cetirizine

Therapeutic Classification: allergy, cold and cough remedies, antihistamines

Pharmacologic Classification: piperazines (peripherally selective)

Indications ⬆ ⬇

REMS

Relief of allergic symptoms caused by histamine release including:
- Seasonal and perennial allergic rhinitis,
- Chronic urticaria.

Acute urticaria.

Action ⬆ ⬇

Antagonizes the effects of histamine at H₁-receptor sites; does not bind to or inactivate histamine.
Anticholinergic effects are minimal, and sedation is dose related.

Therapeutic effects:

Decreased symptoms of histamine excess (sneezing, rhinorrhea, ocular tearing and redness, pruritus).

Pharmacokinetics ⬆ ⬇

Absorption: Well absorbed following oral administration. IV administration results in complete bioavailability.

Distribution: Unknown.

Protein Binding: 93%.

Metabolism/Excretion: Excreted primarily unchanged by the kidneys.

Half-Life: 7.4–9 hr (↓ in children to 6.2 hr, ↑ in renal impairment up to 19–21 hr).

Time/Action Profile ⬆ ⬇

(antihistaminic effects)

ROUTE	ONSET	PEAK	DURATION
PO	30 min	4–8 hr	24 hr
IV	unknown	unknown	unknown

Contraind./Precautions ⬆ ⬇

Contraindicated in:

Hypersensitivity to cetirizine, levocetirizine, hydroxyzine, or any component;
Pedi: Children 6 yr with renal or hepatic impairment.

Use Cautiously in:

Patients with hepatic or renal impairment (dose ↓ recommended if CCr ≤31 mL/min or hepatic function is impaired);
OB: Use during pregnancy only if potential maternal benefit justifies potential fetal risk;
Lactation: Use while breastfeeding only if potential maternal benefit justifies potential risk to infant;
Pedi: Children 6 mo (safety and effectiveness not established);
Geri: Initiate at lower doses in older adults.

Adv. Reactions/Side Effects ⬆ ⬇

Derm: acute generalized exanthematous pustulosis

EENT: pharyngitis

GI: dry mouth

Neuro: dizziness, drowsiness (significant with oral doses >10 mg/day), fatigue

Interactions ⬆ ⬇

Drug-drug:

Additive CNS depression may occur with alcohol, opioid analgesics, or sedative/hypnotics.
Theophylline may ↓ clearance and ↑ toxicity.

Route/Dosage ⬆ ⬇

PO (Adults and Children ≥6 yr): 5–10 mg given once or divided twice daily.
PO (Children 2–5 yr): 2.5 mg once daily initially, may be ↑ to 5 mg once daily or 2.5 mg every 12 hr.
PO (Children 1–2 yr): 2.5 mg once daily initially; may be ↑ to 2.5 mg every 12 hr.
PO (Children 6–12 mo): 2.5 mg once daily.
IV (Adults and Children ≥12 yr): 10 mg every 24 hr as needed.
IV (Children 6–11 yr): 5–10 mg every 24 hr as needed.
IV (Children 6 mo–5 yr): 2.5 mg every 24 hr as needed.
PO (Adults and Children ≥12 yr): CCr ≤31 mL/min, hepatic impairment or hemodialysis: 5 mg once daily.
PO (Children 6–11 yr): start therapy at <2.5 mg/day.

Availability ⬆ ⬇

(Generic available)

Capsules: 10 mg^OTC
Chewable tablets: 5 mg^OTC; 10 mg^OTC
Orally disintegrating tablets: 10 mg
Syrupbanana-grape and bubblegum flavors: 1 mg/mL^OTC
Tablets: 5 mg^OTC; 10 mg^OTC; 20 mg
Solution for injection: 10 mg/mL
In combination with: pseudoephedrine (Zyrtec-D 12 hr) (See Appendix [not included in this PDA edition]).

Assessment ⬆ ⬇

Assess allergy symptoms (rhinitis, conjunctivitis, hives) before and periodically during therapy.
Assess lung sounds and character of bronchial secretions. Maintain fluid intake of 1500–2000 mL/day to decrease viscosity of secretions.
Assess severity of urticaria before and periodically after injection.

Lab Test Considerations:

May cause false-negative result in allergy skin testing.

Implementation ⬆ ⬇

Do not confuse cetirizine with sertraline. Do not confuse Zyrtec with Lipitor, Zocor, Zyprexa, or Zyrtec-D.
PO: Administer once daily without regard to food.

IV Administration:

Administer undiluted. Solution is clear and colorless; do not administer solutions that are cloudy, discolored, or contain precipitate matter.
Rate: Administer IV push over 1–2 min.

Patient/Family Teaching ⬆ ⬇

Instruct patient to take medication as directed.
May cause dizziness and drowsiness. Caution patient to avoid driving or other activities requiring alertness until response to medication is known.
Advise patient to avoid taking alcohol or other CNS depressants, including opioids, concurrently with this drug.
Advise patient that good oral hygiene, frequent rinsing of mouth with water, and sugarless gum or candy may minimize dry mouth. Patient should notify dentist if dry mouth persists >2 wk.
Instruct patient to contact health care professional if rash or dizziness occurs or if symptoms persist.
Rep: Advise females of reproductive potential to notify health care professional if pregnancy is planned or suspected or if breastfeeding.

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Pronunciation ⬇

Classifications ⬆ ⬇