Hydroxyzine

Identification

Summary

Hydroxyzine is an antihistamine used to treat anxiety and tension associated with psychoneuroses, as well as allergic conditions such as pruritus and chronic urticaria.

Brand Names

Atarax, Vistaril

Generic Name

Hydroxyzine

DrugBank Accession Number

DB00557

Background

Hydroxyzine is a first-generation histamine H₁-receptor antagonist of the dephenylmethane and piperazine classes that exhibits sedative, anxiolytic, and antiemetic properties.^2,12 It was first developed in 1955,¹⁰ and has since remained a relatively common treatment for allergic conditions such as pruritus, urticaria, dermatoses, and histamine-mediated pruritus.¹⁸ The active metabolite of hydroxyzine, cetirizine, is also available as an active ingredient in allergic medications, and is responsible for much of its hydroxyzine's antihistaminic effect.¹³ Hydroxyzine is also used for generalized anxiety disorder, tension caused by psychoneurosis, and other conditions with manifestations of anxiety.¹⁸

Type

Small Molecule

Groups

Approved

Structure

3D

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MOLSDF3D-SDFPDBSMILESInChI

Similar Structures

Structure for Hydroxyzine (DB00557)

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Weight

Average: 374.904
Monoisotopic: 374.176105825

Chemical Formula

C₂₁H₂₇ClN₂O₂

Synonyms

• Hidroxizina
• Hychotine
• Hydroksyzyny
• Hydroxine
• Hydroxizine
• Hydroxizinum
• Hydroxycine
• Hydroxyzin
• Hydroxyzine
• Hydroxyzinum
• Idrossizina

External IDs

• U.C.B-4492

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Pharmacology

Indication

Hydroxyzine is indicated for the symptomatic relief of anxiety and tension associated with psychoneuroses, and as an adjunct in organic disease states in which anxiety is manifested.¹⁸ It is also indicated in the treatment of histamine-mediated pruritus and pruritus due to allergic conditions such as chronic urticaria.¹⁸

Canadian labeling states that hydroxyzine is also indicated in adults and children as a premedication prior to medical procedures, such as dental surgery.¹⁵ It is also used in the control of nausea and vomiting, excluding nausea and vomiting of pregnancy.¹⁵

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Associated Conditions

Indication Type	Indication	Combined Product Details	Approval Level	Age Group	Patient Characteristics	Dose Form
Prevention of	Anxiety		••••••••••••
Adjunct therapy in treatment of	Anxiety		••••••••••••
Symptomatic treatment of	Anxiety		••••••••••••
Symptomatic treatment of	Nausea and vomiting		••••••••••••
Treatment of	Pruritus		••••••••••••

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Pharmacodynamics

Hydroxyzine blocks the activity of histamine to relieve allergic symptoms such as pruritus.¹⁸ Activity at off-targets also allows for its use as a sedative anxiolytic and an antiemetic in certain disease states.¹⁵

Hydroxyzine is relatively fast-acting, with an onset of effect that occurs between 15 and 60 minutes and a duration of action between 4-6 hours.² Hydroxyzine may potentiate the effects of central nervous system (CNS) depressants following general anesthesia - patients maintained on hydroxyzine should receive reduced doses of any CNS depressants required.¹⁸ Hydroxyzine is reported to prolong the QT/QTc interval based on postmarketing reports of rare events of Torsade de Pointes, cardiac arrest, and sudden death, and should be used with caution in patients with an increased baseline risk for QTc prolongation.^15,10

Mechanism of action

The H₁ histamine receptor is responsible for mediating hypersensitivity and allergic reactions. Exposure to an allergen results in degranulation of mast cells and basophils, which then release histamine and other inflammatory mediators. Histamine binds to, and activates, H₁ receptors, which results in the further release of pro-inflammatory cytokines, such as interleukins, from basophils and mast cells. These downstream effects of histamine binding are responsible for a wide variety of allergic symptoms, such as pruritus, rhinorrhea, and watery eyes.¹¹

Hydroxyzine is a potent inverse agonist of histamine H₁-receptors² - inverse agonists are agents that are considered to have a "negative efficacy", so rather than simply blocking activity at a receptor they actively dampen its activity.¹⁴ Inverse agonism at these receptors is responsible for hydroxyzine's efficacy in the treatment of histaminic edema, flare, and pruritus.

