ZyrTEC, cetirizine, Aller Relief, Reactine, Rhinaris Relief,

 Indications

Relief of allergic symptoms caused by histamine release

including: Seasonal and perennial allergic rhinitis,

Chronic 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.

Distribution: Unknown.

Protein Binding: 93%.

Metabolism and Excretion: Excreted primarily

unchanged by the kidneys.

Half-life: 7.4–9 hr (pin children to 6.2 hr,qin renal

impairment up to 19–21 hr).

TIME/ACTION PROFILE (antihistaminic

effects)

ROUTE ONSET PEAK DURATION

PO 30 min 4–8 hr 24 hr

Contraindications/Precautions

Contraindicated in: Hypersensitivity to cetirizine,

hydroxyzine or any component; Lactation: Excreted in

breast milk; not recommended for use.

Use Cautiously in: Patients with hepatic or renal

impairment (doseprecommended if CCr 31 mL/min

or hepatic function is impaired); OB, Pedi: Safety not

established for pregnant women or children 6 mo;

Geri: Initiate at lower doses.

Adverse Reactions/Side Effects

CNS: dizziness, drowsiness (significant with doses 10

mg/day), fatigue. Derm: acute generalized exanthematous

pustulosis. EENT: pharyngitis. GI: dry mouth.

Interactions

Drug-Drug: Additive CNS depression may occur with

alcohol, opioid analgesics, or sedative/hypnotics.

Theophylline maypclearance andqtoxicity.

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 beqto 5 mg once daily or 2.5 mg every 12 hr.

PO (Children 1–2 yr): 2.5 mg once daily; may beq

to 2.5 mg every 12 hr.

PO (Children 6–12 mo): 2.5 once daily.

Hepatic/Renal Impairment

PO (Adults and Children 12 yr): CCr 31 mL/

min, hepatic impairment or hemodialysis—5 mg

once daily.

Hepatic/Renal Impairment

PO (Children 6–11 yr): start therapy at 2.5 mg/

day.

Hepatic/Renal Impairment

PO (Children 6 yr): use not recommended.

Availability (generic available)

Tablets: 5 mgOTC, 10mgOTC. Capsules: 5 mgOTC, 10

mgOTC. Chewable tablets (grape): 5 mgOTC, 10mgOTC.

Orally disintegrating tablets: 10 mg. Syrup (banana-

grape and bubblegum flavors): 1 mg/mLOTC.

In combination with: pseudoephedrine (Zyrtec-D

12 hr) (See Appendix B).