Hydroxyzine (injection): Difference between revisions

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{{drugbox
{{DrugProjectFormSinglePage
| IUPAC_name =  
|authorTag={{VP}}<!--Overview-->
'''Hydroxyzine:'''<br />
|genericName=Hydroxyzine
2-(2-{4-[(4-chlorophenyl)(phenyl)methyl]piperazin-1-yl}ethoxy)ethanol
|aOrAn=an
|drugClass=[[antihistamine]]
|indicationType=treatment
|indication=for symptomatic relief of [[anxiety]] and tension associated with [[psychoneurosis]], [[pruritus]] due to allergic conditions such as chronic [[urticaria]] and atopic and contact [[dermatoses]], and in [[histamine]]-mediated [[pruritus]], [[sedative]] when used as premedication and following [[general anesthesia]]
|adverseReactions=[[xerostomia]], [[headache]], [[somnolence]]


'''Hydroxyzine pamoate:'''<br />
<!--Black Box Warning-->
''1-(p-chlorobenzhydryl) 4- [2-(2-hydroxyethoxy) ethyl] diethylenediamine salt of 1,1'-methylene bis(2-hydroxy-3-naphthalene carboxylic acid)''
|blackBoxWarningTitle=Title
| image = Hydroxyzine.png
|blackBoxWarningBody=<i><span style="color:#FF0000;">ConditionName: </span></i>
| image2 = Hydroxyzine-3d-sticks.png
 
| CAS_number = 68-88-2
* Content
| CAS_supplemental = (hydroxyzine)
 
| ChemSpiderID = 3531
<!--Adult Indications and Dosage-->
| ATC_prefix = N05
 
| ATC_suffix = BB01
<!--FDA-Labeled Indications and Dosage (Adult)-->
| ATC_supplemental =  
|fdaLIADAdult======Symptomatic relief of anxiety=====
| PubChem = 3658
 
| DrugBank = APRD00688
* Dosing Information
| synonyms = '''Hydroxyzine pamoate''':<br /> Vistaril
 
'''Hydroxyzine hydrochloride''':<br />  Atarax
:*For symptomatic relief of [[anxiety]] and tension associated with [[psychoneurosis]] and as an adjunct in organic disease states in which [[anxiety]] is manifested: in adults, 50–100 mg q.i.d.
[http://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?id=1494], Ucerax [http://emc.medicines.org.uk/emc/assets/c/html/displaydoc.asp?DocumentID=9417], Serecid [http://www.medsafe.govt.nz/Profs/Datasheet/s/Serecidcap.htm], ANX
 
| C=21 | H=27 | Cl=1 | N=2 | O=2
=====Chronic Urticaria=====
| molecular_weight = 374.904 g/mol
 
| bioavailability = High [[In vivo|in-vivo]]
* Dosing Information
| protein_bound = 93%
 
| metabolism = [[Renal]]
:*For use in the management of [[pruritus]] due to allergic conditions such as chronic [[urticaria]] and atopic and contact dermatoses, and in histamine-mediated [[pruritus]]: in adults, 25 mg t.i.d. or q.i.d.
| smiles=C1CN(CCN1CCOCCO)C(C2=CC=CC=C2)C3=CC=C(C=C3)Cl
 
| elimination_half-life = 20 to 25 hours
=====Sedative when used as premedication and following general anesthesia=====
| pregnancy_AU = A
 
| pregnancy_US = C
* Dosing Information
| legal_status = Rx-only
 
| routes_of_administration = [[Mouth|Oral]], [[intramuscular injection]]
:*As a sedative when used as premedication and following general anesthesia, Hydroxyzine may potentiate [[meperidine]] (Demerol®) and barbiturates, so their use in [[pre-anesthetic]] adjunctive therapy should be modified on an individual basis. Atropine and other belladonna alkaloids are not affected by the drug. Hydroxyzine is not known to interfere with the action of digitalis in any way and it may be used concurrently with this agent.
| excretion = Urine, Feces
 
}}
:*As a [[sedative]] when used as a premedication and following general anesthesia: 50–100 mg in adults.
{{SI}}
 
<!--Off-Label Use and Dosage (Adult)-->
 
<!--Guideline-Supported Use (Adult)-->
|offLabelAdultGuideSupport=There is limited information regarding <i>Off-Label Guideline-Supported Use</i> of {{PAGENAME}} in adult patients.
 
<!--Non–Guideline-Supported Use (Adult)-->
|offLabelAdultNoGuideSupport======Seasonal allergic rhinitis=====
 
* Dosing Information
 
:* Pretreatment with oral hydroxyzine was effective in relieving symptoms of [[seasonal allergic rhinitis]].
 
<!--Pediatric Indications and Dosage-->
 
<!--FDA-Labeled Indications and Dosage (Pediatric)-->
|fdaLIADPed======Symptomatic relief of anxiety=====
 
* Dosing Information
 
:*For symptomatic relief of anxiety and tension associated with psychoneurosis and as an adjunct in organic disease states in which anxiety is manifested: children under 6 years, 50 mg daily in divided doses and over 6 years, 50–100 mg daily in divided doses.
 
=====Chronic Urticaria=====
 
* Dosing Information
 
:*For use in the management of pruritus due to allergic conditions such as chronic urticaria and atopic and contact dermatoses, and in histamine-mediated pruritus: children under 6 years, 50 mg daily in divided doses and over 6 years, 50–100 mg daily in divided doses.
 
=====Sedative when used as premedication and following general anesthesia=====
 
* Dosing Information
 
:*As a sedative when used as premedication and following general anesthesia, Hydroxyzine may potentiate meperidine (Demerol®) and barbiturates, so their use in pre-anesthetic adjunctive therapy should be modified on an individual basis. Atropine and other belladonna alkaloids are not affected by the drug. Hydroxyzine is not known to interfere with the action of digitalis in any way and it may be used concurrently with this agent.
 
:*As a sedative when used as a premedication and following general anesthesia: 0.6 mg/kg in children.
 
<!--Off-Label Use and Dosage (Pediatric)-->
 
<!--Guideline-Supported Use (Pediatric)-->
|offLabelPedGuideSupport=There is limited information regarding <i>Off-Label Guideline-Supported Use</i> of {{PAGENAME}} in pediatric patients.
 
<!--Non–Guideline-Supported Use (Pediatric)-->
|offLabelPedNoGuideSupport=There is limited information regarding <i>Off-Label Non-Guideline-Supported Use</i> of {{PAGENAME}} in pediatric patients.
 
<!--Contraindications-->
|contraindications=*Hydroxyzine, when administered to the pregnant mouse, rat, and rabbit, induced fetal abnormalities in the rat and mouse at doses substantially above the human therapeutic range. Clinical data in human beings are inadequate to establish safety in early [[pregnancy]]. Until such data are available, hydroxyzine is contraindicated in early pregnancy.
 
*Hydroxyzine is contraindicated for patients who have shown a previous [[hypersensitivity]] to it.
 