Hydroxyzine is not a cortical depressant, so its sedative properties likely occur at the subcortical level of the CNS.¹⁸ These sedative properties allow activity as an anxiolytic. Antiemetic efficacy is likely secondary to activity at off-targets.¹³

Target	Actions	Organism
AHistamine H1 receptor	inverse agonist	Humans
UPotassium voltage-gated channel subfamily H member 2	inhibitor	Humans

Absorption

The absolute bioavailability of hydroxyzine has not been ascertained, as intravenous formulations are unavailable due to a risk of hemolysis.² Hydroxyzine is rapidly absorbed from the gastrointestinal tract upon oral administration,¹⁸ reaching its maximum plasma concentration (T_max) approximately 2 hours following administration.⁹

Volume of distribution

The mean volume of distribution is 16.0 ± 3.0 L/kg. Higher concentrations are found in the skin than in the plasma.²

Protein binding

Hydroxyzine has been shown to bind to human albumin in vitro,⁸ but the extent of protein binding in plasma has not been evaluated.

Metabolism

Hydroxyzine is metabolized in the liver² by CYP3A4 and CYP3A5.¹⁸ While the precise metabolic fate of hydroxyzine is unclear, its main and active metabolite (~45 to 60% of an orally administered dose),¹³ generated by oxidation of its alcohol moiety to a carboxylic acid, is the second-generation antihistamine cetirizine.² Hydroxyzine is likely broken down into several other metabolites, though specific structures and pathways have not been elucidated in humans.⁷

Hover over products below to view reaction partners

• Hydroxyzine
  • Cetirizine

Route of elimination

Approximately 70% of hydroxyzine's active metabolite, cetirizine, is excreted unchanged in the urine.³ The precise extent of renal and fecal excretion in humans has not been determined.¹⁸

Half-life

The half-life of hydroxyzine is reportedly 14-25 hours,² and appears to be, on average, shorter in children (~7.1 hours) than in adults (~20 hours).⁶ Elimination half-life is prolonged in the elderly, averaging approximately 29 hours,³ and is likely to be similarly prolonged in patients with renal or hepatic impairment.¹⁵

Clearance

Clearance of hydroxyzine has been reported to be 31.1 ± 11.1 mL/min/kg in children and 9.8 ± 3.3 mL/min/kg in adults.⁶

Adverse Effects

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Toxicity

The oral LD₅₀ is 840 mg/kg in rats and 400 mg/kg in mice.¹⁶

Overdose from hydroxyzine is most commonly characterized by hypersedation, but may also manifest as convulsions, stupor, nausea, and vomiting.¹⁸ In cases of overdose, consider the induction of vomiting and the use of gastric lavage. Other treatment should involve general symptomatic and supportive care. Hypotension may be controlled by intravenous fluids and pressors, and caffeine and sodium benzoate injection may be used to counteract any observed CNS depressant effects. Hemodialysis is unlikely to provide any benefit in the treatment hydroxyzine overdose.¹⁸

Pathways

Pathway	Category
Hydroxyzine H1-Antihistamine Action	Drug action

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Interactions

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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.

• Approved
• Vet approved
• Nutraceutical
• Illicit
• Withdrawn
• Investigational
• Experimental
• All Drugs

Drug	Interaction
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1,2-Benzodiazepine	Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of 1,2-Benzodiazepine.
Abametapir	The serum concentration of Hydroxyzine can be increased when it is combined with Abametapir.
Abatacept	The metabolism of Hydroxyzine can be increased when combined with Abatacept.
Acalabrutinib	The metabolism of Hydroxyzine can be decreased when combined with Acalabrutinib.
Acebutolol	The risk or severity of QTc prolongation can be increased when Acebutolol is combined with Hydroxyzine.

Food Interactions

• Avoid alcohol. Co-administration with alcohol may potentiate the CNS adverse effects of hydroxyzine.
• Avoid grapefruit products. Co-administration with grapefruit inhibits hydroxyzine metabolism and can result in elevated serum concentrations.

Products

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Product Ingredients

Ingredient	UNII	CAS	InChI Key
Hydroxyzine hydrochloride	76755771U3	2192-20-3	ANOMHKZSQFYSBR-UHFFFAOYSA-N
Hydroxyzine pamoate	M20215MUFR	10246-75-0	ASDOKGIIKXGMNB-UHFFFAOYSA-N

Product Images

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International/Other Brands

Hyzine (Hyrex) / Masmoran (Pfizer) / Rezine / Vistaject-50 / Vistazine

Brand Name Prescription Products

Name	Dosage	Strength	Route	Labeller	Marketing Start	Marketing End	Region	Image
Atarax	Syrup	10 mg/5mL	Oral	Roerig	2006-06-20	2016-06-16
Atarax	Syrup	10 mg / 5 mL	Oral	Searchlight Pharma Inc	1956-12-31	Not applicable
Atarax	Tablet	25 mg/1	Oral	Roerig	2006-06-20	2016-06-16
Atarax	Tablet	100 mg/1	Oral	Roerig	2006-06-20	2016-06-16
Atarax	Tablet	10 mg/1	Oral	Roerig	2006-06-20	2016-06-16

