复方托吡卡胺滴眼液致突发性耳聋

1名60岁女性糖尿病患者，行眼底检查前用复方托吡卡胺滴眼液散瞳，随后出现听力明显下降伴耳呜，检查提示双耳感音神经性耳聋。经高压氧、葛根素治疗后，听力明显恢复。因眼科检查需要，再次用复方托吡卡胺滴眼液，用药后患者又出现听力明显下降，经对症治疗后好转。当患者第4次使用该药后出现耳聋，治疗1月余，听力仍未恢复。     

托吡卡胺滴眼液防治青少年假性近视效果分析

目的 观察托吡卡胺滴眼液防治青少年假性近视的效果,探讨其临床价值.方法 回顾性分析68例(136只眼)青少年假性近视患者资料,观察应用托吡卡胺滴眼液的验光情况及治疗前后裸眼视力变化.结果 托吡卡胺滴眼液不同滴眼间隔(间隔1 min或间隔5min)散瞳效果差异无统计学意义(P＞0.05),且滴眼间隔不同的假性近视青少年第一次复光的屈光度检查差异无统计学意义(P＞0.05);治疗前、治疗后1周散瞳验光裸眼远视力差异有统计学意义(x2=16.3308,P=0.000969964);治疗1周、治疗4周散瞳光情况差异有统计学意义(x2=50.2750,P=6.98115 × 10-11).结论 0.25％托吡卡胺滴眼液间隔1 min、5 min滴眼散瞳效果满意.托吡卡胺短期内使用能够有效解除青少年假性近视的调节痉挛和调节麻痹现象,而且无明显药物不良反应,具有临床使用价值.     

Reversal of tropicamide-induced mydriasis by thymoxamine eye drops

In a study in 12 healthy volunteers, local instillation of thymoxamine eye drops (0.5%), completely reversed the mydriasis produced by tropicamide (0.5%), but only incompletely that by tropicamide (1.0%). The difference between these effects was statistically significant (p less than 0.025). The thymoxamine eye drops were well tolerated.     

糖尿病视网膜病变患者围手术期散瞳策略

目的：探讨糖尿病视网膜病变患者围手术期最佳散瞳方法,以利于玻璃体切割手术顺利进行。方法：回顾性分析我院2007年6月-2011年6月所有糖尿病视网膜病变患者的手术资料,选取术前常规应用复方托吡卡胺滴眼液、术中瞳孔直径≥7mm的患者手术时散瞳药的应用记录,共189例,204眼。术前点复方托吡卡胺滴眼液,每5min1次,共6次。点滴眼液后,0.5h内瞳孔散大（直径≥7mm）者为A组（78眼）;超过0.5h,但瞳孔散大时间在1h以内者为B组（75眼）;瞳孔散大时间大于1h者为C组（51眼）。B、C组于术前一天随机应用硫酸阿托品眼用凝胶或盐酸环喷托酯滴眼液,术前1h频点复方托吡卡胺滴眼液。结果：术中瞳孔直径能维持≥7mm的眼数比例,B、C组应用硫酸阿托品眼用凝胶者与应用盐酸环喷托酯滴眼液者差异均无统计学意义（P〉0.5）。术中有134眼因白内障同时行超声乳化白内障摘除术,其术中瞳孔直径能维持≥7mm的眼数比例,B组应用盐酸环喷托酯滴眼液者瞳孔维持的比例较用硫酸阿托品眼用凝胶者高（P〈0.5）,C组中二者比较差异无统计学意义（P〉0.5）。结论：对于术前单用复方托吡卡胺滴眼液散瞳时间超过0.5h者,术前点硫酸阿托品眼用凝胶或盐酸环喷托酯滴眼液有利于维持术中瞳孔大小,且二者效果差异无统计学意义。     

Pharmacodynamics of a new ophthalmic mydriatic insert in healthy volunteers: potential alternative as drug delivery system prior to cataract surgery

