{"title":"Time dependent changes in the pharmacokinetics of aspirin.","authors":"A Markiewicz, K Semenowicz","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>In an experiment carried out on six volunteers, measurement of total serum salicylate concentration was used to describe aspirin kinetics after a single 1500 mg oral dose. The availability of the drug was significantly better when it was administered at 6(00) than at 18(00) or 22(00). Also a significant time-dependence was found between the morning and evening values of both the serum half-life time of salicylate and kel. The possible relation between these results and the appearance of undesirable side effects in patients should be examined.</p>","PeriodicalId":75937,"journal":{"name":"International journal of clinical pharmacology and biopharmacy","volume":"17 10","pages":"409-11"},"PeriodicalIF":0.0,"publicationDate":"1979-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"11777471","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}
{"title":"Interindividual differences of protein binding in man.","authors":"H Walther, F P Meyer","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>Using equilibrium dialysis protein unbound fractions of phenytoin (390 patients) and phenobarbital (220 patients) revealed serum protein bindings of 8 to 40 per cent and 25 to 80 per cent, respectively. For the purpose of therapy service, this pronounced interindividual variability required in the case of a great number of patients the determination of the extent of protein binding so as to exactly evaluate therapeutical failures or occurrence of undesirable effects.</p>","PeriodicalId":75937,"journal":{"name":"International journal of clinical pharmacology and biopharmacy","volume":"17 10","pages":"392-5"},"PeriodicalIF":0.0,"publicationDate":"1979-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"11704560","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}
B Magnani, E Ambrosioni, F Tartagni, L Pasetti, G Melandri
{"title":"Total body potassium and long-term treatment with amiloride HCL and/or hydrochlorothiazide.","authors":"B Magnani, E Ambrosioni, F Tartagni, L Pasetti, G Melandri","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>The potassium sparing effect of 5 mg of amiloride (A) given either alone, or in combination with 50 mg of hydrochlorothiazide (HCTH) was evaluated in 23 patients with essential hypertension on a daily diet containing 70 mEq of K and 130 mEq of Na. Two studies were carried out. In the first, patients received HCTH alone (2 months) followed by A alone (2 months) and the two combined (6 months). The results of this study demonstrate that A is capable of correcting and preventing the loss of serum and total body potassium (TBK) and of reducing the increase of serum uric acid induced by HCTH. In the second study, each patient received from the beginning A + HCTH for 12 months; no statistically significant changes for serum and total body potassium and for serum uric acid appeared in any patient after six and twelve months. This study proves that A is capable of clinical potassium sparing effect in hypertensives and that this effect is a long lasting one.</p>","PeriodicalId":75937,"journal":{"name":"International journal of clinical pharmacology and biopharmacy","volume":"17 10","pages":"404-8"},"PeriodicalIF":0.0,"publicationDate":"1979-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"11705426","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}
P van Brummelen, F R Bühler, W Kiowski, P Bolli, O Bertel
{"title":"Antihypertensive efficacy of a new long acting hydralazine like vasodilator, ISF 2469 in combination with a betablocker and a diuretic.","authors":"P van Brummelen, F R Bühler, W Kiowski, P Bolli, O Bertel","doi":"","DOIUrl":"","url":null,"abstract":"","PeriodicalId":75937,"journal":{"name":"International journal of clinical pharmacology and biopharmacy","volume":"17 10","pages":"380-5"},"PeriodicalIF":0.0,"publicationDate":"1979-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"11263267","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}
{"title":"The effect of gastro-intestinal filling on the absorption of sulfametoxydiazine.","authors":"S Kaumeier, E Kisslinger, A Neiss","doi":"","DOIUrl":"","url":null,"abstract":"","PeriodicalId":75937,"journal":{"name":"International journal of clinical pharmacology and biopharmacy","volume":"17 10","pages":"412-5"},"PeriodicalIF":0.0,"publicationDate":"1979-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"11705427","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}
{"title":"Improvement of the quantitative determination of verapamil in human plasma.","authors":"K Nelson, B G Woodcock, R Kirsten","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>An improvement in the extraction procedure for the quantitative determination of verapamil in human plasma is described. The advantages are: 1. the time involved in the extraction procedure is only 1/3 of that in the original method allowing the extraction of 100 samples in a working day. 2. increased mean recovery from 67% to 85% over the range of 3--90 ng verapamil/ml plasma. 3. less expenditure a) use of cheap plastic tubes instead of stoppered glass tubes. b) 1/2 the amount of heptane required as compared to the original procedure. c) use of air instead of N2 for evaporation. The lower limit of detection is 3 ng/ml which is comparable to that for the original extraction procedure. Within-batch precision over the range of 9--90 ng/ml averages 5.8% and at the lower limit of detection 17.3%. Between-batch precision over the range of 9--90 ng/ml averages 8.5% and at the lower limit of detection 19.7%. No significant difference could be found in the quantitative determination of verapamil in 27 plasma samples from patients undergoing verapamil treatment using the original and modified extraction procedures. This improvement of the extraction procedures simplifies the determination of verapamil and the only additional material required is liquid nitrogen or a suitable solvent cooled with dry ice.</p>","PeriodicalId":75937,"journal":{"name":"International journal of clinical pharmacology and biopharmacy","volume":"17 10","pages":"375-9"},"PeriodicalIF":0.0,"publicationDate":"1979-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"11704559","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}
