scholarly journals Comparison of single-dose cefuroxime axetil with ciprofloxacin in treatment of uncomplicated gonorrhea caused by penicillinase-producing and non-penicillinase-producing Neisseria gonorrhoeae strains.

1996 ◽  
Vol 40 (12) ◽  
pp. 2775-2780 ◽  
Author(s):  
E M Thorpe ◽  
J R Schwebke ◽  
E W Hook ◽  
A Rompalo ◽  
W M McCormack ◽  
...  
Keyword(s):  
Single Dose ◽  
Oral Dose ◽  
Confidence Interval ◽  
Neisseria Gonorrhoeae ◽  
Single Oral Dose ◽  
Cefuroxime Axetil ◽  
Female Patients ◽  
Male Patients ◽  
Males And Females ◽  
Uncomplicated Gonorrhea

A randomized, multicenter, investigator-blind trial was conducted to compare the efficacies of cefuroxime axetil and ciprofloxacin for treatment of patients with uncomplicated gonorrhea caused by penicillinase-producing Neisseria gonorrhoeae (PPNG). A total of 832 patients (434 females and 398 males) received a single oral dose of cefuroxime axetil (1,000 mg [417 patients]) or ciprofloxacin (500 mg [415 patients]). N. gonorrhoeae was eradicated from the cervix in 114 of 118 (97%) and 118 of 119 (99%) bacteriologically evaluable females treated with cefuroxime axetil and ciprofloxacin, respectively (P = 0.213; difference, -2%; 95% confidence interval, -6 to 1%), and from the urethra in 154 of 166 (93%) and 171 of 171 (100%) bacteriologically evaluable male patients treated with cefuroxime axetil and ciprofloxacin, respectively (P < 0.001; difference, -7%; 95% confidence interval, -11 to -3%). Both treatments were effective in eradicating N. gonorrhoeae in females with rectal infections (cefuroxime axetil, 29 of 30 [97%]; ciprofloxacin, 25 of 25 [100%]; P = 1.00). In small numbers of patients, cefuroxime axetil was less effective than ciprofloxacin in treating males with pharyngeal infections (eradication in 4 of 10 and in 8 of 8 patients, respectively; P = 0.013). PPNG was eradicated from the cervix in 22 of 23 (96%) and 32 of 32 (100%) bacteriologically evaluable female patients treated with cefuroxime axetil and ciprofloxacin, respectively (P = 0.418; difference, -4%; 95% confidence interval, -13 to 4%), and from the urethra in 35 of 36 (97%) and 34 of 34 (100%) bacteriologically evaluable male patients treated with cefuroxime axetil and ciprofloxacin, respectively (P = 1.00; difference, -3%; 95% confidence interval, -8 to 3%). The incidences of drug-related adverse events were similar for the two study drugs. In summary, treatment with a single oral dose of cefuroxime axetil is as effective as treatment with a single oral dose of ciprofloxacin in eradicating PPNG from males and females with uncomplicated gonorrhea (urethral and endocervical), and both regimens are well-tolerated. However, in the present study, cefuroxime axetil was less effective than ciprofloxacin in treating urethral gonococcal infections in male patients, although both study drugs were highly effective in treating cervical gonococcal infections in female patients.

Comparison of single-dose oral grepafloxacin with cefixime for treatment of uncomplicated gonorrhea in men. The STD Study Group.

1997 ◽  
Vol 41 (8) ◽  
pp. 1843-1845 ◽  
Author(s):  
E W Hook ◽  
W M McCormack ◽  
D Martin ◽  
R B Jones ◽  
K Bean ◽  
...  
Keyword(s):  
Single Dose ◽  
Neisseria Gonorrhoeae ◽  
Open Study ◽  
Study Group ◽  
Dose Oral ◽  
Male Patients ◽  
Resistant Strains ◽  
Oral Doses ◽  
Uncomplicated Gonorrhea

In a randomized open study, 351 male patients with uncomplicated gonorrhea were given single oral doses of grepafloxacin (400 mg) or cefixime (400 mg). In the 299 microbiologically evaluable patients, urethral infections were cured in 99% (147 of 149) of those receiving grepafloxacin and 97% (145 of 150) of those given cefixime. Eradication rates for both regimens were 100% in the 16% (47 of 299) of participants who were infected with penicillin-resistant Neisseria gonorrhoeae and 97% in the 21% (62 of 299) of participants infected with tetracycline-resistant strains. Grepafloxacin is a well-tolerated alternative to cefixime for treatment of uncomplicated gonorrhea in males.

