Levocetirizine 5mg Tablets
It is used to ease allergy signs.It is used to treat hives.
Drug Class
Antihistamine
Pharmacologic Class
H1-receptor antagonist, second-generation
Pregnancy Category
Category B
FDA Approved
Jan 2007
DEA Schedule
Not Controlled
Overview
What is this medicine?
Levocetirizine is an antihistamine that helps relieve allergy symptoms like sneezing, runny nose, itchy eyes, and hives. It works by blocking a natural substance (histamine) that your body makes during an allergic reaction. It's often taken once a day, usually in the evening.
How to Use This Medicine
Taking Your Medication
To use this medication correctly, follow your doctor's instructions and read all the information provided. Take your dose in the evening, with or without food, as directed. If you need to split your tablets, only do so along the score line to ensure the correct dose.
Storing and Disposing of Your Medication
Keep your medication at room temperature in a dry place, avoiding storage in a bathroom. Store all medications in a safe location, out of the reach of children and pets. When disposing of unused or expired medication, do not flush it down the toilet or pour it down the drain unless instructed to do so. Instead, check with your pharmacist for guidance on proper disposal or participate in a local drug take-back program if available.
Missing a Dose
If you miss a dose, take it as soon as you remember. However, if it's close to the time for your next scheduled dose, skip the missed dose and resume your regular dosing schedule. Do not take two doses at the same time or take extra doses to make up for a missed one.
To use this medication correctly, follow your doctor's instructions and read all the information provided. Take your dose in the evening, with or without food, as directed. If you need to split your tablets, only do so along the score line to ensure the correct dose.
Storing and Disposing of Your Medication
Keep your medication at room temperature in a dry place, avoiding storage in a bathroom. Store all medications in a safe location, out of the reach of children and pets. When disposing of unused or expired medication, do not flush it down the toilet or pour it down the drain unless instructed to do so. Instead, check with your pharmacist for guidance on proper disposal or participate in a local drug take-back program if available.
Missing a Dose
If you miss a dose, take it as soon as you remember. However, if it's close to the time for your next scheduled dose, skip the missed dose and resume your regular dosing schedule. Do not take two doses at the same time or take extra doses to make up for a missed one.
Lifestyle & Tips
- Avoid alcohol and other medications that can cause drowsiness (e.g., sedatives, tranquilizers) while taking levocetirizine, as this can increase drowsiness.
- Use caution when driving or operating machinery until you know how this medication affects you, as it can cause drowsiness or dizziness.
- Take the medication in the evening, as it may cause drowsiness.
Available Forms & Alternatives
Available Strengths:
Dosing & Administration
Adult Dosing
Standard Dose:
5 mg orally once daily, in the evening
Dose Range:
2.5 - 5 mg
Condition-Specific Dosing:
chronic_idiopathic_urticaria:
5 mg orally once daily, in the evening
seasonal_allergic_rhinitis:
5 mg orally once daily, in the evening
perennial_allergic_rhinitis:
5 mg orally once daily, in the evening
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established (oral solution for 6 months to <6 years)
Child:
6 to 11 years: 2.5 mg orally once daily, in the evening (oral solution or tablet)
Adolescent:
12 years and older: 5 mg orally once daily, in the evening
Dose Adjustments
Renal Impairment:
Mild:
CrCl 50-80 mL/min: 2.5 mg orally once daily
Moderate:
CrCl 30-49 mL/min: 2.5 mg orally every other day
Severe:
CrCl 10-29 mL/min: 2.5 mg orally twice weekly
Dialysis:
CrCl <10 mL/min or ESRD requiring dialysis: Contraindicated
Confidence:
High
Hepatic Impairment:
Mild:
No adjustment needed
Moderate:
No adjustment needed
Severe:
No adjustment needed
Confidence:
High
Pharmacology
Mechanism of Action
Levocetirizine, the active (R)-enantiomer of cetirizine, is a potent and highly selective peripheral H1-receptor antagonist. It inhibits the release of histamine from mast cells and reduces the migration of inflammatory cells (e.g., eosinophils), thereby alleviating allergic symptoms such as sneezing, rhinorrhea, pruritus, and urticaria.
Pharmacokinetics
Absorption:
Bioavailability:
Approximately 100%
Tmax:
0.9-1 hour
FoodEffect:
Food may delay Tmax by 1.25 hours and decrease Cmax by 36%, but does not affect the extent of absorption (AUC).
