Talk:Hydroxyzine

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Summary sheet: Hydroxyzine

Template:SubstanceBox/Hydroxyzine

Hydroxyzine is a antihistamine substance of the diphenylmethylpiperazine/ethano-piperidine class. It is in the piperazine/ethanopiperidine family of chemicals.[1] It's main mechanism of action is as a potent and selective histamine H1 receptor antagonist.[2][3]

Hydroxyzine is used in the treatment of itchiness, anxiety, insomnia, and nausea due to motion sickness.[4]

Ferreri et al. (1995), in a placebo-controlled study, found hydroxyzine to be effective for the treatment of GAD (Generalized Anxiety Disorder) and Insomnia after 1 week of treatment and maintained the improvement throughout the study. It is effective at treating nausea and allergic reaction as well. [5]

Recreational use of Hydroxyzine is not common but is seen in some places. Being a sedative and relaxant, it can have quite some abuse potential, but is looked over amongst downer enthusiasts because it is much less potent than Benzodiazepines or Alcohol. Tolerance to this drug can develop rapidly and can be harmful. Psychological addiction is also common amongst users who use for sleep. After treatment is stopped, people often experience a form of insomnia rebound and feel like they need the drug to sleep.

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 it’s anxilotyc purposes in medecine. It is commonly given as a substitute to a Benzodiazepine anxilotyc in surgeries to decrease anxiety and act as an anesthetic. [6][7] In the United Kingdom 28 doses cost less than a pound.[8] In the United States the wholesale cost in 2018 was about 0.05 USD per dose.[9] In the United States about 8 million prescriptions were written for hydroxyzine in 2016.[10]

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[11]

Pharmacology

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Hydroxyzine is as a potent and selective histamine H1 receptor antagonist. This action is responsible for its antihistamine and sedative effects.[12][13] Hydroxyzine also has very low affinity for the NMDA receptors and muscarinic acetylcholine receptors, and in accordance, has low propensity for producing anticholinergic or hallucinatory side effects except for in high doswa. In addition to its antihistamine activity, hydroxyzine has also been shown to act more weakly as an antagonist of the serotonin 5-HT2A receptor, and a partial agonist of the dopamine D2 receptor, GABAa receptor, and the α1-adrenergic receptor, what causes relaxant and anxiolytic effects.[14][15]

Subjective effects

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Disclaimer: The effects listed below cite the Subjective Effect Index (SEI), a research literature based on anecdotal reports and the personal experiences of PsychonautWiki contributors. As a result, they should be regarded with a healthy degree of skepticism. It is 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 much more likely with higher doses and may include addiction, serious injury, or death.

Physical effects
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Hydroxyzine acts on the mind in many ways and causes CNS depression similar to other sedatives.

  • Sedation - Hydroxyzine is reported to be weakly or moderately sedating. It can be helpfull to fall a sleep.
  • Perception of bodily heaviness - Hydroxyzine makes your body heavy and unwilling to perform tasks. This action is usually caused by it’s depressant activity.
  • Motor control loss

Common amongst most CNS depressants and sedatives, must be taken into caution. Can cause injury and death.

Visual effects
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Cognitive 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 effect histamine but has been showed to effect Acetylcholine, Glutamate, and GABA. Being a dissociative at very high doses, it can act more similarly to Ketamine and PCP (structural relative), than 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. It’s sedative effects are found to be more powerful than that of Diphenhydramine or Doxylamine, and happens to have more of an anxylotic/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 who use for anxiety and insomnia. 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

Hydroxyzine is available only by prescription in the United States and is not scheduled due to the fact that it is not a drug of abuse concern.

See also

External links

Literature

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References

  1. "Hydroxyzine Hydrochloride Monograph for Professionals". Drugs.com. American Society of Health-System Pharmacists. Retrieved 21 Nov 2018.
  2. 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.
  3. Hosák L, Hrdlička M, et al. (2017). Psychiatry and Pedopsychiatry. Charles University in Prague, Karolinum Press. p. 364. ISBN 9788024633787.
  4. "Hydroxyzine Hydrochloride Monograph for Professionals". Drugs.com. American Society of Health-System Pharmacists. Retrieved 21 Nov 2018.
  5. Rosario B. Hidalgo, David V. Sheehan, in Handbook of Clinical Neurology, 2012
  6. "Hydroxyzine Hydrochloride Monograph for Professionals". Drugs.com. American Society of Health-System Pharmacists. Retrieved 21 Nov 2018.
  7. Shorter E (2009). Before Prozac: the troubled history of mood disorders in psychiatry. Oxford [Oxfordshire]: Oxford University Press. ISBN 9780195368741.
  8. British national formulary : BNF 74 (74 ed.). British Medical Association. 2017. p. X. ISBN 978-0857112989.
  9. "NADAC as of 2018-11-21". Centers for Medicare and Medicaid Services. Retrieved 21 Nov 2018.
  10. British national formulary : BNF 74 (74 ed.). British Medical Association. 2017. p. X. ISBN 978-0857112989.
  11. 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).
  12. 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.
  13. Hosák L, Hrdlička M, et al. (2017). Psychiatry and Pedopsychiatry. Charles University in Prague, Karolinum Press. p. 364. ISBN 9788024633787.
  14. Snowman AM, Snyder SH (1990). "Cetirizine: actions on neurotransmitter receptors". J. Allergy Clin. Immunol. 86 (6 Pt 2): 1025–8. doi:10.1016/S0091-6749(05)80248-9. PMID 1979798.
  15. 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.