Single-Dose Therapy of Anogenital and Pharyngeal Gonorrhoea with Ciprofloxacin

1992 ◽  
Vol 3 (1) ◽  
pp. 49-51 ◽  
Author(s):  
T Balachandran ◽  
A P Roberts ◽  
B A Evans ◽  
B S Azadian
Keyword(s):  
Adverse Reaction ◽  
Single Dose ◽  
Oral Dose ◽  
Neisseria Gonorrhoeae ◽  
Treatment Failure ◽  
Single Oral Dose ◽  
Open Study ◽  
Dose Therapy ◽  
Single Dose Therapy

A single dose of ciprofloxacin, 250 mg by mouth, was used in an open study to treat pharyngeal or rectal gonorrhoea or both in 64 patients (32 men and 32 women). The study also included 151 men with urethral gonorrhoea and 53 women with cervical or urethral gonorrhoea. Ciprofloxacin cured 63 (98%) patients with pharyngeal or rectal gonorrhoea (including 5 patients with penicillinase-producing Neisseria gonorrhoeae; PPNG), 147 (97%) men with urethral gonorrhoea (including 8 with PPNG) and 52 (98%) women with cervical or urethral gonorrhoea. All the isolates of N. gonorrhoeae were sensitive to 0.03 mg/l of ciprofloxacin. Five of the 6 patients with treatment failure were subsequently cured by a single oral dose of ciprofloxacin 250 mg. None of the patients reported an adverse reaction. Ciprofloxacin 250 mg as a single oral dose is effective and safe in treating patients with pharyngeal or rectal gonorrhoea, including those with PPNG strains.

scholarly journals Pharmacodynamic Evaluation of Dosing, Bacterial Kill, and Resistance Suppression for Zoliflodacin Against Neisseria gonorrhoeae in a Dynamic Hollow Fiber Infection Model

2021 ◽  
Vol 12 ◽  
Author(s):  
Susanne Jacobsson ◽  
Daniel Golparian ◽  
Joakim Oxelbark ◽  
Emilie Alirol ◽  
Francois Franceschi ◽  
...  
Keyword(s):  
Single Dose ◽  
Oral Dose ◽  
Neisseria Gonorrhoeae ◽  
Single Oral Dose ◽  
Hollow Fiber ◽  
Dose Range ◽  
World Health ◽  
Dose Fractionation ◽  
Infection Model ◽  
Pharmacokinetic Data

Antimicrobial resistance in Neisseria gonorrhoeae is threatening the treatment and control of gonorrhea globally, and new treatment options are imperative. Utilizing our dynamic in vitro hollow fiber infection model (HFIM), we examined the pharmacodynamics of the first-in-class spiropyrimidinetrione (DNA gyrase B inhibitors), zoliflodacin, against the N. gonorrhoeae reference strains World Health Organization F (susceptible to all relevant antimicrobials) and WHO X (extensively drug resistant, including resistance to ceftriaxone) over 7 days. Dose-range experiments with both strains, simulating zoliflodacin single oral dose regimens of 0.5–8 g, and dose-fractionation experiments with WHO X, simulating zoliflodacin oral dose therapy with 1–4 g administered as q12 h and q8 h for 24 h, were performed. A kill-rate constant that reflected a rapid bacterial kill during the first 6.5 h for both strains and all zoliflodacin doses was identified. In the dose-range experiments, the zoliflodacin 2–8 g single-dose treatments successfully eradicated both WHO strains, and resistance to zoliflodacin was not observed. However, zoliflodacin as a single 0.5 g dose failed to eradicate both WHO strains, and a 1 g single dose failed to eradicate WHO X in one of two experiments. The zoliflodacin 1 g/day regimen also failed to eradicate WHO X when administered as two and three divided doses given at q12 h and q8 h in the dose-fractionation studies, respectively. All failed regimens selected for zoliflodacin-resistant mutants. In conclusion, these data demonstrate that zoliflodacin should be administered at &gt;2 g as a single oral dose to provide effective killing and resistance suppression of N. gonorrhoeae. Future studies providing pharmacokinetic data for zoliflodacin (and other gonorrhea therapeutic antimicrobials) in urogenital and extragenital infection sites, particularly in the pharynx, and evaluation of gonococcal strains with different gyrB mutations would be important.