Generic Prescription Products

Name	Dosage	Strength	Route	Labeller	Marketing Start	Marketing End	Region	Image
Hydroxyzine	Injection, solution	25 mg/1mL	Intramuscular	General Injectables & Vaccines	2010-03-01	2017-01-17
Hydroxyzine	Tablet, film coated	10 mg/1	Oral	Ncs Health Care Of Ky, Inc Dba Vangard Labs	2007-03-20	Not applicable
Hydroxyzine	Injection, solution	50 mg/1mL	Intramuscular	General Injectables & Vaccines, Inc	2010-03-01	2023-08-31
Hydroxyzine	Injection, solution	50 mg/1mL	Intramuscular	General Injectables & Vaccines, Inc	2010-03-01	Not applicable
Hydroxyzine	Solution	10 mg/5mL	Oral	Preferred Pharmaceuticals, Inc.	2015-08-21	Not applicable

Over the Counter Products

Name	Dosage	Strength	Route	Labeller	Marketing Start	Marketing End	Region	Image
ซีนิซ	Tablet	10 mg	Oral	บริษัท ไทยนครพัฒนา จำกัด	2007-03-26	Not applicable
ดร็อกซิม	Tablet	25 mg	Oral	บริษัท บุคคโล เทรดดิ้ง จำกัด จำกัด	2008-06-25	Not applicable

Mixture Products

Name	Ingredients	Dosage	Route	Labeller	Marketing Start	Marketing End	Region	Image
ATARAX FILM TABLET, 30 ADET	Hydroxyzine (10 mg) + Hydroxyzine (25 mg)	Tablet	Oral	UCB PHARMA A.Ş.	1997-03-05	Not applicable
ATARAX FILM TABLET, 30 ADET	Hydroxyzine (10 mg) + Hydroxyzine (25 mg)	Tablet	Oral	UCB PHARMA A.Ş.	1997-03-05	Not applicable

Unapproved/Other Products

Name	Ingredients	Dosage	Route	Labeller	Marketing Start	Marketing End	Region	Image
MKH Dose Pack	Hydroxyzine hydrochloride (10 mg/1) + Ketamine hydrochloride (25 mg/1) + Midazolam (3 mg/1)	Troche	Sublingual	Imprimis Njof, Llc	2019-03-04	Not applicable

Categories

ATC Codes

N05BB01 — Hydroxyzine

• N05BB — Diphenylmethane derivatives
• N05B — ANXIOLYTICS
• N05 — PSYCHOLEPTICS
• N — NERVOUS SYSTEM

N05BB51 — Hydroxyzine, combinations

• N05BB — Diphenylmethane derivatives
• N05B — ANXIOLYTICS
• N05 — PSYCHOLEPTICS
• N — NERVOUS SYSTEM

Drug Categories

• Anti-Anxiety Agents
• Antipruritics
• Central Nervous System Depressants
• Cytochrome P-450 CYP2D6 Inhibitors
• Cytochrome P-450 CYP2D6 Inhibitors (strength unknown)
• Cytochrome P-450 CYP3A Substrates
• Cytochrome P-450 CYP3A4 Substrates
• Cytochrome P-450 CYP3A5 Substrates
• Cytochrome P-450 Enzyme Inhibitors
• Cytochrome P-450 Substrates
• Dermatologicals
• Diphenylmethane Derivatives
• Histamine Agents
• Histamine Antagonists
• Histamine H1 Antagonists
• Histamine Receptor Antagonists
• Miscellaneous Anxiolytics Sedatives and Hypnotics
• Nervous System
• Neurotransmitter Agents
• P-glycoprotein substrates
• Piperazines
• Potential QTc-Prolonging Agents
• Psycholeptics
• QTc Prolonging Agents

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

N-alkylpiperazines / Chlorobenzenes / Aralkylamines / Aryl chlorides / Trialkylamines / Dialkyl ethers / Azacyclic compounds / Primary alcohols / Organopnictogen compounds / Organochlorides / Hydrocarbon derivatives

show 1 more

Substituents

1,4-diazinane / Alcohol / Amine / Aralkylamine / Aromatic heteromonocyclic compound / Aryl chloride / Aryl halide / Azacycle / Chlorobenzene / Dialkyl ether / Diphenylmethane / Ether / Halobenzene / Hydrocarbon derivative / N-alkylpiperazine / Organic nitrogen compound / Organic oxygen compound / Organochloride / Organohalogen compound / Organoheterocyclic compound / Organonitrogen compound / Organooxygen compound / Organopnictogen compound / Piperazine / Primary alcohol / Tertiary aliphatic amine / Tertiary amine

show 17 more

Molecular Framework

Aromatic heteromonocyclic compounds

External Descriptors

monochlorobenzenes, N-alkylpiperazine, hydroxyether (CHEBI:5818)

