Summary: A histamine H1 antagonist used in the treatment of motion sickness, vertigo, and nausea during pregnancy and radiation sickness.

Top Publications

  1. Lin J, Ho Y, Lee J, Liu C, Yang T, Wu C. Induction of apoptosis and cell-cycle arrest in human colon cancer cells by meclizine. Food Chem Toxicol. 2007;45:935-44 pubmed
    b>Meclizine (MEC), a histamine H1 antagonist, is used for the treatment of motion sickness and vertigo. In this study, we demonstrate that MEC dose-dependently induced apoptosis in human colon cancer cell lines (COLO 205 and HT 29 cells)...
  2. Wang Z, Lee B, Pearce D, Qian S, Wang Y, Zhang Q, et al. Meclizine metabolism and pharmacokinetics: formulation on its absorption. J Clin Pharmacol. 2012;52:1343-9 pubmed publisher
    b>Meclizine, an antihistamine, has been widely used for prophylactic treatment and management of motion sickness. However, the onset of action of meclizine was about 1 hour for the treatment of motion sickness and vertigo...
  3. Huang W, Zhang J, Wei P, Schrader W, Moore D. Meclizine is an agonist ligand for mouse constitutive androstane receptor (CAR) and an inverse agonist for human CAR. Mol Endocrinol. 2004;18:2402-8 pubmed
    ..Here we identify the widely used antiemetic meclizine (Antivert; Bonine) as both an agonist ligand for mCAR and an inverse agonist for hCAR...
  4. Gohil V, Sheth S, Nilsson R, Wojtovich A, Lee J, Perocchi F, et al. Nutrient-sensitized screening for drugs that shift energy metabolism from mitochondrial respiration to glycolysis. Nat Biotechnol. 2010;28:249-55 pubmed publisher
    ..We identify several clinically used drugs never linked to energy metabolism, including the antiemetic meclizine, which attenuates mitochondrial respiration through a mechanism distinct from that of canonical inhibitors...
  5. Gohil V, Offner N, Walker J, Sheth S, Fossale E, Gusella J, et al. Meclizine is neuroprotective in models of Huntington's disease. Hum Mol Genet. 2011;20:294-300 pubmed publisher
    ..Here, we show that meclizine, a clinically used drug that we have recently shown to silence oxidative metabolism, suppresses apoptotic cell ..
  6. Dornhoffer J, Chelonis J, Blake D. Stimulation of the semicircular canals via the rotary chair as a means to test pharmacologic countermeasures for space motion sickness. Otol Neurotol. 2004;25:740-5 pubmed
    ..Lorazepam 1 mg, meclizine 25 mg, promethazine 25 mg, scopolamine 0.4 mg, or placebo...
  7. Paule M, Chelonis J, Blake D, Dornhoffer J. Effects of drug countermeasures for space motion sickness on working memory in humans. Neurotoxicol Teratol. 2004;26:825-37 pubmed
    ..DMTS) procedure was used to assess visual working memory before and after drug countermeasures (meclizine 25 mg, scopolamine 0...
  8. Estrada A, LeDuc P, Curry I, Phelps S, Fuller D. Airsickness prevention in helicopter passengers. Aviat Space Environ Med. 2007;78:408-13 pubmed
    ..these, 16 subjects were randomly assigned to each of 4 groups: (1) promethazine (25 mg) + caffeine (200 mg); (2) meclizine (25 mg); (3) Scopolamine patch (1.5 mg); and 4) acustimulation wristband...
  9. Amorim C, Henriques M, Weg V, Cordeiro R, Vargaftig B. Effect of PAF-acether antagonists on active anaphylactic mouse paw edema. Lipids. 1991;26:1396-9 pubmed
    ..In contrast, vasoactive amines appear to be involved, because meclizine and methysergide reduced the edema...

More Information


  1. Levinson H. Dramatic favorable responses of children with learning disabilities or dyslexia and attention deficit disorder to antimotion sickness medications: four case reports. Percept Mot Skills. 1991;73:723-38 pubmed
    ..These cases were selected from a prior quantitative study in which three antihistamines (meclizine, cyclizine, dimenhydrinate) and three stimulants (pemoline, methylphenidate, dextroamphetamine) were tested in ..
  2. Kimura S, Nishiyama T, Imai T, Otagiri M. Improved dissolution and absorption of drugs using low molecular gelatin. Acta Pharm Nord. 1990;2:65-72 pubmed
    Kneaded mixtures of a basic drug, meclizine dihydrochloride (MZ), and a neutral drug, prednisolone (PN), with low molecular gelatin at the weight ratio of 1:1 were prepared, and their in vitro dissolution and in vivo absorption behaviour ..
