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8 of 216 medications
Chloroprocaine 3%
Iheezo®Local Anesthetic
GoodRxApproved uses
Ocular surface anesthesia for a planned procedure
3 drops applied topically to the ocular surface over the area of the planned procedure, reapplied as needed to maintain the effect
A gel rather than a drop, so it stays where it is put; onset and duration are longer than proparacaine
Contraindications
IHEEZO TM is contraindicated in patients with a history of hypersensitivity to any component of this preparation.
Available Forms3% chloroprocaine hydrochloride ophthalmic gel in a single-patient-use container.
Mechanism of ActionChloroprocaine, like other local anesthetics, blocks the generation and conduction of nerve impulses, presumably by raising the threshold for electrical excitation of the nerve.
Warnings & Precautions
- Not for injection or intraocular administration.
- Corneal injury due to insensitivity: the anesthetized eye is unprotected, so patients must not rub it.
- Corneal opacification has been reported with prolonged use.
- For administration by a healthcare provider only; it is not intended for patient self-administration.
Common Side Effects
The most common adverse reactions in these studies, (incidence greater than or equal to 5%) following IHEEZO TM administration were mydriasis, conjunctival hyperemia and eye irritation.
Pregnancy & LactationPregnancy: Not stated on the FDA label.
Lactation: Not stated on the FDA label.
Pediatric UseSafety and effectiveness in pediatric patients have not been established.
Cocaine 1% to 4%
CocaineLocal Anesthetic
GoodRxApproved uses
Local anaesthesia of the nasal mucous membranes for diagnostic procedures and surgery
Applied intranasally per the label for the specific procedure
Its eye-care role, testing for Horner syndrome, is off-label and absent from this label
OFF-LABELNot in the FDA label for this product
Horner syndrome, confirming an oculosympathetic palsy
One drop of 4% to 10% solution in each eye, read at 40 to 60 minutes; compounded, as no ophthalmic product is marketed
n=169 · 0.8 mm confirms
Cocaine blocks noradrenaline reuptake at the iris dilator, so a pupil with any oculosympathetic lesion dilates less than its fellow and the anisocoria widens. Tested in 119 patients with Horner syndrome against 50 normal subjects, the odds of Horner syndrome rose with the size of the post-cocaine anisocoria: at 0.8 mm the odds ratio was about 1050 to 1, with a lower 95% confidence limit of 37 to 1. The authors also found that simply measuring the anisocoria AFTER cocaine predicted better than calculating the change from baseline. It confirms the diagnosis and says nothing about where the lesion sits.
Contraindications
Hypersensitivity to cocaine hydrochloride or other ester-based local anesthetics.
Available FormsCocaine hydrochloride nasal solution 4%, a clear blue-green solution.
Mechanism of ActionBlocks reuptake of norepinephrine, causes vasoconstriction, and provides corneal anesthesia
Warnings & Precautions
- For intranasal use only; do not apply to damaged nasal mucosa.
- Cocaine is a Schedule II controlled substance with a risk of abuse and dependence.
- Cardiovascular events, including myocardial ischaemia, arrhythmia and hypertensive crisis, have been reported; avoid in uncontrolled hypertension or known cardiovascular disease.
- Seizures and other central nervous system effects can follow systemic absorption.
- Do not use with a monoamine oxidase inhibitor.
Common Side Effects
Hypertension, tachycardia, and sinus tachycardia.
Pregnancy & LactationPregnancy: Cocaine crosses the placenta and is associated with placental abruption, preterm birth and fetal growth restriction; avoid.
Lactation: Cocaine is present in human milk and can cause serious adverse reactions in the infant; advise against breastfeeding for at least 48 hours after a dose.
Pediatric UseNo studies
Fluorescein 0.25% / Benoxinate 0.4%
Altafluor®Diagnostic DyeLocal Anesthetic
GoodRxApproved uses
Ophthalmic procedures requiring a disclosing agent with topical anesthesia
1 to 2 drops in the eye as needed to achieve adequate anesthesia; extend by repeat instillation 10 to 20 minutes after the last dose
Maximal corneal anesthesia in 5 to 45 seconds, lasting about 20 minutes after a single instillation.
