Peringatan Keamanan

The oral and intraperitoneal LD50 in mouse are 1600 mg/kg and 625 mg/kg, respectively. The lowest published toxic dose (TDLo) in rats via the oral route is 800 mg/kg.MSDS

Symptoms of overdose mainly involve CNS depression with drowsiness, coma, and convulsions. Hypotension may also occur, particularly in the elderly. In children, anticholinergic effects and CNS stimulation, characterized by hallucinations, seizures, trouble sleeping, are more likely to occur. In case of overdose, symptomatic and supportive treatment is recommended. In case of recent ingestion, induction of emesis or gastric lavage should be initiated to limit further drug absorption. Although there is no known antidote to meclizine, physostigmine may be useful to counteract the CNS anticholinergic effects of meclizine.L6766

Meclizine

DB00737

small molecule approved

Deskripsi

Meclizine is a histamine H1 antagonist with antiemetic and antivertigo properties. It is used in the symptomatic treatment of motion sickness and control of vertigo associated with vestibular system diseases. It also exhibits anticholinergic, central nervous system depressant, and local anesthetic effects.L6760 Commonly marketed under the brand name Antivert in the U.S., meclizine is available as oral tablets.

Struktur Molekul 2D

Berat 390.948
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) Meclizine has a plasma elimination half-life of about 5-6 hours in humans.[L6772]
Volume Distribusi The volume of distribution of meclizine in humans has not been fully studied. It is proposed that meclizine may be excreted into breast milk.[L6760]
Klirens (Clearance) There is limited data on the clearance of meclizine.

Absorpsi

Most histamine H1 antagonists are reported to be readily absorbed following oral administration.L6760 Upon oral administration, the time to reach peak plasma concentrations (Cmax) of meclizine is about 3 hours post-dose, with the value ranging from 1.5 to 6 hours.L6772

Metabolisme

There is limited human data on meclizine metabolism. According to the findings of in vitro studies, meclizine may undergo aromatic hydroxylation or benzylic oxidation mediated by the hepatic CYP2D6 enzyme.A179584

Rute Eliminasi

Meclizine is excreted in the urine as metabolites and in the feces as unchanged drug.L6760

