What Is Levocetirizine 5 Mg Used to Treat?
What is Xyzal and how is it used?
Xyzal is a prescription medicine used to treat the symptoms of Allergic Rhinitis and Chronic Urticaria. Xyzal may be used lone or with other medications.
Xyzal belongs to a grade of drugs called Antihistamines, 2nd Generation.
It is not known if Xyzal is prophylactic and effective in children younger than vi months of age.
What are the possible side effects of Xyzal?
Xyzal may cause serious side furnishings including:
- worsening allergy or urticaria symptoms,
- painful or difficult urination,
- niggling or no urination,
- lightheadedness,
- fever,
- ear pain or total feeling,
- problem hearing,
- drainage from the ear, and
- fussiness in a kid
Get medical aid correct away, if you lot take any of the symptoms listed above.
The most common side effects of Xyzal include:
- drowsiness,
- tiredness,
- sinus pain,
- ear infection,
- coughing,
- fever,
- nosebleed,
- vomiting,
- diarrhea,
- constipation,
- dry oral fissure, and
- weight gain
Tell the doc if you lot have any side effect that bothers you lot or that does not go abroad.
These are not all the possible side furnishings of Xyzal. For more information, inquire your doctor or pharmacist.
Phone call your doctor for medical advice near side effects. You may written report side effects to FDA at ane-800-FDA-1088.
DESCRIPTION
Levocetirizine dihydrochloride, the agile component of XYZAL tablets and oral solution, is an orally active H1-receptor adversary. The chemical name is (R)-[two-[4-[(4-chlorophenyl) phenylmethyl]-i-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 C21H25ClN2Oiii•2HCl. The molecular weight is 461.82 and the chemical construction is shown below:
Levocetirizine dihydrochloride is a white, crystalline powder and is water soluble.
XYZAL 5 mg tablets are formulated as immediate release, white, movie-coated, oval-shaped scored tablets for oral administration. The tablets are imprinted on both halves of the scored line with the letter Y in reddish (Opacode® Red). Inactive ingredients are: microcrystalline cellulose, lactose monohydrate, colloidal anhydrous silica, and magnesium stearate. The film blanket contains hypromellose, titanium dioxide, and macrogol 400.
XYZAL 0.5 mg/mL oral solution is formulated as an firsthand 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.
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INDICATIONS
Perennial Allergic Rhinitis
XYZAL is indicated for the relief of symptoms associated with perennial allergic rhinitis in children 6 months to 2 years of historic period.
Chronic Idiopathic Urticaria
XYZAL is indicated for the treatment of the uncomplicated peel manifestations of chronic idiopathic urticaria in adults and children 6 months of age and older.
DOSAGE AND ADMINISTRATION
XYZAL is available as 2.5 mg/five mL (0.v mg/mL) oral solution and as 5 mg breakable (scored) tablets, allowing for the assistants of 2.5 mg, if needed. XYZAL can exist taken without regard to food consumption.
Perennial Allergic Rhinitis
Children 6 Months To ii Years Of Age
The recommended initial dose of XYZAL is 1.25 mg (1/2 teaspoon oral solution) (2.5 mL) once daily in the evening. The i.25 mg once daily dose should not be exceeded based on comparable exposure to adults receiving 5 mg [see CLINICAL PHARMACOLOGY].
Chronic Idiopathic Urticaria
Adults And Children 12 Years Of Age And Older
The recommended dose of XYZAL is 5 mg (1 tablet or ii teaspoons [10 mL] oral solution) once daily in the evening. Some patients may be adequately controlled past 2.5 mg (one/2 tablet or 1 teaspoon [5 mL] oral solution) once daily in the evening.
Children vi To 11 Years Of Age
The recommended dose of XYZAL is two.5 mg (1/2 tablet or 1 teaspoon [5 mL] oral solution) once daily in the evening. The two.5 mg dose should not be exceeded considering the systemic exposure with 5 mg is approximately twice that of adults [see CLINICAL PHARMACOLOGY].
Children 6 Months To five Years Of Age
The recommended initial dose of XYZAL is 1.25 mg (1/2 teaspoon oral solution) (two.5 mL) in one case daily in the evening. The 1.25 mg one time daily dose should not exist exceeded based on comparable exposure to adults receiving 5 mg [see CLINICAL PHARMACOLOGY].
Dose Adjustment For Renal And Hepatic Harm
In adults and children 12 years of age and older with:
- Mild renal damage (creatinine clearance [CLCR] = 50-eighty mL/min): a dose of 2.five mg once daily is recommended;
- Moderate renal impairment (CLCR = 30-50 mL/min): a dose of two.5 mg once every other twenty-four hour period is recommended;
- Astringent renal impairment (CLCR = x-30 mL/min): a dose of 2.5 mg twice weekly (administered once every 3-4 days) is recommended;
- End-phase renal disease patients (CLCR <ten mL/min) and patients undergoing hemodialysis should not receive XYZAL.
No dose adjustment is needed in patients with solely hepatic damage. In patients with both hepatic impairment and renal impairment, adjustment of the dose is recommended.
HOW SUPPLIED
Dosage Forms And Strengths
XYZAL oral solution is a clear, colorless liquid containing 0.5 mg of levocetirizine dihydrochloride per mL.
