Antibacterial Drugs - Antifolates Flashcards
Sulphonamindes - Drugs
Sodium Sulfacetamide
Silver Sulfadiazine
Sulfamethoxazole
Sulphonamindes - MOA
Bacteriostatic
Inhibit production of DNA, RNA and protein by acting as folate antagonists
Compete for dihydropteroate synthetase
Decrease dihydropteroic acid
Sulphonamindes - Kinetics
Good GIT absorbtion
Acetylated in liver
pH 2- 7
Sulfamethoxazole - Spectrum
UTIs Respiratory Infxns Sinusitis Pneumonia Bronchitis
Silver Sulfadiazine - Spectrum
Ulcerative colitis
Enteritis and enteric bacteria
IBD
Sulphonamindes - Spectrum
Both gram +ve and -ve
Broad spectrum
Sulphonamindes - Adverse Effects
Rashes Renal failure (low pH - crystalluria) Blood dyscrasias GIT (nausea, vomiting, anorexia) Kernicterus (neonates) Decreased efficacy of COCP
Sulphonamindes - C/I
Neonates and Infants Last trimester of pregancy Porphyria G6DP deficiency Allergy
Sulphonamindes - D/I
Oral anti-coagulants
Sulfonylureas
Phenytoin
Methotrexate (potentiates effects)
Sodium Sulfacetamide - Administration
Topical
Silver Sulfadiazine - Administration
Topical
Sulfamethoxazole - Administration
Oral administration
Trimethoprim - MOA
Bacteriostatic
Inhibits dihydrofolate reductase, preventing formation of tetrahydrofolate
NB: Affinity for bacterial enzyme = 50000 x > than human
Trimethoprim - Kinetics
Half life: 8 - 11 hours
Excreted unaltered by kidneys
Trimethoprim - Spectrum
Broad spectrum
UTIs
RTIs
Chronic Prostatitis