Interaksi Makanan

1 Data
  • 1. Avoid alcohol. Alcohol may cause additive CNS depressant effects.

Interaksi Obat

1112 Data
Buprenorphine Meclizine 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 Meclizine.
Dronabinol Dronabinol may increase the central nervous system depressant (CNS depressant) activities of Meclizine.
Droperidol Droperidol may increase the central nervous system depressant (CNS depressant) activities of Meclizine.
Hydrocodone Meclizine 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 Meclizine.
Magnesium sulfate The therapeutic efficacy of Meclizine can be increased when used in combination with Magnesium sulfate.
Methotrimeprazine Meclizine may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
Metyrosine Meclizine may increase the sedative activities of Metyrosine.
Minocycline Minocycline may increase the central nervous system depressant (CNS depressant) activities of Meclizine.
Mirtazapine Meclizine 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 Meclizine.
Orphenadrine Meclizine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
Paraldehyde Meclizine 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 Meclizine.
Pramipexole Meclizine may increase the sedative activities of Pramipexole.
Ropinirole Meclizine may increase the sedative activities of Ropinirole.
Rotigotine Meclizine may increase the sedative activities of Rotigotine.
Rufinamide The risk or severity of adverse effects can be increased when Rufinamide is combined with Meclizine.
Sodium oxybate Meclizine may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Suvorexant Meclizine 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 Meclizine.
Thalidomide Meclizine may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
Zolpidem Meclizine may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
Benzylpenicilloyl polylysine Meclizine may decrease effectiveness of Benzylpenicilloyl polylysine as a diagnostic agent.
Betahistine The therapeutic efficacy of Betahistine can be decreased when used in combination with Meclizine.
Methadone The risk or severity of adverse effects can be increased when Methadone is combined with Meclizine.
Mirabegron The serum concentration of Meclizine can be increased when it is combined with Mirabegron.
Ethanol Meclizine may increase the central nervous system depressant (CNS depressant) activities of Ethanol.
Azelastine Meclizine 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 Meclizine.
Citalopram The risk or severity of adverse effects can be increased when Meclizine is combined with Citalopram.
Trazodone The risk or severity of adverse effects can be increased when Meclizine is combined with Trazodone.
Sertraline The risk or severity of adverse effects can be increased when Meclizine is combined with Sertraline.
Sibutramine The risk or severity of adverse effects can be increased when Meclizine is combined with Sibutramine.
Nefazodone The risk or severity of adverse effects can be increased when Meclizine is combined with Nefazodone.
Zimelidine The risk or severity of adverse effects can be increased when Meclizine is combined with Zimelidine.
Dapoxetine The risk or severity of adverse effects can be increased when Meclizine is combined with Dapoxetine.
Milnacipran The risk or severity of adverse effects can be increased when Meclizine is combined with Milnacipran.
Desvenlafaxine The serum concentration of Meclizine can be increased when it is combined with Desvenlafaxine.
Seproxetine The risk or severity of adverse effects can be increased when Meclizine is combined with Seproxetine.
Indalpine The risk or severity of adverse effects can be increased when Meclizine is combined with Indalpine.
Alaproclate The risk or severity of adverse effects can be increased when Meclizine is combined with Alaproclate.
Amphetamine Amphetamine may decrease the sedative activities of Meclizine.
Phentermine Phentermine may decrease the sedative activities of Meclizine.
Pseudoephedrine Pseudoephedrine may decrease the sedative activities of Meclizine.
Benzphetamine Benzphetamine may decrease the sedative activities of Meclizine.
Diethylpropion Diethylpropion may decrease the sedative activities of Meclizine.
Lisdexamfetamine Lisdexamfetamine may decrease the sedative activities of Meclizine.
Mephentermine Mephentermine may decrease the sedative activities of Meclizine.
MMDA MMDA may decrease the sedative activities of Meclizine.
Midomafetamine Midomafetamine may decrease the sedative activities of Meclizine.
2,5-Dimethoxy-4-ethylamphetamine 2,5-Dimethoxy-4-ethylamphetamine may decrease the sedative activities of Meclizine.
4-Bromo-2,5-dimethoxyamphetamine 4-Bromo-2,5-dimethoxyamphetamine may decrease the sedative activities of Meclizine.
Tenamfetamine Tenamfetamine may decrease the sedative activities of Meclizine.
Chlorphentermine Chlorphentermine may decrease the sedative activities of Meclizine.
Methylenedioxyethamphetamine Methylenedioxyethamphetamine may decrease the sedative activities of Meclizine.
Dextroamphetamine Dextroamphetamine may decrease the sedative activities of Meclizine.
Metamfetamine Metamfetamine may decrease the sedative activities of Meclizine.
Iofetamine I-123 Iofetamine I-123 may decrease the sedative activities of Meclizine.
Ritobegron Ritobegron may decrease the sedative activities of Meclizine.
Mephedrone Mephedrone may decrease the sedative activities of Meclizine.
Methoxyphenamine Methoxyphenamine may decrease the sedative activities of Meclizine.
Gepefrine Gepefrine may decrease the sedative activities of Meclizine.
2,5-Dimethoxy-4-ethylthioamphetamine 2,5-Dimethoxy-4-ethylthioamphetamine may decrease the sedative activities of Meclizine.
Phendimetrazine Phendimetrazine may decrease the sedative activities of Meclizine.
Trospium The risk or severity of adverse effects can be increased when Trospium is combined with Meclizine.
Oxyphenonium The risk or severity of adverse effects can be increased when Oxyphenonium is combined with Meclizine.
Benzatropine The risk or severity of adverse effects can be increased when Benzatropine is combined with Meclizine.
Disopyramide The risk or severity of adverse effects can be increased when Disopyramide is combined with Meclizine.
Ipratropium The risk or severity of adverse effects can be increased when Ipratropium is combined with Meclizine.
Metixene The risk or severity of adverse effects can be increased when Metixene is combined with Meclizine.
Buclizine The risk or severity of adverse effects can be increased when Buclizine is combined with Meclizine.
Trihexyphenidyl The risk or severity of adverse effects can be increased when Trihexyphenidyl is combined with Meclizine.
Oxyphencyclimine The risk or severity of adverse effects can be increased when Oxyphencyclimine is combined with Meclizine.
Procyclidine The risk or severity of adverse effects can be increased when Procyclidine is combined with Meclizine.
Profenamine The risk or severity of adverse effects can be increased when Profenamine is combined with Meclizine.
Cyproheptadine The risk or severity of CNS depression can be increased when Cyproheptadine is combined with Meclizine.
Methscopolamine bromide The risk or severity of adverse effects can be increased when Methscopolamine bromide is combined with Meclizine.
Tridihexethyl The risk or severity of adverse effects can be increased when Tridihexethyl is combined with Meclizine.
Anisotropine methylbromide The risk or severity of adverse effects can be increased when Anisotropine methylbromide is combined with Meclizine.
Atropine The risk or severity of adverse effects can be increased when Atropine is combined with Meclizine.
Pirenzepine The risk or severity of adverse effects can be increased when Pirenzepine is combined with Meclizine.
Homatropine methylbromide The risk or severity of adverse effects can be increased when Homatropine methylbromide is combined with Meclizine.
Benzquinamide The risk or severity of adverse effects can be increased when Meclizine is combined with Benzquinamide.
Propiomazine The risk or severity of CNS depression can be increased when Meclizine is combined with Propiomazine.
Propantheline The risk or severity of adverse effects can be increased when Meclizine is combined with Propantheline.
Dicyclomine The risk or severity of adverse effects can be increased when Meclizine is combined with Dicyclomine.
Biperiden The metabolism of Meclizine can be decreased when combined with Biperiden.
Maprotiline The risk or severity of CNS depression can be increased when Meclizine is combined with Maprotiline.
Methantheline The risk or severity of adverse effects can be increased when Meclizine is combined with Methantheline.
Cycrimine The risk or severity of adverse effects can be increased when Meclizine is combined with Cycrimine.
Glycopyrronium The risk or severity of adverse effects can be increased when Meclizine is combined with Glycopyrronium.
Tolterodine The risk or severity of adverse effects can be increased when Meclizine is combined with Tolterodine.
Oxybutynin The metabolism of Meclizine can be decreased when combined with Oxybutynin.
Flavoxate The risk or severity of adverse effects can be increased when Meclizine is combined with Flavoxate.
Diphenidol The risk or severity of adverse effects can be increased when Meclizine is combined with Diphenidol.
Tiotropium The risk or severity of adverse effects can be increased when Meclizine is combined with Tiotropium.
Solifenacin The risk or severity of adverse effects can be increased when Meclizine is combined with Solifenacin.
Isopropamide The risk or severity of adverse effects can be increased when Meclizine is combined with Isopropamide.

