SEARCH · Search PubMed

Results for “BMI”

Search indexed PubMed citations on genomics, clinical trials, systematic reviews and public health. Explore titles, authors and supplied subject terms, then open the PubMed record.

SourceResearch connectionFrom yearThrough year

Quote a phrase for an exact phrase match. Source license links do not imply unrestricted reuse.

At least 109 records · Page 6Linked to original sources

PubMed1997

[3-[4-(4,5-Diphenyl-2-oxazolyl)-5-oxazolyl]phenoxy]acetic acid (BMY 45778) is a potent non-prostanoid prostacyclin partial agonist: effects on platelet aggregation, adenylyl cyclase, cAMP levels, protein kinase, and iloprost binding.

[3-[4-(4,5-diphenyl-2-oxazolyl)-5-oxazolyl]phenoxy]acetic acid (BMY 45778) inhibits human (IC50 = 35 nM), rabbit (136 nM) and rat (1.3 microM) platelet aggregation. This compound activates adenylyl cyclase (ED50 = 6-10 nM) and stimulates GTPase in human platelet membrane preparations. The potency (EC50) of BMY 45778 stimulating adenylyl cyclase is comparable to iloprost. However, maximal stimulation of GTPase by BMY 45778 is approximately half the iloprost-stimulated activity, and BMY 45778 limits the GTPase stimulation by iloprost suggesting that BMY 45778 is a partial agonist at the IP receptor. BMY 45778 completely prevents [3H]]Iloprost binding to platelet membranes (IC50 = 7 nM). In whole platelets, BMY 45778 causes elevation of platelet cAMP levels (cAMP content doubles at 13 nM) and activation of the cAMP-dependent protein kinase (cAMP-protein kinase ratio is twice basal at 2 nM). BMY 45778 treatment of whole platelets also desensitizes the adenylyl cyclase activation by iloprost. These results indicate that BMY 45778, which is structurally different from prostacyclin and most prostacyclin agonists, acts by stimulating prostacyclin (IP) receptors.

Acetates↗

PubMed2000

A comparison between BMI and Conicity index on predicting coronary heart disease: the Framingham Heart Study.

PURPOSE: This study examined the relationship of mortality and morbidity of coronary heart disease with body mass index (BMI) and Conicity index (CI). METHODS: Among 5209 Framingham Heart Study participants, 1882 men and 2373 women had waist and weight measurement at the 4th examination period and height measured on the 5th visit. These were used for BMI and CI. RESULTS: During a 24-year follow-up, 597 men and 468 women developed CHD and 248 men and 150 women died from CHD associated causes. In men the relative risks (RR) (95% confidence interval) adjusted for age, hypertension, diabetes, smoking status, and total cholesterol for CHD incidence in 2nd, 3rd, and 4th quartiles of BMI were 1.28 (1.0, 1.65), 1.45 (1.13, 1.86), and 1.53 (1.19, 1.96). The RR for CHD incidence in the 4th quartile of BMI in women was 1.56 (1.16, 2.08). No CI quartiles were risk factors for CHD incidence. There was 86% higher risk of CHD related death in the 4th quartile of BMI than the 1st quartile of BMI in women. In men no significantly higher risks of death were found across the quartiles of BMI. No associations were found between CI quartiles and CHD mortality. CONCLUSIONS: Obesity as measured by BMI is an important risk factor for CHD incidence in men and women and for CHD mortality in women. CI was not associated with an increase in CHD incidence or mortality. Thus, BMI is a better marker than CI for predicting CHD incidence and mortality.

Adult↗

PubMed1999

Relation of BMI to a dual-energy X-ray absorptiometry measure of fatness.

Dual-energy X-ray absorptiometry (DXA) is a valid technique for measuring the fat, bone and lean (muscle, organs and water) masses of the body. We evaluated relationships of BMI (kg/m2) with independent measurements of fat and lean masses using DXA in 226 adult volunteers. The evaluation was an application of a general approach to compositional data which has not previously been used for describing body composition. Using traditional regression analyses, when lean mass was held constant, BMI varied with fat mass (men r 0.75, P < 0.05; women r 0.85, P < 0.05); when fat mass was held constant, BMI varied with lean mass (men r 0.63, P < 0.05; women r 0.47, P < 0.05). In contrast, a regression model for compositional data revealed that BMI was: (a) strongly associated with log fat mass in both sexes (b1 4.86, P < 0.001 for all women and b1 5.96, P < 0.001 for all men); (b) not associated with bone mass, except in older men; (c) related to lean mass in women but not in men (b3 -4.04, P < 0.001 for all women and b1 -2.59, P < 0.15 for all men). Women with higher BMI tended to have more fat mass and more lean mass than women with lower BMI. Men with higher BMI had more fat mass but similar lean mass to men with lower BMI. Investigators need to be alert to the inaccuracy of BMI to assign a fatness risk factor to individuals, especially among women.