XYZAL tablets are white, film-coated, oval-shaped, scored, imprinted (with the letter of the alphabet Y in red colour on both halves of the scored tablet) and incorporate 5 mg levocetirizine dihydrochloride.
Storage And Handling
XYZAL tablets are white, picture show-coated, oval-shaped, scored, imprinted (with the letter Y in red color on both halves of the scored tablet) and contain 5 mg levocetirizine dihydrochloride. They are supplied in unit of measurement of utilise HDPE bottles.
90 Tablets (NDC 0024-5803-90)
XYZAL oral solution is a clear, colorless liquid containing 0.5 mg of levocetirizine dihydrochloride per mL.
Oral Solution in 5 oz polypropylene bottles (NDC 0024-5804-05)
Storage
Store at 20°C to 25°C (68°F to 77°F); excursions permitted to 15°C to thirty°C (59°F to 86°F) [see USP Controlled Room Temperature].
Manufactured for: A SANOFI COMPANY, sanofi-aventis, U.S. LLC Bridgewater, NJ 08807. Revised: April 2019
QUESTION
Allergies tin best be described every bit: Encounter AnswerSIDE Furnishings
Use of XYZAL has been associated with somnolence, fatigue, asthenia, and urinary retentivity [see WARNINGS AND PRECAUTIONS].
Clinical Trials Experience
The safe data described below reverberate exposure to XYZAL in 2708 patients with allergic rhinitis or chronic idiopathic urticaria in 14 controlled clinical trials of 1 week to 6 months elapsing.
The short-term (exposure up to 6 weeks) safety information for adults and adolescents are based upon viii clinical trials in which 1896 patients (825 males and 1071 females aged 12 years and older) were treated with XYZAL 2.5, five, or 10 mg in one case daily in the evening.
The short-term prophylactic information 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 XYZAL five 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 XYZAL 1.25 mg twice daily for 2 weeks, and one clinical trial in which 45 children (28 males and 17 females half dozen to 11 months of age) with symptoms of allergic rhinitis or chronic urticaria were treated with XYZAL 1.25 mg once daily for 2 weeks.
The long-term (exposure of iv or 6 months) safety data in adults and adolescents are based upon 2 clinical trials in which 428 patients (190 males and 238 females) with allergic rhinitis were exposed to treatment with XYZAL 5 mg once daily. Long term safety data are likewise available from an 18-month trial in 255 XYZAL-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 some other drug and may non reflect the rates observed in do.
Adults And Adolescents 12 Years Of Age And Older
In studies up to half-dozen weeks in duration, the hateful 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 XYZAL ii.5 mg and 5 mg groups, respectively, had at least one adverse upshot compared to 43% in the placebo grouping.
In placebo-controlled trials of one-6 weeks in duration, the almost common adverse reactions were somnolence, nasopharyngitis, fatigue, dry mouth, and pharyngitis, and most were balmy to moderate in intensity. Somnolence with XYZAL showed dose ordering between tested doses of 2.5, v and 10 mg and was the most mutual agin reaction leading to discontinuation (0.5%).
Tabular array 1 lists adverse reactions that were reported in greater than or equal to 2% of subjects anile 12 years and older exposed to XYZAL 2.5 mg or 5 mg in eight placebo-controlled clinical trials and that were more common with XYZAL than placebo.
Table 1: Agin Reactions Reported in ≥ii%* of Subjects Anile 12 Years and Older Exposed to XYZAL 2.5 mg or 5 mg In one case Daily in Placebo-Controlled Clinical Trials 1-6 Weeks in Elapsing
| Adverse Reactions | XYZAL ii.5 mg (n = 421) | XYZAL five mg (n = 1070) | Placebo (n = 912) |
| Somnolence | 22 (5%) | 61 (6%) | xvi (2%) |
| Nasopharyngitis | 25 (6%) | forty (4%) | 28 (three%) |
| Fatigue | five (1%) | 46 (4%) | twenty (2%) |
| Dry Mouth | 12 (3%) | 26 (2%) | 11 (one%) |
| Pharyngitis | 10 (two%) | 12 (1%) | 9 (1%) |
| * Rounded to the closest unit percentage | |||
Boosted agin reactions of medical significance observed at a higher incidence than in placebo in adults and adolescents anile 12 years and older exposed to XYZAL are syncope (0.two%) and weight increased (0.v%).
Pediatric Patients 6 To 12 Years Of Age
A total of 243 pediatric patients 6 to 12 years of historic period received XYZAL 5 mg once daily in ii curt-term placebo controlled double-blind trials. The mean age of the patients was nine.8 years, 79 (32%) were six to eight years of age, and l% were Caucasian. Table 2 lists adverse reactions that were reported in greater than or equal to 2% of subjects aged 6 to 12 years exposed to XYZAL 5 mg in placebo-controlled clinical trials and that were more than common with XYZAL than placebo.
