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Artemether

Catalog No. DB06697 Name DrugBank
CAS Number 71963-77-4 Website http://www.ualberta.ca/
M. F. C16H26O5 Telephone (780) 492-3111
M. W. 298.37464 Fax (780) 492-1071
Purity Email david.wishart@ualberta.ca
Storage Chembase ID: 4435

SYNONYMS

IUPAC name
10-methoxy-1,5,9-trimethyl-11,14,15,16-tetraoxatetracyclo[10.3.1.0^{4,13}.0^{8,13}]hexadecane
IUPAC Traditional name
artemisinine,methyl ether (α)
Brand Name
Coartem
Synonyms
Dihydroartemisinin methyl ether

DATABASE IDS

CAS Number 71963-77-4

PROPERTIES

DETAILS

Description (English)
Item Information
Drug Groups approved
Description Artemether is an antimalarial agent used to treat acute uncomplicated malaria. It is administered in combination with lumefantrine for improved efficacy. This combination therapy exerts its effects against the erythrocytic stages of Plasmodium spp. and may be used to treat infections caused by P. falciparum and unidentified Plasmodium species, including infections acquired in chloroquine-resistant areas.
Indication Artemether and lumefantrine combination therapy is indicated for the treatment of acute uncomplicated malaria caused by Plasmodium falciparum, including malaria acquired in chloroquine-resistant areas. May also be used to treat uncomplicated malaria when the Plasmodium species has not been identified. Indicated for use in adults and children greater than 5 kg.
Pharmacology In the body, artemether is metabolized into the active metabolite metabolite dihydroartemisinin. The drug works against the erythrocytic stages of P. falciparum by inhibiting nucleic acid and protein synthesis. Artemether is administered in combination with lumefantrine for improved efficacy. Artemether has a rapid onset of action and is rapidly cleared from the body. It is thought that artemether provides rapid symptomatic relief by reducing the number of malarial parasites. Lumefantrine has a much longer half life and is believed to clear residual parasites.
Toxicity Common side effects of combination artemether/lumefantrine therapy in adults include headache, anorexia, dizziness, and asthenia. Common side effects in children include pyrexia, cough, vomiting, anorexia, and headache. Possible serious adverse effects include QT prolongation, bullous eruption, urticaria, splenomegaly (9%), hepatomegaly (adults, 9%; children, 6%), hypersensitivty reaction, and angioedema.
Affected Organisms
Plasmodium
Biotransformation Rapidly metablized to its active metabolite, dihydroartemisinin.
Absorption Food increases absorption.
Half Life Artemether, 1.6 +/- 0.7 and 2.2 +/- 1.9 hr; Dihydroartemisinin, 1.6 +/- 0.6 and 2.2 +/- 1.5 hr
Protein Binding Artemether, 95.4%; Dihydroartemisinin, 47-76%
References
Artemether and Lumefantrine (2010). AHFS Drug Information [Electronic versionb]. Retrieved October 24, 2010.
Artemether/Lumefantrine (2010). DrugPoints? System [Electronic version]. Retrieved October 24, 2010.
Novartis. Coartem (artemether/lumefantrine) tablets prescribing information. East Hanover, NJ; 2010 Feb.
External Links
Wikipedia
RxList
Drugs.com

REFERENCES

  • Novartis. Coartem (artemether/lumefantrine) tablets prescribing information. East Hanover, NJ; 2010 Feb.
  • Artemether and Lumefantrine (2010). AHFS Drug Information [Electronic versionb]. Retrieved October 24, 2010.
  • Artemether/Lumefantrine (2010). DrugPoints? System [Electronic version]. Retrieved October 24, 2010.