Brand names: Baqsimi, GlucaGen, Gvoke
Drug class: Glycogenolytic Agents
CAS number: 16941-32-5

Medically reviewed by Drugs.com on Aug 9, 2024. Written by ASHP.

Introduction

Antihypoglycemic agent; hormone synthesized and secreted by the α₂ cells of the pancreatic islets of Langerhans that increases blood glucose concentration by stimulating hepatic glycogenolysis.

Uses for Glucagon

Hypoglycemia

Emergency treatment of severe hypoglycemia in patients with diabetes mellitus; effective only if liver glycogen available.

Convenient for use in emergency situations when dextrose cannot be administered IV. To ensure availability if needed, the American Diabetes Association states glucagon should be prescribed for all patients with diabetes mellitus who are at increased risk of level 2 (glucose concentration <54 mg/dL) or level 3 hypoglycemia (severe events characterized by altered mental and/or physical status requiring assistance for treatment of hypoglycemia).

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

Administer supplemental carbohydrate as soon as possible after patient responds to glucagon therapy, especially to pediatric patients.

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

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.

Concomitant use with anticholinergics not recommended. (See Specific Drugs under Interactions.)

β-Adrenergic or Calcium-channel Blocking Agent Overdosage

Has been used with some success as a cardiac stimulant for management of severe cardiovascular instability (e.g., bradycardia, hypotension, myocardial depression) associated with β-adrenergic blocking agent overdosage^{† [off-label]} or calcium-channel blocking agent overdosage^{† [off-label]} that is refractory to standard measures, including vasopressors. Resuscitation following cardiac arrest from such overdosage should follow standard basic life support (BLS) and advanced cardiac life support (ACLS) algorithms.

Sensitivity Reactions

Has been used in treatment of anaphylaxis that is unresponsive to epinephrine in patients receiving β-adrenergic blocking agents^{† [off-label]}.

Glucagon Dosage and Administration

General

Emergency Treatment of Hypoglycemia

• Inform diabetic patients and their caregivers of the signs and symptoms of severe hypoglycemia.

• Effective treatment of severe hypoglycemia requires assistance from other individuals; patients should inform family members and friends about the availability of glucagon and provide them with instructions for use of the drug.

• Administer as soon as possible after severe hypoglycemia is recognized.

• Immediately following administration, summon emergency assistance. If patient has not responded within 15 minutes after the initial dose, may administer an additional dose while awaiting emergency assistance.

• After clinical response is achieved, administer oral carbohydrates to restore liver glycogen stores and prevent recurrence of hypoglycemia.

Use as Diagnostic Aid in Radiographic Examinations

• Cardiac monitoring recommended in those with cardiac disease.

• Monitor blood glucose concentration in patients with diabetes mellitus.

• Following the radiographic examination, administer oral carbohydrates to patients who have been fasting (if compatible with the procedure).

Administration

Administer glucagon and glucagon hydrochloride by IV, IM, or sub-Q injection. May also administer glucagon intranasally.

Has been administered by IV infusion in patients with severe cardiovascular instability associated with β-adrenergic blocking agent overdosage^{† [off-label]} or calcium-channel blocking agent overdosage^{† [off-label]}.

IV, IM, or Sub-Q Administration

Reconstituted solutions of glucagon or glucagon hydrochloride: Administer IV (under medical supervision only) or by IM or sub-Q injection into upper arms, thighs, or buttocks.

Glucagon injection in prefilled syringes or auto-injectors (Gvoke): For sub-Q use only. Each syringe or auto-injector contains one 0.5- or 1-mg dose of glucagon and cannot be reused. Keep in foil pouch until time of administration. Inject appropriate dose into lower abdomen, outer thigh, or outer upper arm.

Reconstitution

Glucagon for injection: Reconstitute by adding 1 mL of sterile diluent provided by manufacturer to vial labeled as containing 1 mg of glucagon to provide a solution containing 1 mg of glucagon per mL. Swirl vial gently until the powder is completely dissolved.

Glucagon hydrochloride for injection (e.g., GlucaGen): Reconstitute by adding 1 mL of 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. Shake vial gently until powder is completely dissolved.

Use reconstituted solutions immediately; discard any unused portion.

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.

Intranasal Administration

Administer intranasally as glucagon nasal powder (Baqsimi). Each intranasal device contains one 3-mg dose of glucagon and cannot be reused.

