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Hydroxyzine
Pronunciation
U.S. Brand Names
Generic Available
Canadian Brand Names
Synonyms
Pharmacological Index
Use
Pregnancy Risk Factor
Contraindications
Warnings/Precautions
Adverse Reactions
Overdosage/Toxicology
Drug Interactions
Stability
Mechanism of Action
Pharmacodynamics/Kinetics
Usual Dosage
Dietary Considerations
Monitoring Parameters
Dental Health: Local Anesthetic/Vasoconstrictor Precautions
Dental Health: Effects on Dental Treatment
Patient Information
Nursing Implications
Dosage Forms
References

Pronunciation
(hye DROKS i zeen)

U.S. Brand Names
Anxanil®; Atarax®; Hyzine-50®; QYS®; Vistacon®; Vistaquel®; Vistaril®; Vistazine®

Generic Available

Yes


Canadian Brand Names
Apo®-Hydroxyzine; Multipax®; Novo-Hydroxyzin; PMS-Hydroxyzine

Synonyms
Hydroxyzine Hydrochloride; Hydroxyzine Pamoate

Pharmacological Index

Antiemetic; Antihistamine


Use

Dental: Treatment of anxiety, as a preoperative sedative in pediatric dentistry

Medical: Treatment of anxiety; as a preoperative sedative; as an antipruritic

Unlabeled uses: Antiemetic; alcohol withdrawal symptoms


Pregnancy Risk Factor

C


Contraindications

Hypersensitivity to hydroxyzine or any component


Warnings/Precautions

Causes sedation, caution must be used in performing tasks which require alertness (ie, operating machinery or driving). Sedative effects of CNS depressants or ethanol are potentiated. S.C., 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 hypertrophy, and bladder neck obstruction; should also be used with caution in patients with asthma or COPD.


Adverse Reactions

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

Respiratory: Thickening of bronchial secretions

Gastrointestinal: Xerostomia

Neuromuscular & skeletal: Tremor, paresthesia, seizure

Ocular: Blurred vision


Overdosage/Toxicology

Symptoms of overdose include seizures, sedation, hypotension

There is no specific treatment for an antihistamine overdose, however, most of its clinical toxicity is due to anticholinergic effects. Anticholinesterase inhibitors may be useful by reducing acetylcholinesterase. For anticholinergic overdose with severe life-threatening symptoms, physostigmine 1-2 mg (0.5 mg or 0.02 mg/kg for children) I.V., slowly may be given to reverse these effects.


Drug Interactions

CNS depressants, anticholinergics, used in combination with hydroxyzine may result in additive effects


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


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 effect: Within 15-30 minutes

Duration: 4-6 hours

Absorption: Oral: Rapid

Metabolism: Exact fate is unknown

Half-life: 3-7 hours

Time to peak serum concentration: Within 2 hours


Usual Dosage

Children:

Oral: 0.6 mg/kg/dose every 6 hours

I.M.: 0.5-1 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


Dietary Considerations

Alcohol: Additive CNS effect, avoid use


Monitoring Parameters

Relief of symptoms, mental status, blood pressure


Dental Health: Local Anesthetic/Vasoconstrictor Precautions

No information available to require special precautions


Dental Health: Effects on Dental Treatment

1% to 10% of patients experience dry mouth


Patient Information

Take this drug as prescribed; do not increase dosage or discontinue without consulting prescriber. Store medication away from light. Maintain adequate hydration (2-3 L/day of fluids unless instructed to restrict fluid intake). Void before taking medication. Do not use excessive alcohol or other CNS depressants or sleeping aids without consulting prescriber. May cause dizziness, drowsiness, or blurred vision (use caution when driving or engaging in tasks requiring alertness until response to drug is known); or nausea, dry mouth, appetite disturbances (small frequent meals, frequent mouth care, or sucking hard candy may help). Report unusual weight gain, unresolved nausea or diarrhea, chest pain or palpitations, muscle or joint pain, excess sedation, sore throat, or difficulty breathing. Pregnancy/breast-feeding precautions: Inform prescriber if you are or intend to be pregnant. Consult prescriber if breast-feeding.


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


Dosage Forms

Hydroxyzine hydrochloride:

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

Syrup: 10 mg/5 mL (120 mL, 480 mL, 4000 mL)

Tablet: 10 mg, 25 mg, 50 mg, 100 mg

Hydroxyzine pamoate:

Capsule: 25 mg, 50 mg, 100 mg

Suspension, oral: 25 mg/5 mL (120 mL, 480 mL)


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.

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.


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