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Hydroxyzine (/haɪˈdrɒksᵻziːn/) is a first-generation antihistamine of the diphenylmethane and piperazine class. It was first synthesized by Union Chimique Belge in 1956 and was marketed by Pfizer in the United States later the same year,^[2] and is still in widespread use today.

Due to its antagonistic effects on several receptor systems in the brain, hydroxyzine has strong anxiolytic and mild antiobsessive as well as antipsychotic properties.^[3] Today it is used primarily for the symptomatic relief of anxiety and tension associated with psychoneurosis and as an adjunct in organic disease states in which anxiety is manifested. Because of its antihistamine effects it can also be used for the treatment of severe cases of itching, hyperalgesia and motion sickness-induced nausea; it has also been used in some cases to relieve the effects of opioid withdrawal.^[4]^[5] Even though it is an effective sedative, hypnotic, and anxiolytic, it shares virtually none of the abuse, dependence, addiction, and toxicity potential of other drugs used for the same range of therapeutic reasons. Hydroxyzine has also been used to potentiate the analgesia of opioids and to alleviate some of their side effects, such as itching, nausea, and vomiting.

Hydroxyzine preparations require a doctor's prescription. The drug is available in two formulations, the pamoate and the dihydrochloride or hydrochloride salts. Vistaril, Equipose, Masmoran, and Paxistil are preparations of the pamoate salt, while Atarax, Alamon, Aterax, Durrax, Tran-Q, Orgatrax, Quiess, and Tranquizine are of the hydrochloride salt.

Other drugs related to hydroxyzine are cyclizine, buclizine, and meclizine, and they share all or most of the benefits, indications, contraindications, cautions, and side effects of hydroxyzine. The second-generation antihistamine cetirizine is in fact one of the metabolites of hydroxyzine produced in the human body. Unlike hydroxyzine, cetirizine is not reported to appreciably cross the blood-brain barrier, but it has been reported to be associated with dystonic reactions as well as sedation. Therefore, it has a narrower spectrum of effects, making it an effective antihistamine but removing some or all of the anxiolytic and other psychoactive properties, but it may cause dystonic reactions and drowsiness in some patients.

Chemistry

Hydroxyzine is synthesized by the alkylation of 1-(4-chlorobenzohydril)piperazine with 2-(2-hydroxyethoxy)ethylchloride:^[6]

Pharmacology

Hydroxyzine's predominant mechanism of action is as a potent H₁ receptor inverse agonist (K_i = 2 nM).^[7]^[8]^[9]^[10] Unlike many other first-generation antihistamines, it has very low affinity for the mACh receptors (K_i = >10,000 nM),^[8]^[9]^[10]^[11]^[12] and in accordance, has a low propensity for producing anticholinergic side effects.^[10]^[13]^[14] In addition to its antihistamine activity, hydroxyzine has also been shown to act as a 5-HT_2A (K_i = ~50 nM), D₂ (K_i = 378 nM), and α₁-adrenergic (K_i = ~300 nM) receptor antagonist.^[8]^[9]^[11] The antiserotonergic effects of hydroxyzine likely underlie its usefulness as an anxiolytic,^[15] as other antihistamines without such properties have not been found to be effective in the treatment of anxiety.^[16]

Prescription and use

Hydroxyzine is classified as an antihistamine and anxiolytic and is also used as a tranquilizer; especially common in dentistry and less so in medicine, where for many years it has been preferred in combination with opioids due to its ability to counteract the side effects of opioid pain medications, namely itchiness and nausea, and the fact that its sedative properties complement the pain relieving effects of opioids.^{[citation needed]}^{[citation needed]}

Hydroxyzine is prescribed when the onset of an organic disease state manifests through anxiety, as generalized anxiety disorder, or in other more serious cases as psychoneurosis, and is therefore prescribed as a means of regulating normal function. Hydroxyzine has shown to be as effective as the benzodiazepine drug bromazepam in the treatment of generalised anxiety disorder.^[17] However, a systematic review concluded that it can not be recommended for generalized anxiety disorder, although compared with other anxiolytic agents (benzodiazepines and buspirone), hydroxyzine was equivalent in efficacy, acceptability and tolerability.^[18]

Hydroxyzine can also be used for the treatment of allergic conditions, such as chronic urticaria, atopic or contact dermatoses, and histamine-mediated pruritus. These have also been confirmed in both recent and past studies to have no adverse effects on the liver, blood, nervous system or urinary tract.^[19]^{[citation needed]}

Use of hydroxyzine for premedication as a sedative has no effects on tropane alkaloids, such as atropine, but may, following general anesthesia, potentiate meperidine and barbiturates, and use in pre-anesthetic adjunctive therapy should be modified depending upon the state of the individual.^[19]^{[citation needed]}

In other cases, the usage of hydroxyzine is as a form of non-barbiturate tranquilizer^[20] used in the pre-operative sedation and treatment of neurological disorders, such as psychoneurosis and other forms of anxiety or tension states.^[20]

For dentistry and obstetrics as well as other surgeries and procedures and acute pain situations like accidents, hydroxyzine is useful as a first line anxiolytic and opioid adjunct because it lacks both antagonism and synergy with benzodiazepines and scopolamine, allowing either of these agents to be used simultaneously or later in the procedure if need be.^{[citation needed]}

Animal behavioral research

Hydroxyzine reduced escape failures in a learned helplessness paradigm in rats.^[21]

Clinical description

Metabolism and pharmacokinetics

Hydroxyzine can be administered orally or via intramuscular injection. When given orally, hydroxyzine is rapidly absorbed from the gastro-intestinal tract. The effect of hydroxyzine is notable in 30 minutes.

