GLUCAGEN HYPOKIT

Indications

• Severe hypoglycemia
• Diagnostic aid in radiologic examinations of the gastrointestinal tract
• Management of certain types of insulinomas

Dosage

Children: In children, for hypoglycemia, administer 0.5 mg to 1 mg intramuscularly or subcutaneously. For infants less than 20 kg, 0.5 mg is recommended. For detailed and specific

Adults: For hypoglycemia, administer 1 mg intramuscularly or subcutaneously. If no response after 15 minutes, a second dose may be given. For diagnostic purposes, doses may vary depending on the procedure; refer to specific guidelines.

Mechanism of action

Glucagon acts on the glucagon receptors (GCGR) located primarily in the liver. Upon binding, it activates adenylate cyclase, increasing the levels of cyclic AMP (cAMP). The rise in cAMP activates protein kinase A (PKA), which in turn promotes the conversion of glycogen to glucose (glycogenolysis) and enhances the synthesis of glucose from non-carbohydrate sources (gluconeogenesis). This results in elevated blood glucose concentrations.

Pharmacodynamics

The pharmacodynamic effects of glucagon include rapid elevation of blood glucose levels, increased heart rate, and reduced gastrointestinal motility. The onset of action is typically within 5 to 15 minutes when administered parenterally, with peak effects observed within 30 minutes. The duration of action is approximately 1 to 2 hours, depending on the dose and route of administration.

Pharmacokinetics

Glucagon is rapidly absorbed following subcutaneous or intramuscular administration, with bioavailability influenced by the administration route. It has a short half-life of about 3 to 6 minutes, primarily due to degradation by the liver and kidneys. It does not require metabolism by the cytochrome P450 system. Its effects can be reversed by the administration of glucose or carbohydrates.

Contra-indications

• Hypersensitivity to glucagon or any of its excipients
• Pheochromocytoma
• Insulinoma

Adverse effects

• Nausea
• Vomiting
• Hypoglycemia
• Allergic reactions
• Tachycardia
• Hypotension

Interactions

• Antidiabetic agents may have reduced efficacy when glucagon is administered
• Beta-blockers may increase the risk of severe hypotension

Precautions

• Use with caution in patients with insulinoma or pheochromocytoma
• Monitor blood glucose levels closely in patients with adrenal insufficiency
• Careful administration is required in patients with cardiovascular disease

Pregnancy

Glucagon is classified as category B; animal reproduction studies have not shown a risk to the fetus, but there are no adequate and well-controlled studies in pregnant women.

Breast-feeding

There is no information on the excretion of glucagon in human milk, but it is unlikely to affect a nursing infant when used as directed.

Storage

Store at 2 to 8 degrees Celsius. Do not freeze. Discard unused portion after reconstitution.

Formulations

• Glucagon for injection: 1 mg/vial