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Glucagon

H04A - Glycogenolytic hormones ATC H04AA01 Protein approved 1998 Parenteral Topical

JFDA label: Glucagen 1 mg INJ

Mechanism of Action

Agonist of Glucagon receptor — Glucagon receptor agonist

TargetActionGene / class
Glucagon receptor efficacy AGONIST GCGR

Indications

Approved

  • Diagnostic aid
  • Hypoglycemia

Off-label

  • Anaphylactic reactions
  • Beta-blocker-induced myocardial depression
  • Calcium channel blocker-induced myocardial depression

Contraindications

Source: Lexicomp

  • Known hypersensitivity to glucagon, lactose, or any component of the formulation Absolute
  • glucagonoma (excluding GlucaGen) Absolute
  • insulinoma Absolute
  • pheochromocytoma Absolute

Adverse Reactions

Very Common >10%Common 1–10%Uncommon 0.1–1% Rare 0.01–0.1%Very Rare <0.01%Not Known

Cardiac disorders (5)

Not Known Hypertension · hypotension (up to 2 hours after GI procedures) · increased blood pressure · increased pulse · tachycardia

Gastrointestinal disorders (2)

Not Known Nausea · vomiting (high incidence with rapid administration of high doses)

General disorders and administration site conditions (2)

Not Known Anaphylaxis · hypersensitivity reaction

Dosing

Source: Lexicomp

Diagnostic aid: Relaxation of stomach, duodenal bulb, duodenum, and small bowel: IM: 1 mg IV: 0.2 to 0.5 mg Relaxation of colon: IM: 1 to 2 mg IV: 0.5 to 0.75 mg Hypoglycemia: IM, IV, SubQ: 1 mg; may repeat in 15 minutes as needed. Note: IV dextrose should be administered as soon as it is available; if patient fails to respond to glucagon, IV dextrose must be given. Anaphylactic reaction (refractory) in patients on beta-blocker therapy (off-label use): IV: Initial: 1 to 5 mg; followed by an infusion of 5 to 15 mcg/minute; titrate the infusion rate to achieve an adequate clinical response (Lieberman 2010). Beta-blocker- or calcium channel blocker-induced myocardial depression (with or without hypotension) unresponsive to standard measures (off-label use; AHA [Vanden Hoek 2010]; Bailey 2003): IV: 3 to 10 mg (or 0.05 to 0.15 mg/kg) bolus followed by an infusion of 3 to 5 mg/hour (or 0.05 to 0.1 mg/kg/hour); titrate infusion rate to achieve adequate clinical response (AHA [Vanden Hoek 2010])
(For additional information see "Glucagon: Pediatric drug information") Hypoglycemia: Note: IV dextrose should be administered as soon as it is available; if patient fails to respond to glucagon, IV dextrose must be given. Infants, Children, and Adolescents: IM, IV, SubQ: Glucagon Emergency Kit: ≥20 kg: 1 mg; may repeat in 15 minutes as needed GlucaGen: Age-based dosing (if weight is unknown): Infants and Children Children ≥6 years and Adolescents: 1 mg; may repeat in 15 minutes if needed Weight-based dosing: ≥25 kg: 1 mg; may repeat in 15 minutes if needed Anaphylactic reaction (refractory) in patients on beta-blocker therapy (off-label use): Children: IV: Initial: 20 to 30 mcg/kg (maximum: 1 mg); followed by an infusion of 5 to 15 mcg/minute; titrate the infusion rate to achieve an adequate clinical response (Lieberman 2010) Beta-blocker- or calcium channel blocker-induced myocardial depression (with or without hypotension) unresponsive to standard measures (off-label use): IV: Children: Initial bolus of 30 to 150 mcg/kg followed by an infusion of 70 mcg/kg/hour (maximum: 5 mg/hour) (Hegenbarth 2008) Adolescents: Initial: 5 to 10 mg over several minutes followed by infusion of 1 to 5 mg/hour (Hegenbarth 2008; PALS [Kleinman 2010])
Refer to adult dosing.

Warnings & Precautions

Source: Lexicomp

Hypersensitivity reactions

Allergic reactions including skin rash and anaphylactic shock (with hypotension and respiratory difficulties) have been reported; reactions have generally been associated with endoscopic patients. Disease-related concerns:

Adrenal insufficiency

Use with caution in patients with adrenal insufficiency; levels of glucose stores in liver may be decreased.

Cardiac disease

Use with caution in patients with cardiac disease.

Chronic hypoglycemia

Use with caution in patients with chronic hypoglycemia; levels of glucose stores in liver may be decreased.