Pharmacokinetically, hydroxyzine is rapidly absorbed and distributed in oral and intramuscular administration, and is metabolized in the liver; the main metabolite (45%), cetirizine, is formed through oxidation of the alcohol moiety to a carboxylic acid by alcohol dehydrogenase, and overall effects are observed within one hour of administration. It has a half-life observed on average of around 3 hours in adults, with higher concentrations found in the skin than in the plasma. Cetirizine, although less sedating, is non-dialyzable and possesses similar anti-histaminergic properties. The other metabolites identified include a N-dealkylated metabolite, and an O-dealkylated 1/16 metabolite with a plasma half-life of 59 hours. These pathways are mediated principally by CYP3A4 and CYP3A5.^[22] "In animals, hydroxyzine and its metabolites are excreted in feces via biliary elimination."^[23]

Administration in geriatrics differs from the administration of hydroxyzine in younger patients; according to the FDA, there have not been significant studies made (2004), which include population groups over 65, which provide a distinction between elderly aged patients and other younger groups. Hydroxyzine should be administered carefully in the elderly with consideration given to possible reduced elimination.^[24]

Similarly, the use of sedating drugs alongside hydroxyzine can cause over-sedation and confusion if administered in large amounts—any form of treatment alongside sedatives should be done under supervision of a doctor.^[20]^[24]

Contraindications

The administration of hydroxyzine in large amounts by ingestion or intramuscular administration during the onset of pregnancy can cause fetal abnormalities—when administered to pregnant rats, mice and rabbits, hydroxyzine caused abnormalities such as hypogonadism with doses significantly above that of the human therapeutic range.^[25] In humans, a significant dose has not yet been established in studies, and by default, the FDA has introduced contraindication guidelines in regard to hydroxyzine.^[25] Similarly the use in those at risk from or showing previous signs of hypersensitivity is also contraindicated.^[25] Hydroxyzine is contraindicated for intravenous (IV) injection, as it has shown to cause hemolysis.

Other contraindications include the administration of hydroxyzine alongside depressants and other compounds which affect the central nervous system.^[25] and if absolutely necessary, it should only be administered concomitantly in small doses.^[25] If administered in small doses with other substances, such as mentioned, then patients should refrain from using dangerous machinery, motor vehicles or any other practice requiring absolute concentration, in accordance with safety law.^[25]

Studies have also been conducted which show that long-term prescription of hydroxyzine can lead to tardive dyskinesia after years of use, but effects related to dyskinesia have also anecdotally been reported after periods of 7.5 months,^[26] such as continual head rolling, lip licking and other forms of athetoid movement. In certain cases, elderly patients' previous interactions with phenothiazine derivatives or pre-existing neuroleptic treatment may have had some contribution towards dyskinesia at the administration of hydroxyzine due to hypersensitivity caused due to the prolonged treatment,^[26] and therefore some contraindication is given to the short-term administration of hydroxyzine to those with previous phenothiazine use.^[26]

Adverse reactions

Several reactions have been noted in manufacturer guidelines — deep sleep, incoordination, sedation, calmness, and dizziness have been reported in children and adults, as well as others such as hypotension, tinnitus, and headaches.^[27] Gastro-intestinal effects have also been observed, as well as less serious effects such as dryness of the mouth and constipation caused by the mild antimuscarinic properties of hydroxyzine.^[27]

Central nervous system problems such as hallucinations or confusion have been observed in rare cases, attributed mostly to overdosage.^[24]^[27] Such properties have been attributed to hydroxyzine in several cases, particularly in patients treated for neuropsychological disorders, as well as in cases where overdoses have been observed. While there are reports of the "hallucinogenic" or "hypnotic" properties of hydroxyzine, several clinical data trials have not reported such side effects from the sole consumption of hydroxyzine, but rather, have described its overall calming effect described through the stimulation of areas within the formatio reticularis. The hallucinogenic or hypnotic properties have been described as being an additional effect from overall central nervous system suppression by other CNS agents, such as lithium or ethanol.^[28]

The effect of hydroxyzine has also been tested on the ability of humans in the registration and storage of memory, and was used in comparison with relatively safe drugs, such as lorazepam, to illustrate the effects of benzodiazepines, which are thought to have adverse effects on the capacity of memory storage. Hydroxyzine was found to have no adverse effects on memory in relation to lorazepam, which caused several deficiencies in the capacity of memory storage.^[29]

