Topic (70) Sulphonamides = SAR, Uses and Adverse Effects | Sulphonamides Antibiotics | B.Pharma

Download the "Solution Pharmacy" Mobile App to Get All Uploaded Notes, Model Question Papers, Answer Papers, Online Tests and other GPAT Materials - https://play.google.com/store/apps/details?id=co.bolton.nqilv

Contents for Unit 04 of Medicinal Chemistry 03

Antifungal agents:
Antifungal antibiotics: Amphotericin-B, Nystatin, Natamycin, Griseofulvin.
Synthetic Antifungal agents: Clotrimazole, Econazole, Butoconazole, Oxiconazole Tioconozole, Miconazole*, Ketoconazole, Terconazole, Itraconazole, Fluconazole, Naftifine hydrochloride,
Tolnaftate*.
Anti-protozoal Agents: Metronidazole*, Tinidazole, Ornidazole, Diloxanide,Iodoquinol, Pentamidine Isethionate, Atovaquone, Eflornithine.
Anthelmintics: Diethylcarbamazine citrate*, Thiabendazole, Mebendazole*, Albendazole, Niclosamide, Oxamniquine, Praziquantel, Ivermectin.

Sulphonamides and Sulfones
Historical development, chemistry, classification and SAR of Sulfonamides: Sulphamethizole, Sulfisoxazole, Sulphamethizine, Sulfacetamide*, Sulphapyridine, Sulfamethoxazole*, Sulphadiazine, Mefenide acetate, Sulfasalazine.

Folate reductase inhibitors: Trimethoprim*, Cotrimoxazole.
Sulfones: Dapsone*.

Sulfonamide
One of the oldest antibacterial agents used to combat infection. Used for coccal infection in 1935
They are bacteriostatic because it inhibits bacterial synthesis of folic acid. Clinical usefulness has decreased because of the effectiveness of other antibiotics and penicillin

Mechanism of action
1. Competitive inhibitor to dihydropteroate synthase enzyme due to resemblance with para-amino benzoic acid.
2. Sulfonamides therefore are reversible inhibitors of folic acid synthesis and bacteriostatic not
bactericidal.
3. Inhibit bacterial growth without affecting normal cells
Antibacterial activity
Gram-positive and gram negative. Nocardia, chlamydia trachomatis, some protozoa.

Chemical modification of the sulphonamide structure has given rise to several important group of drugs.
➢Gloucoma – Acetazolamide
➢Diuretic – Thiazides
➢Anti-mycobacterial – Sulphones
➢Oral hypoglycemic – Sulphonyl ureas
Classification
A. Sulphonamides employed for treatment of systemic infection. Depending upon duration , they
can be further subdivided into
a) Short to intermediate acting sulphonamides: Sulphamethoxazole, Sulphadiazine, Slpfisoxazole
Sulphaphenazole
b. Long acting sulphonamides: Sulphamethoxypyridazine, Sulphadimethoxine
c. Extra long-acting sulphonamides: Sulphasalazine, Sulphadiazine
d. Poorly absorbed sulphonamides: Sulphacetamid, Silver Sulphadiazin
e. Topically used sulphonamides: Sulphaguanidine, Succinyl Sulphathiazole

Structure-activity relationShipGeneral
1. Sulphonamide skeleton is the minimum structural requirement for antibacterial activity.
2. The active form of sulphonamide is the ionized form. Maximum activity is observed between the pka value 6.6-7.4.
3. Sulphonamides compete for binding sites on plasma albumin with causes increased action of drugs like Aspirin, Phenylbutazone, methotrexate, etc.

Therapeutic uses
1. Urinary tract infections
2. Upper respiratory tract infections: Nocardiosis, Sulfasalazine in IBD.
3. Sulfacetamide in bacterial conjunctivitis & trachoma
4. Silver sulfadiazine for prevention of infection of burn wounds.

Adverse effects
• Hypersensitivity reactions
• Crystalluria,hematuria,renal obstruction.
• Allergic nephritis
• Haemolytic anaemia, aplastic anaemia, thrombocytopenia.
• Kernicterus in new born

Get in touch with the solution by just clicking the following links-

Facebook Group- https://www.facebook.com/groups/solutionpharamcy
Mobile App - https://play.google.com/store/apps/details?id=co.bolton.nqilv
New Channel (Pharmacy Dictionary) https://www.youtube.com/channel/UCt6OXVV_2oxf5DD0Mad6e9A
E-Mail for official and other work - solutionpharmacy@gmail.com
#solutionpharmacy #Pharmacologyclass #Pharmacognosyvideos #GPAT

Видео Topic (70) Sulphonamides = SAR, Uses and Adverse Effects | Sulphonamides Antibiotics | B.Pharma канала Solution- Pharmacy