Peringatan Keamanan

Most common adverse reactions include hypoglycemia (diabetic patients), headache,
back pain,fatigue, decrease in lymphocytes,upper respiratory tract infection, and nasopharyngitis. Moreover, the safety and efficacy of coadministration with other weight loss products has not been established, and cardiovascular effects on mortality and morbidity have not been established.

Lorcaserin

DB04871

small molecule approved withdrawn

Deskripsi

Lorcaserin (previously APD-356), a highly selective 5HT2C receptor agonist, is used for the treatment of obesity. It has been shown to reduce body weight and food intake in animal models of obesity, and it is thought that targeting the 5HT2C receptor may alter body weight by regulating satiety. Lorcaserin is marketed as a salt form called Belviq, which is lorcaserin hydrochloride.

In February 2020, the FDA issued a Drug Safety Communication requesting the manufacturer of Belviq (lorcaserin hydrochloride tablets, 10 mg) and Belviq XR (lorcaserin hydrochloride extended-release tablets, 20 mg) to voluntarily withdraw these products from the U.S. market, and the company has submitted a request to voluntarily withdraw the drug. This decision was based on the results of a clinical trial assessing the risk of heart-related problems that found that patients treated with lorcaserin may have a higher risk of cancer.L44042,L44047

Struktur Molekul 2D

Berat 195.69
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The plasma half life is approximately 11 hours.
Volume Distribusi The volume of distribution was not determined, but lorcaserin distributes to the central nervous system and cerebrospinal fluid.
Klirens (Clearance) The clearance value was not determined.

Absorpsi

Lorcaserin has a peak plasma concentration of about 1.5 - 2 hours, but the bioavailability was not determined.

Metabolisme

Lorcaserin has extensive hepatic metabolism producing inactive compounds. Lorcaserin sulfamate (M1) is the major metabolite circulating in the plasma, and N-carbamoyl glucuronide lorcaserin (M5) is the major metabolite in urine. Other minor metabolites that are both excreted in urine are glucuronide or sulfate conjugates.

Rute Eliminasi

Lorcaserin is eliminated by hepatic metabolism, and the metabolites are eliminated mostly in the urine (92.3%) and some through feces (2.2%).

