Varicella Pneumonitis Medications

There are currently no drugs listed for "Varicella Pneumonitis".

Learn more about Varicella Pneumonitis

Micromedex Care Notes:

• Varicella

Medical Encyclopedia:

• Chickenpox

Drug List:

Urokinase 10,000 I.U.

1. Name Of The Medicinal Product

Urokinase medac 10,000 I.U.

Powder for solution for injection or infusion

2. Qualitative And Quantitative Composition

Each vial contains 10,000 I.U. of human urokinase extracted from human urine.

For a full list of excipients, see section 6.1.

3. Pharmaceutical Form

Powder for solution for injection or infusion

4. Clinical Particulars

4.1 Therapeutic Indications

Intravascular lysis of blood clots in the following conditions:

• extensive acute proximal deep vein thrombosis

• acute massive pulmonary embolism

• acute occlusive peripheral arterial disease with limb threatening ischemia

• thrombosed arteriovenous haemodialysis shunts

• thrombosed central venous catheters

4.2 Posology And Method Of Administration

Urokinase medac should only be used by physicians experienced in the management of thrombotic diseases in hospitals where adequate diagnostic and monitoring techniques are available.

Depending on the indication, the route of administration of Urokinase medac is by systemic intravenous infusion, by local intra-arterial catheter-directed infusion during arteriography, or by local instillation.

It must not be given by subcutaneous or intramuscular injection.

For instructions regarding reconstitution and further dilution, see section 6.6.

Adults

The dosage may be adjusted individually depending on the clinical condition. The following dose regimens should be used as a guideline.

Deep vein thrombosis

Urokinase medac should be administered by intravenous infusion into a peripheral vein using an initial dose of 4,400 I.U./kg bodyweight infused over 10 – 20 min, followed by a maintenance dose of 100,000 I.U. per hour for 2 – 3 days.

Pulmonary embolism

Urokinase medac should be administered by intravenous infusion into a peripheral vein using an initial dose of 4,400 I.U./kg bodyweight infused over 10 – 20 min, followed by a maintenance dose of 4,400 I.U./kg bodyweight per hour for 12 hours.

Occlusive peripheral arterial disease

Urokinase medac should be administered by local intra-arterial catheter-directed graded infusion using an initial dose of 4,000 I.U./min (i.e. 240,000 I.U. per hour) for 2 – 4 hours or until restoration of antegrade flow, followed by a dose of 1,000 – 2,000 I.U./min until complete lysis or a maximum of 48 hours.

Thrombosed arteriovenous haemodialysis shunts

Urokinase medac should be administered by local forced periodic infusion (pulse spray) into both branches of the shunt at a concentration of 5,000 to 25,000 I.U./ml up to a total dose of 250,000 I.U. If necessary, the application can be repeated every 30 – 45 minutes up to a maximum of 2 hours.

Thrombosed central venous catheters

Urokinase medac should be dissolved in physiological saline at a concentration of 5,000 I.U./ml. A volume sufficient to completely fill the lumen of the occluded catheter should be instilled and either locked for a duration of 20 to 60 minutes or pushed with aliquots of saline before the lysate is aspirated. The procedure may be repeated if necessary.

Special populations

• Elderly patients: Available data are limited in patients over 65 years and it is not known whether they respond differently from younger subjects. Urokinase medac should be used with caution in elderly patients (see section 4.4).

• Patients with renal or hepatic impairment: A dose reduction may be required in patients with impaired renal and/or hepatic function. In these cases, the fibrinogen level should not fall below 100 mg/dl.

Paediatric patients

There is very limited experience with urokinase in children with thromboembolic occlusive vascular disease and urokinase should not be used in this indication.

Urokinase medac may be used in children of all ages for the treatment of thrombosed central venous catheters using the same lock procedure as in adults.

Therapeutic monitoring

Before starting thrombolytic therapy, haemostasis tests should be performed including haematocrit, platelet count, thrombin time (TT) and activated partial thromboplastin time (aPTT).

If heparin has been given, it should be discontinued and the aPTT should be less than twice the normal control value before urokinase therapy is initiated.

For systemic administration, a 3 to 5 fold prolongation of the TT measured 4 hours after initiation of therapy is generally considered sufficient. However, results of coagulation tests and fibrinolytic activity do not reliably predict either efficacy or risk of bleeding.

Follow-up treatment

In order to prevent recurrent thrombosis subsequent administration of anticoagulants should be instituted provided the aPTT is less than twice the normal control value.

4.3 Contraindications

• Hypersensitivity to the active substance or to any of the excipients

• Active clinically relevant bleeding

• Aneurysm and arteriovenous malformation

• Intracranial neoplasm or other neoplasm with risk of haemorrhage

• Decreased blood coagulation (haemorrhagic diathesis, concomitant therapy with anticoagulants, spontaneous fibrinolysis) and severe thrombocytopenia

• Severe uncontrolled arterial hypertension (systolic > 200 mmHg, diastolic > 100 mmHg; grade III or IV hypertensive retinopathy)

• Acute pancreatitis, pericarditis, bacterial endocarditis, sepsis

• Recent cerebrovascular accident (e.g. within 2 months)

• Recent trauma including cardiopulmonary resuscitation, thoracic surgery or neurosurgery (e.g. within 2 months)

• Recent major surgery until primary wound healing, recent organ biopsy, lumbar puncture, translumbal aortography (e.g. within 10 days)

4.4 Special Warnings And Precautions For Use

In the following conditions, the risk of bleeding may be increased and should be weighed against the anticipated benefits:

• Recent severe gastrointestinal bleeding

• Recent surgery other than thoracic or neurosurgery, recent obstetrical delivery, puncture of non-compressible vessels

• Moderate coagulation defects including those due to severe hepatic or renal diseases

• Cavernous pulmonary diseases

• Genitourinary tract diseases with existing or potential sources of bleeding (e.g. implanted bladder catheter)

• High likelihood of a left heart thrombus (e.g. mitral stenosis with atrial fibrillation) with possible risk of cerebral embolism

• Known septic thrombotic disease

• Severe cerebrovascular disease

• Elderly patients (especially those over 75 years)

Concomitant administration of urokinase with other thrombolytic agents, anticoagulants, or agents inhibiting platelet function may further increase the risk of serious bleeding (see section 4.5).

When bleeding occurs in patients receiving urokinase, it may be difficult to control. Although urokinase is intended to produce sufficient amounts of plasmin to lyse intravascular deposits of fibrin, other fibrin deposits including those which provide haemostasis (at sites of needle puncture, catheter insertion, cut, etc.) are also subject to lysis, and bleeding from such sites may result. Oozing of blood from sites of percutaneous trauma occurs frequently.

The possibility of bruising or haematoma formation, especially after intramuscular injections, is high during urokinase therapy. Intramuscular injections and unnecessary handling of the patient should be avoided. Venipunctures and invasive venous procedures should be performed as infrequently as possible and with care to minimize bleeding. If bleeding from an invasive site is not serious, urokinase therapy may be continued while closely observing the patient; local measures such as application of pressure should be initiated immediately.

Arterial invasive procedures must be avoided before and during urokinase treatment to minimise bleeding. If an arterial puncture is absolutely essential, it should be performed by a physician experienced in the procedure, using a radial or brachial rather than a femoral artery. Direct pressure should be applied at the puncture site for at least 30 minutes, a pressure dressing applied, and the site checked frequently for evidence of bleeding.

If severe bleeding occurs following systemic treatment with urokinase, infusion should be stopped immediately and measures to manage the bleeding implemented. Plasma volume expanders other than dextrans may be used to replace blood volume deficits; if blood loss has been extensive, administration of packed red blood cells is preferred to whole blood. If very rapid reversal of the fibrinolytic state is required, administration of an antifibrinolytic agent such as epsilon-aminocaproic acid may be considered (see section 4.9).

Urokinase medac is a highly purified enzyme produced from human urine. It also contains human serum albumin. Products manufactured from human source materials have the potential to transmit infectious agents. Procedures to control such risks strongly reduce but cannot completely eliminate the risk of transmitting infectious agents.

4.5 Interaction With Other Medicinal Products And Other Forms Of Interaction

Anticoagulants

Oral anticoagulants or heparin may increase the risk of haemorrhage and should not be used concomitantly with urokinase.

Active substances affecting platelet function

Due to increased risk of haemorrhage, concomitant use of urokinase and active substances that affect platelet function (e.g., acetylsalicylic acid, other non-steroidal anti-inflammatory agents, dipyridamole, dextrans) should be avoided.

Contrast agents

Contrast agents may delay fibrinolysis.

4.6 Pregnancy And Lactation

There are no adequate data from the use of urokinase in pregnant women. Animal studies are insufficient with respect to effects on pregnancy, embryonal/fetal development, parturition or postnatal development. The potential risk for humans is unknown. However, low-molecular urokinase fragments and active plasmin cross the placenta.

Urokinase should not be used during pregnancy or in the immediate post-partum period unless clearly necessary.

It is unknown whether urokinase is excreted into human breast milk. Breast-feeding should be avoided during treatment with urokinase.

4.7 Effects On Ability To Drive And Use Machines

Not relevant.

4.8 Undesirable Effects

Haemorrhage

The most frequent and severe adverse effect of urokinase therapy is haemorrhage. The haemostatic status of the patient may be more profoundly altered with urokinase therapy than with heparin or coumarin-derivative anticoagulant therapy.

Severe spontaneous bleeding, including fatalities resulting from cerebral haemorrhage, has occurred during urokinase therapy. Less severe spontaneous bleeding has occurred approximately twice as frequently as that occurring during heparin therapy. Patients with pre-existing haemostatic defects have the greatest risk of spontaneous bleeding.

