levocetirizine dihydrochloride .5 mg/mL Solution
🆔 Identity & classification
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🏷️ RxNorm drug class
This medicine belongs to the Histamine-1 Receptor Antagonist class.
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🏭 Manufacturer & labeler
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🩺 Clinical
Levocetirizine is used to treat allergy symptoms: sneezing runny nose itching of the nose or throat red, itchy, or watery eyes It is also used to treat symptoms of urticaria (hives). Levocetirizine is in a class of medications called antihistamines. It works by blocking the action of histamine, a substance in the body that causes allergic symptoms.
Read the full MedlinePlus article ↗- It's an antihistamine used to relieve the classic allergy symptoms — runny nose, sneezing, itchy and watery eyes, and itching of the nose or throat — caused by seasonal hay fever o...
- What exactly is levocetirizine used for?
- It can, yes — drowsiness is the most commonly reported side effect and it's more likely at higher doses. Many people tolerate it fine, but until you know how it affects you, it's s...
- Yes, you can take it with or without food — either way works. If you take it with a high-fat meal, it may take a little longer to kick in and the peak level in your blood may be sl...
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🧪 Inactive Ingredients / Excipients
Inactive ingredients, also called excipients, are components of the drug product other than the active ingredient. They may include fillers, dyes, coatings, preservatives, flavors, or other formulation ingredients.
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UNII Q40Q9N063P
Acetic acid is a weak organic acid commonly used in medicines as a buffer and pH adjuster. It helps maintain the proper acidity level to ensure the drug remains stable and effective in its formulation.
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Glycerin is a clear, thick liquid derived from plant oils or fats. It acts as a humectant to retain moisture, a sweetener, and a solvent in medications.
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Maltitol is a sugar alcohol made by hydrogenating maltose. It's used as a sweetener and filler in medicines to improve taste and add bulk to tablets and capsules.
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Methylparaben is a preservative derived from benzoic acid that prevents growth of bacteria, fungi, and mold in medicines. It extends the product's shelf life and maintains safety during storage.
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Propylparaben is a chemical preservative used to prevent bacterial and fungal growth in medicines and personal care products. It helps extend shelf life and maintain product safety during storage.
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Saccharin is an artificial sweetener derived from benzoic sulfinilanide. It's added to medicines to improve taste and make them easier to take, especially in liquid or chewable formulations.
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Sodium acetate is a salt derived from acetic acid. It acts as a buffer to help maintain the medicine's pH stability and may serve as a preservative or solubilizer in liquid formulations.
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Water is a liquid solvent that dissolves and mixes ingredients together in liquid medicines, syrups, and injections. It helps distribute the active drug evenly throughout the product.
8 inactive ingredients listed in the exact product block matched to this NDC.
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ingredient classCode="IACT" elements from the exact product block matched by this NDC. Label-section narrative from DailyMed / the openFDA label index is shown separately when available.Inactive ingredient FAQ
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💲 Pricing
A drug doesn't have one price. Each row is a different public payment system, and none is what you'd pay at the counter — that depends on your insurance. The ⓘ on each row explains what it measures.
| Price system | Per mL | Per package |
|---|---|---|
| Retail pharmacies payNADAC · weekly | Not in the retail survey — common for institutional, discontinued, or low-volume packs. | |
| Medicaid paysCMS SDUD · 12 mo | No recent Medicaid claims on file for this NDC — rare and low-volume NDCs are suppressed in the public data. | |
| Medicare drug plans payPart D · Q2 2026 | $0.2807 | $41.54 / 148 ml |
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🔁 Therapeutic equivalents
| Product | Labeler | Pack | NADAC/unit | TE | Status | Price vs. this |
|---|---|---|---|---|---|---|
| levocetirizine dihydrochloride 2.5 mg/5mL 31722-0659-31 | Camber | 1 bottle | $0.166 | AA | Availability likely | — |
| levocetirizine dihydrochloride .5 mg/mL 45802-0680-28 | Padagis | 148 ml | $0.166 | AA | Availability likely | — |
| Levocetirizine Dihydrochloride .5 mg/mL 62135-0917-38 | Chartwell | 148 ml | $0.166 | AA | Availability likely | — |
| Childrens Xyzal Allergy 2.5 mg/5mL 41167-3533-00 | Chattem, | 1 bottle | — | — | FDA listed | — |
| Childrens Xyzal Allergy 2.5 mg/5mL 41167-3535-00 | Chattem, | 1 bottle | — | — | FDA listed | — |
| Xyzal .5 mg/mL 41167-5804-05 | Chattem, | 1 bottle | — | — | FDA listed | — |
| levocetirizine dihydrochloride .5 mg/mLthis 63629-2533-01 | Bryant | 1 bottle | — | AA | FDA listed | — |
| levocetirizine dihydrochloride .5 mg/mL 72162-1424-02 | Bryant | 148 ml | — | AA | FDA listed | — |
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⏳ Availability & generic status
This product is an FDA-approved generic. Other versions of the same drug are listed under Therapeutic equivalents, least expensive first.