In a comparative study with lorazepam on memory effects, patients who had taken hydroxyzine experienced sedative effects like drowsiness, but recalled that they felt capable, attentive and able to continue with a memory test under these conditions.^[30] Conversely, those under the effects of lorazepam felt unable to continue due to the fact they felt out of control with its effects; 8 out of 10 patients describing tendencies of problems with balance and control of simple motor functions.^[30]

Somnolence with or without vivid dreams or nightmares may occur in users with antihistamine sensitivities in combination with other CNS depressants. Hydroxyzine exhibits anxiolytic and sedative properties in many psychiatric patients. Other studies have suggested that hydroxyzine acts as an acute hypnotic, reducing sleep onset latency and increasing sleep duration — also showing that some drowsiness did occur. This was observed more in female patients, who also had greater hypnotic response.^[31]

Because of potential for more severe side effects, this drug is on the list to avoid in the elderly.^[32]

In popular culture

In her confessional memoir Prozac Nation, Elizabeth Wurtzel describes how she made a prepubescent attempt at suicide by taking an overdose of Atarax.^[33]
A scene from the film Love and Other Drugs displays an advertisement for Vistaril on the mega screen during the employee recruiter convention scene.
Hydroxyzine is the only word in the English language to have, in order, x, y, and z.^[34]

References

^ Simons FE, Simons KJ, Frith EM (January 1984). "The pharmacokinetics and antihistaminic of the H1 receptor antagonist hydroxyzine". The Journal of Allergy and Clinical Immunology. 73 (1 Pt 1): 69–75. doi:10.1016/0091-6749(84)90486-x. PMID 6141198.
^ Shorter, Edward (2009). Before Prozac: the troubled history of mood disorders in psychiatry. Oxford [Oxfordshire]: Oxford University Press. ISBN 0-19-536874-6.
^ SCHRAM, WS (March 1959). "Use of hydroxyzine in psychosis.". Diseases of the Nervous System. 20 (3): 126–9. PMID 13639831.
^ FDA DrugInfo: http://dailymed.nlm.nih.gov/dailymed/archives/fdaDrugInfo.cfm?archiveid=51459
^ "Hydroxyzine Facts and Comparisons at Drugs.com".
^ H. Morren, U.S. Patent 2,899,436 (1959); H. Morren, DE 1049383 (1954); H. Morren, DE 1061786 (1954); H. Morren, DE 1068262 (1954); H. Morren, DE 1072624 (1954); H. Morren, DE 1075116 (1954).
^ Gillard M, Van Der Perren C, Moguilevsky N, Massingham R, Chatelain P (February 2002). "Binding characteristics of cetirizine and levocetirizine to human H(1) histamine receptors: contribution of Lys(191) and Thr(194)". Molecular Pharmacology. 61 (2): 391–9. doi:10.1124/mol.61.2.391. PMID 11809864.
^ ^a ^b ^c Snowman AM, Snyder SH (December 1990). "Cetirizine: actions on neurotransmitter receptors". The Journal of Allergy and Clinical Immunology. 86 (6 Pt 2): 1025–8. doi:10.1016/S0091-6749(05)80248-9. PMID 1979798.
^ ^a ^b ^c Kubo N, Shirakawa O, Kuno T, Tanaka C (March 1987). "Antimuscarinic effects of antihistamines: quantitative evaluation by receptor-binding assay". Japanese Journal of Pharmacology. 43 (3): 277–82. doi:10.1254/jjp.43.277. PMID 2884340.
^ ^a ^b ^c WHITE RP, BOYAJY LD (September 1960). "Neuropharmacological comparison of atropine, scopolamine, banactyzine, diphenhydramine and hydroxyzine". Archives Internationales de Pharmacodynamie et de Thérapie. 127: 260–73. PMID 13784865.
^ ^a ^b Haraguchi K, Ito K, Kotaki H, Sawada Y, Iga T (June 1997). "Prediction of drug-induced catalepsy based on dopamine D1, D2, and muscarinic acetylcholine receptor occupancies". Drug Metabolism and Disposition: the Biological Fate of Chemicals. 25 (6): 675–84. PMID 9193868.
^ Orzechowski RF, Currie DS, Valancius CA (January 2005). "Comparative anticholinergic activities of 10 histamine H1 receptor antagonists in two functional models". European Journal of Pharmacology. 506 (3): 257–64. doi:10.1016/j.ejphar.2004.11.006. PMID 15627436.
^ Berger, F. M. (1957). "THE CHEMISTRY AND MODE OF ACTION OF TRANQUILIZING DRUGS". Annals of the New York Academy of Sciences. 67 (10): 685–700. doi:10.1111/j.1749-6632.1957.tb46006.x. ISSN 0077-8923.
^ K. D. Tripathi (2013). Essentials of Medical Pharmacology. JP Medical Ltd. p. 165. ISBN 978-93-5025-937-5.
^ Barbara Olasov Rothbaum; Stein, Dan J.; Hollander, Eric (2009). Textbook of Anxiety Disorders. American Psychiatric Publishing, Inc. ISBN 1-58562-254-0.
^ Lamberty Y, Gower AJ (September 2004). "Hydroxyzine prevents isolation-induced vocalization in guinea pig pups: comparison with chlorpheniramine and immepip". Pharmacology, Biochemistry, and Behavior. 79 (1): 119–24. doi:10.1016/j.pbb.2004.06.015. PMID 15388291.
^ Llorca PM, Spadone C, Sol O, et al. (November 2002). "Efficacy and safety of hydroxyzine in the treatment of generalized anxiety disorder: a 3-month double-blind study" (PDF). J Clin Psychiatry. 63 (11): 1020–7. doi:10.4088/JCP.v63n1112. PMID 12444816.
^ Giuseppe Guaiana1, Corrado Barbui, Andrea Cipriani (8 December 2010). "Hydroxyzine for generalised anxiety disorder". The Cochrane Library. Cochrane Depression, Anxiety and Neurosis Group. doi:10.1002/14651858.CD006815.pub2.
^ ^a ^b United States Food & Drug Administration, (2004), p1
^ ^a ^b ^c Dolan, C. M., (1958)
^ Porsolt, Roger D.; P. Martin; A.Lenégre; S. Fromage; C. E. Giurgea (1989). "Prevention of "learned helplessness" in the rat by hydroxyzine". Drug Development Research. 17 (3): 227–236. doi:10.1002/ddr.430170306.
^ "Ucerax (hydroxyzine hydrochloride) 25 mg film-coated tablets. Summary of product characteristics" (PDF). Irish Medicines Board. Retrieved 9 February 2014.
^ [1] "The extent of renal excretion of VISTARIL has not been determined"[2]
^ ^a ^b ^c United States Food & Drug Administration, (2004), p3
^ ^a ^b ^c ^d ^e ^f United States Food & Drug Administration, (2004), p2
^ ^a ^b ^c Clark, B. G., Araki, M., et al. (1976)
^ ^a ^b ^c UCB South-Africa, et al., (2004)
^ Anderson, P. O., Knoben, J. E., et al. (2002), p794-796
^ Brabander, A. DE, Debert, W., (1990), p1
^ ^a ^b Brabander, A. DE, Debert, W., (1990), p3
^ Alford, C.; N. Rombautt, J. Jones, S. Foley, C. Idzikowskit and I. Hindmarch (1992).
^ NCQA’s HEDIS Measure: Use of High Risk Medications in the Elderly, http://www.ncqa.org/Portals/0/Newsroom/SOHC/Drugs_Avoided_Elderly.pdf
^ Wurtzell, Elizabeth (1995). Prozac Nation: a Memoir. New York, London: Riverhead. ISBN 978-1573225120.
^ http://dictionary.reference.com/slideshows/unique_words#hydroxyzine

