Artemether + Lumefantrine


Thông tin thuốc gốc
Chỉ định và Liều dùng
Oral
Acute uncomplicated falciparum malaria
Adult: Available preparation:
Artemether 20 mg and lumefantrine 120 mg

≥35 kg: Initially, 4 tab, followed by 4 tab given at 8, 24, 36, 48, and 60 hours thereafter to a total of 24 tab over 3 days.
Child: ≥2 months to ≤16 years 5-<15 kg: Initially 1 tab, followed by 1 tab given at 8, 24, 36, 48, and 60 hours thereafter; 15-<25 kg: Initially 2 tab, followed by 2 tab given at 8, 24, 36, 48, and 60 hours thereafter; 25-<35 kg: Initially 3 tab, followed by 3 tab given at 8, 24, 36, 48, and 60 hours thereafter. >16 years weighing ≥35 kg: Same as adult dose.
Cách dùng
Should be taken with food.
Chống chỉ định
Hypersensitivity, history of sudden death or congenital prolongation of QT interval, history of cardiac arrhythmias, bradycardia, CHF with reduced left ventricle ejection fraction, electrolyte disturbances (e.g. hypokalaemia, hypomagnesemia). Concomitant use with strong CYP3A4 inducers, and with drugs known to prolong QT interval.
Thận trọng
Severe renal and hepatic impairment. Children. Pregnancy and lactation. Not indicated for the prevention and treatment of severe or complicated malaria.
Tác dụng không mong muốn
Blood and lymphatic system disorders: Anaemia, splenomegaly.
Cardiac disorders: Palpitations, QT prolongation.
Gastrointestinal disorders: Abdominal pain, nausea, vomiting, diarrhoea.
General disorders and administration site conditions: Asthenia, fatigue, fever, malaise.
Hepatobiliary disorders: Hepatomegaly.
Infections and infestations: Malaria.
Investigations: Increased serum AST.
Metabolism and nutrition disorders: Decreased appetite.
Musculoskeletal and connective tissue disorders: Arthralgia, chills, myalgia.
Nervous system disorders: Dizziness, headache, paraesthesia, clonus, gait disturbance vertigo.
Psychiatric disorders: Sleep disorder, insomnia.
Respiratory, thoracic and mediastinal disorders: Cough, rhinitis.
Skin and subcutaneous tissue disorders: Pruritus, rash.
Potentially Fatal: Anaphylaxis.
Thông tin tư vấn bệnh nhân
This drug may cause dizziness, and fatigue, if affected, do not drive or operate machinery.
Chỉ số theo dõi
Monitor adequate food consumption during treatment.
Tương tác
May reduce effectiveness of hormonal contraceptives.
Potentially Fatal: Decreased plasma concentration with strong CYP3A4 inducers (e.g. phenytoin, carbamazepine, rifampicin). Additive QT prolongation effect with antiarrhythmics Class I and II (e.g. quinidine, amiodarone), antipsychotics (e.g. pimozide, ziprasidone), neuroleptics, antidepressants, antibiotics (e.g. macrolide, fluoroquinolone), triazole antifungals, non-sedating antihistamines (e.g. terfenadine, astemizole), cisapride, flecainide, halofrantine.
Tương tác với thức ăn
Increased plasma level with grapefruit juice. Increased absorption with high fat meal. Decreased plasma concentration with St. John’s wort.
Tác dụng
Description: Artemether and lumefantrine exert their antimalarial action in the food vacuole of the parasite. They interfere with the conversion of haem (a toxic intermediate produced during haemoglobin breakdown) to the nontoxic haemozoin, malarial pigment. Both inhibit nucleic acid and protein synthesis.
Artemether and its active metabolite dihydroartemisinin (DHA) are rapid schizontocides. Its anti-malarial activity is attributed to their endoperoxide moiety.
Lumefantrine is a dichlorobenzylidine derivative. The exact mechanism of action of is still unknown, but it is thought to inhibit the formation of β-hematin by complexing with hemin.
Synonym: benflumentol.
Pharmacokinetics:
Absorption: Artemether: Rapidly absorbed from the gastrointestinal tract. Food, particularly high fat meal, increases absorption. Time to peak plasma concentration: Approx 2 hours.
Lumefantrine: Absorbed from the gastrointestinal tract after a lag-time of up to 2 hours. Food, particularly high fat meal, increases absorption. Time to peak plasma concentration: Approx 6-8 hours.
Distribution: Artemether: Plasma protein binding: Approx 95% (artemether); 47-76% (DHA).
Lumefantrine: Plasma protein binding: 99.7%.
Metabolism: Artemether: Metabolised in the liver by CYP3A4/5 enzymes via demethylation to its active metabolite, dihydroartemisinin (DHA) and to lesser extent by CYP2B6, C9, C19.
Lumefantrine: Metabolised in the liver by CYP3A4 enzyme to metabolite, desbutyl-lumefantrine.
Excretion: Artemether: Via urine (<0.01% as DHA). Elimination half-life: Approx 2 hours.
Lumefantrine: Via faeces as unchanged drug; urine (small amount). Elimination half-life: 3-6 days.
Đặc tính

Chemical Structure Image
Artemether

Source: National Center for Biotechnology Information. PubChem Database. Artemether, CID=68911, https://pubchem.ncbi.nlm.nih.gov/compound/Artemether (accessed on Jan. 21, 2020)


Chemical Structure Image
Lumefantrine

Source: National Center for Biotechnology Information. PubChem Database. Lumefantrine, CID=6437380, https://pubchem.ncbi.nlm.nih.gov/compound/Lumefantrine (accessed on Jan. 21, 2020)

Bảo quản
Store at 25°C.
Phân loại MIMS
Thuốc chống sốt rét
Phân loại ATC
P01BF01 - artemether and lumefantrine ; Belongs to the class of artemisinin and derivatives, combinations. Used in the management of malaria.
Tài liệu tham khảo
Anon. Artemether and Lumefantrine. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 08/03/2018.

Buckingham R (ed). Artemether. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 08/03/2018.

Buckingham R (ed). Lumefantrine. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 08/03/2018.

Coartem Tablets for Oral Use (Novartis Pharmaceuticals Corporation). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 22/03/2018.

Joint Formulary Committee. Artemether with Lumefantrine. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 08/03/2018.

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