Chemical formula: C₂₁H₂₅ClN₂O₃ Molecular mass: 388.89 g/mol PubChem compound: 1549000
Levocetirizine interacts in the following cases:
The dosing intervals must be individualised according to renal function. Refer to the following table and adjust the dose as indicated. To use this dosing table, an estimate of the patient’s creatinine clearance (CLcr) in ml/min is needed.
The CLcr (ml/min) may be estimated from serum creatinine (mg/dl) determination using the following formula:
CLcr = [140 – age (years)] x weight (kg) / 72 x serum creatinine (mg/dl) (x 0.85 for women)
Dosing adjustments for patients with impaired renal function:
| Group | Creatinine clearance (ml/min) | Dosage and frequency |
|---|---|---|
| Normal | ≥80 | 5 mg once daily |
| Mild | 50–79 | 5 mg once daily |
| Moderate | 30–49 | 5 mg once every 2 days |
| Severe | <30 | 5 mg once every 3 days |
| End-stage renal disease-Patients undergoing dialysis | <10 | Contra-indicated |
In paediatric patients suffering from renal impairment, the dose will have to be adjusted on an individual basis taking into account the renal clearance of the patient and his body weight. There are no specific data for children with renal impairment.
Precaution is recommended with concurrent intake of alcohol. In sensitive patients, the concurrent administration of cetirizine or levocetirizine and alcohol or other CNS depressants may cause additional reductions in alertness and impairment of performance.
In a multiple dose study of ritonavir (600 mg twice daily) and cetirizine (10 mg daily), the extent of exposure to cetirizine was increased by about 40% while the disposition of ritonavir was slightly altered (-11%) further to concomitant cetirizine administration.
A small decrease in the clearance of cetirizine (16%) was observed in a multiple dose study with theophylline (400 mg once a day); while the disposition of theophylline was not altered by concomitant cetirizine administration.
Caution should be taken in patients with epilepsy and patients at risk of convulsion as levocetirizine may cause seizure aggravation.
Response to allergy skin tests are inhibited by antihistamines and a wash-out period (of 3 days) is required before performing them.
Caution should be taken in patients with predisposing factors of urinary retention (e.g. spinal cord lesion, prostatic hyperplasia) as levocetirizine may increase the risk of urinary retention.
There are no or limited amount of data (less than 300 pregnancy outcomes) from the use of levocetirizine in pregnant women. However, for cetirizine, the racemate of levocetirizine, a large amount of data (more than 1000 pregnancy outcomes) on pregnant women indicate no malformative or feto/neonatal toxicity. Animal studies do not indicate direct or indirect harmful effects with respect to pregnancy, embryo/fetal development, parturition or postnatal development.
The use of levocetirizine may be considered during pregnancy, if necessary.
Cetirizine, the racemate of levocetirizine, has been shown to be excreted in human. Therefore, the excretion of levocetirizine in human milk is likely. Adverse reactions associated with levocetirizine may be observed in breastfed infants. Therefore, caution should be exercised when prescribing levocetirizine to lactating women.
For levocetirizine no clinical data are available.
Comparative clinical trials have revealed no evidence that levocetirizine at the recommended dose impairs mental alertness, reactivity or the ability to drive.
Nevertheless, some patients could experience somnolence, fatigue and asthenia under therapy with levocetirizine. Therefore, patients intending to drive, engage in potentially hazardous activities or operate machinery should take their response to the medicinal product into account.
In therapeutic studies in women and men aged 12 to 71 years, 15.1% of the patients in the levocetirizine 5 mg group had at least one adverse drug reaction compared to 11.3% in the placebo group. 91.6 % of these adverse drug reactions were mild to moderate.
In therapeutic trials, the dropout rate due to adverse events was 1.0% (9/935) with levocetirizine 5 mg and 1.8% (14/771) with placebo.
Clinical therapeutic trials with levocetirizine included 935 subjects exposed to the medicinal product at the recommended dose of 5 mg daily. From this pooling, following incidence of adverse drug reactions were reported at rates of 1% or greater (common: ≥1/100 to <1/10) under levocetirizine 5 mg or placebo:
Further uncommon incidences of adverse reactions (uncommon ≥1/1000 to <1/100) like asthenia or abdominal pain were observed.
The incidence of sedating adverse drug reactions such as somnolence, fatigue, and asthenia was altogether more common (8.1%) under levocetirizine 5 mg than under placebo (3.1%).
In two placebo-controlled studies in paediatric patients aged 6-11 months and aged 1 year to less than 6 years, 159 subjects were exposed to levocetirizine at the dose of 1.25 mg daily for 2 weeks and 1.25 mg twice daily respectively. The following incidence of adverse drug reactions was reported at rates of 1% or greater under levocetirizine or placebo.
Even if clinical data presented in this section are available in children aged 6 months to 12 years, we do not have sufficient data to support the administration of the product to infants and toddlers aged less than 2 years.
Adverse reactions from post-marketing experience are per System Organ Class and per frequency. The frequency is defined as follows: very common (≥1/10); common (≥1/100 to <1/10); uncommon (≥1/1,000 to <1/100); rare (≥1/10,000 to <1/1,000); very rare (<1/10,000), not known (cannot be estimated from the available data).
Not known: hypersensitivity including anaphylaxis
Not known: increased appetite
Not known: aggression, agitation, hallucination, depression, insomnia, suicidal ideation, nightmare
Not known: convulsion, paraesthesia, dizziness, syncope, tremor, dysgeusia
Not known: vertigo
Not known: visual disturbances, blurred vision
Not known: palpitations, tachycardia
Not known: dyspnoea
Not known: nausea, vomiting, diarrhoea
Not known: hepatitis
Not known: dysuria, urinary retention
Not known: angioneurotic oedema, fixed drug eruption, pruritus, rash, urticaria
Not known: myalgia, arthralgia
Not known: oedema
Not known: weight increased, abnormal liver function tests
Methyl parahydroxybenzoate and propyl parahydroxybenzoate may cause allergic reactions (possibly delayed).
After levocetirizine discontinuation, pruritus has been reported.
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