Peringatan Keamanan

The oral TDLO of mefloquine in humans is 11 mg/kg/2W (intermittent) and 880 mg/kg in the rat. Intraperitoneal LD50 in the rat is 130 mg/kg.L30668
Symptoms of an overdose with mefloquine may manifest as a worsening of adverse effects. In the case of an overdose, symptomatic and supportive care should be provided. There is no known antidote for an overdose with mefloquine.L8953 Monitor cardiac function by ECG, follow neuropsychiatric status for at least 24 hours, and provide treatment as required.L8953

Mefloquine

DB00358

small molecule approved investigational

Deskripsi

Malaria is a protozoan disease that places an enormous burden on human health in endemic areas around the world. The 2020 World Health Organization malaria report indicates a 60% decrease in the global malaria fatality rate between 2000 to 2019.L30618 Despite this, malaria remains a significant cause of morbidity and mortality; 90% of deaths from malaria occur in Africa. Individuals at the highest risk for malaria are those in disease naïve populations, children under age 5, refugees in Central and Eastern Africa, nonimmune civilian and military travelers, pregnant women, and immigrants traveling to their place of origin.L30623

Mefloquine, commonly known as Lariam, is an antimalarial drug used for the prevention and treatment of malaria caused by infection with Plasmodium vivax and Plasmodium falciparum. The drug was initially discovered by the Walter Reed Army Institute of Research (WRAIR) during a malaria drug discovery program between 1963 until 1976. It was approved by the FDA in 1989, and was first marketed by Hoffman Laroche.A226838 This drug has been the subject of widespread controversy due to concerns regarding neurotoxic effects; product information warns of potential serious neuropsychiatric effects.A226838,L8953

Struktur Molekul 2D

Berat 378.3122
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) The terminal elimination half-life of mefloquine ranges from 0.9 - 13.8 days, according to one pharmacokinetic review.[A226868] In various studies of healthy adults, the mean elimination half-life of mefloquine varied between 2 and 4 weeks, with a mean half-life of approximately 21 days.[L8953]
Volume Distribusi The apparent volume of distribution is in healthy adults is about 20 L/kg with wide tissue distribution.[L8953] Various estimates of the total apparent volume of distribution range from 13.3 to 40.9L/kg.[A226868] Mefloquine can accumulate in erythrocytes that have been infected with malaria parasites.[L8953]
Klirens (Clearance) The systemic clearance of mefloquine ranges from 0.022 to 0.073 L/h/kg, with an increased clearance during pregnancy.[A226868] Prescribing information mentions a clearance rate of 30 mL/min.[L8953]

Absorpsi

Mefloquine is readily absorbed from the gastrointestinal tract; food significantly increases absorption and increases bioavailability by 40%. The bioavailability of tablets compared with the oral solution preparation of mefloquine is over 85%. Cmax is achieved in 6 to 24 hours in healthy volunteers after a single dose.A226868,L8953 Average blood concentrations range between 50 to 110 ng/ml/mg/kg.A226868 A weekly dose of 250 mg leads to steady-state plasma concentrations of 1000 to 2000 ?g/L, after 7 to 10 weeks of administration.L8953

Metabolisme

Mefloquine is heavily metabolized in the liver by the CYP3A4 enzyme.A38732,L8953 Two metabolites have been identified; the main metabolite, 2,8-bis-trifluoromethyl-4-quinoline carboxylic acid, which inactive against plasmodium falciparum. The second metabolite, an alcohol, is found in small quantities.L8953

Rute Eliminasi

Mefloquine is believed to be excreted in the bile and feces. In healthy volunteers who have achieved steady-state concentrations of mefloquine, the unchanged drug was excreted at 9% of the ingested dose, and excretion of its carboxylic metabolite under was measured at 4% of the ingested dose. Concentrations of other metabolites could not be determined.A226948,L8953

Interaksi Makanan

3 Data
  • 1. Avoid alcohol.
  • 2. Take with a full glass of water.
  • 3. Take with food. The presence of food significantly enhances the rate and extent of absorption, leading to about a 40% increase in bioavailability.