Table 2: Adverse Reactions Reported in ≥2%* of Subjects Aged 6-12 Years Exposed to XYZAL 5 mg Once Daily in Placebo-Controlled Clinical Trials 4 and 6 Weeks in Duration
| Agin Reactions | XYZAL 5 mg (north = 243) | Placebo (n = 240) |
| Pyrexia | 10 (4%) | 5 (2%) |
| Cough | viii (iii%) | 2 (<ane%) |
| Somnolence | seven (3%) | 1 (<1%) |
| Epistaxis | half-dozen (2%) | 1 (<1%) |
| * Rounded to the closest unit percentage | ||
Pediatric Patients 1 To five Years Of Age
A total of 114 pediatric patients 1 to 5 years of historic period received XYZAL 1.25 mg twice daily in a ii week placebo-controlled double-blind safety trial. The mean age of the patients was three.8 years, 32% were 1 to 2 years of age, 71% were Caucasian and 18% were Black. Table three lists agin reactions that were reported in greater than or equal to 2% of subjects aged 1 to 5 years exposed to XYZAL 1.25 mg twice daily in the placebo-controlled condom trial and that were more common with XYZAL than placebo.
Table 3: Adverse Reactions Reported in ≥two%* of Subjects Aged 1-5 Years Exposed to XYZAL one.25 mg Twice Daily in a 2-Calendar week Placebo-Controlled Clinical Trial
| Agin Reactions | XYZAL i.25 mg Twice Daily (n = 114) | Placebo (n = 59) |
| Pyrexia | 5 (4%) | 1 (ii%) |
| Diarrhea | 4 (4%) | two (iii%) |
| Vomiting | four (four%) | 2 (3%) |
| Otitis Media | 3 (3%) | 0 (0%) |
| * Rounded to the closest unit percentage | ||
Pediatric Patients 6 To 11 Months Of Historic period
A total of 45 pediatric patients 6 to 11 months of historic period received XYZAL 1.25 mg once daily in a two calendar week placebo-controlled double-blind safety trial. The mean age of the patients was 9 months, 51% were Caucasian and 31% were Black. Agin reactions that were reported in more than than 1 bailiwick (i.e. greater than or equal to three% of subjects) aged 6 to 11 months exposed to XYZAL 1.25 mg in one case daily in the placebo-controlled prophylactic trial and that were more common with XYZAL than placebo included diarrhea and constipation which were reported in 6 (xiii%) and i (4%) and 3 (seven%) and ane (4%) children in the XYZAL and placebo-treated groups, respectively.
Long-Term Clinical Trials Experience
In two controlled clinical trials, 428 patients (190 males and 238 females) aged 12 years and older were treated with XYZAL 5 mg once daily for 4 or 6 months. The patient characteristics and the safety profile were like to that seen in the brusque-term studies. Ten (ii.3%) patients treated with XYZAL discontinued considering of somnolence, fatigue or asthenia compared to 2 (<i%) in the placebo group.
There are no long term clinical trials in children below 12 years of historic period with allergic rhinitis or chronic idiopathic urticaria.
Laboratory Test Abnormalities
Elevations of blood bilirubin and transaminases were reported in <1% of patients in the clinical trials. The elevations were transient and did not lead to discontinuation in any patient.
Postmarketing Experience
In addition to the adverse reactions reported during clinical trials and listed above, the following adverse reactions have as well been identified during postapproval use of XYZAL. Because these reactions are reported voluntarily from a population of uncertain size, it is not always possible to reliably estimate their frequency or found a causal relationship to drug exposure.
- Cardiac disorders: palpitations, tachycardia
- Ear and labyrinth disorders: vertigo
- Eye disorders: blurred vision, visual disturbances
- Gastrointestinal disorders: nausea, vomiting
- General disorders and assistants site conditions: edema
- Hepatobiliary disorders: hepatitis
- Immune organization disorders: anaphylaxis and hypersensitivity
- Metabolism and nutrition disorders: increased appetite
- Musculoskeletal, connective tissues, and bone disorders: arthralgia, myalgia
- Nervous system disorders: dizziness, dysgeusia, delirious seizure, motion disorders (including dystonia and oculogyric crisis), paresthesia, seizure (reported in subjects with and without a known seizure disorder), tremor
- Psychiatric disorders: aggression and agitation, depression, hallucinations, indisposition, nightmare, suicidal ideation
- Renal and urinary disorders: dysuria, urinary retention
- Respiratory, thoracic, and mediastinal disorders: dyspnea
- Skin and subcutaneous tissue disorders: angioedema, stock-still drug eruption, pruritus, rash and urticaria
Also these reactions reported under treatment with XYZAL, other potentially astringent adverse events have been reported from the postmarketing experience with cetirizine. Since levocetirizine is the principal pharmacologically agile component of cetirizine, one should take into account the fact that the following adverse events could also potentially occur nether treatment with XYZAL.
- Cardiac disorders: severe hypotension
- Gastrointestinal disorders: cholestasis
- Nervous system disorders: extrapyramidal symptoms, myoclonus, orofacial dyskinesia, tic
- Pregnancy, puerperium and perinatal conditions: stillbirth
- Renal and urinary disorders: glomerulonephritis
- Skin and subcutaneous tissue disorders: astute generalized exanthematous pustulosis (AGEP); rebound pruritus -pruritus within a few days subsequently discontinuation of cetirizine, usually afterwards long-term use (eastward.one thousand. months to years) of cetirizine.