Moderate decreases in haematocrit not accompanied by clinically detectable bleeding have been reported in approximately 20 % of patients receiving urokinase.

Hypersensitivity reactions

In contrast to streptokinase, urokinase is reportedly non-antigenic. However, mild allergic reactions including bronchospasm and rash have been reported rarely. In addition, very rare cases of fatal anaphylaxis have been reported.

Infusion reactions

Fever and chills, including shaking chills (rigors), have been reported occasionally in patients receiving urokinase. Symptomatic treatment is usually sufficient to alleviate discomfort caused by urokinase-induced fever; however, acetylsalicylic acid should not be used.

Other infusion reactions reported with urokinase therapy include dyspnoea, cyanosis, hypoxemia, acidosis, back pain, and nausea and/or vomiting; these reactions generally occurred within one hour of beginning urokinase infusion.

The following frequency convention was used as a basis for the evaluation of undesirable effects:

Very common
Common:
Uncommon:
Rare:
Very rare	< 1/10,000

Immune system disorders

Rare	Hypersensitivity reactions including dyspnoea, hypotension, flushing, urticaria, rash
Very rare	Anaphylactic reactions

Vascular disorders

Very common	Haemorrhage from puncture sites, wounds
Haematoma
Epistaxis, gingival bleeding
Haematuria (microscopic)
Common	Intracranial haemorrhage
Gastrointestinal haemorrhage, retroperitoneal haemorrhage
Urogenital haemorrhage
Muscle haemorrhage
Embolism, including cholesterol embolism
Uncommon	Intrahepatic haemorrhage

General disorders and administration site conditions

Common

Fever, chills

Investigations

Very common

Decrease in haematocrit without clinically detectable haemorrhage Transient increase in transaminases

4.9 Overdose

Haemorrhage that occurs during treatment with urokinase may be controlled with local pressure and treatment continued. If severe bleeding occurs, treatment with urokinase must be stopped and inhibitors such as aprotinin, epsilon-aminocaproic acid, p-aminoethylbenzoic acid or tranexamic acid can be given. In serious cases, human fibrinogen, factor XII, packed red cells or whole blood should be given as appropriate. For correction of volume deficiency, dextrans should be avoided.

5. Pharmacological Properties

5.1 Pharmacodynamic Properties

ATC code: B01A D04, antithrombotic agent.

Urokinase medac is a highly purified form of naturally occurring human urokinase extracted from urine. Urokinase exists in two distinct molecular entities, a high molecular weight (approximately 54,000 daltons) and a low molecular weight (approximately 33,000 daltons). Urokinase medac contains more than 85 % of the HMW form.

Urokinase is a thrombolytic agent which converts plasminogen into plasmin (fibrinolysin) a proteolytic enzyme that degrades fibrin as well as fibrinogen and other plasma proteins. The activity of urokinase leads to a dose-dependent decrease in plasminogen and fibrinogen levels and to increased presence of fibrin and fibrogen degradation products, which have an anticoagulant effect and potentiate the effect of heparin. These effects persist for 12 – 24 hours after the end of urokinase infusion.

5.2 Pharmacokinetic Properties

Urokinase is eliminated rapidly from the circulation by the liver with a half-life of 10 to 20 minutes. The inactive degradation products are excreted via the bile and primarily via the kidneys.

Elimination is delayed in patients with liver disease and impaired kidney function.

5.3 Preclinical Safety Data

There is no preclinical safety data of additional value to the prescribing physician.

6. Pharmaceutical Particulars

6.1 List Of Excipients

Disodium phosphate dodecahydrate, sodium dihydrogen phosphate dihydrate, human albumin.

6.2 Incompatibilities

No information is available regarding loss of activity in PVC containers or plastic bags/syringes.

6.3 Shelf Life

26 months

Use reconstituted material immediately.

After reconstitution and dilution, chemical and physical stability has been demonstrated for 72 hours at room temperature. From a microbiological point of view, the product should be used immediately after reconstitution and dilution. If not used immediately, in-use storage times and conditions prior to use are the responsibility of the user and would normally not be longer than 24 hours at 2 °C to 8 °C.

6.4 Special Precautions For Storage

Do not store above 25 ºC.

Keep the vial in the outer container to protect from light.

6.5 Nature And Contents Of Container

All presentations are contained in borosilicate clear type 1 glass vials closed with chlorobutyl rubber stoppers and sealed with an aluminium flip-off cap.

6.6 Special Precautions For Disposal And Other Handling

The powder for solution for infusion should be dissolved in water for injection and further diluted with 0.9 % sodium chloride solution or glucose 5 % or glucose 10 % solution.

The powder is to be reconstituted as follows:

For a 10,000 I.U. vial use 2 ml of water for injection.

After reconstitution the solution must be clear and colourless.

7. Marketing Authorisation Holder

medac

Gesellschaft für klinische

Spezialpräparate mbH

Fehlandtstr. 3

20354 Hamburg

Germay

Phone: +49 (0)4103 8006-0

Fax: +49 (0)4103 8006-100

8. Marketing Authorisation Number(S)

PL 11587/0065

9. Date Of First Authorisation/Renewal Of The Authorisation

17/03/2010

10. Date Of Revision Of The Text

22/09/2010

Urogesic Blue

Dosage Form: tablet
UROGESIC-BLUE™

Rx Only

Description

Each tablet contains:

	Methenamine, USP	81.6 mg
	Monobasic Sodium Phosphate, USP	40.8 mg
	Methylene Blue, USP	10.8 mg
	Hyoscyamine Sulfate, USP	0.12 mg

Inactive Ingredients include: microcrystalline cellulose, NF, mannitol, USP, croscarmellose sodium, NF, magnesium stearate, NF and lake blend blue.

HYOSCYAMINE SULFATE is an alkaloid of belladonna. Exists as a white crystalline powder. Affected by light. It is very soluble in water; freely soluble in alcohol; practically insoluble in ether.

METHENAMINE exists as colorless, lustrous crystals or white crystalline powder. Its solutions are alkaline to litmus. Freely soluble in water; soluble in alcohol and in chloroform.

METHYLENE BLUE exists as dark green crystals. It is soluble in water and in chloroform; sparingly soluble in alcohol.

MONOBASIC SODIUM PHOSPHATE exists as a white crystalline powder. Its solutions are acidic to litmus. It is freely soluble in water and practically insoluble in alcohol.

Urogesic Blue - Clinical Pharmacology

HYOSCYAMINE is a parasympatholytic which relaxes smooth muscles and thus produces an antispasmodic effect. It is well absorbed from the gastrointestinal tract and is rapidly distributed throughout body tissues. Most is excreted in the urine within 12 hours, 13% to 50% being unchanged. Its biotransformation is hepatic. Its protein binding is moderate.

METHENAMINE degrades in an acidic urine environment releasing formaldehyde which provides bactericidal or bacteriostatic action. It is well absorbed from the gastrointestinal tract. 70% to 90% reaches the urine unchanged at which point it is hydrolyzed if the urine is acidic. Within 24 hours it is almost completely (90%) excreted; of this amount at pH 5, approximately 20% is formaldehyde. Protein binding: some formaldehyde is bound to substances in the urine and surrounding tissues. Methenamine is freely distributed to body tissue and fluids but is not clinically significant as it does not hydrolyze at pH greater than 6.8.

METHYLENE BLUE possesses weak antiseptic properties. It is well absorbed in the gastrointestinal tract and is rapidly reduced to leukomethylene blue which is stabilized in some combination form in the urine. 75% is excreted unchanged.

MONOBASIC SODIUM PHOSPHATE helps to maintain an acid pH in the urine necessary for the degradation of methenamine.

Indications and Usage for Urogesic Blue

UROGESIC-BLUE™ is indicated for the treatment of symptoms of irritative voiding. Indicated for the relief of local symptoms, such as hypermotility which accompany lower urinary tract infections and as antispasmodic. Indicated for the relief of urinary tract symptoms caused by diagnostic procedures.

Contraindications

UROGESIC-BLUE™ is contraindicated in patients with a hypersensitivity to any of the ingredients. Risk-benefit should be considered when the following medical problems exist: Cardiac disease (especially cardiac arrythmias, congestive heart failure, coronary heart disease, mitral stenosis); gastrointestinal tract obstructive disease; glaucoma; myasthenia gravis; acute urinary retention may be precipitated in obstructive uropathy (such as bladder neck obstruction due to prostatic hypertrophy).

Warnings

Do not exceed recommended dosage. If rapid pulse, dizziness, or blurring of vision occurs discontinue use immediately.

Precautions

Cross sensitivity and/or related problems

patients intolerant of belladonna alkaloids may be intolerant of this medication also.

Pregnancy/Reproduction

Pregnancy Category C

hyoscyamine and methenamine cross the placenta. Studies have not been done in animals or humans. It is not known whether UROGESIC-BLUE™ tablets cause fetal harm when administered to a pregnant woman or can affect reproduction capacity. UROGESIC-BLUE™ tablets should be given to a pregnant woman only if clearly needed.

Breast-feeding

problems in humans have not been documented; however, methenamine and traces of hyoscyamine are excreted in breast milk.

Prolonged use

there have been no studies to establish the safety of prolonged use in humans. No known long-term animal studies have been performed to evaluate carcinogenic potential.

Pediatric

infants and young children are especially susceptible to the toxic effect of the belladonna alkaloids.

Geriatric

use with caution in elderly patients as they may respond to usual doses of hyoscyamine with excitement, agitation, drowsiness, or confusion.

