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1. |
Comparative Double-Blind Multicentre Study of Single-Dose Pefloxacin and Amoxicillin Plus Probenecid for Treatment of Acute Uncomplicated Gonorrhoea |
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Drug Investigation,
Volume 2,
Issue 4,
1990,
Page 203-207
J. Dubois,
C. St-Pierre,
C. Olivier,
B. Clecner,
T.W. Austin,
R. Phillips,
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摘要:
In a double-blind, randomised multicentre study, 129 patients (92 males, 37 females) with culture proven acute uncomplicated genital gonorrhoea were given single oral doses of either pefloxacin 800mg (n = 65) or amoxicillin 3.0g plus probenecid 1.0g (n = 64). Data from 36 patients (19 pefloxacin and 17 amoxicillin plus probenecid) were not evaluable. All 146 strains ofNeisseria gonorrhoeaeisolated from evaluable patients were sensitive to pefloxacin whereas 139 of 146 were sensitive to penicillin (statistically significant at p < 0.05, binomial test).84% of gonococcal infections involved only a genital site whereas implication of other sites was observed in 11% of patients; 4% of the patients were asymptomatic carriers of infected participants. Cure (negative post-treatment culture) rates were 100% (65/65) in pefloxacin-treated patients and 94% (60/64) in the amoxicillin plus probenecid group: the 4 treatment failures were 3 men with positiveN. gonorrhoeaeurethral cultures and a woman with a positive throat culture. Postgonococcal urethritis was observed in 9 pefloxacin and 4 amoxicillin plus probenecid-treated patients. 18% of pefloxacin-treated patients and 15% of amoxicillin plus probenecid-treated patients presented drug-related adverse events consisting mainly of gastrointestinal (nausea, diarrhoea) or CNS (headache) disturbances of mild intensity. Two amoxicillin plus probenecid patients presented post-treatmentCandida albicansvaginitis requiring antifungal therapy. In conclusion, results from this study indicate that a single oral 800mg dose of pefloxacin can be considered as well tolerated and as effective as the amoxicillin plus probenecid combination for the treatment of acute uncomplicated gonorrhoea.
ISSN:0114-2402
出版商:ADIS
年代:1990
数据来源: ADIS
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2. |
Probucol Promotes Hepatic Uptake of High Density Lipoprotein in Rats |
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Drug Investigation,
Volume 2,
Issue 4,
1990,
Page 208-213
Koki Takata,
Itaru Horiuchi,
Makato Okahashi,
Hironori Tokumo,
Kazunori Koide,
Yasuhiko Hirata,
Goro Kajiyama,
Toshio Kawamoto,
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摘要:
Probucol significantly reduced high density lipoprotein (HDL)-cholesterol and apolipoprotein AI in rats. Hepatic uptake of radiolabelled human HDL3increased significantlyin vivoand in the isolated perfused rat liver preparation.In vivo,uptake of HDL3by the adrenal glands also increased significantly. Hepatic cholesterol content in probucol-treated rats tended to increase, whereas newly synthesised cholesterol decreased significantly. The results of the present study suggest that enhanced uptake of HDL is one of the mechanisms of lowering serum HDL with probucol treatment.
ISSN:0114-2402
出版商:ADIS
年代:1990
数据来源: ADIS
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3. |
Efficacy and Tolerability of 2 Combination Diuretics in the Treatment of Essential Hypertension |
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Drug Investigation,
Volume 2,
Issue 4,
1990,
Page 214-218
R.L. Lins,
A. Daelemans,
W. Hoff,
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摘要:
In a double-blind placebo-controlled randomised crossover study, the antihypertensive activity and tolerability of 2 combination preparations, containing a diuretic and a potassium-sparing agent, were evaluated in the treatment of essential hypertension. 20 patients with diastolic blood pressures between 95 and 120mm Hg were included, of whom 18 completed the study. Each combination, xipamide 10mg + triamterene 30mg or hydrochlorothiazide 50mg + amiloride 5mg, was administered for 6 weeks. Blood pressures and pulse rates were recorded before and after the washout phase and thereafter at 3-week intervals. Serum urea, creatinine, electrolytes, lipid concentrations and 24-hour urinary electrolyte excretion were monitored every 3 weeks. After 3 and even more after 6 weeks a significant reduction in blood pressure (more than 10mm Hg) was obtained with both combinations in 55 and 50% of patients, respectively. Only 3 patients showed a distinct reduction in serum potassium with one or both drugs (minimum 3.4 or 3.3 mmol/L). There was no marked change in total lipids, cholesterol or triglycerides.
