Peringatan Keamanan

In the mouse, rat and guinea pig, the oral LD50s were 1,100-1,550 mg/kg; 1,450 mg/kg; and 1,490 mg/kg; respectively. High doses of naltrexone (generally >1,000 mg/kg) produce salivation, depression/reduced activity, tremors, and convulsions.

Naltrexone

DB00704

small molecule approved investigational vet_approved

Deskripsi

Derivative of noroxymorphone that is the N-cyclopropylmethyl congener of naloxone. It is a narcotic antagonist that is effective orally, longer lasting and more potent than naloxone, and has been proposed for the treatment of heroin addiction. The FDA has approved naltrexone for the treatment of alcohol dependence.

Struktur Molekul 2D

Berat 341.4009
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) 4 hours for naltrexone and 13 hours for the active metabolite 6 beta-naltrexol.
Volume Distribusi * 1350 L [intravenous administration]
Klirens (Clearance) * ~ 3.5 L/min [after IV administration]

Absorpsi

Although well absorbed orally, naltrexone is subject to significant first pass metabolism with oral bioavailability estimates ranging from 5 to 40%.

Metabolisme

Hepatic. When administered orally, naltrexone undergoes extensive biotransformation and is metabolized to 6 beta-naltrexol (which may contribute to the therapeutic effect) and other minor metabolites.

Rute Eliminasi

Both parent drug and metabolites are excreted primarily by the kidney (53% to 79% of the dose), however, urinary excretion of unchanged naltrexone accounts for less than 2% of an oral dose and fecal excretion is a minor elimination pathway. The renal clearance for naltrexone ranges from 30 to 127 mL/min and suggests that renal elimination is primarily by glomerular filtration.

Farmakogenomik

1 Varian
OPRM1 (rs1799971)

Patients with this genotype have an increased number of abstinent days when using naltrexone to treat alcohol addiction.

