levocetirizine (OTC)

Brand and Other Names:Xyzal Allergy 24HR Tablets, Xyzal Allergy 24HR Oral Solution, more...Xyzal
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

tablet

  • 5mg

oral solution

  • 2.5mg/5mL

Allergic Rhinitis

Indicated for relief of symptoms associated with seasonal and perennial allergic rhinitis

5 mg PO qDay in evening

Some patients may respond to 2.5 mg/day

Chronic Urticaria

Indicated for uncomplicated skin manifestations of chronic idiopathic urticaria

5 mg PO qDay in evening

Dosage Modifications

Renal impairment

  • CrCl 50-80 mL/min: 2.5 mg PO qDay
  • CrCl 30-50 mL/min: 2.5 mg PO every other day
  • CrCl 10-30 mL/min: 2.5 mg PO 2x/wk (ie, q3-4 days)
  • CrCl <10 mL/min and or hemodialysis: Contraindicated

Hepatic impairment

  • No dose adjustment required

Dosage Forms & Strengths

tablet

  • 5mg

oral solution

  • 2.5mg/5mL

Allergic Rhinitis

Indicated for relief of symptoms associated with seasonal and perennial allergic rhinitis

<6 months: Safety and efficacy not established

6 months to 5 years: 1.25 mg PO qDay in evening

6-12 years: 2.5 mg PO qDay in evening

>12 years: 5 mg PO qDay in evening; some patients may respond to 2.5 mg/day

Chronic Urticaria

Indicated for uncomplicated skin manifestations of chronic idiopathic urticaria

<6 months: Safety and efficacy not established

6 months to 5 years: 1.25 mg PO qDay in evening

6-12 years: 2.5 mg PO qDay in evening

>12 years: 5 mg PO qDay in evening

Dosage Modifications

Renal impairment

  • Aged ≥12 years
    • CrCl 50-80 mL/min: 2.5 mg PO qDay
    • CrCl 30-50 mL/min: 2.5 mg PO every other day
    • CrCl 10-30 mL/min: 2.5 mg PO 2x/wk (ie, q3-4 days)
    • CrCl <10 mL/min and or hemodialysis: Contraindicated
  • Aged 6 months to 11 years
    • Any degree of renal impairment: Contraindicated

Hepatic impairment

  • No dose adjustment required
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Interactions

Interaction Checker

and levocetirizine

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    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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            Adverse Effects

            Varies in incidence & severity with the individual drug; also individual patients vary in susceptibility

            1-10%

            Dry mouth

            Fatigue

            Nasopharyngitis

            Pharyngitis

            Frequency Not Defined

            CNS depression

            Drowsiness

            Sedation ranging from mild drowsiness to deep sleep (most frequent)

            Dizziness

            Lassitude

            Disturbed coordination

            Restlessness, insomnia, tremors, euphoria, nervousness, delirium, palpitation, seizures is less common

            Epigastric distress

            Anorexia

            Nausea

            Vomiting

            Diarrhea

            Constipation

            Cholestasis, hepatitis, hepatic failure, hepatic function abnormality, jaundice is rare

            Tachycardia, palpitation ECG changes (eg, widened QRS)

            Arrhythmias (eg, extrasystole, heart block)

