Artemether + Lumefantrine

Indications

Artemether + Lumefantrine is used for: Acute uncomplicated malaria, Falciparum malaria

Adult Dose

Oral Adults (weighing 35 kg and above): Administer 24 tablets over 3 days; use a 3-day treatment schedule with total of 6 doses. Day 1: 4 tablets initially and 4 tablets again after 8 hours. Days 2 & 3: 4 tablets BID (morning & evening).

Child Dose

Oral Children (weighing 35 kg and above or more than 12 years of age): Administer 24 tablets over 3 days; use a 3-day treatment schedule with total of 6 doses. Day 1: 4 tablets initially and 4 tablets again after 8 hours. Days 2 & 3: 4 tablets BID (morning & evening). Children: < 12 years 5 to <15 kg: Administer 6 tablets over 3 days; 1 tablet initially and again after 8 hours on first day; follow by 1 tablet BID (morning & evening) for the next 2 days. 15 to <25 kg: Administer 12 tablets over 3 days; 2 tablets initially and again after 8 hours on first day; follow by 2 tablets BID (morning & evening) for the next 2 days. 25 to <35 kg: Administer 18 tablets over 3 days; 3 tablets initially and again after 8 hr on 1st day; follow by 3 tablets BID (morning & evening) for the next 2 days.

Renal Dose

Administration

Should be taken with food.

Contra Indications

Hypersensitivity.

Precautions

Pregnancy and lactation. Avoid concomitant use of drugs known to prolong QT interval or monitor such patients. Lactation: not known if either component enters breast milk, use caution

Pregnancy-Lactation

Pregnancy Published data from clinical studies and pharmacovigilance data have not established an association between drug use during pregnancy and major birth defects, miscarriage, or adverse maternal or fetal outcomes Malaria during and after pregnancy increases risk for adverse pregnancy and neonatal outcomes, including maternal anemia, severe malaria, spontaneous abortion, stillbirths, preterm delivery, low birth weight, intrauterine growth restriction, congenital malaria, and maternal and neonatal mortality Contraception May reduce efficacy of hormonal contraceptives; advise patients using hormonal contraceptives to use an alternative non-hormonal contraceptive method or add a barrier method of contraception during treatment Infertility In animal fertility studies, administration of repeated doses to female rats (for 2 to 4 weeks) resulted in pregnancy rates that were reduced by one half Male rats dosed for approximately 3 months, abnormal sperm cells, showed decreased sperm motility, and increased testes weight Lactation There are no data on presence of drug in human milk, effects on breastfed infant or on milk production; drug components are transferred into rat milk; when a drug is transferred into animal milk, it is likely that the drug will also be transferred into human milk The developmental and health benefits of breastfeeding should be considered along with the mother’s clinical need for therapy and any potential adverse effects on breastfed infant from drug or from underlying maternal condition

Interactions

Artemether causes QT prolongation in some patients. Thus concomitant use of erythromycin, terfenadine, procainamide, quinidine, disopyramide, amiodarone, bretylium, bepridil, sotalol, astemizole, probucol, tricyclic antidepressants, phenothiazines may be avoided.

Adverse Effects

Side effects of Artemether + Lumefantrine : >10% Abdominal pain (17%), Anorexia (40%), Arthralgia (34%), Asthenia (38%), Chills (23%), Dizziness (39%), Fatigue (17%), Headache (56%), Myalgia (32%), Nausea (26%), Palpitations (18%), Pyrexia (25%), Sleep disorder (22%), Vomiting(17%) 1-10% Anemia (4%), Cough (6%), Diarrhea (7%), Hepatomegaly (9%), Malaise (3%), Nasopharyngitis (3%), Pruritus (4%), Rash (3%), Splenomegaly (9%), Vertigo (3%)

Mechanism of Action

Artemether is a potent and rapidly acting blood schizontocide. Artemether and active metabolite (DHA): via endoperoxide. Lumefantrine: unknown; possibly inhibits beta-hematin formation Both artemether and lumentantrine inhibit nucleic acid and protein synthesis