Levocetirizine
Levocetirizine Uses, Dosage, Side Effects, Food Interaction and all others data.
Levocetirizine Dihydrochloride is a preparation of Levocetirizine Dihydrochloride. Levocetirizine is the active (levo) isomer of Cetirizine. It is a new highly effective and well-tolerated non-sedating antihistamine with potent antiallergic properties. It has a two-fold higher affinity for H1-receptors than Cetirizine. Levocetirizine has a rapid and long-lasting action, allowing once-a-day administration.
Levocetirizine is a second generation histamine H1 antagonist used to treat various allergic symptoms. It has a long duration of action as it is generally taken once daily, and a wide therapeutic window as animal studies show the maximal nonlethal dose is over 100x a normal dose. Patients are cautioned to avoid tasks that require complete alertness, avoid alertness, and use caution in patients with factors predisposing urinary retention.
| Trade Name | Levocetirizine |
| Availability | Rx and/or OTC |
| Generic | Levocetirizine |
| Levocetirizine Other Names | Levocetirizina, Levocetirizine |
| Related Drugs | prednisone, hydroxyzine, cetirizine, loratadine, fluticasone nasal, promethazine, diphenhydramine, Zyrtec, Vistaril, Atarax |
| Weight | 0.5mg/ml, 5mg, |
| Type | Oral Solution, Oral Tablet, Tablet |
| Formula | C21H25ClN2O3 |
| Weight | Average: 388.89 Monoisotopic: 388.1553704 |
| Protein binding | Plasma protein binding of levocetirizine was on average 96.1% 1 hour post dose and 91.9% 6 hours post dose. |
| Groups | Approved |
| Therapeutic Class | Non-sedating antihistamines |
| Manufacturer | Glenmark Pharmaceuticals Europe Ltd, Pratapa Nirmala |
| Available Country | United Kingdom, United States, Indonesia, Netherlands |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Levocetirizine 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 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 works
Levocetirizine 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 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 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 Disease Interaction
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 Cmax of 0.27±0.04µg/mL with a Tmax 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 Tmax by 1.25 hours and lowers Cmax 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 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 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
You find simplified version here Levocetirizine
Levocetirizine contains Levocetirizine see full prescribing information from innovator Levocetirizine Monograph, Levocetirizine MSDS, Levocetirizine FDA label
FAQ
What is Levocetirizine used for?
Levocetirizine is used to relieve runny nose; sneezing; and redness, itching, and tearing of the eyes caused by hay fever, seasonal allergies, and allergies to other substances such as dust mites, animal dander, and mold.Levocetirizine is also used to treat symptoms of hives, including itching and rash.
How safe is Levocetirizine?
Many people using Levocetirizine do not have serious side effects. Tell your doctor right away if you have any serious side effects, including: difficulty urinating, weakness. A very serious allergic reaction to this drug is rare.
What are the common side effects of Levocetirizine?
The common side effects of Levocetirizine are include:
- drowsiness
- tiredness
- weakness
- sore throat
- dry mouth
- fever
- cough
- nosebleed
This is not a complete list of Levocetirizine side effects. Ask your doctor or pharmacist for more information.
How does Levocetirizine work?
Levocetirizine works by blocking the action of histamine, a substance in the body that causes allergic symptoms.
How long does Levocetirizine take to work?
Levocetirizine dihydrochloride 5 mg was found to have an onset of action 1 hour after oral intake.
Is Levocetirizine safe during pregnancy?
Levocetirizine should be used during pregnancy only if clearly needed. Animal studies have failed to reveal evidence of fetal harm and teratogenicity. There are no controlled data in human pregnancy.
Is Levocetirizine safe during breastfeeding?
Levocetirizine are considered safe to use during breastfeeding, as minimal amounts are excreted in the breast milk and would not cause any adverse effects on a breastfeeding infant.
Can I drink alcohol with Levocetirizine?
Alcohol can increase the nervous system side effects of levocetirizine such as dizziness, drowsiness, and difficulty concentrating.You should avoid or limit the use of alcohol while being treated with Levocetirizine .
Can I drive after taking Levocetirizine?
Levocetirizine can cause drowsiness. Do not drive or operate heavy machinery until you know how it affects you.
What is the best time to take Levocetirizine?
Levocetirizine comes as a tablet to take by mouth. It is usually taken once a day in the evening with or without food. Take Levocetirizine at the same time every day.
How long does Levocetirizine take to work?
You can expect to feel relief about an hour after taking a dose. You can expect Levocetirizine to start preventing allergy symptoms after taking it for 2 days in a row.
Can Levocetirizine make Me sleepy?
Levocetirizine is called a non-drowsy antihistamine.However, it can still cause drowsiness in a few people.
Who should not take Levocetirizine?
You should not use this medicine if you are allergic to Levocetirizine. You should not take take if you have end-stage kidney disease or if you are on dialysis. Any child younger than 12 years old with kidney disease should not take Levocetirizine.
Is It safe to take Levocetirizine everyday?
The recommended dose of Levocetirizine dihydrochloride tablets is 5 mg (1 tablet) once daily in the evening.
Does Levocetirizine help anxiety?
Levocetirizine is an antihistamine. It is approved for the treatment of anxiety.
How long does Levocetirizine stay in my system?
The onset of action of Levocetirizine lasts for 28 hours. However, it takes 50 hours to be eliminated from your system. You should avoid taking Levocetirizine if you are suffering from kidney disease or are undergoing dialysis.
What happens if I miss a dose of Levocetirizine?
Take Levocetirizine as soon as you can, but skip the missed dose if it is almost time for your next dose. Do not take two doses at one time.
Can I take Levocetirizine for a long time?
Levocetirizine oral tablet is used for short-term treatment of seasonal allergies and long-term treatment of chronic itching. It comes with risks if you don't take it as prescribed.
Is Levocetirizine safe for kidneys?
You should not take Levocetirizine if you have end-stage kidney disease or if you are on dialysis.
Can I take overdose of Levocetirizine?
If you take too much: You could have dangerous levels of the drug in your body. Symptoms of an overdose of this drug can include: increased drowsiness (adults) agitation and restlessness, followed by drowsiness (children).