<!--Warnings-->
|warnings=====Precautions====
 
*THE POTENTIATING ACTION OF HYDROXYZINE MUST BE CONSIDERED WHEN THE DRUG IS USED IN CONJUNCTION WITH [[CENTRAL NERVOUS SYSTEM DEPRESSANTS]] SUCH AS [[NARCOTICS]], NON-NARCOTIC [[ANALGESICS]] AND [[BARBITURATES]]. Therefore when central nervous system depressants are administered concomitantly with hydroxyzine their dosage should be reduced.


*Since [[drowsiness]] may occur with use of this drug, patients should be warned of this possibility and cautioned against driving a car or operating dangerous machinery while taking Atarax. Patients should be advised against the simultaneous use of other [[CNS depressant]] drugs, and cautioned that the effect of alcohol may be increased.


<!--Adverse Reactions-->


==Overview==
<!--Clinical Trials Experience-->
'''Hydroxyzine''' ({{pronEng|haɪˈdrɒksɨziːn}}) is a first-generation antihistamine, of the [[piperazine]] class that is an [[histamine receptor|H<sub>1</sub> receptor]] antagonist. It was synthesised in the early 1950s and the medicinal formulation of this drug was announced in the 04 August 1956 issue of ''Chemistry Week''. It is used primarily as an [[antihistamine]] for the treatment of itches and irritations, an [[antiemetic]] for the reduction of [[nausea]], as a weak [[analgesic]] by itself and as an opioid potentiator, and as an [[anxiolytic]] ''''''''for the treatment of anxiety''''''''.<ref name="rxlist_hyd">''RxList, et al.'' (2004)</ref> 
|clinicalTrials=*Side effects reported with the administration of Atarax (hydroxyzine hydrochloride) are usually mild and transitory in nature.


Its most common formulation is 25 mg small white, capsule-shaped and scored tablets of the hydrochloride salt made by UCB in the Netherlands.  In the United States, a nearly-spherical dark green tablet is the most-commonly encountered version of it, with 25 and 100 mg capsules being available as well as a series of colour-coded round tablets from Mallinkrodt (25 mg white, 50 mg orange, 100 mg blue).  Hydroxyzine preparations usually require a doctor's prescription as do other potent antihistamines in many countries whereas some countries allow hydroxyzine and all or most other antihistamines to be sold over the counter.
*Anticholinergic
:*[[Dry mouth]].


Even though it is an effective [[sedative]], [[hypnotic]], and [[tranquilizer]], it shares almost none of the abuse, dependence, addiction, and toxicity potential of other drugs used for the same range of therapeutic reasons. The drug is available in two [[formulation]]s, the pamoate and the dihydrochloride or hydrochloride salts. Vistaril, Equipose, Masmoran, Paxistil, and Vistaril Pamoate are preparations of the pamoate salt. Atarax, Alamon, Aterax, Durrax, Tran-Q, Orgatrax, Quiess, Vistaril Parenteral, and Tranquizine are hydroxyzine hydrochloride.
*Central Nervous System
:*[[Drowsiness]] is usually transitory and may disappear in a few days of continued therapy or upon reduction of the dose. [[Involuntary motor activity]] including rare instances of tremor and convulsions have been reported, usually with doses considerably higher than those recommended. Clinically significant respiratory depression has not been reported at recommended doses.


Other drugs related to hydroxyzine are [[cyclizine]] (Marezine), [[buclizine]], and [[meclizine]] (Dramamine II) 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, therefore having a narrower spectrum of effects, making it an effective antihistamine but removing some or all of the anxiolytic and analgesic-sparing properties.
<!--Postmarketing Experience-->
|postmarketing=There is limited information regarding <i>Postmarketing Experience</i> of {{PAGENAME}} in the drug label.


== Prescription and use ==
<!--Drug Interactions-->
Hydroxyzine is both an [[antihistamine]] and [[anxiolytic]] (see below) and its use as a mild [[tranquilizer]] is especially common in dentistry and it retains some popularity in obstetrics, where for many years it was especially preferred for its ability to boost the effectiveness of [[alphaprodine]] (Nisentil), a narcotic analgesic related to [[pethidine]] as well as permit later use of scopolamine or benzodiazepines better than other drugs might.
|drugInteractions=<!--Use in Specific Populations-->
|useInPregnancyFDA=* '''Pregnancy Category'''
|useInPregnancyAUS=* '''Australian Drug Evaluation Committee (ADEC) Pregnancy Category'''


Hydroxyzine hydrochloride is distributed by several manufacturers as tablets with strengths of 10, 25, 50, and 100 mg and hydroxyzine pamoate is distributed as capsules with strengths of 25, 50, and 100 mg. Oral liquids and ampules and multi-dose vials for injection are also available. Less commonly manufactured are tablet strengths of 5, 10, 20, and 30 mg , as are 25 mg suppositories.  The latter four tablet strengths are used both in human medical and veterinary settings.
There is no Australian Drug Evaluation Committee (ADEC) guidance on usage of {{PAGENAME}} in women who are pregnant.
|useInLaborDelivery=There is no FDA guidance on use of {{PAGENAME}} during labor and delivery.
|useInNursing=*It is not known whether this drug is excreted in human milk. Since many drugs are so excreted, hydroxyzine should not be given to nursing mothers.
|useInPed=There is no FDA guidance on the use of {{PAGENAME}} with respect to pediatric patients.
|useInGeri=*A determination has not been made whether controlled clinical studies of ATARAX included sufficient numbers of subjects aged 65 and over to define a difference in response from younger subjects. Other reported clinical experience has not identified differences in responses between the elderly and younger patients. In general, dose selection for an elderly patient should be cautious, usually starting at the low end of the dosing range, reflecting the greater frequency of decreased hepatic, renal or cardiac function, and of concomitant disease or other drug therapy.


Hydroxyzine is prescribed when the onset of an organic disease state manifests through anxiety, as [[general anxiety disorder]], or in other more serious cases as [[neurosis|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.<ref>{{cite journal |author=Llorca PM, Spadone C, Sol O, ''et al'' |title=Efficacy and safety of hydroxyzine in the treatment of generalized anxiety disorder: a 3-month double-blind study |journal=J Clin Psychiatry |volume=63 |issue=11 |pages=1020–7 |year=2002 |month=November |pmid=12444816 |doi= |url=http://www.psychiatrist.com/privatepdf/2002/v63n11/v63n1112.pdf}}</ref> Hydroxyzine can also be used for the treatment of [[allergy|allergic conditions]], such as chronic [[urticaria]], [[atopic dermatitis|atopic]] or [[contact dermatitis|contact dermatoses]], and [[histamine]]-mediated [[pruritus]].<ref name="rxlist_hyd" /> 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.<ref name="fda_vistaril">''United States Food & Drug Administration'', (2004), p1</ref>
*The extent of renal excretion of ATARAX has not been determined. Because elderly patients are more likely to have decreased [[renal function]], care should be taken in dose selections.


