Details
Stereochemistry | ACHIRAL |
Molecular Formula | C20H22ClN3O.2ClH |
Molecular Weight | 428.783 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
Cl.Cl.CCN(CC)CC1=CC(NC2=CC=NC3=C2C=CC(Cl)=C3)=CC=C1O
InChI
InChIKey=ROEBJVHPINPMKL-UHFFFAOYSA-N
InChI=1S/C20H22ClN3O.2ClH/c1-3-24(4-2)13-14-11-16(6-8-20(14)25)23-18-9-10-22-19-12-15(21)5-7-17(18)19;;/h5-12,25H,3-4,13H2,1-2H3,(H,22,23);2*1H
Molecular Formula | C20H22ClN3O |
Molecular Weight | 355.861 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
Molecular Formula | ClH |
Molecular Weight | 36.461 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
DescriptionCurator's Comment: description was created based on several sources, including
https://www.drugbank.ca/drugs/DB00613 | https://www.drugs.com/international/amodiaquine.html | https://www.ncbi.nlm.nih.gov/pubmed/9825729 | https://www.ncbi.nlm.nih.gov/pubmed/22949374 | https://www.ncbi.nlm.nih.gov/pubmed/18855526
Curator's Comment: description was created based on several sources, including
https://www.drugbank.ca/drugs/DB00613 | https://www.drugs.com/international/amodiaquine.html | https://www.ncbi.nlm.nih.gov/pubmed/9825729 | https://www.ncbi.nlm.nih.gov/pubmed/22949374 | https://www.ncbi.nlm.nih.gov/pubmed/18855526
Amodiaquine is a medication used to treat malaria, including Plasmodium falciparum malaria when uncomplicated. The mechanism of plasmodicidal action of amodiaquine is not completely certain. Like other quinoline derivatives, it is thought to inhibit heme polymerase activity. This results in accumulation of free heme, which is toxic to the parasites. The drug binds the free heme preventing the parasite from converting it to a form less toxic. This drug-heme complex is toxic and disrupts membrane function. The side effects of amodiaquine are generally minor to moderate and are similar to those of chloroquine. Rarely liver problems or low blood cell levels may occur. When taken in excess headaches, trouble seeing, seizures, and cardiac arrest may occur. After oral administration amodiaquine hydrochloride is rapidly absorbed,and undergoes rapid and extensive metabolism to desethylamodiaquine which concentrates in red blood cells. It is likely that desethylamodiaquine, not amodiaquine, is responsible for most of the observed antimalarial activity, and that the toxic effects of amodiaquine after oral administration may in part be due to desethylamodiaquine.
CNS Activity
Curator's Comment: Although in use for more than 40 year, there exists little information regarding the disposition of amodiaquine in man. Chloroquine, a 4-aminoquinoline derivative which resembles amodiaquine structurally, is widely distributed into the body tissues, especially in liver, spleen, kidney, lungs, brain, and spinal cord.
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: Heme degradation by glutathione Sources: https://www.ncbi.nlm.nih.gov/pubmed/9825729 |
|||
Target ID: Heme polymerization |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | Coarsucam Approved UseTherapeutic Indication. ARTESUNATE AMODIAQUINE WINTHROP is indicated for the treatment of uncomplicated cases of malaria due to Plasmodium falciparum strains which are susceptible to amodiaquine as well as to artesunate. |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
21 mg/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/8983859/ |
10 mg/kg single, oral dose: 10 mg/kg route of administration: Oral experiment type: SINGLE co-administered: |
AMODIAQUINE blood | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
322 mg/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/8983859/ |
10 mg/kg single, intravenous dose: 10 mg/kg route of administration: Intravenous experiment type: SINGLE co-administered: |
AMODIAQUINE blood | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
415 mg/L EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/8983859/ |
10 mg/kg single, intravenous dose: 10 mg/kg route of administration: Intravenous experiment type: SINGLE co-administered: |
