Cefcapene Research Articles

Assessment of the Safety of Exposure to Cefcapene Pivoxil during the First Trimester of Pregnancy: A Prospective Cohort Study in Japan.

Cefcapene pivoxil hydrochloride is an antibiotic often used by women who are or may be pregnant. However, the safety of exposure to it during the first trimester of pregnancy has not been assessed. In this study, we aimed to clarify the effects of exposure during the first trimester of pregnancy on maternal and fetal outcomes. Data were obtained from pregnant women who were counseled on drug use during pregnancy at two Japanese facilities from April 1988 to December 2017. The incidence of major malformations in singleton pregnancy was compared between neonates born to women who took cefcapene pivoxil hydrochloride (n = 270) and control drugs (n = 1594) during their first trimester. The adjusted odds ratio of the incidence of major malformations was calculated using multivariate logistic regression analysis adjusted for smoking during pregnancy and maternal age. The incidence of major malformations was 2.6% in the cefcapene pivoxil hydrochloride group and 1.8% in the control group. There were no significant differences in the incidence between the cefcapene pivoxil hydrochloride and control groups (adjusted odds ratio: 1.48 [95% confidence interval: 0.64-3.42], p = 0.36). This prospective cohort study showed that exposure to cefcapene pivoxil hydrochloride during the first trimester of pregnancy was not associated with increased risk of major malformations in infants. Our findings will help healthcare providers in choosing appropriate medicines.

Efficacy, safety, and tissue penetration of solithromycin in Japanese patients with otorhinolaryngological infections

ObjectiveTo assess the efficacy, safety, and tissue penetration of solithromycin for the treatment of otorhinolaryngological infections, we conducted three studies: a tissue penetration study with patients scheduled to undergo otorhinolaryngological tissue removal, an open-label study comprising patients with otitis media, pharyngitis, laryngitis, and tonsillitis, and a non-inferiority study compared with high-dose cefcapene-pivoxil (CFPN-PI). MethodsTissue penetration study; 17 patients with chronic rhinosinusitis, chronic otitis media, chronic tonsillitis, or palatine tonsillar hypertrophy, who required resection or removal of their tissue, were enrolled. Solithromycin was administered orally, and otorhinolaryngological tissues were collected 3.5–6 h after drug administration; blood was collected within 15 min before and after drug administration. The collected tissues and blood concentrations were measured at a central laboratory. Open-label study; 55 patients who were diagnosed with acute otitis media, laryngopharyngitis, or tonsillitis were enrolled. Solithromycin was administered orally 800 mg on Day 1, while on days 2–7, 400 mg of the drug was administered once daily. The primary endpoint is the clinical response at Test-of-Cure (TOC: 5–10 days after completion) Non-inferiority study; 283 patients with acute rhinosinusitis or acute exacerbation of chronic rhinosinusitis were randomized into either the solithromycin group or CFPN-PI group. Solithromycin was administered 800 mg once daily on Day 1 and 400 mg once daily while on Days 2–7 in solithromycin group, and CFPN-PI was administered 150 mg three times a day while on Days 1–7 in CFPN-PI group. The primary endpoint is the clinical response at TOC. ResultsIn the tissue penetration study, the tissue concentration ratios (tissue concentration/plasma concentration) of solithromycin were 4.19 in the sinonasal mucosa, 1.33 in the middle ear mucosa, and 6.12 in the palatine tonsil tissue. In the open-label study, the efficacy rates at the TOC were 97.0 % for acute otitis media, 100 % for laryngopharyngitis, and 81.8 % for tonsillitis. In the non-inferiority study comprising patients with rhinosinusitis, the efficacy rate at the TOC was 87.7 % for solithromycin and 89.7 % for CFPN-PI. The difference in the efficacy rate (95 % confidence interval) was -2.0 % (-9.4 % to 5.4 %), verifying the non-inferiority of solithromycin to CFPN-PI. The most common adverse events in patients administered solithromycin were diarrhea (20.7 %), nausea and nasopharyngitis (3.6 %,), pharyngitis and elevated hepatic function test results (3.1 %), and abnormal hepatic function (2.1 %). ConclusionBased on the findings, it is suggested that solithromycin is useful for the treatment of otorhinolaryngological infections.

