Xyzal 2.5mg/5ml Solution
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 called 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 Correctly
To get the most benefit from your medication, follow your doctor's instructions carefully. Read all the information provided with your prescription and follow the instructions closely.
Take your medication in the evening, with or without food.
If you're using the liquid form, measure your dose accurately using the measuring device that comes with the medication. If one is not provided, ask your pharmacist for a suitable measuring device.
Storing and Disposing of Your Medication
To maintain the quality and safety of your medication:
Store it at room temperature in a dry place, avoiding bathrooms.
Keep all medications in a secure location, out of the reach of children and pets.
* Dispose of unused or expired medications properly. Do not flush them down the toilet or pour them down the drain unless instructed to do so by your pharmacist. Check with your pharmacist for guidance on the best disposal method, as there may be drug take-back programs available in your area.
What to Do If You Miss 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 the missed one.
To get the most benefit from your medication, follow your doctor's instructions carefully. Read all the information provided with your prescription and follow the instructions closely.
Take your medication in the evening, with or without food.
If you're using the liquid form, measure your dose accurately using the measuring device that comes with the medication. If one is not provided, ask your pharmacist for a suitable measuring device.
Storing and Disposing of Your Medication
To maintain the quality and safety of your medication:
Store it at room temperature in a dry place, avoiding bathrooms.
Keep all medications in a secure location, out of the reach of children and pets.
* Dispose of unused or expired medications properly. Do not flush them down the toilet or pour them down the drain unless instructed to do so by your pharmacist. Check with your pharmacist for guidance on the best disposal method, as there may be drug take-back programs available in your area.
What to Do If You Miss 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 the missed one.
Lifestyle & Tips
- Take the medication once daily in the evening, with or without food.
- Avoid or limit alcohol consumption while taking this medication, as it can increase drowsiness.
- Be cautious when driving or operating machinery until you know how this medication affects you, as it can cause drowsiness or dizziness.
- Store at room temperature away from moisture and heat.
Available Forms & Alternatives
Available Strengths:
Generic Alternatives:
Dosing & Administration
Adult Dosing
Standard Dose:
5 mg (10 mL) orally once daily in the evening
Dose Range:
2.5 - 5 mg
Condition-Specific Dosing:
chronicUrticaria:
5 mg (10 mL) orally once daily in the evening
allergicRhinitis:
5 mg (10 mL) orally once daily in the evening
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established for infants under 6 months. For 6 months to <2 years: 1.25 mg (2.5 mL) orally once daily in the evening.
Child:
2 to 5 years: 1.25 mg (2.5 mL) orally once daily in the evening. 6 to 11 years: 2.5 mg (5 mL) orally once daily in the evening.
Adolescent:
12 years and older: 5 mg (10 mL) orally once daily in the evening.
Dose Adjustments
Renal Impairment:
Mild:
CrCl 50-80 mL/min: 2.5 mg (5 mL) orally once daily in the evening.
Moderate:
CrCl 30-49 mL/min: 2.5 mg (5 mL) orally every other day in the evening.
Severe:
CrCl 10-29 mL/min: 2.5 mg (5 mL) orally twice weekly (e.g., once every 3-4 days) in the evening.
Dialysis:
CrCl <10 mL/min or End-Stage Renal Disease (ESRD) on dialysis: Contraindicated.
Hepatic Impairment:
Mild:
No adjustment needed.
Moderate:
No adjustment needed.
Severe:
No adjustment needed (levocetirizine is minimally metabolized by the liver).
Pharmacology
Mechanism of Action
Levocetirizine, the (R)-enantiomer of cetirizine, is a potent and highly selective H1-receptor antagonist. It competitively binds to peripheral H1 receptors, thereby inhibiting the effects of histamine, including vasodilation, increased vascular permeability, pruritus, and bronchoconstriction. It also inhibits histamine-induced wheal and flare reactions and reduces eosinophil migration and release of inflammatory mediators.
Pharmacokinetics
Absorption:
Bioavailability:
Not available (well-absorbed)
Tmax:
0.9 hours (oral solution)
FoodEffect:
Food may delay Tmax by 1.25 hours and decrease Cmax by 36%, but the extent of absorption (AUC) is not affected.
