GLUCAGON injection: Patient information

GLUCAGON for injection

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GLUCAGON for injection

Glucagon is an antihypoglycemic agent and a gastrointestinal motility inhibitor. It is produced by solid phase peptide synthesis. The chemical structure of the glucagon is identical to human glucagon. Glucagon is a single-chain polypeptide containing 29 amino acid residues.

Molecular Formula = C153H225N43O49S

Molecular Weight = 3483

Glucagon for Injection is a sterile, lyophilized white powder in a 3 mL vial for subcutaneous, intramuscular or intravenous use. The reconstituted solution contains glucagon as hydrochloride 1 mg per mL and lactose monohydrate (107 mg). Glucagon for Injection is supplied at pH 2.5 to 3.5, hydrochloric acid and/or sodium hydroxide may be added to adjust pH, and is soluble in water.

Mechanism of Action

Glucagon increases blood glucose concentration by activating hepatic glucagon receptors, thereby stimulating glycogen breakdown and release of glucose from the liver. Hepatic stores of glycogen are necessary for glucagon to produce an antihypoglycemic effect. Extrahepatic effects of glucagon include relaxation of the smooth muscle of the stomach, duodenum, small bowel, and colon.

Treatment of Severe Hypoglycemia: Blood glucose concentration rises within 10 minutes of injection and maximal concentrations are attained at approximately 30 minutes after injection. The duration of hyperglycemic action after intravenous or intramuscular injection is 60 to 90 minutes.

In a study in healthy subjects, a subcutaneous dose of 1 mg Glucagon for Injection resulted on average a peak blood glucose concentration of 79.3 mg/dL with a median time of 50 minutes after injection.

Pharmacokinetics

Absorption: Following subcutaneous administration of Glucagon for Injection, the median time to reach the maximum baseline uncorrected plasma glucagon concentrations of 3533 pg/mL was approximately 10 to 13 minutes after dosing Following intramuscular administration of 1 mg dose, the maximum baseline uncorrected plasma glucagon concentrations of 3391 pg/mL were attained approximately 10 minutes after dosing.

Elimination: The mean apparent half-life of glucagon was about 42 minutes after subcutaneous administration. The mean apparent half-life of glucagon was 26 minutes after intramuscular administration.

Metabolism: Glucagon is degraded in the liver, kidney, and plasma.

Indications and usage

Severe Hypoglycemia: Glucagon for Injection is indicated for the treatment of severe hypoglycemia in pediatric and adult patients with diabetes.

Diagnostic Aid: Glucagon for Injection is indicated as a diagnostic aid for use during radiologic examinations to temporarily inhibit movement of the gastrointestinal tract in adult patients.

Important Administration Instructions for Using the Glucagon Emergency Kit for Low Blood Sugar to Treat Severe Hypoglycemia

Glucagon for Injection is for subcutaneous, intramuscular, or intravenous injection. Administer intravenously ONLY under medical supervision.

Instruct patients and their caregivers on the signs and symptoms of severe hypoglycemia. Because severe hypoglycemia requires the help of others to recover, instruct the patient to inform those around them about Glucagon for Injection and its Instructions for Use. Administer Glucagon for Injection as soon as possible when severe hypoglycemia is recognized.

Instruct the patient or caregiver to read the Instructions for Use at the time they receive a prescription for Glucagon for Injection. Emphasize the following instructions to the patient or caregiver:

  • Using the supplied prefilled syringe, carefully insert the needle through the rubber stopper of the vial containing Glucagon for Injection powder and inject all the liquid from the syringe into the vial.
  • Shake the vial gently until the powder is completely dissolved and no particles remain in the fluid. The reconstituted solution should be clear and colorless. Inspect visually for particulate matter and discoloration. If the resulting solution is cloudy or contains particulate matter do not use.
  • The reconstituted solution is 1 mg per mL glucagon.
  • Immediately after reconstitution, inject the solution subcutaneously or intramuscularly in the upper arm, thigh, or buttocks. In addition, healthcare providers may administer intravenously.
  • Call for emergency assistance immediately after administering the dose.
  • If there has been no response after 15 minutes, an additional dose of Glucagon for Injection may be administered while waiting for emergency assistance.
  • When the patient has responded to the treatment and is able to swallow, give oral carbohydrates to restore the liver glycogen and prevent recurrence of hypoglycemia.
  • Discard any unused portion.

Dosage in Adults and Pediatric Patients for Using the Glucagon Emergency Kit for Low Blood Sugar to Treat Severe Hypoglycemia

Adults and Pediatric Patients Weighing More Than 25 kg or for Pediatric Patients with Unknown Weight 6 Years and Older:

  • The recommended dosage is 1 mg (1 mL) injected subcutaneously or intramuscularly into the upper arm, thigh, or buttocks, or intravenously.
  • If there has been no response after 15 minutes, an additional 1 mg dose (1 mL) of Glucagon for Injection may be administered using a new kit while waiting for emergency assistance.