  3. Kallen B, Mottet I. Delivery outcome after the use of meclozine in early pregnancy. Eur J Epidemiol. 2003;18:665-9 pubmed
    ..If anything, delivery outcome is better than expected when the mother used meclozine. These beneficial effects are probably secondary to NVP. Meclozine can apparently be used without risk at this condition. ..
  4. Lau A, Yang G, Rajaraman G, Baucom C, Chang T. Differential effect of meclizine on the activity of human pregnane X receptor and constitutive androstane receptor. J Pharmacol Exp Ther. 2011;336:816-26 pubmed publisher
    Conflicting data exist as to whether meclizine is an activator of human pregnane X receptor (hPXR)...
  5. Forrester C, Benfield D, Matern C, Kelly J, Pellegrini J. Meclizine in combination with ondansetron for prevention of postoperative nausea and vomiting in a high-risk population. AANA J. 2007;75:27-33 pubmed
    ..b>Meclizine, a long-acting drug with a low side-effect profile, may be ideal in combination with ondansetron for at-risk ..
  6. Ahmed M. Comparison of impact of the different hydrophilic carriers on the properties of piperazine-containing drug. Eur J Pharm Biopharm. 2001;51:221-5 pubmed
    ..was to determine the impact of a series of nonionic surfactants on the solubility of piperazine-containing drug (meclizine, MZ) in comparison to that of natural cyclodextrins (alpha-CD and beta-CD) and dimethyl-beta-cyclodextrin (DM-..
  7. Chang T, Waxman D. Synthetic drugs and natural products as modulators of constitutive androstane receptor (CAR) and pregnane X receptor (PXR). Drug Metab Rev. 2006;38:51-73 pubmed
    ..This article discusses the importance of these receptors for pharmacology and toxicology, emphasizing the role of individual drugs and natural products as agonists, indirect activators, inverse agonists, and antagonists of CAR and PXR. ..
  8. Arayne M, Sultana N, Siddiqui F, Zuberi M, Mirza A. Spectrophotometric methods for the simultaneous analysis of meclezine hydrochloride and pyridoxine hydrochloride in bulk drug and pharmaceutical formulations. Pak J Pharm Sci. 2007;20:149-56 pubmed
    ..The suggested procedures were successfully applied to the determination of these compounds in synthetic mixtures and in pharmaceutical preparations, with high percentage of recovery, good accuracy and precision. ..
  9. Castro Faria Neto H, Bozza P, Silva A, Silva P, Lima M, Martins M, et al. Interference of azelastine with anaphylaxis induced by ovalbumin challenge in actively sensitized rats. Eur J Pharmacol. 1992;213:183-8 pubmed
    ..Pretreatment with meclizine or terfenadine (15-30 mg/kg i.p.) inhibited antigen-induced haemoconcentration, whereas WEB 2086 (2-10 mg/kg i.p...
  10. Lavich T, Cordeiro R, Calixto J, E Silva P, Martins M. Combined action of vasoactive amines and bradykinin mediates allergen-evoked thermal hyperalgesia in rats. Eur J Pharmacol. 2003;462:185-92 pubmed
    ..Allergen-evoked hyperalgesia was inhibited by intraperitoneal treatment with meclizine or methysergide, histamine and 5-hydroxytryptamine receptor antagonists...
  11. Parada C, Tambeli C, Cunha F, Ferreira S. The major role of peripheral release of histamine and 5-hydroxytryptamine in formalin-induced nociception. Neuroscience. 2001;102:937-44 pubmed
    ..was demonstrated by the treatment of the rat hindpaws with selective histamine H1 (pyrilamine and meclizine) and histamine H2 (cimetidine) receptor antagonists or selective 5-hydroxytryptamine(1A) (WAY100,135) and 5-..
  12. Patel P, Ezzo D. Withdrawal symptoms after discontinuation of transdermal scopolamine therapy: treatment with meclizine. Am J Health Syst Pharm. 2009;66:2024-6 pubmed publisher
    The case of a patient who treated withdrawal symptoms from trans-dermal scopolamine with meclizine is reported...
  13. Kvist C, Andersson S, Fors S, Wennergren B, Berglund J. Apparatus for studying in vitro drug release from medicated chewing gums. Int J Pharm. 1999;189:57-65 pubmed
    ..nicotine), Travvell((R)) (dimenhydrinate), V6((R)) (xylitol) and an experimental formulation containing meclizine. The main usage of the present apparatus should be within quality control but the present study has also shown ..
