Amodiaquine
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Amodiaquine
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| Systematic (IUPAC) name | |
| 4-[(7-chloroquinolin-4-yl)amino]-2-[(diethylamino)methyl]phenol | |
| Clinical data | |
| AHFS/Drugs.com | International Drug Names |
| Pregnancy cat. | ? |
| Legal status | ? |
| Pharmacokinetic data | |
| Half-life | 5.2 ± 1.7 (range 0.4 to 5.5) minutes |
| Identifiers | |
| CAS number | 86-42-0  |
| ATC code | P01BA06 |
| PubChem | CID 2165 |
| DrugBank | DB00613 |
| ChemSpider | 2080 |
| UNII | 220236ED28 |
| KEGG | D02922 |
| ChEBI | CHEBI:2674 |
| ChEMBL | CHEMBL682 |
| Chemical data | |
| Formula | C20H22ClN3O |
| Mol. mass | 355.861 g/mol |
| SMILES | eMolecules & PubChem |
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Amodiaquine (trade names Camoquin, Flavoquine) is a 4-aminoquinoline compound related to chloroquine, used as an antimalarial and anti-inflammatory agent.
Amodiaquine has been shown to be more effective than chloroquine in treating CRPF (chloroquine-resistant Plasmodium falciparum) malaria infections and may afford more protection than chloroquine when used as weekly prophylaxis. Amodiaquine, like chloroquine, is generally well tolerated. Although licensed, this drug is not marketed in the United States but is widely available in Africa. Its use, therefore, is probably more practicable in long-term visitors and persons who will reside in Africa.[1]
Amodiaquine is a histamine N-methyltransferase inhibitor.
Pharmacogenetics
Amodiaquine has become an important drug in the combination therapy for malaria treatment in Africa[2] . Amodiquine is bioactivated hepatically to its primary metabolite N-desethylamodiaquine by the cytochrome p450 enzyme CYP2C8. Among amodiaquine users, several rare but serious side effects have been reported and linked to variants in the CYP2C8 alleles. CYP2C8*1 is characterized as the wild-type allele, which shows an acceptable safety profile while CYP2C8*2, *3 and *4 all show a range of “poor metabolizer” phenotypes. People that are poor metabolizers of amodiaquine display lower treatment efficacy against malaria as well as increased toxicity[3]. Several studies have been conducted to determine the prevalence of CYP2C8 alleles amongst malaria patients in Eastern Africa, and have tentatively shown that the variant alleles have significant prevalence in that population[4] . About 3.6% of the population studied shows high risk for a poor reaction to or reduced treatment outcomes when treated with amodiaquine. This information is useful in developing programs of pharmacovigilance in East Africa. These findings have important clinical considerations for prescribing anti-malarial medications in regions with high CYP2C8 variant frequency.
Notes
- ^ CDC recommendations for travel to areas with malaria
- ^ Kerb, Reinhold; Fux, Morike, Kremsner, Gil, Gleiter (2009). "Pharmacogenetics of antimalarial drugs: effect on metabolism and transport". Lancet Infectious Disease 9: 760-774.
- ^ Elyazar, Iqbal; Hay, Baird (2011). "Malaria Distribution, Prevalence, Drug Resistance, and control in Indonesia". Advanced Parasitology (74): 41-175. doi:10.1016/B978-0-12-385897-9.00002-1.
- ^ Roederer, Mary; Mcleod, Juliano (2011). "Can pharmacogenetics improve malaria". Bulletin of World Health Organization 89: 838-845. doi:10.2471/BLT.11.087320.
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