SULFONAMIDES

WEDNESDAY, 1st October 2014

10 am -12 pm
Learning objectives
At the end of this session you will be able to:
Classify sulfonamides.
Explain the mechanism of action of
Sulfonamides along with uses, side effects and
contraindications.
Discuss sequential blockade with reference to
cotrimoxazole
Sulfonamides: Mechanism of
Action
Spectrum: both gram + ve & gram ve
including S. pyogenes, S. pneumoniae, H.
influenzae
Bacteriostatic action
Prevent synthesis of folic acid required for
synthesis of purines and nucleic acid
Does not affect human cells or certain
bacteriathey can use preformed folic
acid
Mechanism of action

P-AMINOBENZOIC ACID

sulfonamide Dihydrofolate synthetase

DIHYDROFOLIC ACID

trimethoprim Dihydrofolate reductase

TETRAHYDROFOLIC ACID

Other drugs that inhibit DHFR enzyme:

Methotrexate, Pyrimethamine (combined
with sulfadoxine for malaria treatment)
Classification:
Sulfonamides
Absorbed Rapidly & excreted rapidly:
Sulphamethoxazole, sulfadiazine: orally for
systemic infections.
Absorbed slowly & excreted slowly:
Sulfadoxine, Long acting, 7-9 days: used
for treatment of malaria along with
pyrimethamine
Not absorbed orally : Sulfasalazine: gets
broken down into 5-ASA and sulfapyridine
in large intestine, 5-ASA acts locally in IBD.
Topically used : Silver sulfadiazine (for
dressing of wound infection),
sulfacetamide eye drops
Sulfonamides: sulfamethoxazole
Therapeutic Uses

Combined with trimethoprim.

Used to treat UTIs, Pneumocystis carinii
pneumonia, ear infections, bronchitis,
gonorrhea
Nocardiosis
Toxoplasmosis : combination of
pyrimethamine & sulfadiazine is
treatment of choice
Adverse Reacions
Hypersensitivity reactions, phototoxicity,
fixed drug eruption.
**Urinary tract disturbances : Crystalluria,

hemorrhagic cystitis. How to avoid them??

Hematopoietic disturbances: **hemolytic

anemia (G6PD deficiency), aplastic anemia

**Drug Interactions : can promote effects

of warfarin, phenytoin ??
Kernicterus

*Contraindicated in pregnancy.
Co-Trimoxazole
Fixed dose combination of Trimethoprim
& sulfamethoxazole
Combination becomes Bactericidal, also
widens the spectrum to include
salmonella
Sequential blockade- Synergistic
1 part of trimethoprim is combined with 5
parts of SMX (80mg TMP + 400mg SMX)
Optimum plasma ratio 1:20
Uses of Co-Trimoxazole
**UTI

Bacterial Respiratory tract infections

GI infections caused by shigella,

salmonella
**Pneumocystis carinii infections:

treatment and prophylaxis of PCP

pneumonia (DOC)
Nocardiosis

Brucellosis : DOC is combination of

Doxycycline and streptomycin / gentamicin