In the case of both the pamoate and hydrochloride salts, use of hydroxyzine for [[premedication]] as a sedative has no effects on belladonna alkaloids, such as [[atropine]], but may, following general anesthesia, potentiate [[pethidine|meperidine]] and [[barbiturate]]s, and use in pre-anesthetic adjunctive therapy should be modified depending upon the state of the individual.<ref name="fda_vistaril" /> Hydroxyzine is also safe to use alongside other medications or cardiac agents derived from the [[digitalis]] plant, as it does not yield any side-effects, due to its effects on the [[sympathetic nervous system|sympathetic]], rather than the [[central nervous system]].<ref name="fda_vistaril" />
*Sedating drugs may cause confusion and over sedation in the elderly; elderly patients generally should be started on low doses of ATARAX and observed closely.
|useInGender=There is no FDA guidance on the use of {{PAGENAME}} with respect to specific gender populations.
|useInRace=There is no FDA guidance on the use of {{PAGENAME}} with respect to specific racial populations.
|useInRenalImpair=There is no FDA guidance on the use of {{PAGENAME}} in patients with renal impairment.
|useInHepaticImpair=There is no FDA guidance on the use of {{PAGENAME}} in patients with hepatic impairment.
|useInReproPotential=There is no FDA guidance on the use of {{PAGENAME}} in women of reproductive potentials and males.
|useInImmunocomp=There is no FDA guidance one the use of {{PAGENAME}} in patients who are immunocompromised.


Whilst the analgesic-sparing (potentiating) effect is most marked with pethidine and relatives in certain cases such as post-operative pain, the effect can be noticed and used with most or all opioid analgesics and other centrally-acting analgesics which are not opioids such as [[orphenadrine]] and [[nefopam]] and may also help reduce muscle spasm and set the stage for [[ibuprofen]], [[naproxen]], other [[Non-steroidal anti-inflammatory drug|NSAIDs]], [[aspirin]] and [[paracetamol]] to work better for the patient, especially if used in conjunction with [[diphenhydramine]] (Tylenol PM, Percogesic Extra-Strength and its aspirin, naproxen, diclofenac, and ibuprofen analogues) or [[phenyltoloxamine]] (Percogesic original forumla, some extra-strength backache remedies like Momentum and Doan's Pills) 
<!--Administration and Monitoring-->
|administration=* Oral
|monitoring=There is limited information regarding <i>Monitoring</i> of {{PAGENAME}} in the drug label.


One of the more common regimens for moderate to moderately-severe pain -- be it acute, recurring acute or chronic -- prescribed in the United States and Canada and some European and Asian countries is a prescription for plain codeine tablets or combination products containing paracetamol, aspirin, ibuprofen,  or similar drug with codeine (Tylenol With Codeine No. 1, 2, 3 & 4, the Emprin With Codeine and 222-292-293-294 series, and many other trade names) and instructions to combine an anti-inflammatory pain reliever like ibuprofen or naproxen with it and to combine this with a prescription for hydroxyzine to be taken in dosages of 12.5 to 100 mg either along with the codeine or at a fixed schedule of its own.  In the case of sports injuries, other injuries, severe sinus infections and others, another part is added to the regimen in the form of a centrally-acting non-benzodiazepine muscle relaxant such as [[orphenadrine]] (Norflex), [[cyclobenzaprine]] (Flexeril), [[chlorzoxazone]] (Parafon), [[baclofen]] (Lioresal) and others.  Of course, the narcotic can be changed to [[hydrocodone]], [[dihydrocodeine]], [[ethylmorphine]], [[tramadol]], [[pentazocine]], [[nicodicodeine]], [[propiram]], [[oxycodone]], [[benzylmorphine]], [[thebacon]], [[nicocodeine]], [[dextropropoxyphene]], [[tilidine]], [[meptazinol]] or others; they can be found alone or in preparations which contain the narcotic along with aspirin, ibuprofen, or other similar drugs with or without paracetamol.  The selection of [[carisoprodol]] (Soma) as the muscle relaxant often yields a particularly powerful combination and the doses of the narcotic as well as the hydroxyzine must be cut down substantially to start the careful titration of the dose.  Such cases may produce enough somnolence to require the elimination of the hydroxyzine or replacement of it with [[cyclizine]] and/or addition of caffeine to the regimen by itself or as an ingredient in the narcotic combination product.
<!--IV Compatibility-->
|IVCompat=There is limited information regarding <i>IV Compatibility</i> of {{PAGENAME}} in the drug label.


In other cases, the usage of hydroxyzine is as a form of non-barbiturate tranquilliser<ref name="calif_dolan">''Dolan, C. M.,'' (1958)</ref> used in the pre-operative sedation and treatment of neurological disorders, such as psychoneurosis and other forms of anxiety or tension states.<ref name="calif_dolan" />  The trade name Atarax for the hydrochloride points to this ataractic (anti-anxiety) effect and Tranquizine and Tran-Q are trade names which point to a similar spectrum of actions.  Physicians and patients both often prefer hydroxyzine to benzodiazepines, babiturates, and meprobamate-glutethemide type depressants as first-line treatments for insomnia and daytime anxiety as hydroxyzine is safer, clears out of the system more quickly than many depressants like diazepam, phenobarbital, chloral hydrate and others, and does not cause physical dependence nor does it generate a morbid seek orientation for the drug in the patient.
<!--Overdosage-->
|overdose====Acute Overdose===


It has been suggested through pharmacological trials that the usage of hydroxyzine on dogs reduced the incidence and duration of ventricular arrythmias,<ref>''Hutcheon, D. E., Scriabine, A., et al.'' (1956)</ref> and that it is able to block the [[spasm]]ogenic actions associated with other substances such as [[serotonin]], [[reserpine]], [[histamine]], [[acetylcholine]] and the effect of pituitary extract on the [[duodenum]].<ref name="calif_dolan" /> Similarly, in experiments conducted on the [[ileum]] of small rabbits, hydroxyzine was found to inhibit [[hypermotility]] caused by the presence of [[barium chloride]].<ref name="calif_dolan" />
====Signs and Symptoms====


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 simultanteously or later in the procedure if need be.
*The most common manifestation of Atarax overdosage is [[hypersedation]]. As in the management of overdosage with any drug, it should be borne in mind that multiple agents may have been taken.


Hydroxyzine is one of the least [[anticholinergic]] first-generation antihistamines at about 8-10 per cent of the [[antimuscarinic]] power of atropine.  It is also, along with its relatives [[cyclizine]], [[buclizine]], [[meclizine]], and others as well as [[phenindamine]] (Thephorin, Nolahist) and [[cyproheptadine]] (Periactin) (the prototype of the piperidine chemical class of first-generation [[antihistamines]]), and the [[phenothiazines]], part of a small number of antihistamines to have clinically significant [[antiserotonergic]] effects as well.
*If [[vomiting]] has not occurred spontaneously, it should be induced. Immediate [[gastric lavage]] is also recommended. General supportive care, including frequent monitoring of the vital signs and close observation of the patient, is indicated. [[Hypotension]], though unlikely, may be controlled with [[intravenous fluids]] and Levophed® (levarterenol), or Aramine® (metaraminol). Do not use [[epinephrine]] as Atarax counteracts its [[pressor]] action.


