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At least 19 recordsLinked to original sources
PubMedDate not supplied

Effect of nalidixic acid, pipemidic acid and cinoxacin on chondrocyte metabolism in explants of articular cartilage.

Explants of immature bovine articular cartilage were exposed to nalidixic acid, pipemidic acid and cinoxacin at one and ten times the human therapeutic plasma level for 7 days. Only nalidixic acid had significant effects on the chondrocyte metabolism. 20 micrograms/ml nalidixic acid caused an increase of 35S-sulfate incorporation into glycosaminoglycans at day 7. Two hundred micrograms/ml nalidixic acid inhibited the incorporation of 3H-thymidine into DNA. The incorporation of 35S-sulfate into glycosaminoglycans was decreased at day 0, while at day 7 the incorporation had returned to the control value. Pipemidic acid and cinoxacin had no significant effects on either the 3H-thymidine or the 35S-sulfate incorporation.

Animals↗
PubMed2006

Liver initiation activity of norfloxacin but not nalidixic acid, pipemidic acid, and ciprofloxacin on in vivo short-term liver initiation assay in rats.

This study aimed to examine the in vivo initiation activity of the quinolone antimicrobials--nalidixic acid (NA), pipemidic acid (PPA), ciprofloxacin (CPFX), and norfloxacin (NFLX)--by using an in vivo short-term liver initiation assay. Rats were subjected to a two-thirds partial hepatectomy on day 0 and 12 h after completion of this procedure were treated once orally with each quinolone or vehicle. Subsequently, they were fed a basal diet for 14 days and a diet containing 0.015% of 2-acetylaminofluorene for the following 10 days. On day 19, a single oral dose of carbon tetrachloride at 0.8 mL/kg body weight was administered. On day 34, they were sacrificed under ether anesthesia, and liver slices were fixed in 10% neutral buffered formalin for immunohistochemical examination of glutathione S-transferase placental form (GST-P) positive foci. Administration of NFLX resulted in a significant increase in the mean number and area of GST-P positive foci; however, administration of the three other quinolones did not produce any increase. These results suggest that only NFLX has an initiation activity in rats under the conditions used in the present study.

2-Acetylaminofluorene↗
PubMed1989

Protein binding of quinolonecarboxylic acids. I. Cinoxacin, nalidixic acid and pipemidic acid.

Binding of cinoxain (CINX), nalidixic acid (NA) and pipemidic acid (PPA) to serum proteins was investigated by equilibrium dialysis, ultrafiltration and circular dichroism (CD) spectroscopy. CINX and NA were found to bind mainly to albumin in human serum, the latter interacting with the protein about ten times as strongly as CINX at pH 7.4 and 37 degrees C. PPA showed little or no significant binding to human serum albumin (HSA), alpha 1-acid glycoprotein, and globulins, but showed 20-30% binding to protein in human serum. The CD results were suggestive of some weak interaction of PPA with human apotransferrin. Binding of the three drugs to HSA was found to depend on the lipophilicity of their substituents at the 7-position. The degree of protein binding for human, dog and rat sera at 37 degrees C was in the order of NA (92-97%) greater than CINX (68-90%) greater than PPA (20-30%) at drug concentrations of 10-30 micrograms/ml. CINX showed relatively large species dependence in serum protein binding, which seemed to be due to different affinities of this drug to the respective albumins. CINX was found to bind to rat serum albumin as strongly as NA.

Animals↗
PubMed1989

Protein binding of quinolonecarboxylic acids. II. Spectral changes on the interaction of cinoxacin, nalidixic acid and pipemidic acid with human and rat albumins.

The interaction of cinoxacin (CINX), nalidixic acid (NA), and pipemidic acid (PPA) with human and rat serum albumins (HSA and RSA) was studied by UV difference absorption and circular dichroism (CD) spectroscopy. CINX and NA bound to the albumins and generated difference absorption and induced CD (ICD) spectra. The difference absorption spectral data explained reasonably our previous observations that CINX bound to HSA more weakly than NA, but to RSA as strongly as NA. We used a quantity delta epsilon/epsilon, designated as relative molar difference absorbance, at positions corresponding to the longest wavelength peaks in the difference spectra. The quantity was found to correlate linearly with percent bound to both HSA and RSA, but with different slopes, from which the binding site for CINX and NA in RSA was supposed to provide a much more nonpolar environment than that in HSA. The magnitude of ICD bands observed at 371 nm for CINX and at 342-348 nm for NA corresponded to the binding degrees of these drugs to both albumins. Anisotropy factors for the ICD bands at 350-271 nm for CINX and 320-348 nm for NA were approximately similar between HSA and RSA, suggesting a similar ability to generate the ICD spectra in these wavelength regions upon binding to the albumins. Spectral results for PPA in albumin solutions showed little or no binding of this drug to HSA and RSA. PPA existed as a betaine form in neutral solution and its positively charged group acted as an unfavorable factor for binding to both albumins.

