Peringatan Keamanan

Side effects include dry mouth, anorexia, insomnia, constipation and headache.

Sibutramine

DB01105

small molecule approved illicit investigational withdrawn

Deskripsi

Sibutramine (trade name Meridia in the USA, Reductil in Europe and other countries), usually as sibutramide hydrochloride monohydrate, is an orally administered agent for the treatment of obesity. It is a centrally acting stimulant chemically related to amphetamines thus it is classified as a Schedule IV controlled substance in the United States. In October 2010, Sibutramine was withdrawn from Canadian and U.S. markets due to concerns that the drug increases the risk of heart attack and stroke in patients with a history of heart disease.

Struktur Molekul 2D

Berat 279.848
Wujud solid

Peta Jejaring Molekuler
Legenda: ObatTargetGenEnzim(Panah → menunjukkan arah efek / relasi)TransporterCarrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) 1.1 hours
Volume Distribusi -
Klirens (Clearance) * Oral cl=1750 L/h [oral administration]

Absorpsi

Rapid absorption following oral administration. Absolute bioavailability is not known, but at least 77% of a single oral dose of sibutramine is absorbed.

Metabolisme

Hepatic

Rute Eliminasi

Sibutramine is metabolized in the liver principally by the cytochrome P450 (3A4) isoenzyme, to desmethyl metabolites, M1 and M2. These active metabolites are further metabolized by hydroxylation and conjugation to pharmacologically inactive metabolites, M5 and M6. Approximately 85% (range 68-95%) of a single orally administered radiolabeled dose was excreted in urine and feces over a 15-day collection period with the majority of the dose (77%) excreted in the urine. The primary route of excretion for M1 and M2 is hepatic metabolism and for M5 and M6 is renal excretion.

Farmakogenomik

1 Varian
GNB3 (rs5443)

Patients with this genotype will lose weight with sibutramine.

