Glucagon for Injection - Scientific Information
|Manufacture:||Fresenius Kabi USA, LLC|
|Condition:||Diagnosis and Investigation, Hypoglycemia|
|Class:||Glucose elevating agents|
|Form:||Liquid solution, Intramuscular (IM), Intravenous (IV)|
|Ingredients:||Glucagon hydrochloride, lactose monohydrate, hydrochloric acid, sodium hydroxide.|
Glucagon for Injection, for intravenous or intramuscular use, is a gastrointestinal motility inhibitor that is produced by solid phase peptide synthesis. Glucagon is a singlechain polypeptide containing 29 amino acid residues. The chemical structure of the glucagon polypeptide is identical to human glucagon and to glucagon extracted from beef and pork pancreas. The structure of glucagon is:
Glucagon for Injection is a sterile, lyophilized white powder in a 3 mL vial. The reconstituted solution contains 1 mg of glucagon as hydrochloride per mL and lactose monohydrate (107 mg). Glucagon for Injection is supplied at pH 2.5 to 3.5 and is soluble in water.
Mechanism of Action
Extra hepatic effects of glucagon include relaxation of the smooth muscle of the stomach, small bowel, and colon.
Table 3 displays the pharmacodynamics properties of Glucagon for Injection as a diagnostic aid during radiologic examination.
|Route of |
|Dosea||Time of Onset of Action for GI |
Smooth Muscle Relaxation
|Duration of Smooth |
|Intravenous||0.25 to |
|45 seconds||9 to 17 minutes|
|Intramuscular||1 mg||8 to 10 minutes||12 to 27 minutes|
|2 mg||4 to 7 minutes||21 to 32 minutes|
a Select from these doses based on type of diagnostic procedure, route of administration and procedure duration.
Following intramuscular administration of 1 mg dose, the maximum plasma glucagon concentrations of 3391 pg/mL were attained approximately 10 minutes after dosing.
The mean apparent halflife of glucagon was 26 minutes after intramuscular administration.
Glucagon is degraded in the liver, kidney, and plasma.
Carcinogenesis, Mutagenesis, Impairment of Fertility
Long term studies in animals to evaluate carcinogenic potential have not been performed.
Synthetic glucagon was negative in the bacterial reverse mutation assay (Ames test). The clastogenic potential of synthetic glucagon in the Chinese Hamster Ovary (CHO) assay was positive in the absence of metabolic activation. Doses of 100 and 200 mg/kg of glucagon of both pancreatic and recombinant origins gave slightly higher incidences of micronucleus formation in male mice but there was no effect in females. The weight of evidence indicates that synthetic and recombinant glucagon are not different and do not pose a genotoxic risk to humans.
Impairment of Fertility
Glucagon (rDNA and synthetic origin) was not tested in animal fertility studies. Studies in rats have shown that pancreatic glucagon does not cause impaired fertility.