Drug Interactions

because of this product's effect on gastrointestinal motility and gastric emptying, it may decrease the absorption of other oral medications during concurrent use such as: urinary alkalizers; thiazide diuretics (may cause the urine to become alkaline reducing the effectiveness of methenamine by inhibiting its conversion to formaldehyde); antimuscarinics (concurrent use may intensify antimuscarinic effects of hyoscyamine because of secondary antimuscarinic activities of these medications); antacids/antidiarrheals (may reduce absorption of hyoscyamine, concurrent use with antacids may cause urine to become alkaline reducing effectiveness of methenamine by inhibiting its conversion to formaldehyde) doses of these medications should be spaced 1 hour apart from doses of hyoscyamine; antimyasthenics (concurrent use with hyoscyamine may further reduce intestinal motility); ketoconazole (patients should be advised to take this combination at least 2 hours after ketoconazole); monoamine oxidase (MAO) Inhibitors (concurrent use may intensify antimuscarinic side effects, opoid (narcotic) analgesics may result in increased risk of severe constipation); sulfonamides (these drugs may precipitate with formaldehyde in the urine, increasing the danger of crystalluria).

Patients should be advised that the urine may become blue to blue green and the feces may be discolored as a result of the excretion of methylene blue.

Adverse Reactions

Cardiovascular – rapid pulse, flushing

Central Nervous System – blurred vision, dizziness

Respiratory – shortness of breath or troubled breathing

Genitourinary – difficulty micturition, acute urinary retention

Gastrointestinal – dry mouth, nausea/vomiting

Drug Abuse and Dependence

A dependence on the use of UROGESIC-BLUE™ has not been reported and due to the nature of its ingredients, abuse of UROGESIC-BLUE™ is not expected.

Overdosage

Emesis or gastric lavage. Slow intravenous administration of physostigmine in doses of 1 mg to 4 mg (0.5 mg to 1 mg in children), repeated as needed in one to two hours to reverse severe antimuscarinic symptoms. Administration of small doses of diazepam to control excitement and seizures. Artificial respiration with oxygen if needed for respiratory depression. Adequate hydration. Symptomatic treatment as necessary.

Urogesic Blue Dosage and Administration

Adults

One tablet orally 4 times per day followed by liberal fluid intake.

Older Children

Dosage must be individualized by physician. Not recommended for use in children up to 6 years of age.

How is Urogesic Blue Supplied

UROGESIC-BLUE™ are light blue to blue, oval, biconvex tablets debossed with "ED UB" with scoreline on one side and plain on the other side. Supplied in bottles of 100 tablets (NDC 0485-0051-01).

CAUTION

RX ONLY

STORAGE

Store at 25° C (77° F); excursions permitted to 15° C to 30° C (59° F to 86° F) [See USP Controlled Room Temperature]. Keep container tightly closed.

Manufactured for:

Edwards Pharmaceutical, Inc.

111 W. Mulberry St. Ripley, Mississippi 38663

Manufactured by:

Belcher Pharmaceuticals, Inc.

Largo, FL 33777

January 2010                    R - 0110

PRINCIPAL DISPLAY PANEL - 100 count Tablet Bottle Label

NDC 0485-0051-01

UROGESIC-BLUE ™

URINARY ANTISEPTIC

ANTISPASMODIC

DESCRIPTION: Each tablet contains:

Methenamine, USP	81.6 mg
Monobasic Sodium Phosphate, USP	40.8 mg
Methylene Blue, USP	10.8 mg
Hyoscyamine Sulfate, USP	0.12 mg

CONTENTS: 100 TABLETS

RX ONLY

Manufactured for

EDWARDS

PHARMACEUTICAL, INC.

Ripley, MS 38663

Urogesic Blue  methenamine, sodium phosphate, monobasic, methylene blue, and hyoscyamine sulfate  tablet

Product Information Product Type HUMAN PRESCRIPTION DRUG NDC Product Code (Source) 0485-0051 Route of Administration ORAL DEA Schedule

Active Ingredient/Active Moiety Ingredient Name Basis of Strength Strength METHENAMINE (METHENAMINE) METHENAMINE 81.6 mg SODIUM PHOSPHATE, MONOBASIC (SODIUM CATION) SODIUM PHOSPHATE, MONOBASIC 40.8 mg METHYLENE BLUE (METHYLENE BLUE) METHYLENE BLUE 10.8 mg HYOSCYAMINE SULFATE (HYOSCYAMINE) HYOSCYAMINE SULFATE 0.12 mg

Inactive Ingredients Ingredient Name Strength CELLULOSE, MICROCRYSTALLINE   MANNITOL   CROSCARMELLOSE SODIUM   MAGNESIUM STEARATE

Product Characteristics Color BLUE Score 2 pieces Shape OVAL (biconvex) Size 13mm Flavor Imprint Code ED;UB Contains

Packaging # NDC Package Description Multilevel Packaging 1 0485-0051-01 100 TABLET In 1 BOTTLE, PLASTIC None

Marketing Information
Marketing Category	Application Number or Monograph Citation	Marketing Start Date	Marketing End Date
Unapproved drug other		04/30/2010

Labeler - EDWARDS PHARMACEUTICAL, INC. (195118880)

Establishment
Name	Address	ID/FEI	Operations
BELCHER PHARMACEUTIALS, INC.		175968069	MANUFACTURE, ANALYSIS, PACK, LABEL

Revised: 04/2010EDWARDS PHARMACEUTICAL, INC.

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Fluor-Op

Pronunciation: flure-oh-METH-oh-lone
Generic Name: Fluorometholone
Brand Name: Examples include Fluor-Op and FML Forte

Fluor-Op is used for:

Treating inflammation (swelling, warmth, redness, pain) of the eyes and eyelids.

Fluor-Op is a corticosteroid. Exactly how Fluor-Op works is unknown.

Do NOT use Fluor-Op if:

• you are allergic to any ingredient in Fluor-Op


• you have a viral infection of the eye (eg, herpes), a fungal or tuberculosis infection of the eye, certain untreated eye infections (eg, infections producing pus or discharge), or vaccinia or chickenpox infection

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

Before using Fluor-Op:

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

• if you are pregnant, plan 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 thinning of the eye tissues (eg, cornea, sclera), other eye problems (eg, glaucoma, cataracts, nerve damage), or diabetes


• if you have recently had cataract surgery

Some MEDICINES MAY INTERACT with Fluor-Op. Because little, if any, of Fluor-Op 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 Fluor-Op 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 Fluor-Op:

Use Fluor-Op as directed by your doctor. Check the label on the medicine for exact dosing instructions.

• Shake well before each use.


• To use Fluor-Op, first, wash your hands. Tilt your head back. Using your index finger, pull the lower eyelid away from the eye to form a pouch. Drop the medicine into the pouch and gently close your eyes. Immediately use your finger to apply pressure to the inside corner of the eye for 1 to 2 minutes. Do not blink. Remove excess medicine around your eye with a clean tissue, being careful not to touch your eye. Wash your hands to remove any medicine that may be on them. To prevent germs from contaminating your medicine, do not touch the applicator tip to any surface, including your eye. Keep the container tightly closed.


• Do not wear soft contact lenses while you are using Fluor-Op. Sterilize contact lenses according to the manufacturer's directions and check with your doctor before using them.


• If your doctor prescribed more than 1 eye medicine, find out the best order for using each medicine.


• If you miss a dose of Fluor-Op, use it as soon as possible. If it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule. Do not use 2 doses at once.

Ask your health care provider any questions you may have about how to use Fluor-Op.

Important safety information:

• Fluor-Op may cause blurred vision. Do not drive, operate machinery, or do anything else that could be dangerous until you know how you react to Fluor-Op.


• If your condition does not improve within 2 days or if it becomes worse, check with your doctor.


• LAB TESTS, including eye pressure, may be performed to monitor your progress or to check for side effects. Be sure to keep all doctor and lab appointments.


• Use Fluor-Op with extreme caution in CHILDREN younger than 2 years of age. Safety and effectiveness in this age group have not been confirmed.


• PREGNANCY and BREAST-FEEDING: If you become pregnant, discuss with your doctor the benefits and risks of using Fluor-Op during pregnancy. It is unknown if Fluor-Op is excreted in breast milk after use in the eye. If you are or will be breast-feeding while you are using Fluor-Op, check with your doctor or pharmacist to discuss the risks to your baby.

Possible side effects of Fluor-Op:

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:

Blurred vision; taste changes; temporary burning or stinging.

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); changes in vision; continuing blurred vision; discharge from eyes; eye pain, itching, redness, swelling, irritation, or sores not present when you began using Fluor-Op.

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.

See also: Fluor-Op side effects (in more detail)

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 Fluor-Op:

Store Fluor-Op below 77 degrees F (25 degrees C). Store away from heat, moisture, and light. Do not freeze. Do not store in the bathroom. Keep Fluor-Op out of the reach of children and away from pets.

General information:

• If you have any questions about Fluor-Op, please talk with your doctor, pharmacist, or other health care provider.


• Fluor-Op 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 a summary only. It does not contain all information about Fluor-Op. 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.

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Choline Magnesium Trisalicylate Liquid

Choline Magnesium Trisalicylate Liquid

500 mg Salicylate content per 5mL

Choline Magnesium Trisalicylate Liquid Description

Choline Magnesium Trisalicylate Liquid is a nonsteroidal, anti-inflammatory preparation containing choline magnesium trisalicylate which is freely soluble in water. The absolute structure of choline magnesium trisalicylate is not known at this time. Choline magnesium trisalicylate has a molecular formula of C26H29O10NMg, a molecular weight of 539.8, and it may be represented in the solid form as:

Choline Magnesium Trisalicylate Liquid is a cherry-flavored liquid providing 500 mg salicylate content per teaspoonful (5 mL) for oral administration.

