Identification
- Summary
Meclizine is a histamine H1 antagonist used to treat nausea, vomiting, and dizziness associated with motion sickness.
- Brand Names
- Antivert, Bonine, Diphen, Dramamine, Travel-ease
- Generic Name
- Meclizine
- DrugBank Accession Number
- DB00737
- Background
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.
- Type
- Small Molecule
- Groups
- Approved
- Structure
Structure for Meclizine (DB00737)
- Weight
- Average: 390.948
Monoisotopic: 390.186276581 - Chemical Formula
- C25H27ClN2
- Synonyms
- Meclizine
- Meclozina
- Meclozine
- External IDs
- U.C.B. 5062
- UCB 170
- UCB 5062
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
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Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Prevention of Motion sickness •••••••••••• Symptomatic treatment of Motion sickness •••••••••••• Management of Vertigo •••••••••••• - Contraindications & Blackbox Warnings
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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
Target Actions Organism AHistamine H1 receptor antagonistHumans UNuclear receptor subfamily 1 group I member 3 inverse agonistHumans - 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
Hover over products below to view reaction partners
- 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.
- Adverse Effects
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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
- Pathways
Pathway Category Meclizine H1-Antihistamine Action Drug action - Pharmacogenomic Effects/ADRs Browse all" title="About SNP Mediated Effects/ADRs" id="snp-actions-info" class="drug-info-popup" href="javascript:void(0);">
- Not Available
Interactions
- Drug Interactions Learn More" title="About Drug Interactions" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">
- 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.
Drug Interaction Integrate drug-drug
interactions in your software1,2-Benzodiazepine The risk or severity of CNS depression can be increased when Meclizine is combined with 1,2-Benzodiazepine. 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. Acetaminophen The metabolism of Meclizine can be decreased when combined with Acetaminophen. - Food Interactions
- Avoid alcohol. Alcohol may cause additive CNS depressant effects.
Products
Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.- Product Ingredients
Ingredient UNII CAS InChI Key Meclizine hydrochloride HDP7W44CIO 31884-77-2 BAAVORPTHSKWGJ-UHFFFAOYSA-N - Product Images
- International/Other Brands
- Chiclida / Meclicot / Navicalm / Nevidoxine / Postafen / Sea-Legs
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Antivert Tablet 50 mg/1 Oral Roerig 1997-04-11 2012-03-31 US 
Antivert Tablet, chewable 25 mg/1 Oral Casper Pharma Llc 2020-01-15 Not applicable US Antivert Tablet 12.5 mg/1 Oral Casper Pharma Llc 2020-01-15 Not applicable US Antivert Tablet 25 mg/1 Oral Roerig 1997-04-11 2010-10-31 US Antivert Tablet 50 mg/1 Oral Casper Pharma Llc 2020-01-15 Not applicable US - Generic Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Meclizine Tablet 12.5 mg/1 Oral Direct Rx 2016-04-28 Not applicable US Meclizine Hydrochloride Tablet 25 mg/1 Oral Golden State Medical Supply, Inc. 1982-01-01 2024-10-31 US Meclizine Hydrochloride Tablet 12.5 mg/1 Oral Nucare Pharmaceuticals,inc. 2010-02-12 Not applicable US Meclizine Hydrochloride Tablet 25 mg/1 Oral REMEDYREPACK INC. 2017-04-12 2020-04-06 US Meclizine Hydrochloride Tablet 25 mg/1 Oral Epic Pharma LLC 2012-04-30 Not applicable US - Over the Counter Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Bonamine Tablet, multilayer, extended release 25 mg Oral Mcneil Consumer Healthcare Division Of Johnson & Johnson Inc Not applicable Not applicable Canada 
