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Cetirizine

Pronunciation

Pronunciation

(se TI ra zeen)

Index Terms

  • Cetirizine Hydrochloride
  • P-071
  • UCB-P071

Dosage Forms

Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product

Capsule, Oral, as hydrochloride:

ZyrTEC Allergy: 10 mg

Solution, Oral, as hydrochloride:

All Day Allergy Childrens: 5 mg/5 mL (118 mL) [contains methylparaben, propylene glycol, propylparaben]

All Day Allergy Childrens: 5 mg/5 mL (118 mL) [dye free, gluten free; contains methylparaben, propylene glycol, propylparaben; grape flavor]

All Day Allergy Childrens: 1 mg/mL (118 mL [DSC]) [dye free, gluten free, sugar free; contains propylene glycol, sodium benzoate; grape flavor]

Cetirizine HCl Allergy Child: 5 mg/5 mL (120 mL) [alcohol free, dye free, gluten free, sugar free; contains methylparaben, propylene glycol, propylparaben; grape flavor]

Cetirizine HCl Allergy Child: 5 mg/5 mL (120 mL) [alcohol free, sugar free; contains methylparaben, propylene glycol, propylparaben]

Cetirizine HCl Childrens: 1 mg/mL (118 mL) [contains methylparaben, propylene glycol, propylparaben]

Cetirizine HCl Hives Relief: 5 mg/5 mL (120 mL) [alcohol free, sugar free; contains methylparaben, propylene glycol, propylparaben; grape flavor]

Generic: 1 mg/mL (120 mL, 473 mL)

Syrup, Oral, as hydrochloride:

Cetirizine HCl Childrens Alrgy: 1 mg/mL (118 mL, 120 mL) [contains methylparaben, propylene glycol, propylparaben; grape flavor]

Cetirizine HCl Childrens Alrgy: 5 mg/5 mL (120 mL [DSC]) [contains methylparaben, propylene glycol, propylparaben]

ZyrTEC Childrens Allergy: 1 mg/mL (118 mL) [contains methylparaben, propylene glycol, propylparaben; banana-grape flavor]

ZyrTEC Childrens Allergy: 1 mg/mL (118 mL) [dye free, sugar free; contains propylene glycol, sodium benzoate]

ZyrTEC Childrens Allergy: 1 mg/mL (118 mL) [dye free, sugar free; contains propylene glycol, sodium benzoate; bubble-gum flavor]

ZyrTEC Childrens Allergy: 5 mg/5 mL (5 mL, 118 mL) [dye free, sugar free; contains propylene glycol, sodium benzoate; grape flavor]

ZyrTEC Childrens Hives Relief: 1 mg/mL (118 mL) [grape flavor]

Generic: 1 mg/mL (120 mL, 473 mL [DSC], 480 mL); 5 mg/5 mL (5 mL, 120 mL [DSC])

Tablet, Oral, as hydrochloride:

All Day Allergy: 10 mg

ZyrTEC Allergy: 10 mg

ZyrTEC Hives Relief: 10 mg

Generic: 5 mg, 10 mg

Tablet Chewable, Oral, as hydrochloride:

All Day Allergy Childrens: 5 mg [DSC]

All Day Allergy Childrens: 10 mg [tutti-frutti flavor]

ZyrTEC Childrens Allergy: 5 mg [grape flavor]

ZyrTEC Childrens Allergy: 10 mg [contains fd&c blue #2 aluminum lake; grape flavor]

Generic: 5 mg, 10 mg

Tablet Dispersible, Oral, as hydrochloride:

ZyrTEC Allergy: 10 mg

ZyrTEC Allergy Childrens: 10 mg

ZyrTEC Allergy Childrens: 10 mg [citrus flavor]

Brand Names: U.S.