DRUG INTERACTIONS
In vitro data indicate that levocetirizine is unlikely to produce pharmacokinetic interactions through inhibition or consecration of liver drug-metabolizing enzymes. No in vivo drug-drug interaction studies have been performed with levocetirizine. Drug interaction studies take been performed with racemic cetirizine.
Antipyrine, 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. In that location 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 event.
Ritonavir
Ritonavir increased the plasma AUC of cetirizine by about 42% accompanied by an increase in one-half-life (53%) and a decrease in clearance (29%) of cetirizine. The disposition of ritonavir was not altered by concomitant cetirizine assistants.
WARNINGS
Included as part of the "PRECAUTIONS" Section
PRECAUTIONS
Somnolence
In clinical trials the occurrence of somnolence, fatigue, and asthenia has been reported in some patients under therapy with XYZAL. Patients should be cautioned against engaging in hazardous occupations requiring complete mental alacrity, and motor coordination such equally operating machinery or driving a motor vehicle later on ingestion of XYZAL. Concurrent use of XYZAL with alcohol or other primal nervous system depressants should be avoided because additional reductions in alacrity and additional impairment of central nervous system operation may occur.
Urinary Memory
Urinary retention has been reported postal service marketing with XYZAL. XYZAL should be used with caution in patients with predisposing factors of urinary retention (eastward.g. spinal cord lesion, prostatic hyperplasia) every bit XYZAL may increment the risk of urinary retentivity. Discontinue XYZAL if urinary retention occurs.
Nonclinical Toxicology
Carcinogenesis, Mutagenesis, Impairment Of Fertility
No carcinogenicity studies have been performed with levocetirizine. However, evaluation of cetirizine carcinogenicity studies is relevant for conclusion of the carcinogenic potential of levocetirizine. In a ii-year carcinogenicity study, in rats, cetirizine was non carcinogenic at dietary doses up to 20 mg/kg (approximately xl, xl, 25, and ten times the MRHDs in adults, children six to 11 years of historic period, children ii-v years, and children half dozen months to two years of historic period, respectively, on a mg/m2 basis). In a 2-year carcinogenicity study in mice, cetirizine acquired an increased incidence of beneficial hepatic tumors in males at a dietary dose of 16 mg/kg (approximately 15, 15, nine, and v times the MRHDs in adults, children half dozen to 11 years of age, children 2-5 years, and children 6 months to 2 years of age, respectively, on a mg/10002 basis). No increased incidence of beneficial tumors was observed at a dietary dose of four mg/kg (approximately 4, four, 2, and 1 times the MRHDs in adults, children six to eleven years of age, children ii-5 years, and children 6 months to 2 years of age, respectively on a mg/m2 basis). The clinical significance of these findings during long-term use of XYZAL is not known.
Levocetirizine was not mutagenic in the Ames exam, and not clastogenic in the human being lymphocyte assay, the mouse lymphoma assay, and in vivo micronucleus test in mice.
Fertility and reproductive functioning were unaffected in male person and female mice and rats that received cetirizine at oral doses up to 64 and 200 mg/kg/day, respectively (approximately 60 and 390 times the MRHD in adults on a mg/mii footing).
Use In Specific Populations
Pregnancy
Risk Summary
Bachelor information from published literature and postmarketing experience with levocetirizine use in significant women are insufficient to place any drug-associated risks of miscarriage, birth defects, or adverse maternal or fetal outcomes. In creature reproduction studies, there was no testify of fetal harm with administration of levocetirizine by the oral route to pregnant rats and rabbits, during the catamenia of organogenesis, at doses upwards to 390 times and 470 times, respectively, the maximum recommended human being dose (MRHD) in adults. In rats treated during belatedly gestation and the lactation period, cetirizine had no furnishings on pup development at oral doses up to approximately threescore times the MRHD in adults. In mice treated during late gestation and the lactation menstruation, cetirizine administered past the oral route to the dams had no furnishings on pup development at a dose that was approximately 25 times the MRHD in adults; however, lower pup weight proceeds during lactation was observed at a dose that was 95 times the MRHD in adults [see Data].
The estimated background risk of major nascency defects and miscarriage for the indicated population is unknown. All pregnancies have a background risk of nativity defect, loss, or other adverse outcomes. In the U.South. general population, the estimated background risks of major nascency defects and miscarriage in clinically recognized pregnancies is ii% to 4% and 15% to 20%, respectively.
Data
Beast data
In embryo-fetal development studies, pregnant rats received daily doses of levocetirizine upwardly to 200 mg/kg/twenty-four hour period from gestation days 6 to fifteen and pregnant rabbits received daily doses of levocetirizine up to 120 mg/kg/24-hour interval from gestation days vi 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/mtwo ground 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 accept 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 mean solar day 15 through lactation twenty-four hours 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/m2 basis with a maternal oral dose of 96 mg/kg/day); however, there were no furnishings on pup weight proceeds at an oral dose in dams that was approximately 25 times the MRHD (on a mg/mii footing 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/mean solar day from gestation solar day 17 to lactation day 22. Cetirizine did not have any adverse effects on rat dams or offspring development at doses upward to approximately 60 times the MRHD (on a mg/mii basis with a maternal oral dose of thirty mg/kg/day). Cetirizine caused excessive maternal toxicity at an oral dose in dams that was approximately 350 times the MRHD (on a mg/m2 footing with a maternal oral dose of 180 mg/kg/day).
