Carebastine
| Carebastine.svg | |
Carebastine is a second-generation antihistamine that is used primarily in the treatment of allergic rhinitis and urticaria. It is the active metabolite of the prodrug ebastine, which is converted to carebastine in the liver. Carebastine is known for its selective antagonism of the H1 receptor, which helps alleviate symptoms associated with allergic reactions.
Pharmacology[edit | edit source]
Mechanism of Action[edit | edit source]
Carebastine works by selectively inhibiting the H1 histamine receptors. Histamine is a chemical mediator released during allergic reactions, and it binds to H1 receptors to cause symptoms such as itching, swelling, and vasodilation. By blocking these receptors, carebastine prevents histamine from exerting its effects, thereby reducing allergic symptoms.
Pharmacokinetics[edit | edit source]
After oral administration of ebastine, it is rapidly absorbed and undergoes extensive first-pass metabolism in the liver to form carebastine. Carebastine has a long half-life, which allows for once-daily dosing. It is highly protein-bound and is excreted primarily in the urine.
Clinical Use[edit | edit source]
Carebastine is indicated for the relief of symptoms associated with:
- Allergic rhinitis, including both seasonal and perennial types.
- Chronic idiopathic urticaria, which is characterized by persistent hives and itching.
Side Effects[edit | edit source]
Carebastine is generally well-tolerated, with a side effect profile similar to other second-generation antihistamines. Common side effects may include:
- Headache
- Drowsiness
- Dry mouth
Serious side effects are rare but can include hypersensitivity reactions.
Contraindications[edit | edit source]
Carebastine should not be used in individuals with known hypersensitivity to ebastine or any of its components. Caution is advised in patients with severe hepatic impairment due to the drug's metabolism in the liver.
Drug Interactions[edit | edit source]
Carebastine may interact with other medications that are metabolized by the cytochrome P450 system, particularly CYP3A4 inhibitors, which can increase the plasma concentration of carebastine.
Also see[edit | edit source]
References[edit | edit source]
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