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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