Identification

Logo pink
Are you a
new drug developer?
Contact us to learn more about our customized products and solutions.
Logo pink
Stay in the know!
As part of our commitment to providing the most up-to-date drug information, we will be releasing #DrugBankUpdates with our newly added curated drug pages.
#DrugBankUpdates
Name
Meclizine
Accession Number
DB00737  (APRD00354)
Type
Small Molecule
Groups
Approved
Description

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.

Structure
Thumb
Synonyms
  • Meclizine
  • Meclozina
  • Meclozine
External IDs
U.C.B. 5062 / UCB 170 / UCB 5062
Product Ingredients
IngredientUNIICASInChI Key
Meclizine hydrochlorideHDP7W44CIO31884-77-2BAAVORPTHSKWGJ-UHFFFAOYSA-N
Product Images
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
AntivertTablet50 mg/1OralRoerig1997-04-11Not applicableUs
AntivertTablet25 mg/1OralRoerig1997-04-11Not applicableUs
AntivertTablet12.5 mg/1OralRoerig1997-04-11Not applicableUs
AntivertTablet25 mg/1OralPhysicians Total Care, Inc.1997-04-112012-06-30Us
Meclizine HydrochlorideTablet12.5 mg/1OralWatson Pharmaceuticals2006-03-28Not applicableUs
Meclizine HydrochlorideTablet25 mg/1OralWatson Pharmaceuticals2006-03-28Not applicableUs
Additional Data Available
  • Application Number
    Application Number

    A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

    Learn more
  • Product Code
    Product Code

    A governmentally-recognized ID which uniquely identifies the product within its regulatory market.

    Learn more
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
MeclizineTablet12.5 mg/1OralDirectrx2016-04-28Not applicableUs
Meclizine HydrochlorideTablet25 mg/1OralH.J. Harkins Company2010-06-04Not applicableUs
Meclizine HydrochlorideTablet25 mg/1OralLiberty Pharmaceuticals, Inc.1981-06-03Not applicableUs
Meclizine HydrochlorideTablet25 mg/1OralNucare Pharmaceuticals, Inc.2012-04-30Not applicableUs
Meclizine HydrochlorideTablet12.5 mg/1Oralbryant ranch prepack2012-04-30Not applicableUs
Meclizine HydrochlorideTablet25 mg/1OralDoh Central Pharmacy2017-10-26Not applicableUs
Meclizine HydrochlorideTablet12.5 mg/1OralREMEDYREPACK INC.2018-09-06Not applicableUs
Meclizine HydrochlorideTablet25 mg/1OralNCS HealthCare of KY, Inc dba Vangard Labs2012-04-302020-04-30Us
Meclizine HydrochlorideTablet12.5 mg/1OralUDL Laboratories, Inc.2008-10-012016-06-30Us
Meclizine HydrochlorideTablet25 mg/1Oralbryant ranch prepack1981-06-032015-09-30Us63629 126620180913 8702 1q5d5qa
Additional Data Available
  • Application Number
    Application Number

    A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

    Learn more
  • Product Code
    Product Code

    A governmentally-recognized ID which uniquely identifies the product within its regulatory market.

    Learn more
Over the Counter Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
BonamineTablet, multilayer, extended releaseOralMcneil Consumer Healthcare Division Of Johnson & Johnson IncNot applicableNot applicableCanada
Bonamine Tab 25mg ChewableTablet, chewableOralMcneil Consumer Healthcare Division Of Johnson & Johnson Inc1954-12-312011-08-04Canada
BonineTablet, chewable25 mg/1OralInsight Pharmaceuticals2009-06-08Not applicableUs
BonineTablet, chewable25 mg/1OralWellSpring Pharmaceutical Corporation2017-04-18Not applicableUs
BonineTablet, chewable25 mg/1OralWellSpring Pharmaceutical Corporation2014-12-15Not applicableUs
CVS Motion Sickness Fast MeltingTablet, orally disintegrating25 mg/1OralCVS Health2015-08-27Not applicableUs
CVS Motion Sickness StripsFilm, soluble25 mg/1OralCVS PHARMACY2019-02-20Not applicableUs
DramamineTablet, chewable25 mg/1OralMedtech Products Inc.2019-02-15Not applicableUs
Dramamine - NTablet25 mg/1OralMedtech Products Inc.2018-01-15Not applicableUs
Dramamine Less DrowsyTablet25 mg/1OralMedtech Products Inc.2011-09-01Not applicableUs
Additional Data Available
  • Application Number
    Application Number

    A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

    Learn more
  • Product Code
    Product Code

    A governmentally-recognized ID which uniquely identifies the product within its regulatory market.

