Comparative Pharmacology
Head-to-head clinical analysis: EPINASTINE HYDROCHLORIDE versus HISTAFED.
Peer-Reviewed Evidence
Head-to-head clinical analysis: EPINASTINE HYDROCHLORIDE versus HISTAFED.
EPINASTINE HYDROCHLORIDE vs HISTAFED
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Selective histamine H1-receptor antagonist. Inhibits histamine release from mast cells and basophils, and reduces chemotaxis and activation of eosinophils. Also suppresses cytokine production from T lymphocytes.
HISTAFED is a combination of pseudoephedrine, a sympathomimetic amine that acts as a decongestant by stimulating alpha-adrenergic receptors in the nasal mucosa causing vasoconstriction, and triprolidine, a first-generation antihistamine that competes with histamine for H1-receptor sites on effector cells in the gastrointestinal tract, blood vessels, and respiratory tract, thereby preventing histamine-mediated effects.
For allergic rhinitis and urticaria: 10 mg twice daily orally (20 mg/day). For ophthalmic use: 1 drop in affected eye(s) twice daily of 0.05% solution.
60 mg orally every 4 to 6 hours as needed; maximum 360 mg per day.
None Documented
None Documented
The terminal elimination half-life is approximately 5.7 to 9.2 hours in healthy adults. In elderly patients, the half-life may be prolonged due to reduced renal function. The half-life supports twice-daily dosing for most indications.
3-4 hours for pseudoephedrine component; shorter in children (2-3 h), prolonged in renal impairment
Renal excretion accounts for approximately 39% of the administered dose, with about 28% as unchanged drug and 11% as metabolites. Fecal excretion is minimal at approximately 10%. Biliary excretion is not a significant route. Overall, renal clearance is the primary elimination pathway.
Renal (approximately 65% as unchanged drug and metabolites), biliary/fecal (35%)
Category A/B
Category C
Antihistamine
Antihistamine/Decongestant Combination