Proguanil

Table of contents

  • Brand Names
  • Drug Combinations
  • Chemistry
  • Pharmacologic Category
  • Mechanism of Action
  • Therapeutic Use
  • Pregnancy and Lactation Implications
  • Warnings and Precautions
  • Adverse Reactions
  • Toxicological Effects
  • Caution and personalized dose adjustment in patients with the following genotypes
  • Substrate of
  • Inhibits
  • Drug Interactions
  • Dosage
  • Pharmacokinetics and Pharmacodynamics

Brand Names

Europe

France: Paludrine; Germany: Paludrine; Italy: Paludrine; Luxembourg: Paludrine; Netherlands: Paludrine; Sweden: Paludrine; UK: Paludrine.

Drug combinations

Proguanil and Atovaquone

Chemistry

Proguanil: C~11~H~17~Cl~2~N~5~. Mw: 290.2. (1) Imidodicarbonimidic diamide, N-(4-chlorophenyl). N’-(1-methylethyl) – monohydrochloride; (2) 1-(p-Chloropheyl)-5-isopropylbiguanide monohydrochloride. CAS-637-32-1 (2000).

Pharmacologic Category

Antiprotozoals; Antimalarials. (ATC-Code: P01BB01; P01BB51).

Mechanism of action

Inhibits dihydrofolate reductase of plasmodia and thereby blocks biosynthesis of purines and pyrimidines, essential for DNA synthesis and cell multiplication. This leads to failure of nuclear division at the time of schizont formation in erythrocytes and liver.

Therapeutic use

Antimalarial agent. Recommended for prevention and suppression of malaria.

Pregnancy and lactiation implications

Should not be used during pregnancy unless potential benefit outweighs risk. Malaria in pregnant women increases risk of maternal death, miscarriage, still-birth and low birth weight with associated risk of neonatal death. Although travel to malarious areas should be avoided during pregnancy, if unavoidable, effective prophylaxis strongly advised in pregnant women. Although excreted in breast milk, amount is insufficient to confer any benefit on infant. Separate chemoprophylaxis required for infant.

Unlabeled use

Contraindications

Warnings and precautions

Use with caution in severe renal impairment. Rare reports exist of hematological changes in such patients. In any locality where drug-resistant malaria is known or suspected, it is essential to take local medical advice on what prophylactic regimen is appropriate. Prophylactic use of proguanil alone may not be sufficient.

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