Lactation
Risk Summary
There are no information 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 [run into Data]. When a drug is present in animal milk, it is likely the drug will be present in human milk. The developmental and wellness benefits of breastfeeding should be considered along with the mother's clinical need for XYZAL and whatever potential agin effects on the breastfed child from XYZAL or from the underlying maternal condition.
Data
Animal data
Cetirizine was detected in the milk of mice. No adverse developmental effects on pups were seen when cetirizine was administered orally to dams during lactation at a dose that was approximately 25 times the MRHD in adults [see Pregnancy]. Studies in beagle dogs indicated that approximately 3% of the dose of cetirizine was excreted in milk. The concentration of drug in animate being milk does non necessarily predict the concentration of drug in human milk.
Pediatric Use
The recommended dose of XYZAL for the handling of the uncomplicated skin manifestations of chronic idiopathic urticaria in patients half-dozen months to 17 years of historic period is based on extrapolation of efficacy from adults 18 years of age and older [encounter Clinical Studies].
The recommended dose of XYZAL in patients vi months to ii 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 XYZAL in adults and pediatric patients and on the rubber profile of XYZAL in both adult and pediatric patients at doses equal to or college than the recommended dose for patients 6 months to 11 years of age.
The prophylactic of XYZAL 5 mg in one case daily was evaluated in 243 pediatric patients 6 to 12 years of age in two placebo-controlled clinical trials lasting 4 and half dozen weeks. The safety of XYZAL 1.25 mg twice daily was evaluated in one ii-week clinical trial in 114 pediatric patients 1 to 5 years of age and the safety of XYZAL 1.25 mg once daily was evaluated in i 2-week clinical trial in 45 pediatric patients 6 to 11 months of age [run into ADVERSE REACTIONS].
The effectiveness of XYZAL 1.25 mg one time daily (6 months to 5 years of age) and 2.five mg in one case 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 XYZAL 5 mg once daily in patients 12 years of age and older based on the pharmacokinetic comparing between adults and children.
Cantankerous-study comparisons indicate that assistants of a 5 mg dose of XYZAL to 6 to 12 yr old pediatric patients resulted in about 2-fold the systemic exposure (AUC) observed when 5 mg of XYZAL was administered to healthy adults. Therefore, in children 6 to eleven years of historic period the recommended dose of 2.v mg one time daily should not be exceeded. In a population pharmacokinetics study the administration of 1.25 mg one time daily in children half dozen months to 5 years of age resulted in systemic exposure comparable to five mg once daily in adults. [see DOSAGE AND ADMINISTRATION, Clinical Studies , and CLINICAL PHARMACOLOGY].
Geriatric Utilise
Clinical studies of XYZAL for each canonical indication did not include sufficient numbers of patients anile 65 years and older to determine whether they answer differently than younger patients. Other reported clinical feel has not identified differences in responses betwixt the elderly and younger patients. In general, dose pick 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 role and of concomitant disease or other drug therapy.
Renal Impairment
XYZAL is known to be substantially excreted by the kidneys and the risk of adverse reactions to this drug may be greater in patients with dumb renal function. Considering elderly patients are more likely to have decreased renal role, care should be taken in dose selection and it may exist useful to monitor renal office [see DOSAGE AND ADMINISTRATION and CLINICAL PHARMACOLOGY].
Hepatic Impairment
As levocetirizine is mainly excreted unchanged by the kidneys, it is unlikely that the clearance of levocetirizine is significantly decreased in patients with solely hepatic damage [run into CLINICAL PHARMACOLOGY].
Overdosage & Contraindications
OVERDOSE
Overdosage has been reported with XYZAL.
Symptoms of overdose may include drowsiness in adults. In children agitation and restlessness may initially occur, followed past drowsiness. There is no known specific antitoxin to XYZAL. Should overdose occur, symptomatic or supportive treatment is recommended. XYZAL is not finer removed by dialysis, and dialysis will exist 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 vi to xi years of age, and approximately 180 times the maximum recommended daily oral dose in children 6 months to 5 years of historic period on a mg/mii 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 xi 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/mtwo basis).
CONTRAINDICATIONS
The use of XYZAL is contraindicated in:
Patients With Known Hypersensitivity
Patients with known hypersensitivity to levocetirizine or any of the ingredients of XYZAL, or to cetirizine. Observed reactions range from urticaria to anaphylaxis [run across Adverse REACTIONS].
Patients With Stop-Stage Renal Disease
Patients with cease-stage renal disease (CLCR <ten mL/min) and patients undergoing hemodialysis
Pediatric Patients With Impaired Renal Part
Children 6 months to xi years of age with impaired renal function
CLINICAL PHARMACOLOGY
Machinery Of Activity
Levocetirizine, the active enantiomer of cetirizine, is an antihistamine; its primary effects are mediated via selective inhibition of H1 receptors. The antihistaminic activity of levocetirizine has been documented in a diverseness of animal and homo models. In vitro binding studies revealed that levocetirizine has an analogousness for the homo Hone-receptor two-fold college than that of cetirizine (Ki = three nmol/50 vs. half-dozen nmol/L, respectively). The clinical relevance of this finding is unknown.
