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VOGLOYD -3D
Composition Voglibose 0.3/0.2 mg + Glimepiride 1/ 2 mg + Metformin 500 mg SR bilayer tablet
Indication Type 2 diabetes mellitus
Mechanism of Action

Voglibose: has general properties similar to acarbose and selectively inhibits α-glucosidase in the enteric canal, delaying the digestion and absorption of carbohydrate, thereby suppressing sharp increase in post-prandial plasma glucose.

Glimepiride stimulates the insulin release from functioning pancreatic β-cells and inhibits gluconeogenesis at hepatic cells. It also increases insulin sensitivity at peripheral target sites. Metformin decreases hepatic gluconeogenesis, decreases intestinal absorption of glucose and improves insulin sensitivity (increases peripheral glucose uptake and utilisation).

Pharmacokinetic's

Voglibose:

Absorption: voglibose is poorly absorbed after oral administration. However, systematic adverse effects have been observed.

Metabolism: the metabolism of voglibose in liver is negligible.

Excretion: The renal excretion is negligible and plasma concentations after oral dose have been undetectable.

Metformin: Absorption: Slowly and incompletely absorbed from the GI tract. Absolute bioavailability: Approx 50-60% (fasting); reduced if taken w/ food. Time to peak plasma concentration: 2-3 hr (immediate-release); 4-8 hr (extended-release).

Distribution: It crosses the placenta and distributed in breast milk (small amounts). Volume of distribution: 654 ± 358 L. Plasma protein binding: Negligible.

Metabolism: Not metabolised.

Excretion: Via urine (90% as unchanged drug). Elimination half-life: Approx 2-6 hr.

Glimepiride: Duration: 24 hr.

Absorption: Completely absorbed from the GI tract. Time to peak plasma concentration: 2-3 hr.

Distribution: Volume of distribution: 8.8 L. Plasma protein binding: >99.5%.

Metabolism: Extensively metabolised in the liver via oxidation by CYP2C9 isoenzyme to 2 main metabolites.

Excretion: Via urine (approx 60%) and faeces (40%). Half-life: Approx 9 hr.

Side effects

Voglibose: Flatulence; abdominal distension; diarrhoea; pain; skin reactions; hypoglycemia; increased LFT. Potentially Fatal: Hepatotoxicity. Diarrhoea, vomiting, metallic taste, rash, isolated transaminase elevations, cholestatic jaundice, allergic skin reactions, photosensitivity reactions, leukopaenia, agranulocytosis, thrombocytopaenia, haemolytic anaemia, aplastic anaemia, pancytopaenia, blurred vision. Potentially Fatal: Lactic acidosis.

Precaution

Voglibose: History of laparotomy or ileus. Roemheld's syndrome, stenosis, severe hepatic or renal impairment. Child <18 yr; elderly. Monitor LFT. Treat hypoglycaemic episodes with glucose (not with sucrose). Renal and hepatic impairment. Avoid alcohol consumption. Hypoglycaemic episodes.

Dosage

Adult: Take as directed. Titrate according to response.