Hydroxyzine has beneficial effects listed in this article but stands out in this pharmacotherapeutic category for its virtually non-existent addiction liability.  The piperazine class of antihistamines is the fourth or even lower of the seven categories of first-generation antihistamines in the generation of euphoria in patients.  The euphoria, which is mild (certainly not at the same level as morphine &c.) and tends to be either transient or long-lasting, appears to be part of the impact either direct or indirect on dopamine, acetylcholine, and possibly serotonin, norepinephrine, and even endorphin levels and ratios and possible activation of parts of the NMDA systems. Therefore, it would also stand to reason that it is reinforced by the alleviation of discomfort, much in the same way as some people experiencing transient euphoria after taking ibuprofen or naproxen.  The ethanolamines ([[diphenhydramine]], [[orphenadrine]], [[dimenhydrinate]], [[carbinoxamine]] and others) and alkylamines ([[triprolidine]], [[pheniramine]], [[brompheniramine]], [[chlorpheniramine]] and others) are the strongest euphoriants amongst antihistamines and some ethylenediamines like [[pyrilamine]] and [[tripelennamine]] are on the list as well.
====Management====


Hydroxyzine is not thought to be an effective treatment for anxiety if used for a period of over 4 months, and it is therefore a prerequisite of any medical professional prescribing such drugs, to re-assess the usefulness for the individual patient. Reasoning for this decision stems from the fact that hydroxyzine is mainly used as an antihistamine and has a somewhat short shelf-life in its common form. Rather than its use as an anxiety-reducing agent, hydroxyzine should be reconsidered if the patient has more intense anxiety or other psychoneurosis; then other compounds specifically designed for such conditions should be considered.<ref name="fda_vistaril_2">''United States Food & Drug Administration'', (2004), p2</ref>
*There is no specific antidote. It is doubtful that [[hemodialysis]] would be of any value in the treatment of overdosage with hydroxyzine. However, if other agents such as [[barbiturates]] have been ingested concomitantly, [[hemodialysis]] may be indicated. There is no practical method to quantitate hydroxyzine in body fluids or tissue after its ingestion or administration.


=== Treatment of learned helplessness  ===
===Chronic Overdose===
Aside from its prescription as an antihistamine, hydroxyzine has also shown slight possibilities for use in other species, such as dogs, from results and effects observed in rats with "[[learned helplessness]]" induced through the use of random inescapable shocks (max 0.8 mA) administered in 1 minute intervals for a period of 15 seconds for an hour.<ref name="rats_learned_p227">Porsolt, R. D.; P. Martin, A. Lenegre, S. Frornage, and C.E. Giurgea (1989), p229</ref> After the condition was induced, rats were then given a conditioned stimulus of a light, and shocked if unable to move to safety from the area producing the current within 3 seconds.<ref name="rats_learned_p228">Porsolt, R. D.; P. Martin, A. Lenegre, S. Frornage, and C.E. Giurgea (1989), p228</ref> Those unable to move were determined as having a conditioned stimulus of expecting shocks from the initial random condition.<ref name="rats_learned_p227" /><ref name="rats_learned_p228" />


In the initial treatment to this condition, rats were given hydroxyzine as a curative treatment for the shocks received and as a treatment for the prevention of learned helplessness by injection beforehand; results indicating that hydroxyzine decreased the overall amount of escape failures by a similar amount to those observed in diazepam, which achieved similar results, however, with side effects of amnesia.<ref name="rats_learned_p230">Porsolt, R. D.; P. Martin, A. Lenegre, S. Frornage, and C.E. Giurgea (1989), p230</ref><ref name="rats_learned_p228" /> Despite the fact that hydroxyzine clearly increased the ability of the rats to avoid stimuli, it had almost no effect on the rats' ability to respond to the shocks nor remove "stress" after exposure to shocks.<ref name="rats_learned_p230" />
There is limited information regarding <i>Chronic Overdose</i> of {{PAGENAME}} in the drug label.


== Clinical description ==
<!--Pharmacology-->
=== Metabolisation and pharmacokinetics  ===
Hydroxyzine can be administered orally as hydroxyzine [[hydrochloride]] or hydroxyzine embonate, or via intramuscular injection as hydroxyzine hydrochloride. When given orally, hydroxyzine is rapidly absorbed from the gastro-intestinal tract. The effect of hydroxyzine is notable in 30 minutes.


[[Pharmacokinetics|Pharmacokinetically]], hydroxyzine is rapidly diffused in the body and absorbed in oral and intramuscular administration, and is metabolised in the liver; the main metabolite (45%) through oxidation of the alcohol moiety to a carboxylic acid, is [[cetirizine]] and overall effects are observed within one hour of administration. It has a half-life observed on average for around 7-10 hours in adults, 6-7 hours in children, and 18-21 hours in the elderly, or those with [[renal insufficiency]], with higher concentrations found in the skin than in the plasma. Cetirizine, although less sedating, is non-[[dialysis|dialyzable]] and  possesses similar anti-histaminergic properties. "In animals, hydroxyzine and its metabolites are excreted in feces via biliary elimination."[http://www.medscape.com/druginfo/monograph?cid=med&drugid=6144&drugname=Vistaril+Oral&monotype=monograph&print=1] "The extent of renal excretion of VISTARIL has not been determined"[http://www.pfizer.com/pfizer/download/uspi_vistaril.pdf]
<!--Drug box 2-->
Administration in geriatrics differs from the administration of hydroxyzine (pamoate or Vistaril) in younger patients; according to the FDA, there have not been significant studies made (2004), which include population groups over 65, and therefore have not provided a distinction between elderly aged patients and other younger groups:<ref name="fda_vistaril_3">''United States Food & Drug Administration'', (2004), p3</ref> any hydroxyzine administered should be done with doses at the small end of the dosing range, and be carried out with the knowledge that any existing concomitant disease, or decrease in the function, or lessened excretion, such as the case may be with [[hepatic]], [[renal]] or [[cardiac]] states.<ref name="fda_vistaril_3" />
|drugBox={{Drugbox2
| verifiedrevid = 461774177
| IUPAC_name = (±)-2-(2-{4-[(4-chlorophenyl)-phenylmethyl]piperazin-1-yl}ethoxy)ethanol
| image = Hydroxyzine.png
| image2 = Hydroxyzine-3d-sticks.png


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 the patient.<ref name="fda_vistaril_3" /><ref name="calif_dolan" />
<!--Clinical data-->
| tradename = Vistaril
| Drugs.com = {{drugs.com|monograph|hydroxyzine-hydrochloride}}
| MedlinePlus = a682866
| pregnancy_AU = A
| pregnancy_US = C
| legal_AU = S4
| legal_status = Rx-only
| routes_of_administration = [[Mouth|Oral]], [[Intramuscular injection|IM]]


=== Contraindications ===
<!--Pharmacokinetic data-->
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 with doses significantly above that of the human therapeutic range.<ref name="fda_vistaril_2" /> In terms of humans, a significant dose has not yet been established in studies, and by default, the [[Food and drug administration|FDA]] has introduced contraindication guidelines in regard to
| bioavailability = High [[In vivo|in-vivo]]
hydroxyzine.<ref name="fda_vistaril_2" /> Similarly, those at risk from, or showing previous signs of [[hypersensitivity]] are also contraindicated.<ref name="fda_vistaril_2" />
| protein_bound = 93%
| metabolism = [[Liver|Hepatic]]
| elimination_half-life = 20–24 hours<ref name="pmid6141198">{{cite journal | author = Simons FE, Simons KJ, Frith EM | title = The pharmacokinetics and antihistaminic of the H1 receptor antagonist hydroxyzine | journal = The Journal of Allergy and Clinical Immunology | volume = 73 | issue = 1 Pt 1 | pages = 69–75 |date=January 1984 | pmid = 6141198 | doi = 10.1016/0091-6749(84)90486-x| url = }}</ref>
| excretion = [[Urine]], [[Feces]]