  • All Day Allergy Childrens [OTC]
  • All Day Allergy [OTC]
  • Cetirizine HCl Allergy Child [OTC]
  • Cetirizine HCl Childrens Alrgy [OTC]
  • Cetirizine HCl Childrens [OTC]
  • Cetirizine HCl Hives Relief [OTC]
  • ZyrTEC Allergy Childrens [OTC]
  • ZyrTEC Allergy [OTC]
  • ZyrTEC Childrens Allergy [OTC]
  • ZyrTEC Childrens Hives Relief [OTC]
  • ZyrTEC Hives Relief [OTC]

Pharmacologic Category

  • Histamine H1 Antagonist
  • Histamine H1 Antagonist, Second Generation
  • Piperazine Derivative

Pharmacology

Competes with histamine for H1-receptor sites on effector cells in the gastrointestinal tract, blood vessels, and respiratory tract

Absorption

Rapid

Distribution

Children: 0.7 L/kg ; Adults: 0.56 L/kg (Simons 1999)

Metabolism

Limited hepatic

Excretion

Urine (70%; 50% as unchanged drug); feces (10%)

Onset of Action

Suppression of skin wheal and flare: 0.7 hours (Simons, 1999)

Time to Peak

Serum: 1 hour

Duration of Action

Suppression of skin wheal and flare: ≥24 hours (Simons, 1999)

Half-Life Elimination

Children: 6.2 hours; Adults: 8 hours

Protein Binding

Plasma: Mean: 93%

Special Populations: Children

Clearance is increased, and half-life is decreased.

Use: Labeled Indications

Upper respiratory allergies: Temporarily relieves symptoms of upper respiratory allergies.

Urticaria: Relieves itching due to urticaria.

Contraindications

Hypersensitivity to cetirizine, hydroxyzine, or any component of the formulation

Dosing: Adult

Upper respiratory allergies, urticaria: Oral: 5 to 10 mg once daily, depending upon symptom severity (maximum dose: 10 mg daily)

Dosing: Geriatric

Upper respiratory allergies, urticaria: Oral: 5 mg once daily (maximum dose: 5 mg daily). The previously available prescription product recommended a maximum dose of 10 mg once daily in patients <77 years of age or 5 mg once daily in patients ≥77 years of age (Zyrtec Prescribing Information, 2006).

Dosing: Pediatric

Upper respiratory allergies, urticaria: Oral:

Infants 6 to <12 months: 2.5 mg once daily

Children 12 months to <2 years: 2.5 mg once daily; may increase to a maximum dose of 2.5 mg every 12 hours if needed

Children 2 to 5 years: Initial: 2.5 mg once daily; may be increased to a maximum dose of 2.5 mg every 12 hours or 5 mg once daily

Children ≥6 years and Adolescents: Refer to adult dosing.

Dosing: Renal Impairment

There are no dosage adjustments provided in the manufacturer’s labeling; however, the following adjustments have been recommended (Aronoff, 2007):

Adults:

GFR >50 mL/minute: No dosage adjustment necessary.

GFR ≤50 mL/minute: 5 mg once daily

Intermittent hemodialysis: 5 mg once daily; 5 mg 3 times per week may also be effective.

Peritoneal dialysis: 5 mg once daily.

Infants, Children, and Adolescents:

GFR ≥30 mL/minute/1.73 m2: No dosage adjustment necessary.

GFR 10 to 29 mL/minute/1.73 m2: Decrease dose by 50%.

GFR <10 mL/minute/1.73 m2: Not recommended.

Intermittent hemodialysis or peritoneal dialysis: Decrease dose by 50%.

Dosing: Hepatic Impairment

There are no dosage adjustments provided in the manufacturer’s labeling.

Administration

May be administered with or without food.

Chewable tablet: Chew tablet before swallowing; may be taken with or without water.

Storage

Store at 20°C to 25°C (68°F to 77°F); excursions are permitted between 15°C and 30°C (59°F and 86°F).

Drug Interactions

AbobotulinumtoxinA: Anticholinergic Agents may enhance the anticholinergic effect of AbobotulinumtoxinA. Monitor therapy

Acetylcholinesterase Inhibitors: May diminish the therapeutic effect of Anticholinergic Agents. Anticholinergic Agents may diminish the therapeutic effect of Acetylcholinesterase Inhibitors. Monitor therapy

Aclidinium: May enhance the anticholinergic effect of Anticholinergic Agents. Avoid combination

Alcohol (Ethyl): CNS Depressants may enhance the CNS depressant effect of Alcohol (Ethyl). Monitor therapy

Amphetamines: May diminish the sedative effect of Antihistamines. Monitor therapy