Cefcapene pivoxil-induced hypocarnitinemic hypoglycemia in elderly man with subclinical ACTH deficiency: a case report

BackgroundDrug-induced hypocarnitinemia has been noted as a cause of hypoglycemia in children. However, adult cases are extremely rare and pre-existing conditions (including endocrine disorders and frailty) have been suggested to be involved. Hypoglycemia due to drug-induced hypocarnitinemia is quite rare, and there were few reports of pivoxil-containing cephalosporin (PCC)-induced hypocarnitinemia in adults.Case presentationWe present a case of an 87-year-old man with malnutrition, and frailty. He developed severe hypoglycemia with unconsciousness after taking cefcapene pivoxil hydrochloride, one of PCC, and hypocarnitinemia was diagnosed. Despite levocarnitine administration, asymptomatic mild hypoglycemia had persisted. Subsequent investigation revealed subclinical ACTH deficiency due to empty sella, which played a key role to maintain mild hypoglycemia as underlying disorder, and PCC-induced hypocarnitinemia triggered severe hypoglycemia. The patient responded to hydrocortisone therapy.ConclusionsWe need to be aware of the facts that PCC can induce severe hypocarnitinemic hypoglycemia in elderly adults associated with frailty, malnutrition, and subclinical ACTH syndrome.

Evaluation of the strategies to reduce third-generation oral cephalosporins in dentistry at a Japanese academic hospital: An interrupted time series analysis.

Third-generation oral cephalosporins, especially cefcapene-pivoxil (CFPN-PI), have been used frequently in the Japanese dental field. In December 2014 and April 2016, the newly published clinical guidelines recommended the use of amoxicillin (AMPC). Thus, it is important to evaluate the impact of these guidelines on the prescription profiles of prophylactic antibiotics, clinical outcomes and cost-effectiveness of antibiotics. We conducted a retrospective study to analyse an interrupted time series analysis from April 2013 to March 2020 at the Department of Dentistry of Hokkaido University Hospital. A segmented regression model was used to estimate the changes in the incidence of infectious complications following tooth extraction. Prescribed antibiotic data were evaluated via days of therapy (DOT). Antibiotic costs were calculated in terms of the Japanese yen (JPY). We identified 17,825 eligible patients. The incidence rates of infectious complications (SSI+dry socket) and SSI after tooth extraction were 3.2% and 2.2%, respectively, during the entire period. The extraction of impacted third molars corresponded to 5.0% and 3.4%, respectively. However, their incidence rates were not significantly different during this period. The use of prophylactic antibiotics and antibiotic cost showed consistent trends following the implementation of guidelines. The mean DOT of CFPN-PI decreased (ranging from 4893.6 DOTs/1000 patients [March 2013 to November 2014] to 3856.4 DOTs/1000 patients [December 2014 to March 2016]; p<0.001, and from 3856.4 DOTs/1000 patients [December 2014 to March 2016] to 2293.9 DOTs/1000 patients [April 2016 to March 2020]; p<0.001). In contrast, the mean DOT of AMPC was found to be increased (ranging from 1379.7 DOTs/1000 patients [March 2013 to November 2014] to 3236.3 DOTs/1000 patients [December 2014 to March 2016]; p<0.001, and from 3236.3 DOTs/1000 patients [December 2014 to March 2016] to 4597.8 DOTs/1000 patients [April 2016 to March 2020]; p<0.001). The mean monthly cost was decreased (ranging from 905.3JPY [March 2013 to November 2014] to 788.7JPY [December 2014 to March 2016]; p=0.003, and from 788.7JPY [December 2014 to March 2016] to 614.0JPY [April 2016 to March 2020]; p<0.001). After December 2014, prophylactic antibiotics were switched from CFPN-PI to AMPC, and the incidence rate of infectious complications was not significantly different over time. However, changing antibiotics is useful from a cost-effectiveness perspective.

Efficacy of perioperative oral cefcapene pivoxil for surgical site infection prophylaxis in patients with urological diseases

Efficacy of perioperative oral cefcapene pivoxil for surgical site infection prophylaxis in patients with urological diseases

The Significance of Age and Causative Bacterial Morphology in the Choice of an Antimicrobial Agent to Treat Acute Uncomplicated Cystitis.

