Rinobil 12.5 mg/5 ml Oral Solution

Uses

Rinobil 12.5 mg/5 ml Oral Solution is used for symptomatic treatment of allergic rhino-conjunctivitis (seasonal and perennial) and urticaria.
Efficacy and safety of Rinobil 12.5 mg/5 ml Oral Solution 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 Rinobil 12.5 mg/5 ml Oral Solution should not be used in these age groups.

Rinobil 12.5 mg/5 ml Oral Solution is also used to associated treatment for these conditions: Chronic Spontaneous Urticaria, Seasonal Allergic Rhinitis

How Rinobil 12.5 mg/5 ml Oral Solution works

Rinobil 12.5 mg/5 ml Oral Solution is a selective histamine H1 receptor antagonist (Ki = 64nM) . During allergic response mast cells undergo degranulation which releases histamine and other subastances. By binding to and preventing activation of the H1 receptor, bilastine reduces the development of allergic symptoms due to the release of histamine from mast cells.

Dosage

Rinobil 12.5 mg/5 ml Oral Solution dosage

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 Rinobil 12.5 mg/5 ml Oral Solution (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 Rinobil 12.5 mg/5 ml Oral Solution tablet (1 tablet) once daily should be swallowed with water on an empty stomach to achieve optimal exposure to Rinobil 12.5 mg/5 ml Oral Solution.

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 Rinobil 12.5 mg/5 ml Oral Solution 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.

Side Effects

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.

Toxicity

The most common adverse effects experienced during clinical trials were abdominal pain, dizziness, headache, and somnolence . Rinobil 12.5 mg/5 ml Oral Solution is associated with Q/T prolongation. The no observed adverse effect level of bilastine is 1200 mg/kg/day in rats and 125 mg/kg/day in dogs .

Precaution

Co-administration of Rinobil 12.5 mg/5 ml Oral Solution and P-glycoprotein inhibitors (e.g. Ketoconazole, Erythromycin, Cyclosporine, Ritonavir or Diltiazem) should be avoided in patients with moderate or severe renal impairment.

Interaction

Concomitant intake of Rinobil 12.5 mg/5 ml Oral Solution and Ketoconazole or Erythromycin or Diltiazem increased C max of Rinobil 12.5 mg/5 ml Oral Solution. The psychomotor performance after concomitant intake of alcohol and Rinobil 12.5 mg/5 ml Oral Solution was similar to that observed after intake of alcohol and placebo. Concomitant intake of Rinobil 12.5 mg/5 ml Oral Solution and Lorazepam 3 mg for 8 days did not potentiate the depressant CNS effects of Lorazepam.

Food Interaction

• Avoid grapefruit products. Avoid other fruit juice as well for optimal absorption.
• Take on an empty stomach. Take at least two hours before or one hour after eating.

Elimination Route

Rinobil 12.5 mg/5 ml Oral Solution has a Tmax of 1.13 h . The absolute bioavailability is 61%. No accumulation observed with daily dosing of 20-100 mg after 14 days. Cmax decreased by 25 % and 33% when taken with a low fat and high fat meal compared to fasted state. Administration with grapefruit juice decreased Cmax by 30%.

Half Life

The mean half life of elimination is 14.5h .

Clearance

Rinobil 12.5 mg/5 ml Oral Solution has a total clearance is 9.20 L/h and a renal clearance of 8.7 L/h .

Elimination Route

Rinobil 12.5 mg/5 ml Oral Solution is mainly excreted in the feces (66.5%) with some excreted in the urine (28.3%) . Nearly all is excreted as the parent compound.

Pregnancy & Breastfeeding use

There are no or limited amount of data from the use of Rinobil 12.5 mg/5 ml Oral Solution 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 Rinobil 12.5 mg/5 ml Oral Solution during pregnancy. The excretion of Rinobil 12.5 mg/5 ml Oral Solution 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 Rinobil 12.5 mg/5 ml Oral Solution therapy for the mother.

Contraindication

Rinobil 12.5 mg/5 ml Oral Solution is contraindicated in patients with hypersensitivity to the active substance or to any of the excipients of the tablet.

Acute Overdose

In clinical trials, after administration of Rinobil 12.5 mg/5 ml Oral Solution 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.

Storage Condition

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

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