Artemether/lumefantrine

Artemether/lumefantrine
Combination of
ArtemetherAntimalarial
LumefantrineAntimalarial
Names
Trade namesCoartem, Riamet, Falcynate-LF, others
Clinical data
Main usesMalaria[1]
Side effectsMuscle and joint pains, fever, loss of appetite, headache[2]
WHO AWaReUnlinkedWikibase error: ⧼unlinkedwikibase-error-statements-entity-not-set⧽
Pregnancy
category
  • AU: D
  • US: C (Risk not ruled out)
    Routes of
    use    		By mouth
    Defined daily dose0.28 g[3]
    External links
    AHFS/Drugs.comMonograph
    MedlinePlusa609024
    Legal
    Legal status
    • AU: S4 (Prescription only)
    • US: ℞-only

    Artemether/lumefantrine, sold under the trade name Coartem among others, is a combination of the two medications artemether and lumefantrine.[2] It is used to treat malaria caused by Plasmodium falciparum that is not treatable with chloroquine.[2] It is not typically used to prevent malaria.[2] It is taken by mouth.[2]

    Common side effects include muscle and joint pains, fever, loss of appetite, and headache.[2] Serious side effects include prolongation of the QT interval.[2] While not well studied, it appears to be safe for use in pregnancy.[2] The dose does not need changing in those with mild or moderate kidney or liver problems.[2]

    The combination came into medical use in 1992.[4] They were both developed in China.[4][5] It is on the World Health Organization's List of Essential Medicines.[6] The wholesale cost in the developing world is between US$0.10 and US$1.2 per day as of 2014.[7] It is not available as a generic medication and a course of treatment costs between US$100 and US$200 in the United States.[8]

    Medical uses

    The combination is an effective and well-tolerated malaria treatment, providing high cure rates even in areas of multi-drug resistance.[9][10]

    Dosage

    The defined daily dose is 0.28 g (by mouth)[3]For those over 35 kg the dose is 160/960 mg by mouth twice per day.[1] For those 25 to 35 kg it is 60/360 mg twice per day.[1] For those 15 to 25 kg it is 40/240 mg twice per day.[1] And for those 5 to 15 kg it is 20/120 mg twice per day.[1] Duration of treatment is three days.[1]

    Side effects

    Coartem can cause anaphylactic reactions. The drug frequently causes headache, dizziness and anorexia, although mild forms in most cases. Other fairly common side effects (more than 3% of patients) include sleep disorder, tinnitus, tremor, palpitation, as well as unspecific reactions like vertigo, gastrointestinal disorders, itch and nasopharyngitis.[11]

    Pregnancy and breastfeeding

    Use in both pregnancy and breastfeeding appear to be okay.[1]

    Interactions

    Food, in particular fat, enhances the absorption of both artemether and lumefantrine, and patients are advised to take the tablets with food as soon as a meal can be tolerated. Coartem has a potential to prolong the QT interval, so combinations with other drugs having that property can cause irregular heartbeat, potentially leading to lethal ventricular fibrillation. The combination with halofantrine, another antimalarial, can cause a life-threatening QT prolongation. Drugs and other substances influencing the activity of the liver enzyme CYP3A4, including grapefruit juice, can either increase or lower blood levels of artemether/lumefantrine, depending on the sort of substance. This can either lead to more severe side effects or to reduced efficiency.[11]

    History

    In 2001, the first fixed dose artemisinin-based combination therapy to meet the World Health Organization's (WHO) pre-qualification criteria for efficacy, safety and quality was created.[12][13] It is approved in over 80 countries worldwide, including various countries in Africa, as well as Swissmedic, the European Medicines Agency (EMA) and the U.S. Food and Drug Administration (FDA).

    Society and culture

    Access to treatment

    Coartem is provided without profit to developing countries using grants from the Global Fund to Fight AIDS, Tuberculosis and Malaria, US President's Malaria Initiative along with other donors. Novartis has lowered the price of Coartem by 50% since 2001, increasing access to patients around the world. The first significant price reduction occurred in 2006, when the price of Coartem decreased from an average of US$1.57 to US$1.00. In 2006, due to an improved supply situation for the natural ingredient artemisinin, Novartis was able to undertake the pharmaceutical industry's most aggressive manufacturing scale-up of its kind from 4 million treatments in 2004 to 62 million treatments in 2006. Novartis and its partners invested heavily in expanding production capacity at their facilities in China, and Suffern, New York. This increase in production capacity ensured that supplies of Coartem met demand which enabled Novartis to further decrease the price of Coartem. In April 2008, Novartis further reduced the public sector price of Coartem by approximately 20%, to an average of US$0.80 (or US$0.37 for a child's treatment pack). This price reduction was made possible through production efficiency gains.