Differentiating patients by age and causative bacterial morphology might aid in making the appropriate choice of antimicrobial agent when treating acute uncomplicated cystitis. In this retrospective analysis, the non-susceptibility rates of the causative bacteria to cefcapene-pivoxil (CFPN-PI) and levofloxacin (LVFX) were determined after dividing patients with acute uncomplicated cystitis by age group (15-54 and 55-74 years old) and by bacterial morphology: gram-positive cocci (GPC) or gram-negative rod (GNR). The overall non-susceptibility rates for CFPN-PI and LVFX were 19.4% and 15.3%, respectively. When the subjects were divided by age, only the non-susceptibility rate for LVFX in the younger group significantly decreased (to 8.7%). When the groups were divided by both age and bacterial morphology, the younger GNR group had non-susceptibility rates of 6.9% to CFPN-PI and 7.8% to LVFX, whereas the younger GPC group showed 10.2% non-susceptibility to LVFX. The older GNR group showed 9.8% non-susceptibility to CFPN-PI, while the older GPC group showed 7.2% non-susceptibility to LVFX. All the non-susceptibility rates were lower than 10.2% in the sub-divided groups. Differentiating patients by age and the morphology of causative bacteria can aid in making the appropriate choice of antimicrobial agent and may improve treatment outcomes in patients with acute uncomplicated cystitis.

Does prophylactic antibiotic administration for tooth extraction affect PT-INR in patients taking warfarin?

BackgroundVarious antibiotics and analgesics have been reported to interact with warfarin. Reports that investigate the effects of medication taken for just a few days during tooth extraction on the prothrombin time-international normalized ratio are rare.MethodsA total of 110 patients receiving long-term stable warfarin therapy underwent tooth extraction without interruption of warfarin treatment. INR values were measured 1 month before the tooth extraction, the day of the extraction, and 1 week after the extraction. We investigated the changes in INR values between the day of extraction and 1 week after extraction, as well as the various risk factors for increases in INR values.ResultsBefore and after tooth extraction, the number of patients taking cefcapene pivoxil, amoxicillin, and azithromycin was 57, 36, and 8, respectively. Nine patients were administered ampicillin before tooth extraction and received amoxicillin after their tooth extraction. One week after tooth extraction, the INR values increased beyond the therapeutic range in 3 out of 110 patients (2.7%). The INR values before tooth extraction in these three patients were close to 3.0. The INR value increased by more than twice as much in 1 out of 110 patients (0.9%).ConclusionOur results suggest that prophylactic antibiotic administration has little effect on INR values when patients on stable warfarin therapy undergo tooth extraction. Surgeons have to take attention if the patients whose INR values are close to 3.0 before their extraction.

Poor penetration of cefcapene into aqueous humor after oral administration of cefcapene pivoxil to patients undergoing cataract surgery

ObjectivesStudies on the penetration of orally administered cephalosporins to the aqueous humor are scarce. Therefore, in this study, we determined the concentration of cefcapene, a third-generation cephalosporin administrated orally as pivalate ester (cefcapene pivoxil), in the aqueous humor of patients undergoing cataract surgery to assess its potential for preventing postoperative endophthalmitis. MethodsForty-four patients were administered a single dose of 100 mg cefcapene pivoxil preoperatively. Blood and aqueous humor samples were obtained at the time of surgery, and cefcapene concentrations were measured using ultra-performance liquid chromatography with tandem mass spectrometric detection. ResultsThe samples were obtained from 41 eyes of 39 patients (two patients underwent surgery in both eyes). The median cefcapene concentrations in the aqueous humor after 1–2 h, 2–3 h, and later than 3 h were 8.3, 18.4, and 23.7 ng/mL, respectively. The median cefcapene concentrations in serum after 1–2 h, 2–3 h, and later than 3 h were 198.5, 287.2, and 170.3 ng/mL, respectively. Aqueous humor penetration of cefcapene after 1–2 h, 2–3 h, and later than 3 h was 4.1, 7.9, and 13.5% respectively. ConclusionsAqueous humor penetration of orally-administered cefcapene pivoxil in patients undergoing cataract surgery was poor. Therefore, cefcapene pivoxil was unlikely to be effective for preventing endophthalmitis after cataract surgery.

