Ebastine

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Ebastine: a clear, low-sedating antihistamine for allergy relief

What it is
- Ebastine is a second‑generation antihistamine used to treat allergic rhinitis (hay fever) and chronic idiopathic urticaria (hives).
- It is designed to cause little drowsiness because it doesn’t enter the brain in significant amounts.

How it works
- Ebastine blocks histamine H1 receptors in peripheral tissues, reducing allergy symptoms.
- It has few central (brain) side effects, so sedation is uncommon.

How it’s used
- Available as 10 mg and 20 mg tablets, fast-dissolving tablets, and a syrup for children.
- Typical daily dose is 10–20 mg, adjusted to how severe the condition is.

Pharmacokinetics (how the body processes it)
- After swallowing, ebastine is converted in the liver by the CYP3A4 enzyme into its active metabolite, carebastine.
- The active metabolite has a half-life of about 15–19 hours.

Safety and side effects
- Generally safe and well tolerated; most side effects are similar to placebo.
- No significant cognitive impairment or sedation; no QT prolongation reported.
- Data on pregnancy safety in humans are limited, and it’s not clear whether ebastine passes into breast milk.

Brand names
- Sold under many brand names worldwide (examples include Kestine and other local names).

History
- Patented in 1983 and brought into medical use in 1990.
- Often provided in micronised form to improve solubility.