    Prior to this program, Novartis was criticised for a court case they launched against India, seeking to prohibit the marketing of cheap generic drugs. An Indian court ruled against Novartis, saying that the case was a "threat to people suffering from cancer [...] and other diseases who are too poor to pay for them".[14]

    United States approval

    On April 8, 2009, the U.S. Food and Drug Administration (FDA) announced that Coartem was approved for the treatment of acute, uncomplicated malaria infections in adults and children weighing at least five kilograms (approximately 11 pounds)[15] becoming the first artemisinin-based combination therapy approved in the United States.

    Dispersible

    In January 2009, Novartis and Medicines for Malaria Venture (MMV) launched Coartem Dispersible, an artemisinin-based combination therapy developed specifically for children with malaria. Coartem Dispersible contains the same ratio of artemether and lumefantrine as Coartem. It works as well as other formulations.[16] The sweet-tasting Coartem Dispersible tablets disperse quickly in small amounts of water, easing administration and ensuring effective dosing.

    Artemether/lumefantrine tablets are available in Pakistan under trade name Malagon AL by Chas.A.Mendoza and Artelum by W. Woodwards Pakistan.

    References

    1. 1 2 3 4 5 6 7 "ARTEMETHER/LUMEFANTRINE = AL oral - Essential drugs". medicalguidelines.msf.org. Archived from the original on 4 March 2021. Retrieved 25 August 2020.
    2. 1 2 3 4 5 6 7 8 9 "Artemether and Lumefantrine". The American Society of Health-System Pharmacists. Archived from the original on 2015-12-08. Retrieved Dec 2, 2015.
    3. 1 2 "WHOCC - ATC/DDD Index". www.whocc.no. Archived from the original on 22 June 2020. Retrieved 22 September 2020.
    4. 1 2 Ravina, Enrique (2011). The evolution of drug discovery : from traditional medicines to modern drugs (1. Aufl. ed.). Weinheim: Wiley-VCH. p. 139. ISBN 9783527326693. Archived from the original on 2015-12-08.
    5. ↑ Nightingale, Charles H. (2007). Antimicrobial pharmacodynamics in theory and clinical practice (2nd ed.). New York: Informa Healthcare. p. 380. ISBN 9781420017137. Archived from the original on 2015-12-08.
    6. ↑ World Health Organization (2019). World Health Organization model list of essential medicines: 21st list 2019. Geneva: World Health Organization. hdl:10665/325771. WHO/MVP/EMP/IAU/2019.06. License: CC BY-NC-SA 3.0 IGO.
    7. ↑ "Artemether + Lumefantrine". International Drug Price Indicator Guide. Archived from the original on 22 January 2018. Retrieved 4 December 2015.
    8. ↑ Hamilton, Richart (2015). Tarascon Pocket Pharmacopoeia 2015 Deluxe Lab-Coat Edition. Jones & Bartlett Learning. p. 45. ISBN 9781284057560.
    9. ↑ Makanga M, Premji Z, Falade C, Karbwang J, Mueller EA, Andriano K, et al. (June 2006). "Efficacy and safety of the six-dose regimen of artemether-lumefantrine in pediatrics with uncomplicated Plasmodium falciparum malaria: a pooled analysis of individual patient data". Am. J. Trop. Med. Hyg. 74 (6): 991–8. PMID 16760509.
    10. ↑ Mueller EA, van Vugt M, Kirch W, Andriano K, Hunt P, de Palacios PI (November 2006). "Efficacy and safety of the six-dose regimen of artemether-lumefantrine for treatment of uncomplicated Plasmodium falciparum malaria in adolescents and adults: a pooled analysis of individual patient data from randomized clinical trials". Acta Trop. 100 (1–2): 41–53. doi:10.1016/j.actatropica.2006.09.007. PMID 17045558.
    11. 1 2 Drugs.com: Coartem Archived May 21, 2016, at the Wayback Machine
    12. ↑ WHO Prequalification Programme: Priority Essential Medicines. Access to Artemesinin-based antimalarial medicinal products of acceptable quality. Available at http://healthtech.whoz.int/pq/lists/%5B%5D mal_suppliers.pdf Accessed May 2008.
    13. ↑ WHO Health Systems and Services: Prequalification Programme. Available at "Archived copy". Archived from the original on 2009-05-13. Retrieved 2009-05-20.{{cite web}}: CS1 maint: archived copy as title (link) Accessed May 2008.
    14. ↑ Make Trade Fair: Patients before Profits. Archived May 15, 2011, at the Wayback Machine
    15. ↑ https://www.fda.gov/bbs/topics/NEWS/2009/NEW01989.html%5B%5D
    16. ↑ Abdulla S, Sagara I, Borrmann S, D'Alessandro U, González R, Hamel M, et al. (November 2008). "Efficacy and safety of artemether-lumefantrine dispersible tablets compared with crushed commercial tablets in African infants and children with uncomplicated malaria: a randomised, single-blind, multicentre trial". Lancet. 372 (9652): 1819–27. doi:10.1016/S0140-6736(08)61492-0. PMID 18926569.
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