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1. FRUSEMIDE (Furosemide):, Imp, Chemistry :, It is sulphamyl benzoic acid derivative or anthranilic acid derivative. It is a high, ceiling diuretic (loop diuretic)., CH, H-N-CH2, H-N-S, 1C-OH, It contains furan heterocycle. It is anthranilic acid derivative in which:, (i), Chloro group is present at 4 position., (ii) Sulphamoyl (sulphanomido) group at 5 position., (iii) N-furfuryl group on aromatic amino group provides a very high degree of, diuretic activity., (iv) The presence of carboxyl group makes the compound sufficiently stronger, acid. The basic nitrogen group accepts proton from -COOH group to give ion, pair which is a lipophilic, absorbable form of frusemide. Thus, it is absorbed, at pH 5 to 8 through intestine when given orally., Chemical name :, 4-chloro, N-furfuryl, 5-sulphamoyl anthranilic acid., Or, 4-chloro, 2-furfurylamino, 5-sulphamoyl benzoic acid., Properties :, It is a white crystalline powder, odourless and tasteless. It is very slightly soluble, in water but soluble in solutions of alkali hydroxide., Chemical properties:, When its alcoholic solution is treated with dimethyl amino benzaldehyde solution,, it first gives green colour which changes to deep red., Scanned by TapScanner, HIN
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12.3, Diuretics, concise Organic Pharmaceutical Chemistry-II, Stability and storage:, u Is stable in air but is affected by light. Hence, it is stored in well-closed, ight-resistant containers., Uses:, It is used, (i) As a diuretic., C) To treat oedema associated with congestive heart failure, cirrhosis of liver, Sew elling, and renal diseases., liver, Laurage, (iii) For management of hypertension., Pharmaceutical formulations:, (i) Frusemide injection., (ii) Frusemide tablets., HzN, o-s, Brand names : Lasix, Salurex., 6-chloro,tati, ,214 6en26円, 2 CHLOROTHIAZIDE, Chemistry:, It is 1, 2, 4-benzothiadiazine (thiazide or benzothiazide) derivative. It is Tow, ceiling diuretic. Chemically, it differs from hydrochlorthiazide in having double bond, between 3 and 4 positions., Properties :, It occurs as white crystalline powder which is odourless and has a bitter taste., It is very slightly soluble in water. It is stored in well-closed containers., Uses :, As given under frusemide. It is also used to prevent renal stone formation (as it, reduces excretion of calcium in urine)., Pharmaceutical formulations : It is available in the form of tablets., Brand name : Saluric., 3. HYDROCHLORTHIAZIDE :, Chemistry:, It is thiazide (1, 2, 4-benzothiadiazine) derivative in which the positions 2, 3 and, * are saturated. Benzothiadiazine is a fused ring system in wiich benzene ring Is, Tused at 5, 6-positions of thiadiazine heterocycle., Scanned by TapScanner, C/
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12.4, Diuretics, Since, the positions of sulphur and two nitrogen atoms in the ring areete, 4 respectively and the position 2 is saturated, it is called as 2H, Concise Organic Pharmaceutical Chemistry -I, 1,, It contains chloro group at 6 position, sulphamoyl group at 7 position., 4., saturat la, S., N-H, S 2, 2H-1, 2, 4–bepzothiadiaze, H., 2H-1, 2, 4-thiadiazine, N', C 6, 7., N-H, NH2, 8 A, O., Covalent-2Hy, bond, Hydrochlorthiazide, Chemical name :, ator, 6-chloro, 3, 4,-dihydro, 7-sulphamoyl, 2H - 1, 2, 4-benzothiadiazine, 1-dioxide., (Properties, stability, storage, uses and pharmaceutical formulations are as, Chlorothiazide.), Brand names : Biduret, Esidrex., 4. BENZTHIAZIDE, H2 N, Chemistry:, It is a thiazide derivative and chemically differs from hydrochlorothia:, having :, (i) Double bond between 3 and 4 positions., (ii) Benzylthiomethyl group at 3 position., Properties :, It occurs as fine, white crystalline powder having characteristic taste, practically insoluble in water. It is not affected by light and air. It is stored, closed containers., Uses and pharmaceutical formulations:, (As under chlorothiazide.), Brand names : Exna, Aquatag., Scanned by TapScanner