External links

Print sources

Hutcheon, D. E.; D.L. Morris; A. Scriabine (December 1956). "Cardiovascular action of hydroxyzine (Atarax)". J Pharmacol Exp Ther. 118 (4): 451–460. PMID 13385806.
Dolan, C. M. (June 1958). "MANAGEMENT OF EMOTIONAL DISTURBANCES—Use of Hydroxyzine (Atarax®) in General Practice". Calif Med. 88 (6): 443–444. PMC 1512309. PMID 13536863.
Pfizer Labs, Division of Pfizer Inc, NY, NY 10017 (2004). Vistaril (hydroxyzine pamoate) Capsules and Oral Suspension (pdf). United States Food and Drug Administration. Retrieved 2007-03-09.
Anderson, Philip O.; James E. Knoben; William G. Troutman (2002). Handbook of Clinical Drug Data. McGraw-Hill Medical. ISBN 0-07-136362-9.
de Brabander, A.; W. Deberdt (1990). "Effect of Hydroxyzine on Attention and Memory". Human Psychopharmacology. John Wiley & Sons. 5 (4): 357–362. doi:10.1002/hup.470050408. Retrieved 2007-03-09.
Clark, B. G.; M. Araki; H. W. Brown (1982). "Hydroxyzine-Associated Tardive Dyskinesia". Ann. Neurol. 11 (4): 435. doi:10.1002/ana.410110423. PMID 7103423.
Porsolt, R. D.; P. Martin; A. Lenegre; S. Frornage; and C.E. Giurgea (1989). "Prevention of "Learned Helplessness" in the Rat by Hydroxyzine". Drug Dev. Res. 17 (3): 227–236. doi:10.1002/ddr.430170306. Retrieved 2007-03-10.
Alford, C.; N. Rombautt; J. Jones; S. Foley; C. Idzikowskit; I. Hindmarch (1992). "Acute Effects of Hydroxyzine on Nocturnal Sleep and Sleep Tendency the Following Day: a C-EEG Study". Human Psychopharmacology. 7 (1): 25–35. doi:10.1002/hup.470070104. Retrieved 2007-03-10.