    Learn more
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing End
Antivert TabMeclizine hydrochloride (12.5 mg) + Niacin (50 mg)TabletOralPfizer Canada Ulc1956-12-312000-01-24Canada
International/Other Brands
Chiclida / Meclicot / Navicalm / Nevidoxine / Postafen / Sea-Legs
Categories
UNII
3L5TQ84570
CAS number
569-65-3
Weight
Average: 390.948
Monoisotopic: 390.186276581
Chemical Formula
C25H27ClN2
InChI Key
OCJYIGYOJCODJL-UHFFFAOYSA-N
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
IUPAC Name
1-[(4-chlorophenyl)(phenyl)methyl]-4-[(3-methylphenyl)methyl]piperazine
SMILES
CC1=CC(CN2CCN(CC2)C(C2=CC=CC=C2)C2=CC=C(Cl)C=C2)=CC=C1

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, labyrinthitis and other vestibular disturbances.5

Associated Conditions
Pharmacodynamics

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 lasting between 8 to 24 hours.4 Meclizine is reported to cause drowsiness due to its anticholinergic actions.5

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 transmit impulses to vomiting center located in the brainstem. Different receptors responding to different factors, including histamine, 5-HT, enkephalins, substance P, and dopamine, are expressed along the brainstem to activate respective pathways and contribute to the control of vomiting. Histamine H1 receptors are expressed on the vestibular nuclei and nucleus of the solitary tract (NTS) that are activated by motion sickness and stimuli from the pharynx and stomach. When activated, H1 receptor signaling from these nuclei is transmitted to the CTZ and vomiting centre.3

Through its antagonistic action on the H1 receptors, meclizine primarily works by inhibiting signaling pathway transduction through histaminergic neurotransmission from the vestibular nuclei and NTS to the CTZ and medullary vomiting center.1 Meclizine may also decrease the labyrinth excitability and vestibular stimulation.4

TargetActionsOrganism
AHistamine H1 receptor
antagonist
Humans
UNuclear receptor subfamily 1 group I member 3
inverse agonist
Humans
Additional Data Available
Adverse Effects

Comprehensive structured data on known drug adverse effects with statistical prevalence. MedDRA and ICD10 ids are provided for adverse effect conditions and symptoms.

Learn more
Additional Data Available
Contraindications

Structured data covering drug contraindications. Each contraindication describes a scenario in which the drug is not to be used. Includes restrictions on co-administration, contraindicated populations, and more.

Learn more
Additional Data Available
Blackbox Warnings

Structured data representing warnings from the black box section of drug labels. These warnings cover important and dangerous risks, contraindications, or adverse effects.

Learn 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) of meclizine is about 3 hours post-dose, with the value ranging from 1.5 to 6 hours.6

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

Protein binding

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

Metabolism

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.2

Route of elimination

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

Half life

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

Clearance

There is limited data on the clearance of meclizine.

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 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.5

Affected organisms
  • Humans and other mammals
Pathways
PathwayCategory
Meclizine H1-Antihistamine ActionDrug action
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
DrugInteraction
1-(2-Phenylethyl)-4-phenyl-4-acetoxypiperidineThe metabolism of Meclizine can be decreased when combined with 1-(2-Phenylethyl)-4-phenyl-4-acetoxypiperidine.
2,5-Dimethoxy-4-ethylamphetamine2,5-Dimethoxy-4-ethylamphetamine may decrease the sedative and stimulatory activities of Meclizine.
2,5-Dimethoxy-4-ethylthioamphetamine2,5-Dimethoxy-4-ethylthioamphetamine may decrease the sedative and stimulatory activities of Meclizine.
4-Bromo-2,5-dimethoxyamphetamine4-Bromo-2,5-dimethoxyamphetamine may decrease the sedative and stimulatory activities of Meclizine.
4-MethoxyamphetamineThe risk or severity of adverse effects can be increased when Meclizine is combined with 4-Methoxyamphetamine.
5-methoxy-N,N-dimethyltryptamineThe risk or severity of adverse effects can be increased when Meclizine is combined with 5-methoxy-N,N-dimethyltryptamine.
7-NitroindazoleThe risk or severity of adverse effects can be increased when Meclizine is combined with 7-Nitroindazole.
7,8-Dichloro-1,2,3,4-tetrahydroisoquinolineThe risk or severity of adverse effects can be increased when Meclizine is combined with 7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline.
AbataceptThe metabolism of Meclizine can be increased when combined with Abatacept.
AbirateroneThe metabolism of Meclizine can be decreased when combined with Abiraterone.
Additional Data Available
  • Extended Description
    Extended Description

    Extended description of the mechanism of action and particular properties of each drug interaction.

