Peringatan Keamanan

A dextromethorphan overdose may present as nausea, vomiting, stupor, coma, respiratory depression, seizures, tachycardia, hyperexcitability, toxic psychosis, ataxia, nystagmus, dystonia, blurred vision, changes in muscle reflexes, and serotonin syndrome.L14363 Overdose should be managed through symptomatic and supportive measures.L14363

Dextromethorphan

DB00514

small molecule approved

Deskripsi

Dextromethorphan is a levorphanol derivative and codeine analog commonly used as a cough suppressant and also a drug of abuse.A215412 Although similar in structure to other opioids, it has minimal interaction with opioid receptors.A215412

Dextromethorphan was granted FDA approval before 3 December 1957.A215412,L14997

Struktur Molekul 2D

Berat 271.404
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) Dextromethorphan has a half life of 3-30 hours.[A215382]
Volume Distribusi The volume of distribution of dextromethorphan is 5-6.7L/kg.[A215382]
Klirens (Clearance) -

Absorpsi

A 30mg oral dose of dextromethorphan reaches a Cmax of 2.9 ng/mL, with a Tmax of 2.86 h, and an AUC of 17.8 ng\*h/mL.A34933

Metabolisme

Dextromethorphan can be N-demethylated to 3-methoxymorphinan by CYP3A4, CYP2D6, and CYP2C9 or O-demethylated to dextrorphan by CYP2D6 and CYP2C9.A415 Dextrorphan is N-demethylated by CYP3A4 and CYP2D6, while 3-methoxymorphinan is O-demethylated by CYP2D6.A415 Both are metabolized to form 3-hydroxymorphinan.A415 Dextrorphan and 3-hydroxymorphinan are both O-glucuronidated or O-sulfated.A415

Rute Eliminasi

Data eliminasi belum tersedia.

Farmakogenomik

2 Varian
CYP2D6 (rs3892097)

Patients with this genotype have reduced metabolism of dextromethorphan.

CYP2D6 (rs5030655)

Patients with this genotype have reduced metabolism of dextromethorphan.

