Generic
Bilastine
70 brands available in the market
At a glance
Bilastine is an antihistamine medication used in the treatment of allergy symptoms such as itching, swelling, and rashes. It blocks the effects of histamine in the body, providing relief from allergic symptoms.
Description
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 high concentrations, it does not show affinity for 30 other receptors including muscarinic, serotonergic, dopaminergic and noradrenergic receptors.
Bilastine is indicated for the symptomatic treatment of allergic rhinoconjunctivitis (seasonal and perennial) and urticaria. It also relieves symptoms of hay fever such as sneezing, itching, runny nose, blocked nose, and red and watery eyes.
Indications
- Allergic rhinoconjunctivitis (seasonal and perennial)
- Urticaria
- Hay fever
Therapeutic class
Non-sedating Antihistamine
Pharmacological class
H1 Receptor Antagonist
Pharmacology
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 high concentration, it does not show affinity for 30 other receptors including muscarinic, serotonergic, dopaminergic and noradrenergic receptors, or for other histamine receptor subtypes (H2, H3 and H4). Bilastine does not undergo any metabolism to be active. It is excreted by feces (66.35%) and urine (28.31%).
Mechanism of action
Bilastine is a selective H1 receptor antagonist. During allergic response, mast cells undergo degranulation which releases histamine and other substances. 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
Adults & adolescents (12 years and over): 20 mg tablet once daily, swallowed with water on an empty stomach. Maximum recommended daily dose is 20 mg (1 tablet) and should not be exceeded.
Children 6-11 years: 10 mg mouth dissolving tablet once daily. Place in mouth; it disperses rapidly in saliva and can be easily swallowed. Alternatively, it can be dispersed in a teaspoon of water before swallowing.
Children 2-11 years (syrup): 4 ml once daily.
Renal impairment: No dosage adjustment necessary in patients with renal impairment.
Hepatic impairment: Changes in liver function are not expected to have a clinically relevant influence.
Children under 2 years: Safety and efficacy not established; should not be used.
Administration
Take on an empty stomach (1 hour before or 2 hours after food) with water. Swallow the tablet whole. Do not chew, crush or break it. For mouth dissolving tablets, place in mouth to disperse in saliva or disperse in a teaspoon of water before swallowing.
Missed dose
If you miss a dose, take the next scheduled dose. Do not take an extra dose.
Side effects
Most commonly reported side effects in clinical trials: headache, dizziness, somnolence (drowsiness), and fatigue. These adverse events occurred with comparable frequency in patients receiving placebo.
Precautions & warnings
- Bilastine does not generally affect driving performance, but very rarely some people may experience drowsiness which could affect their ability to drive or use machines.
- Stop taking Bilastine at least three days before taking an allergy test as it can affect the test results.
- Be cautious while driving or doing anything that requires concentration as it may cause dizziness and sleepiness.
- Do not drink alcohol while taking this medication as it may cause increased sleepiness.
Contraindications
Hypersensitivity to the active substance or to any of the excipients of the tablet.
Drug interactions
- Concomitant use with ketoconazole, erythromycin, cyclosporine or diltiazem increases bilastine concentration, but these changes do not affect the safety profile of any of the drugs.
- Alcohol and 20 mg bilastine show similar psychomotor performance to alcohol and placebo.
- Concomitant intake of bilastine 20 mg and lorazepam 3 mg for 8 days did not potentiate the depressant CNS effects of lorazepam.
Food interactions
Caution is advised when consuming alcohol with Bilastine as it may increase sleepiness. Food interaction: Take 1 hour before or 2 hours after food. Avoid fruit juice.
Use in pregnancy
There are limited data on the use of Bilastine during pregnancy. Animal studies do not indicate direct or indirect harmful effects. As a precautionary measure, it is preferable to avoid use during pregnancy.
Pregnancy Category: B — always consult a doctor before taking during pregnancy.
Use in lactation
The excretion of Bilastine in human milk has not been studied. A decision must be made considering the benefit of breastfeeding for the child and the benefit of Bilastine therapy for the mother.
Pediatric use
Efficacy and safety in children under 2 years have not been established; clinical experience in children aged 2-5 years is limited, therefore Bilastine should not be used in these age groups.
Geriatric use
Elderly patients (≥65 years) showed no difference in efficacy or safety compared to younger patients.
Renal / hepatic impairment
Hepatic impairment: Bilastine is not metabolized in humans. Changes in liver function are not expected to have a clinically relevant influence.
Overdose effects
In clinical trials, at doses 10-11 times therapeutic dose (220 mg single dose; or 200 mg/day for 7 days), treatment-emergent adverse events were two times higher than placebo. Most frequently reported: dizziness, headache, nausea. No serious adverse events or significant QTc prolongation reported.
Storage conditions
Store below 30°C, protected from light and moisture. Keep out of reach of children.
Chemical structure
Molecular Formula: C₂₈H₃₇N₃O₃