Interaksi Makanan

1 Data
  • 1. Take with or without food.

Interaksi Obat

1707 Data
Deferasirox The serum concentration of Lorcaserin can be increased when it is combined with Deferasirox.
Peginterferon alfa-2b The serum concentration of Lorcaserin can be increased when it is combined with Peginterferon alfa-2b.
Leflunomide The serum concentration of Lorcaserin can be decreased when it is combined with Leflunomide.
Teriflunomide The serum concentration of Lorcaserin can be decreased when it is combined with Teriflunomide.
Buprenorphine Lorcaserin may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
Doxylamine Doxylamine may increase the central nervous system depressant (CNS depressant) activities of Lorcaserin.
Dronabinol Dronabinol may increase the central nervous system depressant (CNS depressant) activities of Lorcaserin.
Droperidol Droperidol may increase the central nervous system depressant (CNS depressant) activities of Lorcaserin.
Hydrocodone Lorcaserin may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Hydroxyzine Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Lorcaserin.
Magnesium sulfate The therapeutic efficacy of Lorcaserin can be increased when used in combination with Magnesium sulfate.
Methotrimeprazine Lorcaserin may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
Metyrosine Lorcaserin may increase the sedative activities of Metyrosine.
Minocycline Minocycline may increase the central nervous system depressant (CNS depressant) activities of Lorcaserin.
Nabilone Nabilone may increase the central nervous system depressant (CNS depressant) activities of Lorcaserin.
Orphenadrine Lorcaserin may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
Paraldehyde Lorcaserin may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.
Perampanel Perampanel may increase the central nervous system depressant (CNS depressant) activities of Lorcaserin.
Pramipexole Lorcaserin may increase the sedative activities of Pramipexole.
Ropinirole Lorcaserin may increase the sedative activities of Ropinirole.
Rotigotine Lorcaserin may increase the sedative activities of Rotigotine.
Rufinamide The risk or severity of adverse effects can be increased when Rufinamide is combined with Lorcaserin.
Sodium oxybate Lorcaserin may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Suvorexant Lorcaserin may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
Tapentadol Tapentadol may increase the central nervous system depressant (CNS depressant) activities of Lorcaserin.
Thalidomide Lorcaserin may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
Zolpidem Lorcaserin may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
Brexpiprazole The metabolism of Brexpiprazole can be decreased when combined with Lorcaserin.
Eliglustat The metabolism of Lorcaserin can be decreased when combined with Eliglustat.
Methysergide The risk or severity of adverse effects can be increased when Lorcaserin is combined with Methysergide.
Cabergoline The risk or severity of adverse effects can be increased when Lorcaserin is combined with Cabergoline.
Methylergometrine The risk or severity of adverse effects can be increased when Lorcaserin is combined with Methylergometrine.
Lisuride The risk or severity of adverse effects can be increased when Lorcaserin is combined with Lisuride.
Ergotamine The risk or severity of adverse effects can be increased when Lorcaserin is combined with Ergotamine.
Nicergoline The risk or severity of adverse effects can be increased when Lorcaserin is combined with Nicergoline.
Ergoloid mesylate The risk or severity of adverse effects can be increased when Lorcaserin is combined with Ergoloid mesylate.
Pergolide The risk or severity of adverse effects can be increased when Lorcaserin is combined with Pergolide.
Bromocriptine The risk or severity of adverse effects can be increased when Lorcaserin is combined with Bromocriptine.
Ergometrine The risk or severity of adverse effects can be increased when Lorcaserin is combined with Ergometrine.
Lysergic acid diethylamide The risk or severity of adverse effects can be increased when Lorcaserin is combined with Lysergic acid diethylamide.
Dihydroergocornine The risk or severity of adverse effects can be increased when Lorcaserin is combined with Dihydroergocornine.
Dihydroergocristine The risk or severity of adverse effects can be increased when Lorcaserin is combined with Dihydroergocristine.
Dihydroergocryptine The risk or severity of adverse effects can be increased when Lorcaserin is combined with Dihydroergocryptine.
Terguride The risk or severity of adverse effects can be increased when Lorcaserin is combined with Terguride.
Metergoline The risk or severity of adverse effects can be increased when Lorcaserin is combined with Metergoline.
Dihydroergotamine The risk or severity of adverse effects can be increased when Lorcaserin is combined with Dihydroergotamine.
Methadone The risk or severity of adverse effects can be increased when Methadone is combined with Lorcaserin.
Atomoxetine The metabolism of Atomoxetine can be decreased when combined with Lorcaserin.
Linezolid The risk or severity of serotonin syndrome can be increased when Linezolid is combined with Lorcaserin.
Dicoumarol The risk or severity of adverse effects can be increased when Lorcaserin is combined with Dicoumarol.
Phenindione The risk or severity of adverse effects can be increased when Lorcaserin is combined with Phenindione.
Coumarin The risk or severity of adverse effects can be increased when Lorcaserin is combined with Coumarin.
Tioclomarol The risk or severity of adverse effects can be increased when Lorcaserin is combined with Tioclomarol.
Phenprocoumon The risk or severity of adverse effects can be increased when Lorcaserin is combined with Phenprocoumon.
4-hydroxycoumarin The risk or severity of adverse effects can be increased when Lorcaserin is combined with 4-hydroxycoumarin.
Ethyl biscoumacetate The risk or severity of adverse effects can be increased when Lorcaserin is combined with Ethyl biscoumacetate.
Fluindione The risk or severity of adverse effects can be increased when Lorcaserin is combined with Fluindione.
Clorindione The risk or severity of adverse effects can be increased when Lorcaserin is combined with Clorindione.
Diphenadione The risk or severity of adverse effects can be increased when Lorcaserin is combined with Diphenadione.
(S)-Warfarin The risk or severity of adverse effects can be increased when Lorcaserin is combined with (S)-Warfarin.
Mirabegron The serum concentration of Lorcaserin can be increased when it is combined with Mirabegron.
Tedizolid phosphate The risk or severity of serotonin syndrome can be increased when Tedizolid phosphate is combined with Lorcaserin.
Abiraterone The serum concentration of Lorcaserin can be increased when it is combined with Abiraterone.
Mirtazapine Lorcaserin may increase the serotonergic activities of Mirtazapine.
Cyproterone acetate The metabolism of Lorcaserin can be increased when combined with Cyproterone acetate.
Ethanol Lorcaserin may increase the central nervous system depressant (CNS depressant) activities of Ethanol.
Azelastine Lorcaserin may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
Brimonidine Brimonidine may increase the central nervous system depressant (CNS depressant) activities of Lorcaserin.
Sibutramine The risk or severity of adverse effects can be increased when Lorcaserin is combined with Sibutramine.
Zimelidine The risk or severity of adverse effects can be increased when Lorcaserin is combined with Zimelidine.
Milnacipran The risk or severity of adverse effects can be increased when Lorcaserin is combined with Milnacipran.
Desvenlafaxine The risk or severity of serotonin syndrome can be increased when Desvenlafaxine is combined with Lorcaserin.
Seproxetine The risk or severity of adverse effects can be increased when Lorcaserin is combined with Seproxetine.
Indalpine The risk or severity of adverse effects can be increased when Lorcaserin is combined with Indalpine.
Alaproclate The risk or severity of adverse effects can be increased when Lorcaserin is combined with Alaproclate.
Methylene blue Lorcaserin may increase the serotonergic activities of Methylene blue.
Trospium The metabolism of Lorcaserin can be decreased when combined with Trospium.
Lamotrigine The risk or severity of CNS depression can be increased when Lamotrigine is combined with Lorcaserin.
Propantheline Propantheline may decrease the excretion rate of Lorcaserin which could result in a higher serum level.
Dicyclomine Dicyclomine may decrease the excretion rate of Lorcaserin which could result in a higher serum level.
Doxacurium The risk or severity of CNS depression can be increased when Doxacurium is combined with Lorcaserin.
Flavoxate Flavoxate may decrease the excretion rate of Lorcaserin which could result in a higher serum level.
Aclidinium Lorcaserin may decrease the excretion rate of Aclidinium which could result in a higher serum level.
Trimebutine Lorcaserin may decrease the excretion rate of Trimebutine which could result in a higher serum level.
Imidafenacin Lorcaserin may decrease the excretion rate of Imidafenacin which could result in a higher serum level.
Propiverine Lorcaserin may decrease the excretion rate of Propiverine which could result in a higher serum level.
Zopiclone The risk or severity of adverse effects can be increased when Lorcaserin is combined with Zopiclone.
Sulpiride The risk or severity of adverse effects can be increased when Lorcaserin is combined with Sulpiride.
Triflupromazine The risk or severity of adverse effects can be increased when Lorcaserin is combined with Triflupromazine.
Fluphenazine The risk or severity of adverse effects can be increased when Lorcaserin is combined with Fluphenazine.
Moricizine The risk or severity of adverse effects can be increased when Lorcaserin is combined with Moricizine.
Acetophenazine The risk or severity of adverse effects can be increased when Lorcaserin is combined with Acetophenazine.
Chlorprothixene The risk or severity of adverse effects can be increased when Lorcaserin is combined with Chlorprothixene.
Alimemazine The risk or severity of adverse effects can be increased when Lorcaserin is combined with Alimemazine.
Periciazine The risk or severity of adverse effects can be increased when Lorcaserin is combined with Periciazine.
Acepromazine The risk or severity of adverse effects can be increased when Lorcaserin is combined with Acepromazine.
Aceprometazine The risk or severity of adverse effects can be increased when Lorcaserin is combined with Aceprometazine.
Molindone The risk or severity of adverse effects can be increased when Lorcaserin is combined with Molindone.
Thioproperazine The risk or severity of adverse effects can be increased when Lorcaserin is combined with Thioproperazine.
Osanetant The risk or severity of adverse effects can be increased when Lorcaserin is combined with Osanetant.

