Artemether Injection 40MG / ML 80MG / ML Anti Malaria Medicine BP / USP

Artemether Injection 40MG / ML 80MG / ML Anti Malaria 6AMPULES / BOX

ARTEMETHER INJECTION 40MG 80MG/1ML

COMPOSITION:

Each 1mL ampule contains:40MG 80MG Artemether.

PHARMACOLOGICAL ACTION:
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 antimalarials.
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 chloroquine.

PHARMACOKINETICS:

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.

INDICATIONS:
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.

CONTRA-INDICATIONS:
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 bradycardia,

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 artemether.
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 artemether.
Neurotoxicity has been observed in animal studies but not in humans.
Cardiotoxicity has been observed following administration of high doses of Artemether.

DRUG INTERACTIONS:

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.

OVERDOSE:

Although no case of overdosage has been documented, in case of accident, symptomatic treatment is

recommended under the instruction of doctors.

STORAGE INSTRUCTIONS:
Preserve in well closed container,protected from light and stored in a cool place.