Prevalence of inappropriate antibiotic prescriptions after the great east Japan earthquake, 2011

Few studies have investigated the appropriateness of antibiotic use in postdisaster settings. We retrospectively evaluated clinical databases on health care delivered at clinics near shelters set up after the Great East Japan Earthquake, 2011. We defined appropriate, acceptable, and inappropriate antibiotic use for each diagnostic category, by applying and adopting precedent studies and clinical guidelines. From March to July, 2011, a total of 23,704 clinic visits occurred at 98 shelters with 7934 residents. Oral antibiotics were prescribed a total of 2253 times. The median age of the patients was 48.5 years old (range 0–97), and 43.7% were male. Of 2253 antibiotic prescriptions, 1944 were judged to be inappropriate (86.3% 95% CI 84.8%–87.7%). The most prescribed antibiotic was clarithromycin (646 times, 28.7%), followed by cefcapene pivoxil (644 times, 28.6%), levofloxacin (380, 16.9%), cefdinir (194, 8.6%), and cefditren pivoxil (98, 4.4%). The most frequent diagnosis for which antibiotics were prescribed was upper respiratory infection (URI, 1040 visits, 46.2%), followed by acute bronchitis (369, 16.4%), pharyngitis (298, 13.2%), traumatic injuries (194, 8.6%), acute gastroenteritis (136, 6.0%), urinary tract infections (UTIs, 123, 5.5%), and allergic rhinitis (5.1%). The majority of antibiotics prescribed at clinics after the Great East Japan Earthquake was inappropriate. Significant improvement of the use of antibiotics in postdisaster settings should be sought immediately in Japan.

Stereoselective or Exclusive Synthesis of Ethyl (Z)-2-(2-Substituted-thiazol-4-yl)pent-2-enoates from Ethyl (E/Z)-2-(2-Bromoacetyl)pent-2-enoate

A stereoselective or exclusive approach to a series of ethyl (<i>Z</i>)-2-(2-substituted-thiazol-4-yl)pent-2-enoates from ethyl (<i>E</i>/<i>Z</i>)-2-(2-bromoacetyl)pent-2-enoate and thioureas or thioamides was reported in good yields. This approach involves a quaternary carbon stereocontrolled <i>cis</i>-configuration formation, and opportunely blocking a potential <i>E</i>/<i>Z</i> isomerization. The practical applicability was highlighted by the synthesis of (<i>Z</i>)-2-(2-<i>tert</i>-butoxycarbonylaminothiazol-4-yl)pent-2-enoic acid, a commercially important side-chain material of cefcapene pivoxil, in a two-step procedure.

各種臨床分離株の経口セフェム系薬に対する薬剤感受性とPharmacokinetics/Pharmacodynamics (PK/PD) 理論を用いたその有効性について

