International journal of clinical pharmacology, therapy, and toxicology最新文献_第4页

Lack of effect of cimetidine on furosemide kinetics and dynamics in patients with hepatic cirrhosis. 西咪替丁对肝硬化患者呋塞米动力学和动力学的影响尚缺乏。

International journal of clinical pharmacology, therapy, and toxicology Pub Date : 1993-09-01

A Sanchis Closa, C Lambert, P du Souich

{"title":"Lack of effect of cimetidine on furosemide kinetics and dynamics in patients with hepatic cirrhosis.","authors":"A Sanchis Closa, C Lambert, P du Souich","doi":"","DOIUrl":"","url":null,"abstract":"The influence of cimetidine on the natriuretic and diuretic responses to furosemide was studied in 10 patients with hepatic cirrhosis. After four days on a low sodium diet, the patients were given 40 mg of furosemide i.v. and from the sixth to the eleventh day they received 400 mg of cimetidine p.o. every 6 h and a second dose of furosemide with the last 6 h dose. Ten healthy subjects received the same dose of furosemide. Multiple blood and urine samples from both groups were analyzed for furosemide, sodium and creatinine. Furosemide kinetics were not affected in patients with hepatic cirrhosis but the effect was lower than in the controls: urinary excretion of sodium (0.47 +/- 0.07 vs 1.59 +/- 0.10 mmol/min, p < 0.05) and urine excretion (4.86 +/- 0.57 vs 9.16 +/- 0.85 ml/min, p < 0.05). The predicted maximal effect of furosemide (Emax) and the furosemide urinary rate of excretion needed to elicit 50% of Emax for the cirrhotic patients and the controls were 1.85 +/- 0.21 and 3.22 +/- 0.41 mmol/min (p < 0.05) and 137 +/- 15 and 99 +/- 12 micrograms/min (p < 0.05), respectively. The amounts of sodium filtered (FNa) and reabsorbed in response to the injection of furosemide were lower in the cirrhotic patients than in the controls, however, relative to the FNa, the cirrhotic patients reabsorbed more sodium than the controls. The administration of cimetidine did not affect the kinetics of furosemide nor its natriuretic or diuretic responses.(ABSTRACT TRUNCATED AT 250 WORDS)","PeriodicalId":13817,"journal":{"name":"International journal of clinical pharmacology, therapy, and toxicology","volume":"31 9","pages":"461-6"},"PeriodicalIF":0.0,"publicationDate":"1993-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"19215131","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Assessing the risk of ovulation in interaction studies of drugs and oral contraceptives. 评估药物和口服避孕药相互作用研究中的排卵风险。

International journal of clinical pharmacology, therapy, and toxicology Pub Date : 1993-09-01

N de la Rey, R Schall, H G Luus, B H Meyer, F O Müller

引用次数: 0

Design and pharmacodynamic evaluation of novel dual release formulations of triazolam. 新型三唑安定双释放制剂的设计与药效学评价。

International journal of clinical pharmacology, therapy, and toxicology Pub Date : 1993-09-01

R B Smith, P D Kroboth, M M Folan, F J Kroboth, T W Rosanske

{"title":"Design and pharmacodynamic evaluation of novel dual release formulations of triazolam.","authors":"R B Smith, P D Kroboth, M M Folan, F J Kroboth, T W Rosanske","doi":"","DOIUrl":"","url":null,"abstract":"Triazolam is an effective hypnotic that can cause amnesia and psychomotor performance decrements, particularly after a 0.5 mg dose. Previous pharmacodynamic studies suggested a relationship between these effects and triazolam plasma concentration. A novel dual release bilayer tablet was designed to mimic the onset of action of a 0.25 mg dose and to maintain the duration of a 0.5 mg dose without the side effects associated with the 0.5 mg dose. The immediate release component of the bilayer tablet contained 0.25 mg triazolam while the sustained release component contained 0.15 mg triazolam. Two prototype formulations of the bilayer tablet, differing in rate of release in the sustained release component, were tested against a conventional 0.5 mg triazolam compressed tablet and placebo in a single-dose, double-blind, four-way crossover study in healthy male subjects. Triazolam plasma concentration time profile was obtained over 12 hours following single administration of each treatment. Effects of triazolam on central nervous system function were evaluated using psychomotor performance tests, immediate and delayed recall tests and rating of sedation. The triazolam plasma concentrations were not significantly different among the active drug treatments, although the dual release tablets did give the expected profiles. There were significant differences in triazolam effects on memory and psychomotor performance. The slowest releasing dual-release tablet showed significantly less psychomotor impairment and memory deficit than the conventional tablet. There was no difference in sedation among the active drug treatments.(ABSTRACT TRUNCATED AT 250 WORDS)","PeriodicalId":13817,"journal":{"name":"International journal of clinical pharmacology, therapy, and toxicology","volume":"31 9","pages":"422-9"},"PeriodicalIF":0.0,"publicationDate":"1993-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"19214501","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Transdermal nicotine substitution: pharmacokinetics of nicotine and cotinine. 经皮尼古丁替代:尼古丁和可替宁的药代动力学。

