LIVOSTIN
Clinical safety rating: caution
Comprehensive clinical and safety monograph for LIVOSTIN (LIVOSTIN).
Levocabastine is a selective histamine H1-receptor antagonist, inhibiting histamine release from mast cells and basophils.
| Metabolism | Not extensively metabolized; minimal hepatic metabolism via cytochrome P450 enzymes. |
| Excretion | Renal excretion as unchanged drug and metabolites: ~70% (48% unchanged, 9% as levocabastine glucuronide, 13% as other metabolites); fecal excretion: ~20% |
| Half-life | Terminal elimination half-life in adults: 35-40 hours; clinical context: supports once-daily dosing, with steady-state reached after approximately 7 days |
| Protein binding | Approximately 55% bound to plasma proteins, primarily albumin |
| Volume of Distribution | 80-100 L/kg; extensive tissue distribution, indicating high extravascular binding |
| Bioavailability | Ophthalmic: negligible systemic absorption (<1%); intranasal: approximately 60-80% systemic bioavailability after intranasal administration |
| Onset of Action | Ophthalmic: 15 minutes; intranasal: 30 minutes |
| Duration of Action | Ophthalmic: 12 hours; intranasal: up to 24 hours with once-daily dosing |
1 drop (0.05% ophthalmic solution) in affected eye twice daily, up to 4 times daily if needed.
| Dosage form | SUSPENSION/DROPS |
| Renal impairment | No dosage adjustment required for renal impairment. Data not established for GFR-based modifications. |
| Liver impairment | No specific adjustment recommended; use with caution in severe hepatic impairment due to potential for increased systemic exposure. |
| Pediatric use | Children ≥3 years: 1 drop (0.05% ophthalmic solution) in affected eye twice daily. Safety and efficacy in children <3 years not established. |
| Geriatric use | No specific adjustment required; use same dosing as adults. Monitor for local adverse effects due to potential age-related ocular surface changes. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for LIVOSTIN (LIVOSTIN).
| Breastfeeding | Unknown if distributed into human milk. M/P ratio not determined. Use with caution in nursing mothers; consider risk-benefit. |
| Teratogenic Risk | FDA Pregnancy Category B. No evidence of teratogenicity in animal studies. Insufficient human data; risk cannot be excluded. Avoid use in first trimester unless clearly needed. |
| Fetal Monitoring | No specific monitoring recommended; monitor for maternal sedation and fetal heart rate if used near term. |
■ FDA Black Box Warning
None.
| Serious Effects |
["Hypersensitivity to levocabastine or any component of the formulation"]
| Precautions | ["Do not use with contact lenses","Solution may cause transient burning or stinging","Use with caution in patients with known hypersensitivity to levocabastine"] |
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| Fertility Effects | No known adverse effects on fertility in animal studies. No human data. |