Bonamine Tab 25mg Chewable Tablet, chewable 25 mg Oral Mcneil Consumer Healthcare Division Of Johnson & Johnson Inc 1954-12-31 2011-08-04 Canada Bonine Tablet, chewable 25 mg/1 Oral WellSpring Pharmaceutical Corporation 2023-02-15 Not applicable US Bonine Tablet, chewable 25 mg/1 Oral Insight Pharmaceuticals 2009-06-08 Not applicable US Bonine Tablet, chewable 25 mg/1 Oral WellSpring Pharmaceutical Corporation 2014-12-15 Not applicable US - Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image Antivert Tab Meclizine hydrochloride (12.5 mg) + Niacin (50 mg) Tablet Oral Pfizer Canada Ulc 1956-12-31 2000-01-24 Canada Diphen Meclizine hydrochloride (25 mg/1) + Acetaminophen (325 mg/1) + Acetaminophen (500 mg/1) + Bacitracin zinc (400 [USP'U]/1g) + Benzalkonium chloride (1.3 mg/1g) + Benzocaine (200 mg/1g) + Bismuth subsalicylate (262 mg/1) + Calcium carbonate (420 mg/1) + Calcium carbonate (27 mg/1) + Dextromethorphan hydrobromide monohydrate (15 mg/1) + Diphenhydramine hydrochloride (25 mg/1) + Guaifenesin (200 mg/1) + Hydrocortisone acetate (10 mg/1g) + Ibuprofen (200 mg/1) + Lidocaine hydrochloride (5 mg/1g) + Loratadine (10 mg/1) + Magnesium oxide (20 mg/1) + Neomycin sulfate (3.5 mg/1g) + Phenylephrine hydrochloride (5 mg/1) + Polymyxin B sulfate (5000 [USP'U]/1g) + Potassium chloride (80 mg/1) Cream; Kit; Liquid; Ointment; Tablet; Tablet, chewable; Tablet, film coated Oral; Topical Remedy Pack LLC 2022-05-10 Not applicable US Novominsyrup Meclizine hydrochloride (25 mg/6mL) + Caffeine (20 mg/6mL) + Pyridoxine hydrochloride (5 mg/6mL) Liquid Oral Lydia Co., Ltd. 2023-01-23 Not applicable US Welly Travel Medicine Kit Meclizine hydrochloride (25 mg/1) + Dimethicone (125 mg/1) + Doxylamine succinate (25 mg/1) + Ibuprofen (200 mg/1) + Loperamide hydrochloride (2 mg/1) Kit Oral Welly Health PBC 2020-04-06 Not applicable US - Unapproved/Other Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image Novominsyrup Meclizine hydrochloride (25 mg/6mL) + Caffeine (20 mg/6mL) + Pyridoxine hydrochloride (5 mg/6mL) Liquid Oral Lydia Co., Ltd. 2023-01-23 Not applicable US
Categories
- ATC Codes
- R06AE55 — Meclozine, combinations
- R06AE — Piperazine derivatives
- R06A — ANTIHISTAMINES FOR SYSTEMIC USE
- R06 — ANTIHISTAMINES FOR SYSTEMIC USE
- R — RESPIRATORY SYSTEM
- Drug Categories
- Anti-Allergic Agents
- Anticholinergic Agents
- Antiemetics
- Antihistamines for Systemic Use
- Antivertigo Preparations
- Autonomic Agents
- Benzene Derivatives
- Benzhydryl Compounds
- Central Nervous System Agents
- Central Nervous System Depressants
- Cholinergic Agents
- Cytochrome P-450 CYP2D6 Substrates
- Cytochrome P-450 Substrates
- Emesis Suppression
- Gastrointestinal Agents
- Histamine Agents
- Histamine Antagonists
- Histamine H1 Antagonists
- Neurotransmitter Agents
- Peripheral Nervous System Agents
- Piperazine Derivatives
- Piperazines
- Chemical TaxonomyProvided by Classyfire
- 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
- 1,4-diazinane / Amine / Aralkylamine / Aromatic heteromonocyclic compound / Aryl chloride / Aryl halide / Azacycle / Benzylamine / Chlorobenzene / Diphenylmethane show 14 more
- Molecular Framework
- Aromatic heteromonocyclic compounds
- External Descriptors
- diarylmethane (CHEBI:6709)
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- 3L5TQ84570
- CAS number
- 569-65-3
- 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
References
- Synthesis Reference
U.S. Patent 2,709,169.
- General References
- 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. [Article]
- 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. [Article]
- 29. (2012). In Rang and Dale's Pharmacology (7th ed., pp. 365-367). Edinburgh: Elsevier/Churchill Livingstone. [ISBN:978-0-7020-3471-8]
- Antivert (meclizine hydrochloride) - Drug Summary - PDR.net [Link]
- BONAMINE® (Meclizine Hydrochloride Tablets 25 mg, USP) - Product Monograph [Link]
- FDA Approved Drug Products: ANTIVERT (meclizine) oral tablets [Link]
- External Links
- Human Metabolome Database
- HMDB0014875
- KEGG Drug
- D08163
- KEGG Compound
- C07116
- PubChem Compound
- 4034
- PubChem Substance
- 46507782
- ChemSpider
- 3894
- BindingDB
- 81467
- 6676
- 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
- MSDS
- Download (25 KB)
Clinical Trials
- Clinical Trials Learn More" title="About Clinical Trials" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">
Phase Status Purpose Conditions Count 4 Unknown Status Other Drug Reaction 1 4 Unknown Status Treatment Meclizine / Sea Sickness 1 3 Completed Treatment Vertigo, Peripheral 1 2 Completed Treatment Smoking, Cessation 1 2 Recruiting Treatment Motion Sickness, Space / Motion Simulation / Parabolic Flight 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