Inactive Ingredients: Each teaspoonful (5 mL) of Choline Magnesium Trisalicylate Liquid contains: caramel, carboxymethylcellulose sodium, edetate disodium, FD&C yellow no. 6, flavor, glycerin, methylparaben, potassium sorbate, sodium citrate, sorbic acid, sorbitol, and water.

Choline Magnesium Trisalicylate Liquid - Clinical Pharmacology

Choline Magnesium Trisalicylate Liquid contains salicylate with anti-inflammatory, analgesic and antipyretic action. On ingestion of Choline Magnesium Trisalicylate Liquid, the salicylate moiety is absorbed rapidly and reaches peak blood levels within an average of one to two hours after single dose of the liquid. The primary route of excretion is renal: the excretion products are chiefly the glycine and glucuronide conjugates. At higher serum salicylate concentrations, the glycine conjugation pathway becomes rapidly saturated. Thus, the slower glucuronide conjugation pathway becomes the rate limiting step for salicylate excretion. In addition, salicylate excreted in the bile as glucuronide conjugate may be reabsorbed. These factors account for the prolongation of salicylate half-life and the nonlinear increase in plasma salicylate level as the salicylate dose is increased. The serum concentration of salicylate is increased by conditions that decrease glomerular filtration rate or proximal tubular secretion.

Unlike aspirin and certain other non-steroidal anti-inflammatory agents, such as arylpropionic acid derivatives and arylacetic acid derivatives, choline magnesium trisalicylate at therapeutic dosage levels does not affect platelet aggregation, as shown by in-vitro and in-vivo studies.

Indications and Usage for Choline Magnesium Trisalicylate Liquid

Osteoarthritis, Rheumatoid Arthritis and Acute Painful Shoulder: Salicylates are considered the base therapy of choice in the arthritides; and choline magnesium trisalicylate preparation is indicated for the relief of the signs and symptoms of rheumatoid arthritis, osteoarthritis and other arthritides. Choline Magnesium Trisalicylate Liquid is indicated in the long-term management of these diseases and especially in the acute flare of rheumatoid arthritis. Choline Magnesium Trisalicylate Liquid is also indicated for the treatment of acute painful shoulder.

Choline Magnesium Trisalicylate Liquid is effective and generally well tolerated, and is logical choice whenever salicylate treatment is indicated. It is particularly suitable when a once-a-day or b.i.d. dosage regimen is important to patient compliance; when gastrointestinal intolerance to aspirin is encountered; when gastrointestinal microbleeding or hematologic effects of aspirin are considered a patient hazard; and when interference (or the risk of interference) with normal platelet function by aspirin or by propionic acid derivatives is considered to be clinically undesirable. Use of Choline Magnesium Trisalicylate Liquid is appropriate when a liquid dosage form is preferred, as in the elderly patient.

The efficacy of Choline Magnesium Trisalicylate Liquid has not been studied in those patients who are designated by the American Rheumatism Association as belonging in

Functional Class IV (incapacitated, largely or wholly bedridden or confined to a wheelchair, with little or no self-care).

Analgesic and Antipyretic Action: Choline Magnesium Trisalicylate Liquid is also indicated for the relief of mild to moderate pain and for antipyresis.

Pediatric Use

In children, Choline Magnesium Trisalicylate Liquid is indicated for conditions requiring anti-inflammatory or analgesic action-such as juvenile rheumatoid arthritis and other appropriate conditions.

Contraindications

Patients who are hypersensitive to non-acetylated salicylates should not take Choline Magnesium Trisalicylate Liquid.

Warnings

Reye Syndrome is a rare but serious disease which may develop in children and teenagers who have chicken pox, influenza, or flu symptoms. While the cause of Reye Syndrome is unknown, some studies suggest a possible association between the development of Reye Syndrome and the use of medicines containing acetylated salicylates or aspirin. Choline Magnesium Trisalicylate Liquid is a combination of choline salicylate and magnesium salicylate which are nonacetylated salicylates, and there have been no reported cases associating Choline Magnesium Trisalicylate Liquid with Reye Syndrome. Nevertheless, Choline Magnesium Trisalicylate Liquid, as a salicylate-containing product, is not recommended for use in children and teenagers with chicken pox, influenza or flu symptoms.

The FDA has determined that routine heavy alcohol use (three or more alcoholic drinks every day), in combination with analgesic/antipyretic drug products containing NSAID ingredients (including choline and magnesium salicylates), increases the risk of adverse GI events, including stomach bleeding.

Precautions

General Precautions

As with other salicylates and non-steroidal anti-inflammatory drugs, Choline Magnesium Trisalicylate Liquid should be used with caution in patients with acute or chronic renal insufficiency, with acute or chronic hepatic dysfunction, or with gastritis or peptic ulcer disease. Although reports exist of cross reactivity, including bronchospasm, with the use of non-acetylated salicylate products in aspirin-sensitive patients, Choline Magnesium Trisalicylate Liquid was found to be well tolerated with regard to pulmonary function and respiratory symptoms when these parameters were monitored in a group of documented aspirin-sensitive asthmatics dosed with Choline Magnesium Trisalicylate Liquid in both controlled and open label studies.1

Concurrent use of other salicylate-containing products and Choline Magnesium Trisalicylate Liquid can lead to an increase in plasma salicylate concentration and may result in potentially toxic salicylate levels.

Laboratory Tests

Plasma salicylate levels can be periodically assessed during treatment with Choline Magnesium Trisalicylate Liquid to determine whether a therapeutically effective antiinflammatory concentration of 15 to 30 mg/100 mL (150-300 micrograms/mL) is being maintained. Manifestations of systemic salicylate intoxication are usually not seen until the concentration exceeds 30 mg/100 mL. However, such tests rarely differentiate between the active free and inactive protein bound salicylate components. Since protein binding of salicylate is affected by age, nutritional status, competitive binding of other drugs, and underlying disease (e.g., rheumatoid arthritis), plasma salicylate level determinations may not always accurately reflect efficacious or toxic levels of active free salicylate. Acidification of the urine can significantly diminish the renal clearance of salicylate and increase plasma salicylate concentrations.

Drug Interactions

Foods and drugs that alter urine pH may affect renal clearance of salicylate and plasma salicylate concentrations. Raising urine pH, as with chronic antacid use, can enhance renal salicylate clearance and diminish plasma salicylate concentration; urine acidification can decrease urinary salicylate excretion and increase plasma levels.

When salicylate drug products are concurrently dosed with other plasma protein bound drug products, adverse effects may result. Although Choline Magnesium Trisalicylate Liquid is a rational choice for anti-inflammatory and analgesic therapy in patients on oral anticoagulants due to their demonstrated lack of effect in vivo and in vitro on platelet aggregation, bleeding time, platelet count, prothrombin time, and serum thromboxane B2 generation1-7, the potential exists for increased levels of unbound warfarin with their concurrent use. Prothrombin time should be closely monitored and warfarin dose appropriately adjusted when therapy with Choline Magnesium Trisalicylate Liquid is initiated. The effect of Choline Magnesium Trisalicylate Liquid on blood prothrombin levels has not been established. Salicylates may increase the therapeutic as well as toxic effects of methotrexate, particularly when administered in chemotherapeutic doses, by inhibition of renal methotrexate excretion and by displacement of plasma protein bound methotrexate. Caution should be exercised in administering Choline Magnesium Trisalicylate Liquid to rheumatoid arthritis patients on methotrexate. When sulfonylurea oral hypoglycemic agents are co-administered with salicylates, the hypoglycemic effect may be enhanced via increased insulin secretion or by displacement of sulfonylurea agents from binding sites. Insulin-treated diabetics on high doses of salicylates should also be closely monitored for a similar hypoglycemic response. Other drugs with which salicylate competes for protein binding sites, and whose plasma concentration or free fraction may be altered by concurrent salicylate administration, include the following: phenytoin, valproic acid, and carbonic anhydrase inhibitors.

The efficacy of uricosuric agents may be decreased when administered with salicylate products. Although low doses of salicylate (1 to 2 grams per day) have been reported to decrease urate excretion and elevate plasma urate concentrations, intermediate doses (2 to 3 grams per day) usually do not alter urate excretion. Larger salicylate doses (over 5 grams per day) can induce uricosuria and lower plasma urate levels.

Corticosteroids can reduce plasma salicylate levels by increasing renal elimination and perhaps by also stimulating hepatic metabolism of salicylates. By monitoring plasma salicylate levels, salicylate dosage may be titrated to accommodate changes in corticosteroid dose or to avoid salicylate toxicity during corticosteroid taper.

Drug/Laboratory Test Interactions

Free T4 values may be increased in patients on salicylate drug products due to competitive plasma protein binding; a concurrent decrease in total plasma T4 may be observed. Thyroid function is not affected.

Carcinogenesis

No long-term animal studies have been performed with Choline Magnesium Trisalicylate Liquid to evaluate its carcinogenic potential.

Use in Pregnancy

Pregnancy Category C. Animal reproduction studies have not been conducted with Choline Magnesium Trisalicylate Liquid. It is also not known whether Choline Magnesium Trisalicylate Liquid can cause fetal harm when administered to a pregnant woman or can affect reproduction capacity. Choline Magnesium Trisalicylate Liquid should be given to a pregnant woman only if clearly needed. Because of the known effect of other salicylate drug products on the fetal cardiovascular system (closure of ductus arteriosus), use during late pregnancy should be avoided.

Labor and Delivery

The effects of Choline Magnesium Trisalicylate Liquid on labor and delivery in pregnant women are unknown. Since prolonged gestation and prolonged labor due to

prostaglandin inhibition have been reported with the use of other salicylate products, the use of Choline Magnesium Trisalicylate Liquid near term is not recommended. Other salicylate products have also been associated with alterations in maternal and neonatal hemostasis mechanisms and with perinatal mortality.