Affected organisms

• Humans and other mammals

Chemical Identifiers

UNII

30S50YM8OG

CAS number

68-88-2

InChI Key

ZQDWXGKKHFNSQK-UHFFFAOYSA-N

InChI

InChI=1S/C21H27ClN2O2/c22-20-8-6-19(7-9-20)21(18-4-2-1-3-5-18)24-12-10-23(11-13-24)14-16-26-17-15-25/h1-9,21,25H,10-17H2

IUPAC Name

2-(2-{4-[(4-chlorophenyl)(phenyl)methyl]piperazin-1-yl}ethoxy)ethan-1-ol

SMILES

OCCOCCN1CCN(CC1)C(C1=CC=CC=C1)C1=CC=C(Cl)C=C1

References

Synthesis Reference

U.S. Patent 2,899,436.

General References

1. Clark BG, Araki M, Brown HW: Hydroxyzine-associated tardive dyskinesia. Ann Neurol. 1982 Apr;11(4):435. [Article]
2. Altamura AC, Moliterno D, Paletta S, Maffini M, Mauri MC, Bareggi S: Understanding the pharmacokinetics of anxiolytic drugs. Expert Opin Drug Metab Toxicol. 2013 Apr;9(4):423-40. doi: 10.1517/17425255.2013.759209. Epub 2013 Jan 21. [Article]
3. Simons KJ, Watson WT, Chen XY, Simons FE: Pharmacokinetic and pharmacodynamic studies of the H1-receptor antagonist hydroxyzine in the elderly. Clin Pharmacol Ther. 1989 Jan;45(1):9-14. doi: 10.1038/clpt.1989.2. [Article]
4. Lee BH, Lee SH, Chu D, Hyun JW, Choe H, Choi BH, Jo SH: Effects of the histamine H(1) receptor antagonist hydroxyzine on hERG K(+) channels and cardiac action potential duration. Acta Pharmacol Sin. 2011 Sep;32(9):1128-37. doi: 10.1038/aps.2011.66. [Article]
5. Crowe A, Wright C: The impact of P-glycoprotein mediated efflux on absorption of 11 sedating and less-sedating antihistamines using Caco-2 monolayers. Xenobiotica. 2012 Jun;42(6):538-49. doi: 10.3109/00498254.2011.643256. Epub 2011 Dec 22. [Article]
6. Paton DM, Webster DR: Clinical pharmacokinetics of H1-receptor antagonists (the antihistamines). Clin Pharmacokinet. 1985 Nov-Dec;10(6):477-97. [Article]
7. Fouda HG, Hobbs DC, Stambaugh JE: Sensitive assay for determination of hydroxyzine in plasma and its human pharmacokinetics. J Pharm Sci. 1979 Nov;68(11):1456-8. doi: 10.1002/jps.2600681134. [Article]
8. Martinez-Gomez MA, Villanueva-Camanas RM, Sagrado S, Medina-Hernandez MJ: Evaluation of enantioselective binding of antihistamines to human serum albumin by ACE. Electrophoresis. 2007 Aug;28(15):2635-43. doi: 10.1002/elps.200600742. [Article]
9. Simons FE, Simons KJ, Frith EM: The pharmacokinetics and antihistaminic of the H1 receptor antagonist hydroxyzine. J Allergy Clin Immunol. 1984 Jan;73(1 Pt 1):69-75. doi: 10.1016/0091-6749(84)90486-x. [Article]
10. Schlit AF, Delaunois A, Colomar A, Claudio B, Cariolato L, Boev R, Valentin JP, Peters C, Sloan VS, Bentz JWG: Risk of QT prolongation and torsade de pointes associated with exposure to hydroxyzine: re-evaluation of an established drug. Pharmacol Res Perspect. 2017 Apr 21;5(3):e00309. doi: 10.1002/prp2.309. eCollection 2017 Jun. [Article]
11. Devillier P, Roche N, Faisy C: Clinical pharmacokinetics and pharmacodynamics of desloratadine, fexofenadine and levocetirizine : a comparative review. Clin Pharmacokinet. 2008;47(4):217-30. [Article]
12. Sawantdesai NS, Kale PP, Savai J: Evaluation of anxiolytic effects of aripiprazole and hydroxyzine as a combination in mice. J Basic Clin Pharm. 2016 Sep;7(4):97-104. doi: 10.4103/0976-0105.189429. [Article]
13. Gengo FM, Dabronzo J, Yurchak A, Love S, Miller JK: The relative antihistaminic and psychomotor effects of hydroxyzine and cetirizine. Clin Pharmacol Ther. 1987 Sep;42(3):265-72. doi: 10.1038/clpt.1987.145. [Article]
14. How drugs act: General principles. (2020). In Rang and Dale's Pharmacology (9th ed.). Edinburgh: Elsevier. [ISBN:9780702080609]
15. Health Canada Product Monograph: Hydroxyzine HCl oral capsules [Link]
16. CaymanChem: Hydroxyzine MSDS [Link]
17. FDA Approved Drug Products: Hydroxyzine HCl oral tablets [Link]
18. FDA Approved Drug Products: Vistaril (hydroxyzine pamoate) [Link]
19. FDA Approved Drug Products: VISTARIL (hydroxyzine pamoate) capsules and suspension [Link]
20. DailyMed: hydroxyzine hydrochloride injection [Link]