Other contraindications include the administration of hydroxyzine alongside depressants and other compounds which affect the central nervous system, such as narcotics, non-narcotic [[analgesic]]s and barbiturates, as well as alcohol,<ref name="fda_vistaril_2" /> and if absolutely necessary, should only administered concomitantly in small doses<ref name="fda_vistaril_2" /> as any pre-existing grogginess from these substances may be enhanced. 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.<ref name="fda_vistaril_2" />
<!--Identifiers-->
| CASNo_Ref = {{cascite|correct|CAS}}
| CAS_number_Ref = {{cascite|correct|??}}
| CAS_number = 68-88-2
| ATC_prefix = N05
| ATC_suffix = BB01
| PubChem = 3658
| DrugBank_Ref = {{drugbankcite|correct|drugbank}}
| DrugBank = DB00557
| ChemSpiderID_Ref = {{chemspidercite|correct|chemspider}}
| ChemSpiderID = 3531
| UNII_Ref = {{fdacite|correct|FDA}}
| UNII = 30S50YM8OG
| KEGG_Ref = {{keggcite|correct|kegg}}
| KEGG = D08054
| ChEBI_Ref = {{ebicite|correct|EBI}}
| ChEBI = 5818
| ChEMBL_Ref = {{ebicite|correct|EBI}}
| ChEMBL = 896


Studies have also been conducted which show that long-term prescription of hydroxyzine can lead to [[tardive dyskinesia]] after years of use, but has also been reported after periods of 7.5 months showed effects related to dyskinesia,<ref name="clark_phen">Clark, B. G., Araki, M., et al. (1976)</ref> 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,<ref name="clark_phen" /> and therefore some contraindication is given to the short-term administration of hydroxyzine to those with previous phenothiazine use.<ref name="clark_phen" />
<!--Chemical data-->
| C = 21 | H = 27 | Cl = 1 | N = 2 | O = 2
| molecular_weight = 374.904 g/mol
| smiles = Clc1ccc(cc1)C(c2ccccc2)N3CCN(CC3)CCOCCO
| InChI = 1/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
| InChIKey = ZQDWXGKKHFNSQK-UHFFFAOYAL
| StdInChI_Ref = {{stdinchicite|correct|chemspider}}
| StdInChI = 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
| StdInChIKey_Ref = {{stdinchicite|correct|chemspider}}
| StdInChIKey = ZQDWXGKKHFNSQK-UHFFFAOYSA-N
}}
 
<!--Mechanism of Action-->
|mechAction=* Atarax is unrelated chemically to the [[phenothiazines]], reserpine, meprobamate, or the [[benzodiazepines]].
 
*Atarax is not a cortical depressant, but its action may be due to a suppression of activity in certain key regions of the subcortical area of the [[central nervous system]]. Primary skeletal muscle relaxation has been demonstrated experimentally. [[Bronchodilator]] activity, and anti- histaminic and analgesic effects have been demonstrated experimentally and confirmed clinically. An [[antiemetic]] effect, both by the apomorphine test and the veriloid test, has been demonstrated. Pharmacological and clinical studies indicate that hydroxyzine in therapeutic dosage does not increase gastric secretion or acidity and in most cases has mild [[antisecretory]] activity. Hydroxyzine is rapidly absorbed from the gastrointestinal tract and Atarax's clinical effects are usually noted within 15 to 30 minutes after oral administration.
 
<!--Structure-->
|structure=* Hydroxyzine hydrochloride is designated chemically as 1-(p-chlorobenzhydryl) 4-[2-(2-hydroxyethoxy)-ethyl] piperazine dihydrochloride.
 
*Inert ingredients for the tablets are: acacia; carnauba wax; dibasic calcium phosphate; gelatin; lactose; magnesium stearate; precipitated calcium carbonate; shellac; sucrose; talc; white wax. The 10 mg tablets also contain: sodium hydroxide; starch; titanium dioxide; Yellow 6 Lake. The 25 mg tablets also contain: starch; velo dark green. The 50 mg tablets also contain: starch; velo yellow. The 100 mg tablets also contain: alginic acid; Blue 1; polyethylene glycol; Red 3.


=== Adverse reactions ===
*The inert ingredients for the syrup are: alcohol; menthol; peppermint oil; sodium benzoate; spearmint oil; sucrose; water.
:''For a full list of side effects, consult [[Hydroxyzine#Drug information pamphlets|the full technical specification]] of hydroxyzine.''
Several reactions have been noted in manufacturer guidelines for two forms of hydroxyzine: Atarax and Vistaril.  In Atarax, symptoms are similar to those of Vistaril -- deep sleep, incoordination and dizziness have been reported, as in children and adults, as well as others such as hypotension, [[tinnitus]] and headaches.<ref name="manufact_sa"> UCB South-Africa, et al., (2004)</ref>  [[Gastro-intestinal]] effects have also been observed in both Vistaril and Atarax, as well as less serious effects such as dryness of the mouth, constipation caused by [[antimuscarinic]] properties of hydroxyzine.<ref name="manufact_sa" />


Central nervous system problems such as hallucinations or confusion have been observed in rare cases, attributed mostly to overdosage.<ref name="manufact_sa" /><ref name="fda_vistaril_3" /> 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 description of 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 pharmacology|lithium]] or [[alcohol]].<ref>''Anderson, P. O., Knoben, J. E., et al.'' (2002), p794-796</ref>
<!--Pharmacodynamics-->
|PD=There is limited information regarding <i>Pharmacodynamics</i> of {{PAGENAME}} in the drug label.


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 hydroxyzine, 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.<ref name="brabander_p1">Brabander, A. DE, Debert, W., (1990), p1</ref>
<!--Pharmacokinetics-->
|PK=There is limited information regarding <i>Pharmacokinetics</i> of {{PAGENAME}} in the drug label.


In a comparative study with lorazepam on memory effects, patients who had taken hydroxyzine experienced sedative effects similar to drowsiness, but recalled that they felt capable, attentive and able to continue with a memory test under these conditions.<ref name="brabander_p3">Brabander, A. DE, Debert, W., (1990), p3</ref> 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.<ref name="brabander_p3" />
<!--Nonclinical Toxicology-->
|nonClinToxic=There is limited information regarding <i>Nonclinical Toxicology</i> of {{PAGENAME}} in the drug label.