    Learn more
  • Severity
    Severity

    A severity rating for each drug interaction, from minor to major.

    Learn more
  • Evidence Level
    Evidence Level

    A rating for the strength of the evidence supporting each drug interaction.

    Learn more
  • Action
    Action

    An effect category for each drug interaction. Know how this interaction affects the subject drug.

    Learn more
Food Interactions
  • Take with food to reduce irritation. Avoid alcohol.

References

Synthesis Reference

U.S. Patent 2,709,169.

General References
  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. 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. 29. (2012). In Rang and Dale's Pharmacology (7th ed., pp. 365-367). Edinburgh: Elsevier/Churchill Livingstone. [ISBN:978-0-7020-3471-8]
  4. Antivert (meclizine hydrochloride) - Drug Summary - PDR.net [Link]
  5. BONAMINE® (Meclizine Hydrochloride Tablets 25 mg, USP) - Product Monograph [Link]
  6. ANTIVERT® - FDA Label [Link]
External Links
Human Metabolome Database
HMDB0014875
KEGG Drug
D08163
KEGG Compound
C07116
PubChem Compound
4034
PubChem Substance
46507782
ChemSpider
3894
BindingDB
81467
ChEBI
6709
ChEMBL
CHEMBL1623
Therapeutic Targets Database
DAP000795
PharmGKB
PA450338
Guide to Pharmacology
GtP Drug Page
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Meclizine
ATC Codes
R06AE55 — Meclozine, combinationsR06AE05 — Meclozine
AHFS Codes
  • 56:22.08 — Antihistamines
MSDS
Download (25 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1CompletedTreatmentHealthy Volunteers1
1RecruitingTreatmentHepatocellular,Carcinoma1
2CompletedTreatmentCessation, Smoking1
3RecruitingTreatmentVertigo, Peripheral1
4RecruitingOtherDrug Reaction1
Not AvailableCompletedPreventionPost-Operative Nausea and Vomiting (PONV)1
Not AvailableCompletedTreatmentBenign Paroxysmal Positional Vertigo (BPPV)1

