Sesquiterpene with an endoperoxide moeity
Active against all human malarial parasites, including multi-drug resistant Plasmodium falciparum strains.
Several proposed including the production of free radicals, other reactive metabolites, and altered membrane transport properties of membranes which may inhibit nutrient flow to the parasite.
No data available
2.4mg/kg dose in adult patients with P. falciparum malaria: Cmax: 11,330 mcg/L; Half-life: 2.7 hours; Volume of distribution: 0.14 L/kg; Table 2
Cardiac: QTc prolongation, bradycardia
GI: Nausea, vomiting, diarrhea, constipation
Central nervous system: headache, tinnitus
Hematologic: Reversible reductio in reticulocyte and neutrophil counts
The conventional i.v. and i.m. dose regimen for severe malaria is 120 mg initially, followed by 60 mg at 4, 24 and 48 h. In some cases, therapy is continued for 5 days.
Co-therapy with mefloquine (15-25 mg/kg), as either a single or divided dose (4-6 h apart) is started when the patient can tolerate oral therapy (normally at 24 or 48 h).
Parenteral dose regimens in uncomplicated falciparum malaria are usually 60-120 mg initially (i.v. or i.m.), followed by 60 mg at 24 and 48 h, with mefloquine (15-25 mg/kg) at 24 or 48 h).
There has been a trend to administer ARTS as a single or divided dose over 24 h total dose = 3-4 mg/kg), with mefloquine (15-25 mg/kg) at 24 h if the patient is aparasitaemic.
The standard oral dose regimen in uncomplicated P. falciparum malaria is 100-200 mg initially, then 100 mg daily for a further 2-4 days. However, ARTS has been used at doses of up to 16 mg/kg/day.
There is no evidence that parenteral artesunate therapy is better than oral therapy, which may be more convenient in the primary care setting and during convalescence.
The recommended rectal dose of artesunate is 10-20 mg/kg/day
No data available
Contraindications/Warnings/Precautions:
No data available
Concomitant administration of artesunate and mefloquine leads to a decreased Cmax and increased oral clearance of mefloquine, however there was no difference in total exposure. It is recommended that mefloquine be administered at least 24 hours after artesunate
Not established. The World Health Organization currently advises against the use of artemisinins in the first trimester of pregnancy, unless in a lifesaving situation where other drugs are not suitable. In the second and third trimesters of pregnancy, artemisinin and its derivatives are not recommended unless alternative drug treatments are unsuitable.
None
PLASMOTRIM (Mepha – THAILAND, BRAZIL)