Animals↗
PubMed1983

In vitro activity of norfloxacin in synthetic media and human urine compared to that of cinnoxacin, nalidixic acid and pipemidic acid.

Activity of norfloxacin was compared to that of cinnoxacin, nalidixic acid and pipemidi acid in DST-agar and human urine solidified by adding 1.2% agar. Norfloxacin was the most active compound when tested on DST-agar but the MIC values increased from 64 to 128 fold when tested in urine. Other compounds also showed an increase in MIC in urine-agar, but the increase was less marked. MICs for norfloxacin in DST-agar and Müller-Hinton-Agar were similar. Higher concentrations were required in Müller-Hinton-Broth than in Müller-Hinton-Agar.

Agar↗
PubMed1986

Influence of ofloxacin, norfloxacin, nalidixic acid, pyromidic acid and pipemidic acid on human gamma-interferon production and blastogenesis.

Several new quinolone derivatives were investigated for their influence on human lymphocyte blastogenesis and gamma-interferon production following concanavalin A stimulation. All the antimicrobials induced inhibition of lymphocyte DNA synthesis. The gamma-interferon measurements showed that nalidixic acid and norfloxacin have a negative influence on lymphokine production and release.

Adult↗
PubMed1999

[Study of the fluorescence of terbium-pipemidic acid system and the determination of pipemidic acid in urine and serum].

Intramolecular energy transfer occurs in the terbium complex with pipemidic acid (PPA) and the terbium(III) ion fluorescence can be sensitized by PPA. The fluorescence intensity of the Tb3+-PPA system is proportional to the amount of PPA. Accordingly, a fluorimetric method for the determination of PPA is proposed. The characteristics of the method include low background noise, high selectivity and long fluorescence lifetime. The method can be applied to the determination of PPA in urine and serum. The recovery is in the range of 94.6%-102%. Its detection limit and linear range for PPA are 3.6 ng/mL and 5.0 x 10(-8)-4.0 x 10(-6) mol/L, respectively.

Fluorescence↗
PubMed1979

[Antibacterial in-vitro activity of pipemidic acid and nalidixic acid (author's transl)].

The in-vitro activity of nalidixic acid and pipemidic acid was investigated in a combined study in 450 freshly isolated bacterial strains using the agar dilution test. Gram-positive cocci were resistant to both substances except for a few pipemidic acid sensitive staphylococci. Both substances had good antibacterial activity in the gram-negative spectrum. However, the MIC values of pipemidic acid were generally clearly lower than those of nalidixic acid. Only pipemidic acid showed activity against Pseudomonas aeruginosa. Thus the in-vitro results showed that pipemidic acid has clear-cut and valuable advantages for the treatment of urinary tract infections when compared with nalidixic acid.

Anti-Bacterial Agents↗
PubMed1988

Evaluation of the DNA-damaging and mutagenic activity of oxolinic and pipemidic acids by the granuloma pouch assay.

The mutagenic and DNA-damaging activities of oxolinic acid and pipemidic acid were evaluated in the rat granuloma pouch assay. After oral administration at high doses both the chemicals produce DNA alkali-labile sites in granuloma tissue cells, and with oxolinic acid an increase of liver and kidney DNA elution rate was also observed. In contrast, after direct injection into the granuloma tissue, DNA damage was absent. This indicates that DNA lesions are induced by a stable intermediate presumably formed in liver and converted to the ultimate DNA-damaging species in extrahepatic tissues. The simultaneous analysis of 6-thioguanine-resistant cells in the granuloma tissue revealed no statistically significant mutation induction either after local treatment or oral administration. No clear dose-response curve was obtained. However, after oral application in some of the animals an enhanced mutation frequency was detected, and the cloning efficiency of cells exposed to the drugs was reduced even after culturing them for 6 days. The most likely explanation is that functional multilocus mutations are induced which cannot be recovered efficiently at the HGPRT locus.