Pharmacodynamics
Studies in developed good for you 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 five mg inhibited the wheal and flare acquired by intradermal injection of histamine in 14 pediatric subjects (aged 6 to 11 years) and the activeness 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 xxx mg of levocetirizine did not demonstrate an effect on the QTc interval. While a single dose of levocetirizine had no result, the effects of levocetirizine may non exist at steady state following single dose. The effect of levocetirizine on the QTc interval following multiple dose administration is unknown. Levocetirizine is non expected to have QT/QTc effects considering of the results of QTc studies with cetirizine and the long postmarketing history of cetirizine without reports of QT prolongation.
Pharmacokinetics
Levocetirizine exhibited linear pharmacokinetics over the therapeutic dose range in adult healthy subjects.
Assimilation
Levocetirizine is apace and extensively absorbed following oral administration. In adults, peak plasma concentrations are accomplished 0.9 60 minutes later on administration of the oral tablet. The accumulation ratio following daily oral administration is 1.12 with steady state achieved after two days. Summit concentrations are typically 270 ng/mL and 308 ng/mL post-obit 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 Tmax was delayed by nigh 1.25 hours and Cmax was decreased by about 36% after administration with a high fatty meal; therefore, levocetirizine can be administered with or without food.
A dose of 5 mg (ten mL) of XYZAL oral solution is bioequivalent to a 5 mg dose of XYZAL tablets. Following oral administration of a five mg dose of XYZAL oral solution to healthy adult subjects, the mean superlative 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. Post-obit oral dosing, the average apparent volume of distribution is approximately 0.4 Fifty/kg, representative of distribution in full body h2o.
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, North-and O-dealkylation, and taurine conjugation. Dealkylation pathways are primarily mediated by CYP3A4 while aromatic oxidation involves multiple and/or unidentified CYP isoforms.
Emptying
The plasma half-life in adult salubrious subjects was about 8 to ix hours after administration of oral tablets and oral solution, and the hateful oral total body clearance for levocetirizine was approximately 0.63 mL/kg/min. The major road of excretion of levocetirizine and its metabolites is via urine, bookkeeping for a mean of 85.4% of the dose. Excretion via feces accounts for but 12.9% of the dose. Levocetirizine is excreted both by glomerular filtration and active tubular secretion. Renal clearance of levocetirizine correlates with that of creatinine clearance. In patients with renal impairment the clearance of levocetirizine is reduced [see DOSAGE AND Assistants].
Drug Interaction Studies
In vitro data on metabolite interaction signal that levocetirizine is unlikely to produce, or exist field of study to metabolic interactions. Levocetirizine at concentrations well to a higher place Cmax level achieved within the therapeutic dose ranges is not an inhibitor of CYP isoenzymes 1A2, 2C9, 2C19, 2A1, 2D6, 2E1, and 3A4, and is not an inducer of UGT1A or CYP isoenzymes 1A2, 2C9 and 3A4.
No formal in vivo drug interaction studies accept been performed with levocetirizine. Studies take been performed with the racemic cetirizine [run across DRUG INTERACTIONS].
Pediatric patients
Data from a pediatric pharmacokinetic study with oral administration of a unmarried dose of 5 mg levocetirizine in 14 children age half dozen to 11 years with body weight ranging betwixt 20 and 40 kg show that Cmax and AUC values are about 2-fold greater than that reported in good for you developed subjects in a cross-study comparison. The mean Cmax was 450 ng/mL, occurring at a mean time of 1.2 hours, weight-normalized, total body clearance was 30% greater, and the elimination half-life 24% shorter in this pediatric population than in adults.
Dedicated pharmacokinetic studies take non been conducted in pediatric patients younger than 6 years of historic period. A retrospective population pharmacokinetic assay was conducted in 323 subjects (181 children 1 to 5 years of age, eighteen children half-dozen to 11 years of age, and 124 adults 18 to 55 years of age) who received single or multiple doses of levocetirizine ranging from ane.25 mg to 30 mg. Information generated from this analysis indicated that administration of one.25 mg one time daily to children half dozen months to 5 years of age results in plasma concentrations similar to those of adults receiving 5 mg in one case daily.
Geriatric Patients
Limited pharmacokinetic data are available in elderly subjects. Post-obit once daily echo oral administration of 30 mg levocetirizine for 6 days in nine elderly subjects (65-74 years of age), the total body clearance was approximately 33% lower compared to that in younger adults. The disposition of racemic cetirizine has been shown to be dependent on renal role rather than on age. This finding would also be applicable for levocetirizine, every bit levocetirizine and cetirizine are both predominantly excreted in urine. Therefore, the XYZAL dose should be adjusted in accordance with renal function in elderly patients [see DOSAGE AND ADMINISTRATION].
Gender
Pharmacokinetic results for 77 patients (40 men, 37 women) were evaluated for potential result of gender. The one-half-life was slightly shorter in women (seven.08 ± 1.72 60 minutes) than in men (eight.62 ± 1.84 hour); however, the trunk weight-adjusted oral clearance in women (0.67 ± 0.16 mL/min/kg) appears to exist comparable to that in men (0.59 ± 0.12 mL/min/kg). The same daily doses and dosing intervals are applicable for men and women with normal renal role.