ISSN:0114-2402
出版商:ADIS
年代:1990
数据来源: ADIS
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4. |
Depot-Protection Against &ggr;-Irradiation in Mice by Parenteral Glutathione-Polyvinylpyrrolidone Coprecipitates and Cellular Drug Uptake |
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Drug Investigation,
Volume 2,
Issue 4,
1990,
Page 219-224
D. Stefanova,
E. Gattavecchia,
E. Ferri,
A. Breccia,
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摘要:
Glutathione (GSH)-polyvinylpyrrolidone (PVP) coprecipitates in various GSH: PVP ratios, and PVP molecular weights were tested as radioprotectorsin vivoon mice andin vitroon Chinese hamster V79 cells.Highest depot protective effectiveness was obtained for 30CoGSH-1 in mice treated 24 and 48 hours before &ggr;-irradiation. Studies on the uptake of35S-GSH and35S-GSH-PVP showed that uptake strongly depends on the drug: PVP ratio, cell contact time and molecular weight of PVP, with a general inhibition of the influx of extracellular GSH.The results indicate that the complex is less penetrable, but more effective in bondage to cytoplasmic proteins and membrane with a consequent increase in radioprotection.
ISSN:0114-2402
出版商:ADIS
年代:1990
数据来源: ADIS
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5. |
Long Term Efficacy and Clinical Safety of Tianeptine in Depressed Alcoholic Patients after Alcohol Withdrawal |
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Drug Investigation,
Volume 2,
Issue 4,
1990,
Page 225-234
R. Malka,
H. Lôo,
H. Ganry,
C. Marey,
A. Kamoun,
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摘要:
A multicentre study was designed to treat patients presenting with a major depressive episode, single or recurrent, or dysthymic disorder with tianeptine for 1 year. 22% of these patients had a concurrent diagnosis of alcoholism. This intermediate analysis presents results obtained with the first 122 depressed alcoholic patients included, of which 63 were treated for 1 year. The results allow the evaluation of the long term efficacy and tolerability of tianeptine.The antidepressant activity of tianeptine was confirmed by an almost 50% reduction of initial Montgomery-Asberg depression rating scale scores after 1 month of treatment. Total scores and subscores of the Hamilton anxiety rating scale and Hopkins symptom checklist self-ratings improved concomitantly. Single item and factor scores of the checklist for assessment of somatic symptoms indicated improvement in complaints present at the beginning of the study and an absence of notable adverse effects, particularly of the anticholinergic type. Three patients took massive doses of tianeptine; despite the association with alcohol, these patients did not show marked adverse effects.These results indicate the potential of tianeptine as an antidepressant in alcoholic patients after withdrawal of alcohol, its long term efficacy, and its good tolerability in patients who are particularly susceptible to the adverse effects of psychotropic drugs. The drug does not provoke orthostatic hypotension or weight change.
ISSN:0114-2402
出版商:ADIS
年代:1990
数据来源: ADIS
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6. |
TheIn VitroEffects of Clindamycin on Polymorphonuclear Leucocyte FunctionA Reassessment |
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Drug Investigation,
Volume 2,
Issue 4,
1990,
Page 235-241
Antonio Arbo,
José Ignacio Santos,
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摘要:
Thein vitroeffects of clindamycin on polymorphonuclear leucocyte (PMN) chemotaxis, chemiluminescence and bacterial killing were evaluatedin vitro.PMNs from adult volunteers were incubated for 30 minutes with Hank's balanced salt solution containing clindamycin 2, 10, 100, and 1000 mg/L. Clindamycin was found to enhance the functional capacity of PMNs at a concentration of 2 mg/L, but not at higher concentrations. Previous studies have failed to show enhanced PMN function using high concentrations of clindamycin; these findings suggest that PMN function may be augmented using concentrations which can be readily attained using therapeutic doses of clindamycin.
