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Journal of Graduate Medical Education Apr 2017
Topics: Alprostadil; Internship and Residency; Pipemidic Acid
PubMed: 28439366
DOI: 10.4300/JGME-D-16-00850.1 -
Archives of Pharmacal Research Jun 2018This article describes the synthesis and antimicrobial activity evaluation of new pipemidic acid derivatives. New compounds were obtained on the basis of Mannich...
This article describes the synthesis and antimicrobial activity evaluation of new pipemidic acid derivatives. New compounds were obtained on the basis of Mannich reaction of 4,5-disubstituted 1,2,4-triazole-3-thiones with pipemidic acid. Antimicrobial tests revealed high antibacterial activity of obtained derivatives. Gram-negative rods belonging to Enterobacteriaceae family were particularly most sensitive to new pipemidic acid derivatives. Synthesized compounds exhibited very strong activity towards Proteus mirabilis ATCC 12453, Salmonella typhimurium ATCC 14028 and Escherichia coli ATCC 25922. The minimum inhibitory concentrations of new pipemidic acid derivatives which inhibited the growth of these bacteria were 0.98-7.81 µg/ml, 0.98-7.81 µg/ml and 0.98-3.91 µg/ml, respectively. The antibacterial activity of newly synthesized pipemidic acid derivatives in many cases was far better than the activity of substances used as positive controls (nitrofurantoin, cefuroxime, ampicillin and pipemidic acid).
Topics: Anti-Bacterial Agents; Gram-Negative Bacteria; Microbial Sensitivity Tests; Pipemidic Acid; Thiones; Triazoles
PubMed: 29619676
DOI: 10.1007/s12272-018-1025-3 -
Acta Medica Indonesiana Jul 2016to evaluate the analgesic effect, the side effects and the safety of analgesics following endoscopic urological procedure. (Randomized Controlled Trial)
Randomized Controlled Trial
Effects of Pipemidic Acid, Phenazopyridine HCL and Sodium Diclofenac on Pain Perception Following Endoscopic Urological Surgery: Double-blinded Randomized-Controlled Trial.
AIM
to evaluate the analgesic effect, the side effects and the safety of analgesics following endoscopic urological procedure.
METHODS
eighty patients who underwent endoscopic urological surgery at Kardinah Hospital, Tegal from June to July 2015 were divided into four groups. The experimental group was administered analgesic for 4 days pipemidic acid (A) 400 mg bid, or phenazopyridine (B) 200 mg tid, or sodium diclofenac (C) 50 mg bid and the control (D) group was administered placebo tid for 4 days. The analgesic effects were assessed using Visual Analog Scale (VAS). Association between variables was assessed using Cramers V and Kruskall Wallis.
RESULTS
the endoscopic urological procedures consisted of 30 patients for URS, 6 patients for lithotripsy, 17 patients for TURP, 24 patients for removal JJ stent and 3 patients for cystoscopy. The mean age of group A, B, C and D (control) was 50.1 (13.7), 50.7 (14.8), 49.1 (13.4), and 49.6 (14.3) years, respectively, and follow-up period was 7 days. The VAS score in all experimental groups was less than control group on day 1 to 7 following endoscopic urological procedures (p<0.05). In the experimental group, there was no difference between groups B and C (p>0.05). Group A demonstrated a more favourable analgesic effect than B and C (p<0.05). No serious side effects were detected in any of the cases.
CONCLUSION
we conclude that oral analgesics are effective for pain relief following endoscopic urological surgery. Pipemidic acid was found to have a superior analgesic effect than phenazopyridine HCl and sodium diclofenac.
Topics: Anesthetics, Local; Anti-Infective Agents, Urinary; Anti-Inflammatory Agents, Non-Steroidal; Diclofenac; Double-Blind Method; Endoscopy; Female; Humans; Male; Middle Aged; Pain Perception; Phenazopyridine; Pipemidic Acid; Prospective Studies; Urologic Surgical Procedures
PubMed: 27840352
DOI: No ID Found -
Environmental Science & Technology Jul 2020Manganese oxides have been proposed as promising geomedia to remove trace organic contaminants in both natural soils and artificial infiltration systems. Although...
