Talk:Hydroxyzine

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Summary sheet: Hydroxyzine
Hydroxyzine
Hydroxyzine.svg
Chemical Nomenclature
Common names Vistaril, Atarax
Substitutive name Hydroxyzine
Systematic name 2-[2-[4-[(4-chlorophenyl)-phenylmethyl]piperazin-1-yl]ethoxy]ethanol
Class Membership
Psychoactive class Depressant
Chemical class Diphenylmethylpiperazine
Routes of Administration

WARNING: Always start with lower doses due to differences between individual body weight, tolerance, metabolism, and personal sensitivity. See responsible use section.



Oral
Dosage
Threshold 10 mg
Light 25 - 50 mg
Common 50 - 100 mg
Strong 100 - 150 mg
Heavy 150 mg +
Duration
Total 4 - 6 hours
Onset 15 - 30 minutes
Peak 2 - 4 hours
After effects 14 - 26 hours









DISCLAIMER: PW's dosage information is gathered from users and resources for educational purposes only. It is not a recommendation and should be verified with other sources for accuracy.

Interactions


Hydroxyzine is a first-generation antihistamine substance of the diphenylmethylpiperazine/ethano-piperidine class. It acts primarily as a potent and selective H1 receptor antagonist,[1][2] with anxiolytic effects attributable to weak antiserotonergic effects.[3]

It belongs to the piperazine/ethanopiperidine family of chemicals.[4] Hydroxyzine is often used in the treatment of itchiness, anxiety, insomnia, and nausea from motion sickness.[5] Unlike many other first-generation antihistamines, hydroxyzine has low affinity for muscarinic acetylcholine receptors, and thus does not produce strong anticholinergic side effects responsible for the deliriant properties of drugs such as diphenhydramine.[6]

Hydroxyzine sees little recreational use, limited mostly to where stronger anxiolytics, such as benzodiazepines or alcohol, are not available. Unlike more commonly abused depressants, it does not impact the neurotransmitter GABA, and acts by antagonizing adrenergic, dopaminergic, and serotonergic receptors. It is effective in the treatment of generalized anxiety disorder (due to its anxiolytic effects), short-term treatment of insomnia (due to its sedative effects), and allergic reactions (due to its antihistamine effects).[7] Despite having limited abuse potential, combining hydroxyzine with other depressants can lead to respiratory depression. Like other antihistamines, high doses of hydroxyzine can prolong the QT interval, which may lead to the development of torsades de pointes, a potentially fatal arrhythmia.[8] It is highly advised to use harm reduction practices if using this substance.

Tolerance to the CNS effects of hydroxyzine develops rapidly, often in as few as 3-7 days.[9] Tolerance to its sedative effects builds faster than tolerance to its anxiolytic effects. Such, it is indicated for use in short-term or as-needed insomnia treatment.

History and culture

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It was first made by Union Chimique Belge in 1956 and was approved for sale by Pfizer in the United States later that year. Originally mostly given for nausea and allergies, it was transitioned over to its anxiolytic purposes in medicine. It is commonly given as a substitute to an anxiolytic Benzodiazepine in surgeries to decrease anxiety and act as an anesthetic. [10][11] In the United Kingdom 28 doses cost less than a pound.[12] In the United States the wholesale cost in 2018 was about 0.05 USD per dose.[13] In the United States about 8 million prescriptions were written for hydroxyzine in 2016.[14]

Chemistry

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Hydroxyzine is a member of the diphenylmethylpiperazine and ethano-piperidine class of drugs.

Analogues of hydroxyzine include buclizine, cetirizine, cinnarizine, cyclizine, etodroxizine, meclizine, and pipoxizine among others.

Hydroxyzine is synthesized by the alkylation of 1-(4-chlorobenzhydryl)piperazine with 2-(2-Chloroethoxy)ethanopiperidine[15]

Pharmacology

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Hydroxyzine acts primarily as a potent histamine H1 receptor antagonist.[16][17] Hydroxyzine is notable for having lower affinity for muscarinic acetylcholine receptor, responsible for the deliriant action of other first-generation antihistamines, like diphenhydramine - subsequently, hydroxyzine is less liable to cause hallucinatory states or delirium. In addition to antihistaminergic activity, hydroxyzine acts as an antagonist for 5-HT2A receptors (responsible for its anxiolytic effects), D2 receptors, and A1 receptors (responsible for the emotional numbing hydroxyzine causes - this is a similar mechanism as antipsychotics, although notably weaker). Hydroxyzine is unique among first-generation antihistamines in that acts as an anxiolytic, likely attributable to its 5-HT2A antagonism. Hydroxyzine easily crosses the blood-brain barrier. Low doses of hydroxyzine (where less than 20% of H1 receptors are bound to) are not associated with somnolence, but high doses (where 50% or more of H1 receptors are bound to) cause sedation.[18]

Hydroxyzine is metabolized rapidly and crosses the blood-brain barrier with ease. When taken orally, it is rapidly absorbed through the gastrointestinal tract and is metabolized in the liver. Effects typically begin within 15-30 minutes. Peak concentration of hydroxyzine occurs at approximatively two hours after administration. Hydroxyzine and its metabolites have long half-lives, but the sedative effects typically at around 4-6 hours. In adults, the elimination half-life of hydroxyzine is 20 hours.

Subjective effects

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Disclaimer: The effects listed below cite the Subjective Effect Index (SEI), an open research literature based on anecdotal user reports and the personal analyses of PsychonautWiki contributors. As a result, they should be viewed with a healthy degree of skepticism.

It is also worth noting that these effects will not necessarily occur in a predictable or reliable manner, although higher doses are more liable to induce the full spectrum of effects. Likewise, adverse effects become increasingly likely with higher doses and may include addiction, severe injury, or death ☠.

