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Chapter: Medicinal Chemistry : Oral Hypogylcaemic Drugs

Oral Hypogylcaemic Drugs : Thiazolidinediones - i. Pioglitazone ii. Ciglitazone iii. Rosiglitazone (Rosicon, Reglit, Rosinorm) iv. α-Glucosidase inhibitors



Thiazolidinediones are a new class of oral antidiabetic agents (commercially known as glitazones) that enhance insulin sensitivity in peripheral tissues. It is relatively safe in patients with impaired renal function because they are highly metabolized by the liver and excreted in the faeces.

Mode of action: These drugs produce gene-mediated transcription for the release of insulin by forming new proteins. They act on the nuclear peroxisome proliferator activated receptor γ (ppar γ) and elicit the genes. It also inhibits the resistance to insulin by activating glucose transporters (Glut and Glut 1) in the plasma membrane.


i. Pioglitazone

Metabolism: It is metabolized and gives eight metabolic products. These products result from oxidation at either carbon adjacent to the pyridine ring. They are found as various conjugates in the urine and bile. Three metabolites appear to contribute to the biological activity of pioglitazone (Fig 1.2).


ii. Ciglitazone


Use: It is used in the treatment of NIDDM.


iii. Rosiglitazone (Rosicon, Reglit, Rosinorm)


Metabolism: The primary metabolites consist of sulphate and glucuronic acid conjugates of hydroxylation and N-demethylation product. These metabolites contribute to the biological activity of rosiglitazone (Fig 1.3).

Uses: It is used in the treatment of NIDDM.

Dose: The dosage for type 2 diabetes mellitus for adult is 4 mg daily, which may be increased after 8–12 week of therapy, according to response and the maximum dosage is 8 mg daily.

iv. α-Glucosidase inhibitors

α-Glucosidase enzyme is responsible for breaking down the complex polysaccharides and sucrose to monosaccharides, which are then absorbed; α-glucosidase inhibitors decrease the rate of breakdown. They are also called starch blockers.

Mode of action: These acts on the final enzymes in the digestion of carbohydrates present in the brush border of small intestine and transport of polysaccharides and sucrose.

Properties and uses: Acarbose is a white or yellowish amorphous hygroscopic powder, very soluble in water, soluble in methanol, and practically insoluble in methylene chloride. It is an alpha-glucosidase inhibitor and used in the treatment of diabetes mellitus.

Assay: It is assayed by adopting liquid chromatography technique.

i. Acarbose

ii. Miglitol

Properties and uses: It is a crystalline substance, soluble in water. It is a α-glucosidase inhibitor and used as an antidiabetic agent.

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