Opexa Tablet

Opexa is indicated for the symptomatic treatment of-

• Allergic rhino conjunctivitis (seasonal and perennial) and
• Urticaria

Opexa is also used to relieve the symptoms of hay fever (sneezing, itchy, runny, blocked-nose and red and watery eyes).

Bilastine is a potent, effective, non-sedating, long-acting histamine antagonist with selective & high affinity to H1 receptor (3 times higher than Cetirizine and 5 times higher than Fexofenadine). Even at a high concentration, Bilastine does not show affinity for the 30 other receptors including muscarinic, serotonergic, dopaminergic and noradrenergic receptors, for the other histamine receptor subtypes (H2, H3 and H4). It shows excellent safety profile and very favorable pharmacokinetic characteristics. Bilastine doesn’t undergo any metabolism to be active. Bilastine is excreted by feces (non -systemic) & urine (systemic) approximately 66.35% & 28.31% respectively.

Adults & adolescents (12 years of age and over): 20 mg tablet once daily for symptomatic relief of allergic rhinitis, urticaria and allergic rhinoconjunctivitis. The maximum recommended daily dose is 20 mg Bilastine (1 tablet) and should not be exceeded. If a dose is missed, the next scheduled dose should be taken. An extra dose should not be taken. 20 mg Bilastine tablet (1 tablet) once daily should be swallowed with water on an empty stomach to achieve optimal exposure to Bilastine.

Children between 6 to 11 years: 10 mg mouth dissolving tablet for the symptomatic relief of allergic rhinitis, allergic rhinoconjunctivitis and urticaria. The Mouth dissolving tablet is for oral use only. It should be placed in the mouth. It will disperse rapidly in saliva and can be easily swallowed. Alternatively, the mouth dissolving tablet can be dispersed in a tea spoon of water before being swallowed by the children. The maximum recommended daily dose for children in between 6 to 11 years is 10 mg Bilastine mouth dissolving tablet (1 tablet) and should not be exceeded. If a dose is missed, the next scheduled dose should be taken. An extra dose should not be taken.

Children between 2 to 11 years: 4 ml once daily.

Concomitant use of Opexa with ketoconazole, erythromycin, cyclosporine or diltiazem increases the concentration of Opexa. But these changes do not appear to affect the safety profile of any of the drugs. Intake of alcohol and 20 mg Opexa shows same psychomotor performance similar to that of alcohol and placebo. Concomitant intake of Opexa 20 mg and lorazepam 3 mg for 8 days did not potentiate the depressant CNS effects of lorazepam.

Bilastine is contraindicated in patients with hypersensitivity to the active substance or to any of the excipients of the tablet.

The most commonly reported side effects in clinical trial are headache, dizziness, somnolence and fatigue. These adverse events occurred with a comparable frequency in patients receiving placebo.

There are no or limited amount of data from the use of Bilastine in pregnant women. Animal studies do not indicate direct or indirect harmful effects with respect to reproductive toxicity, parturition or postnatal development. As a precautionary measure, it is preferable to avoid the use of Bilastine during pregnancy. The excretion of Bilastine in milk has not been studied in humans. A decision must be made taking into account the benefit of breast-feeding for the child and the benefit of Bilastine therapy for the mother.

Treatment with Opexa 20 mg does not affect the driving performance. However, patients should be informed that very rarely some people experience drowsiness, which may affect their ability to drive or use machines. In clinical trials elderly patients (≥65 years) showed no difference in effcacy or safety with respect to younger patients. The maximum plasma concentration of Opexa after administration of 20 mg in patients with severe renal impairment is below the safety threshold of most common adverse e?ects and cardiac or CNS safety. No dosage adjustment is necessary in patients with renal impairment. Opexa is not metabolized in human. Since renal elimination is the major excretion, biliary excretion is expected to be only marginally involved in the elimination of Opexa. Changes in liver function are not expected to have a clinically relevant influence.

Efficacy and safety of Opexa in children under 2 years of age have not been established and there is little clinical experience in children aged 2 to 5 years, therefore Opexa should not be used in these age groups.

In clinical trials, after administration of Opexa at doses 10 to 11 times the therapeutic dose (220 mg as single dose; or 200 mg/day for 7 days) frequency of treatment-emergent adverse events was two times higher than with placebo. The adverse reactions most frequently reported were dizziness, headache and nausea. No serious adverse events and no significant prolongation in the QTc interval were reported.

Non-sedating antihistamines

Keep below 30°C temperature, protected from light and moisture. Keep out of reach of children.

Molecular Formula :	C28H37N3O3
Chemical Structure :