  14. Lauter J, Lynch O, Wood S, Schoeffler L. Physiological and behavioral effects of an antivertigo antihistamine in adults. Percept Mot Skills. 1999;88:707-32 pubmed
    12 neurologically normal adults were tested before and after administration of meclizine, an over-the-counter medication for motion sickness...
  15. Horak F, Jones Rycewicz C, Black F, Shumway Cook A. Effects of vestibular rehabilitation on dizziness and imbalance. Otolaryngol Head Neck Surg. 1992;106:175-80 pubmed
    ..This study takes the first step toward determining the efficacy of a specific exercise approach for reducing dizziness and imbalance in patients with chronic peripheral vestibular disorders. ..
  16. Sharma S, Saxena R, Talwar S. Simultaneous spectrophotometric analysis of a ternary mixture of pharmaceuticals--assay for meclozine hydrochloride, pyridoxine hydrochloride and caffeine. J Pharm Biomed Anal. 1989;7:321-7 pubmed
    ..01 M methanolic sodium hydroxide as the solvent, the absorbance of the solution of the mixture is recorded at 230, 273 and 307 nm. The concentration of each component is determined by the solution of three simultaneous equations. ..
  17. Fagan J, Kaplan B, Raymond J, Edgington E. The failure of antimotion sickness medication to improve reading in developmental dyslexia: results of a randomized trial. J Dev Behav Pediatr. 1988;9:359-66 pubmed
    ..5 mg meclizine, both methylphenidate and meclizine, or placebo...
  18. Burda A, Webster K, Leikin J, Chan S, Stokes K. Nefazadone-induced acute dystonic reaction. Vet Hum Toxicol. 1999;41:321-2 pubmed
    ..Chief complaint was lip smacking with hand and arm gesturing. The patient also took 25 mg meclizine which she had used before with no adverse effects...
  19. de Alencar N, Mota M, Rodrigues N, Martins J, do Nascimento K, Assreuy A, et al. Neutrophil-infiltrated paw edema induced by mannose-binding Dioclea violacea lectin. Pharmacol Rep. 2013;65:220-5 pubmed
    ..Dexamethasone, meclizine and N?-nitro-L-arginine methyl ester hydrochloride (L-NAME) inhibited this effect...
  20. Paul M, MacLellan M, Gray G. Motion-sickness medications for aircrew: impact on psychomotor performance. Aviat Space Environ Med. 2005;76:560-5 pubmed
    ..The purpose of this study was to assess the impact on psychomotor performance of promethazine, meclizine, and dimenhydrinate and to determine if the addition of pseudoephedrine or damphetamine to promethazine would ..
  21. Bent S, Fehling U, Braam U, Schunack W, Schmutzler W. The influence of H1-, H2- and H3-receptors on the spontaneous and ConA induced histamine release from human adenoidal mast cells. Agents Actions. 1991;33:67-70 pubmed
    ..This enhancement might be taken as an indication of the existence of H3-receptor dependent autoregulation although presently other mechanism cannot be excluded...
  22. Ho Y, Wu H, Wu S, Chen S, Kou H. Quantitative enantiomeric analysis of chlorcyclizine, hydroxyzine, and meclizine by capillary electrophoresis. Anal Bioanal Chem. 2003;376:859-63 pubmed
    ..Enantioseparation of chlorcyclizine, hydroxyzine, and meclizine was performed in glycine buffer (0.6 mol L(-1); pH 3...
  23. Goenechea V, Rucker G, Brzezinka H, Hoffmann G, Neugebauer M, Glanzmann G. [Biotransformation of meclozine in the human body]. J Clin Chem Clin Biochem. 1988;26:105-15 pubmed
    ..The structure of compound 11 was confirmed after enzymatic cleavage and identification of the aglycon. A further metabolite was detected, but not identified. ..
  24. Sarang S, Yoshida T, Cadet R, Valeras A, Jensen R, Gullans S. Discovery of molecular mechanisms of neuroprotection using cell-based bioassays and oligonucleotide arrays. Physiol Genomics. 2002;11:45-52 pubmed
    ..We identified 26 neuroprotective compounds, of which megestrol, meclizine, verapamil, methazolamide, sulindac, and retinol were examined in greater detail...
  25. Wang Z, Qian S, Zhang Q, Chow M. Quantification of meclizine in human plasma by high performance liquid chromatography-mass spectrometry. J Chromatogr B Analyt Technol Biomed Life Sci. 2011;879:95-9 pubmed publisher
    b>Meclizine is an antihistamine and has been widely used for prophylactic treatment of motion sickness...
