pyrimethamine/sulfadoxine (Discontinued)Brand and Other Names:Fansidar, Pyrimethamine-sulfadoxine

 
 
 

Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

tablet

  • 25mg/500mg
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Malaria Treatment

Discontinued in the United States

2-3 tablet PO once

Malaria Prophylaxis

1 tablet qWeek OR 2 tablets q2Weeks

Administration

Swallow tablet whole with plenty of fluids after a meal

Maintain adequate fluid intake to avert crystalluria or stone formation

Prophylaxis: take 1st dose 1-2 days before arrival to endemic area, continue throughout stay & 4-6 weeks after return

Other Indications & Uses

Chloroquine-resistant P. falciparum malaria treatment & prophylaxis

Off-label: toxoplasmosis

Dosage Forms & Strengths

tablet

  • 25mg/500mg
more...

Malaria Treatment

Discontinued in the United States

5-10 kg: 0.5 tablet

11-20 kg: 1 tablet

21-30 kg: 1.5 tablet

31-45 kg: 2 tablet

>45 kg: 3 tablet

Malaria Prophylaxis

5-10 kg: 0.25 tablet

11-20 kg: 0.5 tablet

21-30 kg: 0.75 tablet

31-45 kg: 1 tablet

>45 kg: 1.5 tablet

Administration

Swallow tablet whole with plenty of fluids after a meal

Maintain adequate fluid intake to avert crystalluria or stone formation

Prophylaxis: give 1st dose 1-2 days before arrival to endemic area, continue throughout stay & 4-6 weeks after return

<2 months old: Safety & efficacy not established

>2 months old: All PO single dose

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Interactions

Interaction Checker

pyrimethamine/sulfadoxine and

No Results

     
     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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            Adverse Effects

            Frequency Not Defined (selected)

            Agranulocytosis

            Anemias

            Insomnia

            Lightheadedness

            Malaise

            Seizures

            Abnl skin pigmentation

            Dermatitis

            Erythema multiforme

            Rash

            Stevens-Johnson syndrome

            TEN

            Anorexia

            N/V

            Diarrhea

            Leukopenia

            Thrombocytopenia

            Pulmonary eosinophilia

            Renal failure

            Interstitial nephritis

            Toxic nephrosis

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            Warnings

            Contraindications

            Hypersensitivity to sulfonamides, pyrimethamine

            Folate deficiency megaloblastic anemia

            Prophylactic use during third trimester of pregnancy/nursing mother

            Repeated prophylactic use in renal/hepatic failure, blood dyscrasias

            <2 mo

            Cautions

            Asthma, epilepsy, hepatic/renal impairment, G-6-PD deficiency

            Risk of Stevens-Johnson syndrome & toxic epidermal necrolysis (TEN)

            • discontinue STAT if skin rash appears

            Significant levels of resistant strains in many parts of the world

            Avoid prolonged sun exposure

            Not routinely used for prophylaxis

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            Pregnancy & Lactation

            Pregnancy Category: C

            Lactation: enters breast milk, contraindicated

            Pregnancy Categories

            A:Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

            B:May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

            C:Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

            D:Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

            X:Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

            NA:Information not available.

            more...
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            Pharmacology

            Protein Bound: pyrimethamine 87%; sulfadoxine 90%

            Half-Life:

            Pyrimethamine: 96 hr

            Sulfadoxine: ~200 hr

            Peak Plasma (1 tab dose)

            Time: 4 hr

            Concentration: Pyr: 0.2 mg/L; Sulf: 60 mg/L

            Other Information

            Metabolism: liver

            Excretion: urine

            Mechanism of Action

            Folic acid antagonists

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