Cataract surgery requires a satisfactory degree of mydriasis throughout the entire operation. A phase I, open-labelled, randomised, cross-over trial was conducted in 18 healthy volunteers to compare mydriasis obtained with subsequent administration of phenylephrine 10% and tropicamide 0.5% eyedrops or a new insoluble-matrix retropalpebral ophthalmic insert containing 5.38 mg phenylephrine and 0.28 mg tropicamide. Phenylephrine serum concentrations were measured over 6 hr following each treatment administration. Secondary end-points included cardiovascular, general and local tolerance and quantification of bacterial colonisation of the conjunctiva and the cultured insert, respectively. When normalized to the pupil diameter after conventional treatment, the diameter achieved with the insert was 1.13 (95% confidence interval, 0.94-1.48, P=0.38). Moreover, standard eye drops provided faster effective mydriasis than the insert, starting 30 min. as compared to 90 min. upon treatment administration (P<0.01, repeated-measures ANOVA). Phenylephrine concentrations remained almost undetectable for both treatments and no change in heart rate or blood pressure were observed throughout the study. Only three superficial punctuate keratitis were diagnosed with the insert and two with the eye drops. No significant bacterial contamination of conjunctiva swab and cultured insert was observed. The new insoluble-matrix retropalpebral ophthalmic mydriatic insert produced similar but delayed effective and prolonged mydriasis as compared to the standard delivery system. In addition to its potential usefulness in patients undergoing cataract surgery, such new ophthalmic delivery system may be an advantage in children who need to undergo fundus photography due to the single administration and excellent tolerance as well.     

早产儿用复方托吡卡胺眼水散瞳的研究

目的研究复方托吡卡胺眼水在不同胎龄早产儿散瞳效果,加强其在早产儿眼底病筛查的管理。方法在低胎龄和高胎龄早产儿的左右眼分别滴用2次和3次复方托吡卡胺眼水。按距双眼第一次点眼散瞳时间长短将其随机平均分成A、B、C三组。A组距双眼第一次点眼散瞳时间45min行双眼瞳孔直径测量及眼底检查;B组为60min;C组是90min。结果 A、B组中左、右眼散瞳直径无差异(P>0.05),C组左眼散瞳直径比右眼小(P<0.05)。无论散瞳时间的长短,低胎龄和高胎龄早产儿组的平均瞳孔直径比较无差异(P>0.05)。结论滴2次复方托吡卡胺眼水60min后行眼底检查更安全有效,并且复发托吡卡胺眼水对不同胎龄的早产儿散瞳效果无差异。     

妥布霉素/地塞米松治疗白内障人工晶体术后迟发性前葡萄膜炎的疗效观察

目的:观察妥布霉素/地塞米松局部滴眼治疗白内障人工晶体植入术后迟发性前葡萄膜炎的疗效。方法:观察组19例(19只眼)给予妥布霉素/地塞米松滴眼液和眼膏治疗;对照组11例(11只眼)给予地塞米松10～20mg静脉滴注,3～5d后改为强的松顿服逐渐减量。2组同时以复方托吡卡胺滴眼液散瞳。结果:所有病例用药后3～5d炎症迅速控制,视力明显好转。观察组在治疗期间未发现不良反应;对照组部分病例出现激动、失眠,血压、血糖异常升高。结论:妥布霉素/地塞米松局部滴眼能有效治疗白内障术后迟发性前葡萄膜炎。     

Why patients with Alzheimer’s disease may show increased sensitivity to tropicamide eye drops: role of locus coeruleus

Rationale Patients suffering from Alzheimer’s disease (AD) may show increased sensitivity to tropicamide, a muscarinic cholinoceptor antagonist. AD is associated with a severe loss of noradrenergic neurones in the locus coeruleus (LC), which can be “switched off” experimentally by the α₂-adrenoceptor agonist clonidine. The possibility arises that increased pupillary sensitivity to tropicamide in AD may be due to diminished LC activity. Objective To examine the hypothesis that clonidine may potentiate tropicamide-evoked mydriasis. Materials and methods Sixteen healthy male volunteers participated in two experimental sessions (0.2 mg clonidine or placebo) conducted 1 week apart. In each session tropicamide (0.01% 10 μl×2) was applied to the left eye and artificial tear (10 μl×2) was applied to the right eye. Pupillary functions (resting pupil diameter and light and darkness reflexes), alertness and non-pupillary autonomic functions (blood pressure, heart rate, core temperature and salivary output) were measured. Data were analysed by ANOVA, with multiple comparisons. Results Tropicamide increased resting pupil diameter, velocity and amplitude of the darkness reflex response, and decreased recovery time of the light reflex response. Clonidine affected all these pupillary measures in the opposite direction with the exception of the recovery time. The mydriatic response to tropicamide was potentiated by pre-treatment with clonidine. Clonidine reduced critical flicker fusion frequency, subjective alertness, blood pressure, salivation and temperature. Conclusions The potentiation of tropicamide-evoked pupil dilatation by clonidine may be due to the abolition of the increase in parasympathetically mediated pupil constriction due to reduced LC activity.     