Interaksi Obat

1675 Data
Cyproheptadine The therapeutic efficacy of Sibutramine can be decreased when used in combination with Cyproheptadine.
Desmopressin The risk or severity of hyponatremia can be increased when Sibutramine is combined with Desmopressin.
Ioflupane I-123 Sibutramine may decrease effectiveness of Ioflupane I-123 as a diagnostic agent.
Linezolid The risk or severity of serotonin syndrome can be increased when Linezolid is combined with Sibutramine.
Metyrosine The risk or severity of extrapyramidal symptoms can be increased when Metyrosine is combined with Sibutramine.
Pimozide The risk or severity of QTc prolongation can be increased when Sibutramine is combined with Pimozide.
Buprenorphine Sibutramine 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 Sibutramine.
Dronabinol Dronabinol may increase the central nervous system depressant (CNS depressant) activities of Sibutramine.
Droperidol Droperidol may increase the central nervous system depressant (CNS depressant) activities of Sibutramine.
Hydrocodone Sibutramine 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 Sibutramine.
Magnesium sulfate The therapeutic efficacy of Sibutramine can be increased when used in combination with Magnesium sulfate.
Methotrimeprazine Sibutramine may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
Minocycline Minocycline may increase the central nervous system depressant (CNS depressant) activities of Sibutramine.
Nabilone Nabilone may increase the central nervous system depressant (CNS depressant) activities of Sibutramine.
Orphenadrine Sibutramine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
Paraldehyde Sibutramine 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 Sibutramine.
Pramipexole Sibutramine may increase the sedative activities of Pramipexole.
Ropinirole Sibutramine may increase the sedative activities of Ropinirole.
Rotigotine Sibutramine may increase the sedative activities of Rotigotine.
Rufinamide The risk or severity of adverse effects can be increased when Rufinamide is combined with Sibutramine.
Sodium oxybate Sibutramine may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Suvorexant Sibutramine 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 Sibutramine.
Thalidomide Sibutramine may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
Zolpidem Sibutramine may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
Metoclopramide The risk or severity of adverse effects can be increased when Metoclopramide is combined with Sibutramine.
Methadone The risk or severity of adverse effects can be increased when Methadone is combined with Sibutramine.
Tedizolid phosphate The risk or severity of serotonin syndrome can be increased when Tedizolid phosphate is combined with Sibutramine.
Acetylsalicylic acid Sibutramine may increase the antiplatelet activities of Acetylsalicylic acid.
Mirtazapine Sibutramine may increase the serotonergic activities of Mirtazapine.
Morphine The risk or severity of serotonin syndrome can be increased when Morphine is combined with Sibutramine.
Hydromorphone The risk or severity of serotonin syndrome can be increased when Hydromorphone is combined with Sibutramine.
Oxycodone The risk or severity of serotonin syndrome can be increased when Oxycodone is combined with Sibutramine.
Butorphanol The risk or severity of serotonin syndrome can be increased when Butorphanol is combined with Sibutramine.
Dextropropoxyphene The risk or severity of serotonin syndrome can be increased when Dextropropoxyphene is combined with Sibutramine.
Pentazocine The risk or severity of serotonin syndrome can be increased when Pentazocine is combined with Sibutramine.
Sufentanil The risk or severity of serotonin syndrome can be increased when Sufentanil is combined with Sibutramine.
Nalbuphine The risk or severity of serotonin syndrome can be increased when Nalbuphine is combined with Sibutramine.
Levorphanol The risk or severity of serotonin syndrome can be increased when Levorphanol is combined with Sibutramine.
Remifentanil The risk or severity of serotonin syndrome can be increased when Remifentanil is combined with Sibutramine.
Diphenoxylate The risk or severity of serotonin syndrome can be increased when Diphenoxylate is combined with Sibutramine.
Oxymorphone The risk or severity of serotonin syndrome can be increased when Oxymorphone is combined with Sibutramine.
Dezocine The risk or severity of serotonin syndrome can be increased when Dezocine is combined with Sibutramine.
Methadyl acetate The risk or severity of serotonin syndrome can be increased when Methadyl acetate is combined with Sibutramine.
Dihydroetorphine The risk or severity of serotonin syndrome can be increased when Dihydroetorphine is combined with Sibutramine.
Diamorphine The risk or severity of serotonin syndrome can be increased when Diamorphine is combined with Sibutramine.
Ethylmorphine The risk or severity of serotonin syndrome can be increased when Ethylmorphine is combined with Sibutramine.
Etorphine The risk or severity of serotonin syndrome can be increased when Etorphine is combined with Sibutramine.
Dextromoramide The risk or severity of serotonin syndrome can be increased when Dextromoramide is combined with Sibutramine.
Desomorphine The risk or severity of serotonin syndrome can be increased when Desomorphine is combined with Sibutramine.
Carfentanil The risk or severity of serotonin syndrome can be increased when Carfentanil is combined with Sibutramine.
Dihydrocodeine The risk or severity of serotonin syndrome can be increased when Dihydrocodeine is combined with Sibutramine.
Alphacetylmethadol The risk or severity of serotonin syndrome can be increased when Alphacetylmethadol is combined with Sibutramine.
Dihydromorphine The risk or severity of serotonin syndrome can be increased when Dihydromorphine is combined with Sibutramine.
Ketobemidone The risk or severity of serotonin syndrome can be increased when Ketobemidone is combined with Sibutramine.
DPDPE The risk or severity of serotonin syndrome can be increased when DPDPE is combined with Sibutramine.
Lofentanil The risk or severity of serotonin syndrome can be increased when Lofentanil is combined with Sibutramine.
Opium The risk or severity of serotonin syndrome can be increased when Opium is combined with Sibutramine.
Normethadone The risk or severity of serotonin syndrome can be increased when Normethadone is combined with Sibutramine.
Piritramide The risk or severity of serotonin syndrome can be increased when Piritramide is combined with Sibutramine.
Alphaprodine The risk or severity of serotonin syndrome can be increased when Alphaprodine is combined with Sibutramine.
Meptazinol The risk or severity of serotonin syndrome can be increased when Meptazinol is combined with Sibutramine.
Phenoperidine The risk or severity of serotonin syndrome can be increased when Phenoperidine is combined with Sibutramine.
Phenazocine The risk or severity of serotonin syndrome can be increased when Phenazocine is combined with Sibutramine.
Tilidine The risk or severity of serotonin syndrome can be increased when Tilidine is combined with Sibutramine.
Carfentanil, C-11 The risk or severity of serotonin syndrome can be increased when Carfentanil, C-11 is combined with Sibutramine.
Naltrexone The risk or severity of serotonin syndrome can be increased when Naltrexone is combined with Sibutramine.
Bezitramide The risk or severity of serotonin syndrome can be increased when Bezitramide is combined with Sibutramine.
Eluxadoline The risk or severity of serotonin syndrome can be increased when Eluxadoline is combined with Sibutramine.
Nicomorphine The risk or severity of serotonin syndrome can be increased when Nicomorphine is combined with Sibutramine.
Codeine The risk or severity of serotonin syndrome can be increased when Codeine is combined with Sibutramine.
Meperidine The risk or severity of serotonin syndrome can be increased when Meperidine is combined with Sibutramine.
Alfentanil The risk or severity of serotonin syndrome can be increased when Alfentanil is combined with Sibutramine.
Fentanyl The risk or severity of serotonin syndrome can be increased when Fentanyl is combined with Sibutramine.
Levacetylmethadol The risk or severity of serotonin syndrome can be increased when Levacetylmethadol is combined with Sibutramine.
Benzhydrocodone The risk or severity of serotonin syndrome can be increased when Benzhydrocodone is combined with Sibutramine.
Naloxegol The risk or severity of serotonin syndrome can be increased when Naloxegol is combined with Sibutramine.
Iobenguane Sibutramine may decrease effectiveness of Iobenguane as a diagnostic agent.
Methyclothiazide The risk or severity of hyponatremia can be increased when Sibutramine is combined with Methyclothiazide.
Chlorthalidone The risk or severity of hyponatremia can be increased when Sibutramine is combined with Chlorthalidone.
Bendroflumethiazide The risk or severity of hyponatremia can be increased when Sibutramine is combined with Bendroflumethiazide.
Metolazone The risk or severity of hyponatremia can be increased when Sibutramine is combined with Metolazone.
Benzthiazide The risk or severity of hyponatremia can be increased when Sibutramine is combined with Benzthiazide.
Hydroflumethiazide The risk or severity of hyponatremia can be increased when Sibutramine is combined with Hydroflumethiazide.
Indapamide The risk or severity of hyponatremia can be increased when Sibutramine is combined with Indapamide.
Chlorothiazide The risk or severity of hyponatremia can be increased when Sibutramine is combined with Chlorothiazide.
Hydrochlorothiazide The risk or severity of hyponatremia can be increased when Sibutramine is combined with Hydrochlorothiazide.
Trichlormethiazide The risk or severity of hyponatremia can be increased when Sibutramine is combined with Trichlormethiazide.
Polythiazide The risk or severity of hyponatremia can be increased when Sibutramine is combined with Polythiazide.
Quinethazone The risk or severity of hyponatremia can be increased when Sibutramine is combined with Quinethazone.
Cyclopenthiazide The risk or severity of hyponatremia can be increased when Sibutramine is combined with Cyclopenthiazide.
Epitizide The risk or severity of hyponatremia can be increased when Sibutramine is combined with Epitizide.
Ethanol Sibutramine may increase the central nervous system depressant (CNS depressant) activities of Ethanol.
Azelastine Sibutramine 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 Sibutramine.
Botulinum toxin type B The risk or severity of adverse effects can be increased when Botulinum toxin type B is combined with Sibutramine.
Botulinum toxin type A The risk or severity of adverse effects can be increased when Botulinum toxin type A is combined with Sibutramine.

