Peringatan Keamanan

Infants and children experiencing an overdose may lead to hallucinations, convulsions, or death.L32985 Adults experiencing an overdose may present with drowsiness, convulsions, coma, or respiratory depression.L32985 Treat overdoses with symptomatic and supportive measures including mechanically assisted ventilation.L32985

In mice the oral LD50 is 203 mg/kg, while in rats it is 1320 mg/kg.L32985 The intraperitoneal LD50 in mice is 149 mg/kg.L32985

Dimenhydrinate

DB00985

small molecule approved

Deskripsi

Dimehydrinate was first described in the literature in 1949,A233120 and patented in 1950.L32995 Early research into dimenhydrinate focused on its role as an antihistamine for urticaria; the treatment of motion sickness was an accidental discovery.A233130

Dimenhydrinate, also known as B-dimethylaminoethyl benzohydrol ether 8-chlorotheophyllinate, is indicated to prevent nausea, vomiting, and dizziness caused by motion sickness.L32980,L32985,L32995 Dimenhydrinate is a combination of Diphenhydramine and 8-chlorotheophylline in a salt form, with 53%-55.5% dried diphenhydramine, and 44%-47% died 8-chlorotheophylline.L32985

The antiemetic properties of dimenhydrinate are primarily thought to be produced by diphenhydramine's antagonism of H1 histamine receptors in the vestibular systemA1540 while the excitatory effects are thought to be produced by 8-chlorotheophylline's adenosine receptor blockade.A33889

When used in large doses, dimenhydrinate has been shown to cause a "high" characterized by hallucinations, excitement, incoordination, and disorientation.A1539

Dimenhydrinate was granted FDA approval on 31 May 1972.L32975

Struktur Molekul 2D

Berat 469.97
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 elimination half life of dimenhydrinate is 5-8 hours.[L33000]
Volume Distribusi The volume of distribution of dimenhydrinate is 3-4 L/kg.[L33000]
Klirens (Clearance) -

Absorpsi

A 50 mg oral film coated tablet reaches a Cmax of 72.6 ng/mL with a Tmax of 2.7 hours.L33000 A 100 mg suppository reaches a Cmax of 112.2 ng/mL with a Tmax of 5.3 hours.L33010

Metabolisme

Dimenhydrinate is a theoclate salt that separates into diphenhydramine and 8-chlorotheophylline.L32985 diphenhydramine can either be N-glucuronidated by UGTs to diphenhydramine N-glucuronide or N-demethylated by CYP2D6, CYP1A2, CYP2C9, and CYP2C19 to N-desmethyldiphenhydramine.A415 N-desmethyldiphenhydramine can be N-demethylated again by the same enzymes to N,N-didesmethyldiphenhydramine, which undergoes oxidative deamination to form diphenylmethoxyacetic acid.A415

Rute Eliminasi

Dimenhydrinate is predominantly eliminated in the urine.L33000 1-3% of the dissociated diphenhydramine is eliminated in the urine unchanged, while 64% of diphenhydramine is eliminated in the urine as metabolites.L33010 The elimination of dimenhydrinate has not been fully studied.L33010

