类视黄素与癌

类视黄素(人工合成维甲酸类仿制品——译注)在皮肤科已得到广泛的应用。目前,用类视黄素预防和治疗皮肤癌及体内其它肿瘤也取得一定效果。近来发现类视黄素可以使鳞状化生的上皮逆转,为癌的化学药物预防提供了证据。临床应用证明,类视黄素及其衍生物诸如Etretinate、Arotionoids等治疗皮肤病及皮肤肿瘤收到了比维甲酸更为良好的效果。     

合理应用维甲酸类药物减轻不良反应

维甲酸类系列药物有较强的角质剥脱作用 ,可抑制皮肤滞留性角化过度 ,防止新的阻塞和炎症性损害的形成。主要用于治疗角化异常性皮肤病、色素性疾病、痤疮、脂溢性皮肤病。尤对治疗痤疮等有显著疗效。痤疮是一种常见皮肤病 ,青少年人群发病率高达 80 % ,可持续数年 ,不及时治疗 ,可导致瘢痕 ,影响外貌而给患者带来苦恼 ,临床迫切需要满意的治疗药物。维甲酸类的发现被认为是药物发展史上的一个里程碑 ,但它的致胚胎毒性和致畸性一直受到关注。因为这类药物的所有活性化合物都是强致畸原 ,而且对人及所有实验动物都不例外 ;外用维甲酸类药物…     

合理应用维甲酸类药物 减轻不良反应

维甲酸类系列药物有较强的角质剥脱作用，可抑制皮肤滞留性角化过度，防止新的阻塞和炎症性损害的形成。主要用于治疗角化异常性皮肤病、色素性疾病、痤疮、脂溢性皮肤病。尤对治疗痤疮等有显著疗效。     

复方维A酸霜的研制与临床应用

复方维A酸霜剂,既保持了维A酸对多种皮肤病的疗效,又可降低维A酸的副作用,对于常见多发的皮肤病(痤疮类皮肤病,角化性皮肤病,球菌性皮肤病)疗效较显著。1 配制方法     

维甲酸类药物治疗皮肤病临床应用

近几年来对维甲酸类药物治疗皮肤病的研究取得了很大的进展，研究发现该类药物可用于治疗多种皮肤病，包括脓疱型银屑病、寻常型银屑病、胶样婴儿、顽固性扁平疣、痤疮、口腔扁平苔藓、皮肤T细胞淋巴瘤、联合甲硝唑治疗毛囊虫病等。本文综述了维甲酸类药物治疗皮肤病的临床研究，为一些皮肤病的治疗提供用药参考。     

异维甲酸治疗3种皮肤病的回顾性分析

目的:探讨异维甲酸治疗3种皮肤病的临床疗效。方法:689入选病例口服异维甲酸,1个月为1疗程,观察1～3个月。结果:异维甲酸对痤疮、酒渣鼻、角化异常性遗传性皮病都有满意疗效,总有效率为74.36%～80.40%。结论:异维甲酸应用于门诊皮肤科对多种皮肤病见效快、疗效高,不失为一种方便、安全、前景看好的药物。     

维甲酸对实验性大肠癌的逆转治疗作用

目的;观察维甲酸(RA)对实验性大肠癌的逆转治疗作用。方法:应用维甲酸对大鼠大肠癌的诱发过程进行干预治疗,观察癌变率及增殖细胞核抗原(PCNA)和核仁组成区嗜银蛋白(AgNOR)的表达。结果:维甲酸治疗组(Ⅱ组)大肠癌的发生率显著低于未加维甲酸治疗的对照组(Ⅰ组)。在诱癌的中晚期PCNA指数及AgNOR数亦显著低于Ⅰ组(P<0.01)。Ⅰ、Ⅱ组的PCNA指数及AgNOR数显著高于未用诱癌剂的Ⅲ、Ⅳ组(P<0.01)。组内对比结果显示,Ⅰ组PCNA指数及AgNOR数有随着诱癌时间延长而增加的趋势,差异有显著性(P<0.05),而Ⅱ、Ⅲ、Ⅳ组内比较差异无显著性(P>0.05)。结论:维甲酸可完全或部分阻逆实验性大肠癌的癌变过程,降低其发生率,为临床应用维甲酸防治大肠癌提供了理论资料。     

克痤隐酮凝胶治疗寻常痤疮疗效观察

寻常痤疮是皮肤科的常见损美性皮肤病之一,因长期不愈易给患者带来严重的精神和心理负担,因此寻求一种安全有效、使用方便的外用药物阻止其继续发展是至关重要的.我科外用克痤隐酮凝胶治疗轻中度寻常痤疮,并与外用0.025%维A酸乳膏对照,现归纳总结如下.     