Severe [[somnolence]] with or without vivid dreams or nightmares may occur in users with antihistamine sensitivities or other CNS depressants available in their systems. Hydroxyzine exhibits very potent [[anxiolytic]] and [[sedative]] properties in many psychiatric patients. Other studies have suggested that hydroxyzine acts as an acute hypnotic, reducing [[sleep onset latency]] and reciprocal increases in sleep duration -- also showing that some drowsiness did occur, but in female patients who also had greater hypnotic response. It did not, however, show any significant or noticeable effect of drowsiness, other than in female patients' subjective responses.<ref name="hydroxy_sleep">Alford, C.; N. Rombautt, J. Jones, S. Foley, C. Idzikowskit and I. Hindmarch (1992).</ref>
<!--Clinical Studies-->
|clinicalStudies=There is limited information regarding <i>Clinical Studies</i> of {{PAGENAME}} in the drug label.


Some users may report shortness of breath or wheezing, a result of a mild allergic reaction to the medication itself.
<!--How Supplied-->
|howSupplied=* Atarax Tablets
:*10 mg–orange tablets
:**100's (NDC 0049-5600-66)
:*25 mg–green tablets
:**100's (NDC 0049-5610-66),
:**500's (NDC 0049-5610-73)
:*50 mg–yellow tablets
:**100's (NDC 0049-5620-66)


In contrast to drugs in the benzodiazepine class, (i.e. [[alprazolam]], [[diazepam]]) which carry a potential for abuse and dependence, hydroxyzine is very unlikely to cause any dependence due to its relative strength compared to other substances.
*Atarax 100 Tablets
:*100 mg–red tablets
:**100's (NDC 0049-5630-66)


== References ==
*Atarax Syrup
=== Notes ===
:*10 mg per teaspoon (5 ml)
{{Reflist}}
:**1 pint bottles (NDC 0049-5590-93)
===  Print sources ===
:**Alcohol Content–Ethyl Alcohol–0.5% v/v
{{sourcesstart}}
* {{cite journal | last = Hutcheon | first = D. E. | coauthors = D.L. Morris, A. Scriabine | title = Cardiovascular action of hydroxyzine (Atarax) | journal = J Pharmacol Exp Ther. | volume = 118 | issue = 4 | pages = 451–460 | month =December | year =1956 | url = http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=13385806&dopt=Abstract | pmid = 13385806 | accessdate = 2007-03-09}}
* {{cite journal | last = Dolan | first = C. M. | title = Management of emotional disturbances -- Use of Hydroxyzine (Atarax) in General Practice | journal = Calif Med. | volume = 88 | issue = 6 | pages = 443–444 | month = June | year = 1958 | url = http://www.pubmedcentral.nih.gov/picrender.fcgi?artid=1512309&blobtype=pdf | pmid = 13536863 | accessdate = 2007-03-09}}
* {{Citation | last = Pfizer Labs, Division of [[Pfizer]] Inc, NY, NY 10017 | title = Vistaril (hydroxyzine pamoate) Capsules and Oral Suspension | publisher = [[Food and Drug Administration|United States Food and Drug Administration]] | year = 2004 | url=http://www.fda.gov/cder/ogd/rld/11795s16.pdf | format = pdf | access-date = 2007-03-09}}
* {{cite book | last = Anderson | first = Philip O. | coauthors = James E. Knoben, William G. Troutman | title = Handbook of Clinical Drug Data | publisher = [[McGraw-Hill]] Medical | year = 2002 | isbn = 0071363629 }}
* {{cite journal | last = de Brabander | first = A. | coauthors = W. Deberdt | title = Effect of Hydroxyzine on Attention and Memory | journal = Human Psychopharmacology | volume = 5 | issue = 4 | pages = 357–362 | publisher = [[Wiley]] | year = 1990 | url = http://www3.interscience.wiley.com/cgi-bin/abstract/109710652/ABSTRACT?CRETRY=1&SRETRY=0 | doi = 10.1002/hup.470050408 | accessdate = 2007-03-09}}
* {{cite journal | last = Clark | first = B. G. | coauthors = M. Araki, H. W. Brown | title = Hydroxyzine-Associated Tardive Dyskinesia | journal = Ann Neurol. | volume = 11 | issue = 4 | pages = 435 | year = 1982| url = http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=7103423&dopt=Abstract | pmid = 7103423 | accessdate = 2007-03-09 | doi = 10.1002/ana.410110423}}
* {{cite journal | last = Porsolt | first = R. D. | coauthors = P. Martin,  A. Lenegre, S. Frornage, and C.E. Giurgea | title = Prevention of “Learned Helplessness” in the Rat by Hydroxyzine | journal = Drug Dev. Res. | volume = 17 | issue = 3 | pages = 227–236 | year = 1989 | url = http://www3.interscience.wiley.com/cgi-bin/abstract/109670961/ABSTRACT?SRETRY=0 | doi = 10.1002/ddr.430170306 | accessdate = 2007-03-10 }}
* {{cite journal | last = Alford | first = C. | coauthors = N. Rombautt, J. Jones, S. Foley, C. Idzikowskit and I. Hindmarch | title = Acute Effects of Hydroxyzine on Nocturnal Sleep and Sleep Tendency the Following Day: a C-EEG Study | journal = Human Psychopharmacology | volume = 7 | issue = 1 | pages = 25–35 | year = 1992 | url = http://www3.interscience.wiley.com/cgi-bin/abstract/109711163/ABSTRACT | doi = 10.1002/hup.470070104 | accessdate = 2007-03-10 }}
{{sourcesend}}


=== Internet-based ===
<!--Patient Counseling Information-->
{{sourcesstart}}
|packLabel=[[File:Hydroxyzine01.png|thumb|none|400px|This image is provided by the National Library of Medicine.]]
*{{cite web | last = RxList , et al. | title = Atarax Indications, Dosage, Storage, Stability | publisher = RxList - The internet drug index | year = 2004 | url = http://www.rxlist.com/cgi/generic/hydrox_ids.htm | accessdate = 2007-03-09}}
[[File:Hydroxyzine02.png|thumb|none|400px|This image is provided by the National Library of Medicine.]]
* {{cite web | last = Medscape | title = Vistaril Oral: Monograph - Hydroxyzine Hydrochloride, Hydroxyzine Pamoate | publisher = medscape.com | year = 2004 | url = http://www.medscape.com/druginfo/monograph?cid=med&drugid=6144&drugname=Vistaril+Oral&monotype=monograph&print=1 | accessdate = 2007-03-09}}
* {{cite web | last = pfizer | title = Non-print version of vistaril fact sheet. | year = 2004 | url = http://www.pfizer.com/pfizer/download/uspi_vistaril.pdf |format=PDF| accessdate = 2007-07-03}}
{{sourcesend}}


=== Drug information pamphlets ===
|fdaPatientInfo=There is limited information regarding <i>Patient Counseling Information</i> of {{PAGENAME}} in the drug label.
{{sourcesstart}}
* UCB South-Africa, et al., (2004). ''ATERAX 25 mg TABLETS; ATERAX 100 mg TABLETS; ATERAX SYRUP'' (Manufacturing guidance package insert) Pharmacare Ltd, (a division of Aspen Pharmacare Ltd)
{{sourcesend}}
{{Anxiolytics}}
{{Antihistamines}}


