"Dramamine II" redirects here. For other uses, see Dramamine (disambiguation) .
Meclizine Trade names Bonine, Antivert, others Other names Meclozine AHFS /Drugs.com Monograph MedlinePlus a682548 License data
Routes of administration By mouth, under the tongue , in the cheek ATC code Legal status
AU : S4 (Prescription only)
CA : OTC
US : OTC
Metabolism Liver Elimination half-life 6 hours show
(RS )-1-[(4-chlorophenyl)(phenyl)methyl]-4-(3-methylbenzyl)piperazine
CAS Number PubChem CID IUPHAR/BPS DrugBank ChemSpider UNII ChEMBL CompTox Dashboard (EPA ) ECHA InfoCard 100.008.477 Formula C 25 H 27 Cl N 2 Molar mass 390.96 g·mol−1 3D model (JSmol ) Boiling point 230 °C (446 °F) show
Clc1ccc(cc1)C(c2ccccc2)N3CCN(CC3)Cc4cccc(c4)C
show
InChI=1S/C25H27ClN2/c1-20-6-5-7-21(18-20)19-27-14-16-28(17-15-27)25(22-8-3-2-4-9-22)23-10-12-24(26)13-11-23/h2-13,18,25H,14-17,19H2,1H3
Y Key:OCJYIGYOJCODJL-UHFFFAOYSA-N
Y
N Y (what is this?)
Meclizine , sold under the brand name Bonine , among others, is an antihistamine used to treat motion sickness and dizziness (vertigo ).[1] It is taken by mouth.[1] Effects generally begin in an hour and last for up to a day.[1]
Common side effects include sleepiness and dry mouth.[1] Serious side effects may include allergic reactions .[1] Use in pregnancy appears safe, but has not been well studied while use in breastfeeding is of unclear safety.[2] It is believed to work in part by anticholinergic and antihistamine mechanisms.[1]
Meclizine was patented in 1951 and came into medical use in 1953.[3] It is available as a generic medication and often over the counter .[1] [4] In 2018, it was the 139th most commonly prescribed medication in the United States, with more than 4 million prescriptions.[5] [6]
Medical uses [ ]
Meclizine is used to treat symptoms of motion sickness . Safety and efficacy in children younger than twelve years of age has not been established; therefore, use in this population is not recommended.[citation needed ] Meclizine should be taken with caution in the elderly due to increased risk of confusion and amnesia .[7]
Motion sickness [ ]
Meclizine is effective in inhibiting nausea, vomiting, and dizziness caused by motion sickness .[8]
The drug is safe for treating nausea in pregnancy and is a first-line therapy for this use.[9] [10] Doxylamine is similarly safe. Meclizine may not be strong enough for especially sickening motion stimuli and second-line defenses should be tried in those cases.[11]
Vertigo [ ]
Meclizine may be used to treat motion sickness or vertigo such as in those with Meniere's disease .[12] [13]
Side effects [ ]
Some common side effects such as drowsiness, dry mouth, and tiredness may occur. Meclizine has been shown to have fewer dry mouth side effects than the traditional treatment for motion sickness, transdermal scopolamine .[14] A very serious allergic reaction to this drug is unlikely, but immediate medical attention should be sought if it occurs. Symptoms of a serious allergic reaction may include rash, itching, swelling, severe dizziness, and trouble breathing.[15]
Drowsiness [ ]
Drowsiness may result as a side effect of taking meclizine. Users are advised not to operate heavy machinery while under the influence. The consumption of alcohol while under the influence of meclizine may result in additional drowsiness.[1]
Elderly [ ]
As with any anticholinergic agent, meclizine may cause confusion or aggravate symptoms in those with dementia in the geriatric population (older than 65 years). Therefore, caution should be used when administering meclizine to the elderly.[16]
Mechanism of action [ ]