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📊 Medicare Part D spend CMS · PART D · 2026 (Q1)
📦 Packaging — all sizes for this product
| Package NDC | Description | Marketing start | Status |
|---|---|---|---|
| 63629-2533-01 You're viewing this | 1 BOTTLE in 1 CARTON (63629-2533-1) / 148 mL in 1 BOTTLE | 2011-11-07 | Active |
🧭 About this NDC listing & data coverage
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| NDC identity (package / product / labeler codes) | ✓ Available |
| Labeler | ✓ Available |
| Product & package description | ✓ Available |
| Marketing category & status | ✓ Available |
| Active ingredient / dosage form / route | ✓ Available |
| FDA label (SPL via DailyMed) | ✓ Available |
| Package photos | ✓ Available |
| Inactive ingredients (structured) | ✓ Available |
| NADAC pharmacy acquisition price (CMS) | — Not published for this NDC CMS publishes NADAC only for NDCs reported in its retail-pharmacy survey. |
| Orange Book / therapeutic-equivalence data | ✓ Available |
| HCPCS J-code billing crosswalk | — Not published for this NDC Most self-administered / retail products have no J-code — that is normal. |
| Medicaid utilization (CMS SDUD) | — Not published for this NDC CMS reports utilization only for NDCs with Medicaid claims above its privacy threshold. |
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📄 Full prescribing information FDA SPL
🎯 Indications and Usage ▾
1 INDICATIONS AND USAGE Levocetirizine dihydrochloride is a histamine H 1 -receptor antagonist indicated for: • The relief of symptoms associated with perennial allergic rhinitis (1.1) • The treatment of the uncomplicated skin manifestations of chronic idiopathic urticaria (1.2)
1.1Perennial Allergic Rhinitis Levocetirizine dihydrochloride is indicated for the relief of symptoms associated with perennial allergic rhinitis in children 6 months to 2 years of age.
1.2Chronic Idiopathic Urticaria Levocetirizine dihydrochloride is indicated for the treatment of the uncomplicated skin manifestations of chronic idiopathic urticaria in adults and children 6 months of age and older.
⏱️ Dosage and Administration ▾
2 DOSAGE AND ADMINISTRATION Levocetirizine dihydrochloride is available as 2.5 mg/5 mL (0.5 mg/mL) oral solution. Levocetirizine dihydrochloride can be taken without regard to food consumption. Perennial Allergic Rhinitis (2.1) • Children 6 months to 2 years of age: 1.25 mg (1/2 teaspoon oral solution) (2.5mL) once daily in the evening Chronic Idiopathic Urticaria (2.2) • 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) (2.5 mL) once daily in the evening • Renal Impairment Adjust the dose in patients 12 years of age and older with decreased renal function (12.3)
2.1Perennial Allergic Rhinitis Children 6 months to 2 Years of Age The recommended initial dose of levocetirizine dihydrochloride is 1.25 mg (1/2 teaspoon oral solution) (2.5mL) once daily in the evening. The 1.25 mg once daily dose should not be exceeded based on comparable exposure to adults receiving 5 mg [see Clinical Pharmacology (12.3)] .
2.2Chronic Idiopathic Urticaria Adults and Children 12 Years of Age and Older The recommended dose of levocetirizine dihydrochloride is 5 mg (2 teaspoons [10 mL] oral solution) once daily in the evening. Some patients may be adequately controlled by 2.5 mg (1 teaspoon [5 mL] oral solution) once daily in the evening. Children 6 to 11 Years of Age The recommended dose of levocetirizine dihydrochloride is 2.5 mg (1 teaspoon [5 mL] oral solution) once daily in the evening.
