LORADINE Tablet

Relief of symptoms associated with allergic rhinitis e.g. sneezing, nasal discharge and itching, as well as ocular itching and burning. Chronic urticaria and other allergic dermatologic disorders.

Dosage and Administration

Adults and children ≥12 years: 1 tablet daily.

In patients who have shown hypersensitivity or idiosyncrasy to their component.

The incidence of most commonly reported adverse effects - fatigue, sedation and headache associated with loratadine tablets has been comparable to that of placebo. In trials, loratadine has shown no clinically significant sedative or anticholinergic properties. During the marketing of loratadine, alopecia has been reported.

1. When administered concomitantly with alcohol, loratadine has no potentiate effects as measured by psychomotor performance studies.

2. Ketoconazole, erythromycin, and cimetidine may increase plasma-loratadine concentration, but without clinically significant changes (including electrocardiographic).

3. Plasma concentration of loratadine possibly increased by amprenavir.

4. Other drugs known to inhibit hepatic metabolism should be co-administered with caution until definitive interaction studies can be completed.

Pregnancy

There are no adequate and controlled studies to date using loratadine in pregnancy women, so it should be used during pregnancy only when the potential benefits justify the possible risks to the fetus.

Lactation

Caution should be exercised when loratadine is administered in a nursing woman because it is distributed readily into breast milk. Due to the increased risk of antihistamines for infants, particularly newborns and premature infants, a decision should be made whether to discontinue nursing or discontinue the drug.

1. Patients with severe liver impairment or renal impairment (creatinine clearance<30mL/min) should be administered a lower initial dose because they may have reduced clearance of loratadine, an initial dose of 5mg once daily or 10mg every other day is recommended.

2. Safety and efficacy of loratadine in children < 2years have not been established yet.

3. Although drowsiness is rare, nevertheless patients should be advised that it can occur and may affect skilled tasks (e.g. driving).

1. Antihistamine used in the treatment of allergy acts by competing with histamine for H1-receptor sites on effector cells.

2. The anticholinergic actions of most antihistamines provide a drying effect in the nasal mucosa, but loratadine has no significant anticholinergic activity.

3. Loratadine is a long-acting antihistamine. It has been characterized as a specific, selective peripheral H1-receptor antagonist and has been referred to as a relatively “non-sedating” or second generation antihistamine.

4. Following single administration, loratadine exhibits antihistamines effects beginning within 1/2-1 hour, reaching a maximum at 8-10 hours, and lasting in excess of 24 hours.

5. Distribution of loratadine has not been fully characterized. Protein binding of loratadine is about 97-99%. It appears to distribute poorly or not appreciably into the CNS at usual dosage. Small amount of it appears to be distributed into milk. The mean elimination half-life is 7-11 hours.

6. Loratadine undergoes extensive metabolism by CYP450. The major metabolite, descarboethoxyloratadine (desloratadine) has potent antihistamine activity. Most of a dose is excreted equally in the urine and faeces, mainly in the form of metabolites.