Pilocarpine used to treat xerostomia in patients submitted to radioactive iodine therapy: a pilot study

Xerostomia complaint is very commonly associated to radioactive iodine therapy. Alternatives to treat this morbidity can offer better quality of life to patients with thyroid cancer submitted to adjuvant iodine therapy.Aimto report on the experience with pilocarpine on the treatment of xerostomia in thyroid cancer patients submitted to adjuvant radioactive iodine therapy (RIT).Materials and methodsThe five patients who met the inclusion criteria received 5mg of pilocarpine, 3 tid for one week. Side effects of the drug and subjective response to xerostomia complaints after treatment were evaluated.Designit is a prospective, non-randomized study.ResultsSudoresis was the most frequent side effect of pilocarpine use, followed by fatigue and headache. Two patients reported relief of xerostomia using pilocarpine, but only one patient was able to tolerate the side effects.ConclusionsPilocarpine seems to relieve xerostomia complaints in thyroid cancer patients because it is able to stimulate salivary flow, but the observed side effects made the patients refuse long-term therapy continuation.     

毛果芸香碱致慢性癫癎大鼠脑内药物转运体表达的变化

目的 研究有机阴离子转运多肽亚型2（Oatp2）及P-糖蛋白（P-gp）在氯化锂-毛果芸香碱诱导的慢性癫癎大鼠脑组织中的表达。方法采用氯化锂-毛果芸香碱诱发Wistar大鼠慢性癫癎模型，免疫组织化学法检测其脑内Oatp2、P-gp的分布及表达情况。结果Oatp2及P-gp免疫反应阳性物质主要定位于脉络丛上皮细胞膜及脑血管内皮细胞膜，神经细胞膜也可见染色；癎性大鼠脑内0atp2的表达低于正常大鼠（P〈0．05）；而P-gp的表达高于正常大鼠（P〈0．05）。结论慢性癫癎大鼠脑内同时存在药物转运体Oatp2及P-gp的表达，两者表达变化相反。在癫癎病理过程中，Oatp2可能具有与P-gp不同的作用。     

边缘癫痫实验模型海马内突触体素表达

目的探讨癫痫时突触体素(P^38)在海马表达的时间变化及意义。方法建立匹罗卡品边缘癫痫模型，用图像分析系统测定海马不同时间点P^38免疫反应吸光度值。结果P^38免疫反应性在海马呈现两次高峰：致痫后3～6h在海马门区及CA3区P^38短期升高，30～60dCA3区呈现第2次高峰。在内分子层，从第7天开始直至第60天P^38呈进行性增多，且与Neo—Timm染色结果相平行。结论P^38在海马第2次表达增高，平行于苔藓纤维出芽，与自发性发作形成有关。急性期表达增高则与癫痫持续状态的产生与维持有关。     

Oral pilocarpine HCl stimulates labial (minor) salivary gland flow in patients with Sjögren's syndrome

Pilocarpine HCl has been shown to stimulate parotid and submandibular gland salivary flow. The purpose of this study was to determine whether this cholinergic-muscarinic drug also stimulates labial (minor) salivary gland (LSG) flow and to relate that with whole unstimulated salivary (WUS) flow rateS. Subjects diagnosed with primary Sjögren's syndrome (SS-1; n = 9) or secondary Sjögren's syndrome (SS-2; n = 9) were enrolled in this study after meeting stringent enrollment criteria. An age-gender matched control group was also enrolled. The labial saliva was collected in a standardized manner on Per-iopaper® for 5 min and the volume was analysed by the Periotron®.Whole unstimulated salivary samples were collected for 5 min by the method of Mandel and Wot-man (1976).Each subject was dosed with pilocarpine HCl (5 mg; tablets; p.o.).After 60 min the LSG flow as well as the WUS flow was determined again as previously. The results indicated a significant (>180%) increase in both labial salivary gland flow as well as whole salivary flow in the SS-1 and SS-2 subjects (mean ± S. e.m.): [SS-1: WUS = 0.1080 ± 0.03 vs 0.2242 ± 0.03 ml per 5 min; LSG = 93.1 ± 22.2 vs 167.8 ± 15.9 μl/5 min; P < 0.001; SS-2: WUS = 0.1384 ± 0.02 vs 0.2775 ± 0.09 ml per 5 min; LSG = 97.7 ± 20.2 vs 182.8 ± 17.9 μl per 5 min; P < 0.001]. These results indicate a significant increase in labial salivary gland flow as well as whole salivary flow as stimulated by pilocarpine HCI in Sjögren's syndrome patients.     

