Meclizine

Synonyms :
Meclizine, Meclozine, Nevidoxine

Status : approved

Category

Anti-Allergic Agents

Therapeutic Classification

ANTIHISTAMINES FOR SYSTEMIC USE

RESPIRATORY SYSTEM
ANTIHISTAMINES FOR SYSTEMIC USE
ANTIHISTAMINES FOR SYSTEMIC USE
Histamine H1 Antagonists

Description

A histamine H1 antagonist used in the treatment of motion sickness, vertigo, and nausea during pregnancy and radiation sickness. [PubChem]

Used

For the prevention and treatment of nausea, vomiting, or dizziness associated with motion sickness.

Mechanism Of Action

Along with its actions as an antagonist at H1-receptors, meclizine also possesses anticholinergic, central nervous system depressant, and local anesthetic effects. Meclizine depresses labyrinth excitability and vestibular stimulation and may affect the medullary chemoreceptor trigger zone.

Dosage

Form Route Strength
Tablet oral 12.5 mg
Tablet oral 25 mg
Tablet oral 50 mg
Tablet oral 50 mg
Tablet (immediate release) oral 25 mg
Tablet (chewable) oral 25 mg
Tablet, orally disintegrating oral 25 mg
Tablet, film coated oral 25 mg
Tablet, chewable oral 25 mg
Tablet, chewable oral 25 mg/251
Film, soluble oral 25 mg

Pharmacodynamics

Meclizine, a piperazine-derivative H1-receptor antagonist similar to buclizine, cyclizine, and hydroxyzine, is used as an antivertigo/antiemetic agent. Meclizine is used in the management of nausea, vomiting, and dizziness associated with motion sickness and vertigo in diseases affecting the vestibular apparatus.

Toxic Effect

Symptoms of overdose include drowsiness and anticholinergic effects. LD50=mg/kg (orally in rat).

Metabolism

Hepatic

Absorption

Well absorbed

Half Life

6 hours

Chemical Classification

This compound belongs to the class of organic compounds known as diphenylmethanes. These are compounds containing a diphenylmethane moiety, which consists of a methane wherein two hydrogen atoms are replaced by two phenyl groups.