Nursing Mothers

Salicylate is excreted in human milk. Peak milk salicylate levels are delayed, occurring as long as 9 to 12 hours post dose, and the milk: plasma ratio has been reported to be as high as 0.34. Because of the potential for significant salicylate absorption by the nursing infant, caution should be exercised when Choline Magnesium Trisalicylate Liquid is administered to a nursing woman.

Geriatric Use

The elderly may be prone to more side effects from salicylates than younger patients due to an age-related decline in renal clearance and/or increased use of concomitant medication. The elderly are more likely than younger patients to be taking a number of medications, some of which may affect the plasma protein binding of salicylate and thus increase the amount of free salicylate.

Adverse Reactions

The most frequent adverse reactions observed with Choline Magnesium Trisalicylate Liquid in clinical trials7-12 are tinnitus and gastrointestinal complaints (including nausea, vomiting, gastric upset, indigestion, heartburn, diarrhea, constipation and epigastric pain). These occur in less than twenty percent (20%) of patients. Should tinnitus develop, reduction of daily dosage is recommended until the tinnitus is resolved. Less frequent adverse reactions, occurring in less than two percent (2%) of patients, are: hearing impairment, headache, lightheadedness, dizziness, drowsiness, and lethargy. Adverse reactions occurring in less than one percent (1%) of patients, are: gastric ulceration, positive fecal occult blood, elevation in serum BUN and creatinine, rash, pruritus, anorexia, weight gain, edema, epistaxis and dysgeusia.

Spontaneous reporting has yielded isolated or rare reports of the following adverse experiences: duodenal ulceration, elevated hepatic transaminases, hepatitis, esophagitis,

asthma, erythema multiforme, urticaria, ecchymoses, irreversible hearing loss and/or tinnitus, mental confusion and hallucinations.

Drug Abuse and Dependence

Drug abuse and dependence have not been reported with Choline Magnesium Trisalicylate Liquid.

Overdosage

Death in adults has been reported following ingestion of doses from 10 to 30 grams of salicylate; however, larger doses have been taken without resulting fatality.

Symptoms: Salicylate intoxication, known as salicylism, may occur with large doses or extended therapy. Common symptoms of salicylism include headache, dizziness, tinnitus, hearing impairment, confusion, drowsiness, sweating, vomiting, diarrhea, and hyperventilation. A more severe degree of salicylate intoxication can lead to CNS disturbances, alteration in electrolyte balance, respiratory and metabolic acidosis, hyperthermia, and dehydration.

Treatment: Reduction of further absorption of salicylate from the gastrointestinal tract can be achieved via emesis, gastric lavage, use of activated charcoal, or a combination of the above. Appropriate I.V. fluids should be administered to correct dehydration, electrolyte imbalance, and acidosis and to maintain adequate renal function. To accelerate salicylate excretion, forced diuresis with alkalinizing solution is recommended. In extreme cases, peritoneal dialysis or hemodialysis should be considered for effective salicylate removal.

Choline Magnesium Trisalicylate Liquid Dosage and Administration

Adults

In rheumatoid arthritis, osteoarthritis, the more severe arthritides, and acute painful shoulder, the recommended starting dosage is 1500 mg given b.i.d. Some patients may be treated with 3000 mg given once per day (h.s.). Dosage should be adjusted in accordance with the patient's response. In patients with renal dysfunction, monitor salicylate levels and adjust dose accordingly.

Elderly

In the elderly patient, a daily dosage of 2250 mg given as 750 mg t.i.d. may be efficacious and well tolerated. Dosage should be adjusted in accordance with the patient's

response. In patients with renal dysfunction, monitor salicylate levels and adjust dose accordingly.

For mild to moderate pain or for antipyresis, the usual dosage is 2000 mg to 3000 mg daily in divided doses (b.i.d.). Based on patient response or salicylate blood levels, dosage may be adjusted to achieve optimum therapeutic effect. Salicylate blood levels should be in the range of 15 to 30 mg/100 mL for anti-inflammatory effect and 5 to 15 mg/100 mL for analgesia and antipyresis.

If the physician prefers, the recommended daily dosage may be administered on a t.i.d. schedule.

As with other therapeutic agents, individual dosage adjustment is advisable, and a number of patients may require higher or lower dosages than those recommended. Certain patients require 2 to 3 weeks of therapy for optimal effect.

Children

Usual daily dose for children for anti-inflammatory or analgesic action: Choline Magnesium Trisalicylate Liquid, 50 mg/kg/day.

Weight (kg)	Total daily dose
12 - 13	500 mg
14 - 17	750 mg
18 - 22	1000 mg
23 - 27	1250 mg
28 - 32	1500 mg
33 - 37	1750 mg

Total daily doses should be administered in divided doses (b.i.d.). The dose of Choline Magnesium Trisalicylate Liquid is calculated as the total daily dose of 50 mg/kg/day for children of 37 kg body weight or less and 2250 mg/day for heavier children.


Choline Magnesium Trisalicylate Liquid is available for greater convenience in treating younger patients and those adult patients unable to swallow a solid dosage form. Choline Magnesium Trisalicylate Liquid may be mixed with fruit juices just before ingestion.

How is Choline Magnesium Trisalicylate Liquid Supplied

Choline Magnesium Trisalicylate Liquid is supplied in bottles of 240 mL.

Store at controlled room temperature 15° to 30°C (59° to 86°F).

REFERENCES:

1. Szczeklik, A et al; Choline magnesium trisalicylate in patients with aspirin-induced asthma; Eur. Respir. J; 3:535-539, 1990.

2. Zucker, MB and Rothwell, KB; Differential influences of salicylate compounds on platelet aggregation and serotonin release; Current Therapeutic Research; 23(2), Feb 1987.

3. Stuart, JJ and Pisko, EJ; Choline magnesium trisalicylate does not impair platelet aggregation; Pharmatherapeutica; 2(8):547, 1981.

4. Danesh, BJZ, Saniabadi, AR, Russell, RI et al; Therapeutic potential of choline magnesium trisalicylate as an alternative to aspirin for patients with bleeding tendencies;

Scottish Medical Journal; 32:167-168, 1987.

5. Danesh, BJZ, McLaren, M, Russell, RI et al; Does non-acetylated salicylate inhibit thromboxane biosynthesis in human platelets? Scottish Medical Journal; 33:315-316,

1988.

6. Danesh, BJZ, McLaren, M, Russell, RI et al; Comparison of the effect of aspirin and choline magnesium trisalicylate on thromboxane biosynthesis in human platelets: role of

the acetyl moiety; Haemostasis; 19:169-173, 1989.

7. Data on file. Medical Department. The Purdue Frederick Company, 1989.

8. Blechman, WJ and Lechner, BL; Clinical comparative evaluation of choline magnesium trisalicylate and acetylsalicylic acid in rheumatoid arthritis; Rheumatology and

Rehabilitation; 18:119-124, 1979.

9. McLaughlin, G; Choline magnesium trisalicylate vs. naproxen in rheumatoid arthritis; Current Therapeutic Research; 32(4):579-585, 1982.

10. Ehrlich, GE, Miller, SB, and Zeiders, RS; Choline magnesium trisalicylate vs. ibuprofen in rheumatoid arthritis; Rheumatology and Rehabilitation; 19:30-41, 1980.

11. Goldenberg, A, Rudnicki, RD, and Koonce, ML; Clinical comparison of efficacy and safety of choline magnesium trisalicylate and indomethacin in treating osteoarthritis;

Current Therapeutic Research; 24(3):245-260, 1978.

12. Guerin, BK and Burnstein, SL; Conservative therapy of acute painful shoulder; Orthopedic Review; XI (7):29-37, 1982.

Manufactured by:

Silarx Pharmaceutical, Inc.

Spring Valley, NY 10977 USA


Revised - March 2006

CHOLINE MAGNESIUM TRISALICYLATE  choline salicylate and magnesium salicylate  liquid

Product Information Product Type HUMAN PRESCRIPTION DRUG NDC Product Code (Source) 54838-522 Route of Administration ORAL DEA Schedule

Active Ingredient/Active Moiety Ingredient Name Basis of Strength Strength Choline Salicylate (SALICYLIC ACID) Choline Salicylate 293 mg  in 5 mL Magnesium Salicylate (SALICYLIC ACID) Magnesium Salicylate 362 mg  in 5 mL

Inactive Ingredients Ingredient Name Strength carboxymethylcellulose sodium   edetate disodium   FD&C yellow no. 6   glycerin   methylparaben   potassium sorbate   sodium citrate   sorbic acid   sorbitol   water

Product Characteristics Color brown (caramel color) Score      Shape Size Flavor CHERRY (black cherry flavor) Imprint Code Contains

Packaging # NDC Package Description Multilevel Packaging 1 54838-522-70 240 mL In 1 BOTTLE, PLASTIC None

Marketing Information
Marketing Category	Application Number or Monograph Citation	Marketing Start Date	Marketing End Date
unapproved drug other		02/05/1997

Labeler - Silarx Pharmaceuticals, Inc (161630033)

Revised: 06/2011Silarx Pharmaceuticals, Inc

More Choline Magnesium Trisalicylate Liquid resources

• Choline Magnesium Trisalicylate Liquid Use in Pregnancy & Breastfeeding
• Choline Magnesium Trisalicylate Liquid Drug Interactions
• Choline Magnesium Trisalicylate Liquid Support Group
• 1 Review for Choline Magnesium Trisalicylate - Add your own review/rating

Compare Choline Magnesium Trisalicylate Liquid with other medications

• Osteoarthritis
• Pain

EtheDent

Generic Name: sodium fluoride (Oral route, Dental route, Oromucosal route)

SOE-dee-um FLOOR-ide

Commonly used brand name(s)

In the U.S.