不同浓度托吡卡胺治疗学龄儿童假性近视的临床观察

目的评价0．5％托吡卡胺滴眼液治疗学龄儿童假性近视的临床效果和用药后的不良反应情况,指导临床应用。方法应用0．5％托吡卡胺滴眼液,隔晚给药;0．25％托吡卡胺滴眼液每晚给药,对假性近视的学龄儿童（每组100例,200眼）进行治疗。治疗前后,记录裸眼远视力,散瞳后的静态屈光度。结果两组假性近视的学龄儿童,治疗后裸眼远视力均有提高,差异有统计学意义（P〈0．01）;治疗后静态屈光状态呈大部分近视度数降低,差异有统计学意义（P〈0．01）。两组间用药后的不良反应出现的频率,差异有统计学意义（P〈0．01）。结论0．5％托吡卡胺滴眼液,隔晚使用,防治青少年假性近视疗效确切。可减少用药后的不良反应,增加用药顺应性。     

玻璃酸钠滴眼液对轻中度干眼病患者角膜表面规则性的影响

目的评价玻璃酸钠滴眼液对干眼病患者的角膜表面规则性的影响。方法应用DICON——CT200角膜地形图仪检测滴玻璃酸钠滴眼液前后33例（64眼）干眼病患者的角膜表面规则指数（surface regularity index,SRI）表面不对称指数（surface asymmetry index,SAI）及角膜预测视力（potential visual acuity,PVA）的变化进行观察。结果干眼病患者的SRI、SAI、PVA值及散光度分别为1.32±0.44、1.11±1.43、20/30.12±20/11.93及2.45±1.9;滴玻璃酸钠滴眼液后SRI、SAI、PVA值分别0.83±0.21、0.59±0.31、20/21.03±20/5.12及1.87±1.13。干眼病患者在滴玻璃酸钠滴眼液后SRI、SAI和散光度均明显降低,而PVA则明显升高。滴玻璃酸钠滴眼液前干眼病患者的角膜地形图43.8%为不规则形,应用玻璃酸钠滴眼液后不规则形降为29.7%。结论SRI和SAI可作为诊断干眼病的客观指标并可用于评价干眼病的严重程度及玻璃酸钠滴眼液的疗效。璃酸钠滴眼液可改善干眼病患者的角膜表面光滑度。     

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)     

Vision and eye problems in seven year olds: a report from the Dunedin Multidisciplinary Health and Development Research Unit

An eye examination, including tests of distance visual acuity, near visual acuity, cover tests, and an examination of pupils, eyes, adnexia, and eye movements, was carried out on 988 Dunedin children within approximately one month of their seventh birthday. Information concerning glasses and patching of one eye was obtained by questionnaire. Eye defects were noted in 9.4% of the children with several having more than one problem. Eye defects noted included 5.1% with unaided distance visual acuity of 6/12 or worse in one or both eyes, 4.4% with near visual acuity of the equivalent of N8 or worse in one or both eyes, 3.9% had manifest strabismus, 2.9% had had occlusion of one eye for amblyopia, and 1.2% had other important eye defects. Glasses had been prescribed for 3.6%.     

Comparative in vitro investigation of the forces exerted by eye drops and eye spray

Topical administration of ophthalmic drugs is predominantly carried out in the form of eye drops. The application of an eye spray represents a feasible alternative to drop instillation with regard to the clinical efficacy. In this study the forces exerted during the application of eye drops and eye spray to a surface were measured in vitro and compared with each other. Whereas the maximal forces that occurred with a falling drop tended to increase with greater application distance, the forces decreased with spraying. From an application distance of 3 cm the eye spray proved to have a more favorable mechanical force effect than the eye drops. In view of the loss of experimental liquid caused by spray application as well as the diameter of the spray cone, a spray distance of from 4 cm to 5 cm can be deemed to be optimal.     

