Oral Hypogylcaemic Drugs : Meglitinides (Benzoic acid derivatives) - i. Meglitinide ii. Repaglinide (Repide, Repa, Eurepa) iii. Nateglinide
Meglitinides (Benzoic acid derivatives)
The
meglitinides are similar in structure to sulphonylureas. The sulphonylurea and
meglitinide classes of oral
hypoglycaemic drugs are referred to as endogenous insulin secretagogues because
they induce the pancreatic release of endogenous insulin.
Mode of action: Even though, these are not sulphonylureas they
act on sulphonylurea receptors as well as the other variant receptors and
closes the ATP dependent k+ channels, leading to insulin secretion by
depolarization.
Synthesis
Synthesis
Properties and uses: Repaglinide is a white powder, practically
insoluble in water, soluble in methanol, and methylene chloride. It stimulates
insulin release and is used in the treatment of diabetes mellitus.
Assay: Dissolve the sample in methanol and add anhydrous acetic acid
and titrate against 0.1 M perchloric acid. Determine the end point
potentiometrically
Dose: The usual initial dose for adults is 0.5 mg, taken within 30 min
of main meals. Initial doses of 1 or 2 mg may be used in patients who have had
previous hypoglycaemic treatment. Dose may be adjusted at intervals of 1–2 week
up to 4 mg before meals; maximum dose is 16 mg daily.
Metabolism: It is metabolized in the liver and 16% is excreted in the urine
unchanged. The major metabolites are hydroxyl derivative (CYP2C9 70%, CYP3A4
30%) that are further conjugated to the glucuronide derivative (Fig 1.1).
Uses: It is used as an oral hypoglycaemic agent in type II diabetic
mellitus.
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