i. Sulphanilamide ii. Sulphacetamide (Albucid) iii. Sulphasalazine iv. Sulphadiazine v. Sulphadimidine vi. Sulphamerazine (Solumedine) vii. Sulphadimethoxine viii. Sulpha methoxy pyridazine ix. Sulphaphenazole x. Sulpha Isoxazole (Lipo Gantrisin, Gantrisin) xi. Sulphamethoxazole (Gantanol) xii. Sulphaguanidine
N-1 Substituted sulphonamides
Synthesis
Route-I. From: Benzene
Route-II. From: Nitrobenzene
Route-III. From: Aniline
Uses: It is used in veterinary medicine as an antibacterial agent.
Synthesis
Properties and uses: It exists as white crystalline powder, bitter in
taste. Used in the treatment of bacterial infections of urinary tract.
Assay: Dissolve the sample in water and hydrochloric acid. Titrate with
sodium nitrite and determine the end point potentiometrically.
Dose: Dose for eyes, as drops 10%, 15%, 20%, and 30%; in ointments
2.5% and 6% of Sulphacetamide.
Synthesis
Metabolism: It undergoes reductive metabolism by gut bacteria, converting
the drug into sulfapyridine and 5-amino salicylic acid, which are active
components.
Properties and uses: Sulphasalazine is a bright yellow or brownish-yellow
fine powder, very slightly soluble in alcohol, practically insoluble in
methylene chloride. It dissolves in dilute solutions of alkali hydroxides. It
is used in the treatment of ulcerative colitis.
Assay: Dissolve and dilute the sample in 0.1 M sodium hydroxide and add
0.1 M acetic acid and measure the absorbance at the maxima of 359 nm using
ultraviolet spectrophotometer.
Dosage forms: Sulphasalazine tablets B.P.
Step-I. Preparation of formyl acetic acid
Step II. Synthesis of 2-Aminopyrimidine
Step III. Synthesis of p-acetamido
benzene sulphonyl chloride (PABS)
Step IV. Condensation of p-acetamido
benzene sulphonyl chloride with 2-aminopyrimidine
Properties and uses: Sulphadiazine is a white or yellowish-white or
pinkish-white crystalline powder or crystals, insoluble in water, slightly
soluble in acetone, very slightly soluble in alcohol, and soluble in solutions
of alkali hydroxides and in dilute mineral acids. It is used in the treatment
of canceroids and rheumatic fever.
Assay: Dissolve the sample in water and hydrochloric acid. Titrate the
mixture with sodium nitrite and determine the end point potentiometrically.
Dose: Usual dose is 2–8 g per day
Dosage forms: Sulphadiazine tablets I.P., Sulphadiazine injection B.P.
Synthesis
Properties and uses: It exists as white crystalline powder with a
bitter taste, insoluble in water, and sparingly soluble in alcohol. It is less
effective in meningeal infection because of its poor penetration into the
cerebrospinal fluid.
Dose: Dose is 3 g initially and subsequent doses up to 6 g per day in
divided doses.
Step I. Preparation of PABS
Synthesized
as mentioned under Sulphadiazine
Step II. Preparation of 2-amino-4-methyl pyrimidine
Step III. Condensation of products of Step I and II
Uses: Used as an antibacterial agent.
Dose: Dose is 4 g initially, and subsequent dose is 1 g every 6 h
Synthesis
Synthesis
Synthesis
Synthesis
Properties and uses: It exists as white to slightly yellowish
crystalline powder and is odourless, soluble in water and in dilute
hydrochloric acid. Used in the treatment of urinary tract infections.
Assay: Dissolve the sample in water and hydrochloric acid. Titrate the
mixture with sodium nitrite and determine the end point potentiometrically.
Dose: Initial dose is 2–4 g orally for adults and maintenance dose is
4–8 g per day in divided doses.
Synthesis
Properties and uses: Sulphamethoxazole is a white or almost white
crystalline powder, practically insoluble in water, soluble in acetone,
sparingly soluble in ethanol, dissolves in dilute solutions of sodium hydroxide
and in dilute acids. Used in the treatment of bacterial infections.
Assay: Dissolve the sample in dilute hydrochloric acid and add
potassium bromide. Cool in ice and titrate against 0.1N Sodium nitrate.
Determine the end point electrometrically.
Dose: Orally 2 g followed by 1 g every 8 h.
Dosage forms: Co-trimoxazole intravenous infusion B.P., Co-trimoxazole oral
suspension B.P., Paediatric co-trimoxazole oral suspension B.P., Co-trimoxazole
tablets B.P., Dispersible co-trimoxazole tablets B.P., Paediatric
co-trimoxazole tablets B.P.
Properties and uses: Sulphaguanidine is a white, fine crystalline
powder, soluble in dilute mineral acids, very slightly soluble in water and
ethanol, slightly soluble in acetone, but insoluble in methylene chloride. Used
in the treatment of local intestinal infections, specifically, bacillary
dysentery.
Assay: Dissolve the sample in dilute hydrochloric acid and add
potassium bromide. Cool in ice and titrate against 0.1N sodium nitrate.
Determine the end point electrometrically.
Synthesis
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