{"title":"Comparison of hemodynamic effects induced by pentaformilgitoxin and deslanoside in patients with heart failure.","authors":"E Ambrosioni, F V Costa, D Bracchetti","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>The effect of pentaformilgitoxin and deslanoside on heart rate, blood pressure and cardiac output was compared in six patients with heart failure. Pentaformilgitoxin caused an increase of cardiac output from 3361 ml/min to 4183 ml/min (p less than 0.01). Deslanoside induced a non significant increase of cardiac output from 3617 to 3848 ml/min. Heart rate decreased significantly by both drugs: the reduction was greater after deslanoside (from 93.7 to 77.5 beats/min) than after pentaformilgitoxin (from 92 to 85 beats/min). Both drugs caused a comparable increase in stroke volume.</p>","PeriodicalId":75937,"journal":{"name":"International journal of clinical pharmacology and biopharmacy","volume":"17 10","pages":"416-20"},"PeriodicalIF":0.0,"publicationDate":"1979-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"11705428","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}
{"title":"The pharmacokinetics of the oral cephalosporins cefaclor, cephradine and cephalexin.","authors":"P G Welling, S Dean, A Selen, M J Kendall, R Wise","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>The pharmacokinetics of the oral cephalosporins cefaclor, cephradine, and cephalexin were examined following single 500 mg oral doses to fasted, healthy volunteers. Absorption of the three compounds was rapid following a brief lag period and peak serum levels were obtained in 1-1.5 hours. Serum levels of cefaclor tended to be lower than those of cephradine and cephalexin during the 2-5 hour postdosing period and cefaclor was eliminated more rapidly than other cephalosporins from serum. No difference was observed in the overall bioavailability of the three antibiotics based on comparable FD/V values. Urine levels of the three cephalosporins greatly exceeded the minimum inhibitory concentrations of susceptible organisms during 0-6 hours postdosing, but were considerably reduced during the 6-12 hour collection period. Total urinary recovery of antibiotic activity accounted for almost 90 percent of dosed cephradine and cephalexin compared to 55 percent of dosed cefaclor. Lower serum levels and reduced urinary recovery of intact cefaclor are probably due primarily to its chemical instability. The reduced levels of cefaclor may be compensated for therapeutically by its greater in vitro antibacterial activity.</p>","PeriodicalId":75937,"journal":{"name":"International journal of clinical pharmacology and biopharmacy","volume":"17 9","pages":"397-400"},"PeriodicalIF":0.0,"publicationDate":"1979-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"11705432","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}
{"title":"Side effects of antihypertensive drugs. Incidence and methods of collection.","authors":"F V Costa, E Ambrosioni, B Magnani","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>A prospective study has been carried out in two groups of hypertensive patients (482 inpatients followed during 2-3 weeks; 120 outpatients followed for 18 months) to evaluate the prevalence of side effects (SE) induced by antihypertensive drugs in current use. Only SE of definite or probable type as operatively defined were taken into consideration. SE were collected in different ways for inpatients and outpatients. Among 120 outpatients, 30 patients were randomly selected for cross over of placebo and drugs. Definite or probable SE were recorded in 236 (48.9%) of 482 patients: the prevalence of SE was below 20% both in single and multiple drug therapy. A prevalence greater than 20% was recorded in the outpatients. The placebo treatment demonstrated that many SE are not related to drug administration.</p>","PeriodicalId":75937,"journal":{"name":"International journal of clinical pharmacology and biopharmacy","volume":"17 9","pages":"405-9"},"PeriodicalIF":0.0,"publicationDate":"1979-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"11705434","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}
{"title":"Comparative bioavailability of sustained-release and conventional tablets of hydroxyethyltheophylline in man.","authors":"P L Sharma, R M Sharma","doi":"","DOIUrl":"","url":null,"abstract":"<p><p>The comparative bioavailability of sustained-release and conventional tablets of hydroxyethyltheophylline was studied in normal subjects. In a single dose study on 7 subjects, 3 conventional tablets or 2 sustained-release tablets were administered orally after a light breakfast and blood samples taken for 6 and 12 hours respectively. With conventional tablets the mean peak concentration (8.10 +/- 0.751 microgram/ml) was reached at 3 hours and concentrations less than 5 microgram/ml were observed in 4 out of 7 subjects at 6 hours. In contrast, with sustained-release tablets of theophylline and hydroxytheophylline complex the mean peak concentration (8.90 +/- 0.88 microgram/ml) was reached at 6 hours and levels above 5 microgram/ml were observed in 4 out of 7 cases at 12 hours. Administration of 2 sustained-release tablets twice a day produced trough plasma concentrations varying between 6.9-13.8 microgram/ml, i.e. within the therapeutic range in all the 5 subjects. It is concluded that this new oral sustained-release preparation provides therapeutic plasma theophylline concentration on a 12 hourly dosage schedule.</p>","PeriodicalId":75937,"journal":{"name":"International journal of clinical pharmacology and biopharmacy","volume":"17 9","pages":"394-6"},"PeriodicalIF":0.0,"publicationDate":"1979-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"11786593","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}