Interaksi Makanan

1 Data
  • 1. Avoid alcohol.

Interaksi Obat

961 Data
Ivabradine Ivabradine may increase the QTc-prolonging activities of Dimenhydrinate.
Buprenorphine Dimenhydrinate 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 Dimenhydrinate.
Dronabinol Dronabinol may increase the central nervous system depressant (CNS depressant) activities of Dimenhydrinate.
Droperidol Droperidol may increase the central nervous system depressant (CNS depressant) activities of Dimenhydrinate.
Hydrocodone Dimenhydrinate may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Magnesium sulfate The therapeutic efficacy of Dimenhydrinate can be increased when used in combination with Magnesium sulfate.
Methotrimeprazine Dimenhydrinate may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
Metyrosine Dimenhydrinate may increase the sedative activities of Metyrosine.
Minocycline Minocycline may increase the central nervous system depressant (CNS depressant) activities of Dimenhydrinate.
Mirtazapine Dimenhydrinate may increase the central nervous system depressant (CNS depressant) activities of Mirtazapine.
Nabilone Nabilone may increase the central nervous system depressant (CNS depressant) activities of Dimenhydrinate.
Orphenadrine Dimenhydrinate may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
Paraldehyde Dimenhydrinate 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 Dimenhydrinate.
Pramipexole Dimenhydrinate may increase the sedative activities of Pramipexole.
Ropinirole Dimenhydrinate may increase the sedative activities of Ropinirole.
Rotigotine Dimenhydrinate may increase the sedative activities of Rotigotine.
Rufinamide The risk or severity of adverse effects can be increased when Rufinamide is combined with Dimenhydrinate.
Sodium oxybate Dimenhydrinate may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Suvorexant Dimenhydrinate 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 Dimenhydrinate.
Thalidomide Dimenhydrinate may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
Zolpidem Dimenhydrinate may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
Benzylpenicilloyl polylysine Dimenhydrinate may decrease effectiveness of Benzylpenicilloyl polylysine as a diagnostic agent.
Betahistine The therapeutic efficacy of Betahistine can be decreased when used in combination with Dimenhydrinate.
Hyaluronidase (ovine) The therapeutic efficacy of Hyaluronidase (ovine) can be decreased when used in combination with Dimenhydrinate.
Hyaluronidase (human recombinant) The therapeutic efficacy of Hyaluronidase (human recombinant) can be decreased when used in combination with Dimenhydrinate.
Hyaluronidase The therapeutic efficacy of Hyaluronidase can be decreased when used in combination with Dimenhydrinate.
Methadone The risk or severity of adverse effects can be increased when Methadone is combined with Dimenhydrinate.
Ethanol Dimenhydrinate may increase the central nervous system depressant (CNS depressant) activities of Ethanol.
Azelastine Dimenhydrinate 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 Dimenhydrinate.
Fluvoxamine The risk or severity of adverse effects can be increased when Dimenhydrinate is combined with Fluvoxamine.
Duloxetine The risk or severity of adverse effects can be increased when Dimenhydrinate is combined with Duloxetine.
Paroxetine The risk or severity of adverse effects can be increased when Dimenhydrinate is combined with Paroxetine.
Sertraline The risk or severity of adverse effects can be increased when Dimenhydrinate is combined with Sertraline.
Sibutramine The risk or severity of adverse effects can be increased when Dimenhydrinate is combined with Sibutramine.
Nefazodone The risk or severity of adverse effects can be increased when Dimenhydrinate is combined with Nefazodone.
Zimelidine The risk or severity of adverse effects can be increased when Dimenhydrinate is combined with Zimelidine.
Dapoxetine The risk or severity of adverse effects can be increased when Dimenhydrinate is combined with Dapoxetine.
Milnacipran The risk or severity of adverse effects can be increased when Dimenhydrinate is combined with Milnacipran.
Desvenlafaxine The risk or severity of adverse effects can be increased when Dimenhydrinate is combined with Desvenlafaxine.
Seproxetine The risk or severity of adverse effects can be increased when Dimenhydrinate is combined with Seproxetine.
Indalpine The risk or severity of adverse effects can be increased when Dimenhydrinate is combined with Indalpine.
Ritanserin The risk or severity of adverse effects can be increased when Dimenhydrinate is combined with Ritanserin.
Alaproclate The risk or severity of adverse effects can be increased when Dimenhydrinate is combined with Alaproclate.
Amphetamine Amphetamine may decrease the sedative activities of Dimenhydrinate.
Phentermine Phentermine may decrease the sedative activities of Dimenhydrinate.
Pseudoephedrine Pseudoephedrine may decrease the sedative activities of Dimenhydrinate.
Benzphetamine Benzphetamine may decrease the sedative activities of Dimenhydrinate.
Diethylpropion Diethylpropion may decrease the sedative activities of Dimenhydrinate.
