Formulations

Film-coated tablets containing 161.2 mg of chloroquine phosphate (equivalent to 100 mg of chloroquine base) plus 200 mg of proguanil hydrochloride.

Efficacy

There is no evidence of synergism or pharmacokinetic interaction between chloroquine and proguanil or cycloguanil (314). Although the combination has some activity against strains of P. falciparum with low levels of resistance to chloroquine, it is significantly less effective than mefloquine or doxycycline as a chemoprophylactic agent (61, 62).

Use

This combination drug was developed for chemoprophylaxis in adult travellers

( 15 years of age and > or < 50 kg body weight) travelling to areas where the combination of chloroquine plus proguanil is recommended. This may include areas in which the response of P. falciparum to chloroquine is already somewhat compromised. Owing to the chloroquine component, the combination will also be suppressive against initial infections of P. vivax, P. ovale and P. malariae but does not have antirelapse activity and does not prevent later recrudescences.

Treatment This combination is not recommended for malaria treatment.

Chemoprophylaxis

One tablet daily (adults).

Chemoprophylaxis of one tablet daily (315, 316) should start at least 24 h before entering the malarious area and continue until 4 weeks after exposure to malaria transmission has ended.

Use in pregnancy

Chloroquine and proguanil are both considered safe for use in pregnancy.

Drug disposition

There is no evidence of any pharmacokinetic interaction between chloroquine and proguanil in this combination drug.

Adverse effects

There are no apparent toxic interactions between chloroquine and proguanil. The combination therefore has the toxicological properties of the two components (see sections on chloroquine and proguanil). With the daily regimen recommended for chemoprophylaxis, the critical cumulative dose of 100 mg of chloroquine base will be reached in less than 3 years of continuous use.

Contraindications

Chloroquine-proguanil is contraindicated in:

• persons with known hypersensitivity to either proguanil or the 4-aminoquinolines,
• renal insufficiency,
• retinopathy related to earlier use of chloroquine,
• persons undergoing dialysis.

Caution is indicated in persons with impaired liver function, a history of epilepsy, or with severe G6PD deficiency