Analgesics (Opioid): Anticholinergic Agents may enhance the adverse/toxic effect of Analgesics (Opioid). Specifically, the risk for constipation and urinary retention may be increased with this combination. Monitor therapy

Anticholinergic Agents: May enhance the adverse/toxic effect of other Anticholinergic Agents. Exceptions: Levocabastine (Nasal). Monitor therapy

Azelastine (Nasal): CNS Depressants may enhance the CNS depressant effect of Azelastine (Nasal). Avoid combination

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. Consider therapy modification

Betahistine: Antihistamines may diminish the therapeutic effect of Betahistine. Monitor therapy

Blonanserin: CNS Depressants may enhance the CNS depressant effect of Blonanserin. Consider therapy modification

Brimonidine (Topical): May enhance the CNS depressant effect of CNS Depressants. Monitor therapy

Buprenorphine: CNS Depressants may enhance the CNS depressant effect of Buprenorphine. Management: Consider reduced doses of other CNS depressants, and avoiding such drugs in patients at high risk of buprenorphine overuse/self-injection. Initiate buprenorphine patches (Butrans brand) at 5 mcg/hr in adults when used with other CNS depressants. Consider therapy modification

Cannabis: May enhance the CNS depressant effect of CNS Depressants. Monitor therapy

Cimetropium: Anticholinergic Agents may enhance the anticholinergic effect of Cimetropium. Avoid combination

CNS Depressants: May enhance the adverse/toxic effect of other CNS Depressants. Exceptions: Levocabastine (Nasal). Monitor therapy

Doxylamine: May enhance the CNS depressant effect of CNS Depressants. Management: The manufacturer of Diclegis (doxylamine/pyridoxine), intended for use in pregnancy, specifically states that use with other CNS depressants is not recommended. Monitor therapy

Dronabinol: May enhance the CNS depressant effect of CNS Depressants. Monitor therapy

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. Consider therapy modification

Eluxadoline: Anticholinergic Agents may enhance the constipating effect of Eluxadoline. Avoid combination

Gastrointestinal Agents (Prokinetic): Anticholinergic Agents may diminish the therapeutic effect of Gastrointestinal Agents (Prokinetic). Monitor therapy

Glucagon: Anticholinergic Agents may enhance the adverse/toxic effect of Glucagon. Specifically, the risk of gastrointestinal adverse effects may be increased. Avoid combination

Glycopyrrolate (Oral Inhalation): Anticholinergic Agents may enhance the anticholinergic effect of Glycopyrrolate (Oral Inhalation). Avoid combination

Hyaluronidase: Antihistamines may diminish the therapeutic effect of Hyaluronidase. Management: Patients receiving antihistamines (particularly at larger doses) may not experience the desired clinical response to standard doses of hyaluronidase. Larger doses of hyaluronidase may be required. Consider therapy modification

Hydrocodone: CNS Depressants may enhance the CNS depressant effect of Hydrocodone. Management: Consider starting with a 20% to 30% lower hydrocodone dose when using together with any other CNS depressant. Dose reductions in the other CNS depressant may also be warranted. Consider therapy modification

HydrOXYzine: May enhance the CNS depressant effect of CNS Depressants. Monitor therapy

Ipratropium (Oral Inhalation): May enhance the anticholinergic effect of Anticholinergic Agents. Avoid combination

Itopride: Anticholinergic Agents may diminish the therapeutic effect of Itopride. Monitor therapy

Kava Kava: May enhance the adverse/toxic effect of CNS Depressants. Monitor therapy

Levosulpiride: Anticholinergic Agents may diminish the therapeutic effect of Levosulpiride. Avoid combination

Lumacaftor: May decrease the serum concentration of P-glycoprotein/ABCB1 Substrates. Lumacaftor may increase the serum concentration of P-glycoprotein/ABCB1 Substrates. Monitor therapy

Magnesium Sulfate: May enhance the CNS depressant effect of CNS Depressants. Monitor therapy

Methotrimeprazine: CNS Depressants may enhance the CNS depressant effect of Methotrimeprazine. Methotrimeprazine may enhance the CNS depressant effect of CNS Depressants. Management: Reduce adult dose of CNS depressant agents by 50% with initiation of concomitant methotrimeprazine therapy. Further CNS depressant dosage adjustments should be initiated only after clinically effective methotrimeprazine dose is established. Consider therapy modification