Manganese oxides have been proposed as promising geomedia to remove trace organic contaminants in both natural soils and artificial infiltration systems. Although MnO-based redox processes have been largely investigated, little is known on the effects of water flow and dissolved Mn on manganese-mediated redox reactions in saturated porous media. Here, we have demonstrated that the reactive transport of a widely used quinolone antibiotic, pipemidic acid (PIP), in MnO-coated sand (MCS) columns is altered by the presence of dissolved Mn, generated as reduced ions or present in inflow solution. Decreasing the flow rate or flow interruption facilitated oxidation reactions and generated redox byproducts (Mn and PIP). However, preloading of MCS columns with dissolved Mn led to suppressed reactivity with PIP. When PIP and Mn are simultaneously injected, competition between PIP and Mn for binding at the edge sites takes place during the initial kinetic phase of reaction, while at a later breakthrough time Mn will occupy both edge and vacancy sites due to the continuous supply of Mn. We also developed a reactive transport model that accounts for adsorption kinetics to predict changes in transport behavior of antibiotics in the presence of different doses of dissolved Mn. This work has strong implications for an accurate assessment of the reactivity of manganese oxides used as engineered geomedia for quinolone remediation and in developing transport models of antibiotics in natural systems.
Topics: Adsorption; Manganese; Manganese Compounds; Oxidation-Reduction; Oxides; Pipemidic Acid
PubMed: 32470299
DOI: 10.1021/acs.est.0c01474 -
International Journal of Molecular... Jan 2019Pipemidic acid (HPPA) is a quinolone antibacterial agent used mostly to treat gram-negative infections of the urinary tract, but its therapeutic use is limited because...
Pipemidic acid (HPPA) is a quinolone antibacterial agent used mostly to treat gram-negative infections of the urinary tract, but its therapeutic use is limited because of its low solubility. Thus, to improve drug solubility, natural cyclodextrins (CDs) are used for their ability of including guest molecules within their cavities. The aim of this work was to evaluate the antibacterial activity and the preliminary anticancer activity of HPPA included into Heptakis (2,3,6-tri-O-methyl)-β-cyclodextrin (TRIMEB) as a possible approach for a new innovative formulation. The inclusion complex of HPPA with TRIMEB was prepared in solid state by the kneading method and confirmed by FT-IR and powered X-ray diffraction. The association in aqueous solutions of pipemidic acid with TRIMEB was investigated by UV-Vis spectroscopy. Job's plots have been drawn by UV-visible spectroscopy to confirm the 1:1 stoichiometry of the host⁻guest assembly. The antibacterial activity of HPPA, TRIMEB and of their complex was tested on , , and . The complex was able to increase 47.36% of the median antibacterial activity of the free HPPA against (IC = 249 µM vs. 473 µM). Furthermore, these samples were tested on HepG-2 and MCF-7. After 72 h, the median tumoral cytotoxicity exerted by the complex was increased by 78.08% and 94.27% for HepG-2 and MCF-7 respectively, showing a stronger bioactivity of the complex than the single HAPPA.
Topics: Anti-Bacterial Agents; Antineoplastic Agents; Bacteria; Cell Line, Tumor; Cell Survival; Dose-Response Relationship, Drug; Humans; Microbial Sensitivity Tests; Molecular Structure; Pipemidic Acid; Spectroscopy, Fourier Transform Infrared; X-Ray Diffraction; beta-Cyclodextrins
PubMed: 30669399
DOI: 10.3390/ijms20020416 -
Acta Pharmaceutica Sinica. B May 2018Nowadays, biodegradable polymers such as poly(lactic acid) (PLA), poly(D,L-lactic--glycolic acid) (PLGA) and poly(-caprolactone) (PCL) remain the most common...
Nowadays, biodegradable polymers such as poly(lactic acid) (PLA), poly(D,L-lactic--glycolic acid) (PLGA) and poly(-caprolactone) (PCL) remain the most common biomaterials to produce drug-loaded nanoparticles (NPs). Pipemidic acid (PIP) is a poorly soluble antibiotic with a strong tendency to crystallize. PIP incorporation in PLA/PLGA NPs was challenging because of PIP crystals formation and burst release. As PIP had a poor affinity for the NPs, an alternative approach to encapsulation was used, consisting in coupling PIP to PCL. Thus, a PCL-PIP conjugate was successfully synthesized by an original drug-initiated polymerization in a single step without the need of catalyst. PCL-PIP was characterized by NMR, IR, SEC and mass spectrometry. PCL-PIP was used to prepare self-assembled NPs with PIP contents as high as 27% (/). The NPs were characterized by microscopy, DLS, NTA and TRPS. This study paves the way towards the production of NPs with high antibiotic payloads by drug-initiated polymerization. Further studies will deal with the synthesis of novel polymer-PIP conjugates with ester bonds between the drug and PCL. PIP can be considered as a model drug and the strategy developed here could be extended to other challenging antibiotics or anticancer drugs and employed to efficiently incorporate them in NPs.
