- April 12, 2022
Loratadine is a tricyclic antihistamine with selective, peripheral H1-receptor activity.
Loratadine has no significant H2-receptor activity.
After oral administration, loratadine is rapidly and well absorbed and undergoes an extensive first pass metabolism, mainly by CYP3A4 and CYP2D6. The major metabolite is active and responsible for a large part of the clinical effect. Loratadine is highly bound (97% to 99%) and its active metabolite is moderately bound (73% to 76%) to plasma proteins. Approximately 40% of the dose is excreted in the urine and 42% in the faeces over a 10-day period and mainly in the form of conjugated metabolites.
Loratadine is indicated for the symptomatic treatment of allergic rhinitis and chronic idiopathic urticaria. The drug may be taken without regard to meal time.