Contraindications
Known hypersensitivity to any component of this product.
Available FormsFluorescein sodium 0.25% (2.5 mg/mL) with benoxinate HCl 0.4% (4 mg/mL) ophthalmic solution, 5 mL glass bottle with sterilized dropper
Mechanism of ActionCombination of a disclosing dye with a rapidly acting ester anesthetic of short duration: fluorescein is excluded by an intact epithelial barrier and fluoresces green under cobalt blue excitation, while benoxinate blocks sodium channel conduction in corneal and conjunctival sensory nerve endings. Maximal corneal anesthesia occurs in about 5 to 45 seconds and lasts about 20 minutes after a single instillation.
Warnings & Precautions
- Corneal toxicity: Prolonged use or abuse may cause epithelial toxicity, manifesting as epithelial defects that can progress to permanent corneal opacification with visual loss.
- Corneal injury from insensitivity: The eye stays insensate for about 20 minutes after instillation; keep the patient from touching or rubbing it during that window, as accidental injury will not be felt.
- Anesthetic abuse keratopathy: Case reports of self-administered oxybuprocaine (benoxinate) describe persistent epithelial defects, stromal infiltration and thinning, descemetocele, endothelial ultrastructural damage, and penetrating keratoplasty, at concentrations as low as 0.05%.
- Solution contamination: Fluorescein supports bacterial growth; 21 of 21 in-use clinic bottles of plain fluorescein solution cultured positive, most often Pseudomonas spp., while unopened bottles were sterile. Chlorobutanol-preserved fluorescein with benoxinate self-sterilizes rapidly, clearing Pseudomonas within 15 seconds in vitro; of four commercial fluorescein-anesthetic preparations inoculated, that formulation was the one that regained sterility, while the other three still grew organisms 1 hour later.
- Soft contact lens staining: Dye is absorbed into the hydrogel matrix in proportion to exposure time and varies with lens power and water content, so soft lenses come out first; rinse with 0.9% saline rather than an oxidizing agent, since 3% hydrogen peroxide decolorizes retained dye without removing it.
- Storage: Refrigerate at 2 to 8 degrees C; after opening, up to 1 month at room temperature or until the labeled expiration date if kept refrigerated.
Common Side Effects
- Ocular, most common: Stinging, burning, and conjunctival redness.
- Ocular, postmarketing: Ocular hyperemia, eye irritation, blurred vision, and punctate keratitis; reported voluntarily from a population of uncertain size, so frequency cannot be estimated.
Pregnancy & LactationPregnancy: No data in pregnant women, and adequate animal reproduction studies have not been conducted for either component; give only if clearly needed.
Lactation: No data on presence in human milk, on the breastfed infant, or on milk production.
Pediatric UseEstablished in pediatric patients, supported by evidence from adequate and well controlled studies.
Fluorescein 0.25% / Proparacaine 0.5%
Fluoracaine®Diagnostic DyeLocal Anesthetic
GoodRxApproved uses
Ophthalmic procedures requiring a disclosing agent with topical anesthesia
1 to 2 drops in each eye as single instillations before foreign body or suture removal and before tonometry; for deep ophthalmic anesthesia, 1 drop in each eye every 5 to 10 minutes for 5 to 7 doses
Its proparacaine component numbs the cornea within 1 minute, with sensitivity back by 45 minutes.
Contraindications
Known hypersensitivity to any component of this product.
Available FormsFluorescein sodium 0.25% (2.5 mg/mL) with proparacaine HCl 0.5% (5 mg/mL) ophthalmic solution, 5 mL fill in a glass bottle with a controlled tip dropper
Mechanism of ActionCombination of a disclosing dye with a rapidly acting anesthetic of short duration. Fluorescein 0.25% is excluded by intact corneal epithelium and pools where the barrier is broken, fluorescing yellow-green under cobalt blue light, while proparacaine 0.5%, an ester anesthetic, blocks sodium channel conduction in corneal and conjunctival sensory nerve endings.