Interaksi Obat

1058 Data
Afatinib The serum concentration of Afatinib can be increased when it is combined with Mefloquine.
Bosutinib The serum concentration of Bosutinib can be increased when it is combined with Mefloquine.
Brentuximab vedotin The serum concentration of Brentuximab vedotin can be increased when it is combined with Mefloquine.
Edoxaban The serum concentration of Edoxaban can be increased when it is combined with Mefloquine.
Ledipasvir The serum concentration of Ledipasvir can be increased when it is combined with Mefloquine.
Naloxegol The serum concentration of Naloxegol can be increased when it is combined with Mefloquine.
Pazopanib The serum concentration of Pazopanib can be increased when it is combined with Mefloquine.
Prucalopride The serum concentration of Prucalopride can be increased when it is combined with Mefloquine.
Ranolazine The serum concentration of Ranolazine can be increased when it is combined with Mefloquine.
Silodosin The excretion of Silodosin can be decreased when combined with Mefloquine.
Topotecan The serum concentration of Topotecan can be increased when it is combined with Mefloquine.
Eliglustat The metabolism of Eliglustat can be decreased when combined with Mefloquine.
Ibrutinib The metabolism of Ibrutinib can be decreased when combined with Mefloquine.
Everolimus The serum concentration of Everolimus can be increased when it is combined with Mefloquine.
Rifaximin The serum concentration of Rifaximin can be increased when it is combined with Mefloquine.
Artemether The risk or severity of QTc prolongation can be increased when Mefloquine is combined with Artemether.
Lumefantrine The risk or severity of QTc prolongation can be increased when Mefloquine is combined with Lumefantrine.
Cilostazol The metabolism of Cilostazol can be decreased when combined with Mefloquine.
Colchicine The serum concentration of Colchicine can be increased when it is combined with Mefloquine.
Iloperidone The metabolism of Iloperidone can be decreased when combined with Mefloquine.
Retapamulin The metabolism of Retapamulin can be decreased when combined with Mefloquine.
Tofacitinib The metabolism of Tofacitinib can be decreased when combined with Mefloquine.
Vardenafil The metabolism of Vardenafil can be decreased when combined with Mefloquine.
Eszopiclone The metabolism of Eszopiclone can be decreased when combined with Mefloquine.
Zopiclone The metabolism of Zopiclone can be decreased when combined with Mefloquine.
Lovastatin The metabolism of Lovastatin can be decreased when combined with Mefloquine.
Lorazepam The therapeutic efficacy of Lorazepam can be decreased when used in combination with Mefloquine.
Pregabalin The therapeutic efficacy of Pregabalin can be decreased when used in combination with Mefloquine.
Butalbital The therapeutic efficacy of Butalbital can be decreased when used in combination with Mefloquine.
Phenytoin The therapeutic efficacy of Phenytoin can be decreased when used in combination with Mefloquine.
Topiramate The therapeutic efficacy of Topiramate can be decreased when used in combination with Mefloquine.
Pentobarbital The therapeutic efficacy of Pentobarbital can be decreased when used in combination with Mefloquine.
Valproic acid The therapeutic efficacy of Valproic acid can be decreased when used in combination with Mefloquine.
Trimethadione The therapeutic efficacy of Trimethadione can be decreased when used in combination with Mefloquine.
Clobazam The therapeutic efficacy of Clobazam can be decreased when used in combination with Mefloquine.
Secobarbital The therapeutic efficacy of Secobarbital can be decreased when used in combination with Mefloquine.
Metharbital The therapeutic efficacy of Metharbital can be decreased when used in combination with Mefloquine.
Methohexital The therapeutic efficacy of Methohexital can be decreased when used in combination with Mefloquine.
Mephenytoin The therapeutic efficacy of Mephenytoin can be decreased when used in combination with Mefloquine.
Lamotrigine The therapeutic efficacy of Lamotrigine can be decreased when used in combination with Mefloquine.
Carbamazepine The therapeutic efficacy of Carbamazepine can be decreased when used in combination with Mefloquine.
Ethosuximide The therapeutic efficacy of Ethosuximide can be decreased when used in combination with Mefloquine.
Thiopental The therapeutic efficacy of Thiopental can be decreased when used in combination with Mefloquine.
Paramethadione The therapeutic efficacy of Paramethadione can be decreased when used in combination with Mefloquine.
Clorazepic acid The therapeutic efficacy of Clorazepic acid can be decreased when used in combination with Mefloquine.
Magnesium sulfate The therapeutic efficacy of Magnesium sulfate can be decreased when used in combination with Mefloquine.
Tizanidine The therapeutic efficacy of Tizanidine can be decreased when used in combination with Mefloquine.
Riluzole The therapeutic efficacy of Riluzole can be decreased when used in combination with Mefloquine.
Ethotoin The therapeutic efficacy of Ethotoin can be decreased when used in combination with Mefloquine.
Oxcarbazepine The therapeutic efficacy of Oxcarbazepine can be decreased when used in combination with Mefloquine.
Primidone The therapeutic efficacy of Primidone can be decreased when used in combination with Mefloquine.
