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At least 523 records · Page 29Linked to original sources
PubMed1996

Improved high-performance liquid chromatographic determination of amoxicillin in human plasma by means of column switching.

A highly sensitive and selective HPLC method was developed for the determination of amoxicillin in human plasma. After addition of buffer and internal standard, the sample was ultrafiltered and injected on to a precolumn to remove polar plasma interferences. Detection was effected with a UV detector set at 230 nm. The limit of quantification for amoxicillin was 50.1 ng/ml with an imprecision of 4.2% using 0.25 ml of plasma. Linearity was confirmed over the whole calibration range (25.4-0.0501 micrograms/ml) and the inter-day variation ranged from 2.0 to 4.5%. The method was validated according to GLP guidelines and its suitability was demonstrated by the analysis of several hundred samples in a bioequivalence study. The method can be used to determine pharmacokinetic parameters of amoxicillin in humans after a single oral dose of 500 mg.

Amoxicillin↗
PubMed1989

Staphylococcus saprophyticus in males with symptoms of chronic prostatitis.

Staphylococcus saprophyticus was isolated in 17 percent (12 of 71 men) during one year, but with a peak in August and September to 21 percent in patients referred to the urology department with a suspicion of chronic bacterial prostatitis. Seven of the 12 men had S. saprophyticus in highest number at the prostatic level. Three of these were designated as chronic bacterial prostatitis. In this study the occurrence of S. saprophyticus appears to follow, and possibly depends on, previous antibiotic therapy. S. saprophyticus disappeared without treatment in all cases.

Adult↗
PubMedDate not supplied

Retained foreign body: a fingernail fragment?

A 19-year-old female presented four and one-half months after an occupational injury from a punch-type machine. Exploration revealed a large fragment of her fingernail embedded in the fingerpad. Foreign bodies are commonly encountered in the practice of emergency medicine and failure to localize and remove them can result in significant morbidity. We present a case of a fingernail as a foreign body. Foreign bodies may be difficult to detect despite sophisticated imaging techniques. Although not visualized often, a radiolucent foreign body may be inferred from boney changes. A thorough history regarding mechanism of injury and resultant wound exploration are required. When an adequate wound examination using digital tourniquet control and proper precautions is performed, the majority of foreign bodies will be detected.

Accidents, Occupational↗
PubMedDate not supplied

Antibiotic use in the emergency department: I. The penicillins and cephalosporins.

The penicillins and cephalosporins are beta-lactam agents that provide broad-spectrum antimicrobial coverage pertinent to many infectious diseases diagnosed in the emergency department. These groups of drugs also have in common their classification into subcategories or "generations" that delineate their usefulness in specific clinical scenarios such as infections with Gram-positive or -negative bacteria, Pseudomonas infections, or febrile neutropenic patients. Understanding these subcategories is essential to both efficacious and cost-effective use of these agents. This article reviews the pharmacology and clinical utility of the beta-lactams--including a new class of antibiotics, the carbacephams--for the emergency physician.

Ampicillin↗
PubMed2006

Human oral drugs absorption is correlated to their in vitro uptake by brush border membrane vesicles.

Brush border membrane vesicles (BBMV) were prepared from the rabbit small intestine for testing drug absorption potency through the enterocyte's apical membrane, which is an important compartment for drug oral absorption. Some modifications have been made to the traditional vesicle assay for adapting it to the 96-well plate format. The accumulation of 23 reference drugs was measured, and the data showed a good correlation with human oral absorption with a correlation coefficient R=0.853 (P<0.001), with the exception of a few false positive results. As the measured drug absorption may contain a membrane/protein binding component as well as drug uptake into vesicles, these two fractions can be discriminated by changing extravesicular osmolarity using different mannitol concentrations. This model can be applied for evaluating drug absorption rate/mechanisms, and helping drug selection in early drug research and development.

Acetaminophen↗
PubMed1999

Enzymatic synthesis of beta-lactam antibiotics using penicillin-G acylase in frozen media.

Penicillin-G acylase (EC 3.5.1.11) from Escherichia coli catalyzed the synthesis of various beta-lactam antibiotics in ice at -20 degrees C with higher yields than obtained in solution at 20 degrees C. The initial ratio between aminolysis and hydrolysis of the acyl-enzyme complex in the synthesis of cephalexin increased from 1.3 at 20 degrees C to 25 at -20 degrees C. The effect on the other antibiotics studied was less, leading us to conclude that freezing of the reaction medium influences the hydrolysis of each nucleophile-acyl-enzyme complex to a different extent. Only free penicillin-G acylase could perform transformations in frozen media: immobilized preparations showed a low, predominantly hydrolytic activity under these conditions.

Amoxicillin↗
PubMed1994

A practical approach to antibiotic treatment in women taking oral contraceptives.

Clinical situations that require the use of systemic antibiotic therapy are common. Because millions of women choose oral contraceptives for birth control, the potential for interaction between these drugs frequently has to be considered. We review the available information and present a practical approach for dealing with this situation based on sharing responsibility with an educated patient.

Adult↗
PubMed1991

[Drainage of large breast abscesses with reference to esthetic and functional aspects].

