Product Information
Registration Status: ActiveAMARYL 3.0 TABLET 3mg is approved to be sold in Singapore with effective from 1998-11-20. It is marketed by SANOFI-AVENTIS SINGAPORE PTE LTD, with the registration number of SIN10462P.
This product contains Glimepiride 3mg in the form of TABLET. It is approved for ORAL use.
This product is manufactured by SANOFI-AVENTIS S.P.A. in ITALY.
It is a Prescription Only Medicine that can only be obtained from a doctor or a dentist, or a pharmacist with a prescription from a Singapore-registered doctor or dentist.
Description
Glimepiride is the first III generation sulphonyl urea it is a very potent sulphonyl urea with long duration of action.
Indication
For concomitant use with insulin for the treatment of noninsulin-dependent (type 2) diabetes mellitus.
Mechanism of Action
The mechanism of action of glimepiride in lowering blood glucose appears to be dependent on stimulating the release of insulin from functioning pancreatic beta cells, and increasing sensitivity of peripheral tissues to insulin. Glimepiride likely binds to ATP-sensitive potassium channel receptors on the pancreatic cell surface, reducing potassium conductance and causing depolarization of the membrane. Membrane depolarization stimulates calcium ion influx through voltage-sensitive calcium channels. This increase in intracellular calcium ion concentration induces the secretion of insulin.
Pharmacokinetics
- Absorption
- Completely (100%) absorbed following oral administration.
- Distribution
- * 21.8 ± 13.9 L [Volunteers] * 19.8 ± 12.7 L [Patients with Type 2 diabetes, Single Dose] * 37.1 ± 18.2 L [Patients with Type 2 diabetes, Multiple Dose]
- Metabolism
- Hepatic. Following either an intravenous or oral dose, glimepiride is completely metabolized by oxidative biotransformation to a major metabolite, cyclohexyl hydroxymethyl derivative (M1), via the hepatic cytochrome P450 II C9 subsystem. M1 is further metabolized to the carboxyl derivative (M2) by one or several cytosolic enzymes. M1, but not M2, possessed approximately one third of the pharmacologic activity of its parent in an animal model. However, whether the glucose-lowering effect of M1 is clinically significant is not clear.
- Elimination
Clearance
* 52.1 +/- 16.0 mL/min [Normal subjects with single oral dose] * 48.5 +/- 29.3 mL/min [Patients with Type 2 diabetes, with single oral dose] * 52.7 +/- 40.3 mL/min [Patients with Type 2 diabetes, with multiple oral dose] * 47.8 mL/min [healthy after intravenous (IV) dosing]
Toxicity
Severe hypoglycemic reactions with coma, seizure, or other neurological impairment.
Active Ingredient/Synonyms
Glimepirida | Glimépiride | Glimepiridum | Glimepiride |
Source of information: Drugbank (External Link). Last updated on: 3rd July 18. *Trade Name used in the content below may not be the same as the HSA-registered product.