Acetazolamide The therapeutic efficacy of Acetazolamide can be decreased when used in combination with Mefloquine.
Diazepam The therapeutic efficacy of Diazepam can be decreased when used in combination with Mefloquine.
Phensuximide The therapeutic efficacy of Phensuximide can be decreased when used in combination with Mefloquine.
Progabide The therapeutic efficacy of Progabide can be decreased when used in combination with Mefloquine.
Methylphenobarbital The therapeutic efficacy of Methylphenobarbital can be decreased when used in combination with Mefloquine.
Tiagabine The therapeutic efficacy of Tiagabine can be decreased when used in combination with Mefloquine.
Zonisamide The therapeutic efficacy of Zonisamide can be decreased when used in combination with Mefloquine.
Felbamate The therapeutic efficacy of Felbamate can be decreased when used in combination with Mefloquine.
Zaleplon The therapeutic efficacy of Zaleplon can be decreased when used in combination with Mefloquine.
Gabapentin The therapeutic efficacy of Gabapentin can be decreased when used in combination with Mefloquine.
Clonazepam The therapeutic efficacy of Clonazepam can be decreased when used in combination with Mefloquine.
Vigabatrin The therapeutic efficacy of Vigabatrin can be decreased when used in combination with Mefloquine.
Phenacemide The therapeutic efficacy of Phenacemide can be decreased when used in combination with Mefloquine.
Thiamylal The therapeutic efficacy of Thiamylal can be decreased when used in combination with Mefloquine.
Phenobarbital The therapeutic efficacy of Phenobarbital can be decreased when used in combination with Mefloquine.
Levetiracetam The therapeutic efficacy of Levetiracetam can be decreased when used in combination with Mefloquine.
Estazolam The therapeutic efficacy of Estazolam can be decreased when used in combination with Mefloquine.
Fosphenytoin The therapeutic efficacy of Fosphenytoin can be decreased when used in combination with Mefloquine.
Amobarbital The therapeutic efficacy of Amobarbital can be decreased when used in combination with Mefloquine.
Hexobarbital The therapeutic efficacy of Hexobarbital can be decreased when used in combination with Mefloquine.
Barbital The therapeutic efficacy of Barbital can be decreased when used in combination with Mefloquine.
Delorazepam The therapeutic efficacy of Delorazepam can be decreased when used in combination with Mefloquine.
Nitrazepam The therapeutic efficacy of Nitrazepam can be decreased when used in combination with Mefloquine.
7-Nitroindazole The therapeutic efficacy of 7-Nitroindazole can be decreased when used in combination with Mefloquine.
Valpromide The therapeutic efficacy of Valpromide can be decreased when used in combination with Mefloquine.
Flunarizine The therapeutic efficacy of Flunarizine can be decreased when used in combination with Mefloquine.
Ezogabine The therapeutic efficacy of Ezogabine can be decreased when used in combination with Mefloquine.
Methsuximide The therapeutic efficacy of Methsuximide can be decreased when used in combination with Mefloquine.
Brivaracetam The therapeutic efficacy of Brivaracetam can be decreased when used in combination with Mefloquine.
Rufinamide The therapeutic efficacy of Rufinamide can be decreased when used in combination with Mefloquine.
Lacosamide The therapeutic efficacy of Lacosamide can be decreased when used in combination with Mefloquine.
Remacemide The therapeutic efficacy of Remacemide can be decreased when used in combination with Mefloquine.
Clomethiazole The therapeutic efficacy of Clomethiazole can be decreased when used in combination with Mefloquine.
Deramciclane The therapeutic efficacy of Deramciclane can be decreased when used in combination with Mefloquine.
Tramiprosate The therapeutic efficacy of Tramiprosate can be decreased when used in combination with Mefloquine.
Gaboxadol The therapeutic efficacy of Gaboxadol can be decreased when used in combination with Mefloquine.
Sulthiame The therapeutic efficacy of Sulthiame can be decreased when used in combination with Mefloquine.
Perampanel The therapeutic efficacy of Perampanel can be decreased when used in combination with Mefloquine.
Ifenprodil The therapeutic efficacy of Ifenprodil can be decreased when used in combination with Mefloquine.
Barbexaclone The therapeutic efficacy of Barbexaclone can be decreased when used in combination with Mefloquine.
Beclamide The therapeutic efficacy of Beclamide can be decreased when used in combination with Mefloquine.
Cannabidiol The therapeutic efficacy of Cannabidiol can be decreased when used in combination with Mefloquine.
Paraldehyde The therapeutic efficacy of Paraldehyde can be decreased when used in combination with Mefloquine.
Stiripentol The therapeutic efficacy of Stiripentol can be decreased when used in combination with Mefloquine.
Eslicarbazepine acetate The therapeutic efficacy of Eslicarbazepine acetate can be decreased when used in combination with Mefloquine.
Doramectin The therapeutic efficacy of Doramectin can be decreased when used in combination with Mefloquine.
Tiletamine The therapeutic efficacy of Tiletamine can be decreased when used in combination with Mefloquine.
Brexanolone The therapeutic efficacy of Brexanolone can be decreased when used in combination with Mefloquine.
Etiracetam The therapeutic efficacy of Etiracetam can be decreased when used in combination with Mefloquine.

