Topically used sulphonamides

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Chapter: Medicinal Chemistry : Antibacterial Sulphonamides

Antibacterial Sulphonamides : Topically used sulphonamides : i. Mafenide (Sulfamylon) ii. Silver Sulphadiazine iii. Dapsone (Avcosulfon) iv. Solapsone


Antibacterial Sulphonamides - Synthesis and Drug Profile

Miscellaneous

a. Topically used sulphonamides

 

i. Mafenide (Sulfamylon)


Uses: It is used in the treatment and cure of gas gangrene. It is also effective against Clostridium welchii on topical application.

Dose: Dose is 5% solution of mafenide hydrochloride or mafenide propionate for topical use.

Synthesis


 

ii. Silver Sulphadiazine


Uses: It is an effective topical antimicrobial agent, especially, against Pseudomonas species; it finds extensive use in burn therapy.

 

iii. Dapsone (Avcosulfon)


Action and use: Dapsone is a white or slightly yellowish-white crystalline powder, very slightly soluble in water, soluble in acetone and dilute mineral acids, sparingly soluble in alcohol. Used as folic acid synthesis inhibitor in the treatment of leprosy and nocardiosis.

Assay: Dissolve the sample in dilute hydrochloric acid, add potassium bromide, cool in ice, and titrate against 0.1N sodium nitrate. Determine the end point electrometrically.

Dose: The dose as a leprostatic is 25 mg twice a week initially for 1 month followed by 25 mg per day each month. As suppressant for dermatitis herpetiformis the dose is 100–200 mg per day.

Dosage forms: Dapsone tablets B.P.

Synthesis


 

iv. Solapsone


Synthesis


Uses: It is used in the treatment of leprosy.

 

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