International journal of clinical pharmacology, therapy, and toxicology Pub Date : 1993-09-01

B Keller-Stanislawski, S Caspary, P G Merz, R Bonn, M Wolff, N Rietbrock

引用次数: 0

Drug-prescription in the five new federal lands--a comparison with the prescription of the old federal lands of Germany. 五个新联邦土地的药物处方——与德国旧联邦土地处方的比较。

International journal of clinical pharmacology, therapy, and toxicology Pub Date : 1993-08-01

K O Haustein

引用次数: 0

Cutaneous and ocular changes associated with the use of chlorpromazine. 与氯丙嗪使用相关的皮肤和眼部变化。

International journal of clinical pharmacology, therapy, and toxicology Pub Date : 1993-08-01

M E Wolf, S Richer, M A Berk, A D Mosnaim

引用次数: 0

Dextromethorphan O-demethylation and dextrorphan glucuronidation in a French population. 法国人群右美沙芬o -去甲基化和右美沙芬葡糖醛酸化。

International journal of clinical pharmacology, therapy, and toxicology Pub Date : 1993-08-01

J C Duché, V Quérol-Ferrer, J Barré, M Mésangeau, J P Tillement

{"title":"Dextromethorphan O-demethylation and dextrorphan glucuronidation in a French population.","authors":"J C Duché, V Quérol-Ferrer, J Barré, M Mésangeau, J P Tillement","doi":"","DOIUrl":"","url":null,"abstract":"The dextromethorphan (DMP) O-demethylation and the dextrorphan (DRP) glucuronidation distributions were studied in 120 French Caucasian subjects. After a single 25 mg DMP oral administration, DMP, free and total DRP concentrations were measured in 8h-urine collection, using an HPLC technique with fluorescent detection. The DMP and free DRP concentrations ratio, in log form, was used to estimate the oxidative demethylation phenotype of the subjects. Two different populations were found. The first one consisted of the extensive metabolizers (90.8%, 95% confidence interval from 85.6 to 95.9%) and the second one consisted of poor metabolizers (9.2%, 95% confidence interval from 4.0 to 14.4%). The antimode value of the distribution was estimated at approximately 0.7 corresponding to a ratio of 5. Moreover, this ratio was compared to the DMP and total DRP concentrations ratio, usually defined to DMP O-demethylation phenotyping. On the other hand, the glucuronide DRP concentration was calculated by subtracting the free DRP concentration from the total DRP concentration. Consequently, the free DRP and glucuronide DRP concentrations ratio was also used to estimate the DRP glucuronidation in the present population. This ratio in log form reflected the UDP-glucuronyltransferase(s) capacity(ies). This log ratio appeared to be normally distributed in the population studied. These results show that log DMP/free DRP ratio can be used, as well as log DMP/total DRP ratio, to determine the oxidative phenotype of subjects and that the DRP conjugation does not exhibit any apparent genetic polymorphism.","PeriodicalId":13817,"journal":{"name":"International journal of clinical pharmacology, therapy, and toxicology","volume":"31 8","pages":"392-8"},"PeriodicalIF":0.0,"publicationDate":"1993-08-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"19215828","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

A comparative bioavailability study on two sustained-release formulations of diclofenac sodium following a single dose administration. 双氯芬酸钠两种缓释制剂单次给药后的生物利用度比较研究。

International journal of clinical pharmacology, therapy, and toxicology Pub Date : 1993-08-01