Target Protein

Fe(II)-protoporphyrin IX
80S ribosomal subunit
Adenosine receptor A2a ADORA2A

Referensi & Sumber

Synthesis reference: Asymmetric Total Synthesis of the Antimalarial Drug (+)-Mefloquine Hydrochloride via Chiral N-Amino Cyclic Carbamate Hydrazones.Org. Lett. 2011, 13, 12, 3118–3121. May 26, 2011. https://doi.org/10.1021/ol2010193
Artikel (PubMed)
  • PMID: 28805982
    Nevin RL: A serious nightmare: psychiatric and neurologic adverse reactions to mefloquine are serious adverse reactions. Pharmacol Res Perspect. 2017 Aug;5(4). doi: 10.1002/prp2.328.
  • PMID: 7682911
    Palmer KJ, Holliday SM, Brogden RN: Mefloquine. A review of its antimalarial activity, pharmacokinetic properties and therapeutic efficacy. Drugs. 1993 Mar;45(3):430-75. doi: 10.2165/00003495-199345030-00009.
  • PMID: 29083100
    Tickell-Painter M, Maayan N, Saunders R, Pace C, Sinclair D: Mefloquine for preventing malaria during travel to endemic areas. Cochrane Database Syst Rev. 2017 Oct 30;10:CD006491. doi: 10.1002/14651858.CD006491.pub4.
  • PMID: 28288098
    Wong W, Bai XC, Sleebs BE, Triglia T, Brown A, Thompson JK, Jackson KE, Hanssen E, Marapana DS, Fernandez IS, Ralph SA, Cowman AF, Scheres SHW, Baum J: Mefloquine targets the Plasmodium falciparum 80S ribosome to inhibit protein synthesis. Nat Microbiol. 2017 Mar 13;2:17031. doi: 10.1038/nmicrobiol.2017.31.
  • PMID: 17404338
    Croft AM: A lesson learnt: the rise and fall of Lariam and Halfan. J R Soc Med. 2007 Apr;100(4):170-4. doi: 10.1177/014107680710011411.
  • PMID: 11914150
    Croft AM, Herxheimer A: Adverse effects of the antimalaria drug, mefloquine: due to primary liver damage with secondary thyroid involvement? BMC Public Health. 2002 Mar 25;2:6. doi: 10.1186/1471-2458-2-6.
  • PMID: 2208897
    Karbwang J, White NJ: Clinical pharmacokinetics of mefloquine. Clin Pharmacokinet. 1990 Oct;19(4):264-79. doi: 10.2165/00003088-199019040-00002.
  • PMID: 30541569
    Sheridan CM, Garcia VE, Ahyong V, DeRisi JL: The Plasmodium falciparum cytoplasmic translation apparatus: a promising therapeutic target not yet exploited by clinically approved anti-malarials. Malar J. 2018 Dec 12;17(1):465. doi: 10.1186/s12936-018-2616-7.
Menampilkan 8 dari 12 artikel.

Contoh Produk & Brand

Produk: 17 • International brands: 15
Produk
  • Lariam
    Tablet • 250 mg/1 • Oral • US • Approved
  • Lariam Tab 250mg
    Tablet • 250 mg • Oral • Canada • Approved
  • Mefloquine
    Tablet • 250 mg • Oral • Canada • Approved
  • Mefloquine Hydrochloride
    Tablet • 250 mg/1 • Oral • US • Generic • Approved
  • Mefloquine Hydrochloride
    Tablet • 250 mg/1 • Oral • US • Generic • Approved
  • Mefloquine Hydrochloride
    Tablet • 250 mg/1 • Oral • US • Generic • Approved
  • Mefloquine Hydrochloride
    Tablet • 250 mg/1 • Oral • US • Generic • Approved
  • Mefloquine Hydrochloride
    Tablet • 250 mg/1 • Oral • US • Generic • Approved
Menampilkan 8 dari 17 produk.
International Brands
  • Eloquine — Unifarm
  • Facital — Zydus Cadila
  • Falcital — Cadila HC
  • Larimef — Ipca
  • Mefax — Alkem
  • Mefliam — Cipla Medpro
  • Meflon — ACI
  • Mefloquina — AC Farma
  • Mefque — Zydus Cadila
  • Mephaquin — Hisamitsu Seiyaku

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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