Lisdexamfetamine Lisdexamfetamine may decrease the sedative activities of Dimenhydrinate.
Mephentermine Mephentermine may decrease the sedative activities of Dimenhydrinate.
MMDA MMDA may decrease the sedative activities of Dimenhydrinate.
Midomafetamine Midomafetamine may decrease the sedative activities of Dimenhydrinate.
2,5-Dimethoxy-4-ethylamphetamine 2,5-Dimethoxy-4-ethylamphetamine may decrease the sedative activities of Dimenhydrinate.
4-Bromo-2,5-dimethoxyamphetamine 4-Bromo-2,5-dimethoxyamphetamine may decrease the sedative activities of Dimenhydrinate.
Tenamfetamine Tenamfetamine may decrease the sedative activities of Dimenhydrinate.
Chlorphentermine Chlorphentermine may decrease the sedative activities of Dimenhydrinate.
Methylenedioxyethamphetamine Methylenedioxyethamphetamine may decrease the sedative activities of Dimenhydrinate.
Dextroamphetamine Dextroamphetamine may decrease the sedative activities of Dimenhydrinate.
Metamfetamine Metamfetamine may decrease the sedative activities of Dimenhydrinate.
Iofetamine I-123 Iofetamine I-123 may decrease the sedative activities of Dimenhydrinate.
Ritobegron Ritobegron may decrease the sedative activities of Dimenhydrinate.
Mephedrone Mephedrone may decrease the sedative activities of Dimenhydrinate.
Methoxyphenamine Methoxyphenamine may decrease the sedative activities of Dimenhydrinate.
Gepefrine Gepefrine may decrease the sedative activities of Dimenhydrinate.
2,5-Dimethoxy-4-ethylthioamphetamine 2,5-Dimethoxy-4-ethylthioamphetamine may decrease the sedative activities of Dimenhydrinate.
Phendimetrazine Phendimetrazine may decrease the sedative activities of Dimenhydrinate.
Amitriptyline The risk or severity of QTc prolongation can be increased when Amitriptyline is combined with Dimenhydrinate.
Cyproheptadine The risk or severity of CNS depression can be increased when Cyproheptadine is combined with Dimenhydrinate.
Imipramine The risk or severity of QTc prolongation can be increased when Imipramine is combined with Dimenhydrinate.
Nortriptyline The risk or severity of CNS depression can be increased when Nortriptyline is combined with Dimenhydrinate.
Amoxapine The risk or severity of CNS depression can be increased when Amoxapine is combined with Dimenhydrinate.
Propiomazine The risk or severity of CNS depression can be increased when Propiomazine is combined with Dimenhydrinate.
Maprotiline The risk or severity of CNS depression can be increased when Maprotiline is combined with Dimenhydrinate.
Doxepin The risk or severity of CNS depression can be increased when Dimenhydrinate is combined with Doxepin.
Desipramine The risk or severity of CNS depression can be increased when Dimenhydrinate is combined with Desipramine.
Pizotifen The risk or severity of CNS depression can be increased when Dimenhydrinate is combined with Pizotifen.
Dosulepin The risk or severity of CNS depression can be increased when Dimenhydrinate is combined with Dosulepin.
Zopiclone The risk or severity of adverse effects can be increased when Dimenhydrinate is combined with Zopiclone.
Dofetilide The risk or severity of QTc prolongation can be increased when Dimenhydrinate is combined with Dofetilide.
Citalopram The risk or severity of QTc prolongation can be increased when Dimenhydrinate is combined with Citalopram.
Anagrelide The risk or severity of QTc prolongation can be increased when Dimenhydrinate is combined with Anagrelide.
Disopyramide The risk or severity of QTc prolongation can be increased when Dimenhydrinate is combined with Disopyramide.
Clemastine The risk or severity of QTc prolongation can be increased when Dimenhydrinate is combined with Clemastine.
Ibutilide The risk or severity of QTc prolongation can be increased when Dimenhydrinate is combined with Ibutilide.
Valproic acid The risk or severity of QTc prolongation can be increased when Dimenhydrinate is combined with Valproic acid.
Terfenadine The risk or severity of QTc prolongation can be increased when Dimenhydrinate is combined with Terfenadine.
Grepafloxacin The risk or severity of QTc prolongation can be increased when Dimenhydrinate is combined with Grepafloxacin.
Quinine The risk or severity of QTc prolongation can be increased when Dimenhydrinate is combined with Quinine.
Sotalol The risk or severity of QTc prolongation can be increased when Dimenhydrinate is combined with Sotalol.
Erlotinib The risk or severity of QTc prolongation can be increased when Dimenhydrinate is combined with Erlotinib.
Toremifene The risk or severity of QTc prolongation can be increased when Dimenhydrinate is combined with Toremifene.
Cisapride The risk or severity of QTc prolongation can be increased when Dimenhydrinate is combined with Cisapride.
Imatinib The risk or severity of QTc prolongation can be increased when Dimenhydrinate is combined with Imatinib.
Astemizole The risk or severity of QTc prolongation can be increased when Dimenhydrinate is combined with Astemizole.
Thioridazine The risk or severity of QTc prolongation can be increased when Dimenhydrinate is combined with Thioridazine.
Trovafloxacin The risk or severity of QTc prolongation can be increased when Dimenhydrinate is combined with Trovafloxacin.