AMODIAQUINE blood | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
AUC
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
77 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/8983859/ |
10 mg/kg single, oral dose: 10 mg/kg route of administration: Oral experiment type: SINGLE co-administered: |
AMODIAQUINE blood | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
T1/2
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
3.7 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/8983859/ |
10 mg/kg single, oral dose: 10 mg/kg route of administration: Oral experiment type: SINGLE co-administered: |
AMODIAQUINE blood | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
10.1 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/8983859/ |
10 mg/kg single, intravenous dose: 10 mg/kg route of administration: Intravenous experiment type: SINGLE co-administered: |
AMODIAQUINE blood | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
2.1 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/8983859/ |
10 mg/kg single, intravenous dose: 10 mg/kg route of administration: Intravenous experiment type: SINGLE co-administered: |
AMODIAQUINE blood | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
7.9 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/20368402/ |
270 mg 1 times / day steady-state, oral dose: 270 mg route of administration: Oral experiment type: STEADY-STATE co-administered: ARTESUNATE |
AMODIAQUINE plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
Doses
Dose | Population | Adverse events |
---|---|---|
73.4 mg 1 times / day multiple, oral (mean) Studied dose Dose: 73.4 mg, 1 times / day Route: oral Route: multiple Dose: 73.4 mg, 1 times / day Sources: |
unhealthy, 17 to 76 years n = 7 Health Status: unhealthy Condition: malaria Age Group: 17 to 76 years Sex: M+F Population Size: 7 Sources: |
Other AEs: Agranulocytosis... |
10 mg/kg 1 times / day single, oral Studied dose Dose: 10 mg/kg, 1 times / day Route: oral Route: single Dose: 10 mg/kg, 1 times / day Sources: |
healthy, 18 to 45 years n = 15 Health Status: healthy Age Group: 18 to 45 years Sex: M+F Population Size: 15 Sources: |
Disc. AE: Hypersensitivity reaction... AEs leading to discontinuation/dose reduction: Hypersensitivity reaction (6.7%) Sources: |
10 mg/kg 1 times / day single, oral Studied dose Dose: 10 mg/kg, 1 times / day Route: oral Route: single Dose: 10 mg/kg, 1 times / day Sources: |
healthy, 18 to 45 years n = 7 Health Status: healthy Age Group: 18 to 45 years Sex: M+F Population Size: 7 Sources: |
Other AEs: Leucopenia, Neutropenia... Other AEs: Leucopenia (grade 1, 14%) Sources: Neutropenia (grade 1, 14%) |
10 mg/kg 1 times / day single, oral Studied dose Dose: 10 mg/kg, 1 times / day Route: oral Route: single Dose: 10 mg/kg, 1 times / day Co-administed with:: artesunate(4 mg/kg; single dose) Sources: |
healthy, 18 to 45 years n = 8 Health Status: healthy Age Group: 18 to 45 years Sex: M+F Population Size: 8 Sources: |
Other AEs: Neutropenia... |
10 mg/kg 1 times / day single, oral Studied dose Dose: 10 mg/kg, 1 times / day Route: oral Route: single Dose: 10 mg/kg, 1 times / day Sources: |
healthy, 18 to 45 years n = 8 Health Status: healthy Age Group: 18 to 45 years Sex: M+F Population Size: 8 Sources: |
Other AEs: Transaminitis... |
45 mg/kg multiple, oral (mean) Studied dose Dose: 45 mg/kg Route: oral Route: multiple Dose: 45 mg/kg Sources: |
unhealthy, adult n = 20 Health Status: unhealthy Condition: onchocerciasis Age Group: adult Sex: M Population Size: 20 Sources: |
Other AEs: Nausea, Vomiting... Other AEs: Nausea (35%) Sources: Vomiting (35%) Lassitude (grade 2, 60%) Diarrhoea (15%) Constipation (10%) Granulocytopenia (15%) |
600 mg 1 times / day multiple, oral Studied dose Dose: 600 mg, 1 times / day Route: oral Route: multiple Dose: 600 mg, 1 times / day Sources: |