  26. Murray J. Psychophysiological aspects of motion sickness. Percept Mot Skills. 1997;85:1163-7 pubmed
    ..Susceptibility can be reduced in most people by medications that involve histamine or neurotransmitters acetylcholine and noradrenaline, and influence the vestibular system. ..
  27. Tauqeer S, Khan R, Siddiqui A. Evaluation of teratogenic effects of risperidone following simultaneous administration with antihypertensive and antiemetic drugs. Pak J Pharm Sci. 2012;25:261-6 pubmed
    ..In present study, the teratogenic effects of multiple drug administration risperidone, meclizine/pyridoxine and hydralazine have been compared with the teratogenic effects of individual drugs in pregnant mice...
  28. Weerts A, De Meyer G, Pauwels G, Vanspauwen R, Dornhoffer J, Van de Heyning P, et al. Pharmaceutical countermeasures have opposite effects on the utricles and semicircular canals in man. Audiol Neurootol. 2012;17:235-42 pubmed publisher
    ..The current study focuses on the effects of lorazepam (1 mg), meclizine (25 mg), promethazine (25 mg), and scopolamine (0...
  29. Kuo C, Pang L, Chang R. Vertigo - part 2 - management in general practice. Aust Fam Physician. 2008;37:409-13 pubmed
    ..A simple program including patient education and home based exercises can be sufficient. ..
  30. Gohil V, Zhu L, Baker C, Cracan V, Yaseen A, Jain M, et al. Meclizine inhibits mitochondrial respiration through direct targeting of cytosolic phosphoethanolamine metabolism. J Biol Chem. 2013;288:35387-95 pubmed publisher
    We recently identified meclizine, an over-the-counter drug, as an inhibitor of mitochondrial respiration. Curiously, meclizine blunted respiration in intact cells but not in isolated mitochondria, suggesting an unorthodox mechanism...
  31. Abdel Ghani N, Shoukry A, Issa Y, Wahdan O. Spectrophotometric determination of meclozine HCl and papaverine HCl in their pharmaceutical formulations. J Pharm Biomed Anal. 2002;28:373-8 pubmed
    ..63-100.80 and 99.75-100.08% and coefficient of variation 0.945-2.210 and 1.020-1.268 for meclozine HCl and papaverine HCl, respectively. ..
  32. Mirza T, Lunn M, Keeley F, George R, Bodenmiller J. Cleaning level acceptance criteria and a high pressure liquid chromatography procedure for the assay of Meclizine Hydrochloride residue in swabs collected from pharmaceutical manufacturing equipment surfaces. J Pharm Biomed Anal. 1999;19:747-56 pubmed
    ..pharmacologically based and visual limit of detection criteria to determine the acceptable residue level for Meclizine Hydrochloride (MH) on pharmaceutical manufacturing equipment surfaces after cleaning is described...
  33. Raymond E, Creinin M, Barnhart K, Lovvorn A, Rountree R, Trussell J. Meclizine for prevention of nausea associated with use of emergency contraceptive pills: a randomized trial. Obstet Gynecol. 2000;95:271-7 pubmed
    We conducted a randomized trial to determine whether pretreatment with meclizine reduces the incidence of nausea and vomiting associated with the Yuzpe regimen of emergency contraception...
  34. Pasquale C, e Silva P, Lima M, Diaz B, Rihoux J, Vargaftig B, et al. Suppression by cetirizine of pleurisy triggered by antigen in actively sensitized rats. Eur J Pharmacol. 1992;223:9-14 pubmed
    The efficacy of cetirizine in comparison with meclizine, another piperazine H1 receptor antagonist, in rat pleurisy caused by allergen or autacoid was investigated...
  35. Baloh R. Approach to the dizzy patient. Baillieres Clin Neurol. 1994;3:453-65 pubmed
    ..Repeated head, eye and body movements (vestibular rehabilitation) help the brain to recalibrate the relationship between visual, proprioceptive and vestibular signals (Chapter 9). ..
  36. Castro Faria Neto H, Martins M, Bozza P, Perez S, Correa Da Silva A, Lima M, et al. Pro-inflammatory activity of enterolobin: a haemolytic protein purified from seeds of the Brazilian tree Enterolobium contortisiliquum. Toxicon. 1991;29:1143-50 pubmed
    ..The H1 antagonist, meclizine (25 mg/kg), was also effective against enterolobin oedema while the PAF-antagonists WEB 2086 and PCA 4248 (20 mg/..
