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Sulphonamides - Coggle Diagram
Sulphonamides
Side Effects
GIT
Nausea
Vomiting
Diarrhea
Headache
Mental depression
Cyanosis
Due to methaemoglobinaemia
Hepatitis
Hypersensitivity reactions
Rash
Anaphylaxis
Fever
Photosensitivity reactions
Bone marrow suppression
Anaemia
Agranulocytosis
Thrombocytosis
Crystallization in the renal tract
Crystalluria
Precipitation of acetylated metabolites in urine
Steven-Johnson Syndrome
Erythema multiforme
Skin/mucus membrane lesions
+/- Systemic illness
Kernicterus risk
Especially in premature infants
Displaces bilirubin from albumin binding site
Encephalitis
Increased activity by Methotrexate and Warfarin
Displaced from albumin
Activity/Use
Decreased therapeutic importance
EXCEPT
Co-trimoxazole
Broad spectrum
Gram + bacteria
Gram - bacteria
Prophylaxis of Malaria caused by chloroquine-resistant strains of plasmodium falciparum
Used in combination with Pyrimethamine
Chlamydia
Co-trimoxazole
Pneumocystis jiroveci
(fungus)
Nocardia
infections
Toxoplasmosis
(protozoa)
Sulfasalazine
Inflammatory bowel disease
Ulcerative colitis
Burns
Prevents bacterial colonization
Often combined with Trimethoprim
Mechanism of Action
Structural analogue of PABA
Compete with PABA for
dihydropteroate synthetase
enzyme
No folic acid synthesis
No DNA synthesis
Bacteriostatic
Local anaesthetics (PABA esters) can antagonise antibacterial effect
Presence of pus/tissue breakdown
Contains thymidine and purines
Bacteria can use to bypass need for folic acid
Effect negated
ADME
Resistance is common
Due to plasmid-mediated synthesis of enzyme insensitive to drug
Administration
PO (usually)
IV
IM
Not really topically due to allergy reaction
EXCEPT silver-sulfadiazine infected burns
Absorption
Good oral absorption except Sulfasalazine
Used for ulcerative colitis
Distribution
Crosses BBB
Crosses placenta
Metabolism/Excretion
Liver metabolism
Renal excretion