Interaksi Makanan

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

Interaksi Obat

1408 Data
Buprenorphine Dextromethorphan may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
Dronabinol Dronabinol may increase the central nervous system depressant (CNS depressant) activities of Dextromethorphan.
Droperidol Droperidol may increase the central nervous system depressant (CNS depressant) activities of Dextromethorphan.
Hydrocodone Dextromethorphan 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 Dextromethorphan.
Magnesium sulfate The therapeutic efficacy of Dextromethorphan can be increased when used in combination with Magnesium sulfate.
Methotrimeprazine Dextromethorphan may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
Metyrosine Dextromethorphan may increase the sedative activities of Metyrosine.
Minocycline Minocycline may increase the central nervous system depressant (CNS depressant) activities of Dextromethorphan.
Nabilone Nabilone may increase the central nervous system depressant (CNS depressant) activities of Dextromethorphan.
Orphenadrine Dextromethorphan may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
Paraldehyde Dextromethorphan 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 Dextromethorphan.
Pramipexole Dextromethorphan may increase the sedative activities of Pramipexole.
Ropinirole Dextromethorphan may increase the sedative activities of Ropinirole.
Rotigotine Dextromethorphan may increase the sedative activities of Rotigotine.
Rufinamide The risk or severity of adverse effects can be increased when Rufinamide is combined with Dextromethorphan.
Sodium oxybate Dextromethorphan may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Suvorexant Dextromethorphan 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 Dextromethorphan.
Thalidomide Dextromethorphan may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
Zolpidem Dextromethorphan may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
Secretin porcine The therapeutic efficacy of Secretin porcine can be decreased when used in combination with Dextromethorphan.
Methadone The risk or severity of adverse effects can be increased when Methadone is combined with Dextromethorphan.
Memantine The risk or severity of adverse effects can be increased when Dextromethorphan is combined with Memantine.
Quinine The metabolism of Dextromethorphan can be decreased when combined with Quinine.
Linezolid The risk or severity of serotonin syndrome can be increased when Linezolid is combined with Dextromethorphan.
Furazolidone The risk or severity of serotonin syndrome can be increased when Furazolidone is combined with Dextromethorphan.
Procaine The risk or severity of serotonin syndrome can be increased when Procaine is combined with Dextromethorphan.
Tranylcypromine The risk or severity of serotonin syndrome can be increased when Tranylcypromine is combined with Dextromethorphan.
Phenelzine The risk or severity of serotonin syndrome can be increased when Phenelzine is combined with Dextromethorphan.
Minaprine The risk or severity of serotonin syndrome can be increased when Minaprine is combined with Dextromethorphan.
Selegiline The risk or severity of serotonin syndrome can be increased when Selegiline is combined with Dextromethorphan.
Procarbazine The risk or severity of serotonin syndrome can be increased when Procarbazine is combined with Dextromethorphan.
Moclobemide The risk or severity of serotonin syndrome can be increased when Moclobemide is combined with Dextromethorphan.
Isocarboxazid The risk or severity of serotonin syndrome can be increased when Isocarboxazid is combined with Dextromethorphan.
Rasagiline The risk or severity of serotonin syndrome can be increased when Rasagiline is combined with Dextromethorphan.
Pargyline The risk or severity of serotonin syndrome can be increased when Pargyline is combined with Dextromethorphan.
Clorgiline The risk or severity of serotonin syndrome can be increased when Clorgiline is combined with Dextromethorphan.
Iproniazid The risk or severity of serotonin syndrome can be increased when Iproniazid is combined with Dextromethorphan.
Nialamide The risk or severity of serotonin syndrome can be increased when Nialamide is combined with Dextromethorphan.
Safinamide The risk or severity of serotonin syndrome can be increased when Safinamide is combined with Dextromethorphan.
7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline The risk or severity of serotonin syndrome can be increased when 7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline is combined with Dextromethorphan.
Hydracarbazine The risk or severity of serotonin syndrome can be increased when Hydracarbazine is combined with Dextromethorphan.
Pirlindole The risk or severity of serotonin syndrome can be increased when Pirlindole is combined with Dextromethorphan.
Toloxatone The risk or severity of serotonin syndrome can be increased when Toloxatone is combined with Dextromethorphan.
Benmoxin The risk or severity of serotonin syndrome can be increased when Benmoxin is combined with Dextromethorphan.
Mebanazine The risk or severity of serotonin syndrome can be increased when Mebanazine is combined with Dextromethorphan.
Octamoxin The risk or severity of serotonin syndrome can be increased when Octamoxin is combined with Dextromethorphan.
Pheniprazine The risk or severity of serotonin syndrome can be increased when Pheniprazine is combined with Dextromethorphan.
Phenoxypropazine The risk or severity of serotonin syndrome can be increased when Phenoxypropazine is combined with Dextromethorphan.
Pivhydrazine The risk or severity of serotonin syndrome can be increased when Pivhydrazine is combined with Dextromethorphan.
Safrazine The risk or severity of serotonin syndrome can be increased when Safrazine is combined with Dextromethorphan.
Caroxazone The risk or severity of serotonin syndrome can be increased when Caroxazone is combined with Dextromethorphan.
Harmaline The risk or severity of serotonin syndrome can be increased when Harmaline is combined with Dextromethorphan.
Brofaromine The risk or severity of serotonin syndrome can be increased when Brofaromine is combined with Dextromethorphan.
Phenindione The risk or severity of adverse effects can be increased when Dextromethorphan is combined with Phenindione.
Coumarin The risk or severity of adverse effects can be increased when Dextromethorphan is combined with Coumarin.
Tioclomarol The risk or severity of adverse effects can be increased when Dextromethorphan is combined with Tioclomarol.
4-hydroxycoumarin The risk or severity of adverse effects can be increased when Dextromethorphan is combined with 4-hydroxycoumarin.
Ethyl biscoumacetate The risk or severity of adverse effects can be increased when Dextromethorphan is combined with Ethyl biscoumacetate.
Clorindione The risk or severity of adverse effects can be increased when Dextromethorphan is combined with Clorindione.
Diphenadione The risk or severity of adverse effects can be increased when Dextromethorphan is combined with Diphenadione.
Mirabegron The serum concentration of Dextromethorphan 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 Dextromethorphan.
Botulinum toxin type A The risk or severity of adverse effects can be increased when Dextromethorphan is combined with Botulinum toxin type A.
Botulinum toxin type B The risk or severity of adverse effects can be increased when Dextromethorphan is combined with Botulinum toxin type B.
Mirtazapine Dextromethorphan may increase the serotonergic activities of Mirtazapine.
Ethanol Dextromethorphan may increase the central nervous system depressant (CNS depressant) activities of Ethanol.
Azelastine Dextromethorphan 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 Dextromethorphan.
Citalopram The risk or severity of adverse effects can be increased when Dextromethorphan is combined with Citalopram.
Sibutramine The risk or severity of adverse effects can be increased when Dextromethorphan is combined with Sibutramine.
Zimelidine The risk or severity of adverse effects can be increased when Dextromethorphan is combined with Zimelidine.
Dapoxetine The risk or severity of adverse effects can be increased when Dextromethorphan is combined with Dapoxetine.
Milnacipran The risk or severity of adverse effects can be increased when Dextromethorphan is combined with Milnacipran.
Desvenlafaxine The risk or severity of serotonin syndrome can be increased when Desvenlafaxine is combined with Dextromethorphan.
Levomilnacipran The risk or severity of serotonin syndrome can be increased when Dextromethorphan is combined with Levomilnacipran.
Indalpine The risk or severity of adverse effects can be increased when Dextromethorphan is combined with Indalpine.
Alaproclate The risk or severity of adverse effects can be increased when Dextromethorphan is combined with Alaproclate.
Sertraline The risk or severity of adverse effects can be increased when Dextromethorphan is combined with Sertraline.
Seproxetine The risk or severity of adverse effects can be increased when Dextromethorphan is combined with Seproxetine.
Codeine The risk or severity of adverse effects can be increased when Dextromethorphan is combined with Codeine.
Hydromorphone The risk or severity of adverse effects can be increased when Dextromethorphan is combined with Hydromorphone.
Oxycodone The risk or severity of adverse effects can be increased when Dextromethorphan is combined with Oxycodone.
Butorphanol The risk or severity of adverse effects can be increased when Dextromethorphan is combined with Butorphanol.
Pentazocine The risk or severity of adverse effects can be increased when Dextromethorphan is combined with Pentazocine.
Sufentanil The risk or severity of adverse effects can be increased when Dextromethorphan is combined with Sufentanil.
Nalbuphine The risk or severity of adverse effects can be increased when Dextromethorphan is combined with Nalbuphine.
Levorphanol The risk or severity of adverse effects can be increased when Dextromethorphan is combined with Levorphanol.
Remifentanil The risk or severity of adverse effects can be increased when Dextromethorphan is combined with Remifentanil.
Diphenoxylate The risk or severity of adverse effects can be increased when Dextromethorphan is combined with Diphenoxylate.
Oxymorphone The risk or severity of adverse effects can be increased when Dextromethorphan is combined with Oxymorphone.
Dezocine The risk or severity of adverse effects can be increased when Dextromethorphan is combined with Dezocine.
Methadyl acetate The risk or severity of adverse effects can be increased when Dextromethorphan is combined with Methadyl acetate.
Dihydroetorphine The risk or severity of adverse effects can be increased when Dextromethorphan is combined with Dihydroetorphine.
Diamorphine The risk or severity of adverse effects can be increased when Dextromethorphan is combined with Diamorphine.
Ethylmorphine The risk or severity of adverse effects can be increased when Dextromethorphan is combined with Ethylmorphine.
Etorphine The risk or severity of adverse effects can be increased when Dextromethorphan is combined with Etorphine.
Dextromoramide The risk or severity of adverse effects can be increased when Dextromethorphan is combined with Dextromoramide.

