Pharmacology Easy

Cetirizine

Remember the name – CETI → settee, the sofa
CETIRIZINE can still land you on the SETTEE — it is the sleepiest of the modern antihistamines.
It crosses into the brain a little more than loratadine or fexofenadine, and sedates roughly one person in ten. For someone who drives for a living, choose another.
Mnemonic: Second generation stays out of the brain
Cetirizine blocks the same H1 receptor as diphenhydramine but barely crosses the blood-brain barrier, so it treats the allergy without the sedation. Of the second-generation drugs it is the most likely to cause some drowsiness.
The mechanism comic and the patient case for Cetirizine are in the app: four panels that show what the drug does in the body, and a short patient story with the practice pearl that goes with it.

Side effects

Common: drowsiness, dry mouth, fatigue

Serious:

Typical dose

10 mg once daily

5 mg is a reasonable starting dose if drowsiness matters. Halve it in renal impairment.

Check yourself

Why does cetirizine cause less sedation than diphenhydramine?

  1. It crosses the blood-brain barrier poorly, so it reaches few central H1 receptors
  2. It blocks a completely different receptor
  3. It is taken at a much lower dose
  4. It is broken down before it reaches the blood
Show answer

A. It crosses the blood-brain barrier poorly, so it reaches few central H1 receptors

Both block H1. Sedation comes from blocking H1 in the brain, and the second-generation drugs are designed not to get there. Cetirizine crosses a little more than loratadine does, which is why it is the drowsiest of the modern ones.

See it, don't memorize it

The app has the mechanism comic and a patient case for Cetirizine – plus the name link, the class mnemonic, pronunciation you can hear, and a self-check, for the top 100 drugs. One purchase, no subscription, no account.

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