Meclizine is an antagonist at H1 receptors. It possesses anticholinergic , central nervous system depressant , and local anesthetic effects. Its antiemetic and antivertigo effects are not fully understood, but its central anticholinergic properties are partially responsible. The drug depresses labyrinth excitability and vestibular stimulation, and it may affect the medullary chemoreceptor trigger zone .[17] It has however been suggested that meclizine only has an inhibitory effect under normal viewing-circumstances, as the drug has been shown to enhance an isolated vestibular response. Much like motion-sickness arises from a discrepancy between multiple senses, Meclizine most likely affects a wide array of sensory mechanisms related to self-motion.[18]
Meclizine also is a dopamine antagonist at D1 -like and D2 -like receptors[citation needed ] but does not cause catalepsy [note 1] in mice, perhaps because of its anticholinergic activity.[19]
Chemistry [ ]
Meclizine is a first-generation antihistamine (nonselective H1 antagonist ) of the piperazine class. It is structurally and pharmacologically similar to buclizine , cyclizine , and hydroxyzine , but has a shorter half-life of six hours compared to cyclizine and hydroxyzine with about 20 hours (though half-life should not be confused with duration).[citation needed ] It is used as an antivertigo/antiemetic agent, specifically in the prevention and treatment of nausea, vomiting, and dizziness associated with motion sickness.[17] Meclizine is sometimes combined with opioids, especially ones of the open-chain class like methadone , dextropropoxyphene , and dipipanone . Similarly, Diconal is a combination drug containing dipipanone and cyclizine .[citation needed ]
Synthesis [ ]
(4-Chlorphenyl)-phenylmethanol is halogenated with thionyl chloride before adding acetylpiperazine. The acetyl group is cleaved with diluted sulfuric acid . An N-alkylation of the piperazine ring with 3-methylbenzylchloride completes the synthesis.[20]
Alternatively, the last step can be replaced by a reductive N-alkylation with 3-methylbenzaldehyde. The reductive agent is hydrogen , and Raney nickel is used as a catalyst .[21] [22]
Meclizine is obtained and used as a racemate , a 1:1 mixture of the two stereoisomers . Drug forms contain the racemic dihydrochloride.[citation needed ]
Names [ ]
Meclizine is an international nonproprietary name .[23]
It is sold under the brand names Bonine, Bonamine, Antivert, Postafen, Sea Legs, and Dramamine II (Less Drowsy Formulation). Emesafene is a combination of meclizine (1/3) and pyridoxine (2/3). In Canada, Antivert Tab (which is no longer available) was a combination of meclizine and nicotinic acid .[24]
Notes [ ]
^ "[C]atalepsy was assessed by the bar method[:] the front paws were gently placed on a horizontal metal bar with 2 mm diameter suspended 4 cm above, and the length of time the mouse maintains this abnormal posture was measured."[19]
References [ ]
^ Jump up to: a b c d e f g h "Meclizine Hydrochloride Monograph for Professionals" . Drugs.com . American Society of Health-System Pharmacists. Retrieved 22 March 2019 .
^ "Meclizine Use During Pregnancy" . Drugs.com . Retrieved 3 March 2019 .
^ Fischer J, Ganellin CR (2006). Analogue-based Drug Discovery . John Wiley & Sons. p. 547. ISBN 9783527607495 .
^ Cappa M, Cianfarani S, Ghizzoni L, Loche S, Maghnie M (2015). Advanced Therapies in Pediatric Endocrinology and Diabetology: Workshop, Rome, October 2014 . Karger Medical and Scientific Publishers. p. 101. ISBN 9783318056372 .
^ "The Top 300 of 2021" . ClinCalc . Retrieved 18 February 2021 .
^ "Meclizine Hydrochloride - Drug Usage Statistics" . ClinCalc . Retrieved 18 February 2021 .
^ MICROMEDEX 2.0 . Accessed 7 November 2010.[full citation needed ]
^ "Drugs & Medications" . www.webmd.com . Retrieved 28 December 2018 .
^ "Antiemetische Therapie bei Schwangerschaftserbrechen" [Antiemetic therapy in pregnancy]. Arznei-Telegramm (in German). 40 : 87–89. 2009.
