Page 99 - 80 guidelines for the treatment of malaria_opt

N
N
CI
2
CH 3
HN
CH 3
H
NH
CH 3
2
H 3 C
F
H 3 C
F
F
F
F N CH 3 CI HN OH N CH 3 CH 3 H N H 3 C O S O N N O N O CH 3 H N N N 2 H 3 C CI
N O O O
O C O C O C
F O O O
ÿ O CH 3 ANNEX 3. Pharmacology of antimalarial medicines O O CH 3
CH 3
O
H H H H 3 C H H HO H H
HO O O O
H H H
HN A3.6.5 Artemotil CH 3 O CH 3
CH 3
Molecular weight: 312.4
CIher of artemisinin,
Artemotil is the ethyl et
H 3 C H 3 C
and is closely related to the more widely CH 3
O O used artemether. It is oil-based so water
O C O C NH 2
O O insoluble. It is given by intramuscular HN
CH 3 CH 3 injection only. CI CI N
O O
H H H H
H 3 C A3 H 3 C
HO H 3 C O O
H H
CH 3 CH 3 H 3 C N
OH
Formulations
• Ampoules containing 150 mg of artemotil in 2 ml of injectable solution.
CI Pharmacokinetics CI
H H H
N
N
N
CI
There is less published information on artemotil than for artemether. Absorption is slower O
CH 3
H NH NH CH 3
and more erratic, with some patients having undetectable plasma artemotil until more H N S NH 2
2
NH
NH
than 24 h after administration. CH 3 H H H O
CI
O N N N CH 3
H Toxicity
As for artemisinin.
OH
O
Drug interactions
None known.
H 2 C H H 3 C CH 3 OH CI
HO CH 3 H N OH O O O CH 3 O CH 3
OH OH N
NH N
N 2 H
H 3 C H O
HO H NH 2 CH 3
OH H HO S
OH H H
O OH O OH O O
H 3 C H 3 C OH N HO OH
H 3 C CH 3
N
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