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Journal of Ocular Pharmacology and... Apr 2022Topical, local anesthetic eye drops in conjunction with antibiotics are commonly used to reduce ocular pain and treat patients in emergency clinics; however, their...
Topical, local anesthetic eye drops in conjunction with antibiotics are commonly used to reduce ocular pain and treat patients in emergency clinics; however, their effects on corneal healing are poorly understood. This study examined whether regular or diluted proparacaine eye drops given in combination with common ophthalmic antibiotics affect corneal wound healing parameters using and models. Primary human corneal fibroblasts generated from donor corneas and New Zealand white rabbits were used. Regular (0.5%) and diluted (0.05%) proparacaine eye drops, twice daily for 3 days, were applied to cultures and rabbit eyes, with or without ophthalmic antibiotics (polymyxin B sulfate and trimethoprim). Trypan blue, 3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyltetrazolium bromide (MTT), and scratch wound assays measured cellular viability, proliferation, and migration, respectively, Slit lamp biomicroscopy, tonometry, fluorescein eye test, hematoxylin and eosin (H&E) staining, and 4',6-diamidino-2-phenylindole (DAPI) immunofluorescence were used for studies. Both regular and diluted proparacaine affected wound healing response in the cornea and in a time-dependent manner. Adjunct antibiotic treatments had additive effects characterized by reduced corneal fibroblast viability, proliferation, and migration and corneal epithelial recovery . Regular proparacaine with antibiotics showed most pronounced effects on corneal wound healing parameters, and diluted proparacaine without antibiotics had minimal negative effects and . Both methods of regular (0.5%) and diluted (0.05%) proparacaine topical application to the cornea are safe, but impede corneal wound healing and . Adjunct antibiotic treatments had additive negative effects on corneal wound repair.
Topics: Anesthetics, Local; Animals; Anti-Bacterial Agents; Cornea; Corneal Injuries; Humans; Ophthalmic Solutions; Propoxycaine; Rabbits; Wound Healing
PubMed: 35275738
DOI: 10.1089/jop.2021.0116 -
Journal of Ocular Pharmacology and... Jun 2021To evaluate whether the standard dilating drop regimen consisting of phenylephrine, tropicamide, and proparacaine produces clinically significant improvement in pupil... (Comparative Study)
Comparative Study Randomized Controlled Trial
To evaluate whether the standard dilating drop regimen consisting of phenylephrine, tropicamide, and proparacaine produces clinically significant improvement in pupil size compared to tropicamide and proparacaine during diagnostic eye examination. Sixty-three adult patients at Washington University School of Medicine Eye Clinic were enrolled in this prospective, randomized trial. Each patient received one of two dilating drop regimens: phenylephrine + tropicamide + proparacaine (PE+T+PP), which is considered the standard therapy, or tropicamide + proparacaine (T+PP). Main outcome measures were the proportion of pupils able to achieve successful clinical examination without need for additional dilating drops and change in predilation to postdilation pupil size. Comparisons were made using McNemar's test, repeated measures analysis of variance, and Fisher's test to determine whether PE is a necessary component of the standard eye examination. There were no statistically significant differences between the PE+T+PP and T+PE treatment groups in predilation to postdilation changes in average resting pupil size (1.58 ± 0.66 and 2.61 ± 0.79; = 0.57) or constricted pupil size (2.52 ± 0.93 and 3.56 ± 0.96; = 0.15). There was no statistically significant difference between patients who obtained a successful dilated pupil examination between those receiving PE+T+PP and those receiving T+PP as determined by the examining physicians (Fisher's, = 0.67). The addition of phenylephrine to tropicamide and proparacaine did not improve pupillary dilation size or ability to conduct a clinical examination. A single dilating agent using tropicamide should be considered in clinical practice.
