cetirizine (Rx, OTC)

Brand and Other Names:Zyrtec, Zyrtec Allergy, more...Children's Zyrtec Allergy, Children's Zyrtec Hives Relief, PediaCare Children's 24 Hour Allergy, Aller-Tec, Wal-Zyr, Quzyttir
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

tablet

  • 5mg (generic, Zyrtec)
  • 10mg (generic, Zyrtec)

tablet, oral-disintegrating

  • 10mg (Zyrtec Allergy)

tablet, chewable

  • 5mg (generic, Zyrtec)
  • 10mg (generic, Zyrtec)

syrup

  • 5mg/5mL (generic)

solution

  • 5mg/5mL (generic)

injectable solution

  • 10mg/mL (Quzyttir)

Allergies/Hay Fever/Urticaria

PO

Perennial and seasonal allergic and vasomotor rhinitis; relief of symptoms from colds, urticaria, angioedema, anaphylactic reactions, pruritus, allergic conjunctivitis

5-10 mg PO qDay, depending on severity of symptoms; not to exceed 10 mg qDay

IV

Indicated for acute urticaria

10 mg IV push q24hr PRN

Dosing Modifications

Renal impairment

  • PO

    • GFR >50 mL/min: Dose adjustment not necessary
    • GFR ≤ 50 mL/min: 5 mg PO qDay
    • Peritoneal dialysis: 5 mg PO qDay
    • Intermittent hemodialysis: 5 mg PO qDay; may also administer 3 times weekly
  • IV
    • Mild-to-severe and patients on dialysis: No dosage adjustment necessary; monitor for antihistaminic side effects

Hepatic impairment

  • PO: Dose adjustment not provided by manufacturer's label

  • IV: No dosage adjustment necessary; monitor for antihistaminic side effects in this patient population

Dosage Forms & Strengths

tablet

  • 5mg (generic, Zyrtec)
  • 10mg (generic, Zyrtec)

tablet, oral-disintegrating

  • 10mg (Zyrtec Allergy)

tablet, chewable

  • 5mg (generic, Zyrtec)
  • 10mg (generic, Zyrtec)

syrup

  • 5mg/5mL (generic)

solution

  • 5mg/5mL (generic)

injectable solution

  • 10mg/mL (Quzyttir)

Allergies/Hay Fever/Urticaria

PO

  • Perennial and seasonal allergic and vasomotor rhinitis
  • <2 years: Safety and efficacy not established
  • 2-6 years: 2.5 mg (0.5 teaspoon) oral solution PO qDay; can increase to 5 mg PO qDay or 2.5 mg PO twice daily; not to exceed 5 mg qDay
  • >6 years: 5-10 mg PO qDay, depending on severity of symptoms; not to exceed 10 mg qDay

IV

  • Indicated for acute urticaria in adults and children aged ≥6 months
  • 6 months to 5 years: 2.5 mg IV push q24hr PRN
  • 6 to <12 years: 5 or 10 mg depending on symptom severity IV push q24hr PRN
  • ≥12 years: 10 mg IV push q24hr PRN

Dosing Modifications

Renal impairment

  • PO
    • GFR ≥30 mL/min/1.73 m2: Dose adjustment not necessary
    • GFR 10-29 mL/min/1.73 m2: Decrease dose by 50%
    • GFR < 10 mL/min/1.73 m2: Not recommended
    • Intermittent hemodialysis or peritoneal dialysis: Decrease dose by 50%
  • IV
    • Mild-to-severe and patients on dialysis: No dosage adjustment necessary; monitor for antihistaminic side effects

Hepatic impairment

PO: Dose adjustment not provided by manufacturer's label

IV: No dosage adjustment necessary; monitor for antihistaminic side effects in this patient population

Dosing Considerations

Limitations of use: Not recommended in pediatric patients <6 years impaired renal or hepatic function

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Interactions

Interaction Checker

and cetirizine

No Results

     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

            All Interactions Sort By:
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            Adverse Effects

            >10%

            Somnolence (2-14%)

            Headache (11-14%)

            1-10%

            Fatigue (5.9%)

            Dry mouth (5%)

            Dizziness (2%)

            Diarrhea (2-3%)

            Malaise (4%)

            Bronchospasm (2-3%)

            Vomiting (2-3%)

            Epistaxis (2-4%)

            <1%

            Stomach pain

            Drowsiness

            Angioedema

            Fussiness

            Hallucinations

            Hypotension

            Tremor

            Tongue discoloration

            Postmarketing Reports

            Cardiac disorders: Severe hypotension

            Gastrointestinal disorders: Cholestasis

            Nervous system disorders: Extrapyramidal symptoms, myoclonus, orofacial dyskinesia, tic

