Actions of Zenoglim M2 in details
Pharmacology: Zenoglim M2 combines Glimepiride (Zenoglim M2), an oral hypoglycaemic drug and Metformin (Zenoglim M2), an antihyperglycaemic drug, giving a synergistic effect for the management of non-insulin dependent diabetes mellitus (NIDDM).
Mechanism of Action: Glimepiride (Zenoglim M2), a sulphonylurea, lowers blood glucose by augmenting the release of insulin from the pancreas, an effect dependent upon functioning β cells in the pancreatic islets. When administered chronically, the blood glucose lowering effects persists despite a gradual decline in the insulin secretory response to Glimepiride (Zenoglim M2). Extra pancreatic effects may be involved in the mechanism of action of sulphonylureas.
Metformin (Zenoglim M2) decreases hepatic glucose production, decreases intestinal absorption of glucose and improves insulin sensitivity by increasing peripheral glucose uptake and utilisation. It lowers both basal and postprandial plasma glucose.
Pharmacokinetics: After oral administration, Glimepiride (Zenoglim M2) is completely (100%) absorbed from the GI tract. Significant absorption occurs within 1 hr of administration and peak drug levels at 2-3 hrs. Protein binding is reported to be >99.5%. It is completely metabolised by oxidative biotransformation with 60% of the excretion via urine and the remaining via faeces.
Following a single oral dose of Metformin (Zenoglim M2) hydrochloride extended-release, Cmax is achieved with a median value of 7 hrs and a range of 4-8 hrs. Metformin (Zenoglim M2) has an absolute oral bioavailability of 50-60%. Higher oral doses are proportionately less bioavailable than lower doses (observed in doses of 0.5-1.5 g). When given with food, AUC increased by 50% from the extended-release Metformin (Zenoglim M2) tablet but there was no effect of food on Cmax and Tmax of Metformin (Zenoglim M2). Following absorption, Metformin (Zenoglim M2) is rapidly distributed and does not bind to plasma proteins. Metformin (Zenoglim M2) undergoes renal excretion and has plasma elimination half-life of 6.2 hrs after oral administration.
In patients with decreased renal function, the plasma and blood half-life of Metformin (Zenoglim M2) is prolonged and the renal clearance is decreased in proportion to the decrease in creatinine clearance.
References
- DailyMed. "GLIMEPIRIDE; PIOGLITAZONE HYDROCHLORIDE: DailyMed provides trustworthy information about marketed drugs in the United States. DailyMed is the official provider of FDA label information (package inserts).". https://dailymed.nlm.nih.gov/dailyme... (accessed September 17, 2018).
- NCIt. "Metformin: NCI Thesaurus (NCIt) provides reference terminology for many systems. It covers vocabulary for clinical care, translational and basic research, and public information and administrative activities.". https://ncit.nci.nih.gov/ncitbrowser... (accessed September 17, 2018).
- NCIt. "Glimepiride: NCI Thesaurus (NCIt) provides reference terminology for many systems. It covers vocabulary for clinical care, translational and basic research, and public information and administrative activities.". https://ncit.nci.nih.gov/ncitbrowser... (accessed September 17, 2018).
Reviews
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Information checked by Dr. Sachin Kumar, MD Pharmacology
