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Pronunciation
(hye DROKS i zeen)
Generic Available (U.S.)
Yes
Index Terms
U.S. Brand Names
Canadian Brand Names
Pharmacologic Category
Pharmacologic Category Synonyms
Use: Labeled Indications
Treatment of anxiety/agitation (including adjunctive therapy in alcoholism); adjunct to pre- and postoperative analgesia and anesthesia; antipruritic; antiemetic
Use: Dental
Treatment of anxiety, as a preoperative sedative in pediatric dentistry
Pregnancy Considerations
Hydroxyzine-induced fetal abnormalities were observed at high dosages in animal studies. Neonatal withdrawal symptoms have been reported following long-term maternal use or the use of large doses near term. Use in early pregnancy is contraindicated by the manufacturer.
Lactation
Excretion in breast milk unknown/not recommended
Contraindications
Hypersensitivity to hydroxyzine or any component of the formulation; early pregnancy; SubQ, intra-arterial, or I.V. injection
Warnings/Precautions
Concerns related to adverse effects:
• CNS depression: May cause CNS depression, which may impair physical or mental abilities; patients must be cautioned about performing tasks which require mental alertness (eg, operating machinery or driving).
Disease-related concerns:
• Glaucoma: Use with caution in patients with narrow-angle glaucoma; condition may be exacerbated by cholinergic blockade. Screening is recommended.
• Prostatic hyperplasia/urinary stricture: Use with caution in patients with prostatic hyperplasia and/or urinary stricture.
• Respiratory disease: Use with caution in patients with asthma or COPD.
Concurrent drug therapy issues:
• Sedatives: Effects may be potentiated when used with other sedative drugs or ethanol.
Special populations:
• Elderly: May be inappropriate in this age group due to potent anticholinergic effects; nonanticholinergic antihistamines preferred for treating allergic reactions (Beers Criteria).
Other warnings/precautions:
• Appropriate administration: I.V., SubQ, and intra-arterial administration are contraindicated since tissue damage, intravascular hemolysis, thrombosis, and digital gangrene can occur.
Adverse Reactions
Frequency not defined.
Central nervous system: Dizziness, drowsiness, fatigue, hallucination, headache, nervousness, seizure
Dermatologic: Pruritus, rash, urticaria
Gastrointestinal: Xerostomia
Neuromuscular & skeletal: Involuntary movements, paresthesia, tremor
Ocular: Blurred vision
Respiratory: Respiratory depression (at higher than recommended doses)
Miscellaneous: Allergic reaction
Metabolism/Transport Effects
Inhibits CYP2D6 (weak)
Drug Interactions
Acetylcholinesterase Inhibitors (Central): Anticholinergics may diminish the therapeutic effect of Acetylcholinesterase Inhibitors (Central). Acetylcholinesterase Inhibitors (Central) may diminish the therapeutic effect of Anticholinergics. If the anticholinergic action is a side effect of the agent, the result may be beneficial. Risk C: Monitor therapy
Alcohol (Ethyl): CNS Depressants may enhance the CNS depressant effect of Alcohol (Ethyl). Risk C: Monitor therapy
Amphetamines: May diminish the sedative effect of Antihistamines. Risk C: Monitor therapy
Anticholinergics: May enhance the adverse/toxic effect of other Anticholinergics. Exceptions: Levocabastine (Nasal); Paliperidone. Risk C: Monitor therapy
Barbiturates: HydrOXYzine may enhance the CNS depressant effect of Barbiturates. Management: Consider a decrease in the barbiturate dose, as appropriate, when used together with hydroxyzine. With concurrent use, monitor patients closely for excessive response to the combination. Risk D: Consider therapy modification
