Dados clínicos mundiais sobre a eficácia e a segurança da ciprofloxacina / World wide clinical data on efficacy and safety of ciprofloxacin

Em ensaios clínicos 8.861 pacientes foram tratados com ciprofloxacina a nível mundial. Dos tratamentos realizados,03.822 foram válidos para análise da eficácia, de acordo cocm os padröes do FDA. Em geral foram administradas as seguintes doses: infecçöes do trato urinário: 100 a 50 mg duas vezes por dia, por via oral ou 100 mg duas vezes por dia, por via intravenosa; infecçöes do trato respiratório: 250 a 1.000 mg, duas vezes ao dia, por via oral ou 200 mg duas vezes por dia, por via intravenosa; septicemia: 200 mg duas vezes por dia, por via intravenosa; gonorréia: 250 a 500 mg, por via oral, em dose única; todas as outras infecçöes: 500 a 1000 mg duas vezes por dia, por via oral ou 200 mg, duas vezes por dia, por via intravenosa. A ciprofloxacina foi administrada em 762 tratamentos de infecçöes respiratórias baixas, 88 infecçöes respiratórias altas, 108 bacteremias, 766 infecçöes de pele e anexos, 142 infecçöes dos ossos e articulaçöes, 149 infecçöes intra-abdominais, 33 infecçöes gastrintestinais, 1.633 infecçöes do trato urinário, 49 infecçöes pélvicas, 279 doenças transmitidas sexualmente, principalmente gonorréia, e em três meningites. A resposta clínica foi cura em 76%, melhora em 18% e falha em apenas 6%. A resposta bacteriológica em relaçäo a todos os locais avaliáveis foi: patógenos erradicados em 74%, acentuadamente reduzidos em 2% e persistentes em 10%. Ocorrem recidivas em 4% e reinfecçöes em outros 6%. A resposta global foi favorável em 90% dos pacientes. A segurança da droga foi estabelecida com base nos dados de 8.861 tratamentos a nível mundial. De acordo com a terminologia de COSTART, foram observadas as seguintes reaçöes adversas: digestivas 5%, metabólico-nutricionais 4,6% sistema nervoso central 1,6%, pele 1,4%, hematológicas e linfáticas 1%, cardiovasculares 0,4%, urogenitais 0,3%, órgäos dos sentidos 0,3%, músculo-esqueléticas 0,1%, respiratórias 0,08%...

Antibacterial treatment of otitis and sinusitis with ciprofloxacin and penicillin V--a comparison.

80 adult outpatients suffering from otitis media, sinusitis (maxillaris or frontalis) or peritonsillitis were treated with 500 mg ciprofloxacin b.i.d. (n = 40) or with 2 g penicillin V t.i.d. (n = 40). The patients were randomly allocated. Three groups of patients resulted, clinically and bacteriologically evaluable, or only clinically evaluable because the isolated strains were resistant to ciprofloxacin or penicillin V or because no strains were isolated. Ciprofloxacin was superior to penicillin V; there were fewer resistant strains (one compared to 11), and the eradication rate (57% compared to 43%) as well as the clinical efficacy (60% compared to 48%) of ciprofloxacin were better than those of penicillin V--even in a daily dose of 6.0 g. Both treatments were well tolerated; side effects were neither reported nor found.

Ciprofloxacin concentrations in tonsils following single or multiple administrations.

Penetration of ciprofloxacin into human tonsils was studied in 20 adult humans undergoing tonsilectomy. Ten patients received a single intravenous infusion of 200 mg ciprofloxacin within 15 min (group A) and 14 patients were treated orally for three days with 500 mg ciprofloxacin b.i.d. prior to a preoperative infusion of 200 mg (group B). Ciprofloxacin concentrations in serum and tonsils were determined microbiologically. Mean ciprofloxacin serum concentrations did not differ significantly between both groups. Similarly, mean distribution ratios between tonsils and serum were not dissimilar, being on average 150% irrespective of whether the drug was administered once or repeatedly. Thus, a significant accumulation of ciprofloxacin was not observed either in the intravascular or in the extravascular space.

