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The effects of drugs on enzyme systems 总被引:1,自引:0,他引:1
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Carbamazepine (5 H-dibenz (b, f) azepine-5-carboxamide), is an antiepileptic drug which is expected to be administered regularly over a substantial part of patients lifetime. As the gender focus in epilepsy the later years has primarily been on women, there certainly is a lack of studies focused on the effects particular to men. The present study was aimed to investigate its effects on germ cell's by employing the sperm morphology assay. Twelve groups of male wistar rats were treated with sterile water 0.5 ml, cyclophosphamide (CP) 20 mg/kg, carbamazepine 9, 18, 36 mg/kg (i.p) and 2% gumacasia 0.25 ml/100 g respectively for 5 consecutive days at intervals of 24 hrs. Following the last exposure, on days 14 and 35 sperm morphology assay was conducted as per the standard procedure. Mann-Whitney 'U' test was used for statistical analysis and the level of significance was P<0.01. Neither carbamazepine nor cyclophosphamide induced formation of abnormally shaped sperms at 14 day time interval. Whereas on day 35, with 18 mg/kg dose level of carbamazepine there was an increase in the number of sperms with heads defects (P<0.01); Whereas in the other two dose levels the number of abnormally shaped sperms had decreased. 2% gumacasia increased the number of sperms with tail defects at day 35. (Mann-Whitney 'U' test). CONCLUSION: Carbamazepine and 2% gumacasia could be germ cell mutagens and could cause infertility on prolonged use therefore further studies with serum drug level estimations are needed. 相似文献
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Immunosuppressive drugs are agents capable of suppressing the development of at least one type of immune responsein vivo at doses with minimal side-effects.After an introduction in which different types of immune responses are briefly discussed, some characteristics regarding the mechanism of action of prednisolone, azathioprine, cylophosphamide and anti-lymphocyte serum (ALS) will be reviewed. Corticosteroids display mainly an anti-inflammatory effect. The immunosuppressive effect of azathioprine is questionable, cyclophosphamide influences the immune system itself and ALS suppresses fairly specific cellular immunity. 相似文献
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1. The effects of a potential anti-Parkinson drug, benapryzine, have been compared with those of benzhexol, atropine and procaine on the excitatory responses induced by acetylcholine and L-glutamate on feline cortical neurones using the microiontophoretic technique.2. All the drugs tested reduced the excitatory responses evoked by acetylcholine and L-glutamate. However, benapryzine, benzhexol and procaine more effectively reduced the excitatory responses to L-glutamate than those to acetylcholine whereas atropine was more effective against acetylcholine-induced excitation.3. In the presence of procaine the amplitude of the extracellular spikes was decreased. This effect was also observed during applications of benapryzine and benzhexol.4. Tests on the isolated frog sciatic nerve indicated that benapryzine and benzhexol had local anaesthetic actions respectively greater than and equivalent to those of procaine.5. It was concluded that the effects of benapryzine and benzhexol on cortical neurones were probably related to their local anaesthetic properties. The possibility that a local anaesthetic action may account for the effects of these drugs and of many other commonly used anti-Parkinson drugs in Parkinson's disease is discussed. 相似文献
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认知功能是指接受、加工、储存和应用信息的能力.它是人们成功地完成各种活动最重要的心理条件.理解力、记忆力、注意力、学习能力、警觉和想象能力等均被认为是重要的认知能力[1].癫痫患儿的认知能力受癫痫发作、社会心理因素、抗癫痫药物(AEDs)等多种因素的影响.儿童较成人而言,由于大脑兴奋性和抑制性尚未达到平衡,更易罹患癫痫,且更易发生认知功能障碍.AEDs在减低致痫神经元兴奋性的同时亦降低了正常神经元的兴奋性,从而损伤认知功能. 相似文献