Benzylpenicilloyl Polylysine: Antihistamines may diminish the diagnostic effect of Benzylpenicilloyl Polylysine. Management: Suspend systemic H1 antagonists for benzylpenicilloyl-polylysine skin testing and delay testing until systemic antihistaminic effects have dissipated. A histamine skin test may be used to assess persistent antihistaminic effects. Risk D: Consider therapy modification
Betahistine: Antihistamines may diminish the therapeutic effect of Betahistine. Risk C: Monitor therapy
CNS Depressants: HydrOXYzine may enhance the CNS depressant effect of CNS Depressants. Management: For patients being treated with hydroxyzine, a reduction in the dose of any other CNS depressants that are to be used in combination is recommended. With concurrent use, monitor patients closely for excessive response to the combination. Risk D: Consider therapy modification
Droperidol: May enhance the CNS depressant effect of CNS Depressants. Management: Consider dose reductions of droperidol or of other CNS agents (e.g., opioids, barbiturates) with concomitant use. Risk D: Consider therapy modification
Meperidine: HydrOXYzine may enhance the CNS depressant effect of Meperidine. Management: Consider a decrease in meperidine dose, as appropriate, when used together with hydroxyzine. With concurrent use, monitor patients closely for excessive response to the combination. Risk D: Consider therapy modification
Pramlintide: May enhance the anticholinergic effect of Anticholinergics. These effects are specific to the GI tract. Risk D: Consider therapy modification
Selective Serotonin Reuptake Inhibitors: CNS Depressants may enhance the adverse/toxic effect of Selective Serotonin Reuptake Inhibitors. Specifically, the risk of psychomotor impairment may be enhanced. Risk C: Monitor therapy
Ethanol/Nutrition/Herb Interactions
Ethanol: May increase CNS depression; monitor for increased effects with coadministration. Caution patients about effects.
Herb/Nutraceutical: Avoid valerian, St John's wort, kava kava, gotu kola (may increase CNS depression).
Storage
Injection: Store at 20°C to 25°C (68°F to 77°F); excursions permitted to 15°C to 30°C (59°F to 86°F). Protect from light.
Tablets: Store at 20°C to 25°C (68°F to 77°F).
Compatibility
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, promethazine, scopolamine, sufentanil. Incompatible: Dimenhydrinate, haloperidol, ketorolac, pentobarbital, ranitidine.
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: Oral: 15-30 minutes; Injection: Rapid
Duration: Decreased histamine-induced wheal and flare areas: 2 to ≥36 hours; Suppression of pruritus: 1-12 hours (Simons, 1984)
Absorption: Oral: Rapid
Distribution: Adults: Vd ~16 L/kg (Simons, 1984); Elderly: ~23 L/kg (Simons K, 1989); Hepatic dysfunction: ~23 L/kg (Simons F, 1989)
Metabolism: Hepatic to multiple metabolites, including cetirizine (active) (Simons F, 1989)
Half-life elimination: Adults: ~20 hours (Simons, 1984); Elderly: ~29 hours (Simons K, 1989); Hepatic dysfunction: ~37 hours (Simons F, 1989)
Time to peak: Oral administration: Serum: ~2 hours; Peak suppression of antihistamine-induced wheal and flare: 4-12 hours (Simons, 1984)
Excretion: Urine
Dosage
Note: Adjust dose based on patient response.
Children:
Preoperative sedation:
Oral: 0.6 mg/kg/dose
I.M.: 1.1 mg/kg/dose
Pruritus, anxiety: Oral:
<6 years: 50 mg daily in divided doses
≥6 years: 50-100 mg daily in divided doses
Antiemetic: I.M.: 1.1 mg/kg/dose
Adults:
Antiemetic: I.M.: 25-100 mg/dose
Anxiety:
Oral: 50-100 mg 4 times/day
I.M.: Initial: 50-100 mg, then every 4-6 hours as needed
Preoperative sedation:
Oral: 50-100 mg
I.M.: 25-100 mg
Pruritus: Oral: 25 mg 3-4 times/day
Elderly: Initiate dosing using the lower end of the recommended dosage range due to an increased potential for anticholinergic side effects. Refer to adult dosing.
