API Ebastine

Ebastine More Info

Ebastine is a second-generation non-sedating antihistamine mainly used to ease symptoms of allergic reactions. It works by blocking the activity of histamine — a chemical the body releases during an allergic response — which helps reduce common allergy-related discomfort.

1. Basic Information

Ebastine belongs to the chemical class of piperidine derivatives. Its CAS Number is 90729-43-4, with a molecular formula of C₃₂H₃₉NO₂ and a molecular weight of 469.66 g/mol.

2. Mechanism of Action

Ebastine itself is a prodrug, meaning it needs to be metabolized in the liver (mainly by the enzyme CYP3A4) to become its active form: ebastine carboxylic acid (carebastine). Carebastine then binds selectively to peripheral histamine H₁ receptors, stopping histamine from attaching to these receptors. This blocks histamine’s downstream effects, such as vasodilation (widening of blood vessels), increased vascular permeability (which causes swelling or edema), itching and skin rashes, and sneezing, runny nose, or itchy/watery eyes.

3. Main Uses

Clinically, ebastine is used to treat several allergic conditions:

Allergic rhinitis: It relieves symptoms like sneezing, nasal congestion, runny nose, and itching in the nose or throat.

Chronic idiopathic urticaria (CIU): It reduces itchy skin and hives (urticaria) that last 6 weeks or longer with no clear cause.

Other allergic skin conditions (e.g., allergic contact dermatitis): It eases itching and rash associated with these issues.

4. Key Features

Non-sedating: Unlike first-generation antihistamines (such as chlorpheniramine), ebastine barely penetrates the central nervous system. This means it rarely causes drowsiness — a big advantage for daily use, like during work or driving.

Long-acting: A single daily dose (usually 10mg) provides symptom relief for 24 hours, which makes it easier for patients to stick to their treatment.

Good tolerability: Common side effects are mild and short-lived, including headache, dry mouth, and abdominal discomfort. Severe adverse reactions (like liver dysfunction or allergic shock) are rare.

5. Precautions

Contraindications: People who are hypersensitive to ebastine or any excipients in its formulations should not use it.

Special populations:

Patients with severe liver impairment may need their dosage adjusted — always consult a healthcare provider first.

The safety of ebastine in pregnant or lactating women is not fully confirmed; use it only if recommended by a doctor.

Drug interactions: Avoid using ebastine with strong CYP3A4 inhibitors (e.g., ketoconazole, erythromycin). These drugs can increase ebastine levels in the body and raise the risk of side effects.

Formulations: Ebastine is available in different forms, including oral tablets, oral drops (for children), and fast-dissolving tablets (for patients who have trouble swallowing).

6. Market & Regulatory Notes

Ebastine is approved for medical use in most countries and regions (e.g., the EU, US, China) under various brand names (e.g., Kestine®).

Prescription vs. OTC status: In some regions, it is sold over-the-counter (OTC) for mild allergic symptoms. In others, it requires a doctor’s prescription — especially for chronic conditions like CIU.