Diphenylmethanes

Organic compounds

Benzenoids

Benzene and substituted derivatives

Diphenylmethanes

Salt : Meclizine Hydrochloride

Chemical Name

Meclizine

Brands

name Dosage form Country
Antivert tablet US
Antivert tablet US
Antivert tablet US
Antivert Tab tablet Canada
Bonamine tablet (immediate release) Canada
Bonamine Tab 25mg Chewable tablet (chewable) Canada
Bonine tablet, chewable US
Bonine tablet, chewable US
Cvs Motion Sickness Fast Melting tablet, orally disintegrating US
Dramamine Less Drowsy tablet US
Less Drowsy Formula Motion Sickness Relief tablet US
Less Drowsy Motion Sickness Relief tablet US
Less Drowsy Motion Sickness Relief tablet US
Less Drowsy Motion Sickness Relief tablet US
Less Drowsy Motion Sickness Relief tablet US
Meclizine tablet US
Meclizine tablet US
Meclizine Hcl tablet US
Meclizine Hcl tablet US
Meclizine Hcl tablet US
Meclizine Hcl tablet US
Meclizine Hcl tablet US
Meclizine Hcl tablet US
Meclizine Hcl tablet US
Meclizine Hcl tablet, chewable US
Meclizine Hcl tablet US
Meclizine Hcl tablet US
Meclizine Hcl tablet US
Meclizine Hcl tablet US
Meclizine Hcl tablet US
Meclizine Hydrochloride tablet US
Meclizine Hydrochloride tablet US
Meclizine Hydrochloride tablet US
Meclizine Hydrochloride tablet US
Meclizine Hydrochloride tablet US
Meclizine Hydrochloride tablet US
Meclizine Hydrochloride tablet US
Meclizine Hydrochloride tablet US
Meclizine Hydrochloride tablet US
Meclizine Hydrochloride tablet US
Meclizine Hydrochloride tablet US
Meclizine Hydrochloride tablet US
Meclizine Hydrochloride tablet US
Meclizine Hydrochloride tablet US
Meclizine Hydrochloride tablet US
Meclizine Hydrochloride tablet US
Meclizine Hydrochloride tablet US
Meclizine Hydrochloride tablet US
Meclizine Hydrochloride tablet US
Meclizine Hydrochloride tablet US
Meclizine Hydrochloride tablet US
Meclizine Hydrochloride tablet US
Meclizine Hydrochloride tablet US
Meclizine Hydrochloride tablet US
Meclizine Hydrochloride tablet US
Meclizine Hydrochloride tablet US
Meclizine Hydrochloride tablet US
Meclizine Hydrochloride tablet US
Meclizine Hydrochloride tablet US
Meclizine Hydrochloride tablet US
Meclizine Hydrochloride tablet US
Meclizine Hydrochloride tablet US
Meclizine Hydrochloride tablet US
Meclizine Hydrochloride tablet US
Meclizine Hydrochloride tablet US
Meclizine Hydrochloride tablet US
Meclizine Hydrochloride tablet US
Meclizine Hydrochloride tablet US
Meclizine Hydrochloride tablet US
Meclizine Hydrochloride tablet US
Meclizine Hydrochloride tablet US
Meclizine Hydrochloride tablet US
Meclizine Hydrochloride tablet US
Meclizine Hydrochloride tablet US
Meclizine Hydrochloride tablet US
Meclizine Hydrochloride tablet US
Meclizine Hydrochloride tablet US
Meclizine Hydrochloride tablet US
Meclizine Hydrochloride tablet US
Meclizine Hydrochloride tablet US
Meclizine Hydrochloride tablet US
Meclizine Hydrochloride tablet US
Meclizine Hydrochloride tablet US
Meclizine Hydrochloride tablet US
Meclizine Hydrochloride tablet US
Meclizine Hydrochloride tablet US
Meclizine Hydrochloride tablet US
Meclizine Hydrochloride tablet US
Meclizine Hydrochloride tablet US
Meclizine Hydrochloride tablet US
Meclizine Hydrochloride tablet US
Meclizine Hydrochloride tablet US
Meclizine Hydrochloride tablet US
Meclizine Hydrochloride tablet US
Meclizine Hydrochloride tablet US
Meclizine Hydrochloride tablet US
Meclizine Hydrochloride tablet US
Meclizine Hydrochloride tablet US
Meclizine Hydrochloride tablet US
Meclizine Hydrochloride tablet US
Meclizine Hydrochloride tablet US
Meclizine Hydrochloride tablet US
Meclizine Hydrochloride tablet US
Medique Medi-meclizine tablet, film coated US
Medique Medi-meclizine tablet US
Motion Relief – Less Drowsy Formula tablet US
Motion Sickness tablet US
Motion Sickness tablet US
Motion Sickness Ii tablet US
Motion Sickness Ii tablet US
Motion Sickness Ii tablet US
Motion Sickness Ii tablet US
Motion Sickness Ii tablet US
Motion Sickness Ii tablet US
Motion Sickness less drowsy formula tablet US
Motion Sickness Less Drowsy Formula tablet US
Motion Sickness less drowsy formula tablet US
Motion Sickness Relief tablet, chewable US
Motion Sickness Relief tablet US
Motion Sickness Relief tablet US
Motion Sickness Relief tablet US
Motion Sickness Relief tablet, chewable US
Motion Sickness Relief tablet US
Motion Sickness Relief tablet, chewable US
Motion Sickness Relief tablet US
Motion Sickness Relief tablet US
Motion Sickness Relief tablet US
Motion Sickness Relief tablet, chewable US
Motion Sickness Relief tablet US
Motion Sickness Relief tablet US
Motion Sickness Relief Less Drowsy tablet US
Motion-time Chewable tablet, chewable US
Naus-ease film, soluble US
Naus-ease tablet US
Rugby Meclizine HCl, 12.5 mg Each ANTIEMETIC tablet US
Rugby Travel Sickness Meclizine HCl, 25 mg Each (ANTIEMETIC) tablet, chewable US
Rugby Travel Sicknessmeclizine Hcl, 25 Mg Each (antiemetic) Meclizine HCl, 25 mg Each (ANTIEMETIC) tablet, chewable US
Rugbymeclizine Hcl, 12.5 Mg Each Antiemetic Meclizine HCl, 12.5 mg Each ANTIEMETIC tablet US
Sea-calm tablet, chewable US
Trav-l-tabs tablet US
Travel Ease tablet, chewable US
Travel Time tablet, chewable US
Travel-ease tablet US
Verticalm tablet US
Zentrip film, soluble US