The 2.5 mg dose should not be exceeded because the systemic exposure with 5 mg is approximately twice that of adults [see Clinical Pharmacology (12.3)] . Children 6 months to 5 Years of Age The recommended initial dose of levocetirizine dihydrochloride is 1.25 mg (1/2 teaspoon oral solution) (2.5 mL) once daily in the evening. The 1.25 mg once daily dose should not be exceeded based on comparable exposure to adults receiving 5 mg [see Clinical Pharmacology (12.3)] .
Dose Adjustment for Renal and Hepatic Impairment In adults and children 12 years of age and older with: • Mild renal impairment (creatinine clearance [CL CR ] = 50-80 mL/min): a dose of 2.5 mg once daily is recommended; • Moderate renal impairment (CL CR = 30-50 mL/min): a dose of 2.5 mg once every other day is recommended; • Severe renal impairment (CL CR = 10-30 mL/min): a dose of 2.5 mg twice weekly (administered once every 3-4 days) is recommended; • End-stage renal disease patients (CL CR < 10 mL/min) and patients undergoing hemodialysis should not receive levocetirizine dihydrochloride.
No dose adjustment is needed in patients with solely hepatic impairment. In patients with both hepatic impairment and renal impairment, adjustment of the dose is recommended.
💊 Dosage Forms and Strengths ▾
3 DOSAGE FORMS AND STRENGTHS Levocetirizine dihydrochloride oral solution is a clear, colorless liquid containing 0.5 mg of levocetirizine dihydrochloride per mL. • Immediate release oral solution, 2.5 mg per 5 mL (0.5 mg per mL) (3)
⛔ Contraindications ▾
4 CONTRAINDICATIONS The use of levocetirizine dihydrochloride is contraindicated in: • Patients with a known hypersensitivity to levocetirizine or any of the ingredients of levocetirizine dihydrochloride or to cetirizine (4.1) • Patients with end-stage renal disease at less than 10 mL/min creatinine clearance or patients undergoing hemodialysis (4.2) • Children 6 months to 11 years of age with renal impairment (4.3)
4.1Patients with Known Hypersensitivity Patients with known hypersensitivity to levocetirizine or any of the ingredients of levocetirizine dihydrochloride, or to cetirizine. Observed reactions range from urticaria to anaphylaxis [see Adverse Reactions (6.2)] .
4.2Patients with End-Stage Renal Disease Patients with end-stage renal disease (CL CR < 10 mL/min) and patients undergoing hemodialysis.
4.3Pediatric Patients with Impaired Renal Function Children 6 months to 11 years of age with impaired renal function.
⚠️ Warnings and Cautions ▾
5 WARNINGS AND PRECAUTIONS • Avoid engaging in hazardous occupations requiring complete mental alertness such as driving or operating machinery when taking levocetirizine dihydrochloride (5.1). • Avoid concurrent use of alcohol or other central nervous system depressants with levocetirizine dihydrochloride (5.1). • Use with caution in patients with predisposing factors of urinary retention (e.g. spinal cord lesion, prostatic hyperplasia). Discontinue levocetirizine dihydrochloride if urinary retention occurs (5.2).
5.1Somnolence In clinical trials the occurrence of somnolence, fatigue, and asthenia has been reported in some patients under therapy with levocetirizine dihydrochloride. Patients should be cautioned against engaging in hazardous occupations requiring complete mental alertness, and motor coordination such as operating machinery or driving a motor vehicle after ingestion of levocetirizine dihydrochloride. Concurrent use of levocetirizine dihydrochloride with alcohol or other central nervous system depressants should be avoided because additional reductions in alertness and additional impairment of central nervous system performance may occur.
5.2Urinary Retention Urinary retention has been reported post-marketing with levocetirizine dihydrochloride. Levocetirizine dihydrochloride should be used with caution in patients with predisposing factors of urinary retention (e.g. spinal cord lesion, prostatic hyperplasia) as levocetirizine dihydrochloride may increase the risk of urinary retention. Discontinue levocetirizine dihydrochloride if urinary retention occurs.
🤒 Adverse Reactions ▾
6 ADVERSE REACTIONS Use of levocetirizine dihydrochloride has been associated with somnolence, fatigue, asthenia and urinary retention [see Warnings and Precautions (5)] . 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 (6.1). To report SUSPECTED ADVERSE REACTIONS, contact Perrigo at 1-866-634-9120 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.
