Brand Name: Alavert
Generic Name: Loratadine
Loratadine is a long-acting tricyclic antihistamine with selective peripheral H1 receptor antagonistic activity. It exhibits a dose-related inhibition of the histamine-induced skin wheal and flare response in humans which is rapid in onset, is apparent at 2 hours and persists throughout the 24 hour observation period. Single oral doses up to 160 mg and repeat daily doses of 40 mg for up to 13 weeks were well tolerated with the incidence of sedation and dry mouth being no different from placebo.
14C-loratadine is rapidly absorbed reaching Cmax values (4.7, 10.8 and 26.1 ng/mL) at 1.5, 1.0 and 1.3 hours for the 10, 20 and 40 mg dose, respectively. The loratadine elimination half-life (T1/2β) ranged from 7.8 to 11 hours.
Descarboethoxy-loratadine, the major active metabolite, reached Cmax values (4.0, 9.9 and 16.0 ng/mL) at 3.7, 1.5 and 2.0 hours after a dose of 10, 20 and 40 mg, respectively. Its T1/2β ranged from 17 to 24 hours. The accumulation indices, calculated by Cmax and the area under the curve (AUC) ratios did not change after the 5th day, indicating little or no accumulation of either loratadine or its metabolite after a multiple once per day dosage regimen. The T1/2β at steady state levels for loratadine and its active metabolite were 14.4 and 18.7 hours, respectively, similar to that reported following a single oral dose.
Approximately 82% of the 14C-loratadine dose is excreted in the urine (40%) and feces (42%) over a 10-day period. Approximately 27% of the dose is eliminated in the urine during the first 24 hours largely in the conjugated form. Unchanged drug is present only in trace quantities in the urine and the active metabolite descarboethoxy-loratadine represents only 0.4 to 0.6% of the administered loratadine dose.
Pseudoephedrine sulfate, one of the naturally occurring alkaloids of Ephedra and an orally administered vasoconstrictor, produces a gradual but sustained decongestant effect facilitating shrinkage of congested mucosa in upper respiratory areas. The mucous membrane of the respiratory tract is decongested through the action of the sympathetic nerves.
In those patients who have shown sensitivity or idiosyncrasy to the components, to adrenergic agents or to other drugs of similar chemical structures. Also contraindicated in patients receiving MAO inhibitor therapy or within 14 days of discontinuing such treatment and in patients with narrow-angle glaucoma, urinary retention, hypertension, severe coronary artery disease and hyperthyroidism
There are no data available to indicate that abuse or dependency occurs with loratadine.
Pseudoephedrine sulfate, like other CNS stimulants, has been abused. At high doses, subjects commonly experience mood elevation, decreased appetite and a sense of increased energy, physical strength, mental capacity and alertness. Anxiety, irritability and loquacity also have been reported. With continued use, tolerance develops; the user increases the dose and ultimately toxicity occurs. Depression may follow rapid withdrawal |