Dosing interval in hepatic impairment: Change dosing interval to every 24 hours in patients with primary biliary cirrhosis (Simons F, 1989).
Dental Usual Dosing
Anxiety: Adults: Oral: 50-100 mg 4 times/day
Preoperative sedation:
Children:
Oral: 0.6 mg/kg/dose
I.M.: 0.5-1 mg/kg/dose
Adults:
Oral: 50-100 mg
I.M.: 25-100 mg
Administration: Oral
Shake suspension vigorously prior to use.
Administration: I.M.
For I. M. use only. Do not administer I.V., SubQ, or intra-arterially. Administer I.M. deep in large muscle. In adults, the preferred site is the upper outer quadrant of the buttock or midlateral thigh. In children, the preferred site is the midlateral thigh. The upper outer quadrant of the gluteal region should be used only when necessary to minimize potential damage to the sciatic nerve. With I.V. administration, extravasation can result in sterile abscess and marked tissue induration.
Administration: I.V.
Extravasation can result in sterile abscess and marked tissue induration.
Administration: I.V. Detail
pH: 3.5-6.0
Monitoring Parameters
Relief of symptoms, mental status, blood pressure
Test Interactions
May cause false-positive serum TCA screen.
Patient Education
Will cause drowsiness. Do not use alcohol. Report hallucinations, seizure activity, tremors or involuntary movements, or loss of sensation.
Geriatric Considerations
Anticholinergic effects are not well tolerated in the elderly and frequently result in bowel, bladder, and mental status changes (ie, constipation, confusion, and urinary retention). Hydroxyzine may be useful as a short-term antipruritic, but it is not recommended for use as a sedative or anxiolytic in the elderly.
This medication is considered to be potentially inappropriate in this patient population (Beers Criteria severity: High).
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
Mental Health: Comment
Commonly used as an anxiolytic, especially in individuals with a history of or active substance use. Postmarketing experience revealed cases of headache and hallucinations.
Nursing: Physical Assessment/Monitoring
Institute precautions to prevent falls.
Dosage Forms
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Capsule, oral, as pamoate: 25 mg, 50 mg, 100 mg
Vistaril®: 25 mg, 50 mg
Injection, solution, as hydrochloride: 25 mg/mL (1 mL); 50 mg/mL (1 mL, 2 mL, 10 mL)
Solution, oral, as hydrochloride: 10 mg/5 mL (473 mL)
Syrup, oral, as hydrochloride: 10 mg/5 mL (118 mL, 473 mL)
Tablet, oral, as hydrochloride: 10 mg, 25 mg, 50 mg
Pricing: U.S. (www.drugstore.com)
Capsules (HydrOXYzine Pamoate)
25 mg (60): $14.98
100 mg (30): $19.99
Capsules (Vistaril)
25 mg (30): $55.64
50 mg (30): $64.04
Solution (HydrOXYzine HCl)
50 mg/mL (25): $44.38
Tablets (HydrOXYzine HCl)
10 mg (30): $17.99
50 mg (30): $30.99
References
Baumgartner T, “Administration of Hydroxyzine Injection,” Am J Hosp Pharm, 1979, 36(12):1660.
Dasgupta A, Wells A, and Datta P, “False-Positive Serum Tricyclic Antidepressant Concentrations Using Fluorescence Polarization Immunoassay due to the Presence of Hydroxyzine and Cetirizine,” Ther Drug Monit, 2007, 29(1):134-9.
Serreau R, Komiha M, Blanc F, et al, “Neonatal Seizures Associated With Maternal Hydroxyzine Hydrochloride in Late Pregnancy,” Reprod Toxicol, 2005, 20(4):573-4.
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 FE, Watson WT, Chen XY, et al, “The Pharmacokinetics and Pharmacodynamics of Hydroxyzine in Patients With Primary Biliary Cirrhosis,” J Clin Pharmacol, 1989, 29(9):809-15.
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.
International Brand Names
Lexi-Comp.com
Last full review/revision May 2011
Content last modified May 2011
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