Internet-based

RxList; et al. (2004). "Atarax Indications, Dosage, Storage, Stability". RxList - The internet drug index. Retrieved 2007-03-09.
Medscape (2004). "Vistaril Oral: Monograph - Hydroxyzine Hydrochloride, Hydroxyzine Pamoate". medscape.com. Retrieved 2007-03-09.
pfizer (2004). "Non-print version of vistaril fact sheet." (PDF). Retrieved 2007-07-03.
U.S. National Library of Medicine: Drug Information Portal - Hydroxyzine

UpToDate Contents

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1. 小児の双極性障害：治療法の選択に関する概要 pediatric bipolar disorder overview of choosing treatment
2. 成人における全般性不安障害に対する薬物療法 pharmacotherapy for generalized anxiety disorder in adults
3. 慢性蕁麻疹：標準的なマネージメントおよび患者教育 chronic urticaria standard management and patient education
4. 成人における全般性不安障害の治療法に対するアプローチ approach to treating generalized anxiety disorder in adults
5. 小児における接触皮膚炎 contact dermatitis in children

English Journal

Development and validation of a GC-MS method for the determination of hydroxyzine and its active metabolite, cetirizine, in whole blood.

Katselou M1, Athanaselis S1, Nikolaou P1, Dona A1, Spiliopoulou C1, Papoutsis I2.
Journal of pharmaceutical and biomedical analysis.J Pharm Biomed Anal.2017 Oct 25;145:765-772. doi: 10.1016/j.jpba.2017.07.059. Epub 2017 Aug 1.
PMID 28818802

Direct coupling of electromembrane extraction to mass spectrometry - Advancing the probe functionality toward measurements of zwitterionic drug metabolites.

Rye TK1, Fuchs D2, Pedersen-Bjergaard S3, Petersen NJ4.
Analytica chimica acta.Anal Chim Acta.2017 Aug 29;983:121-129. doi: 10.1016/j.aca.2017.05.038. Epub 2017 Jun 19.
PMID 28811018

A novel non-opioid protocol for medically supervised opioid withdrawal and transition to antagonist treatment.

Rudolf G1, Walsh J2, Plawman A2, Gianutsos P3, Alto W3, Mancl L4, Rudolf V2.
The American journal of drug and alcohol abuse.Am J Drug Alcohol Abuse.2017 Aug 10:1-8. doi: 10.1080/00952990.2017.1334209. [Epub ahead of print]
PMID 28795846

Japanese Journal

症例ヒドロキシジンパモ酸塩による急性汎発性発疹性膿疱症を発症後,尋常性乾癬へ移行した1例

皮膚科の臨床 60(2), 231-235, 2018-02
NAID 40021475861

Identification of compounds that suppress Toxoplasma gondii tachyzoites and bradyzoites

Plos One 12(6), e0178203, 2017-06-13
NAID 120006391021

悪性症候群の診断と治療に対する集学的取り組みにおいて薬学的アプローチが有用であった一例

薬学雑誌. 乙号 136(6), 925-929, 2016
NAID 130005154164

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★リンクテーブル★

リンク元	「ヒドロキシジン」
拡張検索	「hydroxyzine pamoate」「hydroxyzine hydrochloride」「hydroxyzine poisoning」

「ヒドロキシジン」

Hydroxyzine
Systematic (IUPAC) name
	(±)-2-(2-{4-[(4-chlorophenyl)-phenylmethyl]piperazin-1-yl}ethoxy)ethanol
Clinical data
Trade names	Vistaril , Atarax
AHFS/Drugs.com	Monograph
MedlinePlus	a682866
Pregnancy; category	AU: A; US: C (Risk not ruled out); ;
Routes of; administration	Oral, IM
Legal status
Legal status	AU: S4 (Prescription only); ℞ (Prescription only);
Pharmacokinetic data
Bioavailability	High in-vivo
Protein binding	93%
Metabolism	Hepatic
Biological half-life	20–24 hours
Excretion	Urine, Feces
Identifiers
CAS Number	68-88-2
ATC code	N05BB01 (WHO)
PubChem	CID 3658
IUPHAR/BPS	7199
DrugBank	DB00557
ChemSpider	3531
UNII	30S50YM8OG
KEGG	D08054
ChEBI	CHEBI:5818
ChEMBL	CHEMBL896
Chemical data
Formula	C21H27ClN2O2
Molar mass	374.904 g/mol
	SMILES Clc1ccc(cc1)C(c2ccccc2)N3CCN(CC3)CCOCCO ;
	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 ; Key:ZQDWXGKKHFNSQK-UHFFFAOYSA-N ;
(verify)

　　[★]

英: hydroxyzine
化: ヒドロキシジン塩酸塩塩酸ヒドロキシジン hydroxyzine hydrochloride、パモ酸ヒドロキシジン　ヒドロキシジンパモ酸塩　 hydroxyzine pamoate
商: アタラックス、アタラックス-P、ハタナジン
関: 精神神経用剤

「hydroxyzine pamoate」

　　[★]

パモ酸ヒドロキシジン、ヒドロキシジンパモ酸塩

関: hydroxyzine、hydroxyzine hydrochloride

「hydroxyzine hydrochloride」

　　[★]

塩酸ヒドロキシジン、ヒドロキシジン塩酸塩

関: hydroxyzine、hydroxyzine pamoate

「hydroxyzine poisoning」

　　[★] ヒドロキシジン系薬中毒

[pmid6141198-1] Simons FE, Simons KJ, Frith EM (January 1984). "The pharmacokinetics and antihistaminic of the H1 receptor antagonist hydroxyzine". The Journal of Allergy and Clinical Immunology. 73 (1 Pt 1): 69–75. doi:10.1016/0091-6749(84)90486-x. PMID 6141198.