Form Route Strength Solution Intramuscular Syrup Oral Tablet, multilayer, extended release Oral 25 mg Tablet, chewable Oral 25 mg Tablet, chewable Oral 50 mg/1 Gum Oral 25. mg Film, soluble Oral 25 mg/1 Cream; kit; liquid; ointment; tablet; tablet, chewable; tablet, film coated Oral; Topical Solution Oral Tablet Oral 12.5 mg/1 Tablet Oral 25 mg/1 Tablet Oral 50 mg/1 Tablet, film coated Oral 25 mg/1 Tablet, chewable Oral 25 mg/251 Liquid Oral Tablet, film coated Oral 12.5 mg/1 Tablet, chewable Oral 25 mg/1 Tablet Oral Capsule, liquid filled Oral 25 mg Tablet Oral 25 mg Tablet, orally disintegrating Oral 25 mg/1 Kit Oral - Prices
Unit description Cost Unit Meclizine HCl 100 25 mg tablet Box 89.97USD box Antivert 50 mg tablet 2.12USD tablet Antivert 25 mg tablet 1.23USD tablet Meclizine hcl powder 1.04USD g Vertin-32 tablet 0.9USD tablet Antivert 12.5 mg tablet 0.82USD tablet Meclizine HCl 25 mg tablet 0.67USD tablet Meclizine 12.5 mg tablet 0.62USD tablet Sm motion sicknes 25 mg tablet 0.5USD tablet Meclizine HCl 12.5 mg tablet 0.43USD tablet Dramamine less drowsy tablet 0.42USD tablet Bonamine 25 mg Chewable Tablet 0.33USD tablet Dramamine 50 mg tablet 0.28USD tablet Meclizine 25 mg tablet 0.07USD tablet Medi-meclizine 25 mg tablet 0.06USD tablet DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.- Patents
- Not Available
Properties
- State
- Solid
- Experimental Properties
Property Value Source melting point (°C) 217-224 U.S. Patent 2,709,169. water solubility 0.1g/100mL BONAMINE® Product Monograph - McNeil Consumer Healthcare, division of Johnson & Johnson Inc. - Predicted Properties
Property Value Source Water Solubility 0.00103 mg/mL ALOGPS logP 5.59 ALOGPS logP 6.39 Chemaxon logS -5.6 ALOGPS pKa (Strongest Basic) 7.71 Chemaxon Physiological Charge 1 Chemaxon Hydrogen Acceptor Count 2 Chemaxon Hydrogen Donor Count 0 Chemaxon Polar Surface Area 6.48 Å2 Chemaxon Rotatable Bond Count 5 Chemaxon Refractivity 119.39 m3·mol-1 Chemaxon Polarizability 44.87 Å3 Chemaxon Number of Rings 4 Chemaxon Bioavailability 1 Chemaxon Rule of Five No Chemaxon Ghose Filter No Chemaxon Veber's Rule Yes Chemaxon MDDR-like Rule No Chemaxon - Predicted ADMET Features
Property Value Probability Human Intestinal Absorption + 0.9318 Blood Brain Barrier + 0.9656 Caco-2 permeable + 0.6369 P-glycoprotein substrate Substrate 0.7422 P-glycoprotein inhibitor I Inhibitor 0.8149 P-glycoprotein inhibitor II Non-inhibitor 0.8042 Renal organic cation transporter Inhibitor 0.7859 CYP450 2C9 substrate Non-substrate 0.8416 CYP450 2D6 substrate Non-substrate 0.5134 CYP450 3A4 substrate Non-substrate 0.6059 CYP450 1A2 substrate Inhibitor 0.806 CYP450 2C9 inhibitor Non-inhibitor 0.9698 CYP450 2D6 inhibitor Inhibitor 0.9521 CYP450 2C19 inhibitor Inhibitor 0.5209 CYP450 3A4 inhibitor Non-inhibitor 0.8896 CYP450 inhibitory promiscuity High CYP Inhibitory Promiscuity 0.7063 Ames test Non AMES toxic 0.8536 Carcinogenicity Non-carcinogens 0.9343 Biodegradation Not ready biodegradable 1.0 Rat acute toxicity 2.3803 LD50, mol/kg Not applicable hERG inhibition (predictor I) Strong inhibitor 0.6113 hERG inhibition (predictor II) Inhibitor 0.8104
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
- Chromatographic Properties
Collision Cross Sections (CCS)
Adduct CCS Value (Å2) Source type Source [M-H]- 210.5416684 predictedDarkChem Lite v0.1.0 [M-H]- 192.43123 predictedDeepCCS 1.0 (2019) [M+H]+ 210.7092684 predictedDarkChem Lite v0.1.0 [M+H]+ 194.78922 predictedDeepCCS 1.0 (2019) [M+Na]+ 211.3491684 predictedDarkChem Lite v0.1.0 [M+Na]+ 201.3326 predictedDeepCCS 1.0 (2019)
Targets
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- 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
- 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. [Article]
- 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. [Article]
- 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. [Article]
- 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. [Article]
- 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
- 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. [Article]
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
- 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. [Article]
Drug created at June 13, 2005 13:24 / Updated at February 20, 2024 23:55