Rupastin 10 mg Tablet

Rupastin 10 mg Tablet

DESCRIPTION

Rupastin (Rupatadine) is a second generation, non-sedating, long-acting histamine antagonist with selective peripheral H1 receptor antagonist activity. It further blocks the receptors of the platelet-activating factor (PAF) according to in vitro and in vivo studies. Both histamine and PAF cause bronchoconstriction which leads to an increase in the vascular permeability and act as a mediator in the inflammatory process.

Rupastin (Rupatadine) possesses anti-allergic properties such as the inhibition of degranulation of mast cells induced by immunological and non-immunological stimuli, and inhibition of the release of cytokines, particularly of the Tumor Necrosis Factor (TNF α) in human mast cells and monocytes. Rupastin (Rupatadine) shows high H1 receptor affinity and little or no activity on other CNS receptors. It also has a very long side chain and little liposolubility; therefore, there is little or no crossing of the blood-brain barrier. These properties account for the observed lack of sedation.

COMPOSITION

Each tablet contains Rupatadine Fumarate INN equivalent to Rupatadine 10 mg.

INDICATION

Rupastin (Rupatadine) is indicated for the symptomatic treatment of seasonal and perennial allergic rhinitis such as sneezing, runny nose, itching in the eyes and nose and urticaria (an allergic skin rash) such as itching and hives (localised skin redness and swelling) in adults and adolescents (over 12 years of age).

DOSAGE AND ADMINISTRATION

™ Adults and adolescents (above 12 years) - 10 mg (one tablet) once daily, with or without food.

™ Elderly - Rupastin (Rupatadine) should be used with caution in elderly. No information is available that indicates the requirement of any dose adjustment in this population.

™ Children - Neither the safety nor the efficacy of Rupastin (Rupatadine) has been established in patients less than 12 years of age.

™ Patients with renal or hepatic insufficiency - Use of Rupastin (Rupatadine) is not recommended in patients with renal or hepatic insufficiency, as no relevant clinical data is available.

OR, AS DIRECTED BY THE PHYSICIAN.

SIDE EFFECTS

The most common undesirable effects associated with Rupatadine use in controlled clinical studies were somnolence (9.5%), headache (6.9%) and fatigue (3.2%). Other common undesirable effects include dizziness, dry mouth and asthenia.

CONTRAINDICATION

The use of Rupastin (Rupatadine) is contraindicated in patients with hypersensitivity to any of the component of this product.

SPECIAL PRECAUTIONS

Administration of a dose of 10 mg daily of Rupatadine has not shown significant effects on the function of the central nervous system as seen in specific studies done for psychomotor function. Nevertheless, the patient should take precaution in driving or managing machines.

USE IN PREGNANCY AND LACTATION

Pregnancy Category is B2. Data on a limited number of exposed pregnancies indicates no adverse effects of Rupatadine on pregnancy or on the health of the foetus/newborn child. Animal studies do not indicate direct or indirect harmful effects with respect to pregnancy, embryonal/foetal development, parturition or postnatal development. Clinical data for Rupatadine or other compounds of the class are inadequate to establish safety in pregnancy. No information is available, whether Rupatadine is excreted in the mother’s milk. Therefore, it should not be used during pregnancy and lactation, unless the potential benefits for the mother justify the potential risk to the infant.

DRUG INTERACTION

CYP3A4 inhibitors like Erythromycin and Ketoconazole inhibits both the presystemic and systemic metabolism of Rupatadine, increasing about 10-fold the exposure of unchanged drug and decreasing the exposure of metabolites. Due to this potential interaction, it is not recommended to use Rupatadine in combination with Ketoconazole, macrolides or any other inhibitors of CYP3A4. Co-administration of

Rupatadine and CNS depressants or alcohol may increase CNS depressant effect.

Supply

Each box contains 3X10 tablets in blister strips.