• APF Gel


• Aquafresh


• CaviRinse


• Control Rx


• Denta 5000 Plus


• Dentagel


• Dentall 1100 Plus


• EtheDent


• Fluorabon


• Fluor-A-Day


• Fluoridex Daily Defense


• Fluoridex Daily Defense Enhanced Whitening

In Canada

• Fluorosol


• Koala Pals Fluoride Tooth Gel - Berrylicious Flavor


• Pdf


• Pedi-Dent

Available Dosage Forms:

• Gel/Jelly


• Tablet, Chewable


• Paste


• Solution


• Liquid


• Tablet, Enteric Coated


• Tablet


• Lozenge/Troche


• Cream

Therapeutic Class: Cariostatic

Uses For EtheDent

Fluoride has been found to be helpful in reducing the number of cavities in the teeth. It is usually present naturally in drinking water. However, some areas of the country do not have a high enough level in the water to prevent cavities. To make up for this, extra fluoride may be added to the diet. Some children may require both dietary fluoride and topical fluoride treatments by the dentist. Use of a fluoride toothpaste or rinse may be helpful as well.

Taking extra oral fluoride does not replace good dental habits. These include eating a good diet, brushing and flossing the teeth often, and having regular dental checkups.

Fluoride may also be used for other conditions as determined by your doctor.

This medicine is available only with a prescription.

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.

People get needed fluoride from fish, including the bones, tea, and drinking water that has fluoride added to it. Food that is cooked in water containing fluoride or in Teflon-coated pans also provides fluoride. However, foods cooked in aluminum pans provide less fluoride.

The daily amount of fluoride 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.

There is no RDA or RNI for fluoride. Daily recommended intakes for fluoride are generally defined as follows:

• Infants and children—


• Birth to 3 years of age: 0.1 to 1.5 milligrams (mg).


• 4 to 6 years of age: 1 to 2.5 mg.


• 7 to 10 years of age: 1.5 to 2.5 mg.

• Adolescents and adults—


• 1.5 to 4 mg.

Remember:

• The total amount of fluoride you get every day includes what you get from the foods and beverages that you eat and what you may take as a supplement.


• This total amount should not be greater than the above recommendations, unless ordered by your health care professional. Taking too much fluoride can cause serious problems to the teeth and bones.

Before Using EtheDent

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

Problems in children have not been reported with intake of normal daily recommended amounts. Doses of sodium fluoride that are too large or are taken for a long time may cause bone problems and teeth discoloration in children.

Geriatric

Problems in older adults have not been reported with intake of normal daily recommended amounts. Older people are more likely to have joint pain, kidney problems, or stomach ulcers which may be made worse by taking large doses of sodium fluoride. You should check with your health care professional.

Breast Feeding

Studies in women suggest that this medication poses minimal risk to the infant when used during 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. Tell your healthcare professional if you are taking any other prescription or nonprescription (over-the-counter [OTC]) medicine.

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. 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 may cause an increased risk of certain side effects but may be unavoidable in some cases. If used together, your doctor may change the dose or how often you use this medicine, or give you special instructions about the use of food, alcohol, or tobacco.

• Dairy Food

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:

• Brown, white, or black discoloration of teeth or


• Joint pain or


• Kidney problems (severe) or


• Stomach ulcer—Sodium fluoride may make these conditions worse.

Proper Use of sodium fluoride

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

Take this medicine only as directed by your health care professional. Do not take more of it and do not take it more often than ordered. Taking too much fluoride over a period of time may cause unwanted effects.

For individuals taking the chewable tablet form of this medicine:

• Tablets should be chewed or crushed before they are swallowed.


• This medicine works best if it is taken at bedtime, after the teeth have been thoroughly brushed. Do not eat or drink for at least 15 minutes after taking sodium fluoride.

For individuals taking the oral liquid form of this medicine:

• This medicine is to be taken by mouth even though it comes in a dropper bottle. The amount to be taken is to be measured with the specially marked dropper.


• Always store this medicine in the original plastic container. Fluoride will affect glass and should not be stored in glass containers.


• This medicine may be dropped directly into the mouth or mixed with cereal, fruit juice, or other food. However, if this medicine is mixed with foods or beverages that contain calcium, the amount of sodium fluoride that is absorbed may be reduced.

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.

• For oral dosage form (lozenges, solution, tablets, or chewable tablets):
  
  • To prevent cavities in the teeth (not enough fluoride in the water):
    
    • Children—Dose is based on the amount of fluoride in drinking water in your area. Dose is also based on the child's age and must be determined by your health care professional.
    
    
  
  

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.

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 EtheDent

The level of fluoride present in the water is different in different parts of the U.S. If you move to another area, check with a health care professional in the new area as soon as possible to see if this medicine is still needed or if the dose needs to be changed. Also, check with your health care professional if you change infant feeding habits (e.g., breast-feeding to infant formula), drinking water (e.g., city water to nonfluoridated bottled water), or filtration (e.g., tap water to filtered tap water).

Do not take calcium supplements or aluminum hydroxide–containing products and sodium fluoride at the same time. It is best to space doses of these two products 2 hours apart, to get the full benefit from each medicine.

Inform your health care professional as soon as possible if you notice white, brown, or black spots on the teeth. These are signs of too much fluoride in children when it is given during periods of tooth development.

EtheDent 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:

Sodium fluoride in drinking water or taken as a supplement does not usually cause any side effects. However, taking an overdose of fluoride may cause serious problems.

• Sores in the mouth and on the lips (rare)

Stop taking this medicine and get emergency help immediately if any of the following effects occur:

• Black, tarry stools


• bloody vomit


• diarrhea


• drowsiness


• faintness


• increased watering of the mouth


• nausea or vomiting


• shallow breathing


• stomach cramps or pain


• tremors


• unusual excitement


• watery eyes


• weakness

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

• Pain and aching of bones


• stiffness


• white, brown, or black discoloration of the teeth—occurs only during periods of tooth development in children

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.

Glucagon

Class: Glycogenolytic Agents
ATC Class: H04AA01
VA Class: HS503
CAS Number: 16941-32-5
Brands: GlucaGen

Introduction

Antihypoglycemic agent; biosynthetic (recombinant DNA-derived) form of human glucagon hormone prepared using special laboratory strains of nonpathogenic Escherichia coli or Saccharomyces cerevisiae.^{1 2 a b c}

Uses for Glucagon

Hypoglycemia

Emergency treatment of severe hypoglycemia; effective only if liver glycogen available.^{a b c}

Convenient for use in emergency situations when dextrose cannot be administered IV;^a however, severe hypoglycemia initially should be treated with IV dextrose, if possible.^b

Do not substitute for IV dextrose in emergency situations in which hypoglycemia is suspected but not established.^a

Increase in blood glucose concentration produced by glucagon not as great in patients with type 1 diabetes mellitus as in those with type 2 diabetes mellitus; administer supplemental carbohydrate as soon as possible, especially to pediatric patients.^{a b c}

Little or no value for treatment of chronic hypoglycemia or hypoglycemia associated with starvation or adrenal insufficiency.^a

Radiographic Examination of GI Tract

Diagnostic aid in radiographic examination of the stomach, duodenum, small intestine, and colon when a hypotonic state would be advantageous; appears to be as effective as antimuscarinic agents and associated with fewer adverse effects.^{a b c}

β-Adrenergic or Calcium-Channel Blocking Agent Overdosage

Has been used with some success as a cardiac stimulant for management of cardiac manifestations (e.g., bradycardia, hypotension, myocardial depression, impaired conduction, cardiogenic shock, cardiac arrest) associated with severe β-adrenergic blocking agent overdosage† or calcium-channel blocking agent overdosage†;^{a d g h i j k l} has successfully reversed such manifestations in patients unresponsive to other drugs (e.g., atropine, dobutamine, dopamine, epinephrine).^{a j l}

Administer early in the management of severe β-adrenergic blocking agent overdosage†.^{a i j k}

Sensitivity Reactions

Has been used rarely in patients with anaphylaxis unresponsive to epinephrine†, particularly in patients receiving β-adrenergic blocking agents, who have an increased incidence and severity of anaphylaxis and may develop a paradoxical response to epinephrine.^{l m} May prevent cardiopulmonary arrest.^l

Glucagon Dosage and Administration

General

• 
  

  Monitor blood glucose concentrations in patients with hypoglycemia until patient is asymptomatic.^{b c}

  
  


• 
  

  After clinical response is achieved or following completion of procedure, administer supplemental carbohydrate to restore liver glycogen and prevent secondary hypoglycemia.^{1 a b c}

  
  

Administration

IV, IM, or Sub-Q Administration

Administer by IV, IM, or sub-Q injection.^{a b c}

Reconstitution

Glucagon (Lilly): Reconstitute by adding 1 mL of sterile diluent to vial labeled as containing 1 mg of glucagon to provide a solution containing 1 mg of glucagon per mL.^{1 b} Do not use concentrations >1 mg/mL.^{1 b} Use only diluent provided by manufacturer; do not use diluent to reconstitute other drugs.^{1 b}

Glucagon hydrochloride (GlucaGen): Reconstitute by adding 1 mL of sterile diluent (if supplied by manufacturer) or sterile water for injection to a vial labeled as containing 1 mg of glucagon to provide a solution containing 1 mg of glucagon per mL.^{2 c}

