Xyzal 5mg Tablets
It is used to ease allergy signs.It is used to treat hives.
Drug Class
Antihistamine
Pharmacologic Class
Second-generation H1-receptor antagonist
Pregnancy Category
Category B
FDA Approved
Dec 2007
DEA Schedule
Not Controlled
Overview
What is this medicine?
Levocetirizine is an antihistamine used to relieve symptoms of allergies 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 is a 'non-drowsy' type of antihistamine, but some people may still feel sleepy.
How to Use This Medicine
Taking Your Medication
To take this medication correctly, follow your doctor's instructions and read all the information provided. Take your dose in the evening, with or without food. If you need to split your tablets, only split them along the score line to ensure the correct dose.
Storing and Disposing of Your Medication
Store your medication at room temperature in a dry place, avoiding bathrooms. Keep 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 take this medication correctly, follow your doctor's instructions and read all the information provided. Take your dose in the evening, with or without food. If you need to split your tablets, only split them along the score line to ensure the correct dose.
Storing and Disposing of Your Medication
Store your medication at room temperature in a dry place, avoiding bathrooms. Keep 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
- Take the medication in the evening, as it may cause drowsiness.
- Avoid alcohol and other CNS depressants while taking this medication, as it can increase drowsiness and impair alertness.
- Do not exceed the recommended dose.
- If you miss a dose, take it as soon as you remember, unless it's almost time for your next dose. Do not double the dose.
- Store at room temperature away from light and moisture.
Available Forms & Alternatives
Available Strengths:
Generic Alternatives:
Dosing & Administration
Adult Dosing
Standard Dose:
5 mg orally once daily in the evening
Dose Range:
2.5 - 5 mg
Condition-Specific Dosing:
chronicIdiopathicUrticaria:
5 mg orally once daily in the evening
allergicRhinitis:
5 mg orally once daily in the evening
Pediatric Dosing
Neonatal:
Not established (contraindicated in infants <6 months)
Infant:
1.25 mg orally once daily in the evening (6 months to <2 years)
Child:
1.25 mg orally once daily in the evening (2 to 5 years); 2.5 mg orally once daily in the evening (6 to 11 years)
Adolescent:
5 mg orally once daily in the evening (âĨ12 years)
Dose Adjustments
Renal Impairment:
Mild:
CrCl 50-80 mL/min: 2.5 mg once daily
Moderate:
CrCl 30-49 mL/min: 2.5 mg every other day
Severe:
CrCl 10-29 mL/min: 2.5 mg twice weekly
Dialysis:
CrCl <10 mL/min or ESRD requiring dialysis: Contraindicated
Hepatic Impairment:
Mild:
No dose adjustment needed
Moderate:
No dose adjustment needed
Severe:
No dose adjustment needed
Pharmacology
Mechanism of Action
Levocetirizine, the active R-enantiomer of cetirizine, is a potent and selective peripheral H1-receptor antagonist. It inhibits the release of histamine from mast cells and reduces the migration of inflammatory cells (e.g., eosinophils) and the release of inflammatory mediators (e.g., leukotrienes) involved in allergic reactions. It provides symptomatic relief from allergic rhinitis and chronic idiopathic urticaria by blocking the effects of histamine.
Pharmacokinetics
Absorption:
Bioavailability:
Not explicitly quantified as a percentage, but rapidly and well absorbed.
Tmax:
Approximately 0.9-1 hour
FoodEffect:
Food delays Tmax by approximately 1.25 hours and decreases Cmax by about 36%, but does not affect the extent of absorption (AUC).
Distribution:
Vd:
Approximately 0.4 L/kg
ProteinBinding:
Approximately 91-92%
CnssPenetration:
Limited (low lipophilicity, P-glycoprotein substrate, contributing to less CNS side effects compared to first-generation antihistamines)
Elimination:
HalfLife:
Approximately 7-10 hours (adults); shorter in children (e.g., 5 hours in 6-11 years)
Clearance:
Approximately 0.63 mL/min/kg
ExcretionRoute:
Primarily renal (85.4% unchanged in urine), with a small amount in feces (12.9%)
Unchanged:
Approximately 85.4% (in urine)
Pharmacodynamics
OnsetOfAction:
Within 1 hour
PeakEffect:
Approximately 1 hour
DurationOfAction:
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. If you notice any of the following symptoms, contact your doctor or seek immediate medical attention:
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. If you experience any of the following side effects or any other unusual symptoms that bother you or do not go away, contact your doctor:
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. If you notice any of the following symptoms, contact your doctor or seek immediate medical attention:
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. If you experience any of the following side effects or any other unusual symptoms that bother you or do not go away, contact your doctor:
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
- Difficulty urinating
- Fast or pounding heartbeat
- Vision changes
- Signs of an allergic reaction (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, over-the-counter, natural products, and vitamins) and health conditions with your doctor and pharmacist. They will help determine whether it is safe to take this medication in conjunction with your other medications and health issues. Never start, stop, or adjust the dosage 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, over-the-counter, natural products, and vitamins) and health conditions with your doctor and pharmacist. They will help determine whether it is safe to take this medication in conjunction with your other medications and health issues. Never start, stop, or adjust the dosage 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.