Target Protein

Sigma non-opioid intracellular receptor 1 SIGMAR1
Aromatase CYP19A1
Glutamate receptor ionotropic, NMDA 3A GRIN3A
Neuronal acetylcholine receptor subunit alpha-2 CHRNA2
Sodium-dependent serotonin transporter SLC6A4
Membrane-associated progesterone receptor component 1 PGRMC1
Neuronal acetylcholine receptor subunit alpha-3 CHRNA3
Neuronal acetylcholine receptor subunit alpha-4 CHRNA4
Neuronal acetylcholine receptor subunit beta-4 CHRNB4
Neuronal acetylcholine receptor subunit beta-2 CHRNB2
Neuronal acetylcholine receptor subunit alpha-7 CHRNA7
Mu-type opioid receptor OPRM1
Delta-type opioid receptor OPRD1
Kappa-type opioid receptor OPRK1
NADPH oxidase CYBB
Sodium-dependent noradrenaline transporter SLC6A2

Referensi & Sumber

Synthesis reference: Mahendra R. Patel, "Sustained Release Suspension Preparation For Dextromethorphan." U.S. Patent US20130115253, issued May 09, 2013.
Artikel (PubMed)
  • PMID: 15505150
    Brooks BR, Thisted RA, Appel SH, Bradley WG, Olney RK, Berg JE, Pope LE, Smith RA: Treatment of pseudobulbar affect in ALS with dextromethorphan/quinidine: a randomized trial. Neurology. 2004 Oct 26;63(8):1364-70.
  • PMID: 2660263
    Olney JW, Labruyere J, Price MT: Pathological changes induced in cerebrocortical neurons by phencyclidine and related drugs. Science. 1989 Jun 16;244(4910):1360-2.
  • PMID: 7976530
    Hargreaves RJ, Hill RG, Iversen LL: Neuroprotective NMDA antagonists: the controversy over their potential for adverse effects on cortical neuronal morphology. Acta Neurochir Suppl (Wien). 1994;60:15-9.
  • PMID: 17573115
    Carliss RD, Radovsky A, Chengelis CP, O'Neill TP, Shuey DL: Oral administration of dextromethorphan does not produce neuronal vacuolation in the rat brain. Neurotoxicology. 2007 Jul;28(4):813-8. Epub 2007 Apr 6.
  • PMID: 10869398
    Hernandez SC, Bertolino M, Xiao Y, Pringle KE, Caruso FS, Kellar KJ: Dextromethorphan and its metabolite dextrorphan block alpha3beta4 neuronal nicotinic receptors. J Pharmacol Exp Ther. 2000 Jun;293(3):962-7.
  • PMID: 19515014
    Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1.
  • PMID: 15342614
    Pope LE, Khalil MH, Berg JE, Stiles M, Yakatan GJ, Sellers EM: Pharmacokinetics of dextromethorphan after single or multiple dosing in combination with quinidine in extensive and poor metabolizers. J Clin Pharmacol. 2004 Oct;44(10):1132-42. doi: 10.1177/0091270004269521.
  • PMID: 30860737
    Journey JD, Agrawal S, Stern E: Dextromethorphan Toxicity .
Menampilkan 8 dari 12 artikel.

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Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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