Distribution:
Vd:
Approximately 0.4 L/kg
ProteinBinding:
Approximately 91-92%
CnssPenetration:
Limited
Elimination:
HalfLife:
Approximately 7-10 hours (adults with normal renal function)
Clearance:
Not available (primarily renal clearance)
ExcretionRoute:
Primarily renal (approximately 85.4% of the dose excreted unchanged in urine)
Unchanged:
Approximately 85.4%
Pharmacodynamics
OnsetOfAction:
Within 1 hour
PeakEffect:
Not available (correlates with Tmax)
DurationOfAction:
At least 24 hours
Safety & Warnings
Side Effects
Urgent Side Effects: Seek Medical Help Right Away
While rare, some people may experience severe and potentially life-threatening side effects when taking this medication. Immediately contact your doctor or seek medical attention if you experience any of the following symptoms:
Signs of an allergic reaction, such as:
+ Rash
+ Hives
+ Itching
+ Red, swollen, blistered, or peeling skin with or without fever
+ Wheezing
+ Tightness in the chest or throat
+ Trouble breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Trouble passing urine
Fever
Ear pain
Other Possible Side Effects
Like all medications, this drug can cause side effects. Although many people may not experience any side effects or only minor ones, it's essential to discuss any concerns with your doctor. Contact your doctor or seek medical help if you experience any of the following side effects or if they bother you or persist:
Feeling tired or weak
Feeling sleepy
Nose or throat irritation
Nosebleed
Dry mouth
Cough
Throwing up
Diarrhea or constipation
Reporting Side Effects
This list is not exhaustive, and you may experience other side effects. If you have questions or concerns about side effects, consult your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
While rare, some people may experience severe and potentially life-threatening side effects when taking this medication. Immediately contact your doctor or seek medical attention if you experience any of the following symptoms:
Signs of an allergic reaction, such as:
+ Rash
+ Hives
+ Itching
+ Red, swollen, blistered, or peeling skin with or without fever
+ Wheezing
+ Tightness in the chest or throat
+ Trouble breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Trouble passing urine
Fever
Ear pain
Other Possible Side Effects
Like all medications, this drug can cause side effects. Although many people may not experience any side effects or only minor ones, it's essential to discuss any concerns with your doctor. Contact your doctor or seek medical help if you experience any of the following side effects or if they bother you or persist:
Feeling tired or weak
Feeling sleepy
Nose or throat irritation
Nosebleed
Dry mouth
Cough
Throwing up
Diarrhea or constipation
Reporting Side Effects
This list is not exhaustive, and you may experience other side effects. If you have questions or concerns about side effects, consult your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
Seek Immediate Medical Attention If You Experience:
- Severe drowsiness or dizziness
- Confusion or difficulty concentrating
- Difficulty urinating (urinary retention)
- Paradoxical excitation (restlessness, agitation, especially in children)
- Allergic reaction symptoms (rash, itching/swelling, severe dizziness, trouble breathing)
Before Using This Medicine
Before Taking This Medication: Important Information to Share with Your Doctor
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Be sure to describe the symptoms you experienced as a result of the allergy.
If you have kidney disease, as this may affect your ability to take this medication.
This list is not exhaustive, and it is crucial to discuss all your medications, including prescription and over-the-counter drugs, natural products, and vitamins, with your doctor and pharmacist. They will help you determine if it is safe to take this medication in combination with your other medications and health conditions.
Remember, do not start, stop, or change the dose of any medication without first consulting your doctor to ensure your safety.
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Be sure to describe the symptoms you experienced as a result of the allergy.
If you have kidney disease, as this may affect your ability to take this medication.
This list is not exhaustive, and it is crucial to discuss all your medications, including prescription and over-the-counter drugs, natural products, and vitamins, with your doctor and pharmacist. They will help you determine if it is safe to take this medication in combination with your other medications and health conditions.
Remember, do not start, stop, or change the dose of any medication without first consulting your doctor to ensure your safety.
Precautions & Cautions
It is essential to inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication.
To ensure your safety, avoid operating a vehicle or engaging in activities that require alertness until you understand how this medication affects you. Be aware that high doses of this drug can cause drowsiness. Adhere strictly to the dosage prescribed by your doctor or as indicated on the package label, and do not exceed it.
Before consuming alcohol, using marijuana or other cannabis products, or taking any prescription or over-the-counter drugs that may impair your reactions, consult with your doctor.
This medication is available in various forms, which may be suitable for children of different ages. Prior to administering this drug to a child, it is crucial to discuss the appropriateness and safety with their doctor.
If you are pregnant, planning to become pregnant, or are breastfeeding, notify your doctor. It is necessary to have a discussion about the potential benefits and risks of this medication to both you and your baby.
To ensure your safety, avoid operating a vehicle or engaging in activities that require alertness until you understand how this medication affects you. Be aware that high doses of this drug can cause drowsiness. Adhere strictly to the dosage prescribed by your doctor or as indicated on the package label, and do not exceed it.
