Which of the following is false about pioglifazone?
Ans. d. It acts on insulin gene and even in absence of insulin helps in metabolism of carbohydrate Pioglitazone deceases insulin resistance in the muscles, adipose tissues and in the liver resulting in increased insulin dependent glucose disposal and decreased hepatic glucose output.*.Pioglitazone is an oral antihyperglycemic agent that acts primarily by decreasing insulin resistance. It deceases insulin resistance in the muscles, adipose tissues and in the liver resulting in increased insulin dependent glucose disposal and decreased hepatic glucose output "Pioglitazone* Pioglitazone belongs to Thiazolidinedione's.* Other drugs of this group are Troglitazone, Rosiglitazone.* It is an oral antihyperglycemic agent that acts primarily by decreasing insulin resistance* Pioglitazone deceases insulin resistance in the muscles, adipose tissues and in the liver resulting in increased insulin dependent glucose disposal and decreased hepatic glucose outputMechanism of action:* Pioglitazone is a potent and highly selective agonist for peroxisome proliferator activated receptor gamma (PPARg)* PPAR receptors are found in tissues important for insulin action such as adipose tissue, skeletal muscle and liver (highest level in adipose tissue).* Activation of (PPARg) nuclear receptors modulates the transcription of a number of insulin responsive genes involved in the control of glucose and lipid metabolism.* Pioglitazone appears to reduce insulin resistance by enhancing fatty acids storage and possibly by increasing adiponectin levels* Pioglitazone depends on the presence of insulin for its mechanism of action* Acts by enhancing the effect of circulating insulin it docs not lower blood glucose in persons that lack endogenous insulinMetabolism:* Extensively metabolized in liver by hydroxylation and oxidation* Multiple CYP isoforms are involved in the metabolism of pioglitazone (CYP2C8 and CYP3A4)* Liver function should be monitored in patients receiving thiazolidinediones even though pioglitazone and rosiglitazone rarely have been associated with hepatotoxicity.* Troglitazone was withdrawn from the market due to an increase incidence of drug induced hepatitis* The withdrawal of troglitazone has also led to concerns of other thiazolidinedione's also increasing the incidence of hepatitis and potential liver failure* FDA recommends 2-3 months checks of liver enzyme for the first year of thiazolidinedione therapy, to check for this rare but potentially catastrophic complication.* Till date newer thiazolidinedione's have been free of this problem* Thiazolidinedione's should not be used in patients with NYHA class III or IV failure.* Main side effect of all thiazolidinedione's is water retention leading to edema.* Sometimes there is significant water retention leading to decompensation of potentially previously unrecognized heart failure* Thiazolidinedione's should be prescribed with both caution and patient warnings about the potential for water retention/weight gain especially in patients with decreased ventricular function.
It PPARY g agonist
It is metabolized in liver
Not given in case of diastolic dysfunction
It acts on insulin gene and even in absence of insulin helps in metabolism of carbohydrate
Endocrinology