Single and multiple dose pharmacokinetics of ciprofloxacin in gynecological tissues.

In a prospective pharmacokinetic study the serum and tissue concentrations of ciprofloxacin (Bay O9867), a new carboxyquinolone antimicrobial agent were studied. 22 patients were given 300 mg ciprofloxacin i. v. before the operation (group A), and 19 patients were premedicated with 500 mg ciprofloxacin orally twice daily for three days followed by 300 mg i. v. preoperatively. Tissue samples weighing approximately 2 g were taken from the fallopian tubes, the ovaries, the fundus myometrium and the cervix. Ciprofloxacin concentrations were measured biologically by the cup plate agar diffusion method. Ciprofloxacin concentrations in serum and gynecological tissues were within the same range in both groups. Maximal serum concentrations of 6 and 4 mg/l, respectively, were recorded immediately after infusion. After 2 h serum concentrations ranged from 0.6 to 1.3 mg/l in both groups. At the same time, the tissue concentrations ranged from 0.62 to 3.3 mg/kg, indicating that tissue levels exceed corresponding serum concentrations. On average ciprofloxacin is concentrated in the extravascular space two-fold, as compared to the corresponding serum concentrations. There is no drug accumulation. The tissue concentrations obtained provide a full antibacterial coverage for gynecological infections, since the MIC for the most pathogenic bacteria is less than 1 mg/l.

Bacterial infections of the skin treated with ciprofloxacin.

Bacterial infections of the skin or soft tissue responded to ciprofloxacin 500 mg tablets b.i.d. The treatment was well tolerated and effective, so that this drug can be recommended in cutaneous infections caused by sensitive bacteria.

Bacterial infections of the lower urinary tract treated with ciprofloxacin or cefalexin--a comparative study.

30/30 patients with lower UTI were enrolled in a randomized study to compare ciprofloxacin (250 mg/b.i.d.) and cefalexin (1 g/t.i.d.). In addition, 59 patients with cefalexin-resistant bacterial strains were treated in an open study arm. Ciprofloxacin showed convincingly better clinical and bacteriological efficacy than cefalexin. Both antibiotics were well tolerated. Ciprofloxacin has proved to be superior to cefalexin in the treatment of lower UTI.

Penetration of ciprofloxacin into gynecologic tissues.

Penetration of ciprofloxacin into gynecologic tissues has been studied after administration of the following: a single oral dose of 500 mg; a single injection of 100 mg; single intravenous infusions of 200 mg and 300 mg, respectively; and repeated oral doses of 500 mg followed by an infusion of 200 mg. In general, tissue concentrations of ciprofloxacin exceeded the corresponding serum concentrations on average twofold to fivefold, irrespective of the route of administration or the size of the dose. For example, mean tissue and serum concentrations of ciprofloxacin determined 12 hours after administration of a single oral dose of 500 mg were as follows: serum, 0.09 mg/liter; ovary, 0.28 mg/kg; uterus, 0.49 mg/kg; endometrium, 0.23 mg/kg; myometrium, 0.34 mg/kg; and fallopian tube, 0.36 mg/kg. Repeated drug administration did not result in an accumulation of ciprofloxacin in either serum or the tissues studied.

Ciprofloxacin in acute male gonorrhea.

100 male adults suffering from acute gonococcal urethritis were hospitalised and treated with decreasing doses from 2000 mg to 100 mg of ciprofloxacin (1-cyclopropyl-6-fluoro-1,4-dihydro-4-oxo-7-(1-piperazinyl)-3-quinoline carboxylic acid, Bay o 9867; designated tradename: Ciprobay). Clinical signs (burning, exudate, edema, inflammation) and bacteriology (native and culture) were assessed hourly during the first 9 h and at 12, 24 and 72 h after start of therapy. Most patients were controlled during 10 days. 99 patients showed clinical and bacteriological cure. One patient with subacute gonococcal urethritis (protocol violation) did not react on 250 mg. No postgonococcal urethritis was seen. No side effects were reported. For the acute male gonococcal urethritis a 100 mg single dose treatment with ciprofloxacin can be recommended.