Before consuming alcohol, using marijuana or other cannabis products, or taking any prescription or over-the-counter drugs that may impair your reactions, consult with your doctor.
This medication is available in various forms, which may be suitable for children of different ages. Prior to administering this drug to a child, it is crucial to discuss the appropriateness and safety with their doctor.
If you are pregnant, planning to become pregnant, or are breastfeeding, notify your doctor. It is necessary to have a discussion about the potential benefits and risks of this medication to both you and your baby.
Overdose Information
Overdose Symptoms:
- Adults: Drowsiness
- Children: Agitation and restlessness, followed by drowsiness
What to Do:
In case of overdose, seek immediate medical attention or call a Poison Control Center (1-800-222-1222). Treatment is symptomatic and supportive. There is no specific antidote. Hemodialysis is not effective in removing levocetirizine.
Drug Interactions
Monitoring
Routine Monitoring
Symptom relief (e.g., reduction in sneezing, rhinorrhea, pruritus, urticaria)
Frequency: Daily
Target: Significant improvement
Action Threshold: Lack of efficacy after 1-2 weeks, consider alternative or re-evaluation
Adverse effects (e.g., drowsiness, fatigue, dry mouth, headache)
Frequency: Daily, especially during initial therapy
Target: Minimal to no adverse effects
Action Threshold: Persistent or severe adverse effects, consider dose reduction or discontinuation
Symptom Monitoring
- Allergic symptoms (sneezing, runny nose, itchy eyes, skin rash/hives)
- Drowsiness/sedation
- Dizziness
- Fatigue
- Dry mouth
- Headache
- Urinary retention (rare)
Special Patient Groups
Pregnancy
Category B. Animal studies have not shown fetal harm. Human data are limited but generally reassuring. Use during pregnancy only if clearly needed and the potential benefit outweighs the potential risk.
Trimester-Specific Risks:
First Trimester:
Limited human data, no clear evidence of increased risk of major birth defects.
Second Trimester:
Limited human data, no clear evidence of increased risk.
Third Trimester:
Limited human data, no clear evidence of increased risk.
Lactation
L3 (Moderately Safe). Levocetirizine is excreted into breast milk. Monitor breastfed infants for drowsiness, irritability, or poor feeding. Consider an alternative if the infant is premature or has underlying medical conditions.
Infant Risk:
Low to moderate risk of drowsiness or irritability in the infant.
Pediatric Use
Dosing varies by age group. Tablets are not recommended for children under 6 years of age; an oral solution is available for children 6 months to less than 6 years. Children may experience paradoxical excitation (agitation, restlessness) instead of drowsiness.
Geriatric Use
Start with the lowest effective dose (e.5 mg daily) due to the higher likelihood of decreased renal function. Monitor closely for adverse effects, particularly sedation and urinary retention, as elderly patients may be more sensitive to these effects.
Clinical Information
Clinical Pearls
- Levocetirizine is the active enantiomer of cetirizine, offering similar efficacy with potentially less sedation for some individuals.
- It is generally recommended to take levocetirizine in the evening due to its potential for causing drowsiness.
- Crucial to adjust dosage in patients with renal impairment to prevent accumulation and increased side effects.
- Effective for both seasonal and perennial allergic rhinitis, as well as chronic idiopathic urticaria.
- While considered a 'non-drowsy' antihistamine compared to first-generation agents, it can still cause drowsiness in a significant number of patients.
Alternative Therapies
- Other second-generation antihistamines (e.g., loratadine, fexofenadine, desloratadine, cetirizine)
- Intranasal corticosteroids (e.g., fluticasone, mometasone)
- Mast cell stabilizers (e.g., cromolyn sodium)
- Decongestants (e.g., pseudoephedrine, phenylephrine - often in combination products)
- Immunotherapy (allergy shots or sublingual tablets)
Cost & Coverage
Average Cost:
$10 - $30 per 30 tablets
Generic Available:
Yes
Insurance Coverage:
Tier 1 or Tier 2 (for generic)
General Drug Facts
If your symptoms or health issues persist or worsen, it is essential to contact your doctor for further guidance. To ensure your safety, never share your medication with others or take someone else's medication. Some medications may come with an additional patient information leaflet, so it's a good idea to check with your pharmacist for more information. If you have any questions or concerns about this medication, don't hesitate to reach out to your doctor, nurse, pharmacist, or other healthcare provider. In the event of a suspected overdose, immediately call your local poison control center or seek medical attention. When seeking help, be prepared to provide details about the medication, including the amount taken and the time it happened, to facilitate prompt and effective treatment.