ALCAINE
Clinical safety rating: caution
Comprehensive clinical and safety monograph for ALCAINE (ALCAINE).
Local anesthetic that stabilizes the neuronal membrane by inhibiting sodium ion influx, thereby blocking nerve impulse transmission.
| Metabolism | Hydrolyzed by plasma esterases. |
| Excretion | Renal excretion of parent drug and metabolites: <5% unchanged. |
| Half-life | Terminal elimination half-life: 0.4–1.2 minutes (rapid enzymatic hydrolysis by plasma esterases); clinical significance: ultra-short duration limits systemic toxicity. |
| Protein binding | Minimal; <5% bound to plasma proteins. |
| Volume of Distribution | Not clinically meaningful due to rapid hydrolysis; Vd estimated <0.5 L/kg (low, consistent with high water solubility and rapid clearance). |
| Bioavailability | Ophthalmic topical: negligible systemic absorption (minimal bioavailability); not applicable systemically. |
| Onset of Action | Topical ophthalmic: within 15–30 seconds. |
| Duration of Action | Topical ophthalmic: 15–20 minutes (corneal anesthesia); prolonged use delays epithelial healing. |
| Molecular Weight | 317.3 Da |
1 to 2 drops of 0.5% solution topically to the eye, repeated as needed for anesthesia.
| Dosage form | SOLUTION/DROPS |
| Renal impairment | No dose adjustment required; negligible systemic absorption. |
| Liver impairment | No dose adjustment required; negligible systemic absorption. |
| Pediatric use | 1 drop of 0.5% solution topically to the eye, repeated as needed; maximum 1 drop per dose in infants and young children to avoid systemic effects. |
| Geriatric use | No specific adjustment; use lowest effective dose due to potential increased corneal sensitivity and delayed healing. |
| 1st trimester | No adequate studies in pregnant women. Use only if potential benefit justifies risk to fetus. |
| 2nd trimester | No adequate studies in pregnant women. Use only if potential benefit justifies risk to fetus. |
| 3rd trimester | Avoid use near term due to potential for neonatal apnea and bradycardia. |
Clinical note
Comprehensive clinical and safety monograph for ALCAINE (ALCAINE).
| Placental transfer | Likely crosses placenta due to low molecular weight. |
| Breastfeeding | Not recommended during breastfeeding as it may be excreted in human milk and cause adverse effects in the infant. |
| Lactation Rating |
■ FDA Black Box Warning
Not for injection or prolonged use; corneal toxicity with repeated or prolonged use.
| Serious Effects |
Known hypersensitivity to proparacaine or any componentOcular infection or trauma (relative, but often considered absolute due to increased risk of toxicity)
| Precautions | Prolonged use may cause corneal epithelial damage and delay wound healing. Avoid contamination of the dropper tip. |
| Food/Dietary | None known. |
| Clinical Pearls | ALCAINE (proparacaine) is a topical ophthalmic anesthetic. Onset within 20 seconds, duration ~15 minutes. Do not dispense for home use due to risk of corneal toxicity with prolonged use. Use a sterile, single-dose vial to prevent contamination. Monitor for stinging or burning on instillation. Avoid in patients with sulfite allergy (contains sodium bisulfite). |
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| L4 |
| Teratogenic Risk | Proparacaine (ALCAINE) is an ophthalmic local anesthetic. Systemic absorption is negligible after topical ocular administration. No adequate well-controlled studies in pregnant women. Animal studies showed no teratogenic effects at doses up to 0.5 mg/kg (SC). Potential fetal risk unlikely to exceed background risk. No known trimester-specific risks. |
| Fetal Monitoring | No specific monitoring required beyond standard ophthalmic use. Inadvertent systemic overdose may cause CNS depression; monitor for respiratory or cardiovascular effects. |
| Fertility Effects | No known effects on fertility based on available animal and human data. Given topical ophthalmic use with minimal systemic absorption, fertility impact is unlikely. |
| Patient Advice | Temporary stinging or burning may occur upon application. · Do not touch the dropper tip to any surface to avoid contamination. · Do not use for more than instructed; prolonged use can damage the cornea. · Remove contact lenses before use and wait at least 15 minutes before reinserting. · Notify your doctor if you have a sulfite allergy. |