Target Protein

Sodium-dependent dopamine transporter SLC6A3
Sodium-dependent serotonin transporter SLC6A4
Sodium-dependent noradrenaline transporter SLC6A2

Referensi & Sumber

Synthesis reference: Chris Senanayake, "Methods of preparing didesmethylsibutramine and other sibutramine derivatives." U.S. Patent US20020183554, issued December 05, 2002.
Artikel (PubMed)
  • PMID: 18671470
    Sharma B, Henderson DC: Sibutramine: current status as an anti-obesity drug and its future perspectives. Expert Opin Pharmacother. 2008 Aug;9(12):2161-73. doi: 10.1517/14656566.9.12.2161 .
  • PMID: 19475780
    Tziomalos K, Krassas GE, Tzotzas T: The use of sibutramine in the management of obesity and related disorders: an update. Vasc Health Risk Manag. 2009;5(1):441-52.
  • PMID: 9758240
    Heal DJ, Aspley S, Prow MR, Jackson HC, Martin KF, Cheetham SC: Sibutramine: a novel anti-obesity drug. A review of the pharmacological evidence to differentiate it from d-amphetamine and d-fenfluramine. Int J Obes Relat Metab Disord. 1998 Aug;22 Suppl 1:S18-28; discussion S29.
  • PMID: 9130038
    Stock MJ: Sibutramine: a review of the pharmacology of a novel anti-obesity agent. Int J Obes Relat Metab Disord. 1997 Mar;21 Suppl 1:S25-9.

Contoh Produk & Brand

Produk: 7 • International brands: 3
Produk
  • Apo-sibutramine
    Capsule • 10 mg • Oral • Canada • Generic • Approved
  • Apo-sibutramine
    Capsule • 15 mg • Oral • Canada • Generic • Approved
  • Meridia
    Capsule • 5 mg/1 • Oral • US • Approved
  • Meridia
    Capsule • 10 mg/1 • Oral • US • Approved
  • Meridia
    Capsule • 15 mg/1 • Oral • US • Approved
  • Meridia
    Capsule • 10 mg • Oral • Canada • Approved
  • Meridia
    Capsule • 15 mg • Oral • Canada • Approved
International Brands
  • Butramin
  • Medaria
  • Reductil

Sekuens Gen/Protein (FASTA)

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