unhealthy, median age 20 years n = 220 Health Status: unhealthy Condition: malaria Age Group: median age 20 years Sex: F Population Size: 220 Sources: |
Other AEs: Weakness generalised, Dizziness... Other AEs: Weakness generalised (84%) Sources: Dizziness (58%) Vomiting (46%) Itching (32%) Nausea (26%) |
71.6 mg 1 times / day multiple, oral (mean) Studied dose Dose: 71.6 mg, 1 times / day Route: oral Route: multiple Dose: 71.6 mg, 1 times / day Sources: |
unhealthy, median age 35 years n = 2 Health Status: unhealthy Condition: malaria Age Group: median age 35 years Sex: M+F Population Size: 2 Sources: |
Other AEs: Hepatotoxicity... |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
Agranulocytosis | 73.4 mg 1 times / day multiple, oral (mean) Studied dose Dose: 73.4 mg, 1 times / day Route: oral Route: multiple Dose: 73.4 mg, 1 times / day Sources: |
unhealthy, 17 to 76 years n = 7 Health Status: unhealthy Condition: malaria Age Group: 17 to 76 years Sex: M+F Population Size: 7 Sources: |
|
Hypersensitivity reaction | 6.7% Disc. AE |
10 mg/kg 1 times / day single, oral Studied dose Dose: 10 mg/kg, 1 times / day Route: oral Route: single Dose: 10 mg/kg, 1 times / day Sources: |
healthy, 18 to 45 years n = 15 Health Status: healthy Age Group: 18 to 45 years Sex: M+F Population Size: 15 Sources: |
Leucopenia | grade 1, 14% | 10 mg/kg 1 times / day single, oral Studied dose Dose: 10 mg/kg, 1 times / day Route: oral Route: single Dose: 10 mg/kg, 1 times / day Sources: |
healthy, 18 to 45 years n = 7 Health Status: healthy Age Group: 18 to 45 years Sex: M+F Population Size: 7 Sources: |
Neutropenia | grade 1, 14% | 10 mg/kg 1 times / day single, oral Studied dose Dose: 10 mg/kg, 1 times / day Route: oral Route: single Dose: 10 mg/kg, 1 times / day Sources: |
healthy, 18 to 45 years n = 7 Health Status: healthy Age Group: 18 to 45 years Sex: M+F Population Size: 7 Sources: |
Neutropenia | grade 2, 12% | 10 mg/kg 1 times / day single, oral Studied dose Dose: 10 mg/kg, 1 times / day Route: oral Route: single Dose: 10 mg/kg, 1 times / day Co-administed with:: artesunate(4 mg/kg; single dose) Sources: |
healthy, 18 to 45 years n = 8 Health Status: healthy Age Group: 18 to 45 years Sex: M+F Population Size: 8 Sources: |
Transaminitis | grade 3, 12% | 10 mg/kg 1 times / day single, oral Studied dose Dose: 10 mg/kg, 1 times / day Route: oral Route: single Dose: 10 mg/kg, 1 times / day Sources: |
healthy, 18 to 45 years n = 8 Health Status: healthy Age Group: 18 to 45 years Sex: M+F Population Size: 8 Sources: |
Constipation | 10% | 45 mg/kg multiple, oral (mean) Studied dose Dose: 45 mg/kg Route: oral Route: multiple Dose: 45 mg/kg Sources: |
unhealthy, adult n = 20 Health Status: unhealthy Condition: onchocerciasis Age Group: adult Sex: M Population Size: 20 Sources: |
Diarrhoea | 15% | 45 mg/kg multiple, oral (mean) Studied dose Dose: 45 mg/kg Route: oral Route: multiple Dose: 45 mg/kg Sources: |
unhealthy, adult n = 20 Health Status: unhealthy Condition: onchocerciasis Age Group: adult Sex: M Population Size: 20 Sources: |
Granulocytopenia | 15% | 45 mg/kg multiple, oral (mean) Studied dose Dose: 45 mg/kg Route: oral Route: multiple Dose: 45 mg/kg Sources: |
unhealthy, adult n = 20 Health Status: unhealthy Condition: onchocerciasis Age Group: adult Sex: M Population Size: 20 Sources: |
Nausea | 35% | 45 mg/kg multiple, oral (mean) Studied dose Dose: 45 mg/kg Route: oral Route: multiple Dose: 45 mg/kg Sources: |
unhealthy, adult n = 20 Health Status: unhealthy Condition: onchocerciasis Age Group: adult Sex: M Population Size: 20 Sources: |
Vomiting | 35% | 45 mg/kg multiple, oral (mean) Studied dose Dose: 45 mg/kg Route: oral Route: multiple Dose: 45 mg/kg Sources: |
unhealthy, adult n = 20 Health Status: unhealthy Condition: onchocerciasis Age Group: adult Sex: M Population Size: 20 Sources: |
Lassitude | grade 2, 60% | 45 mg/kg multiple, oral (mean) Studied dose Dose: 45 mg/kg Route: oral Route: multiple Dose: 45 mg/kg Sources: |
