What is levocetirizine?
Levocetirizin is the active enantiomer (left-turning form) of cetirizin and belongs to the second generation of antihistamines. It is used in allergic rhinitis (heuschnupfen), perennial rhinitis and chronic idiopathic urticaria.
With a dosage of only 5 mg, Levocetirizin achieves the same effectiveness as 10 mg of cetirizin, but with a tendingly more favorable side effect profile. Levocetirizin is available as a generic (e.g. Levocetirizin-ratiopharm®, Levocetirizin HEXAL®) and under the brand name Xusal®.
It is considered one of the most effective oral antihistamines and has a very rapid effect.
Active Ingredients & Mechanism of Action
Active ingredient: Levocetirizindihydrochlorid
Levocetirizin selectively blocks the H1 histamine receptors:
Active mechanism:
- High affinity blockade of peripheral H1 receptors
- Double receptor affinity compared to cetirizin (R-enantiomer is ineffective)
- inhibits histamine-mediated vasodilatation, edema formation and itching
- Additional anti-inflammatory properties
Pharmacokinetics:
- Fast resorption: Effect after 30–60 minutes
- High oral bioavailability (> 85 %)
- half-life: 7–10 hours
- duration of action: over 24 hours with one-time administration
Advantages:
- Fastest action under oral antihistamines
- High efficiency at low dose
- Lower sedation as cetirizin (because the seding R-enantiomer is missing)
Who is it suitable for?
Levocetirizin is suitable for:
- Adults and children from 6 years old with seasonal allergic rhinitis
- Patients with perennial (gance-year-old) allergic rhinitis
- Chronic idiopathic urticaria
Especially recommended at:
- Patients who need a very fast symptom relief
- If Cetirizin makes 10 mg too tired (Levocetirizin 5 mg often better tolerate)
- Strong allergic symptoms that require a potent antihistaminic
Not suitable:
- Children under 2 years
- Heavy renal insufficiency (Kreatinin-Clearance < 10 ml/min)
- hypersensitivity to levocetirizine, cetirizine or hydroxyzine
Available Dosages
Adults and young people aged 12:
- 5 mg once a day (a film tablet)
Children:
- 6–11 years: 5 mg once a day
- 2–5 years: 1.25 mg twice a day (as drops)
Available dosage forms:
- 5 mg film tablets
- Drop to take (for children)
Dosis adjustment for kidney failure:
- Light (CrCl 50–79): 5 mg daily
- Moderate (CrCl 30–49): 5 mg every 2 days
- Heavy (CrCl 10–29): 5 mg every 3 days
- Dialysis: contraindicated
How to Take
Intake:
- Once a day, preferably in the evening (with slight fatigue)
- Regardless of meals (food delays admission easily)
- Swallow film tablet with water
- drops directly into the mouth or on a spoon
Important notes:
- Regular intake for optimal effect
- In case of tiredness: transfer to the evening
- Alcohol can strengthen the sedative effect – Careful
- Not together with other sedative drugs
Application duration:
- Seasonal allergy: During pollen flight time
- Perennial allergy: all year after medical recommendation
- Urtikaria: Up to symptom freedom
Contraindications
**Levocetirizin may not be taken at:* *
- hypersensitivity to levocetirizine, cetirizine or hydroxyzine
- Heavy renal insufficiency (Kreatinin-Clearance < 10 ml/min)
- dialysis-prone kidney failure
Preview at:
- Restricted kidney function (dose adjustment required)
- Epilepsy or increased cramp readiness
- Simultaneous alcohol consumption
- Predisposition for urine retention (e.g. spinal cord lesion, prostate hyperplasia)
pregnant and breastfeeding: No sufficient data for use in pregnancy. Go to breast milk. In pregnancy and breastfeeding only after medical consultation.
Possible Side Effects
Family (1–10 %):
- Headaches
- Sleepiness/ fatigue (less than Cetirizin)
- Mouth dryness
- Fatigue
** Occasionally (0.1-1 %):* *
- stomach pain
- nausea
- Squeeze
- visual disorders
- Palpitations
Selten:
- Weight gain
- Sensitivity reactions
- Crampfans
- Liver malfunction
- Aggression, agitation
** Compared to cetirizine 10 mg, the sedation rate at levocetirizine is 5 mg somewhat lower, since the inactive R-enantiomer is lacking.
Interactions
Preview with simultaneous use of:
- Alcohol (reinforced sedation possible)
- Other CNS-damping substances (benzodiazepines, opioids)
- Theophylline (light inhibition of levocetirizine clearance)
- Ritonavir (can increase Levocetirizin levels)
No relevant interaction with:
- Pseudoephedrine
- Food (light delay, but no loss of effect)
- CYP-enzyme-dependent medications (minimal CYP metabolism)
** Levocetirizin has a relatively favorable interaction profile since it is hardly hepatically metabolized and is mainly renal excreted.
Frequently Asked Questions
Similar Medications
Is levocetirizine right for you?
A licensed doctor will review your information and issue a prescription if suitable. Discreet and secure.
Important Notice
This information does not replace medical advice. If you have questions about your health or the suitability of this medication, please consult a doctor or pharmacist.
Important Safety Information
This service operates under German pharmaceutical law (HWG). For risks and side effects, read the package leaflet and consult your doctor or pharmacist. All medications are dispensed from a licensed pharmacy in Germany.