LASTACAFT
Clinical safety rating: caution
Comprehensive clinical and safety monograph for LASTACAFT (LASTACAFT).
Selective histamine H1 receptor antagonist; inhibits mast cell degranulation and reduces release of inflammatory mediators.
| Metabolism | Not extensively metabolized; primarily excreted unchanged in urine. |
| Excretion | Renal: approximately 70% as unchanged drug; fecal: approximately 30% as metabolites. |
| Half-life | Terminal elimination half-life is approximately 2 hours; clinically, dosing is twice daily. |
| Protein binding | Approximately 60% bound to plasma proteins, primarily albumin. |
| Volume of Distribution | Volume of distribution is not well defined for ocular administration; systemic Vd is estimated to be 1.4 L/kg, indicating extensive tissue distribution. |
| Bioavailability | Ocular: systemic bioavailability is low due to local administration and extensive metabolism; no oral bioavailability data as it is not administered orally. |
| Onset of Action | Ocular: relief of ocular itching occurs within 3 minutes after instillation. |
| Duration of Action | Duration of action is approximately 8-12 hours; recommended dosing every 8-12 hours as needed. |
| Molecular Weight | 322.36 |
1 drop in each affected eye twice daily (approximately every 8 hours)
| Dosage form | SOLUTION/DROPS |
| Renal impairment | No dosage adjustment required for any degree of renal impairment. |
| Liver impairment | No dosage adjustment required for any degree of hepatic impairment. |
| Pediatric use | Approved for children 2 years and older: 1 drop in each affected eye twice daily. Safety and efficacy in children under 2 years not established. |
| Geriatric use | No specific dosage adjustment recommended. Use same dose as younger adults. |
| 1st trimester | Data insufficient; no human studies; caution advised. |
| 2nd trimester | Data insufficient; no human studies; caution advised. |
| 3rd trimester | Data insufficient; no human studies; caution advised. |
Clinical note
Comprehensive clinical and safety monograph for LASTACAFT (LASTACAFT).
| Placental transfer | Unknown; likely crosses placenta due to molecular weight and lipophilicity. |
| Breastfeeding | No human data; likely present in breast milk; caution advised due to potential for infant exposure. |
| Lactation Rating | L3 (Limited Data) |
■ FDA Black Box Warning
None
| Serious Effects |
Hypersensitivity to alcaftadine or any component of the formulation
| Precautions | To minimize contamination, do not touch dropper tip to eyelids or surfaces., Contact lenses should be removed before instillation and may be reinserted after 10 minutes., Temporary blurred vision may occur. |
| Food/Dietary | No known food interactions. Avoid rubbing eyes after instillation to prevent systemic absorption through conjunctival vessels. |
| Clinical Pearls | LASTACAFT (alcaftadine 0.25% ophthalmic solution) is a topical mast cell stabilizer and H1-antihistamine for allergic conjunctivitis. Onset of action is within 3-5 minutes, with dosing twice daily. Do not use while wearing contact lenses; remove before instillation and wait 10 minutes before reinserting. Preservative-free unit-dose vials are preferred for patients with ocular surface sensitivity. |
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| Teratogenic Risk | LASTACAFT (alcaftadine ophthalmic solution) is classified as Pregnancy Category B. Animal studies in rats and rabbits at doses up to 82 and 820 times the maximum recommended human ophthalmic dose (based on systemic AUC) showed no teratogenic effects. There are no adequate and well-controlled studies in pregnant women. Because animal reproduction studies are not always predictive of human response, use during pregnancy only if clearly needed. No known fetal risks across trimesters based on limited human data. |
| Fetal Monitoring | No specific maternal or fetal monitoring is required for ophthalmic use. Systemic exposure is expected to be low after topical ocular administration. Monitor for any systemic adverse effects (e.g., headache, dysgeusia) as per routine clinical practice. |
| Fertility Effects | No fertility studies have been conducted with alcaftadine. Based on its low systemic absorption after ophthalmic dosing, effects on fertility are unlikely. |
| Patient Advice | Shake the bottle well before each use. · Remove contact lenses before using and wait at least 10 minutes after instillation before reinserting. · Do not touch the dropper tip to any surface to avoid contamination. · If you miss a dose, use it as soon as possible; do not double dose. · Some people may experience temporary blurred vision; wait until clear before driving. · Common side effects: eye irritation, headache, or altered taste (dysgeusia). |