External Links

Human Metabolome Database

HMDB0014697

KEGG Drug

D08054

KEGG Compound

C07045

PubChem Compound

3658

PubChem Substance

46508556

ChemSpider

3531

BindingDB

22875

RxNav

5553

ChEBI

5818

ChEMBL

CHEMBL896

Therapeutic Targets Database

DAP000324

PharmGKB

PA449943

RxList

RxList Drug Page

Drugs.com

Drugs.com Drug Page

PDRhealth

PDRhealth Drug Page

Wikipedia

Hydroxyzine

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	Completed	Basic Science	Healthy Subjects (HS)	1
4	Completed	Prevention	Nausea / Pruritus / Vomiting	1
4	Completed	Treatment	Chronic Urticaria	1
4	Completed	Treatment	Dental Caries in Children / Hydroxyzine / Meperidine / Midazolam / Pediatric Dental Sedation	1
4	Completed	Treatment	Nausea / Sleep Disturbance / Smoking, Cessation / Stress (Psychology)	1

Pharmacoeconomics

Manufacturers

• Baxter healthcare corp anesthesia and critical care
• Altana inc
• App pharmaceuticals llc
• Hospira inc
• Luitpold pharmaceuticals inc
• Pharmafair inc
• Smith and nephew solopak div smith and nephew
• Solopak medical products inc
• Solopak laboratories inc
• Watson laboratories inc
• Wyeth ayerst laboratories
• Organon usa inc
• Pfizer laboratories div pfizer inc
• Roerig div pfizer inc
• Actavis mid atlantic llc
• Alpharma us pharmaceuticals division
• Hi tech pharmacal co inc
• Kv pharmaceutical co
• Vintage pharmaceuticals inc
• Wockhardt eu operations (swiss) ag
• Pfizer inc
• Able laboratories inc
• Actavis totowa llc
• Amneal pharmaceutical
• Halsey drug co inc
• Heritage pharmaceuticals inc
• Hetero drugs ltd unit iii
• Invagen pharmaceuticals inc
• Ivax pharmaceuticals inc
• Kvk tech inc
• Mutual pharmaceutical co inc
• Mylan pharmaceuticals inc
• Northstar healthcare holdings ltd
• Pliva inc
• Purepac pharmaceutical co
• Quantum pharmics ltd
• Sandoz inc
• Sun pharmaceutical industries inc
• Superpharm corp
• Usl pharma inc
• Vintage pharmaceuticals llc
• Barr laboratories inc
• Duramed pharmaceuticals inc sub barr laboratories inc
• Ivax pharmaceuticals inc sub teva pharmaceuticals usa
• Par pharmaceutical inc
• Vangard laboratories inc div midway medical co
• Teva pharmaceuticals usa inc

