Monograph: |
Artemether
COMPOSITION
LARITHER Injection
Each ml contains
Artemether 80 mg
LARITHER Capsules
Each capsule contains
Artemether 40 mg
CHEMISTRY
Artemether is the methyl ether of dihydroartemisinin. Artemisinin is a novel Sesquiterpene
Lactone and possesses a Endoperoxide bridge which is a rare feature in natural products.
PHARMACOLOGY
Artemether is active against all Plasmodia including those which may be resistant to other
antimalarials.
The schizonticidal activity of artemether is mainly due to destruction of the asexual
Erythrocytic forms of P. falciparum and P. vivax. There is inhibition of protein synthesis during
growth of trophozoites. There is no cross resistance with chloroquine.
After Intramuscular administration peak plasma concentrations are attained within about
6 hours.
CUNICAL EFFICACY
In multicentric clinical trial conducted in India, the average mean fever clearance time (PCT)
was 40.33 hours with Larither Injection and 30.08 hours with Larither Capsules.
The average mean parasite clearance time (PCT) - as observed in the above mentioned trial -
was 32.52 hours with Larither Injection and 40.32 hours with Larither Capsules.
INDICATIONS
Severe malaria including cerebral malaria and as a second line drug in chloroquine resistant
malaria cases only.
DOSAGE AND ADMINISTRATION
LARITHER Injection : Artemether Injection is for intramuscular use only. Total adult dose
should not exceed 480 mg in adults and 9.6 mg / kg in children.
The injection must be given in aseptic conditions in the upper external quadrant of the buttock
Association with other drugs in the same syringe should be avoided.
Adults : 1 ampoule containing 80mg twice a day by 1.M. route (160 mg/day) for 1st day
followed by 1 ampoule containing 80 mg once a day by I.M. injection for the next four days.
Children : 1.6 mg/kg twice a day \M. injection on the first day and 1.6 mg/kg once a day for
the next four days.
LARITHER Capsules
Adults : 4 capsules (160 mg) given in two divided doses 12 hourly on 1st day followed by 2
capsules (80 mg) once daily for 4 days.
The total dosage recommended for Arternether Capsules is 480 mg.
Children : 1.6 mg/kg of bodyweight (as given under Larither Injection)
DRUG INTERACTIONS
Since electrocardiographic QT prolongation has been reported in some patients treated with
artemether, it is recommended to avoid prescription of medications known to produce a
prolongation of QT interval or patients receiving such medication :
Erythromycin, Terfenadine, Astemizole, Probucol, Class la anti-arrhythmic agents (Quinidine,
Procainamide, Disopyramide), Class III anti-arrythmic agents (Amiodarone, Bretylium),
Bepridil, Sotalol, Tricyclic antidepressants, some Neuroleptics and Phenothiazines are to be
monitored closely.
ADVERSE DRUG REACTIONS
Decrease in reticutocytes count, slight rise of SGOT and SGPT may occur in individual cases.
Cardiotoxicity has been observed following administration of high doses of Artemether.
PRECAUTIONS AND WARNINGS
1. Do not exceed the prescribed dose. In case of overdosage, urgent symptomatic treatment
in a specialized unit is required.
Z.EtectrocardiogtaphicOT prolongation has been reported in some patients treated with
Artemether.
3. It is not known whether Artemether is secreted in human milk. Because many drugs are
secreted in human milk, caution should be exercised when Artemether is used by nursing
women.
CONTRAINDICATION
Artemether Injection and Capsules are contraindicated in pregnancy unless the doctor
considers it essential (as in the case of cerebral malaria).
PRESENTATION
LARITHER Injection Box of 6x1 ml
LARITHER Capsules Strip of 6's
STORAGE -
LARITHER Injection
Store in a cool dark place.
LARITHER Capsules
Store in a cool dry dark place.
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