Sulphanomides Flashcards
From which compound Are sulfanamides derived from
Para- aminobenzene sulphonamide
Classify sulphonamides
- Systemic acting
- local acting
- others
Name systemic acting Sulphonamides
- Short acting- sulphadiazine
- Intermediate- sulphamethoxazole
- Long - sulphadoxine
Name local acting sulphonamides
- Sulphacetamide
- Silver sulphadizine
- Mafenide
Name a Sulphonamides that acts both locally and systemically
Sulphasalazine
What is the mechanism of action of Sulphonamides
PABA is a precursor of folic acid which is essential to growth of bacteria.
Sulphonamides are similar to PABA and competitively inhibit folate synthetase enzyme and prevents information folic acid
In what compounds are Sulphonamides not effective
- Pus (it is rich in PABA)
- Purines
- Thymidine

Which enzyme is inhibited by sulphonamides
Folate synthetase enzyme 
What are the possible reasons for Sulphonamides resistance
- Decreased affinity of Folate synthetase
- Efflux Of drug
- Development of alternate metabolic pathway for folate synthesis
Which process metabolizes sulphonamides in the liver
Acetylation
What are the pharmacokinetics off  Sulphonamides
- Distributed in the whole body including CSF
- cross placental barrier
- Bound to plasma proteins especially albumin
- Metabolized in the liver
What are the adverse effects of Sulphonamides
1. Acetylated products are Poorly soluble in acidic urine. Cause crystalluria, hematouria, or obstruction of UT
2. Hypersensitivity (Skin rashes, itching, fever and Steven Johnson syndrome)
3. Patients with glucose-6-phosphate dehydrogenase deficiency hemolytic anaemia
4. Can cause hepatitis and suppression of bone marrow
5. In babies can cause displacement of bilirubin and kernicterus
Sulphonamides inhibit the metabolism of which drugs and prevents them from plasma protein binding
- Phenytoin
- Methotrexate
- oral anticoagulants
- oral hypoglycaemic agents
What are the therapeutic uses of sulphonamides
- Chloroquine resistant plasmodium falciparum malaria
- Toxoplasmosis
- Nocardiosis
- P. Jiroveci In patients with AIDS
- Ophthalmic infections
- prevent infections of burn wounds
- inflammatory bowel disease
- rheumatic arthritis
- prophylaxis of rheumatic fever

Which drugs are used to treat choloroquinone resistant plasmodium falciparum malaria
Sulphadoxine and pyrimethamine used in combination with artesunate