^ Embryotox: Meclozin (in German)
^ Lawson BD, McGee HA, Castaneda MA, Golding JF, Kass SJ, McGrath CM (2 December 2009). "Evaluation of several common antimotion sickness medications and recommendations concerning their potential usefulness during special operations" . Pensacola, Florida: Naval Aerospace Research Lab. Archived from the original on 27 April 2016. Retrieved 7 February 2016 .
^ Nakashima, T; Pyykkö, I; Arroll, MA; Casselbrant, ML; Foster, CA; Manzoor, NF; Megerian, CA; Naganawa, S; Young, YH (12 May 2016). "Meniere's disease". Nature Reviews. Disease Primers . 2 : 16028. doi :10.1038/nrdp.2016.28 . PMID 27170253 . S2CID 3987838 .
^ "Meclizine" . LiverTox . 2017. PMID 31643231 .
^ Dahl E, Offer-Ohlsen D, Lillevold PE, Sandvik L (July 1984). "Transdermal scopolamine, oral meclizine, and placebo in motion sickness". Clinical Pharmacology and Therapeutics . 36 (1): 116–20. doi :10.1038/clpt.1984.148 . PMID 6734040 . S2CID 40691502 .
^ Meclizine - oral, Antivert, D-vert, Dramamine II . Accessed 7 November 2010.
^ Merck Manuals, Online Medical Library: Meclizine (Drug Information Provided by Lexi-Comp) , revised January 2010, accessed 7 November 2010.
^ Jump up to: a b Clinical Pharmacology. Clinical Pharmacology , revised 20 November 2009, accessed 7 November 2010.[full citation needed ]
^ Wibble, T; Engström, J; Verrecchia, L; Pansell, T (2020). "The effects of meclizine on motion sickness revisited" . Br J Clin Pharmacol . 86 (8): 1510–1518. doi :10.1111/bcp.14257 . PMC 7373708 . PMID 32077140 .
^ Jump up to: a b Haraguchi K, Ito K, Kotaki H, Sawada Y, Iga T (June 1997). "Prediction of drug-induced catalepsy based on dopamine D1 , D2 , and muscarinic acetylcholine receptor occupancies" . Drug Metabolism and Disposition . 25 (6): 675–84. PMID 9193868 .
^ Fuhrkop JH, Li G (2003). Organic Synthesis. Concepts and Methods . Wiley. p. 237. ISBN 978-3-527-30272-7 .
^ US 2 709 169 (UCB, 1955)
^ Kleemann A, Engel J, Kutscher B, Reichert D (2001). Pharmaceutical Substances. Synthesis, Patents, Applications (4th ed.). Thieme. ISBN 3-13-115134-X .
^ Guidelines on the Use of INNs for Pharmaceutical Substances (1997). Accessed November, 2013 "Guidance on INN." WHO.
^ DrugBank. Drugbank: Drug card for Meclizine David Wishard: University of Alberta, Canada. Accessed 7 November 2010.