6.1Clinical Trials Experience The safety data described below reflect exposure to levocetirizine dihydrochloride in 2708 patients with allergic rhinitis or chronic idiopathic urticaria in 14 controlled clinical trials of 1 week to 6 months duration. The short-term (exposure up to 6 weeks) safety data for adults and adolescents are based upon eight clinical trials in which 1896 patients (825 males and 1071 females aged 12 years and older) were treated with levocetirizine dihydrochloride 2.5, 5, or 10 mg once daily in the evening.
The short-term safety data from pediatric patients are based upon two clinical trials in which 243 children with allergic rhinitis (162 males and 81 females 6 to 12 years of age) were treated with levocetirizine dihydrochloride 5 mg once daily for 4 to 6 weeks, one clinical trial in which 114 children (65 males and 49 females 1 to 5 years of age) with allergic rhinitis or chronic idiopathic urticaria were treated with levocetirizine dihydrochloride 1.25 mg twice daily for 2 weeks, and one clinical trial in which 45 children (28 males and 17 females 6 to 11 months of age) with symptoms of allergic rhinitis or chronic urticaria were treated with levocetirizine dihydrochloride 1.25 mg once daily for 2 weeks.
The long-term (exposure of 4 or 6 months) safety data in adults and adolescents are based upon two clinical trials in which 428 patients (190 males and 238 females) with allergic rhinitis were exposed to treatment with levocetirizine dihydrochloride 5 mg once daily. Long term safety data are also available from an 18-month trial in 255 levocetirizine dihydrochloride-treated subjects 12-24 months of age. Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trial of another drug and may not reflect the rates observed in practice.
Adults and Adolescents 12 years of Age and Older In studies up to 6 weeks in duration, the mean age of the adult and adolescent patients was 32 years, 44% of the patients were men and 56% were women, and the large majority (more than 90%) was Caucasian. In these trials 43% and 42% of the subjects in the levocetirizine dihydrochloride 2.5 mg and 5 mg groups, respectively, had at least one adverse event compared to 43% in the placebo group. In placebo-controlled trials of 1-6 weeks in duration, the most common adverse reactions were somnolence, nasopharyngitis, fatigue, dry mouth, and pharyngitis, and most were mild to moderate in intensity.
Somnolence with levocetirizine dihydrochloride showed dose ordering between tested doses of 2.5, 5 and 10 mg and was the most common adverse reaction leading to discontinuation (0.5%). Table 1 lists adverse reactions that were reported in greater than or equal to 2% of subjects aged 12 years and older exposed to levocetirizine dihydrochloride 2.5 mg or 5 mg in eight placebo-controlled clinical trials and that were more common with levocetirizine dihydrochloride than placebo. Table 1: Adverse Reactions Reported in ≥ 2%* of Subjects Aged 12 Years and Older Exposed to Levocetirizine dihydrochloride 2.5 mg or 5…
🔄 Drug Interactions ▾
7 DRUG INTERACTIONS In vitro data indicate that levocetirizine is unlikely to produce pharmacokinetic interactions through inhibition or induction of liver drug-metabolizing enzymes. No in vivo drug-drug interaction studies have been performed with levocetirizine. Drug interaction studies have been performed with racemic cetirizine.
7.1Antipyrine, Azithromycin, Cimetidine, Erythromycin, Ketoconazole, Theophylline, and Pseudoephedrine Pharmacokinetic interaction studies performed with racemic cetirizine demonstrated that cetirizine did not interact with antipyrine, pseudoephedrine, erythromycin, azithromycin, ketoconazole, and cimetidine. There was a small decrease (~16%) in the clearance of cetirizine caused by a 400 mg dose of theophylline. It is possible that higher theophylline doses could have a greater effect.
7.2Ritonavir Ritonavir increased the plasma AUC of cetirizine by about 42% accompanied by an increase in half-life (53%) and a decrease in clearance (29%) of cetirizine. The disposition of ritonavir was not altered by concomitant cetirizine administration.