[isbn0-19-536874-6-2] Shorter, Edward (2009). Before Prozac: the troubled history of mood disorders in psychiatry. Oxford [Oxfordshire]: Oxford University Press. ISBN 0-19-536874-6.

[3] SCHRAM, WS (March 1959). "Use of hydroxyzine in psychosis.". Diseases of the Nervous System. 20 (3): 126–9. PMID 13639831.

[4] FDA DrugInfo: http://dailymed.nlm.nih.gov/dailymed/archives/fdaDrugInfo.cfm?archiveid=51459

[urlHydroxyzine_Facts_and_Comparisons_at_Drugs.com-5] "Hydroxyzine Facts and Comparisons at Drugs.com".

[6] H. Morren, U.S. Patent 2,899,436 (1959); H. Morren, DE 1049383 (1954); H. Morren, DE 1061786 (1954); H. Morren, DE 1068262 (1954); H. Morren, DE 1072624 (1954); H. Morren, DE 1075116 (1954).

[pmid11809864-7] Gillard M, Van Der Perren C, Moguilevsky N, Massingham R, Chatelain P (February 2002). "Binding characteristics of cetirizine and levocetirizine to human H(1) histamine receptors: contribution of Lys(191) and Thr(194)". Molecular Pharmacology. 61 (2): 391–9. doi:10.1124/mol.61.2.391. PMID 11809864.

[pmid1979798-8] Snowman AM, Snyder SH (December 1990). "Cetirizine: actions on neurotransmitter receptors". The Journal of Allergy and Clinical Immunology. 86 (6 Pt 2): 1025–8. doi:10.1016/S0091-6749(05)80248-9. PMID 1979798.

[pmid2884340-9] Kubo N, Shirakawa O, Kuno T, Tanaka C (March 1987). "Antimuscarinic effects of antihistamines: quantitative evaluation by receptor-binding assay". Japanese Journal of Pharmacology. 43 (3): 277–82. doi:10.1254/jjp.43.277. PMID 2884340.

[pmid13784865-10] WHITE RP, BOYAJY LD (September 1960). "Neuropharmacological comparison of atropine, scopolamine, banactyzine, diphenhydramine and hydroxyzine". Archives Internationales de Pharmacodynamie et de Thérapie. 127: 260–73. PMID 13784865.

[pmid9193868-11] Haraguchi K, Ito K, Kotaki H, Sawada Y, Iga T (June 1997). "Prediction of drug-induced catalepsy based on dopamine D1, D2, and muscarinic acetylcholine receptor occupancies". Drug Metabolism and Disposition: the Biological Fate of Chemicals. 25 (6): 675–84. PMID 9193868.

[pmid15627436-12] Orzechowski RF, Currie DS, Valancius CA (January 2005). "Comparative anticholinergic activities of 10 histamine H1 receptor antagonists in two functional models". European Journal of Pharmacology. 506 (3): 257–64. doi:10.1016/j.ejphar.2004.11.006. PMID 15627436.

[Berger1957-13] Berger, F. M. (1957). "THE CHEMISTRY AND MODE OF ACTION OF TRANQUILIZING DRUGS". Annals of the New York Academy of Sciences. 67 (10): 685–700. doi:10.1111/j.1749-6632.1957.tb46006.x. ISSN 0077-8923.

[Tripathi2013-14] K. D. Tripathi (2013). Essentials of Medical Pharmacology. JP Medical Ltd. p. 165. ISBN 978-93-5025-937-5.

[isbn1-58562-254-0-15] Barbara Olasov Rothbaum; Stein, Dan J.; Hollander, Eric (2009). Textbook of Anxiety Disorders. American Psychiatric Publishing, Inc. ISBN 1-58562-254-0.

[pmid15388291-16] Lamberty Y, Gower AJ (September 2004). "Hydroxyzine prevents isolation-induced vocalization in guinea pig pups: comparison with chlorpheniramine and immepip". Pharmacology, Biochemistry, and Behavior. 79 (1): 119–24. doi:10.1016/j.pbb.2004.06.015. PMID 15388291.

[17] Llorca PM, Spadone C, Sol O, et al. (November 2002). "Efficacy and safety of hydroxyzine in the treatment of generalized anxiety disorder: a 3-month double-blind study" (PDF). J Clin Psychiatry. 63 (11): 1020–7. doi:10.4088/JCP.v63n1112. PMID 12444816.