Packagers

• Advanced Pharmaceutical Services Inc.
• American Regent
• Amerisource Health Services Corp.
• Anda Inc.
• Apotheca Inc.
• APP Pharmaceuticals
• A-S Medication Solutions LLC
• Atlantic Biologicals Corporation
• Barr Pharmaceuticals
• Blenheim Pharmacal
• Bryant Ranch Prepack
• C.O. Truxton Inc.
• Caraco Pharmaceutical Labs
• Cardinal Health
• Caremark LLC
• Carlisle Laboratories Inc.
• Central Texas Community Health Centers
• Clint Pharmaceutical Inc.
• Co Med Pharmaceuticals Inc.
• Comprehensive Consultant Services Inc.
• Corepharma LLC
• Darby Dental Supply Co. Inc.
• Dept Health Central Pharmacy
• Direct Dispensing Inc.
• Direct Pharmaceuticals Inc.
• Dispensing Solutions
• Diversified Healthcare Services Inc.
• Eon Labs
• Glenmark Generics Ltd.
• Goldline Laboratories Inc.
• H and H Laboratories
• H.J. Harkins Co. Inc.
• Harris Pharmaceutical Inc.
• Heartland Repack Services LLC
• Heritage Pharmaceuticals
• Hi Tech Pharmacal Co. Inc.
• Innoviant Pharmacy Inc.
• InvaGen Pharmaceuticals Inc.
• Ivax Pharmaceuticals
• Kaiser Foundation Hospital
• Keltman Pharmaceuticals Inc.
• KVK-Tech Inc.
• Lake Erie Medical and Surgical Supply
• Liberty Pharmaceuticals
• Luitpold Pharmaceuticals Inc.
• Major Pharmaceuticals
• Martica Enterprises Inc.
• Martin Surgical Supply
• Medisca Inc.
• Medvantx Inc.
• Merit Pharmaceuticals
• Merrell Pharmaceuticals Inc.
• Monument Pharmaceutical Co. Inc.
• Murfreesboro Pharmaceutical Nursing Supply
• Mutual Pharmaceutical Co.
• Mylan
• National Pharmaceuticals
• Nightingale Medical Of Indiana LLC
• Northstar Rx LLC
• Nucare Pharmaceuticals Inc.
• Palmetto Pharmaceuticals Inc.
• Patheon Inc.
• Patient First Corp.
• PCA LLC
• PD-Rx Pharmaceuticals Inc.
• Pfizer Inc.
• Pharmaceutical Utilization Management Program VA Inc.
• Pharmacy Service Center
• Pharmedix
• Physicians Total Care Inc.
• Piramal Healthcare
• Pliva Inc.
• Preferred Pharmaceuticals Inc.
• Prepackage Specialists
• Prepak Systems Inc.
• Prescript Pharmaceuticals
• Prescription Dispensing Service Inc.
• Qualitest
• Rebel Distributors Corp.
• Redpharm Drug
• Remedy Repack
• Resource Optimization and Innovation LLC
• Sandhills Packaging Inc.
• Southwood Pharmaceuticals
• St Mary's Medical Park Pharmacy
• Stat Rx Usa
• Sun Pharmaceutical Industries Ltd.
• Talbert Medical Management Corp.
• UDL Laboratories
• United Research Laboratories Inc.
• Vangard Labs Inc.
• Veratex Corp.
• Vintage Pharmaceuticals Inc.
• Watson Pharmaceuticals
• Wockhardt Ltd.

Dosage Forms

Form	Route	Strength
Capsule, liquid filled	Oral	25 mg
Tablet, film coated	Oral	50 mg
Tablet	Oral	10.00 mg
Injection, solution	Intramuscular
Syrup	Oral	10 mg/5mL
Tablet	Oral	10 mg/1
Tablet	Oral	100 mg/1
Tablet	Oral	25 mg/1
Tablet	Oral	50 mg/1
Syrup	Oral	200 ml
Tablet	Oral
Solution	Intramuscular	50 mg / mL
Syrup	Oral
Tablet, film coated	Oral
Tablet, film coated	Oral	30 mg
Syrup	Oral	300 mg
Tablet	Oral	500 mg
Tablet, chewable	Buccal	25 mg
Tablet, coated	Oral	50 mg
Solution	Intramuscular	100 mg
Solution	Oral	10 mg
Solution	Oral	250 mg
Syrup	Oral	250 mg
Solution	Oral	0.25 g
Tablet	Oral	2500000 mg
Syrup	Oral	0.25 g
Capsule	Oral	10 mg
Capsule	Oral	25 mg
Capsule	Oral	50 mg
Injection, solution	Intramuscular	50 mg/1mL
Solution	Oral	10 mg/5mL
Tablet, film coated	Oral	10 mg/1
Tablet, film coated	Oral	25 mg/1
Tablet, film coated	Oral	50 mg/1
Liquid	Intramuscular	50 mg / mL
Tablet, film coated	Oral	10.000 mg
Tablet, film coated	Oral	25.000 mg
Capsule	Oral	100 mg/1
Capsule	Oral	25 mg/1
Capsule	Oral	50 mg/1
Tablet, film coated	Oral	10 mg
Troche	Sublingual
Capsule	Oral	10 mg / cap
Capsule	Oral	25 mg / cap
Injection, solution	Intramuscular	25 mg/1mL
Syrup	Oral	10 mg / 5 mL
Tablet	Oral	10.000 mg
Solution / drops	Oral	10 ml
Solution / drops	Oral	20 ml
Solution	Intramuscular	50 mg/1mL
Suspension	Oral	25 mg/5mL
Tablet, coated	Oral	25 mg
Tablet	Oral	25 mg
Tablet	Oral	10 mg
Tablet, film coated	Oral	25 mg
Solution		10 mg/5ml
Tablet, coated	Oral	10 mg

