Dosing & Uses
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
Interactions
Interaction Checker
No Results
Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor
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
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
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.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%)
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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Patient Handout
Formulary
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