摘要:

The pharmacokinetics and clinical efficacy of ceftizoxime in premature infants and neonates were investigated.The serum half-life (t½) of ceftizoxime (20 mg/kg, bolus intravenous administration) at ages 0 to 3, 4 to 7, 8 to 14 and 15 to 30 days was 4.1, 3.0, 2.6 and 2.0 hours for neonates and 5.3, 4.6, 3.7 and 2.6 hours for premature infants, respectively.The excretion rate (percentage of administered dose) of ceftizoxime in urine over the first 6 hours after intravenous bolus injection of 20 mg/kg in neonates aged 0 to 3 days, was about 35% and 45 to 55% in those 4 days old and over. Percentage excretion was about 30% in premature infants aged 0 to 3 days and about 45% in those aged 4 days and over.The clinical efficacy of ceftizoxime was investigated in a total of 112 patients; 83 had bacterial infections, and the prophylactic use was studied in the other 29. In 83 patients (86 infections), ceftizoxime showed good therapeutic effect, i.e. the efficacy percentage (total ‘excellent’ and ‘good’ efficacy cases/total number of cases) for 40 cases (group A) with identified pathogenic bacteria was 95.0% and that for 46 cases without identified pathogenic bacteria was 95.7%. The bacteriological effects of ceftizoxime were studied with 41 strains found in group A; 89.5% of Gram-positive bacteria and 95.5% of Gramnegative bacteria were sensitive to the drug.No adverse effects were observed; mild and transient abnormalities in clinical laboratory tests were noted, however, these were not considered clinically significant.These results suggest that ceftizoxime is an effective and well tolerated antibiotic for the treatment of neonatal infections.

ISSN:0114-2402    

出版商:ADIS    

年代:1990

数据来源: ADIS

摘要:

In contrast to the initial drug treatment of hypertension, ‘second line’ therapy has not been extensively studied. As a prelude to a more definitive controlled trial, a multicentre randomised open study was conducted with bisoprolol, a new&bgr;-blocker with high&bgr;1-selectivity and once-daily dosage. 558 patients with uncomplicated mild to moderate essential hypertension were initially treated with bisoprolol 10mg once daily for 4 weeks. A target diastolic blood pressure of below 95mm Hg was reached in 74.9% of the population. The ‘nonresponders’ (135 patients) were randomised into 4 different groups: I, bisoprolol 20mg; II, bisoprolol 10mg + hydrochlorothiazide 25mg + amiloride 2.5mg; III, bisoprolol 10mg + enalapril 10mg; IV, bisoprolol 10mg + nifedipine 20mg twice daily. Target blood pressure was achieved in Group I: 91% (21/23); Group II: 83% (34/41); Group III: 88% (35/40); Group IV: 94% (29/31) [differences statistically nonsignificant]. Mild clinical adverse drug reactions were recorded in 4 patients in Group I, 3 in Group II, 1 in Group III, and 3 in Group IV.Thus, in those who failed to reach target blood pressure with bisoprolol 10mg for 4 weeks, bisoprolol 20mg appears to have a similar efficacy rate to a treatment combining bisoprolol with another antihypertensive agent. Combinations of bisoprolol 10mg with enalapril or nifedipine seem as efficacious as the more traditional combination with a diuretic.

ISSN:0114-2402    

出版商:ADIS    

年代:1990

数据来源: ADIS

摘要:

