bilastine

Action and Spectrum

Actions and Spectrum: 

Actions: 

bilastine acts as a potent and selective antagonist of histamine H1 receptors. By blocking these receptors, it inhibits the effects of histamine, which is released during allergic reactions. This action helps relieve symptoms associated with allergic rhinitis (such as sneezing, itching, nasal congestion, and rhinorrhea) and chronic urticaria (itching and hives). 

Spectrum: 

bilastine is primarily indicated for treating allergic rhinitis (seasonal or perennial) and chronic urticaria. However, it may also be effective in other allergic conditions, such as allergic conjunctivitis and pruritus associated with skin disorders. 

Drug Interaction

Adverse Reaction

Frequency defined 

1-10% 

Upper abdomen pain 

Dizziness 

Somnolence  

Headache 

Black Box Warning

Black Box Warning: 

None 

Contraindication / Caution

Contraindication/Caution: 

Contraindications: 

• Hypersensitivity 
• History of QT prolongation 

Cautions: 

• Advanced age or compromised immune system  
• Pre-existing medical conditions 
• Concurrent use of other medications 

Pregnancy / Lactation

Pregnancy consideration:  

Incomplete information is available regarding the use of bilastine during pregnancy. 

Breastfeeding warnings:  

No data is available regarding the secretion of the drug in breast milk. 

Pregnancy category: 

• Category A: well-controlled and Satisfactory studies do not show fetal risks in the first or later trimester.        
• Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women. 
• Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.       
• Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.        
• Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.        
• Category N: No data for the drug under this category is available. 

Pharmacology

Pharmacology: 

bilastine exerts its therapeutic effects by blocking the H1 receptors, which are present on various cells throughout the body, including those involved in allergic reactions. 

By blocking the H1 receptors, bilastine prevents the binding of histamine, a chemical released during allergic reactions, and reduces the symptoms associated with allergic conditions.

Pharmacodynamics: 

bilastine selectively blocks H1 receptors, inhibiting the effects of histamine released during allergic reactions. 

It has a high affinity for H1 receptors, explicitly targeting and binding them. 

bilastine has a long half-life, allowing for once-daily dosing and sustained symptom relief. 

Pharmacokinetics: 

Absorption 

bilastine is well absorbed orally, reaching peak blood concentrations within 1 to 1.5 hours after administration. Food does not significantly affect its absorption, so that it can be taken with or without food.  

Distribution 

bilastine has a moderate volume of distribution, indicating that it is distributed throughout the body’s tissues. It is highly bound to plasma proteins, primarily albumin. 

Metabolism 

bilastine is minimally metabolized in the liver by cytochrome P450 enzymes. The major metabolic pathway involves oxidative metabolism mediated by CYP3A4. The metabolites formed are pharmacologically inactive. 

Elimination and Excretion 

The elimination half-life of bilastine is around 14 to 15 hours in adults. It is primarily eliminated unchanged in the urine (around 70-80%) and, to a lesser extent, in the feces (around 10-12%).

Adminstartion

Administration: 

bilastine is administered orally, usually as tablets or oral suspension. The recommended dosage varies based on the indication and individual factors. The tablets should be swallowed whole with water and taken with or without food. The oral suspension should be shaken well before use, and the prescribed dose should be measured using the provided dosing device. 

Patient Information Leaflet

Patient information leaflet 

Generic Name:  bilastine 

Pronounced as: bi-lah-es-tin 

Why do we use bilastine? 

bilastine is indicated for the symptomatic treatment of allergic rhinitis, characterized by inflammation and irritation of the nasal passages because of an allergic reaction. It is also used to manage chronic idiopathic urticaria, a condition characterized by itchy, raised welts on the skin, also known as hives.