Talk:Hydroxyzine: Difference between revisions
>Average Dropout m Incorrectly placed possessive apostrophes and commas within a run-on sentence; fixes of some minor spelling errors. Addition of periods where necessary. Minor sentence structure changes for clarity. |
>Vanillaaaa add more info to page (still need to add more to toxicity/harm potential, chemistry, and history/culture) |
||
Line 3: | Line 3: | ||
{{SubstanceBox/Hydroxyzine}} | {{SubstanceBox/Hydroxyzine}} | ||
'''Hydroxyzine''' is a [[psychoactive class::antihistamine]] substance of the [[chemical class::diphenylmethylpiperazine/ethano-piperidine]] class. | '''Hydroxyzine''' is a first-generation [[psychoactive class::antihistamine]] substance of the [[chemical class::diphenylmethylpiperazine/ethano-piperidine]] class. It acts primarily as a potent and selective H1 receptor antagonist,<ref>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.</ref><ref>Hosák L, Hrdlička M, et al. (2017). Psychiatry and Pedopsychiatry. Charles University in Prague, Karolinum Press. p. 364. ISBN 9788024633787.</ref> with anxiolytic effects attributable to weak antiserotonergic effects.<ref>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.</ref> | ||
Hydroxyzine is used in the treatment of [[itchiness]], [[anxiety]], [[insomnia]], and [[nausea]] | It belongs to the [[psychoactive class::piperazine/ethanopiperidine]] family of chemicals.<ref>"Hydroxyzine Hydrochloride Monograph for Professionals". Drugs.com. American Society of Health-System Pharmacists. Retrieved 21 Nov 2018.</ref> Hydroxyzine is often used in the treatment of [[itchiness]], [[anxiety]], [[insomnia]], and [[nausea]] from motion sickness.<ref>"Hydroxyzine Hydrochloride Monograph for Professionals". Drugs.com. American Society of Health-System Pharmacists. Retrieved 21 Nov 2018.</ref> 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]].<ref>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.</ref> | ||
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).<ref>Rosario B. Hidalgo, David V. Sheehan, in Handbook of Clinical Neurology, 2012</ref> 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.<ref>British national formulary : BNF 74 (74 ed.). British Medical Association. 2017. p. X. ISBN 978-0857112989.</ref> 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.<ref> 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.</ref> 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== | ==History and culture== | ||
Line 26: | Line 25: | ||
==Pharmacology== | ==Pharmacology== | ||
{{pharmacology}} | {{pharmacology}} | ||
Hydroxyzine | |||
Hydroxyzine acts primarily as a potent [[histamine]] H1 receptor [[antagonist]].<ref>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.</ref><ref>Hosák L, Hrdlička M, et al. (2017). Psychiatry and Pedopsychiatry. Charles University in Prague, Karolinum Press. p. 364. ISBN 9788024633787.</ref> 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]].<ref name="pmid16890992">{{cite journal | vauthors = Yanai K, Tashiro M | title = The physiological and pathophysiological roles of neuronal histamine: an insight from human positron emission tomography studies | journal = Pharmacology & Therapeutics | volume = 113 | issue = 1 | pages = 1–15 | date = January 2007 | pmid = 16890992 | doi = 10.1016/j.pharmthera.2006.06.008 }}</ref> | |||
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== | ==Subjective effects== | ||
Line 33: | Line 35: | ||
{{effects/base | {{effects/base | ||
|{{effects/physical | |{{effects/physical| | ||
*'''[[Effect::Sedation]]''' - Hydroxyzine | *'''[[Effect::Sedation]]''' - Hydroxyzine has milder sedative effects than other first-generation antihistamines, such as [[diphenhydramine]]. Tolerance to its sedative effects builds rapidly. | ||
*'''[[Effect::Motor control loss]]''' | *'''[[Effect::Motor control loss]]''' | ||
*'''[[Effect::Respiratory depression]]''' | |||
*'''[[Effect::Perception of bodily heaviness]]''' | |||
*'''[[Effect::Dizziness]]''' | |||
*'''[[Effect::Abnormal heartbeat]]''' | |||
*'''[[Effect::Increased heart rate]]''' | |||
*'''[[Effect::Difficulty urinating]]''' | |||
*'''[[Effect::Itchiness]]''' - Itchiness is suppressed in low doses but increased in high doses. | |||
