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At least 19 recordsLinked to original sources

Soft drugs 15: mydriatic activity and transcorneal penetration of phenylsuccinic soft analogs of methscopolamine as short acting mydriatics.

Soft drug analogs of methscopolamine (4 a-c) were tested for mydriatic activity in rabbits' eyes. After unilateral administration of equieffective doses, the AUC24hrs and the mydriatic recovery times were found to be significantly lower with the soft drugs compared to methscopolamine. At equieffective doses, the AUC24hrs for soft drugs ranged from 22.4% to 60% of that of methscopolamine. Significant dilation of the untreated eye was observed with methscopolamine but not with the soft drugs after unilateral administration. Soft drug 4a exhibited only 10.4% of the AUC6hrs (untreated eye) of that of methscopolamine. Shorter durations of mydriatic action combined with potentially reduced systemic side effects make these compounds candidates for further study. In vitro rabbit transcorneal penetration of soft analog 4a was found to be significantly higher than methscopolamine.

Animals↗

Systemic response to mydriatic eyedrops in neonates: mydriatics in neonates.

During routine dilation of 48 newborns, systemic responses and pupil dilation were monitored. Both 10 percent aqueous and viscous phenylephrine caused blanching around the eyes and produced considerable rise in blood pressure. Dilatation average 4.7 mm. In a double blind study, a 2.5 percent solution caused no skin blanching and no change in pressure or heart rate. Average dilation was 4.5 mm. No blood pressure changes were observed with either one percent cyclopentolate or one percent tropicamide. Average dilatations were 5.0 mm and 5.3 mm respectively. The above agents, used individually for a total dosage of three drops in each eye did not provide adequate dilation for a thorough funduscopic examination. Our protocol at United Hospitals Medical Center is a safe combination of drugs and provides excellent dilatation averaging greater th an 7 mm. No skin blanching or change in heart rate was observed.

Birth Weight↗

Mydriatic efficacy of a cycloplegic spray in the pediatric population.

BACKGROUND: The topical administration of eyedrops is often an unpleasant procedure in the pediatric population. We sought to learn whether a combination mydriatic-cycloplegic solution would be an effective mydriatic if applied as a spray. METHODS: We used a prospective, examiner-masked, parallel-group study design and randomized 38 subjects (age range 6 months-12 years, mean = 7.3 years) into four groups such that the same combination mydriatic-cycloplegic solution was administered under the following conditions: 1) eyedrops to eyes that were closed; 2) eyedrops to eyes that were open; 3) spray to eyes that were closed; 4) spray to eyes that were open. Both eyes of each subject received the solutions administered under one of the four conditions. Photographs were taken of each subject's pupils at times 0, 5, 15, 25, 40, and 55 mins following administration of the medications. RESULTS: Repeated measures analysis of variance revealed no statistically significant difference (p > 0.05) in mydriatic efficacy among the four methods of drug administration. CONCLUSIONS: The results of this study suggest that the mydriatic efficacy of a mydriatic-cycloplegic spray is comparable to that associated with eyedrop instillation. Mydriatic sprays may have important clinical advantages over conventional ophthalmic solutions in the pediatric population.

Aerosols↗

A pupillographic evaluation of a phenylephrine HCl 5%-tropicamide 0.8% combination mydriatic.

A continuously recording high-resolution pupillometer was used to measure changes in pupil size and pupil reactivity to temporally modulated light, following topical application of a phenylephrine HCl 5%-tropicamide 0.8% combination mydriatic (Phenyltrope). A controlled light stimulus induced pupillary changes in the left eye while changes in the consensual pupillary responses were measured in the mydriatic-treated right eye. The effects on pupil light reactivity of a single drop of the combination mydriatic were also compared to those caused by one drop of tropicamide 1% alone. Phenyltrope was introduced onto the ophthalmic market ostensibly offering faster mydriasis because of its combined effect of both the parasympathetic and sympathetic innervation to the pupil. In the present study, we looked for any differences in the pupil reaction times and amplitudes as a function of time after drug administration, iris coloration and type of mydriatic instilled. Our results show that while the combination is a fast acting mydriatic providing a large and stable pupillary dilation in subjects with either blue or brown irides, it does not differ appreciably in efficacy from the mydriatic effect of tropicamide 1% alone in healthy subjects between 20 to 36 years of age. Applications of our findings to the clinical environment are presented.

