COMPOSITION : Each tablet contains:-
Pioglitazone belongs to class of thiazolidinedione. Pioglitazone decreases insulin resistance in the periphery and in the liver that helps the body make better use of insulin it produces and also decreases the glucose output from
Following oral administration, pioglitazone is rapidly absorbed, and peak plasma concentrations of unchanged pioglitazone are usually achieved 2 hours after administration. Proportional increases of the plasma concentration were observed for doses from 2 – 60 mg. Steady state is achieved after 4–7 days of dosing. Repeated dosing does not result in accumulation of the compound or metabolites. Absorption is not influenced by food intake. Absolute bioavailability is greater than 80 %.
The estimated volume of distribution in humans is 0.25 l/kg. Pioglitazone and all active metabolites are extensively bound to plasma protein (> 99 %).
Pioglitazone undergoes extensive hepatic metabolism by hydroxylation of aliphatic methylene groups. This is predominantly via cytochrome P450 2C8 although other isoforms may be involved to a lesser degree. Three of the six identified metabolites are active (M-II, M-III, and M-IV).When activity, concentrations and protein binding are taken into account, pioglitazone and metabolite M-III contribute equally to efficacy. On this basis M-IV contribution to efficacy is approximately three-fold that of pioglitazone, whilst the relative efficacy of M-II is minimal.In vitro studies have shown no evidence that pioglitazone inhibits any subtype of cytochrome P450. There is noinduction of the main inducible P450 isoenzymes 1A, 2C8/9, and 3A4 in man. Interaction studies have shown that pioglitazone has no relevant effect on either the pharmacokinetics or pharmacodynamics of digoxin, warfarin, phenprocoumon and metformin. Concomitant administration of pioglitazone with gemfibrozil (an inhibitor of cytochrome P450 2C8) or with rifampicin (an inducer of cytochrome P450 2C8) is reported to increase or decrease, respectively, the plasma concentration of pioglitazone.
Following oral administration of radiolabelled pioglitazone to man, recovered label was mainly in faeces (55%) and a lesser amount in urine (45%). In animals, only a small amount of unchanged pioglitazone can be detected in either urine or faeces. The mean plasma elimination half-life of unchanged pioglitazone in man is 5 to 6 hours and for its total active metabolites 16 to 23 hours.
INDICATION : Type 2 diabetes mellitus.
DOSAGE : As directed by the physician
SIDE EFFECTS : Bone fracture, Sinuses, Bladder cancer, Visual disturbance, Impaired liver cell function, Infection of nose, Decreased sensitivity to stimulation, Weight gain, Inability to sleep, Pharynx or larynx