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Summary Mescaline, LSD-25, psilocybin, and a combination of these three drugs were each administered in moderate doses at 7-day intervals to 24 volunteer subjects according to a latin square design. Primary suggestibility, that type closely related to hypnosis, was measured both before and 2 hrs following each administration of drugs, using the 17-item Stanford Suggestibility Scale. A Trance Indicator Score was also obtained, representing both behavioral observations and subjective reports concerning the degree of trance-like or hypnotic-like experiences which may have accompanied each suggestibility testing session.Major findings were that mescaline, LSD-25, and the combination of drugs each produced an average enhancement in primary suggestibility closely comparable to that produced by an induction of hypnosis, the latter being tested for each subject after the completion of the drug series. Psilocybin did not enhance primary suggestibility. Associated trance phenomena were also substantially increased during all of the drug trials, but significantly less so for psilocybin. Significant correlations were obtained between suggestibility and Trance Indicator Scores following each drug and after induction of hypnosis, although psilocybin produced substantially less correlation.Although these results confirm speculations previously made in the literature that LSD-25 may increase suggestibility, it must be emphasized that they cannot be generalized beyond the specific type of suggestibility measured. Second, the differences between psilocybin and the other drugs on primary suggestibility restrict generalizations regarding the action of otherwise similar psychotomimetic drugs.Grateful appreciation is due Drs. Andre M. Weitzenhofffer, and Ernest R. Hilgard for their valuable assistance in the planning of this research, which in expanded form has been submitted to Stanford University as the senior author's Ph.D. dissertation and will be available from University Microfilms, Ann Arbor, Michigan. This study was supported in part by grant MH 03030 and was performed at Veterans Administration Hospital, Palo Alto, Calif. 相似文献
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认知功能是指接受、加工、储存和应用信息的能力。它是人们成功地完成各种活动最重要的心理条件。理解力、记忆力、注意力、学习能力、警觉和想象能力等均被认为是重要的认知能力。癫痫患儿的认知能力受癫痫发作、社会心理因素、抗癫痫药物(AEDs)等多种因素的影响。儿童较成人而言,由于大脑兴奋性和抑制性尚未达到平衡,更易罹患癫痫,且更易发生认知功能障碍。 相似文献
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Summary Many drugs affect tests of thyroid function through alterations in the synthesis, transport and metabolism of thyroid hormones, as well as via influences on thyrotrophin (TSH) synthesis and secretion. Despite effects on circulating thyroid hormone and TSH levels, few drugs result in important changes in clinical thyroid state, but difficulty in interpretation of thyroid function tests often results. Commonly prescribed drugs including anti-convulsants, non-steroidal anti-inflammatory drugs, beta-adrenoceptor antagonists, steroid hormones and heparin may result in abnormal thyroid function tests in the absence of clinical features of thyroid dysfunction. In contrast, lithium and iodine containing drugs, including radiographic contrast agents and amiodarone, may result rarely in overt thyroid disease. 相似文献
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Daily fluctuations of the behavioral and pharmacological effects of drugs of abuse such as cocaine, morphine or alcohol are observed for several years. Since the discovery of the molecular components of the biological clock, the so-called "clock genes", several studies have further confirmed the inter-relationship between drugs of abuse and biological rhythms. Indeed, drugs of abuse have been shown to clearly induce specific expression changes in clock genes depending on the brain area, the mode of administration or the specific clock gene. On the other hand, increasing evidence for a clear involvement of several clock genes in the development of several drug-induced behaviors has been shown. The present review summarizes these recent findings and reveals the complexity, as well as the specificity, of the interrelation between drugs of abuse and clock genes. 相似文献
