Each tablet contains Loratadine 10 mg.
Excipients/Inactive Ingredients: Lactose monohydrate, maize starch, povidone, purified talc, magnesium stearate, ethanol 96%, purified water.
Pharmacology: Loratadine is a potent long acting tricyclic antihistamine with selective peripheral H1-receptor antagonistic activity.
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.
Whole body autoradiographic studies in rats and monkeys, radiolabeled tissue distribution studies in mice and rats, and in vivo radioligand studies in mice have shown that neither Loratadine or its metabolites readily cross the blood-brain barrier. Radioligand binding studies with guinea pig pulmonary and brain H1-receptors indicate that there was preferential binding to peripheral versus central nervous system H1-receptors.
Repeated application of Loratadine rapidly disintegrating tablets to the hamster cheek pouch did not cause local irritation.
Pharmacokinetics: Loratadine was rapidly absorbed following oral administration of 10 mg tablets, once daily for 10 days to healthy adult volunteers with times to maximum concentration (Tmax) of 1.3 hours for Loratadine and 2.5 hours for its major active metabolite, descarboethoxyloratadine. Based on a cross-study comparison of single doses of Loratadine syrup and tablets given to healthy adult volunteers, the plasma concentration profile of descarboethoxyloratadine for the two formulations is comparable. The pharmacokinetics of Loratadine and descarboethoxyloratadine are independent of dose over the dose range of 10 to 40 mg and are not altered by the duration of treatment. In a single dose study, food increased the systemic bioavailability (AUC) of Loratadine and descarboethoxyloratadine by approximately 40% and 15%, respectively. The time to peak plasma concentration (Tmax) of Loratadine and descarboethoxyloratadine was delayed by 1 hour.
Peak plasma concentrations (Cmax) were not affected by food.
Pharmacokinetic studies showed that Loratadine rapidly disintegrating tablets provide plasma concentrations of Loratadine descarboethoxyloratadine similar to those achieved with Loratadine tablets. Following oral administration of 10 mg Loratadine once daily for 10 days with each dosage forms in a randomized crossover comparison in 24 normal adult subjects, similar mean exposures (AUC) and peak plasma concentrations (Cmax) of Loratadine were observed Loratadine rapidly disintegrating tablets mean AUC and Cmax were 11% and 6% greater than that of the Loratadine tablet values, respectively. Descarboethoxyloratadine bioequivalence was demonstrated between the two formulations. After 10 days of dosing, mean peak plasma concentrations were attained at 1.3 hours and 2.3 hours (Tmax) for parent and metabolite, respectively.
In a single dose study with Loratadine rapidly disintegrating tablets, food increased the AUC of Loratadine by approximately 48% and did not appreciably affect the AUC of descarboethoxyloratadine. The times to peak plasma concentration (Tmax) of Loratadine and descarboethoxyloratadine were delayed approximately 2.4 and 3.7 hours, respectively, when food was consumed prior to Loratadine rapidly disintegrating tablets administration. Parent and metabolite peak concentrations (Cmax) were not affected by food.
In a single-dose study with Loratadine rapidly disintegrating tablets in 24 subjects, the AUC of Loratadine was increased by 26% when administered without water compared to administration with water, while Cmax was not substantially affected. The bioavailability of descarboethoxyloratadine was not different when administered without water.
Approximately 80% of the total Loratadine dose administered can be found equally distributed between urine and feces in the form of metabolic products within 10 days. In nearly all patients, exposure (AUC) to the metabolite is greater than to the parent Loratadine. The mean elimination half-life in normal adult subjects (n = 54) were 8.4 hours (range = 3 to 20 hours) for Loratadine and 28 hours (range = 8.8 to 92 hours) for descarboethoxyloratadine. Loratadine and descarboethoxyloratadine reached steady state in most patients by approximately the fifth dosing day. There was considerable variability in the pharmacokinetic data in all studies of Loratadine tablets and syrup, probably due to the extensive first-pass metabolism.
In vitro studies with human liver microsomes indicate that Loratadine is metabolized to descarboethoxyloratadine predominantly to cytochrome P450 3A4 (CYP3A4) and, to a lesser extent, by cytochrome P450 2D6 (CYP2D6). In the presence of CYP3A4 inhibitor ketoconazole, Loratadine is metabolized to descarboethoxyloratadine predominantly by CYP2D6. Concurrent administration of Loratadine with either Ketoconazole, Erythromycin (both CYP3A4 inhibitors), or Cimetidine (CYP2D6 and CYP3A4 inhibitor) to healthy volunteers was associated with substantially increased plasma concentrations of Loratadine.