Administration, Topical↗

[Effects of pre-instilled mydriatics on the intraocular concentration and anti-inflammatory action of topical 0.1% pranoprofen (2)--Study on multiple dosing].

We studied the effects of multiple dosing and pre-instilled mydriatics (0.5% tropicamide and 0.5% phenylephrine) on the intraocular concentration and anti-inflammatory action of topical 0.1% pranoprofen (PPF) in rabbit eyes. PPF was applied in a single or multiple doses: 1 to 4 times consecutively at 5-minute intervals with or without pre-instilled mydriatics. PPF concentrations in the aqueous humor increased dose-dependently. The PPF concentrations also increased dose-dependently, and reached the maximal concentration by instillation 3 times in the presence of pre-instilled mydriatics, and the concentrations were 3.4 to 5.8 times higher than those without mydriatics. The PPF concentrations in the cornea, secondary aqueous, and iris-ciliary body increased in a dose-dependent manner, and the concentrations were higher in the presence of mydriatics. PPF reduced the protein rise in the secondary aqueous and miotic responses which were seen after paracentesis. The percent inhibitions ranged from 75 to 83, but the inhibitory actions were not enhanced by increases of intraocular PPF concentrations. These data indicate that the potent anti-inflammatory actions of PPF were obtainable by a single instillation, but it might be useful to instill the drug 3 times consecutively to ensure higher intraocular drug concentrations in combination with pre-instilled mydriatics.

Administration, Topical↗

Mydriatics slow gastric emptying in preterm infants.

OBJECTIVE: Preterm infants are more likely to have episodes of abdominal distention, emesis, and gastric residuals 24 hours after their first screening examination for retinopathy of prematurity (ROP) than on the day preceding the examination. Because these feeding problems reflect abnormalities in motor function, the purpose of this study was to compare antral and duodenal motor activity and gastric emptying in preterm infants before and after the instillation of mydriatics. STUDY DESIGN: Using a low compliance continuous perfusion manometric system, we recorded antral and duodenal fasting motor activity in 11 preterm infants before and after the instillation of mydriatics for their first screening examination for ROP. Gastric emptying was compared before and after the eye examination. RESULTS: Although the number of antral motor contractions remained relatively constant throughout the study, duodenal motor contractions decreased nearly fourfold after the instillation of mydriatics versus that seen before (P <.01). Gastric emptying was significantly delayed after the completion of the eye examination compared with that seen before the examination (P <.05). CONCLUSION: Current doses of mydriatics inhibit duodenal motor activity and delay gastric emptying, and these gastrointestinal effects of mydriatics may underlie the feeding difficulties seen in preterm infants on the day of screening examinations for ROP.

Duodenum↗

Efficacy of a mydriatic spray in the pediatric population.

BACKGROUND: Children often resist instillation of mydriatic drops for dilated fundus evaluation. As cycloplegic sprays have proven useful, this study's aim was to demonstrate efficacy of a mydriatic spray. METHODS: Twenty-two healthy subjects, ages 2 to 8 years, participated in the study. All but two had dark brown irides. Subjects were given either one drop each of 1% tropicamide and 2.5% phenylephrine in each eye or one application of mydriatic spray (containing concentrations of 0.5% tropicamide and 2.5% phenylephrine) to each closed eyelid. Pupils were measured with a pupil gauge before drug delivery and every 10 min thereafter, for 40 min. RESULTS: Repeated measures analysis of variance for the five time intervals demonstrated no significant difference between the two application methods nor in the method/time interaction, but a statistically significant increase in pupil size over time (p < 0.0005) for each method. A t-test revealed no statistically significant difference in pupil size (p > 0.05) between the two methods of drug administration at 40 min after application. CONCLUSIONS: This study suggests that use of mydriatic sprays on closed eyelids is as efficacious as use of mydriatic drops in open eyes for children.