M M Hasan, N M Najib, H Muti

{"title":"A comparative bioavailability study on two sustained-release formulations of diclofenac sodium following a single dose administration.","authors":"M M Hasan, N M Najib, H Muti","doi":"","DOIUrl":"","url":null,"abstract":"A single dose comparative bioavailability study and an in vitro evaluation were conducted on two sustained-release formulations of diclofenac sodium (Voltaren \"V\" and Diclogesic \"D\"). The two products were found similar in weight and content uniformity. The in vitro dissolution, however, revealed that product D has a significantly faster rate of drug release compared to product V. The bioavailability study was carried out on 15 healthy male volunteers, who received a single oral dose (100 mg tablet) of each product according to a randomized crossover design. Blood samples were obtained over a 12 h period, and drug concentrations were determined by an HPLC assay. The two products were not found to be statistically different with respect to the lag time between dosing and appearance of the drug in the serum (0.8 +/- 0.2 and 0.6 +/- 0.1 h for V and D, respectively), or in the time needed to attain the peak concentrations (4.5 +/- 0.8 and 4.1 +/- 0.9 h for V and D, respectively). The two products, however, varied in the peak serum concentration (736 +/- 125 and 536 +/- 63 ng.ml-1 for V and D, respectively), but this difference was not statistically significance. In terms of the extent of absorption, assessed by estimating the area under the concentration-time curve over 12 h, the two products were not significantly different (3,340 +/- 270 and 3,045 +/- 294 ng.h.ml-1 for V and D, respectively). These in vitro and in vivo findings indicate that Diclogesic is characterized by sustained-release properties which are comparable to Voltaren.","PeriodicalId":13817,"journal":{"name":"International journal of clinical pharmacology, therapy, and toxicology","volume":"31 8","pages":"387-91"},"PeriodicalIF":0.0,"publicationDate":"1993-08-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"19215826","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Effects of dopaminergic antagonists on dopamine-induced cardiovascular and insulin secretion actions in hypertensive patients. 多巴胺能拮抗剂对高血压患者多巴胺诱导的心血管和胰岛素分泌的影响。

International journal of clinical pharmacology, therapy, and toxicology Pub Date : 1993-08-01

P Forte, G Martin, A Luchsinger, O Hernandez, E Romero, M Velasco

{"title":"Effects of dopaminergic antagonists on dopamine-induced cardiovascular and insulin secretion actions in hypertensive patients.","authors":"P Forte, G Martin, A Luchsinger, O Hernandez, E Romero, M Velasco","doi":"","DOIUrl":"","url":null,"abstract":"A comparative study between two dopaminergic antagonists: metoclopramide and domperidone, was undertaken in nineteen (19) hypertensive patients at the Vargas Hospital, Caracas. The patients were pretreated with labetalol, 800-1,200 mg/day, orally, over a period of one week, after which they were divided into two groups: group A, a total of eleven patients were intravenously infused with dopamine hydrochloride 0.5-3 micrograms/kg/min, before and after treatment with metoclopramide (10 mg, i.v. as a bolus); group B (n = 8), was pretreated with domperidone, 20 mg b.i.d., p.o. over a period of one week and intravenously infused with dopamine hydrochloride, 0.5-3 micrograms/kg/min. In group A, dopamine induced a decrease of blood pressure from 171.9 +/- 6.35/103.6 +/- 3.12 to 152.7 +/- 7.55/93.8 +/- 2.97 mmHg (p < 0.001) without altering heart rate, and it increased plasma insulin levels from 8.29 +/- 0.70 microunits/ml to 12.09 +/- 1.83 microunits/ml (p < 0.01). Metoclopramide caused no changes of blood pressure or plasma insulin levels. However, hypotensive responses and plasma insulin rises due to dopamine were blocked by metoclopramide. In group B, domperidone also blocked dopamine-induced antihypertensive effect (from 170.0 +/- 9.23/102.8 +/- 3.80 to 160.2 +/- 9.84/95.5 +/- 2.50 mmHg) although it was less effective than metoclopramide. Domperidone also blocked dopamine-induced increase of plasma insulin levels from 9.65 +/- 4.50 microunits/ml to 11.78 microunits/ml. We conclude that a dopaminergic receptor may be involved in some cardiovascular responses and in modulating insulin secretion in man.","PeriodicalId":13817,"journal":{"name":"International journal of clinical pharmacology, therapy, and toxicology","volume":"31 8","pages":"404-6"},"PeriodicalIF":0.0,"publicationDate":"1993-08-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"19214498","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Pharmacokinetics of intravenous ataprost alfadex, a new prostaglandin I2 analog in healthy volunteers. 新型前列腺素I2类似物阿他前列素在健康志愿者体内的药代动力学。

International journal of clinical pharmacology, therapy, and toxicology Pub Date : 1993-08-01

T Uematsu, K Umemura, M Nakano, K Kosuge, M Nakashima

引用次数: 0