迪维霜治疗痤疮100例疗效观察

痤疮俗称“青春痘” ,是一种毛囊皮脂腺及导管慢性皮肤病 ,好发于青年男女 ,发病率较高 ,严重影响病人容貌。目前 ,国内治疗痤疮的外用药品虽然不少 ,但尚不尽人意。 2 0 0 1年元月以来 ,我科使用重庆华邦制药有限公司提供的外用药迪维霜 (0 1 %维A酸 )取得了令人满意的疗效 ,报告如下。1　资料与方法1 1　一般资料　1 0 0例痤疮患者均来自我院皮肤科门诊 ,其中男 5 6例 ,女 44例 ,年龄 1 4～ 3 2岁 ,病程 6个月至 8年。皮损分布以颜面部为主 ,部分颈项 ,上胸及背部受累。皮疹特点以炎性丘疹、脓疱、黑头粉刺为主 ,少数为结节及囊肿 ,随…     

维生素甲酸(维生素A酸)

【作用特点】维生素甲酸(简称维甲酸、维A酸)系多种用途的防治角化异常类皮肤、粘膜疾病的药物。维甲酸在生物体内是维生素甲(维甲醇)代谢的中间产物,主要影响骨的生长和上皮代谢。外涂维甲酸对皮肤穿透很快,能使表皮细胞置换明显地增加(7～8倍),在涂药三天后最明显,如继续涂药则逐渐减退。维甲酸治疗痤疮的机理是在于产生一种角化类型明显不同于“固位角化过度”的细胞、形成不粘     

Chronic oral administration of CG-3703, a thyrotropin releasing hormone analog, increases wake and decreases cataplexy in canine narcolepsy.

The effects on cataplexy and daytime sleep of acute and chronic oral administration of CG-3703, a potent TRH analog were assessed in canine narcolepsy. CG-3703 was found to be orally active and to reduce cataplexy (0.25 to 16 mg/kg) and sleep (8 and 16 mg/kg) in a dose-dependent manner. Two-week oral administration of CG-3703 (16 mg/kg) significantly reduced cataplexy and daytime sleep. The anticataplectic effects of CG-3703 were not associated with changes in general behavior, heart rate, blood pressure, rectal temperature, blood chemistry and thyroid function. Although drug tolerance for the effects on cataplexy and sleep were observed during the second week of chronic drug administration, therapeutic efficacy on cataplexy was improved with individual dose adjustment (final dose range: 16 to 28 mg/kg, p.o.). These results suggest that TRH analogs could be a promising new form of treatment for human narcolepsy.     

Residual effects of repeated doses of 0.5 and 1 mg flunitrazepam

Summary 9 normal subjects were tested on a large battery of tests the morning after a hypnotic dose of flunitrazepam (0.5 mg and 1 mg) and a placebo. Each drug was given for 8 nights and assessments were made 10 and 13 h later on days 1, 4 and 8. Self-ratings of sleep were made every morning. The tests comprised mood and bodily symptom self-ratings, tapping rate, visual reaction time, symbol copying and substitution tests, critical flicker fusion threshold, digit span and cancellation test. The EEG was recorded under eyes open and eyes closed conditions and analysed using broad waveband filters. Subjectively, the 0.5 mg dose was associated with increased alertness, contentment and calmness, the 1 mg dose with minimal decrease in alertness and contentment. Sleep onset was accelerated by flunitrazepam initially but effects on quality of sleep were not major due to subject selection. The 1 mg dose occasionally impaired performance on tapping, symbol copying and substitution and critical flicker fusion. The 0.5 mg dose marginally impaired symbold substitution and improved symbol copying. The EEG showed definite dose-related effects which tended to increase over the 8 nights of ingestion of the drug. It is concluded that whereas the 1 mg dose may sometimes be associated with definite residual effects the next day, the 0.5 mg dose possesses positive qualities in producing useful subjective effects the next day without appreciable impairment of psychological performance.     

