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L - Caution when used during Lactation.
Proguanil, an anti-malarial drug, is prescribed for the prevention of malaria. The drug is either prescribed as a monotherapy or as a combined therapy with other prophylactic drugs.
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.
In Prophylaxis of malaria (Orally) and in Uncomplicated falciparum malaria (orally).
Proguanil can cause skin reactions including itching, lower back pain, vomiting, blood urine, stomach pain, painful urination or stinging, diarrhoea, vomiting, oral cankers, anorexia, temporary alopecia, nausea and headache.
Avoid travelling to geographical areas endemic to malaria. Use effective mosquito-repellent or mosquito net to avoid bite.
Renal impairment. Lactation
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.
Proguanil may interact with dicumarol, warfarin, typhoid vaccine, chloroquine and aurothioglucose.
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.
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.
Take Proguanil preferably after food intake to avoid GI upset.
Category B: Either animal-reproduction studies have not demonstrated a foetal risk but there are no controlled studies in pregnant women or animal-reproduction studies have shown an adverse effect (other than a decrease in fertility) that was not confirmed in controlled studies in women in the 1st trimester (and there is no evidence of a risk in later trimesters).
It is unclear whether the drug could pass through the breast milk to a breast feeding a baby. Consult your physician before taking Proguanil, if you are nursing mother.
Hypersensitivity. Severe renal failure; known resistance of Plasmodium spp.