Amodiaquine
- Atc Codes:P01BA06
- CAS Codes:86-42-0
- PHARMGKB ID:86-42-0
Table of contents
- Chemistry
- Pharmacologic Category
- Mechanism of Action
- Therapeutic Use
- Pregnancy and Lactation Implications
- Contraindications
- Warnings and Precautions
- Adverse Reactions
- Toxicological Effects
- Caution and personalized dose adjustment in patients with the following genotypes
- Other genes that may be involved
- Substrate of
- Inhibits
- Drug Interactions
- Dosage
- Pharmacokinetics and Pharmacodynamics
Brand Names
Drug combinations
Chemistry
Amodiaquine: C~20~H~22~ClN~3~O. Mw: 355.86. (1) Phenol, 4-[(7-chloro-4-quinolinyl)amino]-2-[(diethylamino)-methyl]-; (2) 4-[(7-Chloro-4-quinolyl)amino]-α – (diethylamino)-o-cresol. CAS-86-42-0.
Pharmacologic Category
Antimalarials; Aminoquinolines. (ATC-Code: P01BA06).
Mechanism of action
Effective against the erythrocytic stages of all four species of Plasmodium falciparum. As effective as chloroquine against chloroquine-sensitive strains of Plasmodium falciparum and also effective against some chloroquine-resistant strains. Amodiaquine accumulates in the lysosomes and brings about loss of function. Binds to and inhibits DNA and RNA polymerase. Interferes with metabolism and hemoglobin utilization by parasites.
Therapeutic use
Amodiaquine is an antimalarial with schizonticidal activity. It is indicated in the treatment of uncomplicated cases of malaria caused by Plasmodium falciparum.
Pregnancy and lactiation implications
Risk benefit ratio should be considered before administering amodiaquine in pregnancy as enough safety data are not available.
Unlabeled use
Contraindications
Contraindicated in patients with known hypersensitivity to amodiaquine or 4-aminoquinolines. Due to resistance and risk of major toxicity, amodiaquine is not recommended for the prophylaxis of malaria. Amodiaquine is also contraindicated in patients with hepatic disorders.
Warnings and precautions
Amodiaquine is no longer recommended for chemoprophylaxis of falciparum malaria as its use is associated with hepatic toxicity and agranulocytosis. Severe neutropenia can occur. Large dosesof amodiaquine have been reported to produce syncope, spasticity, convulsions and involuntary movements. Due to the occasional development of irreversible retinopathy, regular ophthalmic examinations should be carried out if the drug is used over a long period. Amodiaquine may cause blood dyscrasias, hepatitis, peripheral neuropathy and hemolytic anemia. As amodiaquine may concentrate in the liver, the drug should be used with caution in patients with hepatic disease or alcoholism and in patients receiving hepatotoxic drugs. Since hemolysis and acute renal failure have been reported to occur in a few patients with glucose 6-phosphate dehydrogenase deficiency receiving chloroquine, this should also be considered when using amodiaquine.