Keep the device in the shrink-wrapped tube until time of administration and do not test prior to administration. If tube has been opened and device exposed to moisture, the drug may not work as expected.

Insert the tip of the intranasal device into one nostril and press the device plunger all the way down until the green line is no longer showing. The dose does not need to be inhaled. Consult manufacturer's prescribing information for additional instructions on use of the intranasal device.

Dosage

Available as glucagon and glucagon hydrochloride; dosage expressed in terms of glucagon.

1 mg of glucagon is equivalent to 1 International Unit (IU, unit).

Pediatric Patients

Hypoglycemia

Reconstituted Glucagon for Injection

IV, IM, or Sub-Q

Children weighing <20 kg: 0.5 mg. Alternatively, 20–30 mcg/kg.

Children weighing ≥20 kg: 1 mg.

May administer an additional dose (equivalent to the initial dose) if no response after 15 minutes.

Reconstituted Glucagon Hydrochloride for Injection (e.g., GlucaGen)

IV, IM, or Sub-Q

Children weighing <25 kg: 0.5 mg.

Children weighing >25 kg: 1 mg.

Alternatively, if weight is not known, usual dose is 0.5 mg in children <6 years of age and 1 mg in children ≥6 years of age.

May administer an additional dose (equivalent to the initial dose) if no response after 15 minutes.

Glucagon Injection (Gvoke)

Sub-Q

Children ≥2 to <12 years of age who weigh <45 kg: 0.5 mg.

Children ≥2 to <12 years of age who weigh ≥45 kg: 1 mg.

Children ≥12 years of age: 1 mg.

May administer an additional dose (equivalent to the initial dose) if no response after 15 minutes.

Glucagon Nasal Powder (Baqsimi)

Intranasal

Children ≥4 years of age: 3 mg.

May administer an additional 3-mg dose if no response after 15 minutes.

Adults

Hypoglycemia

Reconstituted Glucagon or Glucagon Hydrochloride for Injection (e.g., GlucaGen)

IV, IM, or Sub-Q

1 mg.

May administer an additional 1-mg dose if no response after 15 minutes.

Glucagon Injection (Gvoke)

Sub-Q

1 mg.

May administer an additional 1-mg dose if no response after 15 minutes.

Glucagon Nasal Powder (Baqsimi)

Intranasal

3 mg.

May administer an additional 3-mg dose if no response after 15 minutes.

Radiographic Examination of GI Tract

Dose depends on the onset of action and duration of effect required for the specific examination. Onset of action depends on the organ under examination and the route of administration. (See Absorption under Pharmacokinetics.)

IV

Stomach, duodenum, or small intestine: Usual dose is 0.2–0.5 mg, although doses up to 2 mg may be used if required. Doses of 2 mg are associated with higher incidence of nausea and vomiting.

Stomach: One manufacturer recommends a dose of 0.5 mg since the stomach is less sensitive to effect of drug.

Colon: Usual dose is 0.5–0.75 mg.

IM

Stomach, duodenum, or small intestine: Usual dose is 1 mg, although doses up to 2 mg may be used if required.

Stomach: One manufacturer recommends a dose of 2 mg since the stomach is less sensitive to effect of drug.

Colon: One manufacturer recommends a dose of 2 mg approximately 10 minutes prior to initiating examination of colon. Other manufacturers recommend a usual dose of 1–2 mg.

Doses of 2 mg are associated with higher incidence of nausea and vomiting.

β-Adrenergic or Calcium-channel Blocking Agent Overdosage†

IV

3–10 mg by direct injection slowly over 3–5 minutes followed by infusion of 2–5 mg/hour has been used. Because of amount of glucagon required to sustain this therapy, consider availability of an adequate drug supply.

Special Populations

Geriatric Patients

When used as diagnostic aid, 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. (See Geriatric Use under Cautions.)

Cautions for Glucagon

Contraindications

• Known hypersensitivity to glucagon or any ingredient in the formulation.

• Pheochromocytoma. (See Pheochromocytoma under Cautions.)

• Insulinoma. (See Insulinoma under Cautions.)

• Use as a diagnostic aid is contraindicated in patients with glucagonoma. (See Glucagonoma under Cautions.)