Administration, Topical↗

Pupillary dilatation with single eyedrop mydriatic combinations.

We studied the mydiatic effect of three solutions containing a combination of two mydriatic drugs in 80 adult patients. The solutions tested were cyclopentolate HCl 0.5% with phenylephrine 2.5%, tropicamide 0.5% with phenylephrine 2.5%, and tropicamide 1.0% with phenylephrine 2.5%. We evaluated the effect of prior instillation of proparacaine 0.5% eyedrops. All three mydriatic combination solutions evaluated produced pupillary dilatation of about 7 mm within 60 minutes. Additional pupillary dilatation of 1 mm occurred when proparacaine was instilled before the mydriatic combination eyedrop. Mydriasis was resistant to bright light during indirect ophthalmoscopy in all patients. Pupils of younger patients dilated better than those of older patients, but sex and iris color were factors in the amount of pupillary dilatation obtained. Wide and sustained pupillary dilatation can be obtained for satisfactory indirect ophthalmoscopy by the instillation of one drop of proparacaine solution followed by a single drop of any of the three mydriatic combination solutions evaluated. By eliminating the need for multiple instillations of drugs, the use of a single eyedrop mydriatic combination is convenient in terms of time saved and also lessens the change of systemic drug toxicity.

Adolescent↗

Novel site-specific chemical delivery system as a potential mydriatic agent: formation of phenylephrine in the iris-ciliary body from phenylephrone chemical delivery systems.

The objective of this study was to test the three novel ester derivatives of phenylephrone (isovaleryl, phenylacetyl, and pivalyl esters) as potential site-specific chemical delivery systems. The mydriatic effect and ocular distribution/metabolism of these compounds were studied by topical application to the eyes of normal rabbits. It was assumed that a reduction-hydrolysis sequence could produce the active phenylephrine in the iris-ciliary body tissues. All the derivatives showed a more pronounced mydriatic effect than that of phenylephrine, whereas phenylephrone was completely devoid of any mydriatic activity. Phenylacetyl ester was the most potent drug, with short duration of action, and showed maximum activity in the presence of 0.01% benzalkonium chloride without causing any visible irritation to the rabbit eye. Administration of the novel compounds to the eyes of the rabbits showed no traces of phenylephrine in the systemic circulation, contrary to topical administration of phenylephrine. Phenylephrone was detected in different compartments of the eye, whereas phenylephrine was present only in the iris-ciliary body tissues following administration of phenylacetyl ester. The conversion of phenylephrone esters to the active drug, phenylephrine, and thus their subsequent activity was dependent on the physicochemical characteristics of the drugs. The results suggest the potential use of phenylacetyl ester as a potent short-term mydriatic agent without systemic side effects.

Animals↗

The sensitivity and specificity of single-field nonmydriatic monochromatic digital fundus photography with remote image interpretation for diabetic retinopathy screening: a comparison with ophthalmoscopy and standardized mydriatic color photography.