The pharmacokinetic profile of Loratadine in children in the 6 to 12 year age group is similar to that of adults. In a single dose pharmacokinetic study of 13 pediatric volunteers (aged 8 - 12 years) given 10 ml of Loratadine syrup containing 10 mg of Loratadine, the ranges of individual subject values of pharmacokinetic parameters (AUC and Cmax) were comparable to those following administration of a 10 mg tablet or syrup to adult volunteers.
For the relief of symptoms associated with seasonal allergic rhinitis, e.g. sneezing, rhinorrhea, itching as well as ocular itching and burning.
For the control of symptoms and signs of idiopathic chronic urticaria and other allergic dermatological disorders.
Adults and children are not less than 12 years: 1 tablet (10 mg) once daily.
Children 2 - 12 years: For body weights are more than 30 kg: 1 tablet (10 mg) once daily.
For body weights are not more than 30 kg: ½ tablet (5 mg) once daily.
Somnolence, tachycardia and headache have been reported with overdoses of Loratadine. A single acute ingestion of 160 mg produced no adverse effects. In the event of overdosage, treatment, which should be started immediately, is symptomatic and supportive.
Treatment: The patients should be induced to vomit even if emesis has occurred spontaneously. Pharmacologically induced vomiting by the administration of ipecac syrup is a preferred method. However, vomiting should not be induced in patients with impaired consciousness. The action of Ipecac is facilitated by physical activity and by the administration of 240 ml - 360 ml of water. If emesis does not occur within 15 minutes, the dose of Ipecac should be repeated. Precautions against aspiration must be taken, especially in children. Following emesis, adsorption of any drugs remaining in the stomach may be attempted by the administration of activated charcoal as slurry with water. If vomiting is unsuccessful or contraindicated, gastric lavage should be performed. Physiologic saline solution is the lavage solution of choice, particularly in children. In adults, tap water can be used; however, as much as possible, the amount of administered should be removed before the next instillation. Saline cathartics draw water into the bowel by osmosis and therefore may be valuable for their action in rapid dilution of bowel content.
Loratadine is not cleared by hemodialysis to any extent. After emergency treatment, the patient should continue to be clinically monitored.
Patients who have shown hypersensitivity or idiosyncrasy to any components of Loratadine.
Children are less than 2 years old.
Patients with severe liver impairment should be administered with a lower initial dose because they may have reduced clearance of Loratadine; an initial dose of 5 mg once daily or 10 mg every other day is recommended.
Use in Children: Efficacy of Loratadine in children less 2 years have not been established. However, the pharmacokinetic profile of Loratadine in infants 1 - 2 years after the administration of a single 2.5 mg dose of Loratadine syrup is similar to that in older children and adult.
Safe use of Loratadine products during pregnancy has not been established; therefore, use only if potential benefit justifies potential risk to fetus.
Since Loratadine is excreted in breast milk and because of the increased risk of antihistamine for infants, particularly newborns and premature infants, a decision should be made whether to discontinue nursing or discontinue the drug.
Loratadine has no clinically significant sedative properties at the daily recommended dose of 10 mg. Most commonly reported dose of 10 mg.
Most commonly reported adverse effects include fatigue, headache, somnolence, dry mouth, gastrointestinal disorders, e.g. nausea, gastritis and also allergic symptoms, i.e. rash.
During the marketing of Loratadine tablet, alopecia, anaphylaxis and abnormal hepatic function have been reported rarely.
In controlled pediatric clinical trials, the incidence of treatment related headache, sedation and nervousness, which were rarely reported events, was similar to that of placebo.
When administered concomitantly with alcohol, Loratadine has no potentiating effects as measured by psychomotor performance studies. Increase in plasma concentrations of Loratadine has 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 metabolism should be co-administered with caution until definitive interaction studies can be completed.
Drug/Laboratory test interaction: Loratadine products should be discontinued approximately 48 hours prior to skin testing procedures since antihistamines may prevent or diminish otherwise positive reactions to dermal reactivity indicators.
R06AX13 - loratadine ; Belongs to the class of other antihistamines for systemic use.
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