*'''[[Effect::Nausea suppression]]''' - Hydroxyzine is indicated for treatment of nausea. | |||
*'''[[Effect::Dehydration]]''' | |||
*'''[[Effect::Cough suppression]]''' | |||
*'''[[Effect::Tactile hallucinations]]''' - This effect only occurs at dangerously high doses, such as intentional overdoses. | |||
}} | }} | ||
{{effects/visual| | {{effects/visual| | ||
*'''[[Effect::Visual acuity suppression]]''' - Like many [[depressants]], hydroxyzine is known to cause blurred or otherwise suppressed visual acuity in high doses. This is less likely to occur than other [[depressants]], however it can still present itself at higher doses, or if the user has a low tolerance. | |||
*'''[[Effect::External hallucinations]]''' - This effect is nowhere near as pronounced as [[diphenhydramine]] and only occurs in extremely high doses or when combined with other CNS depressants, such as [[lithium]], [[valproate]], [[antipsychotics]], or [[ethanol]].<ref> Anderson PO, Knoben JE, Troutman WG (2002). Handbook of Clinical Drug Data. pp. 794-6. ISBN 9780071363624. PMC 1875767. PMID 20313924.</ref> These experiences are often reported by individuals with psychiatric comorbidities who are prescribed [[mood stabilizers]], [[antipsychotics]], or [[tricylic]]/[[tetracyclic]] [[antidepressants]]. | |||
}} | |||
{{effects/paradoxical| | |||
Paradoxical reactions to hydroxyzine occur mostly in high doses and can include nausea, itchiness, agitation, restlessness, and muscle spasms. Extremely high doses can result in seizures, vomiting, uncontrollable shaking, and other effects typical of an antihistamine overdose. | |||
}} | }} | ||
|{{effects/cognitive| | |{{effects/cognitive| | ||
The general head space of hydroxyzine is described by many as one of mild to moderate sedation. | |||
The most prominent of these cognitive effects generally include: | |||
*'''[[Effect::Anxiety suppression]]''' - This effect is mild compared to [[benzodiazepines]]. | |||
*'''[[Effect::Disinhibition]]''' - This effect is mild compared to [[benzodiazepines]]. | |||
*'''[[Effect::Thought deceleration]]''' | |||
*'''[[Effect::Analysis suppression]]''' | *'''[[Effect::Analysis suppression]]''' | ||
*'''[[Effect:: | *'''[[Effect::Amnesia]]''' - This only occurs in very high doses and is less pronounced than other [[depressants]]. | ||
*'''[[Effect:: | *'''[[Effect::Emotion suppression]]''' - Antagonizing dopamine, adrenaline, and serotonin receptors, hydroxyzine exhibits similar emotional suppression to [[antipsychotics]], but far less pronounced. | ||
*'''[[Effect:: | *'''[[Effect::Language suppression]]''' - This only occurs in very high doses and may be indictive of an overdose. | ||
*'''[[Effect::Confusion]]''' | *'''[[Effect::Confusion]]''' | ||
*'''[[Effect::Creativity suppression]]''' | *'''[[Effect::Creativity suppression]]''' | ||
*'''[[Effect::Decreased libido]]''' | *'''[[Effect::Decreased libido]]''' | ||
}} | }} | ||
{{effects/ | {{effects/aftereffects| | ||
*'''[[Effect::Anxiety|Rebound anxiety]]''' - Rebound anxiety is a commonly observed effect with [[anxiety suppression|anxiety relieving]] substances like hydroxyzine. It typically corresponds to the total duration spent under the substance's influence along with the total amount consumed in a given period, an effect which can easily lend itself to cycles of dependence and addiction. Because hydroxyzine is a weak anxiolytic compared to [[benzodiazepines]], addiction is extremely rare, but physical dependence is possible with frequent use. | |||
*'''[[Effect::Sleepiness|Residual sleepiness]]''' - While hydroxyzine can be used as an effective [[hypnotic|sleep-inducing]] aid, its effects may persist into the morning afterward, which may lead users to feeling "groggy" or "dull" for up to a few hours. | |||
*'''[[Effect:: | *'''[[Effect::Thought deceleration]]''' | ||
*'''[[Effect:: | *'''[[Effect::Thought disorganization]]''' | ||
}} | }} | ||
}} | }} | ||
===Experience reports=== | ===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: | There are currently no anecdotal reports which describe the effects of this compound within our [[experience index]]. Additional experience reports can be found here: |