👥 Use in Specific Populations ▾
8 USE IN SPECIFIC POPULATIONS • Renal Impairment Because levocetirizine dihydrochloride is substantially excreted by the kidneys, the risk of adverse reactions to this drug may be greater in patients with impaired renal function (8.6, 12.3). • Pediatric Use Do not exceed the recommended doses of 2.5 mg and 1.25 mg once daily in children 6 to 11 years and 6 months to 5 years of age, respectively. Systemic exposure with these doses in respective pediatric age groups is comparable to that from a 5 mg once daily dose in adults (12.3).
8.1Pregnancy Risk Summary Available data from published literature and post-marketing experience with levocetirizine use in pregnant women are insufficient to identify any drug-associated risks of miscarriage, birth defects, or adverse maternal or fetal outcomes. In animal reproduction studies, there was no evidence of fetal harm with administration of levocetirizine by the oral route to pregnant rats and rabbits, during the period of organogenesis, at doses up to 390 times and 470 times, respectively, the maximum recommended human dose (MRHD) in adults.
In rats treated during late gestation and the lactation period, cetirizine had no effects on pup development at oral doses up to approximately 60 times the MRHD in adults. In mice treated during late gestation and the lactation period, cetirizine administered by the oral route to the dams had no effects on pup development at a dose that was approximately 25 times the MRHD in adults; however, lower pup weight gain during lactation was observed at a dose that was 95 times the MRHD in adults (see Data) . The estimated background risk of major birth defects and miscarriage for the indicated population is unknown.
All pregnancies have a background risk of birth defect, loss, or other adverse outcomes. In the U.S. general population, the estimated background risks of major birth defects and miscarriage in clinically recognized pregnancies is 2% to 4% and 15% to 20%, respectively. Data Animal Data In embryo-fetal development studies, pregnant rats received daily doses of levocetirizine up to 200 mg/kg/day from gestation days 6 to 15 and pregnant rabbits received daily doses of levocetirizine up to 120 mg/kg/day from gestation days 6 to 18.
Levocetirizine produced no evidence of fetal harm in rats and rabbits at doses up to 390 and 470 times the MRHD, respectively (on a mg/m 2 basis with maternal oral doses of 200 and 120 mg/kg/day in rats and rabbits, respectively). No prenatal and postnatal development (PPND) studies in animals have been conducted with levocetirizine. In a PPND study conducted in mice, cetirizine was administered at oral doses up to 96 mg/kg/day from gestation day 15 through lactation day 21.
Cetirizine lowered pup body weight gain during lactation at an oral dose in dams that was approximately 95 times the MRHD (on a mg/m 2 basis with a maternal oral dose of 96 mg/kg/day); however, there were no effects on pup weight gain at an oral dose in dams that was approximately 25 times the MRHD (on a mg/m 2 basis with a maternal oral dose of 24 mg/kg/day). In a PPND study conducted in rats, cetirizine was administered at oral doses up to 180 mg/kg/day from gestation day 17 to lactation day 22. Cetirizine did not have any adverse effects on rat dams or offspring development at doses up to approximately 60 times the MRHD (on a mg/m 2 basis with a maternal oral dose of 30 mg/kg/day).
Cetirizine caused excessive maternal toxicity at an oral dose in dams that was approximately 350 times the MRHD (on a mg/m 2 basis with a maternal oral dose of 180 mg/kg/day).
8.2Lactation Risk Summary There are no data on the presence of levocetirizine in human milk, the effects on the breastfed infant, or the effects on milk production. However, cetirizine has been reported to be present in human breast milk. In mice and beagle dogs, studies indicated that cetirizine was excreted in milk (see Data) . When a drug is present in animal milk, it is likely the drug will b…
🤰 Pregnancy ▾
8.1Pregnancy Risk Summary Available data from published literature and post-marketing experience with levocetirizine use in pregnant women are insufficient to identify any drug-associated risks of miscarriage, birth defects, or adverse maternal or fetal outcomes. In animal reproduction studies, there was no evidence of fetal harm with administration of levocetirizine by the oral route to pregnant rats and rabbits, during the period of organogenesis, at doses up to 390 times and 470 times, respectively, the maximum recommended human dose (MRHD) in adults.
In rats treated during late gestation and the lactation period, cetirizine had no effects on pup development at oral doses up to approximately 60 times the MRHD in adults. In mice treated during late gestation and the lactation period, cetirizine administered by the oral route to the dams had no effects on pup development at a dose that was approximately 25 times the MRHD in adults; however, lower pup weight gain during lactation was observed at a dose that was 95 times the MRHD in adults (see Data) . The estimated background risk of major birth defects and miscarriage for the indicated population is unknown.
