Indications
Relief of symptoms of seasonal allergic rhinitis. Management
of chronic idiopathic urticaria.
Action
Antagonizes the effects of histamine at peripheral histamine–
1 (H1) receptors, including pruritus and urticaria.
Also has a drying effect on the nasal mucosa.
Therapeutic Effects: Decreased sneezing, rhinorrhea,
itchy eyes, nose, and throat associated with seasonal
allergies. Decreased urticaria.
Pharmacokinetics
Absorption: Rapidly absorbed after oral administration.
Distribution: Unknown.
Metabolism and Excretion: 80% excreted in
urine, 11% excreted in feces.
Half-life: 14.4 hr (qin renal impairment).
TIME/ACTION PROFILE (antihistaminic effect)
ROUTE ONSET PEAK DURATION
PO within 1 hr 2–3 hr 12–24 hr
Contraindications/Precautions
Contraindicated in: Hypersensitivity.
Use Cautiously in: Impaired renal function (qdosing
interval recommended); OB: use only if maternal
benefit outweighs potential risk to fetus; Lactation: Usually
compatible with breast feeding (AAP).
Adverse Reactions/Side Effects
CNS: drowsiness, fatigue. GI: dyspepsia. Endo: dysmenorrhea.
Interactions
Drug-Drug: Magnesium and aluminum-containing
antacidspabsorption and may decrease effectiveness.
Drug-Food: Apple, orange, and grapefruit juice
pabsorption and may decrease effectiveness.
Route/Dosage
PO (Adults and Children 12 yr): 60 mg twice
daily, or 180 mg once daily.
PO (Children 2–11 yr): 30 mg twice daily.
PO (Children 6 mo–2 yr): 15 mg twice daily.
Renal Impairment
PO (Adults): 60 mg once daily as a starting dose.
PO (Children 6–11 yr): 30 mg once daily as a starting
dose.
Availability (generic available)
Tablets: 30 mgOTC, 60mgOTC, 120 mgOTC, 180 mgOTC.
Orally disintegrating tablets: 30 mgOTC. Gelcaps:
180 mgOTC. Suspension (berry flavor): 30 mg/5
mLOTC. In combination with: pseudoephedrine (Allegra-
D). See Appendix B.
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