Brand Names/Manufacturer

Proguanil is available as Proguanil Tablets BP or BNF (containing Proguanil hydrochloride) and as Paludrine® manufactured by AstraZeneca (tablets with Proguanil hydrochloride).

Class

Proguanil belongs to the biguanide class of medications.

Antiparasitic Activity

Proguanil is primarily employed for preventing falciparum malaria. Additionally, cycloguanil, a derivative, exhibits in vitro activity against T. gondii.

Proguanil Mechanism of Action

By inhibiting dihydrofolate reductase post cytochrome P450-catalyzed cyclization, Proguanil disrupts the development of malaria.

Mechanism of Resistance

Resistance emerges through various mutations in the gene responsible for coding this enzyme.

Pharmacokinetics

After oral administration, Proguanil is well absorbed. Its half-life (t1/2) is approximately 16.5 hours, with about 60% excreted unchanged in urine. Proguanil acts as a pro-drug, converting into cycloguanil and 4-chlorophenyl-biguanide, the former being a potent antimalarial compound.

Dosage of Proguanil

For falciparum malaria prevention, a daily adult dose of 200 mg (may be divided or taken at once) is commonly paired with weekly chloroquine.

Disease State Based Dosing

Proguanil is relatively contraindicated in patients with renal dysfunction.

Adverse Effects

With a high therapeutic index, severe adverse effects are rare. Prolonged usage may lead to temporary hair loss and mouth ulcers.

Proguanil Drug Interactions

Proguanil has not shown significant clinical interactions with other drugs.

Pregnancy

While no evidence links Proguanil to birth defects, pregnant women are advised to avoid malaria-prone areas.