Each uncoated tablet contains: Loratadine 10mg.
It is (H) receptor antagonist, penetrates very poorly into the central system, and hence is devoid of CNS depressant effects. Structurally it is related to azatadine. Loratadine also suppresses mast cell mediator release. It has a molecular weight of 382.89, and empirical formula of C22H23CIN2O2; its chemical name is ethyl 4-(8-chloro-5,6-dihydro-11H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-ylidene)-1-piperidinecarboxylate.
Excipients/Inactive Ingredients: Lactose monohydrate, Maize starch, Magnesium stearate, Colloidal silicon dioxide, Povidone (K30), Purified water, Purified talc.
Pharmacology: Pharmacodynamics: Mechanism of Action: Loratadine is a tricyclic antihistamine with long-acting selective peripheral H1 receptor antagonist activity. It does not readily cross the blood brain barrier.
Human histamine skin wheal studies following single and repeated 10 mg oral doses of loratadine have shown that the drug exhibits an antihistaminic effect beginning within 1 to 3 hours, reaching a maximum at 8 to 12 hours, and lasting in excess of 24 hours. There was no evidence of tolerance to this effect after 28 days of dosing with loratadine.
Pharmacokinetics: After oral administration, loratadine is rapidly and well absorbed, and undergoes extensive first pass metabolism, mainly by CYP3A4 and CYP2D6. The major metabolite - desloratadine (DL) - is pharmacologically active and responsible for a large part of the clinical effect. Loratadine and DL achieve maximum plasma concentrations (Tmax) between 1-1.5 hours and 1.5-3.7 hours after administration, respectively.
Increase in plasma concentrations of loratadine has been reported after concomitant use with ketoconazole, erythromycin, and cimetidine in controlled trials, but without clinically significant changes (including electrocardiographic).
Loratadine is highly bound to plasma proteins (97% to 99%), its active metabolite moderately bound (73% to 76%) to plasma proteins.
In healthy subjects, the plasma distribution half-lives of loratadine and its active metabolite are approx. 1 and 2 hours, respectively. The mean elimination half-lives in healthy adult subjects were 8.4 hours (range = 3 to 20 hours) for loratadine and 28 hours (range = 8.8 to 92 hours) for the major active metabolite.
Approximately 40% of the dose is excreted via urine and 42% in the faeces over a 10 day period and mainly in the form of conjugated metabolites. Approximately 27% of the dose is excreted in the urine during the first 24 hours. Less than 1% of the active substance is excreted unchanged in active form, as loratadine or DL.
The bioavailability parameters of loratadine and of the active metabolite are dose proportional.
The pharmacokinetic profile of loratadine and its metabolites is comparable in healthy adult volunteers and healthy geriatric volunteers.
Concomitant ingestion of food can delay slightly the absorption of loratadine but without influencing the clinical effect.
In patients with chronic renal impairment, both the AUC and peak plasma levels (Cmax) increased for loratadine and its metabolite as compared to the AUCs and peak plasma levels (Cmax) of patients with normal renal function. The mean elimination half-lives of loratadine and its metabolite were not significantly different from that observed in normal subjects. Haemodialysis does not have an effect on the pharmacokinetics of loratadine or its active metabolite in subjects with chronic renal impairment.
In patients with chronic alcoholic liver disease, the AUC and peak plasma levels (Cmax) of loratadine were double while the pharmacokinetic profile of the active metabolite was not significantly changed from that in patients with normal liver function. The elimination half-lives for loratadine and its metabolite were 24 and 37 hours, respectively, and increased with increasing severity of liver disease.
Loratadine and its active metabolite are excreted in the breast milk of lactating women.
Loratadine is indicated for the symptomatic treatment of allergic rhinitis and chronic idiopathic urticaria.
Adults and children 12 years of age and over: 10 mg daily (one tablet once daily).
The tablets may be taken without regard to mealtime.
Children aged 2 to under 12 years with Body weight more than 30 kg: 10 mg daily (one tablet once daily).
Body weight 30 kg or less: The 10mg strength tablet is not appropriate in children with a body weight less than 30 kg.
Efficacy and safety of in children under 2 years of age have not been established.
Patients with severe liver impairment should be administered a lower initial dose because they may have reduced clearance of loratadine. An initial dose of one tablet every other day is recommended for adults and children weighing more than 30 kg.
No dosage adjustment are required in the elderly or in patients with renal insufficiency.
In adults, somnolence, tachycardia, and headache have been reported with overdoses greater than 10 mg with the Tablet formulation (40 mg-180 mg). In the event of overdosage, general symptomatic and supportive measures should be instituted promptly and maintained for as long as necessary.
Discontinuation of use, gastric lavage or induction of emesis (except in patients with impaired consciousness) and support of vital functions are advised.
Loratadine is contraindicated in patients who are hypersensitive to this medication or to any of its ingredients.
Loratadine should be used with caution in the treatment of patients with severe liver impairment.
Patients with rare hereditary problems of galactose intolerance, the Lapp lactase deficiency or glucose-galactose malabsorption should not take this medicinal product.
The administration of tablets should be discontinued at least 48 hours before skin tests, as antihistamines may prevent or reduce otherwise positive reactions to dermal reactivity index.
Effects on ability to drive and use machines: In clinical trials that assessed driving ability, no impairment occurred In patients receiving loratadine. However, patients should be informed that very rarely some people experience drowsiness, which may affect their ability to drive or use machines.
Use in Pregnancy: Pregnancy Category B: Loratadine was not found to be teratogenic in animal studies. There are no adequate and well-controlled studies in pregnant woman; use during pregnancy only if clearly needed.
Use in Lactation: Nursing Mothers: Loratadine and its (metabolite, descarboethoxyloratadine, pass easily into breast milk and achieve concentrations that are equivalent to plasma level with an AUCmilk/AUCplasma ratio of 1.17 and 0.85 for loratadine and descarboethoxyloratadine, respectively. A decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother. Caution should be exercised when Loratadine is administered to a nursing woman.
Use in Children: The safety and effectiveness of loratadine in children under 2 years of age have not been established.
Clinical studies have Reported following Adverse Events With An Incidence Of More Than 2% In Placebo-Controlled Allergic Rhinitis Clinical Trials In Patients 12 Years Of Age And Older (Percent Of Patients): Headache(12%), somnolence (8%), fatigue (4%) Dry Mouth (3%).
Drug Abuse And Dependence: There is no information to indicate that abuse or dependency occurs with loratadine.
When administered concomitantly with alcohol, loratadine has no potentiating effects as measured by psychomotor performance studies. Increases in plasma concentrations of loratadine have been reported after concomitant use with ketoconazole, erythromycin or cimetidine in controlled clinical trials, but without clinically significant changes (including electrocardiographic). Other drugs known to inhibit hepatic function metabolism should be coadministered with caution until definitive interaction studies can be completed.
Laboratory Test Interactions: Loratadine should be discontinued approximately, 48 hours prior to skin testing procedures since antihistamine may prevent or diminish otherwise positive reactions to dermal reactivity indicators.
Store below 30°C in a dry place.
Protect from light and moisture.
R06AX13 - loratadine ; Belongs to the class of other antihistamines for systemic use.
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