No

Antimalarial Agent

Prophylaxis of malaria, regardless of species, in all areas where the disease is endemic

C

Retinal or visual field changes, known hypersensitivity to chloroquine or primaquine

Use with caution in patients with psoriasis, porphyria, hepatic dysfunction, G-6-PD deficiency

1% to 10%: Gastrointestinal: Diarrhea, nausea

<1%: Hypotension, EKG changes, fatigue, personality changes, headache, pruritus, hair bleaching, anorexia, vomiting, stomatitis, blood dyscrasias, retinopathy, blurred vision

Symptoms of overdose include headache, visual changes, cardiovascular collapse, seizures, abdominal cramps, vomiting, cyanosis, methemoglobinemia, leukopenia, respiratory and cardiac arrest

Following initial measures (immediate GI decontamination), treatment is supportive and symptomatic

Decreased absorption if administered concomitantly with kaolin and magnesium trisilicate

Increased toxicity/levels with cimetidine

Chloroquine concentrates within parasite acid vesicles and raises internal pH resulting in inhibition of parasite growth; may involve aggregates of ferriprotoporphyrin IX acting as chloroquine receptors causing membrane damage; may also interfere with nucleoprotein synthesis. Primaquine eliminates the primary tissue exoerythrocytic forms of P. falciparum; disrupts mitochondria and binds to DNA.

Absorption: Oral: Both drugs are readily absorbed

Distribution: Concentrated in liver, spleen, kidney, heart, and brain

Protein binding: ~55%; binds strongly to melanin

Metabolism: 25% of chloroquine is metabolized

Elimination: Drug may remain in tissue for 3-5 days; up to 70% excreted unchanged

Oral: Start at least 1 day before entering the endemic area; continue for 8 weeks after leaving the endemic area

Note: Liquid doses contain approximately 40 mg of chloroquine base and 6 mg primaquine base per 5 mL, prepared from chloroquine phosphate with primaquine phosphate tablets

10-15 lb (4.5-6.8 kg): 20 mg chloroquine base and 3 mg primaquine base (2.5 mL)

16-25 lb (7.3-11.4 kg): 40 mg chloroquine base and 6 mg primaquine base (5 mL)

26-35 lb (11.8-15.9 kg): 60 mg chloroquine base and 9 mg primaquine base (7.5 mL)

36-45 lb (16.4-20.5 kg): 80 mg chloroquine base and 12 mg primaquine base (10 mL)

46-55 lb (20.9-25 kg): 100 mg chloroquine base and 15 mg primaquine base (12.5 mL)

56-100 lb (25.4-45.4 kg): 150 mg chloroquine base and 22.5 mg primaquine base (1/2 tablet)

>100 lb (>45.4 kg): 300 mg chloroquine base and 45 mg primaquine base (1 tablet)

Adults: 1 tablet/week on the same day each week

Periodic CBC, examination for muscular weakness, and ophthalmologic examination in patients receiving prolonged therapy

May rarely cause fatigue or personality changes

May cause blood dyscrasias; use caution with clozapine and carbamazepine

No information available to require special precautions

No effects or complications reported

See individual agents. Pregnancy/breast-feeding precautions: Inform prescriber if you are or intend to get pregnant. Do not breast-feed.

Monitor periodic CBC, examination for muscular weakness and ophthalmologic examination in patients receiving prolonged therapy

Tablet: Chloroquine phosphate 500 mg [base 300 mg] and primaquine phosphate 79 mg [base 45 mg]

Panisko DM and Keystone JS, "Treatment of Malaria - 1990," Drugs, 1990, 39(2):160-89.

White NJ, "The Treatment of Malaria," N Engl J Med, 1996, 335(11):800-6.

Wyler DJ, "Malaria Chemoprophylaxis for the Traveler," N Engl J Med, 1993, 329(1):31-7.

Wyler DJ, "Malaria: Overview and Update," Clin Infect Dis, 1993, 16(4):449-56.