EUROPEAN JOURNAL OF
PHARMACEUTICAL AND MEDICAL RESEARCH

( An ISO 9001:2015 Certified International Journal )

An International Peer Reviewed Journal for Pharmaceutical, Medical & Biological Sciences

An Official Publication of Society for Advance Healthcare Research (Reg. No. : 01/01/01/31674/16)

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 ISSN 2394-3211

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Abstract

PHARMACOLOGICAL ASPECT OF ARTEMISININ AND ARESUNATE AS POTENT ANTI MALARIAL AGENTS - OVERVIEW

Fateh AL Rahman Magbool* and Salah Eldin Omar Hussein

ABSTRACT

Artemisia annua. It comprises a new generation of antimalarial compounds that feature a nitrogenfree sesquiterpene lactone. Because artemisinin itself has physical properties such as poor bioavailability that limit its effectiveness, semi-synthetic derivatives of artemisinin, including artemether (ARM), artemotil, arteether, artenimol, and artesunate (ARST), have been developed, and are known as more effective than its parent material- artemisinin. Since 2001 the World Health Organization has recommended using artemisinin-based combination therapy (ACT) as first-line treatment for uncomplicated malaria in areas experiencing resistance to older medications. In Sudan Artesunate-SP combination is most common. Artesunate is an antimalarial agent. It is a water-soluble hemisuccinate derivative of artemisinin. Artesunate and its active metabolite dihydroartemisinin are potent blood schizonticides, active against the ring stage of the parasite. Artesunate is powerful especially in the treatment of advanced and potentially lethal cases of P. falciparum infection. It is a sesquiterpene with an unusual endoperoxide linkage structurally unrelated to other known antimalarials. ARST was developed as a pro-drug for the treatment of both uncomplicated and severe P. falciparum malaria. It is available in both enteral and parenteral formulations. It is more potent than artemisinin and is active by virtue of the endoperoxide. Their activity against strains of the parasite that had become resistant to conventional chloroquine therapy and the ability due to its lipophilic structure, to cross the blood brain barrier, it was particularly effective for the deadly cerebral malaria. Oral artesunate is hydrolyzed rapidly back to the metabolite dihydroartemisinin (DHA), which is intrinsically more active as antimalaria agent, as this metabolite is the main contributor to the overall antimalaria activity. Artemisinin and its analogs appear to be better tolerated than most antimalarials. In recent times, emergence resistant of Plasmodium sp to many of the cheap and readily available antimalarials has resulted in the continued use and dependence of artemisinins and its based combination. In Sudan, artesunate tablet is the commonest artemisinin product in the market and is available in various strengths from both local and foreign manufacturers. The quality of these antimalarials if not properly safeguarded could lead to therapeutic failure in patients and the development of drug resistance.

Keywords: Artemisinin (ARN), Artemisia annua, schizonticides.


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Google Scholar Indian Science Publications InfoBase Index (In Process) SOCOLAR, China Research Bible, Fuchu, Tokyo. JAPAN International Society for Research activity (ISRA) Scientific Indexing Services (SIS) Polish Scholarly Bibliography Global Impact Factor (GIF) (Under Process) Universal Impact Factor International Scientific Indexing (ISI), UAE Index Copernicus CAS (A Division of American Chemical Society) USA (Under Process) Directory of Open Access Journal (DOAJ, Sweden, in process) UDLedge Science Citation Index CiteFactor Directory Of Research Journal Indexing (DRJI) Indian citation Index (ICI) Journal Index (JI, Under Process) Directory of abstract indexing for Journals (DAIJ) Open Access Journals (Under Process) Impact Factor Services For International Journals (IFSIJ) Cosmos Impact Factor Jour Informatics (Under Process) Eurasian Scientific Journal Index (ESJI) International Innovative Journal Impact Factor (IIJIF) Science Library Index, Dubai, United Arab Emirates Pubmed Database [NLM ID: 101669306] (Under Process) IP Indexing (IP Value 2.40) Web of Science Group (Under Process) Directory of Research Journals Indexing Scholar Article Journal Index (SAJI) International Scientific Indexing ( ISI ) Scope Database Academia