Prices

Unit description	Cost	Unit
Hydroxyzine Hcl 50 mg/ml	4.42USD	ml
Hydroxyzine 50 mg/ml vial	3.96USD	ml
Hydroxyzine 25 mg/ml vial	3.6USD	ml
Hydroxyzine hcl powder	2.75USD	g
Hydroxyzine pamoate powder	2.14USD	g
Vistaril 50 mg capsule	2.03USD	capsule
HydrOXYzine HCl 50 mg/ml vial	1.78USD	vial
Vistaril 25 mg capsule	1.71USD	capsule
Vistaril 100 mg capsule	1.7USD	capsule
Hydroxyzine hcl 50 mg tablet	1.19USD	tablet
Hydroxyzine hcl 10 mg tablet	0.72USD	tablet
Hydroxyzine hcl 25 mg tablet	0.7USD	tablet
HydrOXYzine Pamoate 100 mg capsule	0.67USD	capsule
Hydroxyzine pam 50 mg capsule	0.64USD	capsule
Hydroxyzine pam 100 mg capsule	0.63USD	capsule
Hydroxyzine pam 25 mg capsule	0.46USD	capsule
Vistaril 25 mg/5ml Suspension	0.45USD	ml
HydrOXYzine Pamoate 25 mg capsule	0.3USD	capsule
HydrOXYzine Pamoate 50 mg capsule	0.23USD	capsule
Apo-Hydroxyzine 50 mg Capsule	0.22USD	capsule
Novo-Hydroxyzin 50 mg Capsule	0.22USD	capsule
Apo-Hydroxyzine 25 mg Capsule	0.15USD	capsule
Novo-Hydroxyzin 25 mg Capsule	0.15USD	capsule
HydrOXYzine HCl 10 mg/5ml Syrup	0.13USD	ml
Apo-Hydroxyzine 10 mg Capsule	0.12USD	capsule
Novo-Hydroxyzin 10 mg Capsule	0.12USD	capsule
Atarax 2 mg/ml Syrup	0.06USD	ml
Pms-Hydroxyzine 2 mg/ml Syrup	0.04USD	ml

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Patents

Not Available

Properties

State

Solid

Experimental Properties

Property	Value	Source
melting point (°C)	200C	Canadian Label

Predicted Properties

Property	Value	Source
Water Solubility	0.0914 mg/mL	ALOGPS
logP	3.43	ALOGPS
logP	3.41	Chemaxon
logS	-3.6	ALOGPS
pKa (Strongest Acidic)	15.12	Chemaxon
pKa (Strongest Basic)	7.45	Chemaxon
Physiological Charge	1	Chemaxon
Hydrogen Acceptor Count	4	Chemaxon
Hydrogen Donor Count	1	Chemaxon
Polar Surface Area	35.94 Å2	Chemaxon
Rotatable Bond Count	8	Chemaxon
Refractivity	107.07 m3·mol-1	Chemaxon
Polarizability	41.99 Å3	Chemaxon
Number of Rings	3	Chemaxon
Bioavailability	1	Chemaxon
Rule of Five	Yes	Chemaxon
Ghose Filter	Yes	Chemaxon
Veber's Rule	Yes	Chemaxon
MDDR-like Rule	Yes	Chemaxon

Predicted ADMET Features

Property	Value	Probability
Human Intestinal Absorption	+	0.8623
Blood Brain Barrier	+	0.9516
Caco-2 permeable	-	0.5565
P-glycoprotein substrate	Substrate	0.7447
P-glycoprotein inhibitor I	Inhibitor	0.8563
P-glycoprotein inhibitor II	Inhibitor	0.6394
Renal organic cation transporter	Inhibitor	0.592
CYP450 2C9 substrate	Non-substrate	0.8352
CYP450 2D6 substrate	Non-substrate	0.9116
CYP450 3A4 substrate	Non-substrate	0.7193
CYP450 1A2 substrate	Non-inhibitor	0.9045
CYP450 2C9 inhibitor	Non-inhibitor	0.9111
CYP450 2D6 inhibitor	Inhibitor	0.8535
CYP450 2C19 inhibitor	Non-inhibitor	0.9026
CYP450 3A4 inhibitor	Non-inhibitor	0.9623
CYP450 inhibitory promiscuity	Low CYP Inhibitory Promiscuity	0.7615
Ames test	Non AMES toxic	0.7558
Carcinogenicity	Non-carcinogens	0.9102
Biodegradation	Not ready biodegradable	1.0
Rat acute toxicity	2.6612 LD50, mol/kg	Not applicable
hERG inhibition (predictor I)	Weak inhibitor	0.5929
hERG inhibition (predictor II)	Inhibitor	0.7898

ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)

