|Licence data||US FDA:|
|(what is this?)|
It is FDA approved for use as a treatment and preventative measure against malaria. The combination is considered to be more effective in treating malaria caused by Plasmodium falciparum than that caused by Plasmodium vivax, for which chloroquine is considered more effective, though in the absence of a species-specific diagnosis the sulfadoxine-pyrimethamine combination may be indicated. Due to side effects, however, it is no longer recommended as a routine preventative, but only to treat serious malaria infections or to prevent them in areas where other drugs may not work.
Common (>1% frequency):
- Hypersensitivity reactions (e.g. itchiness, contact dermatitis and hives)
- GI effects (e.g. nausea, vomiting and diarrhoea)
Rare (<1% frequency):
- Abnormal liver function test results (e.g. elevated serum ALT, AST, alkaline phosphatase, and bilirubin concentrations)
- Megaloblastic anaemia caused by folate deficiency
- Hypersensitivity to pyrimethamine, sulfonamides, or any ingredient in the formulation
- Repeated prophylactic (prolonged) use in patients with renal or hepatic failure or blood dyscrasias
- Infants <2 months of age
- Prophylaxis in pregnancy at term
- Prophylaxis in nursing women
- Acute porphyria
Sulfadoxine is a sulfonamide antibiotic that competes with p-aminobenzoic acid (PABA) in the biosynthesis of folate. Pyrimethamine serves as a selective inhibitor of protozoal dihydrofolate reductase, hence preventing the synthesis of tetrahydrofolate — the active form of folate. There is a great degree of synergy between the two drugs due to their inhibition of two different steps in the biosynthesis of tetrahydrofolate.
|Half-life||111 hours||169 hours|
|Cmax||0.2 mg/L||60 mg/L|
|Tmax||4 hours||4 hours|
|Excretion||Renal (16-30%)||Renal (30%)|
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