In 11 puerperal women, a breast abscess was treated by drainage from the inframammary fold. Eight patients wished to continue breast feeding. During the healing period, the babies were not breast fed on the operated side. In 3 patients, the skin over the abscess necrotised, resulting in a defect of 1 to 2 cm. In 2 patients, a small seroma had to be punctured after removing the drainage tube. Aesthetic results were judged by the patients as good. Resumation of suckling on the operated side revealed only 15 to 20% milk yield compared to that of the other breast. This treatment meets aesthetic and function-preserving criteria.

Abscess↗
PubMed2000

beta-lactam antibiotics as substrates for OCTN2, an organic cation/carnitine transporter.

Therapeutic use of cephaloridine, a beta-lactam antibiotic, in humans is associated with carnitine deficiency. A potential mechanism for the development of carnitine deficiency is competition between cephaloridine and carnitine for the renal reabsorptive process. OCTN2 is an organic cation/carnitine transporter that is responsible for Na(+)-coupled transport of carnitine in the kidney and other tissues. We investigated the interaction of several beta-lactam antibiotics with OCTN2 using human cell lines that express the transporter constitutively as well as using cloned human and rat OCTN2s expressed heterologously in human cell lines. The beta-lactam antibiotics cephaloridine, cefoselis, cefepime, and cefluprenam were found to inhibit OCTN2-mediated carnitine transport. These antibiotics possess a quaternary nitrogen as does carnitine. Several other beta-lactam antibiotics that do not possess this structural feature did not interact with OCTN2. The interaction of cephaloridine with OCTN2 is competitive with respect to carnitine. Interestingly, many of the beta-lactam antibiotics that were not recognized by OCTN2 were good substrates for the H(+)-coupled peptide transporters PEPT1 and PEPT2. In contrast, cephaloridine, cefoselis, cefepime, and cefluprenam, which were recognized by OCTN2, did not interact with PEPT1 and PEPT2. The interaction of cephaloridine with OCTN2 was Na(+)-dependent, whereas the interaction of cefoselis and cefepime with OCTN2 was largely Na(+)-independent. Furthermore, the Na(+)-dependent, OCTN2-mediated cellular uptake of cephaloridine could be demonstrated by direct uptake measurements. These studies show that OCTN2 plays a crucial role in the pharmacokinetics and therapeutic efficacy of certain beta-lactam antibiotics such as cephaloridine and that cephaloridine-induced carnitine deficiency is likely to be due to inhibition of carnitine reabsorption in the kidney.

Acetylcarnitine↗
PubMed2006

Quantitative structure/activity relationship modelling of pharmacokinetic properties using genetic algorithm-combined partial least squares method.

Quantitative structure/activity relationship (QSAR) approaches have widely been applied to gain deeper understandings of the relationships between ADME parameters and molecular structure and properties. QSAR models for predicting ADME properties are required to cover structurally diverse compounds. In the present investigation, we describe application of genetic algorithm-combined partial least squares (GA-PLS) method to QSAR modelling of various ADME properties. By selecting an appropriate set of molecular descriptors automatically by the use of genetic algorithm, many ADME properties could be well-explained by simple molecular descriptors derived from 2-dimensional chemical structure.

Algorithms↗
PubMed1998

In-vitro activity of 21 beta-lactam antibiotics against penicillin-susceptible and penicillin-resistant Streptococcus pneumoniae.

MICs of 21 beta-lactams were determined by agar dilution against 283 penicillin-susceptible (pen-S), 122 intermediate (pen-I) and 23 fully penicillin-resistant (pen-R) pneumococci. MICs of all beta-lactams increased with increasing MICs of penicillin. Clometocillin was the most active penicillin against pen-I or pen-R pneumococci. All oral cephalosporins except cefuroxime and cefpodoxime were less active than penicillin and none was satisfactory against pen-I or pen-R pneumococci. The parenteral third- and fourth-generation cephalosporins (except ceftazidime) were similar in activity to penicillin against pen-S isolates. Cefpirome showed the lowest mean MICs against pen-I and pen-R strains.

Amoxicillin↗
PubMedDate not supplied

Management of streptococcal pharyngitis reconsidered.

Adequate treatment of GABHS pharyngitis with penicillin shortens the course of illness, reduces the spread of streptococci and prevents suppurative complications. It has also been a major factor in the markedly accelerated decline in the incidence of acute rheumatic fever in this country. Difficulties in the clinical diagnosis of GABHS pharyngitis make bacteriologic confirmation highly desirable. Currently a properly performed throat culture is the best way to obtain this bacteriologic confirmation. However, it is possible that rapid antigen detection tests will replace the throat culture in the future. These diagnostic tools should be used more selectively and only in conjunction with clinical and epidemiologic data. Greater selectivity will help control costs and will increase the chances of identifying patients who are truly infected and are not merely streptococcal carriers. Penicillin is still the drug of choice and an oral preparation given twice daily is as effective as more frequent doses. Patients at risk for noncompliance should be treated with a single injection of benzathine penicillin combined with procaine penicillin to lessen the local discomfort. Routine follow-up cultures of asymptomatic patients should be abandoned. Persistence of GABHS following a course of treatment may no longer be an important risk factor for the development of rheumatic fever. However, there are exceptional cases, as noted in the text, in which eradication of GABHS carriage with a short course of rifampicin may be desirable.

Administration, Oral↗