ISSN:0114-2402
出版商:ADIS
年代:1990
数据来源: ADIS
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7. |
A Double-Blind Randomised Study of Metronidazole (Flagyl®) 1% Cream in the Treatment of Acne RosaceaA Placebo-Controlled Study |
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Drug Investigation,
Volume 2,
Issue 4,
1990,
Page 242-248
Antoine Bitar,
Jean Bourgouin,
Norman Doré,
Richard Dubuc,
Jean Mario Giroux,
Madeleine Landry,
Marie Christine Roy,
Andrée Mathieu-Serra,
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摘要:
A double-blind, placebo-controlled study was conducted with 100 adult patients presenting with acne rosacea. 50 patients were randomly assigned to treatment with metronidazole 1% cream, while the other 50 patients received placebo cream. The cream was applied morning and evening in a dose of 0.25 cm2per application. Clinical assessments were performed prior to drug administration and after 1 and 2 months of treatment.The number and severity of rosacea lesions (papules and pustules) were significantly reduced with both treatments during the first month, but the response was significantly greater with metronidazole 1% cream (p < 0.05). During the second month, lesion counts continued to decline with metronidazole 1% cream, but remained the same or worsened with placebo. Metronidazole was significantly better than placebo (p < 0.05).Lesions occurring at all facial sites (forehead, cheeks, chin, nose) responded to metronidazole cream. The most dramatic effect occurred on the forehead, where lesions were eradicated in 11 of 19 patients (58%). At other sites, metronidazole eradicated lesions in approximately 25% of the patients versus approximately 10% with placebo.Other symptoms of acne rosacea, such as erythema, erythrosis and telangiectasiae improved slightly, but there were no significant differences between treatments. Metronidazole 1% cream was well tolerated throughout the study, with no serious adverse effects or laboratory abnormalities.
ISSN:0114-2402
出版商:ADIS
年代:1990
数据来源: ADIS
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8. |
Topical 5′-Methylthioadenosine for the Treatment of Sports-Related Acute Soft-Tissue Injuries |
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Drug Investigation,
Volume 2,
Issue 4,
1990,
Page 249-254
B. Anselmi,
G.C. Caroli,
C.M. Costa,
G. Di Fraia,
E. Maggioni Moratti,
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摘要:
149 patients with acute soft-tissue injuries which occurred less than 24 hours prior to the entry into the trial were treated with topical 5′-methylthioadenosine (MTA) 0.5% 3 or 4 times a day in a multicentre open clinical trial. The injuries were divided into the following groups: contusion, sprain, tendinitis, epicondylitis, strain, other. MTA efficacy was evaluated on the basis of the changes observed in 4 clinical parameters: pain, redness, swelling, functional impairment, rated through a 100mm visual analogue scale. Clinical improvement (assessed as a decrease of greater than 50% in at least 2 of the 4 clinical parameter scores) was achieved in 11% of patients after 1 day, in 62% after 3 days of therapy and in 92% at the end of the trial. Tolerability was rated on a 4-point ordinal scale as ‘excellent’ in all cases both by investigators and patients. In conclusion, topical MTA may be proposed as an original, effective and well tolerated treatment for acute soft-tissue injuries.
ISSN:0114-2402
出版商:ADIS
年代:1990
数据来源: ADIS
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9. |
Pharmacokinetics of Omeprazole and Metabolites Following Single Intravenous and Oral Doses of 40 and 80mg |
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Drug Investigation,
Volume 2,
Issue 4,
1990,
Page 255-263
Tommy Andersson,
Carl-Gunnar Regårdh,
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摘要:
This study was performed to investigate the influence of dose on the kinetics of omeprazole and 2 main primary metabolites in plasma. 10 healthy subjects were given solutions of 40 and 80mg omeprazole, orally and intravenously on 4 different occasions, and plasma concentrations were followed for 8 hours. The 4 experiments were performed in random order.The kinetics following intravenous administration were nonlinear in the dose range 40 to 80mg, resulting in a 19% lower clearance and a 16% longer elimination half-life (0.81versus0.70 hours) for the 80mg dose compared to the 40mg dose. Following oral administration of a solution of omeprazole the AUC increased disproportionally when increasing the dose from 40 to 80mg. The nonlinear kinetics at higher dose levels of omeprazole appear mainly to be a result of partial saturation of the transformation of omeprazole into hydroxyomeprazole. The further metabolism of this metabolite exhibited linear kinetics. On the other hand, the formation of omeprazole-sulphone did not appear to be saturable in the dose range studied while its further metabolism seemed to be. The slight dose-dependency in clearance has no clinical relevance for the parenteral use of omeprazole - a drug with a wide therapeutic range. Furthermore, since omeprazole is given orally as slowly absorbed enteric-coated granules in lower doses the potential for dose-dependent kinetics would be much less in the clinical situation than in the present investigation.
ISSN:0114-2402
出版商:ADIS
年代:1990
数据来源: ADIS
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10. |
Clinical Study of Acarbose |
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Drug Investigation,
Volume 2,
Issue 4,
1990,
Page 264-267
J. Rybka,
A. Gregorová,
A. Zmydlená,
P. Jaron,
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ISSN:0114-2402
出版商:ADIS
年代:1990
数据来源: ADIS
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