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Saturday, November 19, 2011

PRIMAQUINE + CHLOROQUINE

Antibacterial activity

Used for prophylaxis of malaria, regardless of species, in all areas where the disease is endemic
Primaquine: effective against Plasmodium vivax,  P. ovale and the gametocyte of  P. falciparum
Chloroquine: effective against Plasmodium vivax, Plasmodium malariae and most strains of Plasmodium falciparum (but not the gametocytes of P. falciparum) and also has amebicidal activity (ex. Entamoeba histolytica)

Pregnancy Risk Factor

Class C

Contraindication/Precaution

Hypersensitivity to primaquine, chloroquine or any component
Do not use concomitantly with quinacrine
Do not use in the presence of retinal or visual field changes, follow visual acuity
Do not use in the presence of porphyria
Do not use if bone marrow depression/suppression
Do not use with nursing mothers
Use caution if G-6-PD deficiency
Use caution if impaired liver function or  liver disease
Use caution if GI disorders
Use caution  in the presence of psoriasis
Use caution if NADH methemoglobin reductase deficiency
Safety and effectiveness in children have not been established, however, no pediatrics-specific problems have been documented to date

Mechanism of Action

Primaquine: eliminates the primary tissue exoerythrocytic forms of P. falciparum; disrupts mitochondria and binds to DNA
Chloroquine: not completely understood: binds to and inhibits DNA and RNA polymerase

Pharmacodynamics

Metabolism: liver
Half-life: 
primaquine 3.7-7.4 hours
chloroquine: 3-5 days
Elimination: excreted in urine

Dosage

Note: 15 mg primaquine base = 26.3 mg primaquine phosphate

Note: 150 mg chloroquine base = 250 mg chloroquine phosphate

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

Children (based on weight):

4.5-6.8 kg: 
20 mg Chloroquine base + 3 mg primaquine base PO qwk
7.3-11.4 kg:
40 mg Chloroquine base + 6 mg primaquine base PO qwk
11.8-15.9 kg:
60 mg Chloroquine base + 9 mg primaquine base PO qwk
20.9-25 kg:
80 mg Chloroquine base + 12 mg primaquine base PO qwk
16.4-20.5 kg:
100 mg Chloroquine base + 15 mg primaquine base PO qwk
25.4-45.4 kg:
150 mg Chloroquine base + 22.5 mg primaquine base PO qwk
>45.4 kg:
300 mg Chloroquine base + 45 mg primaquine base PO qwk

Adults:

300 mg Chloroquine base + 45 mg primaquine base PO qwk

Dose VS renal function

Cr. clearance (ml/min):
N/A

Dialysis
Hemo: N/A
CAPD: N/A

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