The inclusion complexes of 4-biphenylylacetic acid (BPAA), an anti-inflammatory agent with&bgr;-cyclodextrin (&bgr;-CyD), heptakis (2,6-di-O-methyl)-&bgr;-CyD (DM-&bgr;-CyD), and 2-hydroxypropyl-&bgr;-CyD (HP-&bgr;-CyD) in a molar ratio of 1 : 1 were prepared and their topical availabilities in the hydrophilic ointment were evaluated in rats. Thein vitrorelease of BPAA from the ointment base was remarkably enhanced by the complexations with&bgr;-CyDs in the order of&bgr;- < DM-&bgr;- ≈ HP-&bgr;-CyD. Thein vivopercutaneous absorption studies in rats revealed that the greater release of BPAA from the vehicle obtained by&bgr;-CyDs not only compensates for negative effects of&bgr;-CyDs on the skin permeation of BPAA, but also delivers BPAA more effectively to the site of action. Furthermore,&bgr;-CyDs enhanced the anti-inflammatory effect of BPAA in the ointment on the acute paws oedema induced by carrageenan in rats; the enhancing efficacy of&bgr;-CyDs was in the order of&bgr;- < DM-&bgr;- < HP-&bgr;-CyD. The present data suggest that HP-&bgr;-CyD is particularly useful in improving the topical availability of BPAA in the ointment formulation tested.

ISSN:0114-2402    

出版商:ADIS    

年代:1990

数据来源: ADIS

摘要:

The aim of this double-blind parallel-group study was to endoscopically evaluate the gastric mucosal reaction after a 7-day oral administration of nimesulide, a nonsteroidal anti-inflammatory agent, at 100 or 200mg twice daily. Placebo was the reference compound.30 dyspeptic patients, randomly allocated in 3 groups, completed the study. After drug administration 1 patient receiving each nimesulide dosage and 2 in the control group had gastric injuries of different degree: 1 subject with slight hyperaemic gastropathy at baseline presented with some superficial ulcerations at the end of the 100mg nimesulide treatment; 1 patient, normal but with an anamnesis of gastric ulcer, had a congested mucosa of the corpus with several erosions and ulcerations after the administration of 200mg nimesulide. In the placebo group 1 patient of hyperaemic antropathy and one case of several petechiae and microerosions were observed.The incidence of adverse effects was comparable in all groups. The administration of the drugs did not induce any significant modification of the considered haematological and haematochemical parameters.

ISSN:0114-2402    

出版商:ADIS    

年代:1990

数据来源: ADIS

摘要:

A balanced 2-way crossover study involving 12 elderly volunteers was used to determine the pharmacokinetic parameters of the antidepressant tianeptine following a single dose administered by oral and intravenous routes. Pharmacokinetic parameters of metabolite MC5, the C5 side-chain&bgr;-oxidation product of tianeptine, were simultaneously determined.Tianeptine was absorbed rapidly [peak concentration (Cmax) = 261 ± 70 μg/L, and time to Cmax(tmax) = 1.59 ± 0.63 hours] and efficiently, with a bioavailability of 84.6 ± 14.0%.After intravenous administration, following limited distribution in the tissues [volume of distribution at steady-state (Vdss) = 0.44 ± 0.08 L/kg] tianeptine was rapidly eliminated from the plasma (t½z= 3.1 ± 1.1 hours) mainly through biotransformation [renal clearance (CLR) < 1 ml/min; total clearance (CLT) = 139 ± 28 ml/min].The MC5 metabolite appeared 0.18 ± 0.04 hours following the beginning of intravenous administration (tmax2.96 ± 0.95 hours; Cmax= 83 ± 29 μg/L). MC5 was excreted with a terminal half-life of 11.9 ± 8.0 hours; its renal clearance was low (3.1 ± 2.3 ml/min). After oral administration, the pharmacokinetics of the MC5 metabolite remained unchanged, except for tmaxwhich was delayed (tmax= 3.70 ± 0.61 hours).This study has shown that the bioavailability of tianeptine is high in elderly subjects. Apart from drowsiness observed only following intravenous administration, tianeptine was well tolerated, particularly with regard to cardiovascular effects.

