PROGUANIL HYDROCHLORIDE Property

Melting point:

120-121 °C

Boiling point:

350.7±52.0 °C(Predicted)

Density 

1.40±0.1 g/cm3(Predicted)

solubility 

DMSO (Slightly), Methanol (Slightly)

form 

Solid

pka

10.77±0.10(Predicted)

color 

White to Off-White

BCS Class

1

Stability:

Hygroscopic

Hazard and Precautionary Statements (GHS)

PROGUANIL HYDROCHLORIDE Chemical Properties,Usage,Production

Uses

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

Definition

ChEBI: Chlorproguanil is a dichlorobenzene.

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.