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Anisodamine
Anisodine
Antihistamines (first-generation) (e.g., brompheniramine , buclizine , captodiame , chlorphenamine (chlorpheniramine) , cinnarizine , clemastine , cyproheptadine , dimenhydrinate , dimetindene , diphenhydramine , doxylamine , meclizine , mequitazine , perlapine , phenindamine , pheniramine , phenyltoloxamine , promethazine , propiomazine , triprolidine )
Atropine
Atropine methonitrate
Atypical antipsychotics (e.g., clozapine , fluperlapine , olanzapine (+fluoxetine ), , quetiapine , tenilapine , zotepine )
Benactyzine
Benzatropine (benztropine)
Benzilone
Benzilylcholine mustard
Benzydamine
Biperiden
Bornaprine
Camylofin
CAR-226,086
CAR-301,060
CAR-302,196
CAR-302,282
CAR-302,668
Caramiphen
Cimetropium bromide
Clidinium bromide
Cloperastine
CS-27349
Cyclobenzaprine
Cyclopentolate
Darifenacin
Desfesoterodine
Dexetimide
Dicycloverine (dicyclomine)
Dihexyverine
Difemerine
Diphemanil metilsulfate
Ditran
Drofenine
EA-3167
EA-3443
EA-3580
EA-3834
Emepronium bromide
Etanautine
Etybenzatropine (ethybenztropine)
Fenpiverinium
Fentonium bromide
Fesoterodine
Flavoxate
Glycopyrronium bromide (+beclometasone/formoterol , +indacaterol )
Hexocyclium
Himbacine
Homatropine
Imidafenacin
Ipratropium bromide (+salbutamol )
Isopropamide
Hyoscyamine
Mamba toxin 3
Mamba toxin 7
Mazaticol
Mebeverine
Meladrazine
Mepenzolate
Methantheline
Methoctramine
Methylatropine
Methylhomatropine
Methylscopolamine
Metixene
Muscarinic toxin 7
N-Ethyl-3-piperidyl benzilate
N-Methyl-3-piperidyl benzilate
Nefopam
Octatropine methylbromide (anisotropine methylbromide)
Orphenadrine
Otenzepad (AF-DX 116)
Otilonium bromide
Oxapium iodide
Oxitropium bromide
Oxybutynin
Oxyphencyclimine
Oxyphenonium bromide
PD-102,807
PD-0298029
Penthienate
Pethidine
Phenglutarimide
Phenyltoloxamine
Pipenzolate bromide
Piperidolate
Pirenzepine
Piroheptine
Pizotifen
Poldine
Pridinol
Prifinium bromide
Procyclidine
Profenamine (ethopropazine)
Propantheline bromide
Propiverine
Quinidine
3-Quinuclidinyl thiochromane-4-carboxylate
Revefenacin
Rociverine
Scopolamine (hyoscine)
Scopolamine butylbromide (hyoscine butylbromide)
Sofpironium bromide
Solifenacin
SSRIs (e.g., femoxetine , paroxetine )
Telenzepine
Terodiline
Tetracyclic antidepressants (e.g., amoxapine , maprotiline , mianserin , mirtazapine )
Tiemonium iodide
Timepidium bromide
Tiotropium bromide
Tofenacin
Tolterodine
Tricyclic antidepressants (e.g., amitriptyline (+perphenazine ), amitriptylinoxide , butriptyline , cidoxepin , clomipramine , desipramine , , dibenzepin , dosulepin (dothiepin) , doxepin , imipramine , lofepramine , nitroxazepine , northiaden (desmethyldosulepin) , nortriptyline , protriptyline , quinupramine , trimipramine )
Tridihexethyl
Trihexyphenidyl
Trimebutine
Tropatepine
Tropicamide
Trospium chloride
Typical antipsychotics (e.g., chlorpromazine , chlorprothixene , cyamemazine (cyamepromazine) , loxapine , mesoridazine , thioridazine )
Umeclidinium bromide (+vilanterol )
WIN-2299
Xanomeline
Precursors (and prodrugs )
Acetyl-coA
Adafenoxate
Choline (lecithin )
Citicoline
Cyprodenate
Dimethylethanolamine
Glycerophosphocholine
Meclofenoxate (centrophenoxine)
Phosphatidylcholine
Phosphatidylethanolamine
Phosphorylcholine
Pirisudanol
See also: Receptor/signaling modulators • Nicotinic acetylcholine receptor modulators • Acetylcholine metabolism/transport modulators
show CAR
Agonists:
Amiodarone
Artemisinin
Carbamazepine
Carvedilol
Chlorpromazine
Chrysin
Clotrimazole
Cyclophosphamide
Cypermethrin
DHEA (prasterone )
Efavirenz
Ellagic acid
Griseofulvin
Methoxychlor
Mifepristone
Nefazodone
Nevirapine
Nicardipine
Permethrin
Phenobarbital
Phenytoin
Pregnanedione (5β-dihydroprogesterone)
Reserpine
Telmisartan
Tolnaftate
Troglitazone
Valproic acid
PXR
See also
Receptor/signaling modulators