Glaritus Mechanism of Action

Pharmacology: Mechanism of Action: The primary activity of insulin, including insulin glargine, is regulation of glucose metabolism. Insulin and its analogs lower blood glucose by stimulating peripheral glucose uptake, especially by skeletal muscle and fat, and by inhibiting hepatic glucose production. Insulin inhibits lipolysis and proteolysis, and enhances protein synthesis.
Pharmacodynamics: The glucose-lowering effect on a molar basis (i.e., when given at the same doses) of intravenous insulin glargine is approximately the same as that for human insulin. Insulin Glargine differs because of its unique structure providing a smooth and peakless profile with a prolonged duration of action of 24 hours (end of observation period) compared to 14.5 hours for NPH human Insulin. The onset of action of Insulin Glargine is slower than NPH human Insulin.
The duration of action of insulin glargine after abdominal, deltoid, or thigh subcutaneous administration is reportedly similar. The time course of action of insulins, including Glaritus, may vary between individuals and within the same individual.
Comparative Pharmacodynamics of Glaritus with Lantus: Pharmacodynamics of insulin glargine from Glaritus was compared with that from Lantus in two separate studies - one in healthy volunteers (n=40 in two-way cross-over design) and second in patients of type 1 diabetes mellitus (n=111 in parallel group design) with successful achievement of bioequivalence of Glaritus to Lantus as displayed in the tables as follows. (See Tables 1 and 2.)


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Pharmacokinetics: Absorption and Bioavailability: After subcutaneous injection of Insulin Glargine, the Insulin serum concentrations indicate a slower, more prolonged absorption and a lack of a peak in comparison to NPH human Insulin. Concentrations are thus consistent with the time profile of the pharmacodynamics activity of Insulin Glargine.
Metabolism and Elimination: A reported metabolism study in humans indicates that insulin glargine is partly metabolized at the carboxyl terminus of the B chain in the subcutaneous depot to form two active metabolites with in vitro activity similar to that of human insulin, M1 (21A-Gly-insulin) and M2 (21A-Gly-des-30B-Thr-insulin). Unchanged drug and these degradation products are also present in the circulation.
Special Populations: Age, Race, and Gender: Effect of age, race, and gender on the pharmacokinetics of Glaritus has not been evaluated. However, in reported clinical studies in adults and pediatric patients, subgroup analyses based on age, race, and gender did not show differences in safety and efficacy between insulin glargine and NPH insulin.
Obesity: Effect of Body Mass Index (BMI) on the pharmacokinetics of Glaritus has not been evaluated.