Animals↗
PubMed1975

Pipemidic acid: absorption, distribution, and excretion.

Pipemidic acid was absorbed well by the oral route. Its peak levels in plasma ranged from 4 to 12 mug/ml at an oral dose of about 50 mg/kg in mice, rats, dogs, monkeys, and men. The protein binding of pipemidic acid was about 20% in dog plasma and about 30% in human serum. Pipemidic acid was distributed to most of the organs and tissues tested at the concentrations comparable to or higher than the plasma level. Its concentrations in bile and urine were much higher than the plasma level. About 25 to 88% of orally administered pipemidic acid was excreted into urine in a bacteriologically active form, the percentage depending on the animals and doses employed. The remainder was excreted into feces in men. The main active principle in vivo was unchanged pipemidic acid itself. The mean lethal dose of pipemidic acid after a single oral dose was more than 16,000 mg/kg in mice. No abnormalities were observed in mice orally receiving pipemidic acid once a day for 4 weeks at doses of 1,000, 2,000, and 4,000 mg/kg per day, and in rats orally receiving the drug once a day for 2 weeks at doses of 400 and 1,600 mg/kg per day.

Adult↗
PubMedDate not supplied

Treatment of acute urinary tract infection in children with pipemidic acid.

Urinary tract infection in children is still an important problem in uronephrology. The disease tends to develop recurrently and results in chronic progressive renal disease in the future. Pipemidic acid is a bactericidal quinolone derivate, with a wide spectrum against gram positive and negative bacteria. Compared with nalidixic acid, pipemidic acid proves to be more effective against Pseudomonas, E. coli, Alkaligenes and Salmonella. Thirty one cases with acute urinary tract infection had been studied descriptively. The etiology revealed as follows: E. coli (45.2%), Alkaligenes (16.2%), Enterobacter (9.6%), Staphylococcus (9.6%), Pseudomonas (9.6%), Paracolon (6.5%), and Proteus (3.3%). Pipemidic acid was administered orally to these patients, 15-20 mg/kg/day divided in 2 equal doses for 10 days. Bacteriological examinations was repeated on the 6th day and 11th day treatment. The result revealed that on the 6th day of treatment, in 27 patients (87.09%) there was no bacteriuria while on the 11th day the urine of 29 patients (93.54%) were sterile. In conclusion, a 5 day treatment of acute urinary tract infection in children with pipemidic acid is quite effective.

Acute Disease↗
PubMed1983

Selective decontamination of the digestive tract by pipemidic acid.

The possible use of pipemidic acid for preventing infections in granulocytopenic patients by selective elimination of the gram-negative rods from the digestive tract was evaluated. Fecal samples were collected before, during, and after therapy from 23 adults who were undergoing treatment of urinary tract infections with pipemidic acid at a dosage of 200 mg orally four times daily for 10 days. The concentration of pipemidic acid in the majority of the stool samples tested was 220 to 600 micrograms/g. However, in 19% of the samples collected on day 5, the concentration was below the detection limit (23 micrograms/ml). Approximately 90% of the fecal samples collected during or shortly after therapy were negative for members of the family Enterobacteriaceae. Resistance of the gastrointestinal tract against colonization by microorganisms from the environment (so-called colonization resistance) remained unimpaired, as measured by the absence of beta-aspartylglycine in the stool.

Adolescent↗
PubMed2004

Determination of pipemidic acid based on flow-injection chemiluminescence due to energy transfer from peroxynitrous acid synthesized on-line.

A flow-injection chemiluminescence (CL) method for the determination of pipemidic acid is described. It is based on energy transfer from excited state peroxynitrous acid to pipemidic acid, in which the excited state peroxynitrous acid is synthesized on-line by the mixing of acid hydrogen peroxide with nitrite in a flow system and the CL is from two excited states of pipemidic acid. The proposed method allows the measurement of pipemidic acid over the range of 2.0 x 10(-7)-2.0 x 10(-5) mol l(-1) . The detection limit is 6.3 x 10(-8) mol l(-1), and the relative standard deviation for 2.0 x 10(-6) mol l(-1) pipemidic acid (n = 9) is 0.9%. This method was evaluated by the analysis of pipemidic acid in pharmaceutical preparations.

Energy Transfer↗