We compared the antimicrobial activity of commercially available oral cephem agents, cefaclor (CCL), cefroxadine (CXD), cefdinir (CFDN), cefixime (CFIX), cefpodoxime (CPDX), cefteram (CFTM), cefcapene (CFPN), and cefditoren (CDTR), against Streptococcus pneumoniae, Haemophilus influenzae, Escherichia coli, Klebsiella pneumoniae, Staphylococcus aureus, Streptococcus agalactiae, Streptococcus pyogenes, and ESBL-producing bacteria isolated from clinical materials in Kansai Medical University Hospital between 2002 and 2003. Based on the Pharmacokinetics/Pharmacodynamics (PK/PD) theory, we determined the concentration of each agent at which the time above MIC (TAM) value was 40% or more, and calculated the rate of efficacy against each type of bacteria. In S. pneumoniae strains, the MIC(50,80,90) values of CDTR were 0.25, 0.5, and 0.5 microg/ml, respectively, lower than those of the other agents, demonstrating the most potent antimicrobial activity. However, the efficacy rate for CDTR calculated based on the PK/PD theory was 58.5%. CFTM showed the highest efficacy rate (66.1%). In H. influenzae strains, the antimicrobial activity of CDTR was most potent, followed by that of CFTM and that of CFPN/CFIX. The MIC90 value of CDTR was lowest (0.25 microg/ml), followed by that of CFTM (0.5 microg/ml). The efficacy rate for CDTR was 100%. This result supports that CDTR frequently eradicates H. influenzae. In E. coli strains, the MIC90 values of the above agents, excluding CCL and CXD, ranged from 0.5 to 1 microg/ml. The antimicrobial activity of CFIX against K. pneumoniae was most potent, followed by that of CFDN/CPDX and that of CFTM. In ESBL-producing bacteria, most agents showed an MIC90 value of more than 4 microg/ml. In S. agalactiae and S. pyogenes strains, all of the agents showed satisfactory MIC values. In methi- cillin-sensitive Staphylococcus aureus (MSSA) strains, CFDN and CXD showed a high efficacy rate, whereas the efficacy rates for the other agents were low. The frequent use of oral agents has increased the number of cephem-resistant bacteria. ESBL-producing bacteria become highly resistant, and the presence or absence of response can be readily evaluated. However, when a mutation of penicillin-binding protein (PBP) occurs, drug resistance is less marked. Therefore, it is difficult to evaluate the treatment response in many cases. In S. pneumoniae strains, the efficacy rates for all of the agents were low in the evaluation using the PK/PD theory, suggesting that a dose higher than the standard dose should be established. Thus, in the future, the efficacy should be evaluated based on the PK/PD theory, appropriate antimicrobial treatment should be administered, and the administration method that does not increase the number of resistant bacteria must be established.

小児呼吸器感染症患者におけるcefcapene pivoxil小児用細粒の遊離型薬剤濃度でのPK/PDブレイクポイントと臨床効果・細菌学的効果

小児呼吸器感染症患者におけるcefcapene pivoxil小児用細粒の遊離型薬剤濃度でのPK/PDブレイクポイントと臨床効果・細菌学的効果

Possible Cefcapene Pivoxil- or Clarithromycin-Induced Severe Hyperglycemia in a Patient With Type 2 Diabetes: A Case Report

There are various reasons for the deterioration of glycemic control observed in patients with diabetes, one of which is drug-induced hyperglycemia. Antibiotics, especially the fluoroquinolones, have been reported to be associated with glucose disturbances. However, induction of hyperglycemia by cephem or macrolide antibiotics has rarely, if ever, been reported. Here, we report the case of possible antibiotics-induced severe hyperglycemia in a patient with type 2 diabetes. A 67-year-old Japanese diabetic man, who was not using oral hypoglycemic agents or insulin but whose condition was controlled with diet and exercise, presented at an otolaryngology clinic with nasal discharge and rhinorrhea. His glycosylated hemoglobin (HbA1c) level had been stable at 6.6-7.2% for several years. He was diagnosed with acute sinusitis and given an oral cephem antibiotic, cefcapene pivoxil, for 1 week. His otolaryngeal symptoms were slight and disappeared soon. Thereafter, therapy was switched to a macrolide antibiotic, clarithromycin, for 3 weeks. Twenty-five days after the initiation of antibiotic therapy, severe hyperglycemia was pointed out; his random serum glucose and HbA1c levels were 29.4 mmol/L and 10.6%, respectively. The patient required insulin and oral hypoglycemic agent therapy. The Naranjo probability scale suggests that the relationship between the administration of cefcapene pivoxil or clarithromycin and the patient’s severe hyperglycemia might be possible. To the best of our knowledge, there has been no previous report of a deterioration in glycemic control in a patient with diabetes administered a cephem (cefcapene pivoxil) or macrolide (clarithromycin) antibiotic. Considering the global prescription of cephem and macrolide antibiotics, awareness of the fact that some patients are at high risk for impaired glucose tolerance is important when prescribing antibiotics. Further studies are warranted to determine the incidence rate of hyperglycemia among patients with diabetes who are administered cephem and macrolide antibiotics. J Med Cases. 2013;4(6):416-419 doi: https://doi.org/10.4021/jmc1274w

Pharmacokinetic Characteristics of Cefcapene Pivoxil Hydrochloride after Single Oral Administration in Healthy Korean Subjects