Warnings/Precautions

Pheochromocytoma

Glucagon may stimulate tumor release of catecholamines in patients with pheochromocytoma, which may cause a marked increase in BP. If patient's BP increases substantially after glucagon administration and a previously undiagnosed pheochromocytoma is suspected, IV administration of 5–10 mg of phentolamine mesylate may effectively lower BP. (See Contraindications under Cautions.)

Insulinoma

Glucagon may produce an initial increase in blood glucose concentrations in patients with insulinoma; however, glucagon may directly or indirectly (through an initial increase in blood glucose concentration) stimulate exaggerated insulin release from an insulinoma and cause hypoglycemia. (See Contraindications under Cautions.) If patient experiences symptoms of hypoglycemia after receiving glucagon, administer IV or oral glucose.

Hypersensitivity Reactions

Allergic reactions (including generalized rash, urticaria, and, occasionally, anaphylactic shock with respiratory distress and hypotension) reported. (See Contraindications under Cautions.)

Decreased Hepatic Glycogen Stores

Glucagon is effective in treating hypoglycemia only if hepatic glycogen stores are sufficient. Patients in states of starvation and those with adrenal insufficiency or chronic hypoglycemia may not have adequate hepatic glycogen stores; use glucose rather than glucagon to treat severe hypoglycemia in these patients.

Necrolytic Migratory Erythema (NME)

NME, a rash commonly associated with glucagonomas and characterized by scaly, pruritic, erythematous plaques, bullae, and erosions, reported in patients receiving continuous IV glucagon infusions. NME lesions may affect the face, groin, perineum, and legs or may be more widespread. NME has resolved following discontinuance of glucagon; treatment with corticosteroids not shown to be effective. If NME occurs, consider risks and benefits of continuing the glucagon infusion.

Use as Diagnostic Aid in Patients with Diabetes Mellitus

Use as diagnostic aid in patients with diabetes mellitus may result in hyperglycemia; monitor blood glucose concentrations and treat if indicated.

Use as Diagnostic Aid in Patients with Cardiac Disease

May increase myocardial oxygen demand, BP, and heart rate, which may be life-threatening and require treatment in patients with cardiac disease. Cardiac monitoring recommended when used as diagnostic aid in patients with cardiac disease.

Glucagonoma

Risk of hypoglycemia in patients with glucagonoma; use as a diagnostic aid in such patients is contraindicated. In patients suspected of having glucagonoma, determine blood glucagon concentration prior to administering glucagon as a diagnostic aid and monitor blood glucose concentrations during treatment. If symptoms of hypoglycemia develop, administer oral or IV glucose.

Immunogenicity

Antibodies to glucagon detected in some patients receiving intranasal glucagon; however, no neutralizing antibodies detected.

Specific Populations

Pregnancy

Available data from case reports and limited number of observational studies involving administration of glucagon in pregnant women over decades of use have not identified a drug-associated risk of major birth defects, spontaneous abortion, or adverse maternal or fetal outcomes. Endogenous glucagon is not transferred across placenta during early gestation. No embryofetal toxicity observed in animals.

Lactation

Not known whether glucagon is distributed into milk. Effects on breast-fed infants and on milk production also unknown. However, glucagon is unlikely to harm an exposed infant because it is a peptide and would be expected to be broken down to its constituent amino acids in the infant's digestive tract.

Pediatric Use

Safety and efficacy established for treatment of hypoglycemia in children. Prefilled syringes and auto-injectors of glucagon have been used safely in children ≥2 years of age. Safety and efficacy of intranasal glucagon established in children ≥4 years of age.

Safety and efficacy not established for use as a diagnostic aid.

Geriatric Use

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

When used as a diagnostic aid, select dosage with caution because of age-related decreases in hepatic, renal, and/or cardiac function and concomitant disease and drug therapy.

Common Adverse Effects

Parenteral administration (frequency not fully established): Injection site reactions (edema, erythema, discomfort), adverse GI effects (nausea, vomiting, abdominal pain, diarrhea), decreased BP, headache, dizziness, asthenia, pallor, somnolence, hyperglycemia or hypoglycemia, urticaria.

Intranasal administration (≥10%): Nausea; vomiting; headache; upper respiratory tract irritation (rhinorrhea, nasal discomfort, nasal congestion, cough, epistaxis); watery eyes; ocular redness; nasal, ocular, or throat pruritus.

Drug Interactions

Specific Drugs

Glucagon Pharmacokinetics

Absorption

Bioavailability

Hydrolyzed and destroyed in GI tract because of polypeptide nature; must administer parenterally or intranasally.

