REZIZFILM-COATED
Contains
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Overdosage
Symptoms: Headache, nausea, anorexia, vomiting, CNS stimulation, megaloblastic anaemia, leukopenia, thrombocytopenia, glossitis and crystalluria. Management: Treatment is symptomatic and supportive. Emesis and gastric lavage to reduce drug absorption. Ensure that patient is adequately hydrated to prevent kidney damage. Monitor renal, hepatic, and haematopoietic systems for at least 1 month after overdosage. Folinic acid may be admin for depressed platelet or WBC counts.
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Contraindications
Severe renal or hepatic impairment, blood dyscrasias, hypersensitivity to components, megaloblastic anaemia due to folate deficiency, pregnancy at term and during lactation, infants = 2 mth old.
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Special precautions
Severe renal or hepatic impairment, blood dyscrasias, hypersensitivity to components, megaloblastic anaemia due to folate deficiency, pregnancy at term and during lactation, infants = 2 mth old.
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Adverse drug reactions
Urticaria, serum sickness, photosensitisation, arthralgia, nausea, vomiting, abdominal pain, diarrhoea, headache, peripheral neuritis, ataxia, tinnitus, vertigo, convulsions, toxic nephrosis and pulmonary infiltrates resembling eosinophilic or allergic alveolitis. Potentially Fatal: Stevens-Johnson syndrome, toxic
epidermal necrolysis, fulminant hepatic necrosis, blood dyscrasias, anaphylactoid reactions.
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Mech of action
Pyrimethamine, a folic acid antagonist, inhibits the reduction of dihydrofolic acid to tetrahydrofolic acid (folinic acid). Sulfadoxine, a structural analog of p-aminobenzoic acid (PABA), competitively inhibits dihydrofolic acid synthesis which is important for PABA conversion to folic acid. This combination results in a synergistic action against susceptible plasmodia. Both have prolonged half-lives enabling single dose admin. Absorption: Peak plasma concentration: 4 hr. Distribution: Volume of distribution: 0.14 L/kg (sulfadoxine);
2.3 L/kg (pyrimethamine). Protein binding: 90% (for both drugs). Both drugs cross placenta and passes into breast milk. Metabolism: Sulfadoxine: 5% appear in blood as acetylated
metabolite, 2-3% as glucuronide. Pyrimethamine converted to several metabolites. Excretion: Elimination half life: 100 hr (pyrimethamine); 200
hr (sulfadoxine). Excreted mainly via kidneys.
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