All pregnancies have a background risk of birth defect, loss, or other adverse outcomes. In the U.S. general population, the estimated background risks of major birth defects and miscarriage in clinically recognized pregnancies is 2% to 4% and 15% to 20%, respectively. Data Animal Data In embryo-fetal development studies, pregnant rats received daily doses of levocetirizine up to 200 mg/kg/day from gestation days 6 to 15 and pregnant rabbits received daily doses of levocetirizine up to 120 mg/kg/day from gestation days 6 to 18.
Levocetirizine produced no evidence of fetal harm in rats and rabbits at doses up to 390 and 470 times the MRHD, respectively (on a mg/m 2 basis with maternal oral doses of 200 and 120 mg/kg/day in rats and rabbits, respectively). No prenatal and postnatal development (PPND) studies in animals have been conducted with levocetirizine. In a PPND study conducted in mice, cetirizine was administered at oral doses up to 96 mg/kg/day from gestation day 15 through lactation day 21.
Cetirizine lowered pup body weight gain during lactation at an oral dose in dams that was approximately 95 times the MRHD (on a mg/m 2 basis with a maternal oral dose of 96 mg/kg/day); however, there were no effects on pup weight gain at an oral dose in dams that was approximately 25 times the MRHD (on a mg/m 2 basis with a maternal oral dose of 24 mg/kg/day). In a PPND study conducted in rats, cetirizine was administered at oral doses up to 180 mg/kg/day from gestation day 17 to lactation day 22. Cetirizine did not have any adverse effects on rat dams or offspring development at doses up to approximately 60 times the MRHD (on a mg/m 2 basis with a maternal oral dose of 30 mg/kg/day).
Cetirizine caused excessive maternal toxicity at an oral dose in dams that was approximately 350 times the MRHD (on a mg/m 2 basis with a maternal oral dose of 180 mg/kg/day).
🧒 Pediatric Use ▾
8.4Pediatric Use The recommended dose of levocetirizine dihydrochloride for the treatment of the uncomplicated skin manifestations of chronic idiopathic urticaria in patients 6 months to 17 years of age is based on extrapolation of efficacy from adults 18 years of age and older [see Clinical Studies (14)] . The recommended dose of levocetirizine dihydrochloride in patients 6 months to 2 years of age for the treatment of the symptoms of perennial allergic rhinitis and 6 months to 11 years of age with chronic idiopathic urticaria is based on cross-study comparisons of the systemic exposure of levocetirizine dihydrochloride in adults and pediatric patients and on the safety profile of levocetirizine dihydrochloride in both adult and pediatric patients at doses equal to or higher than the recommended dose for patients 6 months to 11 years of age.
The safety of levocetirizine dihydrochloride 5 mg once daily was evaluated in 243 pediatric patients 6 to 12 years of age in two placebo-controlled clinical trials lasting 4 and 6 weeks. The safety of levocetirizine dihydrochloride 1.25 mg twice daily was evaluated in one 2-week clinical trial in 114 pediatric patients 1 to 5 years of age and the safety of levocetirizine dihydrochloride 1.25 mg once daily was evaluated in one 2-week clinical trial in 45 pediatric patients 6 to 11 months of age [see Adverse Reactions (6.1)] .
The effectiveness of levocetirizine dihydrochloride 1.25 mg once daily (6 months to 5 years of age) and 2.5 mg once daily (6 to 11 years of age) for the treatment of the symptoms of perennial allergic rhinitis and chronic idiopathic urticaria is supported by the extrapolation of demonstrated efficacy of levocetirizine dihydrochloride 5 mg once daily in patients 12 years of age and older based on the pharmacokinetic comparison between adults and children. Cross-study comparisons indicate that administration of a 5 mg dose of levocetirizine dihydrochloride to 6 to 12 year old pediatric patients resulted in about 2-fold the systemic exposure (AUC) observed when 5 mg of levocetirizine dihydrochloride was administered to healthy adults.
Therefore, in children 6 to 11 years of age the recommended dose of 2.5 mg once daily should not be exceeded. In a population pharmacokinetics study the administration of 1.25 mg once daily in children 6 months to 5 years of age resulted in systemic exposure comparable to 5 mg once daily in adults [see Dosage and Administration (2.2); Clinical Studies (14); and Clinical Pharmacology (12.3)] .
