Pharmacologic Category
Histamine H1 Antagonist; Histamine H1 Antagonist, Second Generation; Piperidine Derivative
Dosing: Adult
Allergic rhinitis: Adults ≤65 years: Intranasal: Two sprays in each nostril twice daily; if necessary, may increase dose to 2 sprays 3 to 4 times daily; consider therapy discontinuation if no response within 3 days. Continuous treatment >10 weeks has not been evaluated.
Dosing: Renal Impairment: Adult
There are no dosage adjustments provided in the manufacturer's labeling; use with caution.
Dosing: Hepatic Impairment: Adult
There are no dosage adjustments provided in the manufacturer's labeling.
Dosing: Pediatric
Allergic rhinitis: Children ≥12 years and Adolescents: Intranasal: Refer to adult dosing.
Use: Labeled Indications
Note: Not approved in the US
Allergic rhinitis: Symptomatic treatment of allergic rhinitis in patients 12 years and older.
Administration: Intranasal
Shake bottle well before each use. Prior to initial use, bottle should be primed until a fine spray is delivered. Instruct patients to blow nose and clear nasal passages before administering spray and to inhale nasally while spraying.
Administration: Pediatric
Intranasal: Shake bottle well before each use. Prior to initial use, bottle should be primed until a fine spray is delivered. Instruct patients to blow nose and clear nasal passages before administering spray and to inhale nasally while spraying.
Storage/Stability
Store at 15°C to 30°C (59°F to 86°F).
Medication Safety Issues
Sound-alike/look-alike issues:
International issues:
Contraindications
Hypersensitivity to levocabastine or any component of the formulation
Warnings/Precautions
Disease-related concerns:
• Renal impairment: Use caution; limited data available regarding use in this population.
Geriatric Considerations
Evaluate the patient's or caregiver's ability to safely administer the correct dose of nasal medication.
Pregnancy Considerations
Adverse events were observed in some animal reproduction studies when using oral doses much larger than the equivalent maximum human nasal dose.
Breast-Feeding Considerations
Following intranasal application, minute amounts of levocabastine have been detected in human breast milk (Simons 1999). The manufacturer recommends that caution be exercised when administering levocabastine to nursing women.
Adverse Reactions
Most adverse reactions are transient. Frequency not always defined.
1% to 10%:
Central nervous system: Fatigue (1%)
Local: Application site burning, application site irritation, application site pain, application site reaction (dryness, discomfort)
Ophthalmic: Eye irritation (3%; mostly with concomitant levocabastine eye drop administration)
Respiratory: Epistaxis (1%), pharyngolaryngeal pain, sinusitis
<1%, postmarketing, and/or case reports: Abdominal pain, anaphylaxis, application site reactions (nasal edema), bronchospasm, cough, dry nose, dysgeusia, dyspnea, eyelid edema, facial edema, hearing loss, hypersensitivity, increased appetite, malaise, nasal congestion, nasal obstruction (aggravated), nausea, palpitations, pruritus of ear (external), pruritus of nose, respiratory tract disease, rhinorrhea, skin rash, tachycardia, throat irritation, weight gain
Toxicology
Metabolism/Transport Effects
None known.
Drug Interactions Open Interactions
There are no known significant interactions.
Product Availability
Not available in the US
Dosage Forms: Canada
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Solution, Nasal:
Livostin: 0.05% (15 mL) [contains benzalkonium chloride, edetate disodium, polysorbate 80, propylene glycol]
Anatomic Therapeutic Chemical (ATC) Classification
Generic Available (US)
Yes
Mechanism of Action
Potent, selective histamine H1-receptor antagonist
Pharmacodynamics/Kinetics
Onset of action: 10 minutes
Absorption: Incomplete
Distribution: Vdss: 1.13 L/kg
Protein binding: ~55%
Metabolism: Hepatic (minimal)
Bioavailability: 60% to 80%
Half-life elimination: 35 to 40 hours
Time to peak: 3 hours
Excretion: Urine (65% to 70% as unchanged drug); feces (10% to 20% as unchanged drug) (Simons, 1999)
Local Anesthetic/Vasoconstrictor Precautions
No information available to require special precautions
Effects on Dental Treatment
Key adverse event(s) related to dental treatment: Xerostomia (normal salivary flow resumes upon discontinuation)
Effects on Bleeding
No information available to require special precautions
Index Terms
Levocabastine Hydrochloride
References
Livostin (levocabastine) [product monograph]. Toronto, Ontario, Canada: Janssen Inc: July 2013.[PubMed 10088031]
Simons FER and Simons KJ, “Clinical Pharmacology of New Histamine H1 Receptor Antagonists,” Clin Pharmacokinet, 1999, 36(5):329-52.[PubMed 10384858]
Brand Names: International
Bilina (ES); Livocab (DE, NL); Livostin (AE, AT, AU, BE, CH, CN, CZ, DK, EG, FI, GR, IL, IS, JP, KR, LB, LU, NO, NZ, PT, QA, SE, SI, VE, ZA)
Last Updated 4/17/19
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