Pediatric Patients Weighing Less Than 25 kg or for Pediatric Patients with Unknown Weight Less Than 6 Years of Age:

  • The recommended dosage is 0.5 mg (0.5 mL) injected subcutaneously or intramuscularly into the upper arm, thigh, or buttocks, or intravenously.
  • If there has been no response after 15 minutes, an additional 0.5 mg dose (0.5 mL) of Glucagon for Injection may be administered using a new kit while waiting for emergency assistance.
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Important Administration Instruction for Using Glucagon for Injection Diagnostic Kit and Glucagon for Injection Single-Dose Vial as a Diagnostic Aid

  • Reconstitute Glucagon for Injection with 1 mL of Sterile Water for Injection. Using a syringe, withdraw all of the Sterile Water for Injection (if supplied) or 1 mL Sterile Water for Injection and inject into the Glucagon for Injection vial.
  • Shake the vial gently until the powder is completely dissolved and no particles remain in the fluid. The reconstituted fluid should be clear and colorless. Inspect visually for particulate matter and discoloration. If the resulting solution is cloudy or contains particulate matter do not use.
  • The reconstituted solution is 1 mg per mL glucagon.
  • Immediately after reconstitution, inject the solution intravenously or intramuscularly into upper arm, thigh, or buttocks.
  • Discard any unused portion.
  • After the end of the diagnostic procedure, give oral carbohydrates to patients who have been fasting, if this is compatible with the diagnostic procedure.

Dosage in Adults for Using Glucagon for Injection Diagnostic Kit and Glucagon for Injection Single-Dose Vial as a Diagnostic Aid:

  • The recommended diagnostic dose for relaxation of the stomach, duodenal bulb, duodenum, and small bowel is 0.2 mg to 0.5 mg administered intravenously or 1 mg administered intramuscularly; the recommended dose to relax the colon is 0.5 mg to 0.75 mg administered intravenously or 1 mg to 2 mg administered intramuscularly.
  • The onset of action after an injection will depend on the organ under examination and route of administration

Contraindications

  • Pheochromocytoma because of the risk of substantial increase in blood pressure
  • Insulinoma because of the risk of hypoglycemia
  • Known hypersensitivity to glucagon or any of the excipients in Glucagon for Injection. Allergic reactions have been reported with glucagon and include anaphylactic shock with breathing difficulties and hypotension
  • Glucagonoma when used as a diagnostic aid because of risk of hypoglycemia

Adverse reactions

  • Hypersensitivity and Allergic Reactions
  • Necrolytic Migratory Erythema
  • Hyperglycemia in Patients with Diabetes Mellitus when Used as a Diagnostic Aid
  • Blood Pressure and Heart Rate Increase in Patients with Cardiac Disease when Used as a Diagnostic Aid

Side effects

  • Nausea
  • Vomiting
  • Injection site swelling
  • Injection site erythema
  • Decreased blood pressure
  • Asthenia
  • Headache
  • Dizziness
  • Pallor
  • Diarrhea
  • Somnolence
  • Hypertension and tachycardia have occurred with glucagon treatment

Drug interactions

Beta-blockers: Patients taking beta-blockers may have a transient increase in pulse and blood pressure when given Glucagon for Injection.

Indomethacin: In patients taking indomethacin, Glucagon for Injection may lose its ability to raise blood glucose or may even produce hypoglycemia.

Anticholinergic Drugs: The concomitant use of anticholinergic drugs and Glucagon for Injection increases the risk of gastrointestinal adverse reactions due to additive effects on inhibition of gastrointestinal motility.

Warfarin: Glucagon for Injection may increase the anticoagulant effect of warfarin.

Insulin: Insulin acts antagonistically to glucagon.

Use in specific populations

Pregnancy: Available data from case reports and a small number of observational studies with glucagon use in pregnant women over decades of use have not identified a drug-associated risk of major birth defects, miscarriage or adverse maternal or fetal outcomes. Multiple small studies have demonstrated a lack of transfer of pancreatic glucagon across the human placental barrier during early gestation. In rat and rabbit reproduction studies, no embryofetal toxicity was observed with glucagon administered by injection during the period of organogenesis at doses representing up to 100 and 200 times the human dose, respectively, based on body surface area (mg/m2 )

Lactation: There is no information available on the presence of glucagon in human or animal milk, the effects of glucagon on the breastfed child or the effects of glucagon on milk production. However, glucagon is a peptide and would be expected to be broken down to its constituent amino acids in the infant’s digestive tract and is therefore, unlikely to cause harm to an exposed infant.

Pediatric Use: The safety and effectiveness of Glucagon for Injection for the treatment of severe hypoglycemia in pediatric patients with diabetes have been established. Safety and effectiveness for use as a diagnostic aid during radiologic examinations to temporarily inhibit movement of the gastrointestinal tract in pediatric patients have not been established.

Overdosage

If overdosage occurs, the patient may experience nausea, vomiting, inhibition of GI tract motility, increase in blood pressure and pulse rate. In case of suspected overdosing, the serum potassium may decrease and should be monitored and corrected if needed. If the patient develops a dramatic increase in blood pressure, phentolamine mesylate has been shown to be effective in lowering blood pressure for the short time that control would be needed.

Recommended Storage

Before Reconstitution: The package containing Glucagon for Injection vials may be stored up to 24 months at 20° to 25° C (68° to 77° F) prior to reconstitution. Do not freeze. Keep in the original package to protect from light.

After Reconstitution: Use reconstituted glucagon solution immediately. Discard any unused portion

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