[[Category:Analgesics]]
<!--Precautions with Alcohol-->
|alcohol=* Alcohol-{{PAGENAME}} interaction has not been established. Talk to your doctor about the effects of taking alcohol with this medication.
|brandNames=* ATARAX®<ref>{{Cite web | title = ATARAX- hydroxyzine hydrochloride tablet ATARAX- hydroxyzine hydrochloride syrup  | url = http://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=7eaf5043-5c73-47af-904b-8e1fae02af2e }}</ref>
|drugShortage=
}}
{{PillImage
|fileName=No image.jpg
}}
[[Category:Drug]]
[[Category:Antihistamines]]
[[Category:Antihistamines]]
[[Category:Anxiolytics]]
[[Category:H1 receptor antagonists]]
[[Category:Sedatives]]
[[Category:Piperazines]]
[[de:Hydroxyzin]]
[[es:Hidroxicina]]
[[fr:Hydroxyzine]]
[[pl:Hydroksyzyna]]
[[fi:Hydroksitsiini]]
[[sv:Hydroxizin]]
{{WH}}
{{WS}}

Latest revision as of 05:11, 15 May 2015

{{DrugProjectFormSinglePage |authorTag=Vignesh Ponnusamy, M.B.B.S. [1] |genericName=Hydroxyzine |aOrAn=an |drugClass=antihistamine |indicationType=treatment |indication=for symptomatic relief of anxiety and tension associated with psychoneurosis, pruritus due to allergic conditions such as chronic urticaria and atopic and contact dermatoses, and in histamine-mediated pruritus, sedative when used as premedication and following general anesthesia |adverseReactions=xerostomia, headache, somnolence

|blackBoxWarningTitle=Title |blackBoxWarningBody=ConditionName:

  • Content


|fdaLIADAdult======Symptomatic relief of anxiety=====

  • Dosing Information
  • For symptomatic relief of anxiety and tension associated with psychoneurosis and as an adjunct in organic disease states in which anxiety is manifested: in adults, 50–100 mg q.i.d.
Chronic Urticaria
  • Dosing Information
  • For use in the management of pruritus due to allergic conditions such as chronic urticaria and atopic and contact dermatoses, and in histamine-mediated pruritus: in adults, 25 mg t.i.d. or q.i.d.
Sedative when used as premedication and following general anesthesia
  • Dosing Information
  • As a sedative when used as premedication and following general anesthesia, Hydroxyzine may potentiate meperidine (Demerol®) and barbiturates, so their use in pre-anesthetic adjunctive therapy should be modified on an individual basis. Atropine and other belladonna alkaloids are not affected by the drug. Hydroxyzine is not known to interfere with the action of digitalis in any way and it may be used concurrently with this agent.
  • As a sedative when used as a premedication and following general anesthesia: 50–100 mg in adults.


|offLabelAdultGuideSupport=There is limited information regarding Off-Label Guideline-Supported Use of Hydroxyzine (injection) in adult patients.

|offLabelAdultNoGuideSupport======Seasonal allergic rhinitis=====

  • Dosing Information


|fdaLIADPed======Symptomatic relief of anxiety=====

  • Dosing Information
  • For symptomatic relief of anxiety and tension associated with psychoneurosis and as an adjunct in organic disease states in which anxiety is manifested: children under 6 years, 50 mg daily in divided doses and over 6 years, 50–100 mg daily in divided doses.
Chronic Urticaria
  • Dosing Information
  • For use in the management of pruritus due to allergic conditions such as chronic urticaria and atopic and contact dermatoses, and in histamine-mediated pruritus: children under 6 years, 50 mg daily in divided doses and over 6 years, 50–100 mg daily in divided doses.
Sedative when used as premedication and following general anesthesia
  • Dosing Information
  • As a sedative when used as premedication and following general anesthesia, Hydroxyzine may potentiate meperidine (Demerol®) and barbiturates, so their use in pre-anesthetic adjunctive therapy should be modified on an individual basis. Atropine and other belladonna alkaloids are not affected by the drug. Hydroxyzine is not known to interfere with the action of digitalis in any way and it may be used concurrently with this agent.
  • As a sedative when used as a premedication and following general anesthesia: 0.6 mg/kg in children.


|offLabelPedGuideSupport=There is limited information regarding Off-Label Guideline-Supported Use of Hydroxyzine (injection) in pediatric patients.

|offLabelPedNoGuideSupport=There is limited information regarding Off-Label Non-Guideline-Supported Use of Hydroxyzine (injection) in pediatric patients.

|contraindications=*Hydroxyzine, when administered to the pregnant mouse, rat, and rabbit, induced fetal abnormalities in the rat and mouse at doses substantially above the human therapeutic range. Clinical data in human beings are inadequate to establish safety in early pregnancy. Until such data are available, hydroxyzine is contraindicated in early pregnancy.

  • Hydroxyzine is contraindicated for patients who have shown a previous hypersensitivity to it.

|warnings=====Precautions====

  • THE POTENTIATING ACTION OF HYDROXYZINE MUST BE CONSIDERED WHEN THE DRUG IS USED IN CONJUNCTION WITH CENTRAL NERVOUS SYSTEM DEPRESSANTS SUCH AS NARCOTICS, NON-NARCOTIC ANALGESICS AND BARBITURATES. Therefore when central nervous system depressants are administered concomitantly with hydroxyzine their dosage should be reduced.
  • Since drowsiness may occur with use of this drug, patients should be warned of this possibility and cautioned against driving a car or operating dangerous machinery while taking Atarax. Patients should be advised against the simultaneous use of other CNS depressant drugs, and cautioned that the effect of alcohol may be increased.


|clinicalTrials=*Side effects reported with the administration of Atarax (hydroxyzine hydrochloride) are usually mild and transitory in nature.

  • Anticholinergic
  • Central Nervous System
  • Drowsiness is usually transitory and may disappear in a few days of continued therapy or upon reduction of the dose. Involuntary motor activity including rare instances of tremor and convulsions have been reported, usually with doses considerably higher than those recommended. Clinically significant respiratory depression has not been reported at recommended doses.

|postmarketing=There is limited information regarding Postmarketing Experience of Hydroxyzine (injection) in the drug label.

|drugInteractions= |useInPregnancyFDA=* Pregnancy Category |useInPregnancyAUS=* Australian Drug Evaluation Committee (ADEC) Pregnancy Category

There is no Australian Drug Evaluation Committee (ADEC) guidance on usage of Hydroxyzine (injection) in women who are pregnant. |useInLaborDelivery=There is no FDA guidance on use of Hydroxyzine (injection) during labor and delivery. |useInNursing=*It is not known whether this drug is excreted in human milk. Since many drugs are so excreted, hydroxyzine should not be given to nursing mothers. |useInPed=There is no FDA guidance on the use of Hydroxyzine (injection) with respect to pediatric patients. |useInGeri=*A determination has not been made whether controlled clinical studies of ATARAX included sufficient numbers of subjects aged 65 and over to define a difference in response from younger subjects. Other reported clinical experience has not identified differences in responses between the elderly and younger patients. In general, dose selection for an elderly patient should be cautious, usually starting at the low end of the dosing range, reflecting the greater frequency of decreased hepatic, renal or cardiac function, and of concomitant disease or other drug therapy.