Evaluation of the effect of thymoxamine solution 0.5% on mydriasis induced by ibopamine solution 1%

Summary The effects of thymoxamine 0.5% solution and of a placebo solution (mannitol) on the mydriasis induced by ibopamine 1% solution were evaluated in 8 healthy volunteers and 12 patients with eye diseases.One drop of ibopamine was instilled into each eye and 30 min later 1 drop of thymoxamine was instilled into one eye and 1 drop of placebo into the contralateral eye. Pupillary diameter was measured before and 30 min after the instillation of ibopamine, immediately before the treatment with thymoxamine and placebo and 30, 60 and 90 min after the instillation of thymoxamine or of placebo.Within 30 min of treatment, ibopamine had produced a statistically and clinically significant mydriatic effect. In eyes treated with thymoxamine, prompt reversal of mydriasis was observed, the baseline diameter being observed within 60 min.No difference in the time-course of the mydriatic effect was detected between healthy subjects and patients. The pupillary response to thymoxamine was not influenced by the colour of the iris. The tolerability of ibopamine and of thymoxamine was good. No local or systemic adverse events were seen or reported.     

盐酸戊乙奎醚对全麻患者瞳孔大小及眼压的影响

目的:观察盐酸戊乙奎醚对手术患者麻醉期间眼局部瞳孔和眼压的变化和对眼部安全性。方法:46例拟在全麻下行腹腔胆囊切除手术的慢性胆囊炎、胆石症患者,ASAⅠ～Ⅱ级,随机分为盐酸戊乙奎醚组、阿托品组各23例。患者入手术室安静10 min后,记录瞳孔大小作为基础值,用0.4%盐酸奥布卡因滴眼液在左右眼球上各滴1滴进行表麻,2—3 min后测量左右眼球的眼压;在右肩三角肌注射阿托品或盐酸戊乙奎醚。30 min后及清醒30 min后再次记录瞳孔大小和眼压值。结果:在给药30 min后阿托品组双眼眼压都高于盐酸戊乙奎醚组(P<0.05)。两组病人的瞳孔大小基础值无统计学差异,在给药30 min后阿托品组双眼瞳孔都大于基础值(P<0.01),也大于盐酸戊乙奎醚组(P<0.01)。结论:在术前使用盐酸戊乙奎醚不升高眼压,对眼部较为安全。     

Ocular Pharmacokinetics and Pharmacodynamics of Phenylephrine and Phenylephrine Oxazolidine in Rabbit Eyes

The aqueous humor concentration of phenylephrine and its corresponding mydriatic response were measured over time in New Zealand albino rabbit eyes following a 10-µl topical instillation of a phenylephrine HC1 viscous solution (10%) or a phenylephrine oxazolidine (prodrug) suspension in sesame oil (1 and 10%). The bioavailability of a 1% prodrug suspension in the rabbit eye (AUC of aqueous humor concentration vs time) was 30% lower than that of a 10% phenylephrine solution (P < 0.1) with the exception that the peak time occurred 34 min earlier with the prodrug. A 10% prodrug suspension increased the aqueous humor bioavailability approximately eightfold but improved the mydriatic activity (AUC of mydriasis vs time) only fourfold. The pharmacokinetic parameters, apparent absorption, and elimination rate constants, of phenylephrine and the prodrug were determined from aqueous humor concentration–time and mydriasis–time profiles. The study showed that the kinetic parameters of phenylephrine estimated from its mydriasis profile do not accurately reflect the kinetics of drug distribution in the iris. These parameters also varied with the instillation of phenylephrine solution or prodrug suspensions. A mydriatic tolerance of the pupil response was apparent after the topical instillation of phenylephrine solution. The mydriatic tolerance may be due to the decrease in receptor number in the iris dilator muscle.     

Characterization of the force effect of aqueous and oily eye drops

During the instillation of eye drops the drop impact affects a mechanical irritation on the eye surface. The force impact occurring in the moment of impact may be measured in vitro. Four commercially available eye drop preparations of different consistency and viscosity were tested. In dependance on the drip distance, the quantity of force impact was determined as well as the maximally effecting force during impact in each case. Whereas the force impact increased with all preparations with rising drip distance, only the higher viscosity solutions showed an approximate linear increase of the maximal force. With the aqueous low-viscosity eye drops, peak forces were ascertained. The drop oscillation was considered as the cause. The test results show that the consistency of eye drop preparations and their resulting physical-chemical properties like viscosity influence the quantity of the maximal force during the drop impact.     

