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α/β Arteether Injection |
R
A P I T H E R - AB |
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| DESCRIPTION |
| Rapither
AB (α/β arteether) is a synthetic derivative of
artemisinin, a product of Chinese plant Artemisia annua.
Rapither AB (α/β arteether) is a fast acting blood
schizontocide specifically indicated for the treatment of
chloroquine resistant P. falciparum malaria and cerebral malaria
cases. |
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| COMPOSITION |
| Each 2 ml contains: |
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| α / β arteether |
150mg |
| Arachis oil |
q.s. |
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| MECHANISM
OF ACTION |
| α
/ β arteether is a fast acting blood schizonticidal agent
for P. falciparum malaria at the erythrocytic stage.
α /β arteether is concentrated in parasitized erythrocytes.
The functional group responsible for antimalarial activity
of α / β arteether is endoperoxide bridge. Iron
from the digested haemoglobin of the parasite's victim reduces
this bridge, releasing a highly reactive free radical iron
species which causes lysis of the parasitic cell.
Lysis of parasitic cell membrane occurs. Damage includes swelling
and deformity of food vacuoles membrane, nuclear membrane,
endoplasmic reticulum and formation of autophagic vacuoles.
It is also proposed that α / β arteether inhibits
the protein synthesis and alters the ribosomal organization
and endoplasmic reticulum. |
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| PHARMACOKINETICS |
| α
/ β arteether is transformed into dihydroartemisinin.
It has a half life of 20 hours. It is eliminated by hepatic
metabolism. The elimination is much slower compared to other
compounds. |
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| INDICATIONS |
| Severe
malaria including cerebral malaria and as a second line drug
in chloroquine resistant malaria cases only. |
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| CONTRAINDICATIONS |
| α
/ β arteether injection is contraindicated in patients
hypersensitive to artemisinin derivatives. |
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| PRECAUTIONS |
| Pregnancy
- Adequate studies regarding safe use of artemisinin
derivatives during pregnancy are not available. Artemisinin
derivatives should not be used in pregnancy as primary drugs
for uncomplicated malaria cases but these can be used for
treatment of severe or complicated P. falciparum malaria infection
in patients of multiple drug resistance, if the potential
benefit justifies the potential risk to the fetus.
Nursing mothers - It is not known whether
α / β arteether is excreted in human milk. Because
many drugs are excreted in human milk caution should be exercised
while using &alpha / β arteether. |
| Drug
interactions |
| Prolonged
QT interval has been reported in some studies with high dosage
of artemisinin derivatives. The cardiac effects of artemisinins
are not very important from a clinical point of view, except
that caution should be exercised against combinations with
other drugs that prolong the QT interval, such as quinine
and halofantrine. |
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| ADVERSE
EFFECTS |
| While
neurotoxicity has been reported in experimental animals, there
is no evidence of neurotoxicity in human beings with artemisinin
derivatives.
&alpha / β arteether is usually well tolerated. However,
nausea, dizziness and depressed GIT activity can occur. Clinical,
neurological, electrocardiographic and biochemical monitoring
did not reveal significant toxicity.
Apart from some increase in eosinophil numbers, no haematological
abnormality was seen. |
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| DOSAGE
AND ADMINISTRATION |
α / β arteether is for intramuscular use only.
Adult - 150mg i.e. 1 ampoule of b arteether
once daily for 3 consecutive days.
Children - 3mg/Kg per day administered
by intramuscular injection over a 3-day period
The injection must be given under aseptic conditions, deep
intramuscularly in the upper lateral quadrant of the buttock.
No other drug should be mixed in the same syringe.
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| Storage |
| Store
in cool dark place . |
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| Presentation |
| Rapither
3 x 2ml |
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