  • The extent of renal excretion of ATARAX has not been determined. Because elderly patients are more likely to have decreased renal function, care should be taken in dose selections.
  • Sedating drugs may cause confusion and over sedation in the elderly; elderly patients generally should be started on low doses of ATARAX and observed closely.

|useInGender=There is no FDA guidance on the use of Hydroxyzine (injection) with respect to specific gender populations. |useInRace=There is no FDA guidance on the use of Hydroxyzine (injection) with respect to specific racial populations. |useInRenalImpair=There is no FDA guidance on the use of Hydroxyzine (injection) in patients with renal impairment. |useInHepaticImpair=There is no FDA guidance on the use of Hydroxyzine (injection) in patients with hepatic impairment. |useInReproPotential=There is no FDA guidance on the use of Hydroxyzine (injection) in women of reproductive potentials and males. |useInImmunocomp=There is no FDA guidance one the use of Hydroxyzine (injection) in patients who are immunocompromised.

|administration=* Oral |monitoring=There is limited information regarding Monitoring of Hydroxyzine (injection) in the drug label.

|IVCompat=There is limited information regarding IV Compatibility of Hydroxyzine (injection) in the drug label.

|overdose====Acute Overdose===

Signs and Symptoms

  • The most common manifestation of Atarax overdosage is hypersedation. As in the management of overdosage with any drug, it should be borne in mind that multiple agents may have been taken.
  • If vomiting has not occurred spontaneously, it should be induced. Immediate gastric lavage is also recommended. General supportive care, including frequent monitoring of the vital signs and close observation of the patient, is indicated. Hypotension, though unlikely, may be controlled with intravenous fluids and Levophed® (levarterenol), or Aramine® (metaraminol). Do not use epinephrine as Atarax counteracts its pressor action.

Management

  • There is no specific antidote. It is doubtful that hemodialysis would be of any value in the treatment of overdosage with hydroxyzine. However, if other agents such as barbiturates have been ingested concomitantly, hemodialysis may be indicated. There is no practical method to quantitate hydroxyzine in body fluids or tissue after its ingestion or administration.

Chronic Overdose

There is limited information regarding Chronic Overdose of Hydroxyzine (injection) in the drug label.


|drugBox={{Drugbox2 | verifiedrevid = 461774177 | IUPAC_name = (±)-2-(2-{4-[(4-chlorophenyl)-phenylmethyl]piperazin-1-yl}ethoxy)ethanol | image = Hydroxyzine.png | image2 = Hydroxyzine-3d-sticks.png

| tradename = Vistaril | Drugs.com = Monograph | MedlinePlus = a682866 | pregnancy_AU = A | pregnancy_US = C | legal_AU = S4 | legal_status = Rx-only | routes_of_administration = Oral, IM

| bioavailability = High in-vivo | protein_bound = 93% | metabolism = Hepatic | elimination_half-life = 20–24 hours[1] | excretion = Urine, Feces

| CASNo_Ref =  ☑Y | CAS_number_Ref =  ☑Y | CAS_number = 68-88-2 | ATC_prefix = N05 | ATC_suffix = BB01 | PubChem = 3658 | DrugBank_Ref =  ☑Y

| DrugBank = DB00557

| ChemSpiderID_Ref =  ☑Y | ChemSpiderID = 3531 | UNII_Ref =  ☑Y | UNII = 30S50YM8OG | KEGG_Ref =  ☑Y | KEGG = D08054 | ChEBI_Ref =  ☑Y | ChEBI = 5818 | ChEMBL_Ref =  ☑Y | ChEMBL = 896

| C = 21 | H = 27 | Cl = 1 | N = 2 | O = 2

| molecular_weight = 374.904 g/mol | smiles = Clc1ccc(cc1)C(c2ccccc2)N3CCN(CC3)CCOCCO | InChI = 1/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 | InChIKey = ZQDWXGKKHFNSQK-UHFFFAOYAL | StdInChI_Ref =  ☑Y | StdInChI = 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 | StdInChIKey_Ref =  ☑Y | StdInChIKey = ZQDWXGKKHFNSQK-UHFFFAOYSA-N }}

|mechAction=* Atarax is unrelated chemically to the phenothiazines, reserpine, meprobamate, or the benzodiazepines.

  • Atarax is not a cortical depressant, but its action may be due to a suppression of activity in certain key regions of the subcortical area of the central nervous system. Primary skeletal muscle relaxation has been demonstrated experimentally. Bronchodilator activity, and anti- histaminic and analgesic effects have been demonstrated experimentally and confirmed clinically. An antiemetic effect, both by the apomorphine test and the veriloid test, has been demonstrated. Pharmacological and clinical studies indicate that hydroxyzine in therapeutic dosage does not increase gastric secretion or acidity and in most cases has mild antisecretory activity. Hydroxyzine is rapidly absorbed from the gastrointestinal tract and Atarax's clinical effects are usually noted within 15 to 30 minutes after oral administration.

|structure=* Hydroxyzine hydrochloride is designated chemically as 1-(p-chlorobenzhydryl) 4-[2-(2-hydroxyethoxy)-ethyl] piperazine dihydrochloride.

  • Inert ingredients for the tablets are: acacia; carnauba wax; dibasic calcium phosphate; gelatin; lactose; magnesium stearate; precipitated calcium carbonate; shellac; sucrose; talc; white wax. The 10 mg tablets also contain: sodium hydroxide; starch; titanium dioxide; Yellow 6 Lake. The 25 mg tablets also contain: starch; velo dark green. The 50 mg tablets also contain: starch; velo yellow. The 100 mg tablets also contain: alginic acid; Blue 1; polyethylene glycol; Red 3.
  • The inert ingredients for the syrup are: alcohol; menthol; peppermint oil; sodium benzoate; spearmint oil; sucrose; water.

|PD=There is limited information regarding Pharmacodynamics of Hydroxyzine (injection) in the drug label.

|PK=There is limited information regarding Pharmacokinetics of Hydroxyzine (injection) in the drug label.

|nonClinToxic=There is limited information regarding Nonclinical Toxicology of Hydroxyzine (injection) in the drug label.

|clinicalStudies=There is limited information regarding Clinical Studies of Hydroxyzine (injection) in the drug label.

|howSupplied=* Atarax Tablets

  • 10 mg–orange tablets
    • 100's (NDC 0049-5600-66)
  • 25 mg–green tablets
    • 100's (NDC 0049-5610-66),
    • 500's (NDC 0049-5610-73)
  • 50 mg–yellow tablets
    • 100's (NDC 0049-5620-66)
  • Atarax 100 Tablets
  • 100 mg–red tablets
    • 100's (NDC 0049-5630-66)
  • Atarax Syrup
  • 10 mg per teaspoon (5 ml)
    • 1 pint bottles (NDC 0049-5590-93)
    • Alcohol Content–Ethyl Alcohol–0.5% v/v

|packLabel=

This image is provided by the National Library of Medicine.
This image is provided by the National Library of Medicine.

|fdaPatientInfo=There is limited information regarding Patient Counseling Information of Hydroxyzine (injection) in the drug label.

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  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.
  2. "ATARAX- hydroxyzine hydrochloride tablet ATARAX- hydroxyzine hydrochloride syrup".