MEDICINAL CHEMISTRY

CH3COOC2H5 Diazoxide (90)
Cl
NH 2
Sn/HCL; Reduction
SO 2Cl 2
2-Amino-5-chlorobenzene
sulphonamide (96)
Cl
5-Chloro-2-nitrobenzene
sulphonamide (95)
NO 2
SO 2NH 2
Official drugs:
Diazoxide, B.P. 7-Chloro-3-methyl-2H-1, 2, 4- benzothiadiazine 1,1-dioxide. It is a
white or almost white, crystalline powder; practically insoluble in water. Diazoxide is
readily absorbed from the gastrointestinal tract. About 20 to 25% of the drug is
eliminated as such by the kidney, and the remaining is metabolized in the liver to the
3- hydroxy methyl and 3-carboxy derivatives. Diazoxide is given intravenously for the
treatment of hypertensive emergencies. The parenteral dose is 1 to 3 mg per kg body
weight within 30 seconds, up to a maximum of 150 mg and repeated after 5 to 15
minutes, if required. Diazoxide is given by mouth in the treatment of intractable
hypoglycemia. The initial dose is 5 mg per kg daily in 2-3 divided doses.
Preparations: Diazoxide Injection, B.P. Diazoxide Tablets, B.P.Proprietary Names:
EUDEMINE; HYPERSTAT I.V.
C (2) Calcium Channel Blockers
H 3 CO
H 3CO
S
N
CH 2 O
H2C N CH3 Diltiazem (11)
CH 3
OCH 3
O-C-CH 3
O
H 3C
CH
(CH2 ) 2-N-(CH2 ) 3 C OCH3 CH 3
Verapamil (10)
CN
CH 3
H 3CO 2C
CH 3
N
H
OCH 3
NO 2
CO 2CH 3
CH 3
Nifedipine (12)