unhealthy, adult n = 20 Health Status: unhealthy Condition: onchocerciasis Age Group: adult Sex: M Population Size: 20 Sources: |
Nausea | 26% | 600 mg 1 times / day multiple, oral Studied dose Dose: 600 mg, 1 times / day Route: oral Route: multiple Dose: 600 mg, 1 times / day Sources: |
unhealthy, median age 20 years n = 220 Health Status: unhealthy Condition: malaria Age Group: median age 20 years Sex: F Population Size: 220 Sources: |
Itching | 32% | 600 mg 1 times / day multiple, oral Studied dose Dose: 600 mg, 1 times / day Route: oral Route: multiple Dose: 600 mg, 1 times / day Sources: |
unhealthy, median age 20 years n = 220 Health Status: unhealthy Condition: malaria Age Group: median age 20 years Sex: F Population Size: 220 Sources: |
Vomiting | 46% | 600 mg 1 times / day multiple, oral Studied dose Dose: 600 mg, 1 times / day Route: oral Route: multiple Dose: 600 mg, 1 times / day Sources: |
unhealthy, median age 20 years n = 220 Health Status: unhealthy Condition: malaria Age Group: median age 20 years Sex: F Population Size: 220 Sources: |
Dizziness | 58% | 600 mg 1 times / day multiple, oral Studied dose Dose: 600 mg, 1 times / day Route: oral Route: multiple Dose: 600 mg, 1 times / day Sources: |
unhealthy, median age 20 years n = 220 Health Status: unhealthy Condition: malaria Age Group: median age 20 years Sex: F Population Size: 220 Sources: |
Weakness generalised | 84% | 600 mg 1 times / day multiple, oral Studied dose Dose: 600 mg, 1 times / day Route: oral Route: multiple Dose: 600 mg, 1 times / day Sources: |
unhealthy, median age 20 years n = 220 Health Status: unhealthy Condition: malaria Age Group: median age 20 years Sex: F Population Size: 220 Sources: |
Hepatotoxicity | 71.6 mg 1 times / day multiple, oral (mean) Studied dose Dose: 71.6 mg, 1 times / day Route: oral Route: multiple Dose: 71.6 mg, 1 times / day Sources: |
unhealthy, median age 35 years n = 2 Health Status: unhealthy Condition: malaria Age Group: median age 35 years Sex: M+F Population Size: 2 Sources: |
Overview
CYP3A4 | CYP2C9 | CYP2D6 | hERG |
---|---|---|---|
OverviewOther
Other Inhibitor | Other Substrate | Other Inducer |
---|---|---|
Drug as perpetrator
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
no |
Drug as victim
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
major | yes (co-administration study) Comment: When administered with efavirenz, 125%, 78%, 80%, and 42.15% increase in the Tmax, Cmax AUCT and T1/2 of amodiaquine respectively |
|||
minor | ||||
minor | ||||
minor | ||||
minor | ||||
minor | ||||
minor | ||||
minor | ||||
minor | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
unlikely | unlikely Comment: Since artesunate is mainly metabolized by CYP2A6, drug–drug interaction between artesunate and AQ is unlikely to occur |
|||
yes |
PubMed
Title | Date | PubMed |
---|---|---|
[National Network study to perpetuate the surveillance of Plasmodium falciparum sensitivity to antimalarials in Madagascar]. | 2002 |
|
[Treatment of malaria in children: 1. Uncomplicated malaria]. | 2002 |
|
In vitro sensitivity of Plasmodium falciparum to amodiaquine compared with other major antimalarials in Madagascar. | 2002 Dec |
|
Sulfadoxine/pyrimethamine alone or with amodiaquine or artesunate for treatment of uncomplicated malaria: a longitudinal randomised trial. | 2002 Dec 21-28 |
|
Cytochrome P450 1A1/2 induction by antiparasitic drugs: dose-dependent increase in ethoxyresorufin O-deethylase activity and mRNA caused by quinine, primaquine and albendazole in HepG2 cells. | 2002 Nov |
|
Efficacy of amodiaquine for uncomplicated Plasmodium falciparum malaria in Harper, Liberia. | 2002 Nov-Dec |
|
Paracellular tightness and catabolism restrict histamine permeation in the proximal colon of pigs. | 2002 Oct |
|
Molecular characterisation of drug-resistant Plasmodium falciparum from Thailand. | 2002 Oct 14 |
|
Chloroquine resistance in Plasmodium falciparum malaria parasites conferred by pfcrt mutations. | 2002 Oct 4 |
