PROGUANIL HYDROCHLORIDE Chemical Properties

Melting point:

120-121 °C

Boiling point:

350.7±52.0 °C(Predicted)

Density 

1.40±0.1 g/cm3(Predicted)

pka

10.77±0.10(Predicted)

PROGUANIL HYDROCHLORIDE Usage And Synthesis

Uses

PROGUANIL HYDROCHLORIDE is an antimalarial agent used in combination with Dapsone (D193250).

Clinical Use

Malaria chemoprophylaxis

Drug interactions

Potentially hazardous interactions with other drugs
Anticoagulants: effect of warfarin possibly enhanced.
Antimalarials: avoid concomitant use with artemether/lumefantrine; increased antifolate effect with pyrimethamine.

Metabolism

Proguanil is metabolised in the liver to the active metabolite, cycloguanil, and to p-chlorophenylbiguanide which is inactive, mainly by cytochrome P450, CYP 2C19 and slightly by CYP 3A4. Unlike proguanil and p-chlorophenylbiguanide, cycloguanil is not concentrated in erythrocytes so concentrations of cycloguanil in plasma and whole blood are similar. About 40-60% of a dose of proguanil is excreted in the urine, 60% of this as the unchanged drug, 30% as cycloguanil, and 8% as p-chlorophenylbiguanide. About 10% of a dose is excreted in the faeces.

PROGUANIL HYDROCHLORIDE(537-21-3)Related Product Information

• Verapamil
• N-(4-CHLOROPHENYL)-N'-(ISOPROPYL)-IMIDODICARBONIMIDIC DIAMIDE
• 1-(4-CHLOROPHENYL)BIGUANIDE HYDROCHLORIDE
• 3-Chlorophenylguanidine
• 1-(3-CHLOROPHENYL)BIGUANIDE HYDROCHLORIDE
• 4-CHLOROPHENYLGUANIDINE HYDROCHLORIDE
• Chlorguanide Hydrochloride
• N-(3,4-Dichlorophenyl)guanidine
• PROGUANIL HYDROCHLORIDE