Not Available

Spectra

Spectrum	Spectrum Type	Splash Key
Predicted GC-MS Spectrum - GC-MS	Predicted GC-MS	splash10-0udj-4291000000-5750700bc5e75e581102
GC-MS Spectrum - EI-B	GC-MS	splash10-0udi-6491000000-95c46c16c2b29900f4d9
Mass Spectrum (Electron Ionization)	MS	splash10-0uxr-4591000000-d2e3424c44feae8a5d9c
MS/MS Spectrum - , positive	LC-MS/MS	splash10-0udi-0593000000-f20d2328497a3a80239b
Predicted MS/MS Spectrum - 10V, Positive (Annotated)	Predicted LC-MS/MS	splash10-004i-0009000000-ea8e9386af034db2f970
Predicted MS/MS Spectrum - 10V, Negative (Annotated)	Predicted LC-MS/MS	splash10-00di-4009000000-82a93759c53ebe3a9537
Predicted MS/MS Spectrum - 20V, Positive (Annotated)	Predicted LC-MS/MS	splash10-0zfr-0096000000-4e9aa5e0b6000400dc11
Predicted MS/MS Spectrum - 20V, Negative (Annotated)	Predicted LC-MS/MS	splash10-03kc-9028000000-ad990344a3859f84c00e
Predicted MS/MS Spectrum - 40V, Positive (Annotated)	Predicted LC-MS/MS	splash10-0ufr-5692000000-b6a27399e087ae28b29c
Predicted MS/MS Spectrum - 40V, Negative (Annotated)	Predicted LC-MS/MS	splash10-001i-9181000000-2983d1840355019c9e57
Predicted 1H NMR Spectrum	1D NMR	Not Applicable
Predicted 13C NMR Spectrum	1D NMR	Not Applicable

Chromatographic Properties

Collision Cross Sections (CCS)

Adduct	CCS Value (Å2)	Source type	Source
[M-H]-	201.4104609	predicted	DarkChem Lite v0.1.0
[M-H]-	185.55614	predicted	DeepCCS 1.0 (2019)
[M+H]+	201.0609609	predicted	DarkChem Lite v0.1.0
[M+H]+	187.91415	predicted	DeepCCS 1.0 (2019)
[M+Na]+	201.2974609	predicted	DarkChem Lite v0.1.0
[M+Na]+	194.821	predicted	DeepCCS 1.0 (2019)

Targets

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Binding Properties

×

Property	Measurement	pH	Temperature (°C)	References
Ki (nM)	2	N/A	N/A	A27840
Ki (nM)	1	N/A	N/A	A27840

Details

Binding Properties1. Histamine H1 receptor

Kind

Protein

Organism

Humans

Pharmacological action

Yes

Actions

Inverse agonist

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. Spahr L, Coeytaux A, Giostra E, Hadengue A, Annoni JM: Histamine H1 blocker hydroxyzine improves sleep in patients with cirrhosis and minimal hepatic encephalopathy: a randomized controlled pilot trial. Am J Gastroenterol. 2007 Apr;102(4):744-53. Epub 2007 Jan 11. [Article]
2. Altamura AC, Moliterno D, Paletta S, Maffini M, Mauri MC, Bareggi S: Understanding the pharmacokinetics of anxiolytic drugs. Expert Opin Drug Metab Toxicol. 2013 Apr;9(4):423-40. doi: 10.1517/17425255.2013.759209. Epub 2013 Jan 21. [Article]

Details2. Potassium voltage-gated channel subfamily H member 2

Kind

Protein

Organism

Humans

Pharmacological action

Unknown

Actions

Inhibitor

General Function

Voltage-gated potassium channel activity involved in ventricular cardiac muscle cell action potential repolarization

Specific Function

Pore-forming (alpha) subunit of voltage-gated inwardly rectifying potassium channel. Channel properties are modulated by cAMP and subunit assembly. Mediates the rapidly activating component of the ...

Gene Name

KCNH2

Uniprot ID

Q12809

Uniprot Name

Potassium voltage-gated channel subfamily H member 2

Molecular Weight

126653.52 Da

References

1. Lee BH, Lee SH, Chu D, Hyun JW, Choe H, Choi BH, Jo SH: Effects of the histamine H(1) receptor antagonist hydroxyzine on hERG K(+) channels and cardiac action potential duration. Acta Pharmacol Sin. 2011 Sep;32(9):1128-37. doi: 10.1038/aps.2011.66. [Article]
2. Sakaguchi T, Itoh H, Ding WG, Tsuji K, Nagaoka I, Oka Y, Ashihara T, Ito M, Yumoto Y, Zenda N, Higashi Y, Takeyama Y, Matsuura H, Horie M: Hydroxyzine, a first generation H(1)-receptor antagonist, inhibits human ether-a-go-go-related gene (HERG) current and causes syncope in a patient with the HERG mutation. J Pharmacol Sci. 2008 Dec;108(4):462-71. Epub 2008 Dec 5. [Article]

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Drug created at June 13, 2005 13:24 / Updated at February 20, 2024 23:55