Absorptiometry, Photon↗

PubMed1999

The oncogene and Polycomb-group gene bmi-1 regulates cell proliferation and senescence through the ink4a locus.

The bmi-1 gene was first isolated as an oncogene that cooperates with c-myc in the generation of mouse lymphomas. We subsequently identified Bmi-1 as a transcriptional repressor belonging to the mouse Polycomb group. The Polycomb group comprises an important, conserved set of proteins that are required to maintain stable repression of specific target genes, such as homeobox-cluster genes, during development. In mice, the absence of bmi-1 expression results in neurological defects and severe proliferative defects in lymphoid cells, whereas bmi-1 overexpression induces lymphomas. Here we show that bmi-1-deficient primary mouse embryonic fibroblasts are impaired in progression into the S phase of the cell cycle and undergo premature senescence. In these fibroblasts and in bmi-1-deficient lymphocytes, the expression of the tumour suppressors p16 and p19Arf, which are encoded by ink4a, is raised markedly. Conversely, overexpression of bmi-1 allows fibroblast immortalization, downregulates expression of p16 and p19Arf and, in combination with H-ras, leads to neoplastic transformation. Removal of ink4a dramatically reduces the lymphoid and neurological defects seen in bmi-1-deficient mice, indicating that ink4a is a critical in vivo target for Bmi-1. Our results connect transcriptional repression by Polycomb-group proteins with cell-cycle control and senescence.

Animals↗

PubMed2004

Cut-off point of BMI and obesity-related comorbidities and mortality in middle-aged Koreans.

OBJECTIVE: The need for a lower BMI to classify overweight in Asian populations has been controversial. Using both disease and mortality outcomes, we investigated whether lower BMI cut-off points are appropriate for identifying increased health risk in Koreans. RESEARCH METHODS AND PROCEDURES: We conducted a cohort study among 773,915 men and women from 30 to 59 years old with 8- to 10-year follow-up periods. Primary outcomes were change of obesity prevalence, obesity-related disease incidence, and all-cause mortality. RESULTS: Prevalence of overweight (BMI of 25.0-29.9) has steadily increased (1.3% annually), whereas obesity (BMI > or = 30) showed a lower prevalence and only a slight increase (0.1%-0.2% annually). Our study revealed that dose-response relationships exist between obesity and related disease incidences (hypertension, type 2 diabetes, and hypercholesterolemia) beginning at lower BMI levels than previously reported. Compared with those in the healthy weight range, Koreans with a BMI > or = 25 were not at greater risk of hypertension, type 2 diabetes, or hypercholesterolemia than has been reported for whites in similar studies. Obesity-related all-cause mortality also did not seem so different from that of whites. DISCUSSION: Our findings did not support the use of a lower BMI cut-off point for defining overweight in Koreans compared with whites for the purpose of identifying different risks. However, populations with BMI > or = 25 are rapidly increasing and have substantial risks of diseases. To preempt the rapid increases in obesity and related health problems that are occurring in Western countries, Korea should consider using a BMI of 25 as an action point for obesity prevention and control interventions.

Adult↗

PubMed2006

Prospective associations between sedentary lifestyle and BMI in midlife.

