Artemisinin(qinghaosu), is a drug used for treatment of malaria. It is extracted from the Chinese herb Artemisia annua. It has three major derivatives— Artemether, Artesunate and Dihydroartemisinin

1. Artemisinin
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2.  Artemisinin (qinghaosu), extracted from
the Chinese herb Artemisia annua.
 It has three major derivatives—
Artemether, Artesunate and
Dihydroartemisinin
 This drug is identified as antimalarial and
found active against all species of the
malaria parasite.
 Since the early 1980s, artemisinin and its
derivatives have been found efficacious
against Schistosoma spp., notably larval
parasites, and artemisinin derivatives
have played a critical role in the
prevention and treatment of human
schistosomiasis in China.
 Schistosomiasis, caused by the infection
with the blood flukes of the genus
Schistosoma, is a major neglected
parasitic disease in the tropical and
subtropical regions.

3. DERIVATIVES OF ARTEMISININ
1. Artemether:
• Artemether is a methyl
ether derivative of
artemisinin.
• Active against S.
japonicum
• It may interact with
haemin & then cleave the
endoperoxide bridge &
generate free radicals
that may form covalent
bond with schistosome
specific proteins.

4. 2. Artesunate:
• It ha an antischistosomal
action.
• Given in a combination with
Praziquantel.
• It causes ligamental
alterations & inhibition on
energy metabolism of
schistosomes.
• Recently it is found that it
kills schistosome parasites
through reducing the
expression of schiotosome
glutathione reductase &
cytochrome C peroxidase

5. 3.
Dihydroartimesinin:
C-10 lactone group is
replaced by a
hemiacetal.
Given in combinaton
with piperaquine.

6. MECHANISM OF ACTION
 Artemisinins are prodrugs of the biologically active
metabolite dihydroartemisinin, which is active during the
stage when the parasite is located inside red blood
cells.
 Although there is no consensus regarding the
mechanism through which artemisinin derivatives kill
the parasites.
 Several lines of evidence indicate that artemisinins
exert their antimalarial action by radical formation that
depends on their endoperoxide bridge.
 When the parasite that causes malaria infects a red
blood cell, it consumes hemoglobin within its digestive
vacuole, a process that generates oxidative stress.

9.  Haemozoin is parasite pigment
deposited within a food vacuole after
digestion of haemoglobin.
 The iron of the heme
directly reduces the peroxide bond in
artemisinin, generating high-valent iron-
oxo species and resulting in a cascade
of reactions that produce reactive
oxygen radicals (disrupts cellular redox
cycle) which damages the parasite and
lead to its death.

10. DOSING
 Artemisinin derivatives have half-lives of
the order of an hour, and therefore
require at least daily dosing over several
days.
 the WHO-approved adult dose of co-
artemether is 4 tablets at 0, 8, 24, 36, 48
and 60 hours (six doses)
 Artemisinin is not soluble in water,
therefore Artemisia annua tea was
postulated not to contain
pharmacologically significant amounts of
artemesinin.

11. ADVERSE EFFECTS
 Side effects:
1. Vomiting
2. Nausea
3. Anorexia
4. dizziness
5. Mild blood abnormalities
 Adverse effects:
i. allergic reaction
ii. significant liver inflammation

12. REFERENCES
 www.wikipedia.com
 Zhang J.-F. Yang Cheng Evening News
Publishing Company; 2005. A Detailed
Chronological Record of Project 523 and
the Discovery and Development of
Qinghaosu (Artemisinin)
 Kremsner P.G., Krishna S. Antimalarial
combinations. Lancet. 2004;364:285–
294. [PubMed]