Diabetes

Use caution if using as diagnostic aid in patients with diabetes on insulin; may cause hyperglycemia.

Glucagonoma

Use with caution in patients with glucagonoma. The use of glucagon is contraindicated in patients with this condition (excluding GlucaGen).

Insulinoma

Exogenous glucagon may cause an initial rise in blood glucose followed by rebound hypoglycemia. The use of glucagon is contraindicated in patients with this condition.

Pheochromocytoma

Exogenous glucagon may cause the release of catecholamines, resulting in an increase in blood pressure. The use of glucagon is contraindicated in patients with this condition.

Starvation/fasting

Use caution with prolonged fasting and/or starvation; levels of glucose stores in liver may be decreased. Concurrent drug therapy issues:

Drug-drug interactions

Potentially significant interactions may exist, requiring dose or frequency adjustment, additional monitoring, and/or selection of alternative therapy. Consult drug interactions database for more detailed information. Dosage form specific issues:

Lactose

May contain lactose; avoid administration in hereditary galactose intolerance, Lapp lactase deficiency, or glucose-galactose malabsorption. Other warnings/precautions:

Appropriate use

Insulin or sulfonylurea overdose: Patients with hypoglycemia should immediately be treated with dextrose. If IV access cannot be established or if dextrose is not available, glucagon may be considered as alternative acute treatment until dextrose can be administered.

Secondary hypoglycemia

Supplemental carbohydrates should be given to patients who respond to glucagon for severe hypoglycemia to prevent secondary hypoglycemia.

Pregnancy & Lactation

Pregnancy

FDA category B

Adverse events have not been observed in animal reproduction studies.

Lactation

Glucagon is not absorbed from the GI tract and therefore, it is unlikely adverse effects would occur in a breast-feeding infant.

Monitoring

Clinical pearlBlood pressure, blood glucose, ECG, heart rate, mentation; signs or symptoms of a hypersensitivity reaction.

Chemistry & Properties

2D structure
CAS9007-92-5
PubChem CID16132283
SMILESCC(C)CC(C(=O)NC(CCSC)C(=O)NC(CC(=O)N)C(=O)NC(C(C)O)C(=O)O)NC(=O)C(CC1=CNC2=CC=CC=C21)NC(=O)C(CCC(=O)N)NC(=O)C(C(C)C)NC(=O)C(CC3=CC=CC=C3)NC(=O)C(CC(=O)O)NC(=O)C(CCC(=O)N)NC(=O)C(C)NC(=O)C(CCCNC(=N)N)NC(=O)C(CCCNC(=N)N)NC(=O)C(CO)NC(=O)C(CC(=O)O)NC(=O)C(CC(C)C)NC(=O)C(CC4=CC=C(C=C4)O)NC(=O)C(CCCCN)NC(=O)C(CO)NC(=O)C(CC5=CC=C(C=C5)O)NC(=O)C(CC(=O)O)NC(=O)C(CO)NC(=O)C(C(C)O)NC(=O)C(CC6=CC=CC=C6)NC(=O)C(C(C)O)NC(=O)CNC(=O)C(CCC(=O)N)NC(=O)C(CO)NC(=O)C(CC7=CN=CN7)N

Biology & Pharmacokinetics

Pharmacokinetics predicted

Bioavailability70.0%
Half-life2.555 h
Volume of distribution0.213 L/kg
Protein binding-10.9%
BBB penetrantNo

Transporters

BCRP (Inhibitor)BSEP (Inhibitor)MRP1 (Inhibitor)OATP1B1 (Inhibitor)OATP1B3 (Inhibitor)P-gp (Inhibitor)P-gp (Substrate)

Drug–drug interactions (23, DDInter)

Interacting drugSeverityManagement
Indomethacin moderate
Acebutolol minor
Atenolol minor
Betaxolol minor
Betaxolol (ophthalmic) minor
Bisoprolol minor
Carteolol minor
Carteolol (ophthalmic) minor
Carvedilol minor
Esmolol minor
Labetalol minor
Levobetaxolol (ophthalmic) minor
Levobunolol (ophthalmic) minor
Metipranolol (ophthalmic) minor
Metoprolol minor
Nadolol minor
Penbutolol minor
Pindolol minor
Propranolol minor
Sotalol minor
Timolol minor
Timolol (ophthalmic) minor
Warfarin minor

Registered Products (1)

BrandForm / strengthPackAgentCitizen (JOD)
Glucagen Powder for Injection 1 mg 1 ml Khoury Drug Store 10.920