PubMed: 29881681
DOI: 10.1016/j.apsb.2018.03.008 -
RSC Advances Jun 2018Three new solid complexes of pipemidic acid (Pip-H) with Ru, Pt and Ir were synthesized and characterized. Pipemidic acid acts as a uni-dentate chelator through the...
Three new solid complexes of pipemidic acid (Pip-H) with Ru, Pt and Ir were synthesized and characterized. Pipemidic acid acts as a uni-dentate chelator through the nitrogen atom of the -NH piperazyl ring. The spectroscopic data revealed that the general formulas of Pip-H complexes are [M(L) (Cl) ]·HO ((1) M = Ru, L: Pip-H, = 3, = 3, = 6; (2) M = Pt, L: Pip-NH, = 2, = 4, = 0 and (3) M = Ir, L: Pip-H, = 3, = 3, = 6). The number of water molecules with their locations inside or outside the coordination sphere were assigned thermal analyses (TG, DTG). The DTG curves refer to 2-3 thermal decomposition steps where the first decomposition step at a lower temperature corresponds to the loss of uncoordinated water molecules followed by the decomposition of Pip-H molecules at higher temperatures. Thermodynamic parameters (*, Δ*, Δ* and Δ*) were calculated from the TG curves using Coats-Redfern and Horowitz-Metzeger non-isothermal models. X-ray powder diffraction (XRD), scanning electron microscopy (SEM) and transmission electron microscopy (TEM) techniques were carefully used to assign properly the particle sizes of the prepared Pip-H complexes. The biological enhancement of Pip-H complexes rather than free chelate were assessed against four kinds of bacteria G(+) ( and ) and G(-) ( and ) as well as against the human breast cancer (MCF-7) tumor cell line.
PubMed: 35539728
DOI: 10.1039/c8ra03879a -
Journal of Taibah University Medical... Feb 2021This study aimed to determine the prevalence of urinary tract infections (UTI) in pregnant women and characterise the uropathogenic bacterial strains associated with...
OBJECTIVES
This study aimed to determine the prevalence of urinary tract infections (UTI) in pregnant women and characterise the uropathogenic bacterial strains associated with symptomatic and asymptomatic bacteriuria in Lahore, Pakistan.
METHODS
Between December 2018 and June 2019, we analysed the uropathogenic bacterial strains from midstream urine samples in 80 pregnant women. The age of the pregnant women ranged from 19 to 45 years, and they resided in urban and rural areas. We also recorded socioeconomic factors in this cohort. The isolated strains were phenotypically identified and evaluated for multiple drug resistance (MDR) patterns against recommended antimicrobial drugs.
RESULTS
Of the 80 pregnant women, 65 had UTI, reflecting an 81% prevalence of UTI in women during pregnancy. The majority of participants aged 24-35 years, were multipara, and were in their third trimester. Results showed that 67 uropathogenic bacterial strains belonged to (31%), (23%), (16%), (4%), (4%), (4%), and (3%) genera, as identified using biochemical characterisation. The highest overall resistance of was seen against amoxicillin, pipemidic acid, and ampicillin; for against pipemidic acid, ampicillin, and cefotaxime; and for against ciprofloxacin and cefotaxime. The three strains with the highest MDR were identified using 16S rRNA as strain UA17, strain UA32, and strain UA47.
CONCLUSION
In this study, the MDR uropathogenic strains showed the highest resistance pattern. The alarming signs of MDR uropathogenic infections are infrequently addressed and thus, urgent attention to this matter is essential.
PubMed: 33603638
DOI: 10.1016/j.jtumed.2020.10.010 -
Characteristics and Antibiotic Resistance of Urinary Tract Pathogens Isolated From Punjab, Pakistan.Jundishapur Journal of Microbiology Jul 2015Urinary tract infection (UTI) is deemed the most prevalent infectious disease in that it has now touched the overall incidence of 18/1000 persons per year in the general...