PURPOSE: To evaluate single-field digital monochromatic nonmydriatic fundus photography as an adjunct in the screening of diabetic retinopathy. DESIGN: Prospective, comparative, observational case series. METHODS: Patients with type I and type II diabetes mellitus (n = 197) were sequentially evaluated by three different techniques: single-field digital monochromatic nonmydriatic photography; dilated ophthalmoscopy by an ophthalmologist; and seven Early Treatment Diabetic Retinopathy Study (ETDRS) standardized 35-mm color stereoscopic mydriatic images. The seven stereoscopic color photographs served as the reference standard and were compared with either ophthalmoscopy or a single digital photograph transmitted electronically to a reading site. Levels of agreement were determined by kappa analyses. The sensitivity and specificity of the three methods were compared based on a threshold for referral to further ophthalmologic evaluation (ETDRS level > or =35). RESULTS: There was highly significant agreement (kappa = 0.97, P =.0001) between the degree of retinopathy detected by a single nonmydriatic monochromatic digital photograph and that seen in seven standard 35-mm color stereoscopic mydriatic fields. The sensitivity of digital photography compared with color photography was 78%, with a specificity of 86%. Agreement was poor (kappa = 0.40, P =.0001) between mydriatic ophthalmoscopy and the seven-field standard 35-mm color photographs. Sensitivity of ophthalmoscopy compared with color photography was 34%, with a specificity of 100%. CONCLUSION: A single nonmydriatic monochromatic wide-field digital photograph of the disk and macula was more sensitive for diabetic retinopathy screening than mydriatic ophthalmoscopy, the currently accepted screening method. When adjudicated by standard seven-field color photographs, the higher sensitivity of digital photography primarily reflected the reduced sensitivity of ophthalmoscopy in detecting early retinopathy.

Adult↗

Effect of postoperative mydriatics on the iris.

PURPOSE: To assess the role postoperative mydriatics play after extracapsular cataract extraction (ECCE) and posterior chamber intraocular lens (IOL) implantation in causing iris modifications and in controlling inflammation. SETTING: Outpatients Department, Ninewells Hospital, Dundee, Scotland. METHODS: The prospective study comprised 136 patients who had standardized ECCE. Half the patients used a mydriatic for 2 weeks postoperatively. Anterior chamber activity, pain, and eye redness were evaluated at 2 weeks postoperatively; pupil shape, peripheral anterior synechias, IOL position, and iris adhesions, at 6 weeks. RESULTS: Iris-lens adhesions were significantly more common in the group using a mydriatic. There was no difference between the two groups in postoperative inflammation. CONCLUSION: Mydriatics should not be used routinely after ECCE with posterior chamber IOL implantation.

Aged↗

[Aberrometry due dilated pupils--Which mydriatic should be used?].

BACKGROUND: For a wavefront-based LASIK procedure aberrometric measurements are necessary via a dilated pupil. The more dilated the pupil is the more aberrations can be identified. There are different mydriatic eyedrops used to dilate the pupil. It is unclear so far which mydriatic is best for measuring aberrations before LASIK. METHODS: We performed aberrometry measurements on 50 eyes under the following different conditions: physiological mydriasis under mesopic environment, tropicamide-induced dilation, phenylephrine-induced dilation, and cyclopentolate-induced dilation. The wavefront measurements were compared with the respective subjective refraction (sr). RESULTS: The refractive myopic error measured by aberrometry was less than after subjective refraction depending on the mydriatic used. Phenylephrine-induced mydriasis resulted in 0.19 D less myopia, tropicamide induced 0.35 D less myopia, and cyclopentolate 0.42 D less on the average. The aberrometry measurements under mesopic conditions led to 0.24 D less myopia than measured subjectively. CONCLUSION: Using cyclopentolate eyedrops wavefront analysis results in a considerable difference in the preoperative refractive error compared to the standard subjective refraction. Regarding the average differences in refraction the aberrometry measurements after neosynephrine-induced dilation of the pupil usually resemble the subjective refractive error. For practical reasons we would like to recommend aberrometry measurements under mesopic conditions without applying mydriatics provided the pupillary diameter is at least 6 mm.

Adult↗

Enhancement of the mydriatic response to tropicamide by bioadhesive polymers.

