MEDICINAL CHEMISTRY

Official Drugs:
Insulin, B.P. It is the natural antidiabetic hormone obtained from the pancreas
of either the pig or the ox and purified. Insulin is a white or almost white
powder; practically insoluble in water. When thawed, insulin should be stored at a
temperature of 2° to 8° and used for the manufacture of preparations within a short
period of time.
Glibenclamide,B.P., I.P. Glybenclamide; Glyburide. 1-(4-[2-(5-Chloro-2-methoxybenzamido)ethyl]benzenesulphonyl)-3-cyclohexyl-urea.
It is a white or almost white
crystalline powder; practically insoluble in water. Glibenclamide has a half-life
of about 10 hours. It is metabolised almost completely in the liver. Glibenclamide
has a duration of action of up to 24 hours. The dose of glibenclamide is 2.5 to 20 mg
once daily, after food.
Preparation: Glibenclamide Tablets, B.P., I.P. Proprietary Names: DAONIL; DIA BETA;
EUGLUCON; MICRONASE
GlipizideB.P.I-Cyclohexyl-3-(4-[2-(5-methy1pyrazine-2-carboxamido)ethyl]benzene
sulphonyl)urea. Glipizide is a white or almost white crystalline powder; practically
insoluble in water. Glipizide has a half-life of approximately 3 to 4 hours. Its
hypoglycaemic effect may persist for up to 24 hours. The usual dose of
glipizide is 2.5 to 5 mg daily given as a single dose 15 to 30 minutes before breakfast.
Preparation: Glipizide Tablets, B.P.Proprietary Names: GLIBENESE; GLUCOTROL;
MINODIAB
Phenformin Hydrochloride I.P. 1-Phenethylbiguanide hydrochloride. It is a white or
almost white crystalline powder; freely soluble in water. Phenformin is not
recommended for patients with renal failure and in patients with severe hepatic and
cardiovascular disease because it causes lactic acidosis. The usual dose of phenformin
hydrochloride by is 50 to 200 mg daily, in divided doses.
Preparation: Phenformin Tablets, B.P.Proprietary Name: DBI
Metformin Hydrochloride, B.P., I.P. 1, 1- Dimethylbiguanide. It is a white
crystalline powder; hygroscopic. It is freely soluble in water. It is stored in
tightly closed containers. Metformin is only partially absorbed from the
gastrointestinal tract. It has a half-life of 1.5 to 3 hours, and is eliminated entirely
by renal excretion. It should not be used in renal failure patients. The dose of
metformin hydrochloride is 0.5 to 2 g daily, in divided doses.
Preparation: Metformin Tablets, B.P., I.P.Proprietary Names: GLUCOPHAGE;
GLYCIPHAGE; ORABET
Suggested Readings
1. M. E. Wolf. Burger's Medicinal Chemistry, 6 th edition, John Wiley and Sons, New York, 2003
2. J. N. Delgado and W. A. Remers, Wilson & Gisvold's: Textbook of Organic Medicinal and
Pharmaceutical Chemistry, Tenth edition, Lippincott Raven Publishers, Philadelphia, New York 1998.