Topics: Adult; Aged; Anesthetics, Local; Diagnostic Techniques, Ophthalmological; Drug Interactions; Drug Therapy, Combination; Female; Humans; Male; Middle Aged; Mydriatics; Ophthalmic Solutions; Outcome Assessment, Health Care; Phenylephrine; Propoxycaine; Prospective Studies; Pupil; Tropicamide
PubMed: 33685234
DOI: 10.1089/jop.2020.0111 -
The Journal of Toxicological Sciences Aug 2015Proparacaine is a widely used topical anesthetic in ophthalmic optometry and surgery, and has been reported to have cytotoxic effects on rabbit corneal endothelial cells...
Proparacaine is a widely used topical anesthetic in ophthalmic optometry and surgery, and has been reported to have cytotoxic effects on rabbit corneal endothelial cells after prolonged and repeated usage. Since rabbit is an exceptive mammal whose corneal endothelial cells still maintaining proliferation abilities even in adulthood, whether proparacaine has cytotoxic effects on human corneal endothelial (HCE) cells need to be further verified. Our objectives in the present study were to investigate the cytotoxicity to HCE cells of proparacaine and its underlying mechanisms in vitro and verify the cytotoxicity using cat corneal endothelial (CCE) cells in an in vivo model of cat corneas. Cytotoxic evaluation results indicated that a dose- and time-dependent toxic response of HCE cells to proparacaine over 0.03125% was rated based on morphology and viability, and a toxic response of CCE cells to 0.5% (clinical applied dosage) proparacaine was also rated based on cell density and histology. Importantly, treatment with proparacaine resulted in significant elevation of plasma membrane permeability, cell cycle arrest at S phase, fragmentation of genomic DNA, formation of apoptotic bodies, and externalization of phosphatidylserine (PS) of HCE cells. Moreover, proparacaine demonstrated disrupting effects on mitochondrial transmembrane potential (MTP) of HCE cells and activating effects on caspase-3, -8 and -9. This study demonstrates that proparacaine has notable cytotoxicity to both HCE cells in vitro and CCE cells in vivo, and its dose- and time-dependent cytotoxicity to HCE cells is achieved by inducing apoptosis via a mitochondrion-mediated caspase-dependent pathway. These findings provide new insights into the cytotoxicity and apoptosis-inducing effect of local anesthetics which should be used with great caution in the eye clinic.
Topics: Anesthetics, Local; Animals; Apoptosis; Caspases; Cats; Cell Cycle; Cell Membrane Permeability; Cells, Cultured; DNA Fragmentation; Dose-Response Relationship, Drug; Endothelial Cells; Endothelium, Corneal; Humans; Membrane Potential, Mitochondrial; Phosphatidylserines; Propoxycaine; Rabbits; S Phase; Time Factors
PubMed: 26165639
DOI: 10.2131/jts.40.427 -
Investigative Ophthalmology & Visual... May 2015Dry eye disease (DED) produces ocular pain and irritation, yet a detailed characterization of ocular sensitivity in a preclinical model of DED is lacking. The aim of the...
PURPOSE
Dry eye disease (DED) produces ocular pain and irritation, yet a detailed characterization of ocular sensitivity in a preclinical model of DED is lacking. The aim of the present study was to assess nociceptive behaviors in an aqueous tear deficiency model of DED in the rat.
METHODS
Spontaneous blinking, corneal mechanical thresholds, and eye wipe behaviors elicited by hypertonic saline (5.0 M) were examined over a period of 8 weeks following the unilateral excision of either the exorbital lacrimal gland or of the exorbital and infraorbital lacrimal glands, and in sham surgery controls. The effect of topical proparacaine on spontaneous blinking and of systemic morphine (0.5-3.0 mg/kg, subcutaneous [SC]) on spontaneous blinking and eye wipe responses were also examined.
RESULTS
Lacrimal gland excision resulted in mechanical hypersensitivity and an increase in spontaneous blinking in the ipsilateral eye over an 8-week period that was more pronounced after infra- and exorbital gland excision. The time spent eye wiping was also enhanced in response to hypertonic saline (5.0 M) at both 1- and 8-week time-points, but only in infra- and exorbital gland excised animals. Morphine attenuated spontaneous blinking, and the response to hypertonic saline in dry eye animals and topical proparacaine application reduced spontaneous blinking down to control levels.
