MEDICINAL CHEMISTRY

Official Drug:
Clofibrate, B.P., I.P. Ethyl 2-(4-chlorophenoxy)-2-methylpropionate. It may be prepared
by refluxing p-chlorophenol, acetone and chloroform in presence of alkali, processing,
and esterification of the carboxylic acid. Clofibrate is a clear, colourless to pale-yellow
liquid, which is practically insoluble in water. Clofibrate is readily absorbed
from gastrointestinal tract and is rapidly hydrolysed to active metabolite
chlorophenoxyisobutyric acid (clofibric acid). Clofibrate is used, in conjunction with
dietary modification, in the treatment of type III hyperlipoproteinaemia and severe
hypertriglyceridaemia. The dosage is up to 2 g daily, in divided doses. It is no more
used for long-term prophylaxis of ischaemic heart disease since such use is associated
with serious toxicity.
Preparation: Clofibrate Capsules, B.P., I.P.Proprietary Name: ATROMID-S
8. Hypoglycemic Agents
Introduction
Hypoglycemic agents are those, which are used to lower the blood sugar and are used to
treat the symptoms of diabetes mellitus. There are three peptide hormones secreted by the
pancreas play a major role in the regulation of metabolism of carbohydrates, lipids &
amino acids. These are insulating glucagons & somatostatin.
The normal blood glucose level in human’s ranges between 70 - 90 mg per
100ml. Hyperglycemia is characterized by more than normal concentration of the blood
sugar and hypoglycemia develops when the blood sugar level falls below the normal
range. Diabetes mellitus is the condition arising due to abnormal metabolism of
carbohydrates, fats and proteins. It is charactererized mainly by an unusually high sugar
level in the blood (hyperglycemia) and the presence of sugar in the urine
(glucosuria). The ancient Greek and Roman physicians used the term Diabetes to mean
large urine volume. The adjective melitus, a Latin word (meaning, honey). The large
urine volume is due to the large amounts of glucose and urea in the urine (osmotic
diuresis). Because the biochemical basis of diabetes is still not clear, the disease is
usually defined by its symptoms. These include, hyperglycemia, hyperlipemia,
glucosuria, polyuria (loss of water and salts), polydipsia (increase in thirst), polyphagia
(excessive hunger), ketonemia (ketone bodies and fatty acids in the blood), ketonuria
(ketone bodies In the urine), azoturia (increased production and excretion of ammonia),
poor wound healing and infection. Sometimes, the disease eventually causes serious
complications. like, kidney damage degeneration, premature atheroscier ( heart disease,
neuro-logical dysfunction a predisposition to gangrene.
Types of Diabetes:
Under current clinical terms, diabetes mellitus can be categorised as under :
(i) Insulin - dependent, type I (IDDM or juvenile or brittle or unstable diabetes),
(ii) Non-insulin dependent type, type II (NIDDM or adult onset or maturity onset
diabetes)