Chemical formula: C₂₆H₂₉FN₂O₂ Molecular mass: 420.528 g/mol PubChem compound: 54385
Levocabastine interacts in the following cases:
Oxymetazoline may temporarily reduce the absorption of nasal levocabastine.
Pregnancy Category B3.
In pregnant rats, levocabastine readily crossed the placental barrier and was distributed extensively in foetal tissues. Reproductive studies in mice and rats showed that levocabastine was embryolethal at oral doses greater than 40 mg/kg/day in both species, and teratogenic at oral doses greater than 40 mg/kg/day in mice and 20 mg/kg/day in rats. The main foetal malformations observed were open eyes in mice, and polydactyly, hydrocephalus, anophthalmia/microphthalmia, hydronephrosis and arthrogryposis in rats. There are limited postmarketing data on the use of levocabastine in pregnant women. The risk for humans is unknown. Therefore, levocabastine should not be used during pregnancy.
Based on determinations of levocabastine concentrations in saliva and breast milk in a nursing woman, who received a single oral dose of 0.5mg levocabastine, it is expected that approximately 0.6% of the total intranasally and approximately 0.3% of the total ophthalmically administered dose of levocabastine may be transferred to a nursing infant. However, due to the limited nature of the clinical and experimental data, it is recommended that levocabastine be avoided in breast-feeding mothers.
Levocabastine, in general, does not cause clinically significant suppression nor disturbes psychomotor function compared to placebo. Therefore, levocabastine is not expected to affect the ability to drive or operate machinery. If drowsiness occurs, caution is required.
The safety of levocabastine eye drops was evaluated in 508 subjects who participated in 4, placebocontrolled clinical trials and one open-label clinical trial. All adverse drug reactions (ADRs) reported by subjects in levocabastine eye drops clinical trials are presented in Table 1.
Table 1. Adverse Drug Reactions Reported by levocabastine eye drops Treated Subjects in 5 Clinical Trials:
| MedDRA System Organ Class-MedDRA PT | Levocabastine (n=508) % | Placebo (n=178) % |
|---|---|---|
| Eye Disorders | ||
| Eye Irritation | 11.6 | 4.5 |
The safety of levocabastine nasal spray was evaluated in 2328 subjects who participated in 12 double-blind, placebo-controlled clinical trials. Adverse drug reactions (ADRs) reported in ≥1% of subjects in these trials are presented in Table 2.
Table 2: Adverse Drug Reactions Reported by ≥1% levocabastine nasal spray Treated Subjects in 12 Double-Blind, Placebo-Controlled Clinical Trials:
| MedDRA System Organ Class-MedDRA PT | Levocabastine (n=2328) % | Placebo (n=1537) % |
|---|---|---|
| Gastrointestinal Disorders | ||
| Nausea | 1.3 | 1.2 |
| General Disorders and Administrative Site Conditions | ||
| Fatigue | 2.1 | 0.9 |
| Pain | 1.2 | 0.9 |
| Infections and Infestations | ||
| Sinusitis | 1.8 | 0.9 |
| Nervous System Disorders | ||
| Headache | 10.1 | 11.9 |
| Somnolence | 2.1 | 0.8 |
| Dizziness | 1.3 | 0.9 |
| Respiratory, Thoracic, and Mediastinal Disorders | ||
| Pharyngolaryngeal pain | 2.9 | 2.3 |
| Epistaxis | 1.6 | 1.0 |
| Cough | 1.7 | 1.3 |
Additional ADRs reported for <1% of levocabastine nasal spray treated subjects in the 12 clinical trials are presented in Table 2.
Table 2. Adverse Drug Reactions Reported by <1% levocabastine nasal spray Treated Subjects in 12 Double-Blind, Placebo-Controlled Clinical Trials:
MedDRA System Organ Class:
MedDRA PT
General Disorders and Administrative Site Conditions:
Application site irritation
Application site pain
Application site dryness
Application site burn
Application site discomfort
Respiratory, Thoracic, and Mediastinal Disorders:
Nasal discomfort
Nasal congestion
Additional adverse drug reactions first identified during postmarketing experience with levocabastine eye drops and nasal spray are included in the following lists. Because these reactions are reported voluntarily from a population of uncertain size, it is not always possible to reliably estimate their frequency or establish a causal relationship to drug exposure. Therefore, the frequencies are provided according to the following convention (3,4): Very Common: ≥1/10, Common: ≥1/100 and <1/10, Uncommon: ≥1/1000 and <1/100, Rare: ≥1/10000 and <1/1000, Very rare: ≥1/10000, including isolated reports.
In the lists below ADR’s are presented by frequency category based on incidence in clinical trials or epidemiology studies when known.
Adverse Drug Reactions Identified During Postmarketing Experience with levocabastine eye drops by Frequency Category Estimated from Spontaneous Reporting Rates:
Very Rare: Palpitations
Very Rare: Eye pain, Conjunctivitism Eyelid oedema, Eye swelling, Blepharitis, Ocular hyperaemia, Vision blurred
Very Rare: Application site reaction including eye burning sensation, eye redness, eye pain, eye swelling, eye itching, watery eyes and vision blurred.
Very Rare: Anaphylaxis, Angioneurotic oedema, Hypersensitivity
Very Rare: Contact dermatitis, Urticaria
Very Rare: Headache
Adverse Drug Reactions Identified During Postmarketing Experience with levocabastine nasal spray by Frequency Category Estimated from Spontaneous Reporting Rates:
Very Rare: Palpitations, Tachycardia
Very Rare: Eyelid Oedema
Very Rare: Malaise
Very Rare: Anaphylaxis, Hypersensitivity
Very Rare: Bronchospasm, Dyspnoea, Nasal oedema
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