[18] Giuseppe Guaiana1, Corrado Barbui, Andrea Cipriani (8 December 2010). "Hydroxyzine for generalised anxiety disorder". The Cochrane Library. Cochrane Depression, Anxiety and Neurosis Group. doi:10.1002/14651858.CD006815.pub2.

[fda_vistaril-19] United States Food & Drug Administration, (2004), p1

[calif_dolan-20] Dolan, C. M., (1958)

[21] Porsolt, Roger D.; P. Martin; A.Lenégre; S. Fromage; C. E. Giurgea (1989). "Prevention of "learned helplessness" in the rat by hydroxyzine". Drug Development Research. 17 (3): 227–236. doi:10.1002/ddr.430170306.

[22] "Ucerax (hydroxyzine hydrochloride) 25 mg film-coated tablets. Summary of product characteristics" (PDF). Irish Medicines Board. Retrieved 9 February 2014.

[23] [1] "The extent of renal excretion of VISTARIL has not been determined"[2]

[fda_vistaril_3-24] United States Food & Drug Administration, (2004), p3

[fda_vistaril_2-25] ^ ^a ^b ^c ^d ^e ^f United States Food & Drug Administration, (2004), p2

[clark_phen-26] Clark, B. G., Araki, M., et al. (1976)

[manufact_sa-27] UCB South-Africa, et al., (2004)

[28] Anderson, P. O., Knoben, J. E., et al. (2002), p794-796

[brabander_p1-29] Brabander, A. DE, Debert, W., (1990), p1

[brabander_p3-30] Brabander, A. DE, Debert, W., (1990), p3

[hydroxy_sleep-31] Alford, C.; N. Rombautt, J. Jones, S. Foley, C. Idzikowskit and I. Hindmarch (1992).

[32] NCQA’s HEDIS Measure: Use of High Risk Medications in the Elderly, http://www.ncqa.org/Portals/0/Newsroom/SOHC/Drugs_Avoided_Elderly.pdf

[33] Wurtzell, Elizabeth (1995). Prozac Nation: a Memoir. New York, London: Riverhead. ISBN 978-1573225120.

[34] ttp://dictionary.reference.com/slideshows/unique_words#hydroxyzine

v t e Antihistamines (R06)

Aminoalkyl ethers	Bromazine (bromodiphenhydramine) Carbinoxamine Clemastine Chlorphenoxamine Diphenylpyraline Diphenhydramine Doxylamine Orphenadrine Phenyltoloxamine

Substituted alkylamines	Brompheniramine Chlorphenamine Dexbrompheniramine (+pseudoephedrine) Dexchlorpheniramine (+betamethasone) Dimetindene Pheniramine Talastine

Substituted ethylenediamines	Chloropyramine Histapyrrodine Mepyramine Methapyrilene Tripelennamine (pyribenzamine)

Phenothiazine derivatives	Alimemazine Fenethazine Hydroxyethylpromethazine Isothipendyl Mequitazine Methdilazine Oxomemazine Promethazine

Piperazine derivatives	Buclizine Cetirizine Levocetirizine Chlorcyclizine Cinnarizine Cyclizine Hydroxyzine Meclizine Oxatomide

Others for systemic use	Antazoline Azanator Azatadine Bamipine Cyproheptadine Deptropine Ebastine Emedastine Epinastine Ketotifen Latrepirdine Mebhydrolin Mizolastine Olopatadine Phenindamine Pimethixene Pyrrobutamine Quifenadine Rupatadine Triprolidine selective (Acrivastine Astemizole Azelastine Bilastine Desloratadine Fexofenadine Loratadine Terfenadine)

For topical use	Bamipine Chloropyramine Chlorphenoxamine Clemastine Dimetindene Diphenhydramine Isothipendyl Mepyramine Promethazine Thenalidine

v t e Antiemetics (A04)

5-HT₃ serotonin ion channel antagonists	Alosetron Azasetron Bemesetron Cilansetron Clozapine Dazopride Dolasetron Granisetron Lerisetron Metoclopramide Mianserin Mirtazapine Olanzapine Ondansetron Palonosetron (+netupitant) Quetiapine Ramosetron Ricasetron Tropisetron Zatosetron

5-HT serotonin G-protein receptor antagonists	Clozapine Cyproheptadine Hydroxyzine Olanzapine Risperidone Ziprasidone

CB₁ agonists (cannabinoids)	Dronabinol Nabilone Tetrahydrocannabinol (cannabis)

D₂/D₃ antagonists	Alizapride Bromopride Chlorpromazine Clebopride Domperidone Haloperidol Hydroxyzine Itopride Metoclopramide Metopimazine Prochlorperazine Thiethylperazine Trimethobenzamide

H₁ antagonists (antihistamines)	Cyclizine Dimenhydrinate Diphenhydramine Hydroxyzine Meclizine Promethazine

mACh antagonists (anticholinergics)	Atropine Diphenhydramine Hydroxyzine (very mild) Hyoscyamine Scopolamine

