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HydrOXYzine


Pronunciation

(hye DROKS i zeen)


U.S. Brand Names

Atarax®; Vistaril®


Synonyms

Hydroxyzine Hydrochloride; Hydroxyzine Pamoate


Generic Available

Yes


Canadian Brand Names

Apo-Hydroxyzine®; Atarax®; Novo-Hydroxyzin; PMS-Hydroxyzine; Vistaril®


Use

Treatment of anxiety; preoperative sedative; antipruritic


Use - Dental

Treatment of anxiety, as a preoperative sedative in pediatric dentistry


Use - Unlabeled/Investigational

Antiemetic; ethanol withdrawal symptoms


Pregnancy Risk Factor

C


Lactation

Enters breast milk/contraindicated


Contraindications

Hypersensitivity to hydroxyzine or any component of the formulation


Warnings/Precautions

Causes sedation, caution must be used in performing tasks which require alertness (eg, operating machinery or driving). Sedative effects of CNS depressants or ethanol are potentiated. SubQ, intra-arterial, and I.V. administration are not recommended since thrombosis and digital gangrene can occur; extravasation can result in sterile abscess and marked tissue induration; should be used with caution in patients with narrow-angle glaucoma, prostatic hyperplasia, and bladder neck obstruction; should also be used with caution in patients with asthma or COPD.

Anticholinergic effects are not well tolerated in the elderly. Hydroxyzine may be useful as a short-term antipruritic, but it is not recommended for use as a sedative or anxiolytic in the elderly.


Adverse Reactions

Central nervous system: Drowsiness, headache, fatigue, nervousness, dizziness

Gastrointestinal: Xerostomia

Neuromuscular & skeletal: Tremor, paresthesia, seizure

Ocular: Blurred vision

Respiratory: Thickening of bronchial secretions


Overdosage/Toxicology

Symptoms of overdose include seizures, sedation, and hypotension. There is no specific treatment for antihistamine overdose. Clinical toxicity is due to blockade of cholinergic receptors. For anticholinergic overdose with severe life-threatening symptoms, physostigmine 1-2 mg I.V. slowly, may be given to reverse these effects.


Drug Interactions

Inhibits CYP2D6 (weak)

Amantadine, rimantadine: Central and/or peripheral anticholinergic syndrome can occur when administered with amantadine or rimantadine

Anticholinergic agents: Central and/or peripheral anticholinergic syndrome can occur when administered with narcotic analgesics, phenothiazines and other antipsychotics (especially with high anticholinergic activity), tricyclic antidepressants, quinidine and some other antiarrhythmics, and antihistamines

Antipsychotics: Hydroxyzine may antagonize the therapeutic effects of antipsychotics

CNS depressants: Sedative effects of hydroxyzine may be additive with CNS depressants; includes ethanol, benzodiazepines, barbiturates, narcotic analgesics, and other sedative agents; monitor for increased effect


Ethanol/Nutrition/Herb Interactions

Ethanol: Avoid ethanol (may increase CNS depression).

Herb/Nutraceutical: Avoid valerian, St John's wort, kava kava, gotu kola (may increase CNS depression).


Stability

Protect from light; store at 15°C to 30°C and protected from freezing; I.V. is incompatible when mixed with aminophylline, amobarbital, chloramphenicol, dimenhydrinate, heparin, penicillin G, pentobarbital, phenobarbital, phenytoin, ranitidine, sulfisoxazole, vitamin B complex with C


Compatibility

Y-site administration: Compatible: Aztreonam, ciprofloxacin, cisatracurium, cladribine, docetaxel, etoposide phosphate, famotidine, filgrastim, foscarnet, gatifloxacin, gemcitabine, granisetron, linezolid, melphalan, ondansetron, propofol, remifentanil, sufentanil, teniposide, thiotepa, vinorelbine. Incompatible: Allopurinol, amifostine, amphotericin B cholesteryl sulfate complex, cefepime, doxorubicin liposome, fluconazole, fludarabine, paclitaxel, piperacillin/tazobactam, sargramostim

Compatibility in syringe: Compatible: Atropine, atropine with meperidine, butorphanol, chlorpromazine, cimetidine, codeine, diphenhydramine, doxapram, droperidol, fentanyl, fluphenazine, glycopyrrolate, hydromorphone, lidocaine, meperidine, methotrimeprazine, metoclopramide, midazolam, morphine, nalbuphine, oxymorphone, pentazocine, perphenazine, procaine, prochlorperazine edisylate, promazine, promethazine, scopolamine, sufentanil. Incompatible: Dimenhydrinate, haloperidol, ketorolac, pentobarbital, ranitidine

Compatibility when admixed: Compatible: Cisplatin, cyclophosphamide, cytarabine, dimenhydrinate, etoposide, lidocaine, mesna, methotrexate, nafcillin. Incompatible: Aminophylline, amobarbital, chloramphenicol, penicillin G potassium, penicillin G sodium, pentobarbital, phenobarbital


Mechanism of Action

Competes with histamine for H1-receptor sites on effector cells in the gastrointestinal tract, blood vessels, and respiratory tract. Possesses skeletal muscle relaxing, bronchodilator, antihistamine, antiemetic, and analgesic properties.


