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Lumefantrine co-artemether

Generic Name
Lumefantrine co-artemether
Brand Names
-
Drug Type
Small Molecule
Chemical Formula
C346H378Cl33N11O16
CAS Number
141204-94-6
Unique Ingredient Identifier
5T2U51A0MW
Background

Lumefantrine Co-Artemether (Riamet) has been investigated for the treatment of Malaria, Malaria, Falciparum, Malaria in Pregnancy, Uncomplicated Malaria, and Uncomplicated Knowlesi Malaria. Lumefantrine Co-Artemether is a tablet formulation of artemether and lumefantrine, a well-tolerated, fast-acting and effective blood schizontocidal drug that serves primarily in the treatment of uncomplicated falciparum malaria that is resistant to other antimalarials. Artemether, an artemisinin derivative, has several proposed mechanisms of action, including interference with plasmodial transport proteins, interference with mitochondrial electron transport, and the production of free radicals to reduce blood antioxidants and glutathione. While artemether results in rapid defervescence, parasite clearance, and clinical improvement, it also has a relatively high recrudescence rate when used as monotherapy. The exact mechanism of action of lumefantrine is not well defined, but it is thought to inhibit -hematin formation, an important detoxification pathway for the parasite. Unlike artemether, lumefantrine has a slower onset of action, resulting in clearance of residual parasites and a decrease in recrudescence rate. The combination is an effective and well-tolerated malaria treatment, providing high cure rates even in areas of multi-drug resistance.

Associated Conditions
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Associated Therapies
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Characterizing the pharmacological interaction of the antimalarial combination artefenomel and piperaquine

A randomized, open-label study with 24 healthy adults used the P. falciparum IBSM model to evaluate the PK/PD relationship of artefenomel and piperaquine. Participants were inoculated with P. falciparum and received single doses of the drugs on day 8. Blood samples were collected to monitor parasitemia and drug concentrations. The study aimed to assess the combination's safety and efficacy, with follow-up until day 45. The study was conducted in Brisbane, Australia, and registered on ClinicalTrials.gov.
contagionlive.com
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Essential Malaria Drug Artemisinin Shows Signs of Partial Resistance in Children

A study in Uganda found partial artemisinin resistance in children with severe malaria, linked to the A675V mutation in the Plasmodium falciparum parasite, impacting standard treatment efficacy.

Azithromycin in severe malaria bacterial co-infection in African children (TABS-PKPD)

A phase I/II trial compared 3 azithromycin doses in children with severe malaria, randomizing 105 cases to 10, 15, or 20 mg/kg over 5 days, while 50 controls received standard care. The study aimed to determine optimal azithromycin doses for future trials, with co-primary outcomes of CRP change and microbiological cure. Results showed similar CRP reductions across doses, with no significant differences in survival or adverse events. Pharmacokinetic analysis suggested allometric dosing for consistent exposure, contrasting with the trial's mg/kg regimens.
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