Description

Simple

A medication used to treat the symptoms of motion sickness.

Clinical

A histamine H1 antagonist used to treat nausea, vomiting, and dizziness associated with motion sickness.

Overview

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.[4] Commonly marketed under the brand name Antivert in the U.S., meclizine is available as oral tablets.

Pharmacology

Indication

Indicated for the symptomatic treatment of nausea, vomiting, and dizziness associated with motion sickness,[6] and management of vertigo due to various causes, including radiation sickness, Meniere’s syndrome, labyrin... Read more

Pharmacodynamic

Meclizine works on the higher centres of the brain to reduce nausea, vomiting, or vertigo. It is effective against nausea and vomiting arising from many causes, including motion sickness and disorders affecting the vestibular system. The onset of action of meclizine is about 1 hour, with effects las... Read more

Mechanism of action

Vomiting is a centrally regulated reflex mechanism that initiates from the vomiting center and the chemoreceptor trigger zone (CTZ) located in the medulla. Motion sickness is also regulated by CTZ. The blood-brain barrier near the CTZ is relatively permeable to circulating mediators and CTZ can tran... Read more

Absorption

Most histamine H1 antagonists are reported to be readily absorbed following oral administration.[4] Upon oral administration, the time to reach peak plasma concentrations (Cmax) o... Read more

Protein binding

There is limited data on the protein binding profile of meclizine.

Volume of distribution

The volume of distribution of meclizine in humans has not been fully studied. It is proposed that meclizine may be excreted into breast milk.[4]

Clearance

There is limited data on the clearance of meclizine.

Half life

Meclizine has a plasma elimination half-life of about 5-6 hours in humans.[6]

Route of elimination

Meclizine is excreted in the urine as metabolites and in the feces as unchanged drug.[4]

Toxicity

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... Read more

Adverse Effects

Contraindications

  • Route:
    • Oral
  • Hypersensitivity:
    • true
  • Sex Group: all
  • Regions: US

Food Interactions

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

Interactions

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  • Paracetamol(acetaminophen)
  • Paxil(paroxetine)
  • Pamelor(nortriptyline)
  • Panadol(acetaminophen)
  • Patanol(olopatadine ophthalmic)
  • Pataday(olopatadine ophthalmic)
  • Parnate(tranylcypromine)
  • Pazeo(olopatadine ophthalmic)
1-(2-Phenylethyl)-4-phenyl-4-acetoxypiperidine
The metabolism of Meclizine can be decreased when combined with 1-(2-Phenylethyl)-4-phenyl-4-acetoxypiperidine.
2,5-Dimethoxy-4-ethylamphetamine
2,5-Dimethoxy-4-ethylamphetamine may decrease the sedative and stimulatory activities of Meclizine.
2,5-Dimethoxy-4-ethylthioamphetamine
2,5-Dimethoxy-4-ethylthioamphetamine may decrease the sedative and stimulatory activities of Meclizine.
4-Bromo-2,5-dimethoxyamphetamine
4-Bromo-2,5-dimethoxyamphetamine may decrease the sedative and stimulatory activities of Meclizine.
4-Methoxyamphetamine
The risk or severity of adverse effects can be increased when Meclizine is combined with 4-Methoxyamphetamine.
5-methoxy-N,N-dimethyltryptamine
The risk or severity of adverse effects can be increased when Meclizine is combined with 5-methoxy-N,N-dimethyltryptamine.
7-Nitroindazole
The risk or severity of adverse effects can be increased when Meclizine is combined with 7-Nitroindazole.
7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline
The risk or severity of adverse effects can be increased when Meclizine is combined with 7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline.
Abatacept
The metabolism of Meclizine can be increased when combined with Abatacept.
Abiraterone
The metabolism of Meclizine can be decreased when combined with Abiraterone.
Acebutolol
The metabolism of Meclizine can be decreased when combined with Acebutolol.
Acepromazine
The risk or severity of adverse effects can be increased when Meclizine is combined with Acepromazine.
Aceprometazine
The risk or severity of adverse effects can be increased when Meclizine is combined with Aceprometazine.
Acetaminophen
The metabolism of Meclizine can be decreased when combined with Acetaminophen.
Acetazolamide
The risk or severity of adverse effects can be increased when Meclizine is combined with Acetazolamide.
Acetophenazine
The risk or severity of adverse effects can be increased when Meclizine is combined with Acetophenazine.
Acetylglycinamide chloral hydrate
The risk or severity of adverse effects can be increased when Meclizine is combined with Acetylglycinamide chloral hydrate.
Aclidinium
Meclizine may increase the central nervous system depressant (CNS depressant) activities of Aclidinium.
Adalimumab
The metabolism of Meclizine can be increased when combined with Adalimumab.
Adinazolam
The risk or severity of adverse effects can be increased when Adinazolam is combined with Meclizine.
6 References
  1. 1 . 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.PubMed: 26381004
  2. 2 . 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.PubMed: 21903894
  3. 3 . 29. (2012). In Rang and Dale's Pharmacology (7th ed., pp. 365-367). Edinburgh: Elsevier/Churchill Livingstone.
  4. 4 . Antivert (meclizine hydrochloride) - Drug Summary - PDR.net Link
  5. 5 . BONAMINE® (Meclizine Hydrochloride Tablets 25 mg, USP) - Product Monograph Link
  6. 6 . ANTIVERT® - FDA Label Link