棘阿米巴角膜炎6例治疗分析

目的总结6例因配戴角膜接触镜(CL)引起的棘阿米巴角膜炎的临床资料,并探讨其成功治疗经验。方法回顾性分析6例棘阿米巴角膜炎的临床资料和治疗经过。结果 6例患者(平均年龄25岁)均配戴CL(1例硬性CL,5例软性CL)。其中5例以角膜剧烈疼痛为主诉就诊。4例初次眼科检查时确诊假树枝状角膜炎,2例表现为放射状角膜神经炎和环状基质混浊。所有病例进行角膜刮片培养并确诊棘阿米巴感染。5例立即开始0.02%氯己定联合抗真菌滴眼液滴眼治疗,最终矫正视力获得不同程度的提高,范围为0.5～1.5。另外1例未能及时治疗,角膜炎症状恶化,视力下降为手动,施行穿透性角膜移植+白内障手术,术后矫正视力提高到0.6。结论棘阿米巴角膜炎病例早期阶段及时应用0.02%氯己定联合抗真菌药物滴眼可提高疗效,避免不必要手术,并产生相对较好的最终视力。     

Pharmaceutical investigation of vancomycin hydrochloride eye drops and their topical application to MRSA eye infection]

Two formulations of 0.5% vancomycin hydrochloride (VM) eye drops (VM-B and VM-C eye drops) were prepared by dissolving commercial VM powder for injection with preserved water B (PWB) containing phosphate buffer and preserved water C (PWC) containing only antimicrobial preservative, respectively. The VM-B eye drops have neutral pH (about 6.3), and the VM-C eye drops acidic pH of about 3.5. The pharmaceutical examination of these eye drops was performed regarding its clinical application to MRSA eye infection. In an irritability test using a rabbit's eye, the average number of winks after instillation of one drop of VM-B eye drops was 0.8 times/min and significantly smaller than that of VM-C eye drops (2.0 times/min). In dark storage at 4 degrees C, no change of VM concentration in both eye drops was observed for 25 weeks after preparation and the mean residual concentrations as determined by the HPLC-UV (240 nm) method were constant over 90% for 8 weeks, of the initial concentration. However, the residual VM concentration of VM-B eye drops under a room condition declined to 58% after 4 weeks and 20% after 8 weeks, and VM in light storage at 40 degrees C was not detectable after 8 weeks. The drug concentration of VM-C eye drops declined to 83% after 4 weeks and 74% after 8 weeks under a room condition, and to 46% after 4 weeks and 20% after 8 weeks under light storage at 40 degrees C. Under these storage conditions, the precipitation of VM related crystals was observed in both the eye drops when the residual percentage of VM was lower than 80%. Judging from HPLC chromatograms of a solution of the precipitated crystals, it was suggested that this crystal was degradation products of VM. The VM-B eye drops was applied to a patient with MRSA eye infection, because other medication was not effective. After continuous instillation of a drop per times every hour to both eyes, MRSA in corneal culture turned out negative after one week, and the clinical condition was remarkably improved. On the basis of the result of eye-irritability, VM-B eye drops with neutral pH was suggested to be superior to acidic VM-C eye drops from a safety point of view. It was also indicated that VM-B eye drops can be effectively used for 8 weeks under dark storage at 4 degrees C for MRSA eye infection, which is a useful piece information for the proper usage of the VM eye drops.     

Efficacy assessment of various anticholinergic agents against topical sarin-induced miosis and visual impairment in rats

Eye exposure to the organophosphorus (OP) irreversible acetylcholinesterase inhibitor sarin results in long-term miosis and reduction in visual function. Anticholinergic drugs, such as atropine or homatropine, which are used topically in order to counter these effects may produce mydriasis and partial cycloplegia, which may worsen visual performance. This study was aimed to test the efficacy of short-acting anticholinergic drugs against sarin-induced miosis and visual impairment, which will minimally insult vision. Long-Evans rats, exposed topically to various sarin doses from 0 to 10 μg, showed a dose-dependent miosis, which returned to pre-exposure levels within 24-48 h. Tropicamide treatment rapidly widened the miotic effect to a different extent depending on time following treatment and dosage given. Cyclopentolate, however, showed a delayed response that finally widened the pupils in a dose-dependent manner. Atropine treatment showed a rapid widening of the pinpoint pupils exceeding baseline level finally causing mydriasis. Light reflex test showed that the contraction ability of the iris following atropine treatment was impaired, as opposed to the use of tropicamide which facilitated the iris contraction, similar to control. Finally, tropicamide and atropine treatments ameliorated the visual impairment, as opposed to cyclopentolate, which worsened visual performance. Considering that tropicamide treatment against sarin exposure did not cause mydriasis nor did it impair the iris contraction flexibility as a response to light, the use of this drug should be taken into consideration as a first-choice topical treatment against OP intoxication.