist can provide you with advice on what is safe and effective for you.

The use of the Thomson Reuters Healthcare products is at your sole risk. These products are provided "AS IS" and "as available" for use, without warranties of any kind, either express or implied. Thomson Reuters Healthcare and Drugs.com make no representation or warranty as to the accuracy, reliability, timeliness, usefulness or completeness of any of the information contained in the products. Additionally, THOMSON REUTERS HEALTHCARE MAKES NO REPRESENTATION OR WARRANTIES AS TO THE OPINIONS OR OTHER SERVICE OR DATA YOU MAY ACCESS, DOWNLOAD OR USE AS A RESULT OF USE OF THE THOMSON REUTERS HEALTHCARE PRODUCTS. ALL IMPLIED WARRANTIES OF MERCHANTABILITY AND FITNESS FOR A PARTICULAR PURPOSE OR USE ARE HEREBY EXCLUDED. Thomson Reuters Healthcare does not assume any responsibility or risk for your use of the Thomson Reuters Healthcare products.