Single-dose Cefuroxime Axetil in the Treatment of Uncomplicated Gonorrhea: A Controlled Trial

1985 ◽  
Vol 12 (4) ◽  
pp. 184-187 ◽  
Author(s):  
RICHARD C. REICHMAN ◽  
FREDERICK S. NOLTE ◽  
STEVEN M. WOLINSKY ◽  
CAROL A. GREISBERGER ◽  
MARY ANNE TRUPEI ◽  
...  
Keyword(s):  
Single Dose ◽  
Controlled Trial ◽  
Cefuroxime Axetil ◽  
Uncomplicated Gonorrhea

scholarly journals The metabolism of 2,6-di-tert.-butyl-4-hydroxymethylphenol (Ionox 100) in the dog and rat

1965 ◽  
Vol 97 (1) ◽  
pp. 303-310 ◽  
Author(s):  
AS Wright ◽  
DAA Akintonwa ◽  
RS Crowne ◽  
DE Hathway
Keyword(s):  
Single Dose ◽  
Oral Dose ◽  
Oral Administration ◽  
Single Oral Dose ◽  
Individual Variation ◽  
Uronic Acid ◽  
Species Difference ◽  
Hydroxybenzoic Acid ◽  
Tert Butyl

1. A single oral dose of [(14)C]Ionox 100 to rats is almost entirely eliminated in 11 days: 89.1-107.2% of the (14)C is excreted and 0.29+/-0.02% of the dose is present in the carcass plus viscera after removal of the gut. Rats exhibit an individual variation in the elimination pattern, 15.6-70.8% of (14)C being excreted in the urine and 75.2-27.0% in the faeces during 11 days. 2. After the oral administration of [(14)C]Ionox 100 to dogs, 87.1-90.3% of the (14)C is excreted in the faeces and urine during 4 days. 3. Dogs and rats do not show a species difference in this pattern of elimination. 4. The rate of elimination from dogs and rats given a single dose of Ionox 100 is not affected by the size of the dose and the presence of triglyceride fat in the diet. 5. Ionox 100 is completely metabolized in dogs and rats: unchanged Ionox 100 is absent from the urine and faeces, and from the carcass when elimination is complete. In rats, 3,5-di-tert.-butyl-4-hydroxybenzoic acid accounts for 50-85% of a dose of Ionox 100 and (3,5-di-tert.-butyl-4-hydroxybenzoyl beta-d-glucopyranosid)uronic acid for 47-10%; in dogs, the unconjugated acid accounts for 85% and the ester glucuronide for 10-12%. 3,5-Di-tert.-butyl-4-hydroxyhippuric acid is not formed. Other metabolites, which have been detected in small quantity in the faeces and urine of animals dosed with Ionox 100, have not been identified. 6. 3,5-Di-tert.-butyl-4-hydroxybenzoic acid and (3,5-di-tert.-butyl-4-hydroxybenzoyl beta-d-glucopyranosid)uronic acid are also the major metabolites of Ionol (2,6-di-tert.-butyl-p-cresol) in rats. 7. The elimination of Ionox 100 metabolites from rats is faster than that of Ionol and its metabolites. Unlike Ionol, unchanged Ionox 100 could not be detected in the bodies of these animals.

