Cefpirome is a new fourth generation injectable cephalosporin antibiotic. Its tolerability profile was established in a programme of 16 clinical studies involving 3103 patients in Europe and the US. The overall incidence of clinical adverse events with cefpirome was 21.9% compared with 27.1% with comparators (ceftazidime, imipenem, ceftriaxone). Adverse events thought possibly related to treatment occurred in 12.5% of patients receiving cefpirome and 13.7% of recipients of comparator agents. Withdrawals from treatment due to adverse events occurred in 5.1 and 5.0% of patients receiving cefpirome and comparators, respectively. The commonest adverse events thought possibly related to treatment were gastrointestinal symptoms (mainly diarrhoea in 1.6 and 1.7%, respectively) and rash (1.4 and 1.4%, respectively). Comparison with data obtained from the literature for ceftazidime, ceftriaxone and the third generation cephalosporins in general shows that the adverse event profile of cefpirome is similar to that of other broad-spectrum injectable cephalosporins.

Cephalosporins↗

PubMed1989

Safety and efficacy of roxatidine acetate. Evidence from pharmacodynamic and clinical trials.

The effects of a new H2-receptor antagonist, roxatidine acetate, have been investigated in both clinical and pharmacodynamic trials in Europe and the United States. A series of four double-blind randomized studies are reviewed, reporting the effects of different dose regimens of roxatidine acetate compared with ranitidine and placebo in healthy volunteers using continuous intragastric pH monitoring. These pharmacodynamic studies clearly demonstrate that roxatidine acetate is an effective gastric antisecretory agent, which is up to twice as potent as ranitidine. The results of several clinical studies of roxatidine acetate in patients with gastric as well as duodenal ulcer conducted in Europe, Japan, and the United States are also reviewed. These studies show that roxatidine acetate is comparable to other potent H2-receptor antagonists in terms of cumulative healing rates, pain relief, and safety. Overall, the pharmacodynamic and clinical data indicate that the efficacy of roxatidine acetate 75 mg twice-daily (b.i.d.) does not differ significantly from ranitidine 150 mg b.i.d. Roxatidine acetate is equally effective in the treatment of peptic disease including gastric ulcer, duodenal ulcer, and reflux esophagitis.

Cimetidine↗

PubMed1988

Clinical characteristics of roxatidine acetate: a review.

Pharmacodynamic studies revealed that 150 mg of roxatidine acetate were optimal in suppressing gastric acid secretion, and that a single bedtime dose of 150 mg was more effective than a dose of 75 mg twice daily in terms of inhibiting nocturnal acid secretion. When administered orally as a capsule containing a granule formulation, the drug displayed modified-release properties, which led to a sustained suppression of gastric acid secretion. Clinical trials revealed that roxatidine acetate, 75 mg twice daily and 150 mg at night, was highly effective in healing duodenal and gastric ulcers and in reducing ulcer pain, over 4, 6, and 8 weeks of therapy. A steady reduction in diameter was observed in those ulcers not completely healed during therapy. The single bedtime dose regimen, while producing the same degree of healing as the divided daily dose during controlled clinical trials, may be of greater value in therapeutic use owing to improved patient compliance. In all efficacy criteria (cure, reduction in ulcer size, and pain relief) there was no significant difference between roxatidine acetate in a total daily dose of 150 mg, ranitidine in a total daily dose of 300 mg, and cimetidine in a total daily dose of 800 mg. Prevention of gastric and duodenal ulcer relapse was achieved by roxatidine acetate, 75 mg at night for 6 months, in about 70% of patients, as determined in open, pilot studies--a rate comparable to those reported for cimetidine and ranitidine. Roxatidine acetate shares with ranitidine an improved safety profile when compared with cimetidine. Human pharmacology studies and short-term and long-term clinical trials have all shown that roxatidine acetate is an exceptionally well tolerated compound, without the antiandrogenic activity and interference with hepatic drug metabolism which have characterized cimetidine treatment. A reason for the improved safety profile of roxatidine acetate may be its greater potency than cimetidine (six times less potent) and ranitidine (half as potent), so that lower doses of roxatidine acetate, representing a lower chemical load, are therapeutically effective. The novel structure of roxatidine acetate probably also underlies the improved safety of the compound.

Cimetidine↗

PubMed1987

The effects of 75 mg HOE 760, a novel H2-receptor antagonist, on daytime peptone-stimulated and nocturnal gastric acid output in healthy volunteers.

