Levocetirizine Tablets

What is Levocetirizine?

Levocetirizine is a modern, non-sedating antihistamine medication belonging to the second-generation H1 receptor antagonist class. It contains the active ingredient levocetirizine dihydrochloride, which is the purified active enantiomer (R-enantiomer) of cetirizine. This refinement means levocetirizine provides targeted histamine blockade with potentially fewer side effects than its parent compound.

Mechanism of Action

Think of histamine as a key that fits into specific locks (H1 receptors) on your cells, triggering allergy symptoms like itching, sneezing, and inflammation. Levocetirizine works by blocking these receptor "locks" so the histamine "key" cannot activate them. This prevents the allergic reaction cascade while having minimal effect on other bodily systems, reducing the likelihood of sedation compared to older antihistamines.

Biologically, levocetirizine competitively antagonizes peripheral H1 receptors with high affinity and specificity. It has minimal anticholinergic effects and does not readily cross the blood-brain barrier at therapeutic doses, which contributes to its favorable side effect profile. The medication begins working within 1 hour of administration, with peak effects occurring at 1-2 hours and lasting for approximately 24 hours.

What is Levocetirizine Used For?

Levocetirizine is clinically approved for the symptomatic treatment of two main allergic conditions:

Before Using Levocetirizine

Before starting levocetirizine, discuss the following with your healthcare provider:

Medical History Assessment Checklist

• ❑ Allergy history: Known hypersensitivity to levocetirizine, cetirizine, hydroxyzine, or any tablet ingredients
• ❑ Kidney function: Any history of renal impairment or current kidney disease
• ❑ Liver function: History of liver disease or hepatic impairment
• ❑ Epilepsy/Seizures: Personal or family history of convulsive disorders
• ❑ Urinary issues: Difficulty urinating, prostate enlargement, or spinal cord lesions
• ❑ Other conditions: Glaucoma, cardiovascular disease, phenylketonuria

Required Baseline Considerations

While routine blood tests are not mandatory before starting levocetirizine, your clinician may recommend:

• Renal function assessment (especially in elderly patients or those with suspected kidney issues)
• Evaluation of current allergy symptoms and triggers
• Review of all current medications including over-the-counter products

Levocetirizine Contraindications

Special Population Considerations

Elderly Patients (65 years and above)

No dose adjustment is routinely required for elderly patients with normal renal function. However, age-related decline in kidney function is common, so renal function should be assessed. If creatinine clearance is 30-50 mL/min, the dose should be reduced to 5mg every other day. If <30 mL/min, use is contraindicated unless under specialist supervision.

Renal Impairment

Hepatic Impairment

Patients with isolated hepatic impairment (normal kidney function) can take the usual 5mg daily dose. Those with combined hepatic and renal impairment require dose reduction based on their renal function level.

Paediatric Population

Levocetirizine 5mg film-coated tablets are NOT recommended for children under 6 years. For children aged 6-12 years, the standard dose is 5mg once daily, but a lower dose may be considered based on body weight and renal function. Alternative formulations (oral solution) may be more appropriate for dose adjustment in children.

Levocetirizine and Other Medicines

Inform your doctor about ALL medications you take, including prescription, over-the-counter, herbal supplements, and recreational drugs.

High-Risk Medication Combinations

• CNS Depressants: Enhanced sedative effects when combined with alcohol, benzodiazepines, opioids, sleeping tablets, or other sedating medications
• Anticholinergic Drugs: Potential additive effects with tricyclic antidepressants, antipsychotics, antispasmodics
• Theophylline: May slightly reduce levocetirizine clearance (monitor for increased side effects)
• Ritonavir: This HIV medication may increase levocetirizine levels

Timing Recommendations

While levocetirizine can generally be taken with other medications, consider these timing suggestions:

• Take levocetirizine at least 2 hours apart from antacids containing aluminum or magnesium
• If taking multiple sedating medications, take levocetirizine at bedtime to minimize daytime drowsiness
• No specific timing requirements with most other medications

Pregnancy & Breastfeeding

Pregnancy

Animal studies show no direct teratogenic effects, but human data is limited. Levocetirizine should only be used during pregnancy if clearly needed and after careful risk-benefit assessment by a healthcare professional. If you become pregnant while taking levocetirizine, inform your doctor immediately.

Breastfeeding

Levocetirizine is excreted in human milk at low concentrations. Use during breastfeeding is not recommended unless essential. If use is necessary, the infant should be monitored for potential side effects such as drowsiness, irritability, or feeding difficulties.