Target Protein

Histamine H1 receptor HRH1

Referensi & Sumber

Synthesis reference: Cusic, J.W.; U.S. Patent 2,499,058; February 28,1950; assigned to G.D. Searle & Co. Cusic, J.W.; U.S. Patent 2,534,813; December 19,1950; assigned to G.D. Searle & Co.
Artikel (PubMed)
  • PMID: 11835984
    Halpert AG, Olmstead MC, Beninger RJ: Mechanisms and abuse liability of the anti-histamine dimenhydrinate. Neurosci Biobehav Rev. 2002 Jan;26(1):61-7.
  • PMID: 4329456
    Jaju BP, Wang SC: Effects of diphenhydramine and dimenhydrinate on vestibular neuronal activity of cat: a search for the locus of their antimotion sickness action. J Pharmacol Exp Ther. 1971 Mar;176(3):718-24.
  • PMID: 3133696
    Spealman RD: Psychomotor stimulant effects of methylxanthines in squirrel monkeys: relation to adenosine antagonism. Psychopharmacology (Berl). 1988;95(1):19-24.
  • PMID: 30406755
    Koch A, Cascorbi I, Westhofen M, Dafotakis M, Klapa S, Kuhtz-Buschbeck JP: The Neurophysiology and Treatment of Motion Sickness. Dtsch Arztebl Int. 2018 Oct 12;115(41):687-696. doi: 10.3238/arztebl.2018.0687.
  • PMID: 18112350
    FLEMING JF: New drug effective in motion sickness. Hosp Top. 1949 Mar;27(3):26.
  • 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: 14856685
    FERMIN H, van DEINSE JB, HAMMELBURG E: The effect of dimenhydrinate upon the labyrinth; (an experimental study). Acta Otolaryngol. 1950 Dec;38(6):543-9. doi: 10.3109/00016485009118417.

Contoh Produk & Brand

Produk: 143 • International brands: 4
Produk
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    Tablet • 50 mg • Oral • Canada • Generic • OTC • Approved
  • Airmit Ace
    Tablet • 25 mg/1 • Oral • US • OTC
  • Anti-nauseant
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    Tablet • 50 mg • Oral • Canada • OTC • Approved
  • Anti-nauseant Liquid Gels
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Menampilkan 8 dari 143 produk.
International Brands
  • Gravol — Church & Dwight
  • Vertirosan — Astellas
  • Vomex A — Astellas
  • Xamamina — Adilna

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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