            Hypotension

            Hypertension

            Dizziness, sedation, and hypotension may occur in geriatric patients

            Dryness of mouth, nose, and throat

            Dysuria

            Urinary retention

            Impotence

            Vertigo

            Visual disturbances

            Blurred vision

            Diplopia; tinnitus

            Acute labyrinthitis

            Insomnia

            Tremors

            Nervousness

            Irritability

            Facial dyskinesia

            Tightness of the chest

            Thickening of bronchial secretions

            Wheezing

            Nasal stuffiness

            Sweating

            Chills

            Early menses

            Toxic psychosis

            Headache

            Faintness

            Paresthesia

            Agranulocytosis

            Hemolytic anemia

            Leukopenia

            Thrombocytopenia

            Pancytopenia

            Postmarketing Reports

            Cardiac disorders: Palpitations, tachycardia

            Ear and labyrinth disorders: Vertigo

            Eye disorders: Blurred vision, visual disturbances

            Gastrointestinal disorders: Nausea, vomiting

            General disorders and administration site conditions: Edema

            Hepatobiliary disorders: Hepatitis

            Immune system disorders: Anaphylaxis and hypersensitivity

            Metabolism and nutrition disorders: Increased appetite

            Musculoskeletal, connective tissues, and bone disorders: Arthralgia, myalgia

            Nervous system disorders: Dizziness, dysgeusia, febrile seizure, movement disorders (including dystonia and oculogyric crisis), paraesthesia, seizure (reported in subjects with and without a known seizure disorder), tremor

            Psychiatric disorders: Aggression and agitation, depression, hallucinations, insomnia, nightmare, suicidal ideation

            Renal and urinary disorders: Dysuria, urinary retention

            Respiratory, thoracic, and mediastinal disorders: Dyspnea

            Skin and allergy: Hypersensitivity and anaphylaxis, angioedema, fixed drug eruption, pruritus, rash, acute generalized exanthematous pustulosis, and urticaria

            Postmarketing reports of cetirizine

            • 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: acute generalized exanthematous pustulosis (AGEP); rebound pruritus-pruritus within a few days after discontinuation of cetirizine, usually after long-term use (eg, months to years)
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            Warnings

            Contraindications

            Documented hypersensitivity

            Lower respiratory disease, eg, asthma (controversial)

            Preemies and neonates

            Nursing women

            Hypersensitivity to levocetirizine or cetirizine

            ESRD (CrCl <10 mL/min) or patients undergoing hemodialysis

            Children aged 6 month to 11 years with renal impairment

            Cautions

            Caution in narrow angle glaucoma, prostatic hypertrophy, stenosing peptic ulcer, pyloroduodenal obstruction, or bladder neck obstruction

            May impair mental alertness

            Avoid alcohol or other CNS depressants

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            Pregnancy & Lactation

            Pregnancy

            Available data from published literature and postmarketing experience in pregnant women are insufficient to identify any drug-associated risks of miscarriage, birth defects, or adverse maternal or fetal outcomes

            Animal data

            • In animal reproduction studies, there was no evidence of fetal harm with administration of levocetirizine by oral route to pregnant rats and rabbits, during period of organogenesis, at doses up to 390 times and 470 times, respectively, maximum recommended human dose (MRHD) in adults
            • Rats treated during late gestation and lactation period, 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 lactation period, drug administered by oral route to 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 MRHD in adults

            Lactation

            There are no data on presence of levocetirizine in human milk, effects on breastfed infant, or on milk production; however, drug has been reported to be present in human breast milk; in mice and beagle dogs, studies indicated cetirizine was excreted in milk; when a drug is present in animal milk, it is likely the drug will be present in human milk; developmental and health benefits of breastfeeding should be considered along with mother’s clinical need for therapy and any potential adverse effects on breastfed child from drug or from underlying maternal condition

            Pregnancy Categories

            A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

            B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

            C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

            D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

            X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

            NA: Information not available.

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            Pharmacology

            Mechanism of Action

            Histamine H1-receptor antagonist

            Absorption

            Peak Plasma Time: 0.5hr (oral solution); 0.9 hr (tablet)

            Peak Plasma Concentration (5 mg x1 dose): 270 ng/mL

            Onset: 1 hr (allergic rhinitis); 1 day (seasonal/perennial)

            Distribution

            Protein Bound: >90%

            Vd: 0.4 L/kg

            Metabolism

            Metabolism: CYP3A4 and other isoforms

            Elimination

            Half-Lfe: 8 hr

            Total Body Clearance: 0.63 mL/kg/min

            Excretion: urine: 85%; feces 13%

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            Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.