Pharmacodynamics/Kinetics

Onset of action: 15-30 minutes

Duration: 4-6 hours

Absorption: Oral: Rapid

Metabolism: Exact fate unknown

Half-life elimination: 3-7 hours

Time to peak: ~2 hours


Dosage

Children:

Oral: 0.6 mg/kg/dose every 6 hours

I.M.: 0.5-1.1 mg/kg/dose every 4-6 hours as needed

Adults:

Antiemetic: I.M.: 25-100 mg/dose every 4-6 hours as needed

Anxiety: Oral: 25-100 mg 4 times/day; maximum dose: 600 mg/day

Preoperative sedation:

Oral: 50-100 mg

I.M.: 25-100 mg

Management of pruritus: Oral: 25 mg 3-4 times/day

Dosing interval in hepatic impairment: Change dosing interval to every 24 hours in patients with primary biliary cirrhosis


Administration

For I.M. administration in children, injections should be made into the midlateral muscles of the thigh; SubQ, intra-arterial, and I.V. administration not recommended since thrombosis and digital gangrene can occur


Monitoring Parameters

Relief of symptoms, mental status, blood pressure


Patient Education

Will cause drowsiness, avoid alcohol and other CNS depressants. Avoid driving and other hazardous tasks until the CNS effects are known. Pregnancy/breast-feeding precautions: Inform prescriber if you are or intend to become pregnant. Do not breast-feed.


Nursing Implications

Extravasation can result in sterile abscess and marked tissue induration; provide safety measures (ie, side rails, night light, and call button); remove smoking materials from area; supervise ambulation


Additional Information

Hydroxyzine hydrochloride: Atarax®, Vistaril® injection

Hydroxyzine pamoate: Vistaril® capsule and suspension


Dental Health: Effects on Dental Treatment

Key adverse event(s) related to dental treatment: Xerostomia (normal salivary flow resumes upon discontinuation).


Dental Health: Vasoconstrictor/Local Anesthetic Precautions

No information available to require special precautions


Oncology: Emetic Potential

Very low (<10%)


Oncology: Vesicant

No; may be an irritant


Dosage Forms

[DSC] = Discontinued product

Capsule, as pamoate (Vistaril®): 25 mg, 50 mg, 100 mg

Injection, solution, as hydrochloride: 25 mg/mL (1 mL); 50 mg/mL (1 mL, 2 mL, 10 mL)

Suspension, oral, as pamoate (Vistaril®): 25 mg/5 mL (120 mL, 480 mL) [lemon flavor]

Syrup, as hydrochloride: 10 mg/5 mL (120 mL, 480 mL)

Atarax®: 10 mg/5 mL (480 mL) [contains alcohol, sodium benzoate; mint flavor] [DSC]

Tablet, as hydrochloride: 10 mg, 25 mg, 50 mg

Atarax®: 10 mg, 25 mg, 50 mg, 100 mg [DSC]


References

Hollister LE, "Hydroxyzine Hydrochloride: Possible Adverse Cardiac Interactions," Psychopharmacol Comm , 1971, 1:61-5.

McKenzie R, Wadhwa RK, Uy NT, et al, "Antiemetic Effectiveness of Intramuscular Hydroxyzine Compared With Intramuscular Droperidol," Anesth Analg , 1981, 60(11):783-8.

Paton DM and Webster DR, "Clinical Pharmacokinetics of H1-Receptor Antagonists (The Antihistamines)," Clin Pharmacokinet , 1985, 10(6):477-97.

Prenner BM, "Neonatal Withdrawal Syndrome Associated With Hydroxyzine Hydrochloride," Am J Dis Child , 1977, 131:529-30.

Simons FE, Simons KJ, and Frith EM, "The Pharmacokinetics and Antihistaminic of the H1 Receptor Antagonist Hydroxyzine," J Allergy Clin Immunol , 1984, 73(1 Pt 1):69-75.

Simons KJ, Watson WT, Chen XY, et al, "Pharmacokinetic and Pharmacodynamic Studies of the H1-Receptor Antagonist Hydroxyzine in the Elderly," Clin Pharmacol Ther , 1989, 45(1):9-14.

Snow JC, "Hydroxyzine for Postoperative Nausea and Vomiting Following Ophthalmologic Surgery," Anesth Analg , 1965, 44(5):487-91.

Tornetta FJ, "A Comparison of Droperidol, Diazepam, and Hydroxyzine Hydrochloride as Premedication," Anesth Analg , 1977, 56(4):496-500.

Tsukuda M, Furukawa S, Kokatsu T, et al, "Comparison of Granisetron Alone and Granisetron Plus Hydroxyzine Hydrochloride for Prophylactic Treatment of Emesis Induced by Cisplatin Chemotherapy," Eur J Cancer , 1995, 31A(10):1647-9.


International Brand Names

Abacus® (TH); AH 3® (DE); Antizine® (TH); Apo-Hydroxyzine® (CA, SG); Atano® (TH); Atarax® (AT, BE, CA, CH, CZ, DE, DK, DO, ES, FI, FR, GB, HK, HU, IN, IT, LU, NL, NO, PL, PT, RO, RU, SE, SG, TH, TR); Aterax® (ZA); Bestalin® (ID); Cedar® (CO); Cerax® (TH); Dalun® (CL); Darax® (TH); Disron® (JP); Dormirex® (CO); Drazine® (TH); Elroquil N® (DE); Fasarax® (CL); Fedox® (CL); Hadarax® (TH); Hiderax® (CO); Hidroxina® (AR); Hidroxizin® (RO); Histan® (TH); Hizin® (TH); Honsa® (TH); Hyderax® (AR); Hydroksyzyna® (PL); Hydroxin® (TH); Hydroxyzine Renaudin® (FR); Hydroxyzinum® (PL); Iterax® (ID); Masarax® (TH); Med-Xyzarax® (TH); Navicalm® (NL); Nexit® (CL); Novo-Hydroxyzin (CA); Otarex® (IL); Phymorax® (SG); PMS-Hydroxyzine (CA); Postarax® (TH); Prurizin® (BR); Q-Med Hydroxyzine® (ZA); R-Rax® (TH); Serecid® (NZ); Taraxin® (TH); Trandrozine® (TH); Ucerax® (GB); Vistaril® (CA, TR)


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