|
Monitoring the drug-sensitivity of Plasmodium falciparum in coastal towns in Madagascar by use of in vitro chemosensitivity and mutation detection tests. | 2002 Sep |
|
Amodiaquine for treating malaria. | 2003 |
|
Evaluation of the quality of amodiaquine and sulphadoxine/pyrimethamine tablets sold by private wholesale pharmacies in Dar Es Salaam Tanzania. | 2003 Apr |
|
Antibody responses to Plasmodium falciparum merozoite surface protein-1 and efficacy of amodiaquine in Gabonese children with P. falciparum malaria. | 2003 Apr 1 |
|
Questions about the antimalarial amodiaquine. | 2003 Apr 5 |
|
Molecular epidemiology of malaria in Cameroon. XV. Experimental studies on serum substitutes and supplements and alternative culture media for in vitro drug sensitivity assays using fresh isolates of Plasmodium falciparum. | 2003 Aug |
|
Short report: association between chloroquine and amodiaquine resistance and allelic variation in the Plasmodium falciparum multiple drug resistance 1 gene and the chloroquine resistance transporter gene in isolates from the upper Nile in southern Sudan. | 2003 Aug |
|
Chloroquine efficacy in the treatment of uncomplicated malaria at three sentinel sites in northern Togo. | 2003 Dec |
|
Atovaquone and proguanil versus amodiaquine for the treatment of Plasmodium falciparum malaria in African infants and young children. | 2003 Dec 1 |
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Distinguishing recrudescence from reinfection in a longitudinal antimalarial drug efficacy study: comparison of results based on genotyping of msp-1, msp-2, and glurp. | 2003 Feb |
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Comparative efficacy of aminoquinoline-antifolate combinations for the treatment of uncomplicated falciparum malaria in Kampala, Uganda. | 2003 Feb |
|
Epidemiological models for the spread of anti-malarial resistance. | 2003 Feb 19 |
|
High-performance liquid chromatographic method for determination of amodiaquine, chloroquine and their monodesethyl metabolites in biological samples. | 2003 Jan 15 |
|
Efficacy of amodiaquine alone and combined with sulfadoxine-pyrimethamine and of sulfadoxine pyrimethamine combined with artesunate. | 2003 Jun |
|
Safety, efficacy and determinants of effectiveness of antimalarial drugs during pregnancy: implications for prevention programmes in Plasmodium falciparum-endemic sub-Saharan Africa. | 2003 Jun |
|
A randomized comparison of chloroquine and chloroquine plus ketotifen in the treatment of acute, uncomplicated, Plasmodium falciparum malaria in children. | 2003 Mar |
|
[Efficacy of amodiaquine and sulfadoxine/pyrimethamine in the treatment of malaria not complicated by Plasmodium falciparum in Nariño, Colombia, 1999-2002]. | 2003 Mar |
|
Conductometric and indirect AAS determination of antimalarials. | 2003 Mar 26 |
|
Chloroquine, sulfadoxine-pyrimethamine and amodiaquine efficacy for the treatment of uncomplicated Plasmodium falciparum malaria in Upper Nile, south Sudan. | 2003 Mar-Apr |
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Effect of intermittent treatment with amodiaquine on anaemia and malarial fevers in infants in Tanzania: a randomised placebo-controlled trial. | 2003 May 31 |
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Vendor-to-vendor education to improve malaria treatment by private drug outlets in Bungoma District, Kenya. | 2003 May 7 |
|
Polymorphism in two merozoite surface proteins of Plasmodium falciparum isolates from Gabon. | 2003 May 9 |
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[Misunderstood neurological side effects of amodiaquine: apropos of 35 cases in children at Central University Hospital of Yopougon at Abidjan, Côte d' Ivoire]. | 2003 Nov |
|
Antimalarial compounds: from bench to bedside. | 2003 Nov |
|
Isoquine and related amodiaquine analogues: a new generation of improved 4-aminoquinoline antimalarials. | 2003 Nov 6 |