ISSN:0114-2402    

出版商:ADIS    

年代:1990

数据来源: ADIS

摘要:

The increasing prevalence of&bgr;-lactamase production by pathogens associated with cellulitis and soft-tissue infections have made the efficacy of standard treatment regimens suspect and demonstrate the need for a reappraisal of optimal medical management for these infections. In an open randomised, prospective study, the efficacy and toxicity of intravenous ampicillin/sulbactam was compared with cefazolin for the treatment of cellulitis and with cefoxitin for the treatment of soft-tissue infections. Ampicillin/sulbactam was given to 24 patients, cefoxitin to 16 and cefazolin to 12 patients. Analysis of clinical and bacteriological responses showed no significant differences between groups despite the fact that byin vitrotesting 82 (98%) of isolates from soft-tissue infections were susceptible to ampicillin/sulbactam but only 68 (81%) were susceptible to cefoxitin (p < 0.001). The addition of sulbactam to ampicillin significantly enhanced itsin vitroactivity against&bgr;-lactamase-producingStaphylococcus aureusand anaerobic bacteria. All adverse reactions were subclinical, demonstrable only by mild laboratory abnormalities. Overall, ampicillin/sulbactam appears to be of comparable clinical efficacy in the treatment of polymicrobial soft-tissue infections with cefoxitin, or in the treatment of cellulitis with cefazolin. Additionally, whenEnterococcus faecalisandS. aureusare recovered from a single culture, ampicillin/sulbactam, as opposed to cefoxitin monotherapy, would remain effective. Therefore, ampicillin/sulbactam will often be a less expensive therapeutic alternative.

ISSN:0114-2402    

出版商:ADIS    

年代:1990

数据来源: ADIS

摘要:

The influence of food intake on the bioavailability of omeprazole was studied after single and repeated administrations of enteric coated (EC) granules. 12 healthy males participated in an open crossover trial consisting of 3 study periods. Omeprazole 20mg was given as a single intravenous dose and orally as EC granules once daily for 7 days either immediately before or immediately after breakfast (periods 2 and 3). Plasma concentrations of omeprazole were followed after the intravenous dose and on days 1 and 7 in the other periods.The time for appearance of omeprazole in plasma seemed to be prolonged when the EC granule formulation was given after food intake. The total amount of drug absorbed, however, was not affected. Starting from identical area under the plasma concentrationtime curve (AUC) values following the first dose, the AUC increased by approximately 60% during repeated administration when the EC granules were given both before and after breakfast.

ISSN:0114-2402    

出版商:ADIS    

年代:1990

数据来源: ADIS

摘要:

The clinical usefulness of 150mg roxatidine acetate hydrochloride once daily before bed in 20 patients with reflux oesophagitis was investigated in a double-blind trial, comparing treatment with 75mg twice daily (after breakfast and before bedtime in 22 patients).In the evaluation of subjective and objective symptoms, there was marked improvement in 8 patients (50.0%) and improvement in 6 patients (37.5%) in the once-daily group, for an overall improvement rate of 87.5%. In the twice-daily group there was marked improvement in 7 patients (35.0%) and improvement in 10 patients (50%), for an overall improvement rate of 85.0%.The endoscopic healing rate was 35.7, 56.3 and 75.0% after 4, 8 and 12 weeks, respectively, in the once-daily group and 35.3, 60.0 and 81.3% in the twice-daily group.In the evaluation of overall improvement, marked improvement or improvement was seen in 81.3 and 93.8% after 8 and 12 weeks, respectively, in the once-daily and 80.0 and 81.2% in the twice-daily group.No side effects were observed in either group. The only abnormal laboratory test value was an increased platelet count in 1 patient in the once-daily group, for which there was no clear cause-effect relationship with the trial drug. In the overall safety evaluation, there were no problems in any patients in either group.The usefulness rates (very useful + useful) were 81.3 and 93.8% after 8 and 12 weeks, respectively, in the once-daily group and 86.7 and 81.2%, respectively, in the twice-daily group.From the above results, it appears that a single, daily dose of roxatidine acetate hydrochloride before bedtime is useful for the treatment of reflux oesophagitis, demonstrating comparable efficacy to the conventional twice-daily, administration schedule.

ISSN:0114-2402    

出版商:ADIS    

年代:1990

数据来源: ADIS

ISSN:0114-2402    

出版商:ADIS    

年代:1990

数据来源: ADIS

ISSN:0114-2402    

出版商:ADIS    

年代:1990

数据来源: ADIS