NK₁ antagonists	Aprepitant Casopitant Ezlopitant Fosaprepitant Maropitant Netupitant Rolapitant Vestipitant

Others	Cerium oxalate Dexamethasone Lorazepam Midazolam Propofol

v t e Anxiolytics (N05B)

5-HT_1A agonists	Buspirone Tandospirone

GABA_AR PAMs	Benzodiazepines: Adinazolam Alprazolam Bromazepam Camazepam Chlordiazepoxide Clobazam Clonazepam Clorazepate Clotiazepam Cloxazolam Diazepam^# Ethyl loflazepate Etizolam Fludiazepam Halazepam Ketazolam Lorazepam^# Medazepam Nordazepam Oxazepam Pinazepam Prazepam Others: Alpidem^‡ Barbiturates Carbamates Chlormezanone^‡ Ethanol Etifoxine; Herbs: Kava Skullcap Valerian

α₂δ VDCC blockers	Gabapentin Gabapentin enacarbil Phenibut Pregabalin

Antidepressants	SSRIs SNRIs SARIs TCAs TeCAs MAOIs; Others: Agomelatine Bupropion Vilazodone Vortioxetine

Sympatholytics	Beta blockers (e.g., propranolol) Clonidine Dexmedetomidine Guanfacine Prazosin

Others	Benzoctamine Cannabidiol Cycloserine Fabomotizole Hydroxyzine Kanna Lavender Lorpiprazole Mebicar Mepiprazole Nicotine Opipramol Oxaflozane^‡ Phenaglycodol Phenibut Picamilon Selank Tiagabine Tofisopam Validolum

v t e Piperazines

Simple piperazines (no additional rings)	1-Cyclohexylpiperazine Aminoethylpiperazine Diethylcarbamazine HEPPS Midafotel Piperazine PIPES

Phenylpiperazines	Acaprazine Antrafenine Aripiprazole Batoprazine Bifeprunox BRL-15,572 Ciprofloxacin CSP-2503 Dapiprazole DCPP DMPP Diphenylpiperazine Dropropizine EGIS-12,233 Elopiprazole Eltoprazine Enpiprazole Ensaculin Etoperidone Flesinoxan Flibanserin Fluprazine Itraconazole Ketoconazole Levodropropizine Lorpiprazole mCPP Mefway MeOPP Mepiprazole Naftopidil Naluzotan Naphthylpiperazine Nefazodone Niaprazine Oxypertine Pardoprunox pCPP pFPP Posaconazole S-14,506 S-14,671 S-15,535 SB-258,585 SB-271,046 SB-357,134 SB-399,885 Sonepiprazole TFMPP Tolpiprazole Trazodone Urapidil Vesnarinone Vilazodone Vortioxetine WAY-100,135 WAY-100,635

Benzylpiperazines	2C-B-BZP Befuraline Bifeprunox Buclizine BZP Chlorbenzoxamine DBZP Fipexide Imatinib MBZP MDBZP Meclozine Methoxypiperamide Piberaline Piribedil Sunifiram Trimetazidine Vesnarinone

Diphenylalkylpiperazines (benzhydrylalkylpiperazines)	Almitrine Amperozide BRL-15,572 Buclizine BW373U86 Cetirizine Chlorbenzoxamine Chlorcyclizine Cinnarizine Clocinizine Cyclizine DBL-583 Diphenylmethylpiperazine Dotarizine DPI-221 DPI-287 DPI-3290 GBR-12,783 GBR-12,935 GBR-13,069 GBR-13,098 GBR-13,119 Hydroxyzine Lidoflazine Manidipine Meclozine Oxatomide SNC-80 Vanoxerine

Pyrimidinylpiperazines	Buspirone Dasatinib Eptapirone Gepirone Ipsapirone Piribedil Prazitone Pyrimidinylpiperazine Revospirone Tandospirone Tirilazad Trimazosin Umespirone Zalospirone

Pyridinylpiperazines	Atevirdine Azaperone Delavirdine Mirtazapine Pyridinylpiperazine

Benzo(iso)thiazolylpiperazines	Lurasidone Perospirone Revospirone Tiospirone Ziprasidone

Tricyclics (piperazine attached via side chain)	Amoxapine Clopenthixol Clorotepine Clozapine Cyanothepin Doclothepin Docloxythepin Flupentixol Fluphenazine Isofloxythepin Loxapine Meperathiepin Metitepine Octomethothepin Olanzapine Opipramol Oxyclothepin Oxyprothepin Peradithiepin Perathiepin Perazine Perphenazine Pirenzepine Prochlorperazine Thiethylperazine Thiothixene Trifluoperazine Trifluthepin Zuclopenthixol

Others/Uncategorized	6-Nitroquipazine Azimilide Cinepazet Cinepazic acid Cinepazide Cyclohexylpiperazine Hexocyclium Indinavir JNJ-7777120 Lodenafil Mirodenafil PB-28 Quipazine Ranolazine SA-4503 Sildenafil Tadalafil Vardenafil VUF-6002 Zipeprol

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hydroxyzine