Levocetirizine dihydrochloride

Uses

Levocetirizine dihydrochloride Dihydrochloride is used for the treatment of symptoms associated with allergic conditions such as seasonal allergic rhinitis, perennial allergic rhinitis and chronic idiopathic urticaria.

Levocetirizine dihydrochloride is also used to associated treatment for these conditions: Allergic Rhinitis (AR), Chronic Idiopathic Urticaria, Common Cold, Nasal Congestion, Perennial Allergic Rhinitis (PAR), Seasonal Allergic Rhinitis

How Levocetirizine dihydrochloride works

Levocetirizine dihydrochloride selectively inhibits histamine H₁ receptors. This action prevents histamine from activating this receptor and causing effects like smooth muscle contraction, increased permeability of vascular endothelium, histidine uptake in basophils, stimulation of cough receptors, and stimulation of flare responses in the nervous system.

Dosage

Levocetirizine dihydrochloride dosage

Adults and children 12 years of age and older: 5 mg once daily in the evening

Children 6 to 11 years of age: 2.5 mg once daily in the evening

Children 6 months to 5 years of age: 1.25 mg (1/2 teaspoon oral solution) once daily in the evening

Renal Impairment: Adjust the dose in patients 12 years of age and older with decreased renal function

Side Effects

The most common adverse reactions (rate ≥2% and > placebo) were somnolence, nasopharyngitis, fatigue, dry mouth, and pharyngitis in subjects 12 years of age and older, and pyrexia, somnolence, cough, and epistaxis in children 6 to 12 years of age. In subjects 1 to 5 years of age, the most common adverse reactions (rate ≥2% and > placebo) were pyrexia, diarrhea, vomiting, and otitis media. In subjects 6 to 11 months of age, the most common adverse reactions (rate ≥3% and > placebo) were diarrhea and constipation.

Toxicity

Patients experiencing an overdose may present with drowsiness. Children may become agitated and restless before drowsiness. Patients should be treated with supportive measures. Dialysis will not assist in removing the drug from the body.

The maximal nonlethal dose in mice and rats is 240mg/kg.

Precaution

Epileptic patients and patients at risk of convulsions. Renal impairment. Pregnancy and lactation.

Food Interaction

• Avoid alcohol.
• Take with or without food.

[Moderate] GENERALLY AVOID: Alcohol may potentiate some of the pharmacologic effects of CNS-active agents.

Use in combination may result in additive central nervous system depression and
MANAGEMENT: Patients receiving CNS-active agents should be warned of this interaction and advised to avoid or limit consumption of alcohol.

Ambulatory patients should be counseled to avoid hazardous activities requiring complete mental alertness and motor coordination until they know how these agents affect them, and to notify their physician if they experience excessive or prolonged CNS effects that interfere with their normal activities.

Levocetirizine dihydrochloride Drug Interaction

Moderate: diphenhydramine, duloxetine, pregabalinUnknown: aspirin, ubiquinone, omega-3 polyunsaturated fatty acids, fluticasone nasal, metoprolol, esomeprazole, albuterol, bifidobacterium infantis / lactobacillus acidophilus, montelukast, budesonide / formoterol, levothyroxine, acetaminophen, cyanocobalamin, ascorbic acid, ergocalciferol, cholecalciferol, cetirizine

Levocetirizine dihydrochloride Disease Interaction

Major: renal impairmentModerate: urinary retention

Volume of Distribution

The volume of distribution of levocetirizine is 0.33±0.02L/kg.

Elimination Route

Following a 5mg oral dose of levocetirizine, a C_max of 0.27±0.04µg/mL with a T_max of 0.75±0.50h. The AUC of levocetirizine is 2.31±0.50µg*h/mL. Taking levocetirizine with food does not affect the AUC but delays T_max by 1.25 hours and lowers C_max by 36%.

Half Life

The average half life of levocetirizine is 7.05±1.54 hours.

Clearance

The average clearance of levocetirizine is 0.57±0.18mL/min/kg.

Elimination Route

168 hours post dose an average of 85.4% of a radiolabeled dose was recovered with an average of 80.8% in the urine and 9.5% in the feces. In the urine, 77% of the dose was recovered as unchanged drug, 0.5% as the M8 and M9 metabolites, 0.4% as the M10a metabolite, 0.4% as the M10b metabolite, 0.3% as the M3 metabolite, 0.3% as the M4 and M5 metabolite, 0.2% as the M2 metabolite, and 0.1% as the M1 metabolite. In the feces, 9.0% of the dose was recovered as unchanged drug, 1.0% as the M4 and M5 metabolite, and 0.1% as the M1 metabolite.

Pregnancy & Breastfeeding use

Pregnancy: The safety of Levocetirizine dihydrochloride in pregnancy has not been established. Therefore, it should be used with caution during pregnancy and only if the potential benefits to the mother outweigh any risks to the foetus.

Lactation: Levocetirizine dihydrochloride passes into breast milk. So, it should be used with caution in nursing mothers and only if the expected benefit to the mother is greater than the risk to the nursing infant.

Contraindication

It is contraindicated in patients who are hypersensitive to this medication or to any of its ingredients.

Special Warning

Paediatric use: Not recommended for use in children less than 6 years of age.

Acute Overdose

Symptoms: Drowsiness, agitation, restlessness, confusion, diarrhoea, dizziness, fatigue, headache, malaise, mydriasis, pruritus, sedation, somnolence, stupor, tachycardia, tremor and urinary retention.

Management: Symptomatic and supportive treatment. Gastric lavage must be considered shortly following ingestion.

Storage Condition

Store between 20-25°C.

Innovators Monograph

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