            Pregnancy, puerperium and perinatal conditions: Stillbirth

            Renal and urinary disorders: Glomerulonephritis

            Skin and subcutaneous tissue disorders: acute generalized exanthematous pustulosis (AGEP); rebound pruritus-pruritus within a few days after discontinuation of cetirizine, usually after long-term use (eg, months to years)

            Postmarketing reports of active metabolite (levocetirizine)

            • Cardiac disorders: Palpitations, tachycardia
            • Ear and labyrinth disorders: Vertigo
            • Eye disorders: Blurred vision, visual disturbances
            • Gastrointestinal disorders: Nausea, vomiting
            • General disorders and administration site conditions: Edema
            • Hepatobiliary disorders: Hepatitis
            • Immune system disorders: Anaphylaxis and hypersensitivity Metabolism and nutrition disorders: Increased appetite
            • Musculoskeletal, connective tissues, and bone disorders: Arthralgia, myalgia
            • Nervous system disorders: Dizziness, dysgeusia, febrile seizure, movement disorders (including dystonia and oculogyric crisis), paraesthesia, seizure (reported in subjects with and without a known seizure disorder), tremor
            • Psychiatric disorders: Aggression and agitation, depression, hallucinations, insomnia, nightmare, suicidal ideation
            • Renal and urinary disorders: Dysuria, urinary retention
            • Respiratory, thoracic, and mediastinal disorders: Dyspnea
            • Skin and subcutaneous tissue disorders: Angioedema, fixed drug eruption, pruritus, rash and urticaria
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            Warnings

            Contraindications

            Hypersensitivity to cetirizine hydrochloride or any of its ingredients, levocetirizine, or hydroxyzine

            Cautions

            Avoid alcohol, sedatives, and tranquilizers, due to increased risk of drowsiness

            May cause CNS depression; avoid activities requiring mental alertness until accustomed to medication

            Use caution in hepatic and renal impairment

            The elderly may be more sensitive to adverse effects

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            Pregnancy & Lactation

            Pregnancy

            There are no adequate and well-controlled studies in pregnant women

            Lactation

            Cetirizine has been reported to be present in human breast milk

            In mice and beagle dogs, studies indicated that cetirizine was excreted in milk

            When a drug is present in animal milk, it is likely it will be present in human milk

            Pregnancy Categories

            A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

            B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

            C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

            D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

            X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

            NA: Information not available.

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            Pharmacology

            Mechanism of Action

            Histamine H1-receptor antagonist; competes with histamine on effector cells in the gastrointestinal tract, blood vessels and respiratory tract

            Absorption

            Peak plasma concentration: 311 ng/mL (PO)

            Peak serum time: 1 hr (PO)

            Duration: >24 hr (suppression of skin wheal and flare reactions) (PO)

            Effects of food

            • No effect on the extent of cetirizine exposure (AUC) but peak plasma time was delayed by 1.7 hr and peak plasma concentration was decreased by 23% in the presence of food when cetirizine hydrochloride was administered orally

            Distribution

            Protein bound: 93%

            Vd: 0.56 L/kg

            Metabolism

            Metabolized to a limited extent by oxidative O-dealkylation to a metabolite with negligible antihistaminic activity

            Enzyme or enzymes responsible for this metabolism have not been identified

            Elimination

            Half-life: 8.3hr

            Clearance:~53 mL/min

            Excretion: Urine (70% [50% unchanged]); feces (10%)

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            Administration

            IV Administration

            Administer as an IV push over 1-2 minutes

            Oral Administration

            May take with or without food

            Storage

            All formulations

            Store at 20-25ºC (68-77ºF), excursions permitted to 15-30ºC (59-86ºF)

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            Images

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            Formulary

            FormularyPatient Discounts

            Adding plans allows you to compare formulary status to other drugs in the same class.

            To view formulary information first create a list of plans. Your list will be saved and can be edited at any time.

            Adding plans allows you to:

            • View the formulary and any restrictions for each plan.
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            • Compare formulary status to other drugs in the same class.
            • Access your plan list on any device – mobile or desktop.

            The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

            Tier Description
            1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
            2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
            3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
            4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            NC NOT COVERED – Drugs that are not covered by the plan.
            Code Definition
            PA Prior Authorization
            Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
            QL Quantity Limits
            Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
            ST Step Therapy
            Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
            OR Other Restrictions
            Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
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            Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.