The effects of HOE 760, a highly specific H2-receptor antagonist, on daytime peptone-stimulated and nocturnal gastric acid output were studied (randomized, double-blind crossover) in 10 healthy men. Acid output was monitored at lunch (1200 h to 1400 h) and dinnertime (1800 h to 2000 h) by continuous automatic intragastric titration; from midnight to 0600 h, output was measured by titration of manually aspirated gastric contents. After a 75-mg oral dose (capsule containing HOE 760 granules) at 0800 h peptone-stimulated acid output decreased for at least 12 h. Compared with placebo, significant reductions (p less than 0.05) of 86% and 32% were observed 4-6 h and 10-12 h after drug administration. After another dose of 75 mg at 2100 h nocturnal acid output was significantly reduced (p less than 0.05) by 88%; gastric pH was increased by about 2 units throughout the night. HOE 760 was well tolerated. No adverse reactions occurred; no clinically relevant changes were noted in haematologic, biochemical, urinary, or electrocardiographic variables.

Adult↗

PubMed1985

Drug-induced changes of the flow pulse contour recorded by directional CW-Doppler devices: a possible estimation of changes in vascular characteristic impedance and peripheral resistance.

Ultrasound Doppler sonography using directional continuous wave Doppler devices is an inexpensive, simple tool used worldwide for the diagnosis and hemodynamic assessment of patients with peripheral vascular disease (PVD). In addition to pressure evaluation, the interpretation of Doppler velocity pulses has become routine within the last years. However, spontaneous variations in characteristic impedance of muscular arteries or in peripheral resistance will lead to respective variations of arterial reflection coefficients, with consequent changes of the arterial flow pulse reflection pattern and flow pulse contour. The authors studied peripheral Doppler wave forms in 20 volunteers after buccal administration of 1.6 mg of glyceryl trinitrate (GTN) and i.a. (femoral) injection of 30 mg tolazoline hydrochloride. Velocity pulse changes due to artificially introduced variation in peripheral resistance (reactive hyperemia, total arterial blockade) were compared to those induced by above maneuvers. An isolated decrease in characteristic impedance of muscular arteries without alteration of the peripheral resistance is characterized by an increase in the amplitudes of foreward as well as the reverse flow phase of the Doppler signal, with predominant increase of the early diastolic reverse flow phase and subsequent decrease in mean velocity. In contrast, isolated changes in peripheral resistance are reflected mainly by subsequent variations of the reverse flow phase amplitude of the Doppler signals.

Adult↗

PubMedDate not supplied

A multicenter, randomized, double-blind comparison of roxatidine with ranitidine in the treatment of patients with uncomplicated benign gastric ulcer disease. The Multicenter Roxatidine Cooperative Study Group.

Roxatidine (150 mg, 312 patients) was compared with ranitidine (300 mg, 308 patients) in a randomized, double-blind, parallel-group, 6-week therapeutic study for the treatment of patients with uncomplicated, benign gastric ulcer disease. The study end points (verified by using endoscopy results) were fully healed ulcers at 4 or 6 weeks. The results of roxatidine therapy were comparable to those of ranitidine therapy: healing rates of 52% and 54% at week 4 and 77% and 76% at week 6 were recorded for roxatidine and ranitidine, respectively. The drugs produced comparable reductions in ulcer diameters and decreases in abdominal pain. Adverse events associated with both roxatidine (27%) and ranitidine (28%) were headache, diarrhea, and dizziness; rash was associated in 6 of 8 cases and in only 1 case with roxatidine. In this trial, roxatidine 150 mg once daily was as efficacious and safe as ranitidine 300 mg once daily for treatment of patients with uncomplicated, benign gastric ulcer disease.

Adult↗

PubMedDate not supplied

Physiological flow variations in the periorbital arteries in Zambian Africans. A screening with bidirectional Doppler ultrasound.

Directional Doppler sonography with direct evaluation of the extracranial carotid artery system and scanning of the periorbital arteries has been performed in 49 black Zambian hypertensive patients and in 19 controls without cardiovascular risk factors. Direct evaluation of the extracranial carotid artery system did not show any abnormalities. In contrast to this periorbital Doppler examination revealed positive findings with retrograde flow direction in the supratrochlear artery in 19% and 21% of all examined carotids in the hypertension and control group, respectively. Compared to direct carotid angiography, 66% of the positive supratrochlear and 13% of the positive supraorbital findings in the hypertensive patient group could be shown to be false positive results. As a possible explanation of this high incidence of a retrograde flow direction in periorbital arteries a different flow physiology in the ophthalmic artery of black Zambians compared to Caucasians is discussed.

Adult↗