Use reconstituted solutions immediately; discard any unused portion.^{1 2 b c}

Dilution

To prepare continuous IV infusion solution for treatment of β-adrenergic or calcium-channel blocking agent overdosage†, dilute reconstituted glucagon in 5% dextrose injection.^{a h}

Dosage

Available as glucagon (rDNA origin, Lilly) and glucagon hydrochloride (rDNA origin, GlucaGen); dosage expressed in terms of glucagon.^{a b c}

1 mg of glucagon is equivalent to 1 International Unit (IU, unit).^{1 b c}

Pediatric Patients

Hypoglycemia

Glucagon (Lilly)

IV, IM, or Sub-Q

Children <20 kg: 0.5 mg.^{1 b d e f} Alternatively, 20–30 mcg/kg may be administered.^{1 b d}

Children ≥20 kg: 1 mg.^{1 b d e f}

An additional dose may be administered if patient does not awaken within 15 minutes following administration of drug; however, seek emergency assistance so that IV dextrose may be administered because of potential serious adverse effects associated with prolonged cerebral hypoglycemia.^{a b c} If patient fails to respond to glucagon, IV dextrose must be given.^{a c}

Glucagon Hydrochloride (GlucaGen)

IV, IM, or Sub-Q

Children <25 kg: 0.5 mg.^{2 c d f}

Children ≥25 kg: 1 mg.^{2 c d f}

Alternatively, if weight is not known, usual dose in children <6–8 years of age is 0.5 mg and in children >6–8 years of age is 1 mg.^{c f}

An additional dose may be administered if patient does not awaken within 15 minutes following administration of drug; however, seek emergency assistance so that IV dextrose may be administered because of potential serious adverse effects associated with prolonged cerebral hypoglycemia.^{a c} If patient fails to respond to glucagon, IV dextrose must be given.^{a c}

β-Adrenergic or Calcium-Channel Blocking Agent Overdosage†

IV

In children, initially, 50–100 mcg/kg as a loading dose (i.e., bolus), followed by a continuous IV infusion of 100 mcg/kg per hour.^d

Alternatively, in adolescents, some experts have suggested a dose of 5–10 mg administered over several minutes, followed by an IV infusion of 1–5 mg/hour for the treatment of β-adrenergic blocking agent overdosage†.^l

Adults

Hypoglycemia

Glucagon (Lilly) and Glucagon Hydrochloride (GlucaGen)

IV, IM, or Sub-Q

1 mg.^{1 2 b c}

An additional dose may be administered if patient does not awaken within 15 minutes following administration of drug; however, seek emergency assistance so that IV dextrose may be administered because of potential serious adverse effects associated with prolonged cerebral hypoglycemia.^{a b} If patient fails to respond to glucagon, IV dextrose must be given.^{a c}

Radiographic Examination of GI Tract

IV

Stomach, duodenum, or small intestine: 0.25–2 mg, depending on onset of action and duration of effect required for specific examination.^{1 2 3 b c} (See Absorption under Pharmacokinetics.)

For relaxation of the stomach, one manufacturer (Lilly) has recommended a dose of 0.5 mg since the stomach is less sensitive to effect of drug.^{1 3 b}

IM

Stomach, duodenum, or small intestine: 1–2 mg, depending on onset of action and duration of effect required for specific examination.^{1 2 3 b c} (See Absorption under Pharmacokinetics.)

For relaxation of the stomach, one manufacturer (Lilly) has recommended a dose of 2 mg since the stomach is less sensitive to effect of drug.^{1 3 b}

Colon: One manufacturer (Lilly) has recommended a dose of 2 mg approximately 10 minutes prior to initiating examinations of colon; may facilitate a more satisfactory radiographic examination.^{1 3 b}

β-Adrenergic or Calcium-Channel Blocking Agent Overdosage†

IV

Initially (as a loading dose), 50–150 mcg/kg (approximately 3–10 mg for a 70-kg patient)^j over 1–2 minutes; higher doses may be needed if ineffective.^{a d h i j k} Loading dose has been repeated every 3–10 minutes, if needed; however, continuous IV infusion should follow loading dose administration because of drug’s short duration of action.^{j k} (See Absorption under Pharmacokinetics.)

Continuous IV infusion: 1–5 mg/hour; infusion rate may be reduced according to response.^{a d h i j k} Alternatively, a continuous IV infusion of 50–100 mcg/kg per hour has been administered.^{i k} Also, some experts suggest an IV infusion rate based on effective loading dose per hour (e.g., if initial effective cumulative loading dose is 10 mg, hourly infusion rate should be 10 mg/hour).^{j k}

Sensitivity Reactions†

IV or IM

1–2 mg every 5 minutes has been administered in patients with anaphylaxis unresponsive to epinephrine†.^l

Special Populations

Geriatric Patients

Select dosage with caution, usually initiating therapy at the low end of the dosage range, because of age-related decreases in hepatic, renal, and/or cardiac function and concomitant disease and drug therapy.^b (See Geriatric Use under Cautions.)

Cautions for Glucagon

Contraindications

• 
  

  Known hypersensitivity to glucagon or any ingredient in the formulation.^{b c}

  
  


• 
  

  Pheochromocytoma.^{b c} (See Pheochromocytoma under Cautions.)

  
  


• 
  

  Glucagon (rDNA origin, GlucaGen): Insulinoma.^c (See Insulinoma under Cautions.)

  
  

Warnings/Precautions

Warnings

Insulinoma

IV administration may produce an initial increase in blood glucose concentrations in patients with insulinoma; however, insulinoma may release insulin and secondary hypoglycemia may occur.^b Administer glucose orally, IV, or by gavage, whichever is most appropriate, or other adequate carbohydrate if patient develops symptoms of hypoglycemia following administration of drug.^{b c}

Use with caution in patients with suspected insulinoma or history suggesting insulinoma.^{a b c}

Glucagon (rDNA origin, GlucaGen) contraindicated in patients with insulinoma.^c

Pheochromocytoma

Exogenous administration of glucagon stimulates release of catecholamines, which may cause a sudden and marked increase in BP in patients with pheochromocytoma.^{a b c} If BP suddenly increases, phentolamine mesylate may be administered IV in an attempt to control BP.^b

Use contraindicated in patients with known pheochromocytoma; use with caution in patients with suspected pheochromocytoma or history suggesting pheochromocytoma.^{a b c}

Sensitivity Reactions

Hypersensitivity Reactions

Consider possibility of hypersensitivity reactions since glucagon is a protein.^a

Allergic reactions, including rash,^{2 c} urticaria, respiratory distress, and rarely, hypotension and anaphylaxis with respiratory distress reported.^{1 2 b} Anaphylactic reactions generally occurred in association with endoscopic examination during which patients often received other agents (e.g., contrast media, local anesthetics).^{2 c}

If patient develops respiratory difficulties following administration of drug, administer standard therapy for anaphylaxis (e.g., epinephrine).^c

Glucagon-specific antibodies not detected during a 3-month study of individuals receiving either animal-source glucagon or biosynthetic glucagon (rDNA origin).^{1 b}

General Precautions

Treatment Considerations

Liver glycogen must be available when glucagon is used for treatment of severe hypoglycemia;^{a b c} otherwise, an inadequate reversal of hypoglycemia may occur.^c Use with caution in patients with conditions associated with reduced concentrations of releasable glucose in the liver (e.g., prolonged fasting, starvation, adrenal insufficiency, chronic hypoglycemia);^{a b c} administer glucose in these patients.^b

Use with caution in patients with diabetes.^c

Cardiovascular Effects

Possible tachycardia and hypertension; may require treatment in patients with CAD.^c

Specific Populations

Pregnancy

Category B.^{b c}

Lactation

Not known whether glucagon is distributed into milk; use with caution.^{b c} However, one manufacturer states that drug is not likely to have an effect on infants if ingested;^c drug has short half-life and intact drug is not absorbed in GI tract.^{b c} (See Absorption and see Elimination under Pharmacokinetics.)

Pediatric Use

Safety and efficacy established for treatment of hypoglycemia.^{1 2 b c}

Safety and efficacy not established for use as a diagnostic aid.^{1 2 b c}

Geriatric Use

Insufficient experience from clinical trials in patients ≥65 years of age to determine whether geriatric patients respond differently than younger patients.^b However, other clinical experience has not identified differences in response between geriatric patients and younger adults.^b

Select dosage with caution because of age-related decreases in hepatic, renal, and/or cardiac function and concomitant disease and drug therapy.^b (See Geriatric Patients under Dosage and Administration.)

