ACTOS (pioglitazone hydrochloride) is an oral antidiabetic agent that acts
primarily by
decreasing insulin resistance. ACTOS is used in the management of type 2 diabetes mellitus
(also known as non-insulin-dependent diabetes mellitus [NIDDM] or adult-onset diabetes).
Pharmacological studies indicate that ACTOS improves sensitivity to insulin in
muscle and adipose tissue and inhibits hepatic gluconeogenesis. ACTOS improves glycemic
control while reducing circulating insulin levels.
Pioglitazone [(±)-5-[[4-[2-(5-ethyl-2-pyridinyl)ethoxy]phenyl]methyl]-2,4-]
thiazolidine- dione monohydrochloride belongs to a different chemical class
and has a different pharmacological action than the sulfonylureas, metformin,
or the a-glucosidase inhibi-
tors. The molecule contains one asymmetric carbon, and the compound is synthesized
and used as the racemic mixture. The two enantiomers of pioglitazone inter-convert in
vivo. No differences were found in the pharmacologic activity between the two
enan-
tiomers. The structural formula is as shown: Pioglitazone hydrochloride is
an odorless white crystalline powder that has a molecular formula of C19H20N2O3S•HCl
and a molecular weight of 392.90 daltons. It is soluble in N,N-dimethylformamide,
slightly soluble in anhydrous ethanol, very slightly soluble in acetone and
acetonitrile, practically insoluble in water, and insoluble in ether.
ACTOS is available as a tablet for oral administration containing 15 mg, 30
mg, or 45 mg of pioglitazone (as the base) formulated with the following excipients: lactose
monohy-
drate NF, hydroxypropylcellulose NF, carboxymethylcellulose calcium NF, and
magne-sium stearate NF.