Physical effects
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Visual effects
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Paradoxical effects
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Cognitive effects
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After effects
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Experience reports

There are currently no anecdotal reports which describe the effects of this compound within our experience index. Additional experience reports can be found here:

Toxicity and harm potential

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Note: Always conduct independent research and use harm reduction practices if using this substance.

It is strongly recommended that one use harm reduction practices when using this substance.

Lethal dosage

Tolerance and addiction potential

Hydroxyzine works in multiple ways and can cause a variety of effects. It is only proven to affect histamine but has been shown to effect Acetylcholine, Glutamate, and GABA. Being a dissociative at very high doses, it can act more similarly to Ketamine and PCP (structural relative)in comparison to other antihistamines like Diphenhydramine (a deliriant). Most abuse of this drug happens at lower doses with the desired effect being sedation. Being a relaxant sedative, it can become habit forming. Its sedative effects are found to be more powerful than that of Diphenhydramine or Doxylamine, and happens to have more of an anxiolytic/anticonvulsant effect than that of those named above. Because of this, it can be a safer substitute to Benzodiazepines and GABAergics, and can provide a similar effect. Tolerance to Hydroxyzine can develop fast and psychological addiction can be common in patients treated for anxiety and insomnia with Hydroxizine. Physical addiction and dependence is present but not common - much of the addiction is psychological. Safe use is recommended with this medication.

Dangerous interactions

This medication can interact with many other substances in dangerous and even lethal ways. Being a CNS depressant, it can be potentiated by other depressant drugs. Alcohol should always be avoided as well as other GABA active drugs like Benzodiazepines (Ex. Alprazolam, Diazepam), Barbiturates (Ex. Secobarbital, Sodium Thiopental), and Anticonvulsants (Ex. Gabapentin, Pregabalin, Carisoprodol, Baclofen). Other depressant drugs that can interact with this are opiates. Opiates can be potentiated by this drug and can increase risk for overdose. Phencyclidine is a piperidine similar in structure to this drug and can basically double dose you. Be careful with any depressant when taking this medication.

Legal status

United States: Hydroxyzine is available by prescription but is not scheduled due to its low abuse concern

See also

External links

Literature

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References

  1. Szepietowski J, Weisshaar E (2016). Itin P, Jemec GB (eds.). Itch - Management in Clinical Practice. Current Problems in Dermatology. 50. Karger Medical and Scientific Publishers. pp. 1–80. ISBN 9783318058895.
  2. Hosák L, Hrdlička M, et al. (2017). Psychiatry and Pedopsychiatry. Charles University in Prague, Karolinum Press. p. 364. ISBN 9788024633787.
  3. Snowman AM, Snyder SH (December 1990). "Cetirizine: actions on neurotransmitter receptors". The Journal of Allergy and Clinical Immunology. 86 (6 Pt 2): 1025–1028. doi:10.1016/S0091-6749(05)80248-9. PMID 1979798.
  4. "Hydroxyzine Hydrochloride Monograph for Professionals". Drugs.com. American Society of Health-System Pharmacists. Retrieved 21 Nov 2018.
  5. "Hydroxyzine Hydrochloride Monograph for Professionals". Drugs.com. American Society of Health-System Pharmacists. Retrieved 21 Nov 2018.
  6. 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): 277–282. doi:10.1254/jjp.43.277. PMID 2884340.
  7. Rosario B. Hidalgo, David V. Sheehan, in Handbook of Clinical Neurology, 2012
  8. British national formulary : BNF 74 (74 ed.). British Medical Association. 2017. p. X. ISBN 978-0857112989.
  9. Levander S, Ståhle-Bäckdahl M, Hägermark O (1 September 1991). "Peripheral antihistamine and central sedative effects of single and continuous oral doses of cetirizine and hydroxyzine". European Journal of Clinical Pharmacology. 41 (5): 435–439. doi:10.1007/BF00626365. PMID 1684750. S2CID 25249362.
  10. "Hydroxyzine Hydrochloride Monograph for Professionals". Drugs.com. American Society of Health-System Pharmacists. Retrieved 21 Nov 2018.
  11. Shorter E (2009). Before Prozac: the troubled history of mood disorders in psychiatry. Oxford [Oxfordshire]: Oxford University Press. ISBN 9780195368741.
  12. British national formulary : BNF 74 (74 ed.). British Medical Association. 2017. p. X. ISBN 978-0857112989.
  13. "NADAC as of 2018-11-21". Centers for Medicare and Medicaid Services. Retrieved 21 Nov 2018.
  14. British national formulary : BNF 74 (74 ed.). British Medical Association. 2017. p. X. ISBN 978-0857112989.
  15. 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).
  16. Szepietowski J, Weisshaar E (2016). Itin P, Jemec GB (eds.). Itch - Management in Clinical Practice. Current Problems in Dermatology. 50. Karger Medical and Scientific Publishers. pp. 1–80. ISBN 9783318058895.
  17. Hosák L, Hrdlička M, et al. (2017). Psychiatry and Pedopsychiatry. Charles University in Prague, Karolinum Press. p. 364. ISBN 9788024633787.
  18. Yanai K, Tashiro M (January 2007). "The physiological and pathophysiological roles of neuronal histamine: an insight from human positron emission tomography studies". Pharmacology & Therapeutics. 113 (1): 1–15. doi:10.1016/j.pharmthera.2006.06.008. PMID 16890992. 
  19. Anderson PO, Knoben JE, Troutman WG (2002). Handbook of Clinical Drug Data. pp. 794-6. ISBN 9780071363624. PMC 1875767. PMID 20313924.