Action of chronically administered antidepressants on the serotonergic postsynapse in a model of depression

A theory of excessive transmission of serotonin (5-HT) in depression has been previously proposed. The purpose of the present study was to test this theory further by using the model of depression in rats induced by L-5-hydroxytryptophan (5-HTP), the precursor of 5-HT. The drug effects on 5-HTP (25 mg/kg) induced behavioral depression were tested by chronic administration using methysergide which is a postsynaptic blocker of 5-HT, or by comparable clinical doses of antidepressant drugs. Methysergide (2 mg/kg) blocked 5-HTP induced depression on days 8 and 22 after initiation of medication by 70% and 83%, respectively. Among antidepressants, mianserin (2 mg/kg) was the first to produce an effect, displaying a 38% effect as early as 1 day after the start of medication and having blocking effects of 52% and 72% on days 8 and 22. Desipramine (5 mg/kg), doxepine (5 mg/kg), imipramine (5 mg/kg) and trazodone (10 mg/kg) showed no significant effect on days 1 and 8, and on day 22, 64, 36, 33 and 32% blocking, respectively. Amitriptyline had an initial effect of 41% at a dose of 10 mg/kg. Clomipramine (5 mg/kg), zimelidine (6 mg/kg) and chlorpromazine (2.5 mg/kg), which is a neuroleptic, showed no effect. Considering these results in light of recent data reported on the 5-HT synapse, it was suggested that 5-HTP induced depression may be induced by excessive transmission of 5-HT and that some antidepressant drugs may produce their effect by blocking this postsynaptic transmission. Based on these results, the mechanisms of human depression were discussed.     

Effects of chlordiazepoxide on depressed performance after reward reduction

Hungry rats were trained to lick either 4 or 32% sucrose solutions. When rats were shifted from the 32 to the 4% solution, depressed performance (relative to control groups) was observed. A single dose of chlordiazepoxide (8 mg/kg, i.p.) reversed the depression, but did not affect licking rates in control rats. When the drug was withdrawn, the depression reappeared. These data are discussed in terms of the possible effects of chlordiazepoxide on behavior that has been suppressed.     

Dose-independent pharmacokinetics of ondansetron in rats: contribution of hepatic and intestinal first-pass effects to low bioavailability

The pharmacokinetic parameters of ondansetron were evaluated after its intravenous (at doses of 1, 4, 8 and 20 mg/kg) and oral (4, 8 and 20 mg/kg) administration to rats. The gastric, intestinal and hepatic first-pass effects of ondansetron were also evaluated after its intravenous, oral, intraportal, intragastric and intraduodenal administration at a dose of 8 mg/kg to rats. After intravenous and oral administration of ondansetron, the drug exhibits dose-independent pharmacokinetics in rats. After oral administration of ondansetron at a dose of 8 mg/kg, the unabsorbed fraction was 0.0158 of the dose, the extent of absolute oral bioavailability (F) value was 0.0407, and the hepatic and intestinal first-pass effects were 40.0% and 34.2% of the oral dose, respectively. The low F of ondansetron in rats was mainly due to considerable hepatic and intestinal first-pass effects. The lower F of ondansetron in rats (4.07%) than that in humans (62+/-15%) was mainly due to greater hepatic metabolism of the drug in rats. Ondansetron was stable in the rat gastric juices and various buffer solutions having pHs ranging from 1 to 13. The equilibrium plasma-to-blood cells partition ratio of ondansetron was 1.74-5.31. Protein binding of ondansetron to fresh rat plasma was 53.2%.     

Experience in use of amoxicillin tablets for treatment of cases mostly of acute tympanitis (author's transl)

Amoxicillin tablets (50 mg (potency)/tablet) were administered to 14 cases of acute tympanitis and one case of acute tonsillitis, and the following results were obtained. (1) Of 15 cases in total, 3 cases were remarkably improved, 11 improved, and one not improved; that is, the effective rate was 93%. (2) Acute simple tympanitis: 6 cases, effective rate 100%. Acute suppurative tympanitis: 8 cases, effective rate 88%. Acute tonsillitis: 1 case, improved. (3) There was one case of diarrhea which appeared to be a side effect of this drug.     

尼美舒利治疗骨关节炎和类风湿关节炎的临床疗效

目的：了解尼美舒利治疗骨关节炎（ＯＡ）及类风湿关节炎（ＲＡ）的疗效及副作用。方法：尼美舒利组：ＯＡ和ＲＡ各３０例，予尼美舒利１００ｍｇ，ｐｏ，ｂｉｄ；对照组：ＯＡ和ＲＡ各３０例，予双氯芬酸２５ｍｇ，ｐｏ，ｔｉｄ，或萘普生２５０ｍｇ，ｐｏ，ｂｉｄ，观察４ｗｋ。结果：治疗前后２组病人各项临床指标均有明显改善；而实验室指标改善不明显（Ｐ＞０．０５）。２组总有效率分别是８８％和８５％，差别无显著意义；副作用发生率分别为３％和１３％，差别有显著意义（Ｐ＜０．０５）。结论：尼美舒利抗炎镇痛疗效肯定，副作用较少，是一种安全性较佳的非甾体类消炎止痛药。     

Comparative effects of long term treatment with etodolac, naproxen and ibuprofen on articular and bone changes associated with adjuvant arthritis in rats