Target Protein

Histamine H1 receptor HRH1
Nuclear receptor subfamily 1 group I member 3 NR1I3

Referensi & Sumber

Synthesis reference: U.S. Patent 2,709,169.
Artikel (PubMed)
  • PMID: 26381004
    Amini A, Heidari K, Kariman H, Taghizadeh M, Hatamabadi H, Shahrami A, Derakhshanfar H, Asadollahi S: Histamine Antagonists for Treatment of Peripheral Vertigo: A Meta-Analysis. J Int Adv Otol. 2015 Aug;11(2):138-42. doi: 10.5152/iao.2015.1169.
  • PMID: 21903894
    Wang Z, Lee B, Pearce D, Qian S, Wang Y, Zhang Q, Chow MS: Meclizine metabolism and pharmacokinetics: formulation on its absorption. J Clin Pharmacol. 2012 Sep;52(9):1343-9. doi: 10.1177/0091270011414575. Epub 2011 Sep 8.
Textbook
  • ISBN: 978-0-7020-3471-8
    29. (2012). In Rang and Dale's Pharmacology (7th ed., pp. 365-367). Edinburgh: Elsevier/Churchill Livingstone.

Contoh Produk & Brand

Produk: 437 • International brands: 6
Produk
  • Antivert
    Tablet • 25 mg/1 • Oral • US • Approved
  • Antivert
    Tablet • 12.5 mg/1 • Oral • US • Approved
  • Antivert
    Tablet • 25 mg/1 • Oral • US • Approved
  • Antivert
    Tablet • 50 mg/1 • Oral • US • Approved
  • Antivert
    Tablet, chewable • 25 mg/1 • Oral • US • Approved
  • Antivert
    Tablet • 12.5 mg/1 • Oral • US • Approved
  • Antivert
    Tablet • 25 mg/1 • Oral • US • Approved
  • Antivert
    Tablet • 50 mg/1 • Oral • US • Approved
Menampilkan 8 dari 437 produk.
International Brands
  • Chiclida
  • Meclicot
  • Navicalm
  • Nevidoxine
  • Postafen
  • Sea-Legs

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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