Race
The effect of race on levocetirizine has not been studied. As levocetirizine is primarily renally excreted, and there are no important racial differences in creatinine clearance, pharmacokinetic characteristics of levocetirizine are not expected to be different across races. No race-related differences in the kinetics of racemic cetirizine have been observed.
Renal Harm
Levocetirizine exposure (AUC) exhibited i.eight-, 3.2-, iv.3-, and 5.vii-fold increase in balmy, moderate, severe, renal impaired, and end-phase renal disease patients, respectively, compared to healthy subjects. The corresponding increases of half-life estimates were 1.4-, 2.0-, 2.nine-, and 4fold, respectively.
The full trunk clearance of levocetirizine after oral dosing was correlated to the creatinine clearance and was progressively reduced based on severity of renal impairment. Therefore, it is recommended to adjust the dose and dosing intervals of levocetirizine based on creatinine clearance in patients with balmy, moderate, or astringent renal impairment. In end-phase renal illness patients (CLCR < 10 mL/min) levocetirizine is contraindicated. The corporeality of levocetirizine removed during a standard 4-hour hemodialysis procedure was <10%.
The dosage of XYZAL should exist reduced in patients with mild renal impairment. Both the dosage and frequency of administration should be reduced in patients with moderate or severe renal damage [run into DOSAGE AND Administration].
Hepatic Harm
XYZAL has not been studied in patients with hepatic impairment. The non-renal clearance (indicative of hepatic contribution) was found to constitute almost 28% of the total body clearance in healthy adult subjects afterwards oral administration.
As levocetirizine is mainly excreted unchanged by the kidney, it is unlikely that the clearance of levocetirizine is significantly decreased in patients with solely hepatic impairment [see DOSAGE AND Assistants].
Clinical Studies
Perennial Allergic Rhinitis
Adults And Adolescents 12 Years Of Historic period And Older
The efficacy of XYZAL was evaluated in four randomized, placebo-controlled, double-blind clinical trials in developed and adolescent patients 12 years and older with symptoms of perennial allergic rhinitis. The four clinical trials include two dose-ranging trials of 4 weeks duration and two efficacy trials (ane vi-week and one 6-month) in patients with perennial allergic rhinitis.
These trials included a full of 1729 patients (752 males and 977 females) of whom 227 were adolescents 12 to 17 years of historic period. Efficacy was assessed using a full symptom score from patient recording of 4 symptoms (sneezing, rhinorrhea, nasal pruritus, and ocular pruritus) in three studies and five symptoms (sneezing, rhinorrhea, nasal pruritus, ocular pruritus, and nasal congestion) in one study. Patients recorded symptoms using a 0-3 categorical severity scale (0 = absent, i = mild, two = moderate, 3 = astringent) once daily in the evening reflective of the 24 hour handling menstruum. The primary endpoint was the mean full symptom score averaged over the first week and over 4 weeks for perennial allergic rhinitis trials.
The two dose-ranging trials were conducted to evaluate the efficacy of XYZAL 2.5, five, and 10 mg once daily in the evening. These trials were 4 weeks in duration and included patients with perennial allergic rhinitis. In these trials, each of the three doses of XYZAL demonstrated greater subtract in the reflective total symptom score than placebo and the deviation was statistically significant for all three doses in the ii studies. Results for i of these trials are shown in Table 4.
Table 4: Mean Reflective Total Symptom Score* in Allergic Rhinitis Dose-Ranging Trials
| Treatment | Due north | Baseline | On Treatment Adjusted Mean | Difference from Placebo | ||
| Approximate | 95% CI | p-value | ||||
| Perennial Allergic Rhinitis Trial – Cogitating full symptom score | ||||||
| XYZAL 2.v mg | 133 | 7.14 | four.12 | 1.17 | (0.71, 1.63) | <0.001 |
| XYZAL five mg | 127 | 7.18 | four.07 | 1.22 | (0.76, 1.69) | <0.001 |
| XYZAL 10 mg | 129 | vii.58 | 4.19 | one.10 | (0.64, one.57) | <0.001 |
| Placebo | 128 | 7.22 | 5.29 | |||
| *Full symptom score is the sum of individual symptoms of sneezing, rhinorrhea, nasal pruritus, and ocular pruritus as assessed by patients on a 0-3 categorical severity scale. | ||||||
Ane clinical trial evaluated the efficacy of XYZAL 5 mg once daily in the evening compared to placebo in patients with perennial allergic rhinitis over a 6-week treatment period. Another trial conducted over a half dozen-month treatment flow assessed efficacy at 4 weeks. XYZAL 5 mg demonstrated a greater decrease from baseline in the reflective total symptom score than placebo and the departure from placebo was statistically significant. Results of the one-time are shown in Table 5.