Drug Drug Interactions

  •  Aclidinium  : May enhance the anticholinergic effect of Anticholinergic Agents.
  •  Amphetamine  : May diminish the sedative effect of Antihistamines.
  •  Benzylpenicilloyl Polylysine  : Antihistamines may diminish the diagnostic effect of Benzylpenicilloyl Polylysine.
  •  Betahistine  : Antihistamines may diminish the therapeutic effect of Betahistine.
  •  Botulinum Toxin Type A  : Anticholinergic Agents may enhance the anticholinergic effect of AbobotulinumtoxinA.
  •  Botulinum Toxin Type A  : Anticholinergic Agents may enhance the anticholinergic effect of OnabotulinumtoxinA.
  •  Botulinum Toxin Type B  : Anticholinergic Agents may enhance the anticholinergic effect of RimabotulinumtoxinB.
  •  Buprenorphine  : CNS Depressants may enhance the CNS depressant effect of Buprenorphine.
  •  Cathinone  : May diminish the sedative effect of Antihistamines.
  •  Doxylamine  : May enhance the CNS depressant effect of CNS Depressants.
  •  Dronabinol  : May enhance the CNS depressant effect of CNS Depressants.
  •  Dronabinol  : May enhance the CNS depressant effect of CNS Depressants.
  •  Droperidol  : May enhance the CNS depressant effect of CNS Depressants.
  •  Glucagon recombinant  : Anticholinergic Agents may enhance the adverse/toxic effect of Glucagon. Specifically, the risk of gastrointestinal adverse effects may be increased.
  •  Hyaluronidase  : Antihistamines may diminish the therapeutic effect of Hyaluronidase.
  •  Hydrocodone  : CNS Depressants may enhance the CNS depressant effect of Hydrocodone.
  •  Hydroxyzine  : May enhance the CNS depressant effect of CNS Depressants.
  •  Itopride  : Anticholinergic Agents may diminish the therapeutic effect of Itopride.
  •  Magnesium Sulfate  : May enhance the CNS depressant effect of CNS Depressants.
  •  Methotrimeprazine  : CNS Depressants may enhance the CNS depressant effect of Methotrimeprazine. Methotrimeprazine may enhance the CNS depressant effect of CNS Depressants.
  •  Metyrosine  : CNS Depressants may enhance the sedative effect of Metyrosine.
  •  Mianserin  : May enhance the anticholinergic effect of Anticholinergic Agents.
  •  Minocycline  : May enhance the CNS depressant effect of CNS Depressants.
  •  Mirabegron  : Anticholinergic Agents may enhance the adverse/toxic effect of Mirabegron.
  •  Mirtazapine  : CNS Depressants may enhance the CNS depressant effect of Mirtazapine.
  •  Nabilone  : May enhance the CNS depressant effect of CNS Depressants.
  •  Orphenadrine  : CNS Depressants may enhance the CNS depressant effect of Orphenadrine.
  •  Paraldehyde  : CNS Depressants may enhance the CNS depressant effect of Paraldehyde.
  •  Perampanel  : May enhance the CNS depressant effect of CNS Depressants.
  •  Potassium Chloride  : Anticholinergic Agents may enhance the ulcerogenic effect of Potassium Chloride.
  •  Pramipexole  : CNS Depressants may enhance the sedative effect of Pramipexole.
  •  Pramlintide  : May enhance the anticholinergic effect of Anticholinergic Agents. These effects are specific to the GI tract.
  •  Ropinirole  : CNS Depressants may enhance the sedative effect of Ropinirole.
  •  Rotigotine  : CNS Depressants may enhance the sedative effect of Rotigotine.
  •  Rufinamide  : May enhance the adverse/toxic effect of CNS Depressants. Specifically, sleepiness and dizziness may be enhanced.
  •  Secretin  : Anticholinergic Agents may diminish the therapeutic effect of Secretin.
  •  Sodium oxybate  : May enhance the CNS depressant effect of CNS Depressants.
  •  Sulpiride  : Anticholinergic Agents may diminish the therapeutic effect of LevoSulpiride.
  •  Suvorexant  : CNS Depressants may enhance the CNS depressant effect of Suvorexant.
  •  Tapentadol  : May enhance the CNS depressant effect of CNS Depressants.
  •  Thalidomide  : CNS Depressants may enhance the CNS depressant effect of Thalidomide.
  •  Tiotropium  : Anticholinergic Agents may enhance the anticholinergic effect of Tiotropium.
  •  Topiramate  : Anticholinergic Agents may enhance the adverse/toxic effect of Topiramate.
  •  Umeclidinium  : May enhance the anticholinergic effect of Anticholinergic Agents.
  •  Zolpidem  : CNS Depressants may enhance the CNS depressant effect of Zolpidem.

Food Interactions

  • Take with food to reduce irritation. Avoid alcohol.

Calculated Property

kind Value Source
logP 5.59 ALOGPS
logS -5.6 ALOGPS
Water Solubility 1.03e-03 g/l ALOGPS
logP 6.39 ChemAxon
IUPAC Name 1-[(4-chlorophenyl)(phenyl)methyl]-4-[(3-methylphenyl)methyl]piperazine ChemAxon
Traditional IUPAC Name meclizine ChemAxon
Molecular Weight 390.948 ChemAxon
Monoisotopic Weight 390.186276581 ChemAxon
SMILES CC1=CC(CN2CCN(CC2)C(C2=CC=CC=C2)C2=CC=C(Cl)C=C2)=CC=C1 ChemAxon
Molecular Formula C25H27ClN2 ChemAxon
InChI 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 ChemAxon
InChIKey InChIKey=OCJYIGYOJCODJL-UHFFFAOYSA-N ChemAxon
Polar Surface Area (PSA) 6.48 ChemAxon
Refractivity 119.39 ChemAxon
Polarizability 44.87 ChemAxon
Rotatable Bond Count 5 ChemAxon
H Bond Acceptor Count 2 ChemAxon
H Bond Donor Count 0 ChemAxon
pKa (strongest basic) 8.16 ChemAxon
Physiological Charge 1 ChemAxon
Number of Rings 4 ChemAxon
Bioavailability 1 ChemAxon
Rule of Five 0 ChemAxon
Ghose Filter 0 ChemAxon
MDDR-Like Rule 0 ChemAxon

Affected organism

Humans and other mammals

Target within organism

  • Histamine H1 receptor : in Human