Pharmacoeconomics

Manufacturers
  • Pfizer inc
Packagers
  • Advanced Pharmaceutical Services Inc.
  • Aidarex Pharmacuticals LLC
  • AJ Bart
  • Apotheca Inc.
  • A-S Medication Solutions LLC
  • Blenheim Pharmacal
  • Bryant Ranch Prepack
  • Cadista Pharmaceuticals Inc.
  • Cardinal Health
  • Dept Health Central Pharmacy
  • Direct Dispensing Inc.
  • Dispensing Solutions
  • Diversified Healthcare Services Inc.
  • Group Health Cooperative
  • H and H Laboratories
  • H.J. Harkins Co. Inc.
  • Heartland Repack Services LLC
  • Innoviant Pharmacy Inc.
  • Kaiser Foundation Hospital
  • Kraft Pharmaceutical Co. Inc.
  • Lake Erie Medical and Surgical Supply
  • Liberty Pharmaceuticals
  • Major Pharmaceuticals
  • Mckesson Corp.
  • Med Tek Pharmaceuticals Inc.
  • Medique Products
  • Medisca Inc.
  • Murfreesboro Pharmaceutical Nursing Supply
  • Nexgen Pharma Inc.
  • Nucare Pharmaceuticals Inc.
  • Palmetto Pharmaceuticals Inc.
  • Par Pharmaceuticals
  • Patheon Inc.
  • Patient First Corp.
  • PCA LLC
  • PD-Rx Pharmaceuticals Inc.
  • Pfizer Inc.
  • Pharmaceutical Utilization Management Program VA Inc.
  • Pharmacia Inc.
  • Pharmedix
  • Pharmpak Inc.
  • Physicians Total Care Inc.
  • Preferred Pharmaceuticals Inc.
  • Prepackage Specialists
  • Prepak Systems Inc.
  • Prescript Pharmaceuticals
  • Qualitest
  • Rebel Distributors Corp.
  • Redpharm Drug
  • Remedy Repack
  • Sandoz
  • Stat Rx Usa
  • Stat Scripts LLC
  • Sunmark
  • Tya Pharmaceuticals
  • UDL Laboratories
  • United Research Laboratories Inc.
  • Vangard Labs Inc.
  • Veratex Corp.
  • Watson Pharmaceuticals
Dosage forms
FormRouteStrength
TabletOral50 mg/1
TabletOral
Tablet, multilayer, extended releaseOral
Tablet, chewableOral
Tablet, orally disintegratingOral25 mg/1
TabletOral12.5 mg/1
TabletOral25 mg/1
Tablet, film coatedOral25 mg/1
Tablet, chewableOral25 mg/251
Film, solubleOral25 mg/1
Tablet, film coatedOral12.5 mg/1
Tablet, chewableOral25 mg/1
Prices
Unit descriptionCostUnit
Meclizine HCl 100 25 mg tablet Box89.97USD box
Antivert 50 mg tablet2.12USD tablet
Antivert 25 mg tablet1.23USD tablet
Meclizine hcl powder1.04USD g
Vertin-32 tablet0.9USD tablet
Antivert 12.5 mg tablet0.82USD tablet
Meclizine HCl 25 mg tablet0.67USD tablet
Meclizine 12.5 mg tablet0.62USD tablet
Sm motion sicknes 25 mg tablet0.5USD tablet
Meclizine HCl 12.5 mg tablet0.43USD tablet
Dramamine less drowsy tablet0.42USD tablet
Bonamine 25 mg Chewable Tablet0.33USD tablet
Dramamine 50 mg tablet0.28USD tablet
Meclizine 25 mg tablet0.07USD tablet
Medi-meclizine 25 mg tablet0.06USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Not Available

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)217-224U.S. Patent 2,709,169.
water solubility0.1g/100mLBONAMINE® Product Monograph - McNeil Consumer Healthcare, division of Johnson & Johnson Inc.
Predicted Properties
PropertyValueSource
Water Solubility0.00103 mg/mLALOGPS
logP5.59ALOGPS
logP6.39ChemAxon
logS-5.6ALOGPS
pKa (Strongest Basic)8.16ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count2ChemAxon
Hydrogen Donor Count0ChemAxon
Polar Surface Area6.48 Å2ChemAxon
Rotatable Bond Count5ChemAxon
Refractivity119.39 m3·mol-1ChemAxon
Polarizability44.87 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability1ChemAxon
Rule of FiveNoChemAxon
Ghose FilterNoChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9318
Blood Brain Barrier+0.9656
Caco-2 permeable+0.6369
P-glycoprotein substrateSubstrate0.7422
P-glycoprotein inhibitor IInhibitor0.8149
P-glycoprotein inhibitor IINon-inhibitor0.8042
Renal organic cation transporterInhibitor0.7859
CYP450 2C9 substrateNon-substrate0.8416
CYP450 2D6 substrateNon-substrate0.5134
CYP450 3A4 substrateNon-substrate0.6059
CYP450 1A2 substrateInhibitor0.806
CYP450 2C9 inhibitorNon-inhibitor0.9698
CYP450 2D6 inhibitorInhibitor0.9521
CYP450 2C19 inhibitorInhibitor0.5209
CYP450 3A4 inhibitorNon-inhibitor0.8896
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.7063
Ames testNon AMES toxic0.8536
CarcinogenicityNon-carcinogens0.9343
BiodegradationNot ready biodegradable1.0
Rat acute toxicity2.3803 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Strong inhibitor0.6113
hERG inhibition (predictor II)Inhibitor0.8104
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
GC-MS Spectrum - EI-BGC-MSsplash10-052r-1920000000-da1d25573308648315fa
Mass Spectrum (Electron Ionization)MSsplash10-0ap0-1910000000-a39cf62803f22b3df281
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-0udi-0090000000-66c42b235873c2a66976
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-0udi-0090000000-02a85fbc5761853f587f
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-0uxr-0590000000-4633d1c1f89a98d9a694
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-0gb9-0940000000-38b1d47fb87eb43db9bd
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-014i-0910000000-0787c462628db9403567
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-014i-0900000000-9b3d5063cf1e4fd0ecda
MS/MS Spectrum - , positiveLC-MS/MSsplash10-0udi-0390000000-10b11855a2539537e5af

