Proguanil

Indications
Oral
Prophylaxis of malaria
Adult: 200 mg daily when used with chloroquine or 100 mg daily when used with 250 mg atovaquone. Recommendation: Start prophylaxis 1 wk before exposure to malaria, or 1-2 days prior to travel. Continue admin throughout exposure and for at least 4 wk (or 1 wk if given with atovaquone) after leaving a malaria-infested area.
Child: Co-admin with chloroquine: ≥45 kg (≥13 yr): Same as adult dose, 25-44.9 kg (8-12 yr): ¾ of adult dose, 16-24.9 kg (4-7 yr): ½ of adult dose, 10-15.9 kg (1-3 yr): 3/8 of adult dose, 6-9.9 kg (3-11 mth): ¼ of adult dose, <6 kg (0-12 wk): 1/8 of adult dose. Co-admin with atovaquone: ≥40 kg: Same as adult dose, 31-40 kg: ¾ of adult dose, 21-30 kg: ½ of adult dose, 11-20 kg: ¼ of adult dose.
CrCl (ml/min)Dosage Recommendation
<1050 mg once wkly.
10-1950 mg every other day.
20-59100 mg daily.

Oral
Uncomplicated falciparum malaria
Adult: 400 mg when used with 1 g of atovaquone as a single daily dose for 3 consecutive days.
Child: ≥40 kg: Same as adult dose, 31-40 kg: ¾ of adult dose, 21-30 kg: ½ of adult dose, 11-20 kg: ¼ of adult dose, 9-10 kg: 3/16 of adult dose, 5-8 kg 1/8 of adult dose.
CrCl (ml/min)Dosage Recommendation
<1050 mg once wkly.
10-1950 mg every other day.
20-59100 mg daily.
Contraindications
Hypersensitivity. Severe renal failure; known resistance of Plasmodium spp.
Warnings / Precautions
Renal impairment. Lactation.
Adverse Reactions
GI disturbances, headache, vertigo, rash, haematological abnormality in persons with renal impairment, dermatological reactions.
Drug Interactions
May reduce bioavailability of cloxacillin. Absorption is reduced when used with magnesium trisilicate. Increased risk of mouth ulcers when used with chloroquine. Fluvoxamine may reduce the metabolism of proguanil to its active metabolite, cycloguanil,
See Below for More proguanil Drug Interactions
Mechanism of Actions
Proguanil is a biguanide derivative which has to be metabolised in the body to the active metabolite, cycloguanil. It acts by inhibiting plasmodial dihydrofolate reductase and preventing nucleic acid synthesis. It is active against pre-erythrocytic forms and is a slow blood schizontocide.
Absorption: Readily absorbed after oral admin.
Distribution: Distributes into breast milk.
Metabolism: In the liver to active metabolite, cycloguanil.
Excretion: About 40-60% excreted in urine, of which 60% unchanged and 30% cycloguanil.
Administration
Should be taken with food. (Take after meals. Tab may be crushed & mixed w/ milk, honey or jam just before swallowing.)
ATC Classification
P01BB01 - proguanil ; Belongs to the class of biguanide antimalarials.
Available As
  • Proguanil 100 mg
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