Amodiaquine
(Synonyms: 阿莫地喹,Amodiaquin) 目录号 : GC42790
A prodrug form of N-desethyl amodiaquine
Cas No.:86-42-0
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Amodiaquine is an aminoquinoline antimalarial compound. It is metabolized primarily by cytochrome P450 2C8 to N-desethylaminodiaquine, which is highly active against P. falciparum and can synergize with amodiaquine. Amodiaquine is commonly used in combination therapy.
| Cas No. | 86-42-0 | SDF | |
| 别名 | 阿莫地喹,Amodiaquin | ||
| Canonical SMILES | OC(C=C1)=C(CN(CC)CC)C=C1NC2=CC=NC3=C2C=CC(Cl)=C3 | ||
| 分子式 | C20H22ClN3O | 分子量 | 355.9 |
| 溶解度 | DMF: 2.5 mg/ml,DMSO: 5 mg/ml,Ethanol: 2 mg/ml | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.8098 mL | 14.0489 mL | 28.0978 mL |
| 5 mM | 0.562 mL | 2.8098 mL | 5.6196 mL |
| 10 mM | 0.281 mL | 1.4049 mL | 2.8098 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Amodiaquine pharmacogenetics
Pharmacogenomics 2008 Oct;9(10):1385-90.PMID:18855526DOI:10.2217/14622416.9.10.1385.
Amodiaquine is a central drug in the new global strategy of combination therapies for the control of malaria. Amodiaquine is mainly metabolized hepatically towards its major active metabolite desethylamodiaquine, by the polymorphic P450 isoform CYP2C8. Amodiaquine is associated with rare but serious side effects, as well as with relatively frequent mild ones. These are expected to be at least partially related to CYP2C8 alleles. Pharmacogenetic knowledge of Amodiaquine exposed populations is important for pharmacovigilance issues and in being a first step for future realistic applications from a personal medicine perspective.
Amodiaquine for treating malaria
Cochrane Database Syst Rev 2000;(2):CD000016.PMID:10796468DOI:10.1002/14651858.CD000016.
Background: Amodiaquine has been widely used to treat malaria. Due to reports of fatal adverse drug reactions, discontinuation or modification of its use has been suggested. Objectives: The objective of this review was to assess the effects of Amodiaquine for treating malaria. Search strategy: We searched the Cochrane Infectious Diseases Group trials register and Medline. We also contacted researchers in the field and drug companies. Selection criteria: Randomised and quasi-randomised trials comparing Amodiaquine with other treatment for uncomplicated malarial infections in adults and children. Data collection and analysis: Both reviewers independently extracted data and assessed trial quality. Main results: Forty trials were included. Allocation was adequately concealed in three trials. Amodiaquine was more effective than chloroquine for parasite clearance. The combined results of parasite clearance at seven days from 24 trials was 83% for Amodiaquine and 56% for chloroquine (odds ratio 4.29, 95% confidence interval 3.51 to 5.24). The odds ratio for parasite clearance at 14 days was 6.00, 95% confidence interval 4.38 to 8.21. Amodiaquine and sulfadoxine/pyrimethamine showed similar results for parasite clearance on day seven, but sulfadoxine/pyrimethamine appeared to be more effective on day 14 and 28. No significant difference for adverse events was observed between Amodiaquine and chloroquine and sulfadoxine/pyrimethamine. Reported adverse effects were minor or moderate, not life threatening. Reviewer's conclusions: There is some evidence to support the continued use of Amodiaquine in the treatment of uncomplicated malaria, although drug resistance should be considered. Monitoring for toxicity should also continue.
Amodiaquine for treating malaria
Cochrane Database Syst Rev 2003;(2):CD000016.PMID:12804382DOI:10.1002/14651858.CD000016.
Background: Amodiaquine has been widely used to treat malaria. Fatal adverse reactions have been reported in adults taking it for prophylaxis. This has led some authorities to suggest it is withdrawn as a first line treatment for malaria. Objectives: To compare Amodiaquine with chloroquine or sulfadoxine-pyrimethamine for treating uncomplicated Plasmodium falciparum malaria. Search strategy: We searched the Cochrane Infectious Diseases Group specialized trials register (February 2003), The Cochrane Central Register of Controlled Trials (The Cochrane Library Issue 1, 2003), MEDLINE (1966 to February 2003), EMBASE (1980 to December 2002), LILACS (February 2003). We contacted researchers in the field and pharmaceutical companies. Selection criteria: Randomised and quasi-randomised trials. Data collection and analysis: Two reviewers independently extracted data and assessed trial quality. Main results: 56 studies included, mostly from Africa. Treatment allocation was adequately concealed in three trials, and unclear or inadequate in the remainder. Amodiaquine was more effective than chloroquine for parasite clearance (day 7, Peto odds ratio 4.42 (95% confidence interval 3.65 to 5.35); day 14, Peto odds ratio 6.44 (95% confidence interval (CI) 5.09 to 8.15). Comparisons with sulfadoxine/pyrimethamine were more mixed, with sulfadoxine/pyrimethamine more effective on day 28 (Peto odds ratio 0.41; 95% CI 0.28 to 0.61). No significant difference for adverse events was observed between Amodiaquine and chloroquine and sulfadoxine/pyrimethamine. Reported adverse effects were minor or moderate. No life threatening events were detected. Reviewer's conclusions: There is evidence to support the continued use of Amodiaquine to treat uncomplicated malaria, although local drug resistance patterns need to be considered. Monitoring for adverse events should continue.
Artesunate-amodiaquine for the treatment of uncomplicated malaria
Expert Opin Investig Drugs 2007 Jul;16(7):1079-85.PMID:17594191DOI:10.1517/13543784.16.7.1079.
Without an effective vaccine for the prevention of malaria, a fundamental component of the strategy for the control of this disease is based on prompt and effective treatment. Due to the high resistance level of Plasmodium falciparum to the most affordable drugs such as chloroquine and sulfadoxine-pyrimethamine, artemisinin-based combination therapies are presently used in many countries or are being developed for registration. One artemisinin combination therapy that is drawing a certain degree of interest is the combination of artesunate (a short half-life drug) plus Amodiaquine (a long half-life drug that is presently used in loose combination in many countries). The short half-life drug achieves substantial and rapid parasite killing, while a high concentration of the long half-life drug kills off the remaining malaria parasites. In addition to the effectiveness of 3 days of treatment (rapid clearance of fever and malaria parasites) in western and central Africa, where resistance to Amodiaquine is low, the combination of artesunate plus Amodiaquine may delay or prevent the emergence of resistance to both drugs. An important step is the recent registration in Morocco (the country where the drug is manufactured) of a fixed combination of artesunate plus Amodiaquine by the Drugs for Neglected Diseases initiative with sanofi-aventis as the industrial partner. A prequalification dossier of this fixed combination has been submitted to the WHO. This new co-formulation will almost certainly increase its effectiveness by improving drug compliance.
Amodiaquine agranulocytosis
Med J Aust 1977 Feb 26;1(9):298-9.PMID:859490DOI:10.5694/j.1326-5377.1977.tb130706.x.
A case of profound neutropenia and severe infection after the administration of Amodiaquine is presented. The recommended dose for malaria prophylaxis was administered.