Taxonomy

Description
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.
Kingdom
Organic compounds
Super Class
Benzenoids
Class
Benzene and substituted derivatives
Sub Class
Diphenylmethanes
Direct Parent
Diphenylmethanes
Alternative Parents
Phenylmethylamines / Benzylamines / Toluenes / N-alkylpiperazines / Chlorobenzenes / Aralkylamines / Aryl chlorides / Trialkylamines / Azacyclic compounds / Organopnictogen compounds
show 2 more
Substituents
Diphenylmethane / Benzylamine / Phenylmethylamine / Chlorobenzene / Halobenzene / Aralkylamine / N-alkylpiperazine / Toluene / Aryl chloride / Aryl halide
show 14 more
Molecular Framework
Aromatic heteromonocyclic compounds
External Descriptors
diarylmethane (CHEBI:6709)

Targets

Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Antagonist
General Function
Histamine receptor activity
Specific Function
In peripheral tissues, the H1 subclass of histamine receptors mediates the contraction of smooth muscles, increase in capillary permeability due to contraction of terminal venules, and catecholamin...
Gene Name
HRH1
Uniprot ID
P35367
Uniprot Name
Histamine H1 receptor
Molecular Weight
55783.61 Da
References
  1. Oishi R, Shishido S, Yamori M, Saeki K: Comparison of the effects of eleven histamine H1-receptor antagonists on monoamine turnover in the mouse brain. Naunyn Schmiedebergs Arch Pharmacol. 1994 Feb;349(2):140-4. [PubMed:7513381]
  2. Martins MA, Pasquale CP, e Silva PM, Pires AL, Ruffie C, Rihoux JP, Cordeiro RS, Vargaftig BB: Interference of cetirizine with the late eosinophil accumulation induced by either PAF or compound 48/80. Br J Pharmacol. 1992 Jan;105(1):176-80. [PubMed:1350745]
  3. Pasquale CP, e Silva PM, Lima MC, Diaz BL, Rihoux JP, Vargaftig BB, Cordeiro RS, Martins MA: Suppression by cetirizine of pleurisy triggered by antigen in actively sensitized rats. Eur J Pharmacol. 1992 Nov 13;223(1):9-14. [PubMed:1362160]
  4. Taniguchi K, Masuda Y, Takanaka K: Inhibitory effects of histamine H1 receptor blocking drugs on metabolic activations of neutrophils. J Pharmacobiodyn. 1991 Feb;14(2):87-93. [PubMed:1678430]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inverse agonist
General Function
Zinc ion binding
Specific Function
Binds and transactivates the retinoic acid response elements that control expression of the retinoic acid receptor beta 2 and alcohol dehydrogenase 3 genes. Transactivates both the phenobarbital re...
Gene Name
NR1I3
Uniprot ID
Q14994
Uniprot Name
Nuclear receptor subfamily 1 group I member 3
Molecular Weight
39942.145 Da
References
  1. Huang W, Zhang J, Wei P, Schrader WT, Moore DD: Meclizine is an agonist ligand for mouse constitutive androstane receptor (CAR) and an inverse agonist for human CAR. Mol Endocrinol. 2004 Oct;18(10):2402-8. Epub 2004 Jul 22. [PubMed:15272053]

Enzymes

Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Substrate
General Function
Steroid hydroxylase activity
Specific Function
Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic...
Gene Name
CYP2D6
Uniprot ID
P10635
Uniprot Name
Cytochrome P450 2D6
Molecular Weight
55768.94 Da

Carriers

Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Binder
General Function
Toxic substance binding
Specific Function
Serum albumin, the main protein of plasma, has a good binding capacity for water, Ca(2+), Na(+), K(+), fatty acids, hormones, bilirubin and drugs. Its main function is the regulation of the colloid...
Gene Name
ALB
Uniprot ID
P02768
Uniprot Name
Serum albumin
Molecular Weight
69365.94 Da
References
  1. Ariga GG, Naik PN, Nandibewoor ST, Chimatadar SA: Quenching of fluorescence by meclizine, a probe study for structural and conformational changes in human serum albumin. J Biomol Struct Dyn. 2017 Nov;35(14):3161-3175. doi: 10.1080/07391102.2016.1245159. Epub 2016 Nov 10. [PubMed:27767393]

Drug created on June 13, 2005 07:24 / Updated on November 20, 2019 12:20