glucagon (Glucagen, Glucagon Emergency Kit, GlucaGen HypoKit)
Classes: Hypoglycemia Antidotes; Diagnostics, Gastrointestinal; Glucose-Elevating Agents
Dosing and uses of Glucagen (glucagon)
Adult dosage forms and strengths
injection, powder
- 1mg/vial
Hypoglycemia
Indicated for severe hypoglycemic reactions in patients with diabetes treated with insulin
1 mg (1 unit) IM/SC/IV if no IV for dextrose
Repeat q15min once or twice; give dextrose as soon as it is available and if no response
Administer supplemental carbohydrate to replete glycogen stores
Radiography of GI
Indicated as diagnostic aid for decreased GI motility
To inhibit motility of stomach and small bowel: 0.2-0.5 mg IV over time period of 1 min or 1 mg Im
To inhibit motility of colon: 0.5-0.75 mg IV over time period of 1 min or 1 mg Im
Bolus doses >1 mg administered IV may cause nausea and vomiting and are not recommended
Beta-Blocker & Calcium Channel Blocker Toxicity (Off-label)
Indicated off-label for overdose of beta blockers or calcium channel blockers
Load: 50-150 mcg/kg IVP over 1 minute, THEn
3-5 mg/hr or 50-100 mcg/kg/hr IV; titrate infusion to achieve adequate clinical response
Pediatric dosage forms and strengths
injection, powder
- 1mg/vial
Hypoglycemia
Indicated for severe hypoglycemic reactions in patients with diabetes treated with insulin
Administer oral glucose/IVdextrose to replete glycogen stores
GlucaGen
- <6 years: 0.5 mg SC/IM/IV; may repeat in 15 min if necessary
- >6 years: 1 mg SC/IM/IV; may repeat in 15 min if necessary
- Alternatively,
- <25 kg: 0.5 mg; may repeat in 15 min if necessary
- ≥25 kg: 1 mg; may repeat in 15 min if necessary
Glucagon Emergency Kit
- <20 kg: 0.5 mg SC/IM/IV q15min PRN, OR 0.02-0.03 mg/kg/dose SC/IM/IV; may repeat in 15 min if necessary
- ≥20 kg: 1 mg SC/IM/IV; may repeat in 15 min if necessary q20min PRN
Chronic Hypoglycemia (Orphan)
Orphan designation for prevention of chronic, severe hypoglycemia related to congential hyperinsulinism
Sponsor
- Xeris Pharmaceuticals, Inc; 3208 Red River Street, Suite 300; Austin, TX 78705
Glucagen (glucagon) adverse (side) effects
Frequency not defined
Nausea and vomiting
Rash
Hypotension
Tachycardia
Increased blood pressure
Increased pulse
Respiratory distress
Urticaria
Hypoglycemic coma
Hypoglycemia
Warnings
Contraindications
Hypersensitivity
Pheochromocytoma
Insulinoma
Glucagonoma
Cautions
Generalized allergic reactions, including urticaria, respiratory distress, and hypotension reported; if symptoms occur discontinue and treat as indicated
Effective in treating hypoglycemia only if sufficient liver glycogen present
Because glucagon is of little or no help in states of starvation, adrenal insufficiency, or chronic hypoglycemia, hypoglycemia in these conditions should be treated with glucose
Increased blood pressure and heart rate in patients with cardiac disease reported; monitor patients with known cardiac disease
Awaken patient following administration to provide oral glucose if possible, otherwise IV dextrose is required to replete glycogen stores
Pregnancy and lactation
Pregnancy category: B
Lactation: Excretion in milk unknown; use with caution
Pregnancy categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.
C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.
D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.
X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.
NA: Information not available.
Pharmacology of Glucagen (glucagon)
Mechanism of action
Insulin antagonist
Stimulates cAMP synthesis to accelerate hepatic glycogenolysis and gluconeogenesis, causing an increase in blood glucose levels
Preexisting hepatic glycogen stores necessary to be effective in treating hypoglycemia
Glucagon also relaxes smooth muscles of GI tract
Pharmacokinetics
Half-Life: 8-18 min IV; 45 min IM (apparent)
Peak Plasma Time: 13 min IM; 20 min SC
Bioavailability: IM: 30%
Vd: 0.2-0.25 L/kg
Metabolism: by blood, liver, & kidney
Onset
- Increase in glucose levels: 5-20 min IV; 30 min IM; 30-45 min SC
- Diagnostic effect: 1 min IV; 4-10 min IM
Duration
- Increase in glucose levels: 60-90 min (IV/IM/SC)
- GI relaxation: 9-25 min IV; 12-32 min IM
Clearance
- Renal: 19-21 mL/kg/min
- Total Body: 135 mL/min/kg
Administration
IV Preparation
Reconstitute by adding 1 or 10 mL of sterile diluent to a vial containing 1 or 10 units of drug, respectively, to yield solutions containing 1 mg/mL
If dose <2 mg, use only diluent provided by Mfr
If >2 mg, use SWI
Use immediately after reconstitution
IV Administration
Bolus may be associated with nausea and vomiting
Continuous infusions may be used in beta-blocker overdose/toxicity
Storage
Before reconstitution, vials may be kept at controlled room temperature 20-25 degree C (68-77 degrees F)
Use immediately following reconstitution; discard any unused portion