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Amodiaquine treatment of uncomplicated malaria in children, in an area of chloroquine-resistant Plasmodium falciparum in north-central Nigeria. | 2003 Oct |
|
The efficacy of antimalarial monotherapies, sulphadoxine-pyrimethamine and amodiaquine in East Africa: implications for sub-regional policy. | 2003 Oct |
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Prevention of increasing rates of treatment failure by combining sulfadoxine-pyrimethamine with artesunate or amodiaquine for the sequential treatment of malaria. | 2003 Oct 15 |
|
Plasmodium falciparum gametocytaemia in Nigerian children: before, during and after treatment with antimalarial drugs. | 2003 Sep |
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Rapid clearance of Plasmodium falciparum hyperparasitaemia after oral amodiaquine treatment in patients with uncomplicated malaria. | 2003 Sep |
|
Identification of human cytochrome P(450)s that metabolise anti-parasitic drugs and predictions of in vivo drug hepatic clearance from in vitro data. | 2003 Sep |
|
The relationship of physico-chemical properties and structure to the differential antiplasmodial activity of the cinchona alkaloids. | 2003 Sep 1 |
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Potentiation of the antimalarial action of chloroquine in rodent malaria by drugs known to reduce cellular glutathione levels. | 2003 Sep 1 |
|
Polymorphism in the Plasmodium falciparum chloroquine-resistance transporter protein links verapamil enhancement of chloroquine sensitivity with the clinical efficacy of amodiaquine. | 2003 Sep 19 |
|
Antimalarial drug toxicity: a review. | 2004 |
|
[Pyrido [3,2-b]indol-4-yl-amines--synthesis and investigation of activity against malaria]. | 2004 Apr |
|
In vitro efficacy of antimalarial drugs against Plasmodium vivax on the western border of Thailand. | 2004 Apr |
|
Antimalarial efficacy of sulfadoxine-pyrimethamine, amodiaquine and a combination of chloroquine plus sulfadoxine-pyrimethamine in Bundi Bugyo, western Uganda. | 2004 Apr |
|
Human liver aldehyde oxidase: inhibition by 239 drugs. | 2004 Jan |
|
Effects of solvent composition and ionic strength on the interaction of quinoline antimalarials with ferriprotoporphyrin IX. | 2004 Jan |
|
Selective and sensitive liquid chromatographic assay of amodiaquine and desethylamodiaquine in whole blood spotted on filter paper. | 2004 Jan 5 |
Patents
Sample Use Guides
For the treatment of acute malarial attacks in non-immune subjects: 600 mg of the base, followed by 200 mg after 6 hours, then 400 mg daily on each of the subsequent two days. Doses may be taken with meals to lessen gastric upset.
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/9825729
The FCR3 strain of Plasmodium falciparum was synchronized and cultivated to the trophozoite stage. Synchronized cultures were seeded at the ring stage and allowed to grow for another 20 hr until most parasites reached the trophozoite stage; parasitemia and cell number were determined, and cultures were cultured 6 drug for 1,2,3 and 4 h. One milliliter of culture was washed twice in wash medium (culture medium without plasma, 37°) to remove the drug, and cells were seeded in 24-well culture plates in full culture medium supplemented with 5 mCi/mL of [3H]hypoxanthine. After 4 hr of further cultivation, triplicate samples were transferred into 96-well plates, and parasiteassociated radioactivity was determined using the Filtermate/Matrix 96 Direct Beta counter. Inhibition of parasite growth was calculated compared to untreated controls.
Substance Class |
Chemical
Created
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admin
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Record UNII |
HOE64181MP
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SOLVATE->ANHYDROUS | |||
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PARENT -> SALT/SOLVATE |
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ACTIVE MOIETY |