Warnings & Precautions
- Corneal opacification from prolonged use: Prolonged use of a topical ocular anesthetic is not recommended and may produce permanent corneal opacification with visual loss.
- Delayed wound healing: Long-term toxicity is unknown and prolonged use may delay wound healing; in cultured human corneal fibroblasts and in rabbits, 0.5% and 0.05% proparacaine twice daily for 3 days both impeded the corneal wound healing response in a time-dependent manner, adding polymyxin B and trimethoprim had additive effects on fibroblast viability, proliferation, and migration and on epithelial recovery, and 0.05% alone had minimal negative effect.
- Systemic toxicity: Exceedingly rare with ophthalmic application of local anesthetics, but central nervous system stimulation followed by depression can occur.
- Allergy, cardiac disease, hyperthyroidism: Use cautiously and sparingly in these patients.
- Corneal protection during anesthesia: Protect the eye from irritating chemicals, foreign bodies, and rubbing until sensation returns, and keep the patient from touching the eye.
- Tonometer rinsing: Tonometers soaked in sterilizing or detergent solutions must be rinsed thoroughly with sterile distilled water before use.
- Dropper contamination: Do not touch the sterile dropper tip to any surface, and replace the container closure immediately after use.
- Contamination of combination solutions: Of four commercial fluorescein-anesthetic solutions inoculated with Pseudomonas or Staphylococcus, only Fluress regained sterility (1 minute for the solution, 5 minutes for the dropper tip), while the other three, which were not individually named, still yielded organisms at least 1 hour after inoculation; separately, reuse of unpreserved single-application fluorescein 0.25% with proxymetacaine 0.5% Minims across consecutive patients grew lid and conjunctival flora from 7 of 41 vials (17%).
- Storage: Refrigerate at 2 to 8 degrees C, with up to 1 month at room temperature.
Common Side Effects
- Ocular, occasional: Temporary stinging, burning, and conjunctival redness, reported after use of ocular anesthetics.
- Ocular, rare: Severe immediate-type hyper-allergic corneal reaction with acute, intense, diffuse epithelial keratitis, a gray ground glass appearance, sloughing of large areas of necrotic epithelium, corneal filaments, and sometimes iritis with descemetitis.
- Dermatologic: Allergic contact dermatitis with drying and fissuring of the fingertips.
Pregnancy & LactationLimited data; potential risks to the fetus not well established
Pediatric UseAll ages
Lidocaine 3.5%
Akten®Local Anesthetic
GoodRxApproved uses
Ocular surface anesthesia for ophthalmologic procedures
2 drops to the ocular surface over the planned procedure site; may be reapplied to maintain effect
Anesthesia begins 20 seconds to 1 minute after instillation and lasts 5 to 30 minutes.
Anesthesia for intravitreal injection
2 drops to the ocular surface before injection, the labeled dose
No better than proparacaine drops for immediate pain at intravitreal injection.
Contraindications
None.
Available FormsLidocaine HCl 3.5% (35 mg/mL) preservative-free ophthalmic gel, 1 mL single-patient-use tube, cartons of 1 or 25 tubes
Mechanism of ActionAmide local anesthetic that stabilizes the neuronal membrane by blocking the voltage-gated sodium channels carrying the ionic flux required for initiation and conduction of impulses, abolishing corneal and conjunctival sensation.
Warnings & Precautions
- Topical ophthalmic use only: Not for injection or intraocular administration.
- Corneal injury from insensitivity: The eye must not be touched for at least 10 to 20 minutes after instillation, since accidental injury can occur while sensation is absent.
- Corneal opacification: Prolonged use of a topical ocular anesthetic may produce permanent corneal opacification and ulceration with accompanying visual loss.
- Provider administration: Indicated for administration under the direct supervision of a healthcare provider, not for patient self-administration.