Table 5: Mean Cogitating Total Symptom Score* in Allergic Rhinitis Trials
| Handling | Due north | Baseline | On Treatment Adjusted Mean | Difference from Placebo | ||
| Estimate | 95% CI | p-value | ||||
| Perennial Allergic Rhinitis Trial – Reflective full symptom score | ||||||
| XYZAL five mg | 150 | 7.69 | three.93 | 1.17 | (0.70, 1.64) | <0.001 |
| Placebo | 142 | 7.44 | 5.x | |||
| * Total symptom score is the sum of individual symptoms of sneezing, rhinorrhea, nasal pruritus, and ocular pruritus as assessed by patients on a 0-3 categorical severity scale. | ||||||
Onset of action was evaluated in two environmental exposure unit studies in allergic rhinitis patients with a single dose of XYZAL 2.5 or 5 mg. XYZAL five mg was found to have an onset of action 1 60 minutes after oral intake. Onset of activity was besides assessed from the daily recording of symptoms in the evening before dosing in the allergic rhinitis trials. In these trials, onset of effect was seen after 1 day of dosing.
Pediatric Patients Less Than 12 Years Of Age
There are no clinical efficacy trials with XYZAL two.5 mg once daily in pediatric patients under 12 years of age, and no clinical efficacy trials with XYZAL 1.25 mg once daily in pediatric patients half dozen months to 5 years of age. The clinical efficacy of XYZAL in pediatric patients under 12 years of age has been extrapolated from adult clinical efficacy trials based on pharmacokinetic comparisons [meet Use In Specific Populations].
Chronic Idiopathic Urticaria
Adult Patients 18 Years Of Age And Older
The efficacy of XYZAL for the treatment of the elementary pare manifestations of chronic idiopathic urticaria was evaluated in two multi-center, randomized, placebo-controlled, double-bullheaded clinical trials of 4 weeks duration in adult patients xviii to 85 years of age with chronic idiopathic urticaria. The two trials included 1 4-week dose-ranging trial and one 4-week single-dose level efficacy trial. These trials included 423 patients (139 males and 284 females). Near patients (>90%) were Caucasian and the hateful age was 41. Of these patients, 146 received XYZAL 5 mg once daily in the evening. Efficacy was assessed based on patient recording of pruritus severity on a severity score of 0-3 (0 = none to 3 = severe). The primary efficacy endpoint was the mean reflective pruritus severity score over the showtime week and over the unabridged treatment catamenia. Boosted efficacy variables were the instantaneous pruritus severity score, the number and size of wheals, and duration of pruritus.
The dose-ranging trial was conducted to evaluate the efficacy of XYZAL 2.5, 5, and x mg once daily in the evening. In this trial, each of the 3 doses of XYZAL demonstrated greater decrease in the reflective pruritus severity score than placebo and the difference was statistically pregnant for all iii doses (encounter Table half-dozen).
The single dose level trial evaluated the efficacy of XYZAL 5 mg once daily in the evening compared to placebo in patients with chronic idiopathic urticaria over a 4-week treatment period.
XYZAL 5 mg demonstrated a greater decrease from baseline in the reflective pruritus severity score than placebo and the difference from placebo was statistically significant.
Duration of pruritus, number and size of wheals, and instantaneous pruritus severity score likewise showed meaning improvement over placebo. The significant improvement in the instantaneous pruritus severity score over placebo confirmed end of dosing interval efficacy (encounter Table 6).
Table 6: Hateful Reflective Pruritus Severity Score in Chronic Idiopathic Urticaria Trials
| Treatment | N | Baseline | On Handling Adapted Mean | Difference from Placebo | ||
| Judge | 95% CI | p-value | ||||
| Dose-Ranging Trial – Reflective pruritus severity score | ||||||
| XYZAL 2.five mg | 69 | two.08 | 1.02 | 0.82 | (0.58, 1.06) | <0.001 |
| XYZAL v mg | 62 | 2.07 | 0.92 | 0.91 | (0.66, ane.16) | <0.001 |
| XYZAL x mg | 55 | 2.04 | 0.73 | 1.11 | (0.85, 1.37) | <0.001 |
| Placebo | lx | 2.25 | 1.84 | |||
| Chronic Idiopathic Urticaria Trial – Reflective pruritus severity score | ||||||
| XYZAL five mg | 80 | 2.07 | 0.94 | 0.62 | (0.38, 0.86) | <0.001 |
| Placebo | 82 | 2.06 | ane.56 | |||
Pediatric Patients
In that location are no clinical efficacy trials in pediatric patients with chronic idiopathic urticaria [see Employ In Specific Populations].
PATIENT INFORMATION
Somnolence
Circumspection patients against engaging in hazardous occupations requiring consummate mental alertness, and motor coordination such every bit operating mechanism or driving a motor vehicle after ingestion of XYZAL.
Concomitant Use Of Alcohol And Other Central Nervous System Depressants
Instruct patients to avert concurrent use of XYZAL with alcohol or other fundamental nervous system depressants considering boosted reduction in mental alertness may occur.
Dosing Of Xyzal
Practise non exceed the recommended daily dose in adults and adolescents 12 years of age and older of v mg once daily in the evening. In children half dozen to xi years of age the recommended dose is 2.5 mg once daily in the evening. In children 6 months to 5 years of historic period, the recommended dose is one.25 mg one time daily in the evening. Suggest patients to not ingest more than the recommended dose of XYZAL because of the increased risk of somnolence at higher doses.
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