Contraception Requirements

No specific contraception requirements are associated with levocetirizine use alone. However, if you are using oral contraceptives, no interaction with levocetirizine has been reported.

Driving & Machine Operation

Impairment Potential Assessment

While levocetirizine is classified as a "non-sedating" antihistamine, individual responses vary. Clinical studies show:

• ~5-10% of patients experience somnolence (drowsiness)
• ~5% experience fatigue or tiredness
• Impairment is dose-related (higher doses increase risk)
• Effects may be enhanced with alcohol or other CNS depressants

Warning Signs to Watch For

• Feeling drowsy or sleepy during daytime hours
• Slowed reaction times or difficulty concentrating
• Heavy eyelids or frequent yawning
• Mental fogginess or confusion

Recommendation: Do not drive or operate dangerous machinery until you know how levocetirizine affects you. If you experience significant drowsiness, consider taking your dose at bedtime. If impairment persists, consult your doctor about alternative treatments.

Levocetirizine Ingredients

Active Ingredient

• Levocetirizine dihydrochloride: 5mg per film-coated tablet (equivalent to 4.4mg levocetirizine base)

Excipients (Inactive Ingredients)

How to Use Levocetirizine

Step-by-Step Administration Guide

1. Wash your hands thoroughly with soap and water
2. Remove one tablet from the blister pack by pushing it through the foil
3. Place the tablet on your tongue
4. Swallow whole with a glass of water (do not chew or crush)
5. The tablet may be taken with or without food, according to your preference
6. If prescribed a half dose, the tablet can be divided along the breakline (G mark)

Levocetirizine Dosage Guidelines

Administration Instructions

Timing Considerations

• Take levocetirizine at approximately the same time each day for consistent symptom control
• If taking for allergic rhinitis, consider taking before anticipated allergen exposure
• For chronic urticaria, regular daily use provides best control regardless of timing

Food and Drink Interactions

Levocetirizine may be taken with or without food. However, note these important considerations:

• Alcohol: Use caution as concurrent use may enhance drowsiness and impair coordination
• Grapefruit juice: No known interaction, but large quantities may theoretically affect metabolism
• High-fat meals: No significant effect on absorption

Missed Dose Management

Overdose Information

Symptoms of Overdose

• Adults: Primarily drowsiness, sedation, lethargy
• Children: Initial excitation, agitation, restlessness followed by drowsiness
• Possible additional symptoms: headache, dry mouth, nausea, dizziness, tachycardia

Treatment Protocol

There is no specific antidote for levocetirizine overdose. Management is supportive and symptomatic:

• Gastric lavage may be considered if presented within 1 hour of ingestion
• Activated charcoal may be administered to reduce absorption
• Vital signs monitoring (heart rate, blood pressure, respiratory rate)
• Symptomatic treatment for any manifestations
• Haemodialysis is not effective due to high protein binding

Levocetirizine Side Effects

Like all medicines, levocetirizine can cause side effects, although not everyone experiences them. Side effects are generally mild to moderate and often diminish with continued use.

Frequency-Based Categorization

Discontinuation Effects

Stopping levocetirizine treatment usually has no negative effects. However, in rare cases, intense itching (pruritus) may occur upon discontinuation, even if this symptom wasn't present before treatment. This usually resolves spontaneously but may require restarting treatment in severe cases.

How to Store Levocetirizine

• Keep out of sight and reach of children
• Store in the original packaging to protect from moisture
• No special temperature requirements - store at room temperature (below 25°C)
• Do not use after the expiry date printed on the carton/blister (EXP)
• Do not dispose of medicines via wastewater or household waste
• Return unused or expired medication to your pharmacy for safe disposal

Levocetirizine Pack Information

Tablet Description

• Appearance: White, oval, film-coated tablets
• Markings: One side has a "G" breakline (G); other side is plain
• Scored: Yes - can be divided into equal halves for dose adjustment

Available Pack Sizes

• 7 tablets*
• 10 tablets*
• 20 tablets*
• 21 tablets*
• 28 tablets*
• 30 tablets
• 50 tablets*
• 90 tablets
• 100 tablets

*Not all pack sizes may be marketed or available through Chemist Doctor

Packaging Materials

• Aluminium/Aluminium blisters OR
• PVC/PVdC - Aluminium blisters

Where to Buy Levocetirizine in the UK