When starting this medication, be cautious and avoid driving or engaging in activities that require alertness until you understand how it affects you. High doses of this medication can cause drowsiness, so it is crucial to adhere to the dosage prescribed by your doctor or as indicated on the package label. Do not exceed the recommended dose.
Before consuming alcohol, using marijuana or other cannabis products, or taking prescription or over-the-counter (OTC) medications 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 medication to a child, consult with their doctor to ensure the appropriate form and dosage are used.
If you are pregnant, planning to become pregnant, or are breastfeeding, inform your doctor. It is necessary to discuss the potential benefits and risks of this medication to both you and your baby to make an informed decision.
When starting this medication, be cautious and avoid driving or engaging in activities that require alertness until you understand how it affects you. High doses of this medication can cause drowsiness, so it is crucial to adhere to the dosage prescribed by your doctor or as indicated on the package label. Do not exceed the recommended dose.
Before consuming alcohol, using marijuana or other cannabis products, or taking prescription or over-the-counter (OTC) medications 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 medication to a child, consult with their doctor to ensure the appropriate form and dosage are used.
If you are pregnant, planning to become pregnant, or are breastfeeding, inform your doctor. It is necessary to discuss the potential benefits and risks of this medication to both you and your baby to make an informed decision.
Overdose Information
Overdose Symptoms:
- Adults: Drowsiness
- Children: Agitation, restlessness, followed by drowsiness
What to Do:
Seek immediate medical attention or call a poison control center. Call 1-800-222-1222
Drug Interactions
Moderate Interactions
Minor Interactions
- Theophylline
Monitoring
Symptom Monitoring
- Effectiveness of symptom relief (e.g., reduction in sneezing, runny nose, itching, hives)
- Occurrence and severity of adverse effects (e.g., drowsiness, fatigue, dry mouth, headache, dizziness)
- Signs of paradoxical excitation (especially in children)
- Urinary retention (especially in elderly patients or those with prostatic hypertrophy)
Special Patient Groups
Pregnancy
Levocetirizine is classified as Pregnancy Category B. Animal studies have not shown harm to the fetus, but there are no adequate and well-controlled studies in pregnant women. Use during pregnancy only if clearly needed and the potential benefit outweighs the potential risk to the fetus.
Trimester-Specific Risks:
First Trimester:
Low risk based on animal data; human data limited but generally reassuring for antihistamines.
Second Trimester:
Low risk based on animal data; human data limited but generally reassuring for antihistamines.
Third Trimester:
Low risk based on animal data; human data limited but generally reassuring for antihistamines.
Lactation
Levocetirizine is excreted into human breast milk. Due to the potential for adverse reactions in nursing infants (e.g., drowsiness, irritability, decreased feeding), a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother.
Infant Risk:
Moderate risk (L3) - potential for infant drowsiness, irritability, or anticholinergic effects.
Pediatric Use
Dosing adjustments are necessary based on age. Contraindicated in infants less than 6 months of age due to lack of safety and efficacy data. Children may experience paradoxical excitation (restlessness, agitation) rather than drowsiness.
Geriatric Use
Use with caution in elderly patients due to increased risk of adverse effects such as drowsiness, fatigue, and urinary retention. Dose adjustment is required for renal impairment, which is more common in the elderly. Start with the lowest effective dose.
Clinical Information
Clinical Pearls
- Levocetirizine is the active enantiomer of cetirizine, offering similar efficacy with potentially less sedation at equivalent doses.
- Best taken in the evening due to potential for drowsiness, even though it's considered a 'non-drowsy' antihistamine.
- Patients should be advised to avoid activities requiring mental alertness (e.g., driving, operating machinery) until they know how the medication affects them.
- Effective for both seasonal and perennial allergic rhinitis, as well as chronic idiopathic urticaria.
- Renal dose adjustment is crucial to prevent accumulation and increased side effects.
Alternative Therapies
- Other second-generation antihistamines (e.g., Cetirizine, Loratadine, Fexofenadine, Desloratadine)
- Intranasal corticosteroids (e.g., Fluticasone, Mometasone)
- Mast cell stabilizers (e.g., Cromolyn sodium)
- Leukotriene receptor antagonists (e.g., Montelukast)
- Immunotherapy (allergy shots)
Cost & Coverage
Average Cost:
Varies, typically $20-$60 per 30 tablets (5mg)
Generic Available:
Yes
Insurance Coverage:
Tier 1 or Tier 2 (generic), Tier 3 (brand)
General Drug Facts
If your symptoms or health issues persist or worsen, it's 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 be sure to check with your pharmacist for more details. 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 information about the medication taken, the amount, and the time it happened.