Bilastine

The European Union approved the selective histamine H1 receptor antagonist bilastine for the medication of allergic disorders. It functions by specifically inhibiting the body's H1 histamine receptors. It is used to treat urticaria, or elevated, itchy skin welts that can develop from a variety of causes and allergic rhinitis. It helps with nasal congestion, itching, running nose, and sneezing. The International Urticaria Guidelines propose using non-sedating second-generation H1-antihistamines, such as bilastine, as the first line of treatment for acute and chronic urticarial symptoms because of their safety profile.

BRAND NAMES:

Blexten: It is available in the form of Bilastine (20 mg) and this drug is used to treat seasonal allergic rhinitis and persistent spontaneous urticaria.

Blexten M: Blexten M available in the combination of Bilastine 20mg and Montelukast 10mg. It is used to treat several kinds of allergy disorders. It lowers inflammation (redness, irritation, heat, and swelling), itching and rashes by inhibiting specific chemical messengers in the body.

MECHANISM OF ACTION:

Bilastine is a selective histamine H1 receptor antagonist. Mainly in allergic reactions, the immune system releases lg-E antibodies, which bind the mast cells and destabilize them by releasing histamines and other inflammatory mediators. Bilastine helps bind the H1 receptors of mast cells, prevents destabilizing and releasing histamines, and provides symptomatic relief from allergies.

PHARMACOKINETICS:

Absorption: After oral administration, it takes 1.3 hours to reach its peak plasma concentration.

The mean value of oral bioavailability is 61%.

Distribution: Bilastine exhibits 14.53 hours of half-life estimated. The plasma protein binding is 84–90%.

Metabolism: It does not interact with cytochrome or undergo significant metabolism in humans.

Excretion: It is excreted mainly through feces (66.5%) and urine (28.3%).

PHARMACODYNAMICS:

Bilastine is a non-sedating drug that can reduce the symptoms caused by seasonal allergies. Bilastine inhibited histamine-induced wounds and nasal infections and was observed for 24 hours. Bilastine 20 mg was administered in patients with rhino conjunctivitis and followed for 24 days It was observed to be effective in reducing symptoms like sneezing, nasal discharge, nasal itching, nasal congestion, ocular tearing, and redness.

In chronic idiopathic urticarial, Bilastine 20 mg was administered once daily for 28 days, and it was observed that it is effective in relieving itching, curing wounds, and increasing sleep in patients.

DOSAGE AND ADMINISTRATION:

It can be orally administered for rhinitis allergies and urticaria and should be taken on an empty stomach to achieve optimal conditions for bilastine. In adults, a 20 mg dose per day was preferred for allergic rhinitis, and after reducing the symptoms of seasonal allergies, we can discontinue the treatment.

Children between 6 and 11 years weighing at least 20 kg can take 10 mg of oral solution or tablets for allergic rhinitis.

Adults can receive 20 mg for urticaria, depending on their condition. Children from 6 to 11 years old weighing at least 20 kg can take 10 mg per day by oral solution or tablets. If a dose is missed, take the next scheduled dose instead of an extra dose.

CONTRAINDICATIONS:

Hypersensitivity to bilastine or any excipients related to it.

DRUG INTERACTIONS:

Administrating bilastine along with drugs like ketoconazole, erythromycin, and cyclosporine

or diltiazem increases the concentration of bilastine. However, these changes do not affect the safety profile of any other medications. Intake of alcohol and bilastine shows psychomotor performance similar to that of alcohol placebo.

FOOD INTERACTIONS:

Avoid grapefruit juice and grapefruits.

ADVERSE EFFECTS:

• Gastrointestinal disorders like abdominal pain, nausea, diarrhea, dry mouth, and abdominal pain

• Increased appetite

• Headache

• Dizziness

• Anxiety

• Fatigue

• Muscular weakness

• Menstruation delayed

• Insomnia