The aim of this work was to evaluate how the addition of mucoadhesive polymers to aqueous solutions affects the ocular response of tropicamide (0.2%; w/v). The polymer solutions tested were carboxymethylcellulose sodium salt (CMC-Na; 1%; w/v), hyaluronic acid sodium salt (HA-Na; 0.1%; w/v) and polyacrylic acid (PAA; 0.2%; w/v). Polymeric solutions were compared to a nonviscous formulation (AS). In vitro mucoadhesion measurements were expressed as a percentage of the adhesion force mucin-mucin, considering this one as 100% mucoadhesion. The values ofmucoadhesion obtained were 172%, 127%, 103% and 87.6% for formulations with CMC, PAA, HA and AS, respectively. The mydriatic response of tropicamide was determined in adult male New Zealand rabbits, weighing 1.7-2 Kg, by pupil diameter measurements at different times after instillation. The area under the mydriatic response-time curve (AUC 0-6 hr) was interpreted as an indication of the bioavailability of tropicamide in each vehicle. The AUC 0-6 hr was related to the in vitro mucoadhesion for each formulation. Tropicamide solutions with CMC-Na and PAA resulted in mucoadhesion and AUC 0-6 hr values approximately 1.9 and 1.4 times higher than AS. Although the solution with HA-Na was less mucoadhesive than PAA, the hyaluronic acid solution resulted in a higher AUC mydriasis/time value. Formulations with HA-Na and PAA presented values of surface tension close to that observed in the lacrimal fluid, with the Imax (maximum pupil diameter) being higher than for CMC-Na and AS. Greater than 90% of the mydriatic effect disappeared 4.5 hr after instillation for PAA and AS. Nevertheless, the mydriatic effect remained up to 5.5 hr for HA-Na and CMC-Na. HA-Na solution enhanced the bioavailability oftropicamide, presenting a value of mucoadhesion similar to the reference mucin-mucin.

Acrylic Resins↗

Consensual pupillary responses to mydriatic and miotic drugs.

1. Three experiments were conducted to examine whether mydriatic or miotic drugs instilled into one eye have any effect on the diameter of the pupil of the untreated fellow eye, in healthy volunteers. 2. In Experiment 1, the effects of four subjects, using photography in an illuminated room to assess pupil diameter. The drug evoked a dose-dependent mydriasis in the index eye which was accompanied by a simultaneous dose-dependent miosis in the fellow eye. 3. In Experiment 2, the same method was used to assess pupil diameter as in Experiment 1. The effects of mydriatic (methoxamine and tyramine) and of miotic (pilocarpine) drugs instilled into the fellow eye, were studied on the sizes of pupillary responses to the same drugs instilled into the index eye. The presence of a mydriatic drug in the fellow eye resulted in a decrease in the size of the mydriatic responses in the index eye. 4. In Experiment 3, the effects of three concentrations of phenylephrine hydrochloride (0.15-0.60 M) and of three concentrations of pilocarpine hydrochloride (0.002-0.008 M), were studied in darkness using an infra-red binocular television pupillometer, in seven subjects. Phenylephrine evoked dose-dependent mydriasis and pilocarpine evoked dose-dependent miosis. The pupillary responses of the index eye were not accompanied by any changes in the diameter of the pupil of the fellow eye. 5. It is concluded that drug-induced mydriasis in the index eye is accompanied by a consensual miosis in the fellow eye.(ABSTRACT TRUNCATED AT 250 WORDS)

Adolescent↗

Short acting soft mydriatics.

Three soft drug analogs of atropine have been tested for mydriatic activity in rabbits' eyes and their in vitro metabolic pathway has been investigated in rat, rabbit and human blood. The three soft drugs were found to produce an equieffective mydriatic activity to atropine and tropicamide. At equieffective concentrations, their durations were shorter with AUC's 12-21% that of 0.25% atropine and 44-80% that of 0.2% tropicamide. The untreated control eyes were observed to dilate after unilateral ocular administration of atropine, but not with unilateral soft drug treatment. In vitro stability studies showed that the soft ethyl analog was less stable in rat blood and rat liver homogenate than in rabbit or human blood. The metabolic product of the soft ethyl derivative in biological media was proven to be the corresponding inactive acidic metabolite predicted by the soft drug design. The ultrashort durations and the potentially nontoxic systemic properties of the soft mydriatics offer promise for use in ophthalmoscopy and in other ocular procedures where a short acting anticholinergic type of mydriatic would be indicated.