Kidney function of pyelonephritis patients with impaired renal function treated with mezlocillin.

Ten patients with pyelonephritis and impaired renal function were treated with 2.0 g mezlocillin (Baypen) 8-hourly. They all recovered from urinary tract infection and showed a distinct improvement of their kidney function measured by blood urea nitrogen, serum creatinine and creatinine clearance. No side effects were seen and the blood coagulation remained within normal limits. An overview of the literature on urinary tract infections treated in patients with impaired kidney function is given.

Ciprofloxacin concentrations in tonsils following a single intravenous infusion.

Penetration of ciprofloxacin into human tonsils was studied following an intravenous infusion of 200 mg over 15 minutes to adult humans undergoing tonsillectomy. Samples were taken one-and-a-half to four hours after dosing. Generally, tissue levels exceeded corresponding serum concentrations by 50% (range of intraindividual ratios between tonsil and serum concentrations 100% to 288%). Ciprofloxacin distribution was homogeneous and independent of sampling time.

[Limitations of indications of clotrimazole-hydrocortisone and its components. A double-blind study]. / Indikationsabgrenzung zwischen Clotrimazol/Hydrocortison und seinen beiden Komponenten. Eine doppelblinde Studie.

Efficacy and tolerability of ointment/water emulsion, containing the combination of clotrimazole and hydrocortisone (Canesten HC) were compared with the two components. 4 groups of indications were chosen and 192 (16 X 3 X 4) patients treated. In all groups and symptoms of this comparison the best efficacy was with the combination product. Side effects which have to be attributed to this topical treatment could not be detected.

[Antibacterial concentrations in serum and tooth-jawbone tissue following perioperative administration of propicillin]. / Antibakterielle Konzentrationen in Serum und Geweben aus dem Zahn-Kieferbereich nach perioperativer Einnahme von Propicillin.

Antibacterial Concentrations in Serum and Dental Tissues after Preoperative Application of Propicillin. After resecting radicular and follicular cysts in the jaws, the serum, bone, capsule and fluid of the cysts from 40 patients were studied for their propicillin concentration. The patients received 1 Mega unit (0.7 g) propicillin orally as oblong tablets one or two hours before surgery. One or two hours after the application of propicillin, the distribution coefficients between serum and the three tissues were 0.78 and 0.87 for the spongious bone, 0.07 and 0.06 for the cyst capsule and 0.14 and 0.08 for the cyst fluid. The mean concentrations in all three tissues were distinctly above the MICs of the bacteria most frequently isolated from the mouth for at least two hours.

Mezlocillin and carbenicillin: a clinical comparison of serious systemic infections in surgical patients.

Eighty patients suffering from severe cases of systemic surgical infections were enrolled in a prospective, controlled randomized study to compare mezlocillin and carbenicillin. The daily dosage was chosen according to international recommendation, i.e. 4 g mezlocillin 6-hourly and 5 g carbenicillin 4-hourly. A clinical, bacteriological and combined "overall" evaluation was made. There was a distinct trend in favour of the mezlocillin group which was not statistically significant. The treatment was well tolerated; no side-effects were observed.

Mezlocillin in serious surgical infections caused by carbenicillin-resistant bacteria.

Fifty-eight surgical patients suffering from severe bacterial infections caused by mezlocillin-sensitive, carbenicillin and/or gentamicin-resistant bacteria were treated with mezlocillin in 1980. At the end of therapy, the infection had been eliminated in 52 patients; they were cured. The remaining six did not need any additional antibacterial treatment. Sixty-two of the bacterial strains isolated had been eliminated, seven markedly reduced in number and three persisted. No development of resistance or side-effects was observed. A randomized comparative study was conducted at the same time.