CONCLUSIONS
These results indicate that aqueous tear deficiency produces hypersensitivity in the rat cornea. In addition, the increase in spontaneous blinks and their reduction by morphine and topical anesthesia indicate the presence of persistent irritation elicited by the activation of corneal nociceptors.
Topics: Analgesics, Opioid; Analysis of Variance; Anesthetics, Local; Animals; Blinking; Cornea; Disease Models, Animal; Dry Eye Syndromes; Fluorescein Angiography; Lacrimal Apparatus; Male; Morphine; Propoxycaine; Rats; Rats, Sprague-Dawley; Sensory Thresholds; Tears
PubMed: 26024120
DOI: 10.1167/iovs.15-16717 -
Psychiatria Danubina Sep 2019
Review
Topics: Behavior, Addictive; Diagnostic Errors; Eye Pain; Humans; Male; Middle Aged; Ophthalmic Solutions; Patient Satisfaction; Prescription Drug Misuse; Propoxycaine; Self Medication
PubMed: 31596831
DOI: 10.24869/psyd.2019.360 -
New application of an old drug proparacaine in treating epilepsy via liposomal hydrogel formulation.Pharmacological Research Jul 2021Proparacaine (PPC) is a previously discovered topical anesthetic for ophthalmic optometry and surgery by blocking the central Nav1.3. In this study, we found that...
Proparacaine (PPC) is a previously discovered topical anesthetic for ophthalmic optometry and surgery by blocking the central Nav1.3. In this study, we found that proparacaine hydrochloride (PPC-HCl) exerted an acute robust antiepileptic effect in pilocarpine-induced epilepsy mice. More importantly, chronic treatment with PPC-HCl totally terminated spontaneous recurrent seizure occurrence without significant toxicity. Chronic treatment with PPC-HCl did not cause obvious cytotoxicity, neuropsychiatric adverse effects, hepatotoxicity, cardiotoxicity, and even genotoxicity that evaluated by whole genome-scale transcriptomic analyses. Only when in a high dose (50 mg/kg), the QRS interval measured by electrocardiography was slightly prolonged, which was similar to the impact of levetiracetam. Nevertheless, to overcome this potential issue, we adopt a liposome encapsulation strategy that could alleviate cardiotoxicity and prepared a type of hydrogel containing PPC-HCl for sustained release. Implantation of thermosensitive chitosan-based hydrogel containing liposomal PPC-HCl into the subcutaneous tissue exerted immediate and long-lasting remission from spontaneous recurrent seizure in epileptic mice without affecting QRS interval. Therefore, this new liposomal hydrogel formulation of proparacaine could be developed as a transdermal patch for treating epilepsy, avoiding the severe toxicity after chronic treatment with current antiepileptic drugs in clinic.
Topics: Animals; Anticonvulsants; Drug Delivery Systems; Electroencephalography; Epilepsy; Hindlimb Suspension; Hydrogels; Liposomes; Male; Maze Learning; Mice, Inbred C57BL; Open Field Test; Propoxycaine; Mice
PubMed: 33932606
DOI: 10.1016/j.phrs.2021.105636 -
Journal of the American Veterinary... Nov 2018OBJECTIVE To evaluate the effects of topical ophthalmic application of 0.5% proparacaine hydrochloride solution (PHCL; containing 0.01% benzalkonium chloride as...