BACKGROUND
Urinary tract infection (UTI) is deemed the most prevalent infectious disease in that it has now touched the overall incidence of 18/1000 persons per year in the general population.
OBJECTIVES
This study sought to determine the characteristics of isolates from patients with UTI and their susceptibility to commonly used antibiotics in Punjab, Pakistan.
PATIENTS AND METHODS
Totally, 1429 urine samples were analyzed from UTI patients for the isolation of uropathogens at Chughtai's Lahore Lab, Lahore, Pakistan, during a period of 14 months. The antimicrobial susceptibility test was performed via the disc diffusion method for the isolates obtained from 392 (26%) positive cultures.
RESULTS
The highest percentage (67%) of isolates was from females in comparison to males (33%). The frequency of Escherichia coli was the highest (62%) in culture-positive urine samples, followed by E. faecalis (15%), Candida (14%), Pseudomonas (6%), Klebsiella spp. (1%), Proteus (1%), and Staphylococcus aureus (1%). E. coli was highly resistant to antimicrobial drugs, viz. cephalexin (95%), cephradine (95%), pipemidic acid (92%), amikacin (91%), and nalidixic acid (91%). Most of the routine β-lactam antibiotics like amoxicillin/clavulanic acid, ampicillin, and aztreonam were also ineffective against E. coli, with resistance rates of 84%, 84%, and 72%, correspondingly. This pathogen showed maximum susceptibility (97%) against three drugs, namely imipenem, meropenem, and cefoperazone. Piperacillin and fosfomycin also provided significant results against E. coli with respective susceptibility rates of 96% and 90%.
CONCLUSIONS
Our results showed that broad-spectrum antibiotics such as imipenem, meropenem, fosfomycin, cefoperazone/sulbactam, and vancomycin would be the first line and the most effective drugs for the empirical treatment of urinary tract pathogens due to their higher resistance rates against other drugs like cephalexin, cephradine, ciprofloxacin, levofloxacin, and norfloxacin.
PubMed: 26421129
DOI: 10.5812/jjm.19272v2 -
Spectrochimica Acta. Part A, Molecular... Feb 2020The self-association of fluoroquinolones (FQ) in water would play a relevant role in their translocations across lipid membranes. Triplet excited states of these drugs...
The self-association of fluoroquinolones (FQ) in water would play a relevant role in their translocations across lipid membranes. Triplet excited states of these drugs have been shown as reporters of FQ self-association using laser flash photolysis technique. A study using low-temperature phosphorescence technique was performed with quinolone derivatives such as enoxacin (ENX), norfloxacin (NFX), pefloxacin (PFX), ciprofloxacin (CPX, ofloxacin (OFX), nalidixic acid (NLA), pipemidic acid (PPA) and piromidic acid (PRA) to explore emission changes associated with self-associations and to shed some light on the triplet excited state energy (E) discrepancies described in the literature for most of these drugs. The emissions obtained at 77 K in buffered aqueous medium revealed that the amphoteric nature of the quinolones CPX, NFX, PFX, ENX, OFX and PPA must generate their self-associations because a redshift of their phosphorescence maxima is produced by FQ concentrations increases. Hence, this effect was not observed for NLA and PRA or when all quinolones were analysed using ethanol or ethylene glycol aqueous mixtures as glassed solvents. Interestingly, the presence of these organic mixtures produced a blue-shift in the phosphorescence emission maximum of each FQ. Additionally, laser flash photolysis experiments with PRA and the amphoteric quinolone PPA, compounds with the same skeleton but different peripheral substituent, confirm the expected correlations between the amphoteric nature of compounds and their self-associations in aqueous media because the excimer generation was only detected for PPA. Now, the discrepancies described in the literature for the E of FQs can be understood considering that changes of medium polarity or proticity as well as the temperature can considerably modify their E values. Thereby, low-temperature phosphorescence technique, is an effective way to detect molecular self-associations and surrounding changes in quinolones that opens the possibility to evaluate these effects in other drug families.
Topics: Buffers; Dimerization; Fluoroquinolones; Luminescent Measurements; Models, Molecular; Photolysis; Water
PubMed: 31670049
DOI: 10.1016/j.saa.2019.117569