scholarly journals 1393. A Phase 1, Randomized, Open-Label, Crossover Study in Healthy Subjects Under Fasting Conditions of Orally Administered Sulopenem Etzadroxil Alone or with Probenecid to Determine the Pharmacokinetics of Sulopenem

2018 ◽  
Vol 5 (suppl_1) ◽  
pp. S428-S429
Author(s):  
Michael Dunne ◽  
Steven Aronin ◽  
Elise Dunzo ◽  
Sailaja Puttagunta
Keyword(s):  
Oral Dose ◽  
Single Oral Dose ◽  
Phase 1 ◽  
Treatment Options ◽  
Parent Compound ◽  
Additional Treatment ◽  
Open Label ◽  
Males And Females ◽  
The Mean ◽  
Mean Time

Abstract Background Antimicrobial resistance to available oral antibiotics is becoming progressively more common, precipitating the need for additional treatment options as step-down from initial intravenous (IV) therapy as well as for treatment of infections in the community. Sulopenem (CP-70,429) is a thiopenem antibiotic active against quinolone non-susceptible and ESBL-producing Enterobacteriaceae. As the key pharmacokinetic-pharmacodynamic variable correlating with efficacy for penem antibiotics is time above minimum inhibitory concentration (T &gt; MIC), we examined the utility of probenecid, an OAT-1 inhibitor of β-lactam excretion, on the pharmacokinetic (PK) parameters for the oral prodrug of sulopenem, sulopenem etzadroxil Methods Twelve healthy males and females received a single oral dose of 500 mg sulopenem etzadroxil as powder in bottle either alone or co-administered with a single oral dose of probenecid 500 mg in a crossover design with a washout period of 6 days. All doses were administered under fasting conditions. Blood samples for plasma PK analysis were collected and PK parameters for sulopenem, the parent compound of sulopenem etzadroxil, were determined. Results Treatment Conclusion Probenecid increases the AUC of sulopenem by 28% in the fasted state and extends the mean time over MIC. Disclosures M. Dunne, Iterum Therapeutics: Employee and Shareholder, Salary. S. Aronin, Iterum Therapeutics: Employee and Shareholder, Salary. E. Dunzo, Parexel: Consultant, Consulting fee. S. Puttagunta, Iterum Therapeutics: Employee and Shareholder, Salary.

scholarly journals Milk iodine concentration in cows treated orally or intramuscularly with a single dose of iodinated fatty acid esters

2012 ◽  
Vol 48 (No. 6) ◽  
pp. 155-162 ◽  
Author(s):  
I. Herzig ◽  
J. Poul ◽  
B. Písaíková ◽  
E. Göpfert
Keyword(s):  
Single Dose ◽  
Fatty Acid ◽  
Oral Dose ◽  
Dairy Cows ◽  
Single Oral Dose ◽  
Experimental Period ◽  
Iodine Concentration ◽  
Fatty Acid Esters ◽  
Oral Application ◽  
Acid Esters

The effect of a single oral dose of iodinated fatty acid esters (IFAE) on iodine levels in colostrum and milk of goats was tested. In experimental goats that received a single oral dose of IFAE before delivery, significantly higher iodine levels in milk were recorded 60 days after the delivery. In the following period since day 75 after the delivery iodine levels decreased, however, remained higher compared to the control, e.g. on day 152 the levels were twice as high as in the controls. Based on these results, the effect of a single oral and parenteral application of IFAE was tested on dairy cows. The results of the experiment showed that a single oral application of IFAE increases milk iodine levels for a shorter period. Intramuscular application resulted in a significantly higher milk iodine levels during the whole experimental period compared to both untreated controls and cows with oral application of IFAE.

Treatment of Uncomplicated Gonorrhea in Women with a Single Oral Dose of Amoxicillin

1974 ◽  
Vol 129 (Supplement 2) ◽  
pp. S258-S261 ◽  
Author(s):  
M. J. Gurwith ◽  
S. McGinnis ◽  
A. R. Ronald ◽  
R. Henry
Keyword(s):  
Oral Dose ◽  
Single Oral Dose ◽  
Uncomplicated Gonorrhea
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