Background: Cefcapene pivoxil hydrochloride (CFPN-PI) is an oral ester cephalosporin antibiotic with a broad spectrum. In this study, we investigated the pharmacokinetics (PK) and tolerability of CFPN-PI following single oral administration in healthy Korean subjects. Methods: An open‐label, dose‐escalation, parallel group study was conducted in 18 healthy male volunteers. A single dose of CFPN-PI was administered to 6 subjects in each treatment group of 100, 150 and 200 mg. Serial blood and urine samples were collected up to 12 h and 24 h after dosing, respectively. Plasma and urine concentrations of cefcapene were measured by HPLC-UV. PK parameters were estimated using non-compartmental analysis. For the safety evaluation, adverse event monitoring, clinical laboratory tests and physical examination were performed throughout the study. Results: Median values of time to peak plasma concentration were observed around 1.5 to 2.0 h. Maximum plasma concentrations (Cmax) were 1.04 ± 0.22, 1.24 ± 0.46 and 1.56 ± 0.43 mg/L (mean ± SD), and area under the plasma concentration‐time curve (AUCinf) were 2.94 ± 0.46, 3.97 ± 1.28 and 4.70 ± 1.19 h*mg/L in 100, 150 and 200 mg dose groups, respectively. The differences of dose‐normalized Cmax and AUCinf among three groups were not statistically significant. The fractions of drug excreted in urine unchanged were 31.5 % 42.9 %. There were no serious adverse events or clinically significant abnormalities related to CFPN-PI. Conclusion: CFPN-PI was well tolerated with single oral administration and showed a linear PK property within 100 200 mg in healthy Korean male subjects.

Determination of cefcapene acid by LC–MS and their application to a pharmacokinetic study in healthy Chinese volunteers

Simple, rapid and specific liquid chromatography–mass spectrometry (LC–MS) methods have been developed and validated for the quantification of cefcapene acid in human plasma and urine. Plasma samples were simply pretreated with methanol for deproteinization. Urine samples were briefly diluted with methanol–water (50:50, v/v), and centrifuged to remove large particles. Chromatographic separation was performed on a Hedera ODS-2 column. For the plasma assay, the isocratic mobile phase consisted of 35% solvent A (Methanol) and 65% solvent B (10mM ammonium acetate buffer solution containing 0.2% folic acid) with a flow rate of 0.3mL/min. For the urine assay, the isocratic mobile phase consisted of 30% solvent A (Methanol) and 70% solvent B (10mM ammonium acetate buffer solution containing 0.2% folic acid) with a flow rate of 0.3mL/min. The assays were linear over the concentration ranges of 0.03–5μg/mL in plasma and 0.1–400μg/mL in urine, and were successfully applied to a pharmacokinetic study after single and multiple oral administrations of cefcapene pivoxil hydrochloride tablets in healthy Chinese volunteers.

Stability-Indicating HPLC Method for the Determination of Cefcapene Pivoxil

The stability-indicating LC assay method was developed and validated for quantitative determination of cefcapene pivoxil in the presence of degradation products formed during forced degradation studies. An isocratic RP-HPLC method was developed with a Lichrospher RP-18 (250 mm × 4.6 mm, 5 μm) column and the mobile phase composed of 45 volumes of acetonitrile and 55 volumes of mixture composed of citric acid 10 mmol L−1 and potassium chloride 18 mmol L−1. The flow rate of the mobile phase was 1 mL min−1. Detection wavelength was 270 nm and temperature was 30 °C. Cefcapene pivoxil, similar to other cephalosporins, was subjected to stress conditions of degradation in aqueous solutions including hydrolysis, oxidation, and thermal degradation. The method was validated with regard to linearity, accuracy, precision, selectivity, and robustness. The method was applied successfully for the determination of cefcapene pivoxil during kinetic studies in aqueous solutions (pH and thermal degradation) and in solid state (oxidative, thermal, and radiolytic degradation).