🧓 Geriatric Use ▾
8.5Geriatric Use Clinical studies of levocetirizine dihydrochloride for each approved indication did not include sufficient numbers of patients aged 65 years and older to determine whether they respond differently than younger patients. Other reported clinical experience has not identified differences in responses between the elderly and younger patients. In general, dose selection for an elderly patient should be cautious, usually starting at the low end of the dosing range reflecting the greater frequency of decreased hepatic, renal, or cardiac function and of concomitant disease or other drug therapy.
🆘 Overdosage ▾
10 OVERDOSAGE Overdosage has been reported with levocetirizine dihydrochloride. Symptoms of overdose may include drowsiness in adults. In children agitation and restlessness may initially occur, followed by drowsiness.
There is no known specific antidote to levocetirizine dihydrochloride. Should overdose occur, symptomatic or supportive treatment is recommended. Levocetirizine dihydrochloride is not effectively removed by dialysis, and dialysis will be ineffective unless a dialyzable agent has been concomitantly ingested.
The acute maximal non-lethal oral dose of levocetirizine was 240 mg/kg in mice (approximately 190 times the maximum recommended daily oral dose in adults, approximately 230 times the maximum recommended daily oral dose in children 6 to 11 years of age, and approximately 180 times the maximum recommended daily oral dose in children 6 months to 5 years of age on a mg/m 2 basis). In rats the maximal non-lethal oral dose was 240 mg/kg (approximately 390 times the maximum recommended daily oral dose in adults, approximately 460 times the maximum recommended daily oral dose in children 6 to 11 years of age, and approximately 370 times the maximum recommended daily oral dose in children 6 months to 5 years of age on a mg/m 2 basis).
🧬 Clinical Pharmacology ▾
12 CLINICAL PHARMACOLOGY
12.1Mechanism of Action Levocetirizine, the active enantiomer of cetirizine, is an antihistamine; its principal effects are mediated via selective inhibition of H 1 receptors. The antihistaminic activity of levocetirizine has been documented in a variety of animal and human models. In vitro binding studies revealed that levocetirizine has an affinity for the human H 1 -receptor 2-fold higher than that of cetirizine (Ki = 3 nmol/L vs .
6 nmol/L, respectively). The clinical relevance of this finding is unknown.
12.2Pharmacodynamics Studies in healthy adult subjects showed that levocetirizine at doses of 2.5 mg and 5 mg inhibited the skin wheal and flare caused by the intradermal injection of histamine. In contrast, dextrocetirizine exhibited no clear change in the inhibition of the wheal and flare reaction. Levocetirizine at a dose of 5 mg inhibited the wheal and flare caused by intradermal injection of histamine in 14 pediatric subjects (aged 6 to 11 years) and the activity persisted for at least 24 hours.
The clinical relevance of histamine wheal skin testing is unknown. A QT/QTc study using a single dose of 30 mg of levocetirizine did not demonstrate an effect on the QTc interval. While a single dose of levocetirizine had no effect, the effects of levocetirizine may not be at steady state following single dose.
The effect of levocetirizine on the QTc interval following multiple dose administration is unknown. Levocetirizine is not expected to have QT/QTc effects because of the results of QTc studies with cetirizine and the long post-marketing history of cetirizine without reports of QT prolongation.
12.3Pharmacokinetics Levocetirizine exhibited linear pharmacokinetics over the therapeutic dose range in healthy adult subjects. Absorption Levocetirizine is rapidly and extensively absorbed following oral administration. In adults, peak plasma concentrations are achieved 0.9 hour after administration of the oral tablet.
The accumulation ratio following daily oral administration is 1.12 with steady state achieved after 2 days. Peak concentrations are typically 270 ng/mL and 308 ng/mL following a single and a repeated 5 mg once daily dose, respectively. Food had no effect on the extent of exposure (AUC) of the levocetirizine tablet, but T max was delayed by about 1.25 hours and C max was decreased by about 36% after administration with a high fat meal; therefore, levocetirizine can be administered with or without food.