- Anesthetic abuse keratopathy: Prolonged use of any topical ocular anesthetic produces a nonhealing epithelial defect with ring-shaped stromal infiltrate and hypopyon that has been mistaken for Acanthamoeba keratitis; in a 19-patient series of proparacaine and tetracaine abusers, mean time to epithelialization was 20 days and 63% kept using the drops while hospitalized for the resulting ulcer.
Common Side Effects
- Ocular: Conjunctival hyperemia, corneal epithelial changes, and burning on instillation are the most common reactions; the label reports no frequencies.
- Systemic: Headache. Topical ocular application is not expected to produce systemic exposure.
Pregnancy & LactationPregnancy: No adequate and well-controlled studies in pregnant women; subcutaneous dosing in pregnant rats at more than 800 times the human dose on a body surface area basis produced no adverse developmental effects.
Lactation: Secreted in human milk; clinical significance unknown.
Pediatric UseEstablished in pediatric patients, extrapolated from adult trials and from pediatric studies of other lidocaine formulations.
Proparacaine 0.5%
Alcaine®Local Anesthetic
GoodRxApproved uses
Corneal anesthesia of short duration (tonometry, gonioscopy, foreign body or suture removal)
1 to 2 drops in each eye as a single instillation before the procedure
Anesthesia is complete within 1 minute and sensitivity returns to baseline by 45 minutes.
Short corneal and conjunctival procedures
1 drop in each eye every 5 to 10 minutes for 5 to 7 doses
Anesthesia starts at 2 minutes, peaks at 15 minutes, and sensitivity is still reduced at 60 minutes.
OFF-LABELNot in the FDA label for this product
Outpatient analgesia for traumatic corneal abrasion
No endorsed regimen, and this entry is not a recommendation. The only randomized trial of take-home proparacaine used a 0.05% dilution; across the trials in the Cochrane review, treatment ran 3 hours to 1 week, most commonly 24 to 48 hours. Neither source states a dosing frequency.
Cochrane · very low certainty
Cochrane review of 9 RCTs and 556 participants: little or no difference from placebo in post-traumatic pain at 24 hours (MD -0.04 on a 10-point scale; 1 RCT, 76 participants) and a 37% higher rate of unresolved epithelial defects (RR 1.37, 95% CI 0.78 to 2.42; 3 RCTs, 221 participants). All outcomes very low certainty, over half the trials at high risk of bias, and the authors do not recommend the practice. The most favorable single trial used dilute 0.05% drops in 33 completers and found better pain reduction than placebo (median VAS improvement 3.9 vs 0.6 cm, P=0.007) with no observed healing delay, but was far too small to detect the complication it is dispensed against.
Contraindications
Known hypersensitivity to any ingredient of the preparation.
Available FormsProparacaine HCl 0.5% (5 mg/mL) ophthalmic solution, 15 mL dropper bottle
Mechanism of ActionEster-type local anesthetic that blocks voltage-gated sodium channels in the sensory nerve endings of the cornea and conjunctiva, preventing initiation and conduction of the impulse.
Warnings & Precautions
- Topical ophthalmic use only: Not for injection.
- Corneal opacification: Prolonged use is not recommended; it may produce permanent corneal opacification with accompanying visual loss.
- Anesthetic abuse keratopathy: Repeated self-administration produces a nonhealing epithelial defect with a ring-shaped stromal infiltrate that mimics Acanthamoeba keratitis and has led to conjunctival flap and penetrating keratoplasty; in a 19-patient series ring keratitis appeared in 58% of eyes, hypopyon in 42%, and mean time to epithelialization was 20 days.
- Outpatient dispensing: A Cochrane review of 9 RCTs and 556 participants found little or no reduction in post-traumatic pain at 24 hours and no evidence of a healing benefit, all outcomes very low certainty; the authors do not recommend the practice.
- Solution appearance: Should be clear to straw-color; discard if it becomes darker.
- Storage: Refrigerate at 2 to 8 degrees C and keep the bottle in its unit carton to protect from light.