A Practical Synthesis of Cefcapene Pivoxil

Cefcapene pivoxil monohydrochloride monohydrate, a broad spectrum third-generation cephalosporin for oral administration, was prepared by reacting three centers of 7β-amino-3-(hydroxymethyl)cephalosporinic acid (7-HACA), derived from 7β-aminocephalosporanic acid. The coupling of 7-HACA and (Z)-2-[2-(Boc-amino)thiazol-4-yl]pent-2-enoic acid, followed by carbamylation with chlorosulfonyl isocyanate, and precipitation with diisopropylamine gave the key intermediate, in which thiazole side chain and carbamoyl group had been introduced into the 7-amino and 3-hydroxymethyl groups of 7-HACA, respectively, in a continuous procedure. Afterwards, the intermediate was esterified with pivaloyloxymethyl iodide to complete the modification of the C4 carboxy group affording Boc-cefcapene pivoxil, from which the desired product was finally obtained by an economical Boc removal and successive formation of the hydrochloride in 36% overall yield on a decagram scale. This synthesis promises an easy entry to cefcapene pivoxil monohydrochloride monohydrate with convenient manipulation, simple isolation, and good yields; it is of potential value for production on an industrial scale.

Prevention of Infectious Complication and Its Risk Factors after Urological Procedures of the Upper Urinary Tract

Background:Invasive upper urinary tract procedures such as retrograde pyelography (RP) or single (S-J) or double J (D-J) stenting are commonly performed to assess or treat ureteral strictures. Urinary tract infection (UTI) can result after such procedures, and prophylactic antimicrobial administration (PAA) may be necessary. This study investigated infectious complications and risk factors, focusing on PAA. Methods:We studied antimicrobial prevention in 353 upper urinary tract examinations or treatments. Procedures included S-J or D-J installation or exchange, RP and percutaneous nephrostomy. We investigated PAA and the occurrence of febrile infectious complications with respect to each procedure and attempted to find the risk factors. Results:Levofloxacin was used in 149 subjects (42.2%) and cefcapene pivoxil in 114 cases (32.3%). There were 16 febrile infectious complication cases (4.5%) after procedures, and pyuria or hydronephrosis prior to examination or treatment was an independent risk factor for infectious complication (p < 0.05) as well. Conclusions:These data showed that it is necessary to evaluate the risk factors before urological procedures of the upper urinary tract and to offer a definite preventive methodology according to these risk factors for the establishment and update of guidelines.

小児感染症患者におけるcefcapene pivoxil小児用細粒の有効性, 安全性および薬物動態の検討

小児感染症患者におけるcefcapene pivoxil小児用細粒の有効性, 安全性および薬物動態の検討

A Randomized, Double-blinded, Open Label Study of the Efficacy and Safety of Cefcapene Pivoxil and Amoxicillin·Clavulanate in Acute Presumed Bacterial Rhinosinusitis

ObjectivesCurrently established first line therapy of acute (presumed bacterial) rhinosinusitis (ARS) consists of 10 to 14 days of oral amoxicillin or cephalosporins. This study compared the clinical efficacy and tolerance of cefcapene pivoxil (CP) and amoxicillin-clavulanate (AMC) in patients with ARS.MethodsA randomized, open labeled, double-blinded trial of ARS patients over 15 years of age was performed. Patients diagnosed with ARS received paranasal sinus X-rays and nasal endoscopies and 2 weeks of either CP (150 mg, 3 times/ day) or AMC (625 mg, amoxicillin 500 mg, 3 times/day). All patients revisited the clinic on days 7, 14, and 28 for evaluation of changes in symptoms, endoscopy, and monitoring of any adverse reactions. Demographics, clinical characteristics and drug efficacy were also compared between the two groups.ResultsAmong the 60 initially enrolled patients (CP 30, AMC 30), 5 patients in the CP group and 6 in the AMC group were excluded due to poor compliance. There were no significant differences in demographic data including age, sex, initial signs and symptoms, endoscopic and X-ray findings between the two groups. Rates of improvement after 2 weeks were 96% and 95.8% in the CP and AMC group, respectively. Sinus symptoms were changed significantly after 2 and 4 weeks, however, there was no difference between groups (P=0.41). The most common adverse reaction was gastrointestinal complication, diarrhea occurred in 1 patient in the CP group and 6 in the AMC group (P=0.04).ConclusionCP and AMC were both effective in treating ARS. The difference of treatment outcome was not found between the two groups, however, gastrointestinal complications were less prevalent in the CP group.