Cetirizine
Zyrtec
Second-generation H1 receptor antagonist (peripheral)
Selective peripheral H1 antagonist. Carboxylic acid structure → poor BBB penetration → minimal sedation compared with first-generation antihistamines like diphenhydramine.
Indications
- •Allergic rhinitis, urticaria, allergic conjunctivitis
- •Pre-medication in patients with contrast or drug allergy history (paired with steroid)
- •Pruritus from non-anaphylactic causes
Dosing
| Context | Adult | Pediatric |
|---|---|---|
| Adult allergy | 10 mg PO daily | — |
| Pre-contrast prophylaxis | 10 mg PO 1 h before contrast (with prednisone 50 mg q13/q7/q1 h) | — |
Pharmacokinetics
PO onset 30–60 min. Peak 1 h. Half-life 8 h. Renal excretion 60% unchanged.
Hemodynamic effects
Minimal.
Respiratory effects
None directly.
Side effects
- !Sedation (less than diphenhydramine but more than fexofenadine; ~10% of users)
- !Dry mouth
- !Headache
Contraindications
- ×Severe renal impairment (reduce dose; CrCl < 30 → 5 mg every other day)
Clinical pearls
- ★AMBULATORY ANESTHESIA: when an H1 blocker is needed pre-op, cetirizine is preferable to diphenhydramine — far less postoperative sedation and Beers-flagging.
- ★CONTRAST PROPHYLAXIS: 'Greenberger protocol' — prednisone 50 mg PO at 13 h, 7 h, 1 h before contrast + cetirizine or diphenhydramine 1 h before. Reduces moderate-severe reactions by ~80%.
- ★RENAL FAILURE: dose reduction matters more than for diphenhydramine because cetirizine is renally cleared.
- ★PRURITUS NEURAXIAL OPIOID: cetirizine is less effective than naloxone or nalbuphine because the itch is opioid-receptor-mediated, not histaminergic.
Other drugs in Antihistamines
- Diphenhydramine
Competitive H1 antagonist with significant anticholinergic + sedating activity from CNS penetration. Crosses BBB freely.
- Famotidine
Reversible competitive antagonist at parietal cell H2 receptors → reduces basal + stimulated gastric acid secretion. Raises gastric pH within 30 min.
Browse all classes: /reference/drugs