Use with caution to inhibit GI motility in geriatric patients with known cardiac disease.^c

Common Adverse Effects

Dose-related nausea,^{a b c} vomiting.^{a b c}

Interactions for Glucagon

Specific Drugs

Drug	Interaction	Comments
Anticholinergic agents	Possible increased adverse effectsa b c
β-Adrenergic blocking agents	Possible increased pulse rate and BPc
Epinephrine	Increased and prolonged hyperglycemic effect of glucagona
Sympatholytic agents (e.g., dihydroergotamine)	Do not appear to inhibit actions of glucagona

Glucagon Pharmacokinetics

Absorption

Bioavailability

Hydrolyzed and destroyed in GI tract because of polypeptide nature;^{a b c} must administer parenterally.^a

Prolonged absorption from injection site following IM administration.^c

Peak plasma glucagon concentrations attained in about 20 or 13 minutes following sub-Q or IM administration, respectively.^{b c}

Peak blood glucose concentrations attained in about 30–45,^{b c} 26–30,^{b c} or 5–20 minutes^c following sub-Q, IM, or IV administration, respectively.^{b c}

Onset

Blood glucose concentrations increase within 10 minutes following IM administration.^c

Unconscious patient with severe hypoglycemia usually awakens within 15 minutes following administration.^b

Smooth muscle relaxation occurs in 45 seconds to 1 minute following IV administration of 0.25–2 mg, and within 8–10 or 4–7 minutes following IM administration of 1 or 2 mg, respectively.^{1 2 b c}

Duration

Hyperglycemic activity persists for about 60–90 minutes.^{2 c}

Smooth muscle relaxation persists for about 9–17 or 22–25 minutes following IV administration of 0.25–0.5 mg or 2 mg, respectively, and for about 12–27 or 21–32 minutes following IM administration of 1 or 2 mg, respectively.^{1 2 b c}

Elimination

Metabolism

Exact metabolic fate not established; extensively degraded in plasma, liver, and kidneys.^{a b c}

Elimination Route

Urinary excretion of intact drug not established.^b

Half-life

8–18 minutes following IV administration.^{1 b}

45 minutes following IM administration.^{2 c}

Stability

Storage

Parenteral

For Injection

Glucagon (rDNA origin, Lilly): 20–25°C.^{1 b} Use reconstituted solution immediately; discard any unused portion.^{a b}

Glucagon hydrochloride (rDNA origin, GlucaGen): 20–25°C for up to 24 months.^c Do not freeze; protect from light.^c Use reconstituted solution immediately; discard any unused portion.^{a c}

ActionsActions

• 
  

  Structurally and pharmacologically identical to endogenous human glucagon, a hormone synthesized and secreted by α₂ cells of pancreatic islets of Langerhans.^{a b c}

  
  


• 
  

  Increases blood glucose concentration by stimulating hepatic glycogenolysis.^{a b c}

  
  


• 
  

  Produces some metabolic effects in various tissues (e.g., liver, adipose tissue) similar to those of epinephrine.^a

  
  


• 
  

  Stimulates formation of adenylate cyclase, which catalyzes conversion of adenosine triphosphate (ATP) to cyclic adenosine-3’,5’-monophosphate (cAMP), particularly in liver and adipose tissue, resulting in initiation of a series of intracellular reactions (e.g., activation of phosphorylase) promoting degradation of glycogen to glucose.^a

  
  


• 
  

  Actions usually antagonistic to insulin; however, may stimulate insulin secretion in healthy individuals and in patients with type 2 diabetes mellitus.^a

  
  


• 
  

  May enhance peripheral utilization of glucose.^a

  
  


• 
  

  Intensity of hyperglycemic effect depends on hepatic glycogen reserve and presence of phosphorylases.^a

  
  


• 
  

  Produces extrahepatic effects independent of hyperglycemic action, although mechanism not fully elucidated; relaxes smooth muscle of the stomach, duodenum, small intestine, and colon.^{a b c}

  
  


• 
  

  Inhibits gastric and pancreatic secretions.^a

  
  


• 
  

  Produces positive inotropic and chronotropic effects.^{a c}

  
  


• 
  

  Decreases plasma amino nitrogen concentrations, enhances renal excretion of electrolytes, decreases synthesis of protein and fat, increases metabolic rate, and produces a diabetic effect, which may persist for several days, following prolonged administration.^a

  
  

Advice to Patients

• 
  

  Importance of advising patients with diabetes about nature of disease, preventing and detecting complications, and managing their condition.^a

  
  


• 
  

  Importance of providing manufacturer’s patient information.^{a b c}

  
  


• 
  

  Importance of understanding proper storage, preparation, and administration techniques before an emergency situation occurs, including appropriate dosages to administer in adults and children.^{a b c}

  
  


• 
  

  Importance of properly instructing patients and family members in detection and treatment of mild hypoglycemia in order to prevent severe hypoglycemia.^{a b c}

  
  


• 
  

  Importance of instructing patients that glucagon should be used only for severe hypoglycemia; provide instruction in detection of severe hypoglycemia.^c

  
  


• 
  

  Provide instructions regarding measures to prevent hypoglycemic reactions due to insulin (e.g., adhering to diet, insulin, and exercise regimens; regular monitoring of blood glucose concentrations; routinely carrying sugar, candy, or other readily absorbable carbohydrate to treat symptoms of hypoglycemia).^{a b}

  
  


• 
  

  Importance of informing family members to arouse patient as quickly as possible because prolonged hypoglycemia may result in damage to CNS, and to administer supplemental carbohydrates as soon as the patient awakens and is able to swallow (particularly in children and adolescents).^{b c}

  
  


• 
  

  Importance of informing clinicians if hypoglycemic reactions occur so that appropriate adjustment of treatment regimen may be made.^{a b c}

  
  


• 
  

  Importance of informing clinician of existing or contemplated concomitant therapy, including prescription and OTC drugs and dietary or herbal products, as well as any concomitant illnesses.^{b c}

  
  


• 
  

  Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.^{b c}

  
  


• 
  

  Importance of advising patients of other important precautionary information.^{b c} (See Cautions.)

  
  

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Glucagon (Recombinant DNA origin)

Routes	Dosage Forms	Strengths	Brand Names	Manufacturer
Parenteral	For injection	1 mg (1 unit)	Glucagon Emergency Kit (with 1 mL diluent available in Hyporet disposable syringe)	Lilly

Glucagon Hydrochloride (Recombinant DNA origin)

Routes	Dosage Forms	Strengths	Brand Names	Manufacturer
Parenteral	For injection	1 mg (1 unit) (of glucagon)	GlucaGen	Bedford
			GlucaGen Diagnostic Kit (with 1 mL sterile water for injection diluent)	Bedford
			GlucaGen HypoKit (with 1 mL sterile water for injection diluent available in disposable syringe)	Novo Nordisk

Comparative Pricing

This pricing information is subject to change at the sole discretion of DS Pharmacy. This pricing information was updated 03/2011. Actual costs to patients will vary depending on the use of specific retail or mail-order locations and health insurance copays.

GlucaGen HypoKit 1MG Solution (NOVO NORDISK): 1/$119.99 or 3/$349.96

Glucagon Emergency 1MG Kit (LILLY): 1/$133.98 or 3/$369.98

Disclaimer

This report on medications is for your information only, and is not considered individual patient advice. Because of the changing nature of drug information, please consult your physician or pharmacist about specific clinical use.

The American Society of Health-System Pharmacists, Inc. and Drugs.com represent that the information provided hereunder was formulated with a reasonable standard of care, and in conformity with professional standards in the field. The American Society of Health-System Pharmacists, Inc. and Drugs.com make no representations or warranties, express or implied, including, but not limited to, any implied warranty of merchantability and/or fitness for a particular purpose, with respect to such information and specifically disclaims all such warranties. Users are advised that decisions regarding drug therapy are complex medical decisions requiring the independent, informed decision of an appropriate health care professional, and the information is provided for informational purposes only. The entire monograph for a drug should be reviewed for a thorough understanding of the drug's actions, uses and side effects. The American Society of Health-System Pharmacists, Inc. and Drugs.com do not endorse or recommend the use of any drug. The information is not a substitute for medical care.

AHFS Drug Information. © Copyright, 1959-2011, Selected Revisions August 2008. American Society of Health-System Pharmacists, Inc., 7272 Wisconsin Avenue, Bethesda, Maryland 20814.

† Use is not currently included in the labeling approved by the US Food and Drug Administration.

References

1. Eli Lilly and Company. Glucagon (rDNA origin) for injection prescribing information. Indianapolis, IN; 1999 Feb.

2. Bedford Laboratories. GlucaGen (glucagon [rDNA origin]) for injection prescribing information. Bedford, OH; 1999 Jul.

3. Bedford Laboratories, Bedford, OH: Personal communication.

a. AHFS Drug Information 2007. McEvoy GK, ed. Glucagon. Bethesda, MD: American Society of Health-System Pharmacists; 2007: 3210-1.

b. Eli Lilly and Company. Glucagon (rDNA origin) for injection prescribing information. Indianapolis, IN; 2005 Feb.

c. Novo Nordisk. GlucaGen (glucagon [rDNA origin]) for injection prescribing information. Princeton, NJ; 2004 Dec.

d. Gunn VL, Nechyba C, eds. The Harriet Lane handbook: a manual for pediatric house officers. 16th ed. Philadelphia, PA: Mosby: 2002:27-8, 49, 705-6.

e. Eli Lilly and Company, Indianapolis, IN: Personal communication.

f. Novo Nordisk, Princeton, NJ: Personal communication.

g. Anon. Pharmaceutical drug overdose. Treat Guidel Med Lett. 2006; 4:61-6. [PubMed 16929234]

h. Shepherd G. Treatment of poisoning caused by beta-adrenergic and calcium-channel blockers. Am J Health Syst Pharm. 2006; 63:1828-35. [PubMed 16990629]

i. Bailey B. Glucagon in beta-blocker and calcium channel blocker overdoses: a systematic review. J Toxicol Clin Toxicol. 2003; 41:595-602. [PubMed 14514004]

j. Kerns W. Management of beta-adrenergic blocker and calcium channel antagonist toxicity. Emerg Med Clin North Am. 2007; 25:309-31; abstract viii. [PubMed 17482022]

k. DeWitt CR, Waksman JC. Pharmacology, pathophysiology and management of calcium channel blocker and beta-blocker toxicity. Toxicol Rev. 2004; 23:223-38. [PubMed 15898828]

l. The American Heart Association. Guidelines 2005 for cardiopulmonary resuscitation and emergency cardiovascular care. Circulation. 2005; 112(Suppl I): IV1-211.

m. Thomas M, Crawford I. Best evidence topic report. Glucagon infusion in refractory anaphylactic shock in patients on beta-blockers. Emerg Med J. 2005; 22:272-3. [PubMed 15788828]

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