Common Side Effects
- Ocular: Occasional temporary stinging, burning, and conjunctival redness.
- Ocular, rare: Severe immediate hyperallergic corneal reaction with acute diffuse epithelial keratitis, a gray ground glass appearance, sloughing of large areas of necrotic epithelium, corneal filaments, and sometimes iritis with descemetitis.
- Dermatologic: Allergic contact dermatitis with drying and fissuring of the fingertips.
Pregnancy & LactationPregnancy: Former Category C. No animal reproduction studies have been conducted, and it is unknown whether the drug can cause fetal harm or affect reproductive capacity; administer only if clearly needed.
Lactation: Excretion in human milk is unknown.
Pediatric UseEstablished in pediatric patients, supported by controlled studies in adults and children over age 12 plus safety data in neonates and other pediatric patients.
Tetracaine 0.5%
Tetcaine® · Opticaine®Local Anesthetic
GoodRxApproved uses
Topical anesthesia for ophthalmic procedures
1 drop topically in the eye(s) as needed
Corneal anesthesia is complete within 1 minute, with sensitivity back to baseline by 45 minutes.
OFF-LABELNot in the FDA label for this product
Corneal abrasion pain, short-term outpatient use
Preservative-free tetracaine 1%, up to every 30 minutes while awake for 24 hours (Waldman 2014); tetracaine every 30 minutes as needed for 24 hours (Shipman 2021)
Cochrane · very low certainty
Waldman 2014 (double-blind RCT, N=116) recorded no complications attributed to the anesthetic, no difference in persistent fluorescein uptake at 48 hours (23.9% vs 21.3%, difference 2.6%, 95% CI -14% to 20%) and no clinical difference in VAS pain, although patients rated it more effective than saline (7.7 vs 3.9 on a 0 to 10 scale). Shipman 2021 (double-blind RCT, 111 analyzed) found lower pain at the 24 to 48 hour visit (1 vs 8, 95% CI for the difference 6 to 8) and less hydrocodone use. The 2023 Cochrane review of topical ophthalmic anesthetics as a class (9 RCTs, 556 participants) graded the evidence very low certainty, concluded that it provides little or no certainty about efficacy for reducing ocular pain in the initial 24 to 72 hours and that the authors have very low confidence in it as a basis for recommending topical anesthetics for corneal abrasion pain, and found no evidence of a substantial effect on epithelial healing (unresolved defects after trauma RR 1.37, 95% CI 0.78 to 2.42, an estimate that crosses no effect) or on complications.
Contraindications
History of hypersensitivity to any component of this preparation.
Available Forms0.5% (5 mg/mL) solution, 5 mL dropper bottle, 15 mL dropper bottle
Mechanism of ActionEster local anesthetic that blocks sodium ion channels required for initiation and conduction of neuronal impulses, producing surface anesthesia. Cleared by plasma pseudocholinesterases and nonspecific esterases in ocular tissue.
Warnings & Precautions
- Intracameral use: Not for injection or intraocular use; intracameral exposure may damage corneal endothelial cells.
- Corneal toxicity: Prolonged use or abuse may cause epithelial defects that progress to permanent corneal damage, and prolonged use may produce corneal opacification and ulceration with visual loss.
- Corneal injury from insensitivity: Eye stays insensitive for up to 20 minutes; accidental injury can follow touching or rubbing within 10 to 20 minutes of instillation.
- Provider administration only: Indicated for use under direct supervision of a healthcare provider, not for patient self-administration.
Common Side Effects
Ocular: Transient stinging, burning, conjunctival redness, eye irritation, eye pain, ocular discomfort (postmarketing reports, frequency not estimable).
Pregnancy & LactationPregnancy: No adequate and well-controlled studies in pregnant women; no animal developmental or reproductive toxicity studies reported in the published literature.
Lactation: No data on presence in human milk, effects on the breastfed child, or effects on milk production.
Pediatric UseSafety demonstrated in pediatric clinical trials.