A dose of 5 mg (10 mL) of levocetirizine dihydrochloride oral solution is bioequivalent to a 5 mg dose of levocetirizine dihydrochloride tablets. Following oral administration of a 5 mg dose of levocetirizine dihydrochloride oral solution to healthy adult subjects, the mean peak plasma concentrations were achieved approximately 0.5 hour post-dose. Distribution The mean plasma protein binding of levocetirizine in vitro ranged from 91 to 92%, independent of concentration in the range of 90-5000 ng/mL, which includes the therapeutic plasma levels observed.
Following oral dosing, the average apparent volume of distribution is approximately
0.4L/kg, representative of distribution in total body water. Metabolism The extent of metabolism of levocetirizine in humans is less than 14% of the dose and therefore differences resulting from genetic polymorphism or concomitant intake of hepatic drug metabolizing enzyme inhibitors are expected to be negligible. Metabolic pathways include aromatic oxidation, N- and O-dealkylation, and taurine conjugation.
Dealkylation pathways are primarily mediated by CYP3A4 while aromatic oxidation involves multiple and/or unidentified CYP isoforms. Elimination The plasma half-life in healthy adult subjects was about 8 to 9 hours after administration of oral tablets and oral solution, and the mean oral total body clearance for levocetirizine was approximately 0.63 mL/kg/min. The major route of excretion of levocetirizine and its metabolites is via urine, accounting for…
🧬 Mechanism of Action ▾
12.1Mechanism of Action Levocetirizine, the active enantiomer of cetirizine, is an antihistamine; its principal effects are mediated via selective inhibition of H 1 receptors. The antihistaminic activity of levocetirizine has been documented in a variety of animal and human models. In vitro binding studies revealed that levocetirizine has an affinity for the human H 1 -receptor 2-fold higher than that of cetirizine (Ki = 3 nmol/L vs .
6 nmol/L, respectively). The clinical relevance of this finding is unknown.
📦 How Supplied / Storage and Handling ▾
16 HOW SUPPLIED/STORAGE AND HANDLING Levocetirizine dihydrochloride oral solution is a clear, colorless liquid containing 0.5 mg of levocetirizine dihydrochloride per mL. Oral solution in 150 mL PET plastic bottles (NDC 63629-2533-1) Storage: Store at 20°C to 25°C (68°F to 77°F); excursions permitted to 15°C to 30°C (59°F to 86°F) [see USP Controlled Room Temperature]. Repackaged/Relabeled by: Bryant Ranch Prepack, Inc. Burbank, CA 91504
📋 Description ▾
11 DESCRIPTION Levocetirizine dihydrochloride, the active component of levocetirizine dihydrochloride oral solution, is an orally active H 1 -receptor antagonist. The chemical name is (R)-[2-[4-[(4-chlorophenyl) phenylmethyl]- 1-piperazinyl] ethoxy] acetic acid dihydrochloride. Levocetirizine dihydrochloride is the R enantiomer of cetirizine hydrochloride, a racemic compound with antihistaminic properties.
The empirical formula of levocetirizine dihydrochloride is C 21 H 25 ClN 2 O 3 •2HCl. The molecular weight is 461.82 and the chemical structure is shown below: Levocetirizine dihydrochloride is a white, crystalline powder and is water soluble. Levocetirizine dihydrochloride 0.5 mg/mL oral solution is formulated as an immediate release, clear, colorless liquid.
Inactive ingredients are: sodium acetate trihydrate, glacial acetic acid, maltitol solution, glycerin, methylparaben, propylparaben, saccharin, flavoring (consisting of triacetin, natural & artificial flavors, dl-alpha-tocopherol), purified water.
💬 Information for Patients ▾
17 PATIENT COUNSELING INFORMATION Somnolence Caution patients against engaging in hazardous occupations requiring complete mental alertness, and motor coordination such as operating machinery or driving a motor vehicle after ingestion of levocetirizine dihydrochloride. Concomitant Use of Alcohol and other Central Nervous System Depressants Instruct patients to avoid concurrent use of levocetirizine dihydrochloride with alcohol or other central nervous system depressants because additional reduction in mental alertness may occur.
Dosing of Levocetirizine dihydrochloride Do not exceed the recommended daily dose in adults and adolescents 12 years of age and older of 5 mg once daily in the evening. In children 6 to 11 years of age the recommended dose is 2.5 mg once daily in the evening. In children 6 months to 5 years of age, the recommended dose is 1.25 mg once daily in the evening.
Advise patients to not ingest more than the recommended dose of levocetirizine dihydrochloride because of the increased risk of somnolence at higher doses.