Peak plasma glucagon concentration attained in about 10–13, 15–20, or 10–50 minutes following IM, intranasal, or sub-Q administration.

Nasal congestion associated with the common cold does not alter pharmacokinetics or pharmacodynamics of intranasal glucagon.

Onset

Blood glucose concentration increases within 10 minutes following parenteral or intranasal administration; peak concentration attained within 30 or approximately 60 minutes following parenteral or intranasal administration, respectively.

GI smooth muscle relaxation occurs within 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.

Duration

Hyperglycemic activity persists for about 60–90 minutes following IV or IM administration.

GI 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.

Elimination

Metabolism

Extensively degraded in plasma, liver, and kidneys.

Half-life

8–18 minutes following IV administration.

26–45 minutes following IM administration (may reflect prolonged absorption).

32–42 minutes following sub-Q administration.

35 minutes in adults and 21–31 minutes in pediatric patients following intranasal administration.

Stability

Storage

Parenteral

For Injection

Glucagon: 20–25°C; do not freeze. Store in original package for protection from light. Use reconstituted solution immediately; discard any unused portion.

Glucagon hydrochloride (e.g., GlucaGen): 20–25°C for up to 24 months; do not freeze. Store in original package for protection from light. Use reconstituted solution immediately; discard any unused portion.

Injection

Glucagon in prefilled syringes or auto-injectors (Gvoke PFS): 20–25°C (may be exposed to 15–30°C); do not refrigerate, freeze, or expose to extreme temperatures. Store in sealed foil pouch until time of use.

Intranasal

Powder

Glucagon powder (Baqsimi): ≤30°C in shrink-wrapped tube for protection from moisture.

Actions

• Structurally and pharmacologically identical to endogenous human glucagon, a hormone synthesized and secreted by α₂ cells of pancreatic islets of Langerhans. Commercially available glucagon is prepared synthetically (e.g., via solid-phase peptide synthesis) or using recombinant DNA technology and special laboratory strains of nonpathogenic Escherichia coli or Saccharomyces cerevisiae.

• Increases blood glucose concentration by stimulating hepatic glycogenolysis.

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

• 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.

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

• May enhance peripheral utilization of glucose.

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

• Produces extrahepatic effects independent of hyperglycemic action, although mechanism not fully elucidated; relaxes smooth muscle of the stomach, duodenum, small intestine, and colon.

• Inhibits gastric and pancreatic secretions.

• Produces positive inotropic and chronotropic effects.

• 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.

Advice to Patients

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

• Importance of providing manufacturer’s patient information.

• Importance of understanding proper storage, preparation, and administration techniques before an emergency situation occurs, including appropriate dosages to administer in adults and children.

• Importance of properly instructing patients and family members in detection and treatment of mild hypoglycemia in order to prevent severe hypoglycemia.

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

• 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).

• 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).

• Importance of informing clinicians if hypoglycemic reactions occur so that appropriate adjustment of antidiabetic treatment regimen may be made.

• Importance of informing patients that allergic reactions can occur with glucagon use. Importance of advising patients to seek immediate medical attention if they experience any symptoms of serious hypersensitivity reactions.

• 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.

• Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.

• Importance of advising patients of other important precautionary information. (See Cautions.)

Additional Information

The American Society of Health-System Pharmacists, Inc. represents that the information provided in the accompanying monograph was formulated with a reasonable standard of care, and in conformity with professional standards in the field. Readers are advised that decisions regarding use of drugs are complex medical decisions requiring the independent, informed decision of an appropriate health care professional, and that the information contained in the monograph is provided for informational purposes only. The manufacturer’s labeling should be consulted for more detailed information. The American Society of Health-System Pharmacists, Inc. does not endorse or recommend the use of any drug. The information contained in the monograph is not a substitute for medical care.

Preparations

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

Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.

* available from one or more manufacturer, distributor, and/or repackager by generic (nonproprietary) name

* available from one or more manufacturer, distributor, and/or repackager by generic (nonproprietary) name

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Frequently asked questions

• When should you use glucagon?
• Are glucagon and glycogen the same thing?
• Insulin vs Glucagon - What do they have in common?
• How does the release of glucagon affect blood glucose levels?
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• How much does Baqsimi cost?
• Is Baqsimi covered by Medicare?
• How do you use Baqsimi nasal powder?
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