OBJECTIVE To evaluate the effects of topical ophthalmic application of 0.5% proparacaine hydrochloride solution (PHCL; containing 0.01% benzalkonium chloride as preservative) on aerobic bacterial culture results for naturally occurring infected corneal ulcers in dogs. DESIGN Clinical trial. ANIMALS 25 client-owned dogs with infected corneal ulcers (24 unilaterally affected and 1 bilaterally affected; only 1 eye included/dog) examined between June 2008 and May 2011. PROCEDURES Swab samples for aerobic bacterial culture were collected from the periphery of each corneal ulcer before and approximately 1 minute after topical ophthalmic application of 1 drop of PHCL. Numbers of aerobic bacterial species isolated from affected eyes were compared between sample collection points and between other variables (ie, side [left or right] of affected eye, prior treatments, and patient age, sex, and neuter status). RESULTS There was no significant difference between numbers of aerobic bacterial species isolated per eye or overall aerobic bacterial culture results (positive or negative) before versus after PHCL application. Similarly, prior treatment had no significant effect on aerobic bacterial culture results for samples collected at either point. The most commonly isolated bacteria before and after PHCL application were Staphylococcus spp (40% and 48%, respectively), followed by Streptococcus spp (23% and 22%, respectively). CONCLUSIONS AND CLINICAL RELEVANCE Topical ophthalmic application of PHCL did not significantly affect aerobic bacterial culture results for naturally occurring infected corneal ulcers in dogs as assessed in this study. Therefore, topical ophthalmic PHCL application could be useful in clinical settings prior to sample collection to relieve patient discomfort and to aid in sample acquisition without compromising aerobic bacterial culture results.
Topics: Administration, Topical; Anesthetics, Local; Animals; Bacterial Infections; Corneal Ulcer; Dog Diseases; Dogs; Female; Male; Ophthalmic Solutions; Propoxycaine
PubMed: 30311533
DOI: 10.2460/javma.253.9.1140 -
Analytical Sciences : the International... 2018Proparacaine, one of the most common local anesthetics to facilitate diagnosis and treatment of eye diseases, was assayed by square wave voltammetry using a paste...
Proparacaine, one of the most common local anesthetics to facilitate diagnosis and treatment of eye diseases, was assayed by square wave voltammetry using a paste electrode prepared with carbon nanotubes. In cyclic voltammetric studies, proparacaine has exhibited a single irreversible anodic peak at around + 900 mV vs. Ag/AgCl in pH 6.0 Britton-Robinson buffer solution. It was suggested that the peak had appeared due to the oxidation of the NH group on the proparacaine molecule. Prior to the determination of the proparacaine by square wave stripping voltammetry (SWSV) on the fabricated multi-walled carbon nanotube paste electrode (MWCNTPE), the accumulation potential (E), accumulation time (t), pulse amplitude (ΔE), step potential (ΔE) and frequency (f ) parameters were optimized. The peak currents plotted in the range of 0.5 - 12.5 mg/L proparacaine exhibited two linear sections with a detection limit of 0.11 mg/L. The results for the determination of proparacaine on a pharmaceutical local anesthetic (Alcaine) showed that relative standard deviation (RSD) and relative error (RE) were 4.1 and -2.0%, respectively. Selectivity has also been investigated and results showed recoveries of 5.0 mg/L proparacaine in the presence of 5.0 mg/L dopamine, ascorbic acid and uric acid as 106.9 ± 0.8, 99.9 ± 1.2 and 94.1 ± 0.7, respectively.
Topics: Administration, Ophthalmic; Electrochemical Techniques; Electrodes; Nanotubes, Carbon; Propoxycaine
PubMed: 29998957
DOI: 10.2116/analsci.17P589 -
Middle East African Journal of... 2014To compare the efficacy and safety of 0.5% intracameral lignocaine to 1% intracameral lignocaine prior to phacotrabeculectomy. (Comparative Study)
Comparative Study Observational Study
AIM
To compare the efficacy and safety of 0.5% intracameral lignocaine to 1% intracameral lignocaine prior to phacotrabeculectomy.
STUDY DESIGN
Prospective, comparative, observational, and interventional study.
SETTING
Tertiary eye care center in central India.
