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GlucaGen

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GlucaGen

CLINICAL PHARMACOLOGY

Mechanism of Action

Antihypoglycemic Action

Glucagon induces liver glycogen breakdown, releasing glucose from the liver. Hepatic stores of glycogen are necessary for glucagon to produce an antihypoglycemic effect.

Gastrointestinal Motility Inhibition

Extra hepatic effects of glucagon include relaxation of the smooth muscle of the stomach, duodenum, small bowel, and colon.

Pharmacodynamics

For the treatment of severe hypoglycemia

Blood glucose concentration rises within 10 minutes of injection and maximal concentrations are attained at approximately 30 minutes after injection (see Figure 1). The duration of hyperglycemic action after intravenous or intramuscular injection is 60 – 90 minutes.

Figure 1: Recovery from Insulin Induced Hypoglycemia (mean blood glucose) After Intramuscular Injection of 1 mg GlucaGen in Type I Diabetic Men

Recovery from Insulin Induced Hypoglycemia - Illustration

For use as a diagnostic aid

Table 2 : Pharmacodynamic Properties of Glucagon

Route of Administration Dose* Time of Maximal Glucose Concentration Time of Onset of Action for GI Smooth Muscle Relaxation Duration of Smooth Muscle Relaxation1
IV 0.25-0.5 mg (0.25-0.5 units) 5-20 minutes 45 seconds 9-17 minutes
2 mg (2 units) 5-20 minutes 45 seconds 22-25 minutes
IM 1 mg (1 unit) 30 minutes 8-10 minutes 12-27 minutes
2 mg (2 units) 30 minutes 4-7 minutes 21-32 minutes
*The usual diagnostic dose for relaxation of the stomach, duodenal bulb, duodenum, and small bowel is 0.2 – 0 .5 mg given intravenously or 1 mg given intramuscularly; the usual dose to relax the colon is 0.5 – 0 .75 mg intravenously and 1 – 2 mg intramuscularly.
1Note: The time of maximal glucose concentration for GlucaGen administered subcutaneously is 30-45 minutes.

Pharmacokinetics

Intramuscular injection of 1 mg GlucaGen resulted in a mean Cmax (CV%) of 1686 pg/mL (43%) and median Tmax of 12.5 minutes. The mean apparent half-life of 45 minutes after intramuscular injection probably reflects prolonged absorption from the injection site. Glucagon is degraded in the liver, kidney, and plasma.

Last reviewed on RxList: 1/13/2012
This monograph has been modified to include the generic and brand name in many instances.

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