Animals↗

The risks of precipitating acute angle-closure glaucoma with the clinical use of mydriatic agents.

The risks of precipitating acute angle-closure glaucoma is always present when eyes have shallow anterior chambers, and early recognition of angle-closure glaucoma is important to prevent permanent loss of vision. Two groups of patients with acute angle-closure glaucoma are presented: in the first the attack was immediately preceded by the use of a mydriatic agent and in the second a mydriatic agent had been used previously without incident but the patient later presented with a spontaneous acute attack. A shallow anterior chamber, and in particular inequality of anterior chamber depths of greater than 0.2 mm, were important indicators of susceptibility to angle closure, which is more common in women than in men. Where there is a risk of angle closure, tropicamide 0.5% appears to be the safest mydriatic agent and should be followed by the administration of a miotic agent in susceptible individuals. The need to carry out a peripheral iridectomy in the other eye is stressed, irrespective of the age of the patient. A case of acute glaucoma after the use of oral drops that contained belladonna for nasal allergy further highlights the risks of the use of systemic mydriatic agents in susceptible individuals.

Acute Disease↗

[Effects of pre-instilled mydriatics on the intraocular concentration and anti-inflammatory action of topical 0.1% pranoprofen (3)--study on permeability factor].

The authors studied a mechanism of an increase in intraocular concentration of topical 0.1% pranoprofen (PPF) induced by pre-instilled mydriatics (0.5% tropicamide and 0.5% phenylephrine) in rabbit eyes. Ingredient solutions of mydriatics were instilled 60 minutes prior to instillation of PPF. The PPF concentrations in the cornea, aqueous humor and iris-ciliary body did not increase with pre-instilled benzalkonium chloride, chlorobutanol and tropicamide. The PPF concentrations were increased by pre-instilled phenylephrine (PHE), and the concentrations were 2 to 3 times higher than those without mydriatics. The PHE concentration in the aqueous humor was increased about 3 times in the presence of PPF. The octanol/water partition coefficient of PPF was increased in the presence of PHE. These data indicate that the increase of intraocular PPF concentration by the pre-instilled mydriatics was caused by PHE, and the enhancement of transcorneal permeability to PPF may have resulted from the formation of ion-pair complexes between PPF, an anionic drug, and PHE, a cationic drug.

Animals↗

Evaluation of a new non-mydriatic digital camera for detection of diabetic retinopathy.

AIMS: To compare the results of fundus photography using a new non-mydriatic digital camera with the results of reference standard of Early Treatment Diabetic Retinopathy Study (ETDRS) retinal photographs, for the detection of diabetic retinopathy (DR). METHODS: Fundus colour photographs were taken with a Topcon non-mydriatic camera of 147 eyes of 74 diabetic patients, without pupillary dilation (five overlapping fields of 45 degrees; posterior pole, nasal, temporal, superior and inferior). Three retinal specialists classified the photographs in a masked fashion, as showing no DR or mild non-proliferative DR (NPDR) not requiring referral, moderate or more severe NPDR and/or macular oedema, or as non-gradable image requiring referral. ETDRS 35-mm colour slides served as reference images for DR detection. RESULTS: For moderately severe to severe DR, the sensitivities of detection reported by the three observers were 92, 100 and 92%, respectively, and the specificities, 87, 85, and 88%. For four levels of DR severity (none or mild NPDR, moderate NPDR, severe NPDR and proliferative DR), the percentages of exact agreement between the three observers on the retinopathy grades assigned to the non-mydriatic photographs and to the ETDRS reference slides were 94.6, 93 and 87.6%, respectively (kappa 0.60-0.80). Sixteen eyes of nine patients (11%) were judged ungradable by at least one observer. In a second series of 110 patients, evaluated in the setting of a screening procedure, fewer photographs were ungradable (< 6%). CONCLUSION: These results suggest that fundus photographs taken by the Topcon TRC-NW6S non-mydriatic camera, without pupillary dilation, are suitable for DR screening.

Adult↗