MATERIALS AND METHODS
This study was comprised of 79 patients (79 eyes) with primary open angle glaucoma scheduled for phacotrabeculectomy. Patients were assigned to 1 of 2 Groups receiving proparacaine 0.5% eye drops and 1% intracameral lignocaine just prior to phacotrabeculectomy (Group 1, n = 39) and 0.5% intracameral lignocaine after completion of phacoemulsification just prior to trabeculectomy (Group 2, n = 40). The visual analogue scale was used to record intraoperative and postoperative pain. Patient comfort, intraoperative painful sensations perceived by the patient, supplemental anesthesia, complications, and surgeon discomfort were noted. An anesthetist also noted the vital parameters and the requirement for intravenous medications.
RESULTS
There was no significant difference in the intraoperative pain score (P = 0.0733) or supplemental anesthesia (P = 0.372) between Groups. Postoperative pain score was statistically significant in Group 2 (P < 0.0001). The overall operating conditions in both Groups were comparable (P = 0.7389). A greater number of patients in Group 2 (88.57%) preferred the same anesthetic technique for combined surgery in the fellow eye. There was no difference in inadvertent eye movements and lid squeezing between Groups and they did not interfere with surgery.
CONCLUSION
Topical anesthetic drops supplemented with 0.5% intracameral lignocaine before performing trabeculectomy is as effective as 1% intracameral lignocaine given at the beginning of phacotrabeculectomy for primary open angle glaucoma.
Topics: Adult; Anesthesia, Local; Anesthetics, Local; Anterior Chamber; Eye Pain; Female; Glaucoma, Open-Angle; Humans; Injections, Intraocular; Lidocaine; Male; Middle Aged; Pain Measurement; Pain, Postoperative; Phacoemulsification; Propoxycaine; Prospective Studies; Trabeculectomy
PubMed: 25100903
DOI: 10.4103/0974-9233.134669 -
Arquivos Brasileiros de Oftalmologia 2015To compare the anesthetic effectiveness of topical proparacaine drops, subconjunctival lidocaine, and 2% lidocaine gel. (Randomized Controlled Trial)
Randomized Controlled Trial
PURPOSE
To compare the anesthetic effectiveness of topical proparacaine drops, subconjunctival lidocaine, and 2% lidocaine gel.
METHODS
Ninety-two patients undergoing intravitreal injections were randomized to 1 of 3 groups: proparacaine 0.5% drops (Group Drops), proparacaine 0.5% drops plus subconjunctival lidocaine (Group SC), or 2% lidocaine gel (Group Gel). Patients were asked to score their pain experience using a visual analog scale of 0 to 10 immediately following the injections and 10 min, 1 h, 6 h, and 24 h after the injections. Patients also graded the overall injection experience as Excellent, Very Good, Fair, Poor, or Awful. The physician evaluated the patients' eye movement during intravitreal injection on 3 levels: (0) none or minimal, (1) not compromising the injection, and (2) compromising the injection.
RESULTS
The patients in Group Drops had the worst mean pain scores during the injection and 10 min after, with the highest occurrence of movements compromising the procedure (Grade 2; 38.7%). The patients in Group SC had a higher percentage of good experiences (37.9%) but a higher incidence of chemosis (16.7%). The patients in Group Gel had similar overall pain scores to Group Drops patients but a higher incidence of keratitis (19.4%). There was no statistically significant correlation between the use of aspirin or anticoagulants and the occurrence of hyperemia or hyposphagma.
CONCLUSION
Subconjunctival lidocaine was most effective in preventing pain and eye movements during intravitreal injections. Although 2% lidocaine gel produced a good overall experience for the patients, the incidence of keratitis was very high (19.4%). Therefore, we do not recommend 2% lidocaine gel as the first anesthetic choice for intravitreal injections. There is no evidence to suspend the use of aspirin or other anticoagulants drugs prior to intravitreal injections.
Topics: Adult; Aged; Aged, 80 and over; Anesthesia, Local; Anesthetics, Local; Eye Movements; Female; Humans; Intravitreal Injections; Keratitis; Lidocaine; Macular Degeneration; Macular Edema; Male; Middle Aged; Pain Measurement; Patient Satisfaction; Propoxycaine; Prospective Studies
PubMed: 25714534
DOI: 10.5935/0004-2749.20150008