Interaksi Makanan

1 Data
  • 1. Take with or without food. The absorption is unaffected by food.

Interaksi Obat

544 Data
Alvimopan The risk or severity of adverse effects can be increased when Naltrexone is combined with Alvimopan.
Desmopressin The risk or severity of hyponatremia can be increased when Naltrexone is combined with Desmopressin.
Codeine The therapeutic efficacy of Codeine can be decreased when used in combination with Naltrexone.
Hydromorphone The therapeutic efficacy of Hydromorphone can be decreased when used in combination with Naltrexone.
Meperidine The therapeutic efficacy of Meperidine can be decreased when used in combination with Naltrexone.
Dextropropoxyphene The therapeutic efficacy of Dextropropoxyphene can be decreased when used in combination with Naltrexone.
Sufentanil The therapeutic efficacy of Sufentanil can be decreased when used in combination with Naltrexone.
Alfentanil The therapeutic efficacy of Alfentanil can be decreased when used in combination with Naltrexone.
Fentanyl The therapeutic efficacy of Fentanyl can be decreased when used in combination with Naltrexone.
Levorphanol The therapeutic efficacy of Levorphanol can be decreased when used in combination with Naltrexone.
Remifentanil The therapeutic efficacy of Remifentanil can be decreased when used in combination with Naltrexone.
Diphenoxylate The therapeutic efficacy of Diphenoxylate can be decreased when used in combination with Naltrexone.
Oxymorphone The therapeutic efficacy of Oxymorphone can be decreased when used in combination with Naltrexone.
Dezocine The therapeutic efficacy of Dezocine can be decreased when used in combination with Naltrexone.
Methadyl acetate The therapeutic efficacy of Methadyl acetate can be decreased when used in combination with Naltrexone.
Dihydroetorphine The therapeutic efficacy of Dihydroetorphine can be decreased when used in combination with Naltrexone.
Diamorphine The therapeutic efficacy of Diamorphine can be decreased when used in combination with Naltrexone.
Bezitramide The therapeutic efficacy of Bezitramide can be decreased when used in combination with Naltrexone.
Ethylmorphine The therapeutic efficacy of Ethylmorphine can be decreased when used in combination with Naltrexone.
Etorphine The therapeutic efficacy of Etorphine can be decreased when used in combination with Naltrexone.
Dextromoramide The therapeutic efficacy of Dextromoramide can be decreased when used in combination with Naltrexone.
Desomorphine The therapeutic efficacy of Desomorphine can be decreased when used in combination with Naltrexone.
Carfentanil The therapeutic efficacy of Carfentanil can be decreased when used in combination with Naltrexone.
Dihydrocodeine The therapeutic efficacy of Dihydrocodeine can be decreased when used in combination with Naltrexone.
Alphacetylmethadol The therapeutic efficacy of Alphacetylmethadol can be decreased when used in combination with Naltrexone.
Dihydromorphine The therapeutic efficacy of Dihydromorphine can be decreased when used in combination with Naltrexone.
Tapentadol The therapeutic efficacy of Tapentadol can be decreased when used in combination with Naltrexone.
Ketobemidone The therapeutic efficacy of Ketobemidone can be decreased when used in combination with Naltrexone.
DPDPE The therapeutic efficacy of DPDPE can be decreased when used in combination with Naltrexone.
Lofentanil The therapeutic efficacy of Lofentanil can be decreased when used in combination with Naltrexone.
Opium The therapeutic efficacy of Opium can be decreased when used in combination with Naltrexone.
Normethadone The therapeutic efficacy of Normethadone can be decreased when used in combination with Naltrexone.
Piritramide The therapeutic efficacy of Piritramide can be decreased when used in combination with Naltrexone.
Alphaprodine The therapeutic efficacy of Alphaprodine can be decreased when used in combination with Naltrexone.
Nicomorphine The therapeutic efficacy of Nicomorphine can be decreased when used in combination with Naltrexone.
Meptazinol The therapeutic efficacy of Meptazinol can be decreased when used in combination with Naltrexone.
Phenoperidine The therapeutic efficacy of Phenoperidine can be decreased when used in combination with Naltrexone.
Phenazocine The therapeutic efficacy of Phenazocine can be decreased when used in combination with Naltrexone.
Tilidine The therapeutic efficacy of Tilidine can be decreased when used in combination with Naltrexone.
Carfentanil, C-11 The therapeutic efficacy of Carfentanil, C-11 can be decreased when used in combination with Naltrexone.
Benzhydrocodone The therapeutic efficacy of Benzhydrocodone can be decreased when used in combination with Naltrexone.
Pegvisomant The therapeutic efficacy of Pegvisomant can be decreased when used in combination with Naltrexone.
Succinylcholine The risk or severity of bradycardia can be increased when Succinylcholine is combined with Naltrexone.
Methylnaltrexone Naltrexone may increase the opioid antagonism activities of Methylnaltrexone.
Naloxegol The therapeutic efficacy of Naloxegol can be decreased when used in combination with Naltrexone.
Nelfinavir The metabolism of Naltrexone can be increased when combined with Nelfinavir.
Phenytoin The metabolism of Naltrexone can be increased when combined with Phenytoin.
Desogestrel The metabolism of Naltrexone can be increased when combined with Desogestrel.
Zidovudine The metabolism of Naltrexone can be increased when combined with Zidovudine.
Ritonavir The metabolism of Naltrexone can be increased when combined with Ritonavir.
Carbamazepine The metabolism of Naltrexone can be increased when combined with Carbamazepine.
Efavirenz The metabolism of Naltrexone can be increased when combined with Efavirenz.
Tipranavir The metabolism of Naltrexone can be increased when combined with Tipranavir.
Ethinylestradiol The metabolism of Naltrexone can be increased when combined with Ethinylestradiol.
Rifampin The metabolism of Naltrexone can be increased when combined with Rifampicin.
Testosterone propionate The metabolism of Naltrexone can be increased when combined with Testosterone propionate.
Seproxetine The risk or severity of serotonin syndrome can be increased when Naltrexone is combined with Seproxetine.
Fluvoxamine The risk or severity of serotonin syndrome can be increased when Naltrexone is combined with Fluvoxamine.
Citalopram The risk or severity of serotonin syndrome can be increased when Naltrexone is combined with Citalopram.
Duloxetine The risk or severity of serotonin syndrome can be increased when Naltrexone is combined with Duloxetine.
Sertraline The risk or severity of serotonin syndrome can be increased when Naltrexone is combined with Sertraline.
Sibutramine The risk or severity of serotonin syndrome can be increased when Naltrexone is combined with Sibutramine.
Nefazodone The risk or severity of serotonin syndrome can be increased when Naltrexone is combined with Nefazodone.
Zimelidine The risk or severity of serotonin syndrome can be increased when Naltrexone is combined with Zimelidine.
Dapoxetine The risk or severity of serotonin syndrome can be increased when Naltrexone is combined with Dapoxetine.
Milnacipran The risk or severity of serotonin syndrome can be increased when Naltrexone is combined with Milnacipran.
Desvenlafaxine The risk or severity of serotonin syndrome can be increased when Naltrexone is combined with Desvenlafaxine.
Indalpine The risk or severity of serotonin syndrome can be increased when Naltrexone is combined with Indalpine.
Ritanserin The risk or severity of serotonin syndrome can be increased when Naltrexone is combined with Ritanserin.
Alaproclate The risk or severity of serotonin syndrome can be increased when Naltrexone is combined with Alaproclate.
Amphetamine Amphetamine may increase the analgesic activities of Naltrexone.
Phentermine Phentermine may increase the analgesic activities of Naltrexone.
Pseudoephedrine Pseudoephedrine may increase the analgesic activities of Naltrexone.
Benzphetamine Benzphetamine may increase the analgesic activities of Naltrexone.
Diethylpropion Diethylpropion may increase the analgesic activities of Naltrexone.
Lisdexamfetamine Lisdexamfetamine may increase the analgesic activities of Naltrexone.
Mephentermine Mephentermine may increase the analgesic activities of Naltrexone.
MMDA MMDA may increase the analgesic activities of Naltrexone.
Midomafetamine Midomafetamine may increase the analgesic activities of Naltrexone.
2,5-Dimethoxy-4-ethylamphetamine 2,5-Dimethoxy-4-ethylamphetamine may increase the analgesic activities of Naltrexone.
4-Bromo-2,5-dimethoxyamphetamine 4-Bromo-2,5-dimethoxyamphetamine may increase the analgesic activities of Naltrexone.
Tenamfetamine Tenamfetamine may increase the analgesic activities of Naltrexone.
Chlorphentermine Chlorphentermine may increase the analgesic activities of Naltrexone.
Methylenedioxyethamphetamine Methylenedioxyethamphetamine may increase the analgesic activities of Naltrexone.
Dextroamphetamine Dextroamphetamine may increase the analgesic activities of Naltrexone.
Metamfetamine Metamfetamine may increase the analgesic activities of Naltrexone.
Iofetamine I-123 Iofetamine I-123 may increase the analgesic activities of Naltrexone.
Ritobegron Ritobegron may increase the analgesic activities of Naltrexone.
Mephedrone Mephedrone may increase the analgesic activities of Naltrexone.
Methoxyphenamine Methoxyphenamine may increase the analgesic activities of Naltrexone.
Gepefrine Gepefrine may increase the analgesic activities of Naltrexone.
2,5-Dimethoxy-4-ethylthioamphetamine 2,5-Dimethoxy-4-ethylthioamphetamine may increase the analgesic activities of Naltrexone.
Phendimetrazine Phendimetrazine may increase the analgesic activities of Naltrexone.
Methadone The therapeutic efficacy of Methadone can be decreased when used in combination with Naltrexone.
Levacetylmethadol The therapeutic efficacy of Levacetylmethadol can be decreased when used in combination with Naltrexone.
Trospium The risk or severity of adverse effects can be increased when Trospium is combined with Naltrexone.
Oxyphenonium The risk or severity of adverse effects can be increased when Oxyphenonium is combined with Naltrexone.
Butabarbital The risk or severity of adverse effects can be increased when Butabarbital is combined with Naltrexone.
Butalbital The risk or severity of adverse effects can be increased when Butalbital is combined with Naltrexone.
Benzatropine The risk or severity of adverse effects can be increased when Benzatropine is combined with Naltrexone.