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This study confirms the presence of α-adrenergic receptors, subserving contraction, and β-adrenergic receptors, subserving relaxation, in both the ampulla and isthmus portions of the oviduct of the anesthetized rabbit. The pressor response to phenylephrine and its contractile responses in the ampulla and isthmus were blocked by phentolamine. The increases in intra-luminal pressure over control levels did not differ significantly between isthmus and ampulla. Propranolol produced a qualitatively similar blockade of the inhibitory effects of isoprenaline on ampulla and isthmus as well as its vasodepressor effect. Angiotensin produced a contractile response in the oviduct that was reduced by phentolamine. 相似文献
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目的 探讨咖啡因对平阳霉素诱发人精子染色体畸变的影响。方法 人精子经平阳霉素(pinyangmycin,PYM)处理与去透明带地鼠卵受精,受精1h后加入咖啡因(caffeine,CAF)后处理,继而制备染色体进行结构畸变精子率依次为27%、40%、76%;断裂均数依次为0.72、1.92、4.36上述各组参数均高于空白对照组(8.0%、0.14),差异有非常显著意义(P〈0.01)。与CAF组和P 相似文献
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《General pharmacology》1995,26(1):1-31
- 1.1. The signal transduction process mediated by cyclic AMP that leads to the characteristic positive inotropic effect (PIE) in association with a positive lusitropic effect (acceleration of rate of twitch relaxation) has been well established. Relationships between accumulation of cyclic AMP, changes in intracellular Ca2+ transients and the PIE differ, however, depending on the mechanism of particular drugs that affect different steps in the metabolism of cyclic AMP. Selective partial agonists of β1-adrenoceptors and inhibitors of phosphodiesterase (PDE) III cause the accumulation of less cyclic AMP for a given PIE than does isoproterenol. In addition, in aequorin-microinjected canine ventricular muscle, selective inhibitors of PDE III, OPC 18790 and Org 9731, produced smaller decreases in the responsiveness of myofilaments to Ca2+ ions than isoproterenol, while a partial agonist of β1-adrenoceptors, denopamine, elicits a decrease in Ca2+ responsiveness of the same extent as does isoproterenol.
- 2.2. Activation of myocardial α1-adrenoceptors, as well as stimulation of receptors for endothelin and angiotensin II, which accelerates hydrolysis of phosphoinositide (PI) to result in production of inositol 1,4,5-trisphosphate (IP3) and diacylglycerol (DAG) are associated with very similar inotropic regulation: (1) the dependence on the species of animals of induction of the PIE; (2) an excellent correlation between the extent of acceleration of hydrolysis of PI and the PIE; (3) isometric contraction curves associated with a negative lusitropic effect; (4) the PIE associated with increases in myofibrillar responsiveness to Ca2+ ions; and (5) the selective inhibition of the PIE by an activator of protein kinase C (PKC), phorbol 12,13-dibutyrate (PDBu), with little effect on the PIE of isoproterenol and Bay k 8644.
- 3.3. A novel class of cardiotonic agents, namely, Ca2+ sensitizers such as EMD 53998 and Org 30029, act on the Ca2+-binding site of troponin C, increasing the affinity of these sites for Ca2+ ions, or at the actin-myosin interface to facilitate the cycling of cross-bridges. These agents produce a PIE with little change or decrease in Ca2+ transients and may bring about a significant breakthrough in the development of drugs for reversal of myocardial failure in the treatment of congestive heart failure.
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Timing behaviour was generated in rats by a schedule which required responses to be spaced at least 15 sec apart in order for them to produce food reinforcement (DRL 15 sec). The behaviour maintained by this schedule was then studied after administration of chlordiazepoxide, phenobarbitone and chlorpromazine. Several doses of both chlordiazepoxide and phenobarbitone were found to disrupt timing behaviour by increasing overall response rates although the highest dose of each of these two drugs produced sedative effects. Chlorpromazine produced mainly a decrease in overall response rates. Analysis of performance in terms of interresponse times (IRTs) showed that both chlordiazepoxide and phenobarbitone markedly increased the percentage of IRTs less than 1.5 sec in duration (response bursts). Chlorpromazine had no consistent effect on response bursts. Reduction of the animals' body weights from 85% to 75% of their pre-experimental levels had no effect on operant performance, suggesting that the effects of the drugs were probably not due to actions on motivational processes. 相似文献