Artemether Injection 40MG / ML 80MG / ML Anti Malaria 6AMPULES /
ARTEMETHER INJECTION 40MG 80MG/1ML
Each 1mL ampule contains:40MG 80MG Artemether.
Artemether is synthetised from Artemisinin using methanol and a
catalyst in hydrochloric acid medium. This
results in the production of predominantly βα-artemether. The
alpha-epimer is also present and causes a difficult purification of
the product.Both the alpha and the βα-epimers are active
It is the purification and separation of alpha from βαthat leads to
low yields and hence this increases the cost
price of Artemether significantly.
Artemether has major antimalarial properties.
Chloroq-uine-resistant or multi-resistant strains of P.falciparum
have a great susceptibility to Artemether. The schizont-icidal
activity of Artemther is due to the destruction of the asexual
erythrocytic forms of P.falciparum and P.
vivax. Artemether is effective against all strains resistant to the
other antimalarial agents. No cross-resistance is detected with
Pharmacokinetic data in humans are sparse, with no data
demonstrating the rate or extent of absorption or
the systemic distribution of artesunate. After parenteral
administration, artesunate is rapidly hydrolyzed to the
active metabolite dihydroartemisinin. The oral formulation is
probably hydrolysed completely before entering
the systemic circulation. Peak serum levels occur within one hour
of an oral dose of artesunate and persist for
up to 4 hours. Following intravenous administration, elimination
half-life of 45 minutes has been reported. Dihydroartemisinin has a
plasma elimination half-life of less than 2 hours, which may slow
the development of resistance to artesunate.
Antimalarial drug. It is indicated for the treatment of all kinds
of malarias, including the chloroquine-resistant malaria and the
first aid of fata malaria.
Artemether is contraindicated in patients with hypersensitivity to
artemether or other artemisinin compounds.
Artemether is not recommended in the first trimester of pregnancy
because of limited data.
DOSAGE AND DIRECTIONS FOR USE:
Intramuscular injection. Five days course with the dose of 480mg
for adults: once (80mg) daily for five
consecutive days with the first dose doubled. For children, the
first dose is 3.2mg/kg bodyweight, followed
with 1.6mg/kg bodyweight every time from the 2nd day to 5th day.
SIDE EFFECTS AND SPECIAL PRECAUTIONS:
Artemether has been remarkably well-tolerated, and appears less
toxic than quinine or chloroquine; adverse effects include
electrocardiogram abnormalities, gastrointestinal disturbances
(nausea, abdominal pain, diarrhoea - oral
therapy only), dizziness, injection site pain, skin reactions, and
fever. Transient decreases in neutrophils and
reticulocytes have been reported in some patients treated with
Drug induced fever has been observed with artemether. Mild
reactions were seen in patients to whom
artemether had been administered intramuscularly. These included
nausea, hypotension, dizziness and tinnitus.
These side effects were also reported: dark urine, sweating,
somnolence, and jaundice. There were no deaths
or any other side effects. No irreversible side effects were seen.
Slight rise of SGOT and SGPT may occur in individual cases.
Neurological side effects have not yet been
observed in clinical use but clinical trials suggest that coma may
be prolonged in patients treated with artemether and there was an
increased incidence of convulsions in one trial in cerebral
malaria. Transient first degree
heart block has been documented in three patients receiving
Neurotoxicity has been observed in animal studies but not in
Cardiotoxicity has been observed following administration of high
doses of Artemether.
Studies and reviews in the literature demonstrated that the active
substance of Artemether had no interactions with other drugs on
decreasing therapeutic effects and increasing toxicity and side
effects in human bodies.
Although no case of overdosage has been documented, in case of
accident, symptomatic treatment is
recommended under the instruction of doctors.
Preserve in well closed container,protected from light and stored
in a cool place.