The effect of prolonged treatment with etodolac (8 mg/kg) on the articular and bone pathology at the tibiotarsal joint associated with adjuvant arthritis in the rat has been studied and compared to the effects produced by treatment with naproxen (8 mg/kg) and ibuprofen (50 mg/kg). Drug effects were assessed by radiologic and histopathologic examinations. The effects on hindpaw edema, hindleg function, and body weight gain were also evaluated. Treatment was initiated on day 16 after adjuvant injection and continued for 28, 56 or 84 days. The degree of relapse which occurred after a 28 day period without treatment following 28 or 56 days of treatment was also assessed. Etodolac prevented the progression of the disease. Further, it appeared to diminish the incidence and severity of the lesions already present on day 16 before drug treatment began. All the parameters measured were improved and there was good agreement between the radiologic and histopathologic assessments of joint damage. At the doses used, the onset of drug activity was more rapid with etodolac than with either of the other two drugs. By comparison naproxen and ibuprofen inhibited the progression of joint damage, but neither drug consistently decreased the magnitude of the joint damage below that of day 16. With all three drugs there was less resurgence of disease symptoms when treatment was stopped after 56 days rather than 28 days of drug administration.     

Pharmacodynamics of the new H1-antagonist 3-amino-9,13b-dihydro-1H-dibenz[c,f]imidazo[1,5-a]azepine hydrochloride in volunteers

The inhibitory effects of 3-amino-9,13b-dihydro-1H-dibenz[1,5-a]azepine hydrochloride (WAL 801 CL), a new H1-receptor antagonist, on histamine-induced skin wheals were studied in 9 volunteers. The study was a double-blind, randomized (Latin square) change-over, intraindividual comparison of the effects of single doses of 2,6 and 18 mg WAL 801 CL and of placebo and 2 mg ketotifen on skin wheals induced by intradermal injections of 5 micrograms hystamine 1, 2, 4, 6 and 8 h after administration of the drugs. The injection of 5 micrograms was also made prior to each drug administration. The effects on psychological performance and the subjective state were also evaluated. The following tests were employed: simple visual reaction time (RT), critical flicker fusion frequency (C3F) and von Zerssen's self-rating scale Bf-S, assessing state of mood. There was a washout period of at least 72 h between each course of treatment. A decrease in the size of the histamine wheal was observed 1 h after WAL 801 CL and was maintained for at least 8 h. The reduction in the size of the histamine wheal was between 44% (2.0 mg) and 71% (18.0 mg). After ketotifen a marked decrease in the wheal area was observed between 4 and 8 h after administration of the drug, with maximum histamine antagonism of 59% after 6 h. The inhibitory effects of 6 and 18 mg WAL 801 CL and 2 mg ketotifen were statistically significant compared with placebo. 8 of 9 subjects felt tired (subjective report) after ketotifen, corresponding changes could be detected by Zerssen's state of mood scale Bf-S, but not by other psychological performance measures (RT, C3F).(ABSTRACT TRUNCATED AT 250 WORDS)     

Antipyretic, analgesic and anti-inflammatory activities of ketoprofen beta-cyclodextrin inclusion complexes in animals

Ketoprofen is a nonsteroidal anti-inflammatory drug (NSAID) orally effective in treating fever, pain, and inflammation but gastrointestinal side effects were observed. Preparation of ketoprofen beta-cyclodextrin inclusion complexes was to increase the solubility and reduce the irritation. The complexes were prepared and preliminarily confirmed using X-ray diffraction and dissolution test. Antipyretic, analgesic and anti-inflammatory models were induced by 10% yeast using rabbits, 0.8% acetic acid using mice and 1% carrageenin using rats, respectively. Results showed that the dissolution rate of ketoprofen was significantly improved by complexation. X-Ray diffraction pattern of the complexes exhibited a diffuse pattern that differed from that of physical mixture of ketoprofen and beta-cyclodextrin. Ketoprofen markedly inhibited the fever reactions at a single dose of 2 mg/kg as follows: 64.53% (inhibition rate %) at 1 h for ketoprofen, 73.04% at 1 h for ketoprofen beta-cyclodextrin inclusion complexes, respectively. Alleviating pain reaction rates following a single dose of 8 mg/kg at 20 min were 39.25% for the inclusion complexes and 26.72% for ketoprofen, respectively. Inhibition rates to rat edema following a single dose of 5 mg/kg at 1 h were 39.47% for the inclusion complexes and 23.86% for ketoprofen. Results for antipyretic, analgesic and anti-inflammatory activities showed that the rapid and stronger effects were found in the treatment group of ketoprofen beta-cyclodextrin inclusion complexes in comparison with those of free ketoprofen.