How Fexofenadine Compares as a Non-Sedating Antihistamine
Welcome to the Allergy, Asthma & Immunology Innovations podcast. In a new series called The Itch Review, co-hosts Kortney, Payel Gupta, MD, and Michael Blaiss, MD, discuss the latest asthma and allergy research. This episode reviews the article “Why fexofenadine is considered as a truly non-sedating antihistamine with no brain penetration: a systematic review”, published in Current Medical Research & Opinion in July 2024.
Our panel starts by comparing first-generation “old-school” antihistamines (diphenhydramine) to newer options (cetirizine, loratadine and fexofenadine). Then, we dive into a systematic review that evaluated more than 60 studies, including PET brain-scan trials, Proportional Impairment Ratio (PIR) tests, driving simulator trials, and quality-of-life surveys.
The researchers wanted to know: Does fexofenadine ever cross the blood–brain barrier and make you drowsy?
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Thank you to Opella for sponsoring this podcast episode.
Key takeaways on ‘Why fexofenadine won’t make you sleepy’
- First- vs. second-generation antihistamines. Old antihistamines like diphenhydramine (Benadryl®) cross into the brain and cause drowsiness. Newer ones like cetirizine, loratadine and fexofenadine do not cross the barrier as easily. This makes them less sedative.
- H1-receptor occupancy. Special PET scans take pictures of your brain. They found that fexofenadine blocks less than 1% of the spots that cause sleepiness.
- PIR test results. Objective and subjective tests found zero significant drowsiness or slowed thinking when on fexofenadine compared to placebo (sugar pill).
- Driving & pilot safety. Simulator and pilot studies showed that people drove and flew just as well as people on a placebo.
- Real-world benefits. Using fexofenadine showed fewer missed school/work days, and it is safe for kids to take.
Timestamps for our episode about allergies and antihistamines
01:26 – What are allergy medicines?
07:07 – Why old allergy pills can make you sleepy
07:56 – What’s a systematic review?
10:47 – Does fexofenadine get into your brain?
17:48 – How we measure drowsiness (PIR tests)
20:16 – How much fexofenadine is taken
21:44 – Looking at tests on thinking and movement
22:03 – Driving test: fexofenadine vs. Benadryl vs. alcohol
23:46 – Flying test: pilots taking fexofenadine
26:52 – Quick look at other studies
29:46 – Our big learnings
31:50 – Why we need different allergy medicines
32:37 – Why doctors warn about old allergy pills