Bilastine is a second-generation antihistamine which was developed in recent times and is primarily prescribed to relieve the symptoms of allergic conditions. Since its approval in the European Union and other countries, it has gained fame in terms of effectiveness and safety. To make it work in the body, the effects it may produce, and how to use it as a medicine, you must learn how it works in the body.
MECHANISM OF ACTION
Bilastine functions as a selective, competitive antagonist of the histamine H1 receptor:
Histamine Blockade: Allergens cause immune cells called mast cells to release histamine during an allergy response. Following this, histamine attaches to H1 receptors that are found all over the body, mostly in the blood vessels, skin, eyes, nose, and lungs. This bonding together causes the usual allergy signs and symptoms, like itching, coughing, and redness and swelling due to dilation and increased arterial permeability.
Selective Antagonism: Bilastine operates by attaching itself to these H1 receptors to a greater degree. By occupying the receptor sites, it literally stops histamine from connecting. This stops the receptor from being triggered, which stops the allergic symptoms that follow. Because it is very selective for the H1 receptor, it doesn't bind to other receptors like muscarinic, serotonin, or adrenergic receptors very well. This is why it doesn't cause many of the side effects that are common with first-generation antihistamines, like drowsiness, sedation, or dry mouth.
Studies also show that bilastine may stop the release of other pro-inflammatory cytokines and binding molecules from human mast cells and basophils. This could have an anti-allergic effect that goes beyond just blocking receptors.
PRIMARY USES
Bilastine is indicated for the treatment of symptoms associated with various allergic conditions in adults and children over 12 years of age. Its main uses include: Allergic Rhinoconjunctivitis: This includes both seasonal allergic rhinitis, also known as hay fever, and perennial allergic rhinitis, which are allergies that last all year and are caused by dust mites or pet hair inside the home. It can help with sneezing, runny nose, itchy nose, and eye problems like red, itchy, and watery eyes.
The typical dose is a single 20 mg tablet taken by mouth each day. An important part of taking it is that you have to do so on an empty stomach, either an hour or two hours after a meal. This is because food can make it less bioavailable and less effective when absorbed.
DRUG INTERACTIONS
Bilastine has a relatively low potential for clinically significant pharmacokinetic drug interactions due to its specific metabolic and excretion pathway. However, several important interactions must be considered.
P-gp Inhibitors: Certain medications have the ability to raise bilastine absorption by blocking the intestinal P-gp transporter and elevating its blood concentrations. Though it is not directly associated with toxicity, potent inhibitors such as ketoconazole, erythromycin, cyclosporine, and ritonavir are to be used with caution.
CNS Depressants: As with any antihistamine, taking it with other drugs that slow down the central nervous system, like alcohol, benzodiazepines, or opioids, could make you sleepier. This risk is much smaller with bilastine than with first-generation antihistamines, though, because it doesn't get very deeply into the brain.
Food and Fruit Juices: As noted, food severely reduces bilastine absorption. Taking bilastine with grapefruit juice is also not a good idea because it has chemicals in it that block both P-gp and CYP enzymes, which could change how bioavailable bilastine is.
In conclusion, bilastine is a powerful and specific non-sedative antihistamine that assists patients with hives and allergic rhinitis. A key clinical issue with it is that it must be consumed on an empty stomach. It does not interact with other drugs to the extent, yet it remains necessary to exercise caution when combining it with P-gp inhibitors. You must never use a new drug without consulting a doctor or a nurse in order to ascertain its safety.
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