Target Protein

Mu-type opioid receptor OPRM1
Kappa-type opioid receptor OPRK1
Delta-type opioid receptor OPRD1
Sigma non-opioid intracellular receptor 1 SIGMAR1

Referensi & Sumber

Synthesis reference: Bao-Shan Huang, Yansong Lu, Ben-Yi Ji, Aris P Christodoulou, "Preparation of naltrexone from codeine and 3-benzylmorphine." U.S. Patent US6013796, issued March, 1990.
Artikel (PubMed)
  • PMID: 11316375
    Schmitz JM, Stotts AL, Rhoades HM, Grabowski J: Naltrexone and relapse prevention treatment for cocaine-dependent patients. Addict Behav. 2001 Mar-Apr;26(2):167-80.
  • PMID: 18070245
    Krystal JH, Gueorguieva R, Cramer J, Collins J, Rosenheck R: Naltrexone is associated with reduced drinking by alcohol dependent patients receiving antidepressants for mood and anxiety symptoms: results from VA Cooperative Study No. 425, "Naltrexone in the treatment of alcoholism". Alcohol Clin Exp Res. 2008 Jan;32(1):85-91. Epub 2007 Dec 7.
  • PMID: 20201811
    Ray LA, Chin PF, Miotto K: Naltrexone for the treatment of alcoholism: clinical findings, mechanisms of action, and pharmacogenetics. CNS Neurol Disord Drug Targets. 2010 Mar;9(1):13-22.
  • PMID: 17080248
    Kariv R, Tiomny E, Grenshpon R, Dekel R, Waisman G, Ringel Y, Halpern Z: Low-dose naltreoxone for the treatment of irritable bowel syndrome: a pilot study. Dig Dis Sci. 2006 Dec;51(12):2128-33. Epub 2006 Nov 1.

Contoh Produk & Brand

Produk: 80 • International brands: 19
Produk
  • Addex-1000
    Pellet, implantable • 1000 mg/1 • Subcutaneous • US
  • Apo-naltrexone
    Tablet • 50 mg • Oral • Canada • Generic • Approved
  • Contrave
    Tablet, film coated, extended release • - • Oral • US • Approved
  • Contrave
    Tablet, film coated, extended release • - • Oral • US • Approved
  • Contrave
    Tablet, extended release • - • Oral • Canada • Approved
  • Contrave Extended-Release
    Tablet, extended release • - • Oral • US • Approved
  • Contrave Extended-Release
    Tablet, extended release • - • Oral • US • Approved
  • Contrave Extended-Release
    Tablet, extended release • - • Oral • US • Approved
Menampilkan 8 dari 80 produk.
International Brands
  • Abernil — Medochemie
  • Adepend — AOP Orphan
  • Antaxon — Zambon
  • Antaxone — Pharmazam
  • Arrop — Quimico
  • Celupan
  • Depade
  • Dependex — Amomed
  • Nalerona — ABL Pharma
  • Nalorex — Bristol-Myers Squibb

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