Metyrosine: CNS Depressants may enhance the sedative effect of Metyrosine. Monitor therapy

Mianserin: May enhance the anticholinergic effect of Anticholinergic Agents. Monitor therapy

Minocycline: May enhance the CNS depressant effect of CNS Depressants. Monitor therapy

Mirabegron: Anticholinergic Agents may enhance the adverse/toxic effect of Mirabegron. Monitor therapy

Mirtazapine: CNS Depressants may enhance the CNS depressant effect of Mirtazapine. Monitor therapy

Nabilone: May enhance the CNS depressant effect of CNS Depressants. Monitor therapy

OnabotulinumtoxinA: Anticholinergic Agents may enhance the anticholinergic effect of OnabotulinumtoxinA. Monitor therapy

Orphenadrine: CNS Depressants may enhance the CNS depressant effect of Orphenadrine. Avoid combination

OxyCODONE: CNS Depressants may enhance the CNS depressant effect of OxyCODONE. Management: When oxycodone is combined with another CNS depressant, a dose reduction of one or both agents should be considered. The extended release oxycodone starting dose should be reduced 50% to 67% when initiated in patients already receiving CNS depressants. Consider therapy modification

Paraldehyde: CNS Depressants may enhance the CNS depressant effect of Paraldehyde. Avoid combination

Perampanel: May enhance the CNS depressant effect of CNS Depressants. Management: Patients taking perampanel with any other drug that has CNS depressant activities should avoid complex and high-risk activities, particularly those such as driving that require alertness and coordination, until they have experience using the combination. Consider therapy modification

P-glycoprotein/ABCB1 Inducers: May decrease the serum concentration of P-glycoprotein/ABCB1 Substrates. P-glycoprotein inducers may also further limit the distribution of p-glycoprotein substrates to specific cells/tissues/organs where p-glycoprotein is present in large amounts (e.g., brain, T-lymphocytes, testes, etc.). Monitor therapy

P-glycoprotein/ABCB1 Inhibitors: May increase the serum concentration of P-glycoprotein/ABCB1 Substrates. P-glycoprotein inhibitors may also enhance the distribution of p-glycoprotein substrates to specific cells/tissues/organs where p-glycoprotein is present in large amounts (e.g., brain, T-lymphocytes, testes, etc.). Monitor therapy

Potassium Chloride: Anticholinergic Agents may enhance the ulcerogenic effect of Potassium Chloride. Management: Patients on drugs with substantial anticholinergic effects should avoid using any solid oral dosage form of potassium chloride. Avoid combination

Pramipexole: CNS Depressants may enhance the sedative effect of Pramipexole. Monitor therapy

Pramlintide: May enhance the anticholinergic effect of Anticholinergic Agents. These effects are specific to the GI tract. Consider therapy modification

Ramosetron: Anticholinergic Agents may enhance the constipating effect of Ramosetron. Monitor therapy

Ranolazine: May increase the serum concentration of P-glycoprotein/ABCB1 Substrates. Monitor therapy

RimabotulinumtoxinB: Anticholinergic Agents may enhance the anticholinergic effect of RimabotulinumtoxinB. Monitor therapy

ROPINIRole: CNS Depressants may enhance the sedative effect of ROPINIRole. Monitor therapy

Rotigotine: CNS Depressants may enhance the sedative effect of Rotigotine. Monitor therapy

Rufinamide: May enhance the adverse/toxic effect of CNS Depressants. Specifically, sleepiness and dizziness may be enhanced. Monitor therapy

Secretin: Anticholinergic Agents may diminish the therapeutic effect of Secretin. Management: Avoid using drugs with substantial anticholinergic effects in patients receiving secretin whenever possible. If such agents must be used in combination, monitor closely for a diminished response to secretin. 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. Monitor therapy

Sodium Oxybate: May enhance the CNS depressant effect of CNS Depressants. Management: Consider alternatives to combined use. When combined use is needed, consider minimizing doses of one or more drugs. Use of sodium oxybate with alcohol or sedative hypnotics is contraindicated. Consider therapy modification

