Radical treatment of vivax or ovale malaria.
contains Primaquine Phosphate, an 8-aminoquinoline derivative which is given by mouth to produce radical cure and prevent relapse of vivax and ovale malarias following treatment with a blood schizontocide. It has also been used to prevent transmission of falciparum malaria by those returning to areas where there is a potential for re-introduction of malaria.
Presystemic metabolism: extensive
Plasma half-life: range 4-10 hours, mean 6 hours
tmax: about 1 - 2 hours
Plasma protein binding: high
Oral Radical treatment of vivax or ovale malaria Adult: A course of treatment w/ a blood schizontocide should be given 1st to kill any erythrocytic parasites. 15 mg daily for 14 days, increased to higher doses or longer course if resistance in P. vivax occurs. Child: 250 mcg/kg once daily for 14 days. Max: 15 mg daily. Should be taken with food. Take w/ meals to avoid GI discomfort.
Primaquine inhibits hepatic drug oxidation and is reported to inhibit the metabolism of chloroquine.
Acutely ill patients suffering from systemic disease manifested by tendency to develop granulocytopenia (e.g. rheumatoid arthritis, lupus erythematosus). Concurrent use w/ other potentially haemolytic drugs or depressants of myeloid elements of the bone marrow. Concomitant admin w/ mepacrine. Patient w/ G6PD deficiency, NADH methaemoglobin reductase deficiency. Childn. Pregnancy and lactation.
Abdominal pain, gastric distress, nausea, vomiting; methaemoglobinaemia, haemolytic anaemia (in patients w/ G6PD deficiency), mild anaemia, leucocytosis; HTN, cardiac arrhythmias, prolonged QT interval on ECG, accommodation disturbance. Rarely, leucopenia, agranulocytosis. Potentially Fatal: Fatal haemolysis in patients w/ G6PD deficiency.
Use in Pregnancy: There is no adequate and well-controlled study in pregnant women. However, clinical experience with Mefloquine has not revealed an embrytoxic or teratogenic effect. Mefloquine should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. Use in Nursing Mothers: Mefloquine is excreted in breast milk in small amounts. the activity of which is unknown. Because of the potential for serious adverse reactions in nursing infants form Mefloquine. a decision should be made whether to discontinue the drug taking into account the importance of the drug to the mother.
Symptoms of overdosage of Primaquine phosphate include abdominal cramps, vomiting, burning epigastric distress, central nervous system and cardiovascular disturbances, including cardiac arrhythmia and QT interval prolongation, cyanosis, methemoglobinemia, moderate leukocytosis or leukopenia, and anemia. The most striking symptoms are granulocytopenia and acute hemolytic anemia in G6PD deficient patients. Acute hemolysis occurs, but patients recover completely if the dosage is discontinued.
Store at 25° C. Protect from light.
.png&w=384&q=75)