Distribution:
Vd:
0.41 L/kg
ProteinBinding:
91-92%
CnssPenetration:
Limited (low potential for blood-brain barrier penetration compared to first-generation antihistamines)
Elimination:
HalfLife:
Approximately 8-9 hours (adults), shorter in children (5-6 hours in 6-11 years, 5 hours in 2-5 years, 3.5 hours in 6 months to <2 years)
Clearance:
Not available (primarily renal)
ExcretionRoute:
Renal (approximately 85.4% of the dose is excreted in urine, 12.9% in feces)
Unchanged:
Approximately 85.4% (in urine)
Pharmacodynamics
OnsetOfAction:
Within 1 hour
PeakEffect:
Approximately 1 hour after administration
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. If you notice any of the following symptoms, contact your doctor or seek medical attention immediately:
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 do not experience any side effects or only have mild ones, it is 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 or seek medical help:
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, contact your doctor for medical advice. 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 medical attention immediately:
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 do not experience any side effects or only have mild ones, it is 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 or seek medical help:
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, contact your doctor for medical advice. 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 sedation
- Dizziness or lightheadedness
- Difficulty urinating
- Paradoxical excitation (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.
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 if it is safe to take this medication 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.
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 if it is safe to take this medication 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. Never exceed the dosage prescribed by your doctor or specified on the package label.
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 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. Never exceed the dosage prescribed by your doctor or specified on the package label.
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 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, sedation, stupor, tachycardia, tremor.
- Children: Agitation, restlessness, irritability, followed by drowsiness.
What to Do:
Seek immediate medical attention or call Poison Control at 1-800-222-1222. Treatment is symptomatic and supportive. There is no specific antidote.
Drug Interactions
Monitoring
Routine Monitoring
Symptom relief (e.g., sneezing, rhinorrhea, pruritus, urticaria)
Frequency: Daily, as needed
Target: Reduction or resolution of symptoms
Action Threshold: Lack of efficacy after 1-2 weeks, consider alternative or re-evaluation.
CNS side effects (e.g., drowsiness, fatigue, dizziness)
Frequency: Daily, especially during initiation or dose changes
Target: Minimal to no CNS effects
Action Threshold: Significant drowsiness or impairment, consider dose reduction or discontinuation.
Symptom Monitoring
- Allergy symptoms (sneezing, runny nose, itchy eyes/nose, hives, itching)
- Drowsiness
- Fatigue
- Dizziness
- Dry mouth
- Headache
Special Patient Groups
Pregnancy
Levocetirizine is 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 only if clearly needed and potential benefits outweigh potential risks.
Trimester-Specific Risks:
First Trimester:
Generally considered low risk, but limited human data.
Second Trimester:
Generally considered low risk.
Third Trimester:
Generally considered low risk, but caution with antihistamines near term due to potential for neonatal effects (e.g., irritability, tremor, sedation) if used in high doses or for prolonged periods.
Lactation
Levocetirizine is excreted in human milk. The American Academy of Pediatrics considers cetirizine (the racemic mixture) to be compatible with breastfeeding. However, levocetirizine may cause drowsiness or other adverse effects in the nursing infant and may decrease milk supply. Use with caution.
Infant Risk:
Moderate risk (L3). Potential for infant drowsiness, irritability, or decreased milk supply. Monitor infant for sedation or unusual fussiness.
Pediatric Use
Dosing varies by age group (6 months to <2 years, 2-5 years, 6-11 years, 12 years and older). Not recommended for infants younger than 6 months. Children may experience paradoxical excitation (restlessness, agitation) instead of drowsiness. Close monitoring for CNS effects is important.
Geriatric Use
Increased risk of adverse effects such as drowsiness, fatigue, and urinary retention due to age-related decline in renal function and increased sensitivity to anticholinergic effects. Dose adjustment is required for renal impairment. Start with the lowest effective dose (2.5 mg daily) and titrate carefully.
Clinical Information
Clinical Pearls
- Levocetirizine is the active enantiomer of cetirizine, offering similar efficacy with potentially less sedation at equipotent doses.
- Administer in the evening to minimize potential daytime drowsiness.
- Patients should be advised to avoid alcohol and other CNS depressants due to additive sedative effects.
- Renal dose adjustments are crucial, especially in elderly patients, to prevent accumulation and increased side effects.
- While generally less sedating than first-generation antihistamines, individual response to sedation can vary.
Alternative Therapies
- Other second-generation antihistamines (e.g., loratadine, fexofenadine, desloratadine, cetirizine)
- First-generation antihistamines (e.g., diphenhydramine, chlorpheniramine - generally not preferred due to higher sedation and anticholinergic effects)
- Nasal corticosteroids (e.g., fluticasone, mometasone for allergic rhinitis)
- Mast cell stabilizers (e.g., cromolyn sodium for allergic rhinitis)
- Leukotriene receptor antagonists (e.g., montelukast for allergic rhinitis and asthma)
Cost & Coverage
Average Cost:
Varies, typically $15-$40 per 150 mL bottle (2.5mg/5mL)
Generic Available:
Yes
Insurance Coverage:
Tier 1 or Tier 2 (for generic), Tier 3 or higher (for 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 safe and effective treatment, 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 information. If you have any questions or concerns about your 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 taken, including the amount and time of ingestion.