二阶导数光谱法测定硝酸毛果芸香碱滴眼液的含量

本文采用二阶导数光谱法测定硝酸毛果芸香碱滴眼液的含量,以230nm 为测定波长,可排除附加剂的干扰,快速简便。平均回收率99.99%,变异系数0.16%。     

梭曼和毒扁豆碱引起大鼠脑电癫痫波的M和N胆碱能成分

在加拉碘铵麻痹，人工呼吸维持和甲基阿托品预防的大鼠上，梭曼ＦＳ０．１ｍｇ·ｋｇ－１ｉｍ（ｎ＝２４）或毒扁豆碱３０．０ｍｇ·ｋｇ－１ｉｖ（ｎ＝１８）使全部大鼠脑电图（ＥＥＧ）上出现早期持续很短的紧张性癫痫波和随后持续很长的阵挛性癫痫波．中枢＃ＦＳＮ＃ＦＫ受体激动剂烟碱１．０ｍｇ·ｋｇ－１ｉｖ（ｎ＝３８）和中枢Ｍ受体激动剂槟榔碱１５０ｍｇ·ｋｇ－１ｉｖ（ｎ＝４６）或匹鲁卡品３８０ｍｇ·ｋｇ－１ｉｖ（ｎ＝２４）能分别在ＥＥＧ癫痫波的特征，出现时间和持续时间上模拟出上述早期紧张性癫痫波和随后的阵挛性癫痫波．预先小剂量ｉｖ烟碱使中枢Ｎ受体脱敏或给小剂量Ｎ受体拮抗剂美加明保护中枢Ｎ受体后，梭曼只能引起潜伏期较长且持续很久的阵挛性癫痫波．胆碱酯酶抑制剂梭曼和毒扁豆碱较大剂量引起大鼠ＥＥＧ癫痫波可能的机理是过量的乙酰胆碱作用于潜伏期短，容易脱敏的Ｎ受体出现早期持续很短的ＥＥＧ紧张性癫痫波，又作用于潜伏期较长，不容易脱敏的Ｍ受体，出现稍后的ＥＥＧ阵挛性癫痫波     

Pattern electroretinogram: Effects of miosis,accommodation, and defocus

The effect of miosis, lens accommodation, and defocusing on the various components of the pattern electroretinogram elicited by checkerboard reversal was investigated by employing aperture stops of different size, varying the mean luminance of the target, and inserting spherical lenses of various optical diopters in front of the eye.After topical administration of pilocarpine (1%) the following changes in the pattern electroretinogram were observed: (i) a decrease of the pupillary diameter leading to a lowered target luminance, which produced attenuation of PERG amplitudes and prolonged latencies, and (ii) defocusing by accommodation of the crystalline lens, which produced attenuation of PERG amplitudes no effect on latencies.     

Effect of pilocarpine in treatment of intraocular pressure elevation following neodymium: YAG laser posterior capsulotomy

A prospective study was conducted in 30 eyes of 30 patients to determine if pilocarpine would prevent increased intraocular pressure following Q-switched neodymium (Nd):YAG laser posterior capsulotomy. Fifteen eyes were given pilocarpine 4%, immediately following laser therapy and every hour until bedtime. Fifteen eyes served as untreated controls. Our results show that without prophylactic therapy, 10 of 15 eyes (67%) had a post-laser intraocular pressure (IOP) elevation of greater than 10 mmHg, while only one of 15 (6.6%) of the pilocarpine-treated eyes had a rise of that magnitude. The facility of outflow was reduced by 42% in the untreated eyes in contrast to an increase of 3% in those eyes treated with pilocarpine. Thus, pilocarpine 4% is effective in reducing the incidence and magnitude of elevated IOP following Nd:YAG posterior capsulotomy.     

Ultrasound biomicroscopic morphometry of the anterior eye segment before and after one drop of pilocarpine

Purpose: To measure anterior eye segment morphometric data using ultrasound biomicroscopy. This is a new high-frequency, high-resolution ultrasound method enabling the visualisation of the anterior segment of the living eye with magnification similar to a light microscope. Methods: Thirteen morphometric parameters of the anterior eye segment were measured before and after the application of one drop of pilocarpine in 10 eyes of 5 persons, using a Zeiss-Humphrey Ultrasound Biomicroscope at a frequency of 50 MHz. In each session, 3 morphometric parameters in the central images (corneal thickness, anterior chamber depth, pupillary diameter) were measured 4 times, and 10 parameters in the radial images (scleral thickness, angle-opening distance, trabecular-iris angle, trabecular-ciliary process distance [TCPD], iris thickness 1, 2 and 3, iris-ciliary process distance, iris-lens contact distance [ILCD], iris elevation) were measured on the 3, 6 and 9 o'clock meridians three times each. Results: Statistically significant changes were noted in the following parameters: pupillary diameter, iris thickness 1 and 2, and TCPD were decreased, while ILCD was increased after pilocarpine. Wide chamber angles showed a tendency to become narrower and narrow ones to become wider after pilocarpine. Conclusion: One drop of pilocarpine caused significant changes in the anterior eye segment morphology. Not only the pupillary diameter decreased but iris thickness and trabecular-ciliary process distance were also decreased simultaneously. At the same time the contact surface between the lens and iris increased significantly. Ultrasound biomicroscopy gives new morphometric image information about the anterior eye segment which is not available using conventional gonioscopy or ophthalmic echography.Abbreviations ACD anterior chamber depth - AOD500 angle-opening distance - CD corneal thickness - Fi1 trabecular-iris angle - ICPD iris-ciliary process distance - ID1, ID2 and ID3 iris thickness 1, 2 and 3 - IE iris elevation - ILCD iris-lens contact distance - PD pupillary diameter - SD scleral thickness - TCPD trabecular-ciliary process distance     

Controlled Delivery of Pilocarpine. 1. In Vitro Characterization of Gelfoam® Matrices

The potential of Gelfoam absorbable gelatin sponge as a carrier for ophthalmic delivery of pilocarpine was examined. Prolonged in vitro release of pilocarpine was achieved through pharmaceutical modification of the device by embedding a retardant in the pores. The device embedded with cetyl ester wax released pilocarpine in a zero-order pattern (release exponent = 0.93 ± 0.04) for up to 5 hr. This result corresponded well with a linear penetrant uptake by this device. The device impregnated with polyethylene glycol 400 mono-stearate exhibited anomalous drug transport with a release exponent of 0.63 ± 0.02. The absorption of water by this retardant and the formation of a gel layer on the surface slowed the penetration of the release medium into the deeper sections of the matrix, as well as the rapid outward diffusion of drug, resulting in a prolonged release of pilocarpine.