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 |
| Molecular Weight | 420.5 |
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 | Limited human data; animal studies not available or insufficient. Avoid use unless clearly needed. |
| 2nd trimester | Limited human data; caution advised. Benefit should outweigh risk. |
| 3rd trimester | Use near term may cause adverse effects in newborn (e.g., drowsiness). Avoid use in late pregnancy. |
Clinical note
Comprehensive clinical and safety monograph for LIVOSTIN (LIVOSTIN).
| Placental transfer | Unknown; likely minimal due to low systemic bioavailability with topical administration. No specific studies available. |
| Breastfeeding | LIVOSTIN (levocabastine) is an antihistamine; minimal excretion into breast milk is expected due to low systemic absorption. However, it is recommended to use with caution and only if clearly needed, monitoring infant for drowsiness or irritability. |
■ FDA Black Box Warning
None.
| Serious Effects |
Hypersensitivity to levocabastine or any componentSevere renal impairment (creatinine clearance <10 mL/min)
| Precautions | Do not use with contact lenses, Solution may cause transient burning or stinging, Use with caution in patients with known hypersensitivity to levocabastine |
| Food/Dietary | No known food interactions. |
| Clinical Pearls | LIVOSTIN (levocabastine) is a topical ophthalmic antihistamine for allergic conjunctivitis; avoid use with contact lenses; may cause transient stinging; not for treatment of contact lens-related irritation. |
Loading safety data…
| Lactation Rating |
| L3 (Limited Data) or may be considered 'Moderately Safe' depending on source; actual rating may vary. Typically rated L3. |
| 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. |
| Fertility Effects | No known adverse effects on fertility in animal studies. No human data. |
| Patient Advice | Shake the bottle well before each use. · Remove contact lenses before instillation and wait at least 10 minutes before reinserting. · Do not touch the dropper tip to any surface to avoid contamination. · Use only in the eyes; do not ingest or inject. · If you experience eye pain, vision changes, or redness that worsens, discontinue use and consult your doctor. |