Target Protein

5-hydroxytryptamine receptor 2C HTR2C

Referensi & Sumber

Synthesis reference: Jandacek RJ: APD-356 (Arena). Curr Opin Investig Drugs. 2005 Oct;6(10):1051-6.
Artikel (PubMed)
  • PMID: 16625817
    Halford JC: Obesity drugs in clinical development. Curr Opin Investig Drugs. 2006 Apr;7(4):312-8.
  • PMID: 18095642
    Smith BM, Smith JM, Tsai JH, Schultz JA, Gilson CA, Estrada SA, Chen RR, Park DM, Prieto EB, Gallardo CS, Sengupta D, Dosa PI, Covel JA, Ren A, Webb RR, Beeley NR, Martin M, Morgan M, Espitia S, Saldana HR, Bjenning C, Whelan KT, Grottick AJ, Menzaghi F, Thomsen WJ: Discovery and structure-activity relationship of (1R)-8-chloro-2,3,4,5-tetrahydro-1-methyl-1H-3-benzazepine (Lorcaserin), a selective serotonin 5-HT2C receptor agonist for the treatment of obesity. J Med Chem. 2008 Jan 24;51(2):305-13. Epub 2007 Dec 21.

Contoh Produk & Brand

Produk: 2 • International brands: 1
Produk
  • Belviq
    Tablet • 10 mg/1 • Oral • US • Approved
  • Belviq XR
    Tablet, film coated, extended release • 20 mg/1 • Oral • US • Approved
International Brands
  • Lorqess

Sekuens Gen/Protein (FASTA)

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