Primaquine Phosphate
Pronouncation: (PRIM-uh-kween FOSS-fate)Class: Antimalarial
Trade Names:
Primaquine Phosphate
- Tablets 26.3 mg (equiv. to 15 mg base)
Pharmacology
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Disrupts metabolic processes of parasitic organism, eliminating tissue (exoerythrocytic) infection and preventing development of blood (erythrocytic) forms of parasite responsible for relapses of vivax malaria.
Pharmacokinetics
Absorption
Rapid. Bioavailability is approximately 96%. T max is approximately 2 to 3 h (primaquine), approximately 7 h (metabolite carboxyprimaquine). C max is 50 to 66 ng/mL (15 mg); 104 ng/mL (30 mg).
Distribution
Extensively distributed. Vd is 248 L. C max is 291 to 736 ng/mL (metabolite) and 432 to 1240 ng/mL (metabolite).
Metabolism
Rapidly converted to carboxyprimaquine. Undetermined if the main plasma metabolite has activity.
Elimination
Urine (less than 2% of dose). The t ½ is 5.8 h (primaquine); 22 to 30 h (metabolite carboxyprimaquine).
Indications and Usage
Radical cure or prevention of relapse in vivax malaria; after termination of chloroquine phosphate suppressive therapy in areas where vivax malaria is endemic.
Unlabeled Uses
With clindamycin, treatment of Pneumocystis carinii pneumonia associated with AIDS.
Contraindications
Concomitant administration of quinacrine and primaquine; acutely ill patient with systemic disease manifested by granulocytopenia (eg, rheumatoid arthritis, lupus erythematosus); concurrent administration of other potentially hemolytic or bone marrow depressant medications.
Dosage and Administration
Begin therapy during last 2 wk of or after course of suppression with chloroquine or comparable drug.
AdultsPO 26.3 mg (15 mg base) for 14ߙdays.
ChildrenPO 0.5 mg/kg/day (0.3 mg/kg/day of base) for 14 days (max, 15 mg/day of base).
General Advice
Administer without regard to meals. Administer with food if GI upset occurs.
Storage/Stability
Store at room temperature in tightly closed, light-resistant container.
Drug Interactions
QuinacrineMay potentiate toxicity of antimalarial compounds that are structurally related to primaquine.
Laboratory Test Interactions
None well documented.
Adverse Reactions
GI
Nausea; vomiting; epigastric distress; abdominal cramps.
Hematologic
Leukopenia; hemolytic anemia in G-6-PD deficiency; methemoglobinemia in NADH methemoglobin reductase deficiency.
Precautions
Pregnancy
Pregnancy category undetermined.
Lactation
Undetermined. To avoid adverse reactions in the infant, do not give to lactating women.
Hemolytic anemia
May occur in patients with following conditions: G-6-PD deficiency, NADH methemoglobin reductase deficiency; idiosyncratic reactions (leukopenia, methemoglobinemia; hemolytic anemia). Discontinue drug if marked darkening of urine or sudden decrease in Hgb or leukocyte count occurs.
Max dose
Hemolytic reactions may occur with doses of drug exceeding recommended dose.
Overdosage
Symptoms
Anemia, methemoglobinemia, leukopenia, acute abdominal cramps, vomiting, epigastric distress, CNS and cardiovascular disturbances, granulocytopenia, hemolytic anemia.
Patient Information
- Tell patient that medicine may be taken with food if stomach upset (eg, nausea, vomiting, abdominal cramps) occurs, and advise patient to contact health care provider if upset persists.
- Emphasize importance of compliance with drug regimen.
- Advise patient to report marked darkening of urine to health care provider.
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More Primaquine Phosphate resources:
Primaquine - Includes detailed dosage instructions.
Primaquine Phosphate Drug Interactions
Malaria, Malaria Prevention, Pneumocystis Pneumonia
