Drug reference

Amodiaquine

Antimalarial

CDSCO approvedSchedule H

EXCRETION

—

not curated

INTERACTIONS

—

none in our sources

PREGNANCY

—

not curated

Mechanism

Amodiaquine is an antimalarial agent, a congener of chloroquine. It is rapidly converted by hepatic CYPs into monodesethyl-amodiaquine, which retains substantial antimalarial activity. This metabolism primarily occurs via CYP2C8 N-Deethylation/N-Dealkylation.

Indications

Treatment of uncomplicated P. falciparum malariahighly effective therapy for uncomplicated malaria (as artesunate-amodiaquine)uncomplicated falciparum malaria (especially when coformulated with artesunate)Malaria

Dosing

Adult: For uncomplicated P. falciparum malaria, a total dose of up to 35 mg/kg body weight administered over 3 days.
Max dose: 35 mg/kg total dose over 3 days (for therapeutic regimen)

Pharmacokinetics

Onset

within 30 min of oral administration (amodiaquine); 2 h after oral administration (monodesethyl-amodiaquine)

Half-life

Amodiaquine: ~3 hours; Monodesethyl-amodiaquine (active metabolite): 9-18 days

Bioavailability

Rapidly absorbed after oral administration.

Metabolism

Rapidly converted by hepatic CYPs into monodesethyl-amodiaquine, primarily via CYP2C8 N-Deethylation/N-Dealkylation.

Contraindications

Chemoprophylaxis of P. falciparum malaria (due to associated hepatic toxicity and agranulocytosis)
chemoprophylaxis of p. falciparum malaria

Side effects

Common

itching (may be less common than chloroquine, but still common)

Serious

Hepatic toxicity (associated with prophylactic use)
Agranulocytosis (associated with prophylactic use)
Neutropenia (increased risk with amodiaquine therapy in HIV patients receiving antiretroviral therapy)
hepatic toxicities
agranulocytosis
neutropenia (in children and HIV patients receiving antiretroviral therapy)
Hepatotoxicity