Bilastin
Bilastin Uses, Dosage, Side Effects, Food Interaction and all others data.
Bilastin is a non-sedating, long-acting histamine antagonist with selective peripheral H 1 receptor antagonist affinity and no affinity for muscarinic receptors. Bilastin inhibits histamine-induced wheal and flare skin reactions for 24 hours following single doses.
Bilastin is an antiallergenic and acts to reduce allergic symptoms such as nasal congestion and urticaria .
Trade Name | Bilastin |
Generic | Bilastine |
Bilastine Other Names | Bilastina, Bilastine |
Weight | 20mg, 12.5mg/5ml |
Type | Tablet, Syrup |
Formula | C28H37N3O3 |
Weight | Average: 463.622 Monoisotopic: 463.283492063 |
Protein binding | Bilastine is 84-90% bound to human plasma proteins . |
Groups | Approved, Investigational |
Therapeutic Class | Non-sedating antihistamines |
Manufacturer | Popular Pharmaceuticals Ltd, |
Available Country | Bangladesh |
Last Updated: | September 19, 2023 at 7:00 am |
Uses
Bilastin is used for symptomatic treatment of allergic rhino-conjunctivitis (seasonal and perennial) and urticaria.
Efficacy and safety of Bilastin 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 Bilastin should not be used in these age groups.
Bilastin is also used to associated treatment for these conditions: Chronic Spontaneous Urticaria, Seasonal Allergic Rhinitis
How Bilastin works
Bilastin 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
Bilastin 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 Bilastin (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 Bilastin tablet (1 tablet) once daily should be swallowed with water on an empty stomach to achieve optimal exposure to Bilastin.
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 Bilastin 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 . Bilastin 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 Bilastin 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 Bilastin and Ketoconazole or Erythromycin or Diltiazem increased C max of Bilastin. The psychomotor performance after concomitant intake of alcohol and Bilastin was similar to that observed after intake of alcohol and placebo. Concomitant intake of Bilastin 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
Bilastin 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
Bilastin has a total clearance is 9.20 L/h and a renal clearance of 8.7 L/h .
Elimination Route
Bilastin 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 Bilastin 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 Bilastin during pregnancy. The excretion of Bilastin 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 Bilastin therapy for the mother.
Contraindication
Bilastin 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 Bilastin 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.
Innovators Monograph
You find simplified version here Bilastin
Bilastin contains Bilastine see full prescribing information from innovator Bilastin Monograph, Bilastin MSDS, Bilastin FDA label