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| β
Arteether Injection |
B E T A M O T I L |
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| DESCRIPTION |
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β arteether is
a synthetic derivative of artemisinin, a product of Chinese
plant Artemisia annua. It is oil soluble ethyl ether derivative
of dihydroartemisinin.
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 2ml contains: |
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| β arteether |
150mg |
| Arachis oil |
q.s. |
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| MECHANISM
OF ACTION |
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β arteether is
a fast acting blood schizonticidal agent for P. falciparum
malaria at the erythrocytic stage.
β arteether is concentrated in parasitized erythrocytes.
The functional group responsible for antimalarial activity
of 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 β arteether inhibits the protein
synthesis and alters the ribosomal organization and endoplasmic
reticulum.
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| PHARMACOKINETICS |
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β arteether is
transformed into dihydroartemisinin. It has a half life of
1 to 2 days. It is eliminated by hepatic metabolism. The elimination
is much slower compared to other compounds. It is more stable
and more lipophilic than other artemisinin compounds.
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| INDICATIONS |
β
arteether is indicated for severe malaria including cerebral
malaria and as a second line drug in chloroquine resistant malaria
cases only.
It is not recommended for the treatment of malaria caused by
P. vivax, P. ovale and P. malariae since other effective antimalarial
drugs are available for this purpose |
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| CONTRAINDICATIONS |
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β arteether injection
is contraindicated in patients hypersensitive to artemisinin
derivatives.
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| PRECAUTIONS |
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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
β arteether is excreted in human milk. Because many drugs
are excreted in human milk caution should be exercised while
using β arteether.
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| Drug
interactions |
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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 |
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While neurotoxicity
has been reported in experimental animals, there is no evidence
of neurotoxicity in human beings with artemisinin derivatives.
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 |
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 |
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Store in cool dark place
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| Presentation |
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Betamotil Injection
3 x 2ml
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