Suvorexant: CNS Depressants may enhance the CNS depressant effect of Suvorexant. Management: Dose reduction of suvorexant and/or any other CNS depressant may be necessary. Use of suvorexant with alcohol is not recommended, and the use of suvorexant with any other drug to treat insomnia is not recommended. Consider therapy modification

Tapentadol: May enhance the CNS depressant effect of CNS Depressants. Management: Start tapentadol at a dose of one-third to one-half of the normal dose if being initiated in a patient who is taking another drug with CNS depressant effects. Monitor closely for evidence of excessive CNS depression. Consider therapy modification

Tetrahydrocannabinol: May enhance the CNS depressant effect of CNS Depressants. Monitor therapy

Thalidomide: CNS Depressants may enhance the CNS depressant effect of Thalidomide. Avoid combination

Thiazide and Thiazide-Like Diuretics: Anticholinergic Agents may increase the serum concentration of Thiazide and Thiazide-Like Diuretics. Monitor therapy

Tiotropium: Anticholinergic Agents may enhance the anticholinergic effect of Tiotropium. Avoid combination

Topiramate: Anticholinergic Agents may enhance the adverse/toxic effect of Topiramate. Monitor therapy

Trimeprazine: May enhance the CNS depressant effect of CNS Depressants. Monitor therapy

Umeclidinium: May enhance the anticholinergic effect of Anticholinergic Agents. Avoid combination

Zolpidem: CNS Depressants may enhance the CNS depressant effect of Zolpidem. Management: Reduce the Intermezzo brand sublingual zolpidem adult dose to 1.75 mg for men who are also receiving other CNS depressants. No such dose change is recommended for women. Avoid use with other CNS depressants at bedtime; avoid use with alcohol. Consider therapy modification

Test Interactions

May cause false-positive serum TCA screen. May suppress the wheal and flare reactions to skin test antigens.

Adverse Reactions

>10%: Central nervous system: Drowsiness (adults 14%; children 2% to 4%), headache (children 11% to 14%, placebo 12%)

2% to 10%:

Central nervous system: Insomnia (children 9%; adults <2%), fatigue (adults 6%), malaise (4%), dizziness (adults 2%)

Gastrointestinal: Abdominal pain (children 4% to 6%), xerostomia (adults 5%), diarrhea (children 2% to 3%), nausea (children 2% to 3%; placebo 2%), vomiting (children 2% to 3%)

Respiratory: Pharyngitis (children 3% to 6%; placebo 3%), epistaxis (children 2% to 4%; placebo 3%), bronchospasm (children 2% to 3%; placebo 2%)

<2% (Limited to important or life-threatening; as reported in adults and/or children): Aggressive behavior, anaphylaxis, angioedema, ataxia, chest pain, confusion, convulsions, depersonalization, depression, dysgeusia, edema, fussiness, hallucination, hemolytic anemia, hepatic insufficiency, hepatitis, hypertension, hypotension (severe), irritability, nervousness, ototoxicity, palpitations, paralysis, paresthesia, skin photosensitivity, skin rash, suicidal ideation, tongue discoloration, tongue edema, tremor, visual field defect, weakness

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:

• Hepatic impairment: Use with caution.

• Renal impairment: Use with caution; consider dosage adjustment.

Concurrent drug therapy issues:

• Drug-drug interactions: Potentially significant interactions may exist, requiring dose or frequency adjustment, additional monitoring, and/or selection of alternative therapy. Consult drug interactions database for more detailed information.

• Sedatives: Effects may be potentiated when used with other sedative drugs or ethanol.

Special populations:

• Elderly: Use with caution in elderly patients; may be more sensitive to adverse effects.

Monitoring Parameters

Relief of symptoms, sedation and anticholinergic effects

Pregnancy Considerations

Maternal use of cetirizine has not been associated with an increased risk of major malformations. The use of antihistamines for the treatment of rhinitis during pregnancy is generally considered to be safe at recommended doses. Although safety data is limited, cetirizine may be a preferred second generation antihistamine for the treatment of rhinitis during pregnancy.

Patient Education

• Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)

• Patient may experience fatigue or dry mouth. Have patient report immediately to prescriber severe loss of strength and energy (HCAHPS).

• Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.

Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for healthcare professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience and judgment in diagnosing, treating and advising patients.

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