  37. Kuykendall J, Rhodes R. Auditory hallucinations elicited by combined meclizine and metaxalone use at bedtime. Ann Pharmacother. 2004;38:1968-9 pubmed
  38. Sansone R, Sears C. The successful use of meclizine in panic disorder. J Clin Psychiatry. 2004;65:1285-6 pubmed
  39. Kvist L, Andersson S, Berglund J, Wennergren B, Fors S. Equipment for drug release testing of medicated chewing gums. J Pharm Biomed Anal. 2000;22:405-11 pubmed
    ..The tested gum formulations comprised nicotine, meclizine, dimenhydrinate and xylitol...
  40. Bopp E, Estrada T, Kilday J, Spradling J, Daniel C, Pellegrini J. Biphasic dosing regimen of meclizine for prevention of postoperative nausea and vomiting in a high-risk population. AANA J. 2010;78:55-62 pubmed
    The purpose of this study was to determine if giving 50 mg of meclizine the night before and on the day of surgery would effectively reduce postoperative nausea and vomiting (PONV) for the entire 24 hours after surgery in patients ..
  41. Brookler K. Vestibular findings in a 62-year-old woman with dizziness and a type I Chiari malformation. Ear Nose Throat J. 2005;84:630-1 pubmed
  42. Wright E, Busby S, Wisecarver S, Vincent J, Griffin P, Fernandez E. Helix 11 dynamics is critical for constitutive androstane receptor activity. Structure. 2011;19:37-44 pubmed publisher
    ..can occur in the absence of exogenous ligand and this activity is enhanced by agonists TCPOBOP and meclizine. We use biophysical and cell-based assays to show that increased activity of CAR(TCPOBOP) relative to CAR(..
  43. Vanspauwen R, Weerts A, Hendrickx M, Buytaert K, Blaivie C, Jorens P, et al. No effects of anti-motion sickness drugs on vestibular evoked myogenic potentials outcome parameters. Otol Neurotol. 2011;32:497-503 pubmed publisher
    To investigate the effects of meclizine (50 mg), baclofen (10 mg), cinnarizine (20 mg) + dimenhydrinate (40 mg), and promethazine (25 mg) + dextro-amphetamine (5 mg) on the parameters of the vestibular evoked myogenic potential (VEMP) ..
  44. Manning C, Scandale L, Manning E, Gengo F. Central nervous system effects of meclizine and dimenhydrinate: evidence of acute tolerance to antihistamines. J Clin Pharmacol. 1992;32:996-1002 pubmed
    Relative daytime drowsiness and performance impairment produced by meclizine and dimenhydrinate was assessed in 24 healthy male volunteers...
  45. Amorim C, Cordeiro R, Vargaftig B. Interference of antihistamines and anti-allergic drugs with antigen-induced paw edema in boosted and unboosted mice. Eur J Pharmacol. 1992;216:429-34 pubmed
    ..The antihistamine meclizine and the mixed anti histamine/anti-5-HT antagonist cyproheptadine reduced the anaphylactic reaction by 55 and 84% ..
  46. Gleyzer N, Scarpulla R. Activation of a PGC-1-related coactivator (PRC)-dependent inflammatory stress program linked to apoptosis and premature senescence. J Biol Chem. 2013;288:8004-15 pubmed publisher
    ..The potential adaptive function of the PRC stress response was investigated by treating cells with meclizine, a drug that promotes glycolytic energy metabolism and has been linked to cardio- and neuroprotection against ..
  47. Fischer M, Paulussen J, Horbach D, Roelofsen E, van Miltenburg J, de Mol N, et al. Inhibition of mediator release in RBL-2H3 cells by some H1-antagonist derived anti-allergic drugs: relation to lipophilicity and membrane effects. Inflamm Res. 1995;44:92-7 pubmed
    ..This could affect several membrane related processes, which are abundant in the early phases of the IgE-mediated signal transduction process. ..
  48. Kochevar I, Moran M, Lyon N, Flotte T, Siebert E, Gange R. Effects of systemic indomethacin, meclizine, and BW755C on chronic ultraviolet B-induced effects in hairless mouse skin. J Invest Dermatol. 1993;100:186-93 pubmed
    ..Indomethacin, a cyclooxygenase inhibitor, and meclizine, an H1 histamine receptor antagonist, were administered from slow-release pellets...
  49. Tsuji Y, Kakegawa H, Miyataka H, Nishiki M, Matsumoto H, Satoh T. Pharmaceutical properties of freeze-dried formulations of egg albumin, several drugs and olive oil. Biol Pharm Bull. 1996;19:636-40 pubmed
    The freeze-dried ternary formulations of meclizine (MZ, an anti-motion sickness drug), prednisolone (PRED, an anti-inflammatory drug) and norfloxacin (NFLX, an anti-microbial drug) which are poorly water-soluble and are low ..