levocetirizine

Therapeutic Class
H1-antagonist
Indications

Relief of symptoms associated with seasonal (adults and children ≥2 yrs) and perennial (adults and children ≥6 months) allergic rhinitis. Treatment of uncomplicated skin manifestations of chronic idiopathic urticaria in adults and children ≥6 months.

Adult: As hydrochloride: 5 mg daily in the evening; 2.5 mg may be adequate in some patients. Max dose: 5 mg daily.

Child: As hydrochloride: 6-11 yr: 2.5 mg once daily. Max dose: 2.5 mg daily. ≥12 yr: 5 mg once daily; 2.5 mg may be adequate is some patients. Max dose: 5 mg daily. All doses to be taken in the evening.

CrCl (ml/min) Dosage Recommendation
50-80 2.5 mg once daily.
30-50 2.5 mg every other day.
10-30 2.5 mg twice wkly (give every 3-4 days).

Special Populations: If CrCl 30-50 mL/minute, 5 mg on alternate days. If CrCl < 30 mL/minute, avoid.

Contraindications

End-stage renal disease (ESRD) (CrCl <10mL/min) .

Patients undergoing hemodialysis.

Pediatrics 6 months-11 yrs with renal impairment.

Lactation

Warnings / Precautions

Renal impairment.

Somnolence, fatigue, and asthenia reported, May impair ability to drive or operate machinery. May impair mental/physical abilities. Urinary retention reported; caution with predisposing factors of urinary retention (eg, spinal cord lesion, prostatic hyperplasia). D/C if urinary retention occurs. Caution in elderly.

Adverse Reactions

Somnolence, fatigue, nasopharyngitis, dry mouth, constipation, diarrhea, cough, pyrexia, pharyngitis,epistaxis.

Drug Interactions

Avoid with alcohol and other CNS depressants because additional reductions in alertness and additional CNS performance impairment may occur. Decreased clearance with theophylline. Increased plasma area under the curve with ritonavir.

Mechanism of Actions

Levocetirizine, an active isomer of cetirizine, selectively inhibits histamine H1-receptors.

Absorption: Rapid and extensive. Cmax=270ng/mL (single dose), 308ng/mL (multiple doses); Tmax=0.9 hr (tab), 0.5 hr (PO sol).

Distribution: Vd=0.4L/kg; plasma protein binding (91-92%); found in breast milk.

Metabolism: <14% metabolized through aromatic oxidation (via CYP isoforms), N- and O-dealkylation (via CYP3A4), and taurine conjugation pathways.

Elimination: Urine (85.4%), feces (12.9%); T1/2=8-9 hrs.

Assesment

Assess for all factors mentioned in Contraindications,  if undergoing hemodialysis. Assess for ESRD, hypersensitivity to the drug, predisposing factors of urinary retention, renal function, pregnancy/nursing status, and possible drug interactions.

Monitoring

Monitor for all sign & symptoms mentioned in Adverse Drug Reactions.

Patient Counselling

Instruct to use caution when engaging in hazardous occupations requiring complete mental alertness and motor coordination (e.g. operating machinery, driving, ) after ingestion of drug. Instruct to avoid alcohol or other CNS depressants, and to not ingest more than the recommended dose.

Administration

Oral route:  May be taken with or without food.

Storage: 20-25°C (68-77°F); excursions permitted to 15-30°C (59-86°F).

Pregnancy Category

B: Drug Pregnancy Category Animal reproduction studies have failed to demonstrate a risk to the fetus and there are no adequate and well-controlled studies in pregnant women OR Animal studies have shown an adverse effect, but adequate and well-controlled studies in pregnant women have failed to demonstrate a risk to the fetus in any trimester.

ATC Classification
R06AE09
GenericPedia Classification
  • ,
  • Sign & Symptoms
  • Fatigue, Abnormal
  • Dry Mouth (Xerostomia)
  • Constipation
  • Diarrhoea
  • Cough
  • Fever (Pyrexia)
  • Epistaxis
  • Available As
  • Levocetirizine 0.8 mg
  • Levocetirizine 1 mg
  • Levocetirizine 10 mg
  • Levocetirizine 2.5 mg
  • Levocetirizine 30 mg
  • Levocetirizine 5 mg
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    One Response to levocetirizine

    1. March 12, 2014 at 1:16 pm #

      Not effevtive

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