OBJECTIVE: A strong positive cross-sectional relationship between BMI and a sedentary lifestyle has been consistently observed in numerous studies. However, it has been questioned whether high BMI is a determinant or a consequence of a sedentary lifestyle. RESEARCH METHODS AND PROCEDURES: Using data from four follow-ups of the University of North Carolina Alumni Heart Study, we examined the prospective associations between BMI and sedentary lifestyle in a cohort of 4595 middle-aged men and women who had responded to questionnaires at the ages of 41 (standard deviation 2.3), 44 (2.3), 46 (2.0), and 54 (2.0). RESULTS: BMI was consistently related to increased risk of becoming sedentary in both men and women. The odds ratios of becoming sedentary as predicted by BMI were 1.04 (95% confidence limits, 1.00, 1.07) per 1 kg/m(2) from ages 41 to 44, 1.10 (1.07, 1.14) from ages 44 to 46, and 1.12 (1.08, 1.17) from ages 46 to 54. Controlling for concurrent changes in BMI marginally attenuated the effects. Sedentary lifestyle did not predict changes in BMI, except when concurrent changes in physical activity were taken into account (p < 0.001). The findings were not confounded by preceding changes in BMI or physical activity, age, smoking habits, or sex. DISCUSSION: Our findings suggest that a high BMI is a determinant of a sedentary lifestyle but did not provide unambiguous evidence for an effect of sedentary lifestyle on weight gain.

Adult↗

PubMed2006

Maternal feeding strategies, child eating behaviors, and child BMI in low-income African-American preschoolers.

OBJECTIVE: To test the hypothesis that low-income African-American preschool children would have a higher BMI if their mothers reported greater "restriction" and "control" in feeding and if mothers reported that children showed greater "food responsiveness" and "desire to drink." In addition, to test whether higher maternal "pressure to eat" would be associated with lower child BMI. RESEARCH METHODS AND PROCEDURES: A questionnaire was completed by 296 low-income African-American mothers of preschool children. It assessed three constructs on maternal feeding strategies ("restriction," "pressure to eat," and "control") and two on child eating behaviors ("food responsiveness" and "desire to drink"). Children's BMI was measured, and mothers' BMI was self-reported. RESULTS: The mean (standard deviation) BMI z-score of the children was 0.34 (1.5), and 44% of the mothers were obese (BMI > or =30 kg/m(2)). Only maternal "pressure to eat" had a significant overall association with child BMI z-score (r = -0.16, p < 0.01). Both maternal "restriction" and "control" were positively associated with children's BMI z-score in the case of obese mothers (r = 0.20, p = 0.03 and r = 0.24, p = 0.007, respectively), but this was not so in the case of non-obese mothers (r = -0.16, p = 0.05 and r = -0.07, p = 0.39, respectively). DISCUSSION: Among low-income African Americans, the positive association between maternal restriction and control in feeding and their preschoolers' BMI was limited to obese mothers. Relations between parent feeding strategies and child weight status in this population may differ on the basis of maternal weight status.

Adult↗

PubMed1998

The association between BMI and haemoglobin and work productivity among Indonesian female factory workers.

OBJECTIVE: To investigate the relationship between body mass index (BMI), haemoglobin (Hb) concentration and work productivity in Indonesian female industrial workers engaged in cigarette rolling. DESIGN: Randomized-stratified, cross-sectional study. SETTING: A clove cigarette factory in Central Java Province, Indonesia. SUBJECTS: Two-hundred and thirty female cigarette-rollers. METHODS: Anthropometric variables (height, weight, mid-upper arm circumference, BMI), body composition (lean body mass and fat mass from skinfolds thicknesses), Hb, work productivity (cigarettes/hour) were determined. RESULTS: Of the 230 selected subjects 40.4% were anaemic and 41.3% had BMI < 18.5. Average production was 620 +/- 86 cigarettes/h. Productivity was positively correlated with work experience (r = 0.214, P < 0.01), lean body mass (r = 0.183, P < 0.01), height (r = 0.150, P < 0.05), Hb (r = 0.141, P < 0.05), and arm muscle area (r = 0.120, P < 0.05). Anaemic subjects produced 4.9% less (P < 0.01) than the non-anaemic ones. No linear relationship existed between BMI and productivity, but subjects with a BMI < 18.5, or < 17.0, produced respectively 5.1% (P < 0.05) and 6.8% (P <0.05) less than subjects with BMI between 18.5-22.5. CONCLUSIONS: Work productivity of persons with low BMI and Hb may be reduced. However, BMI was not a good screening tool to detect low producers. When using BMI < 18.5 and a production < 550 cigarettes/h as cut-offs sensitivity (64.7%) and specificity (55.5%) were low.

Adult↗

PubMed1999

Determinants of geographical variations in body mass index (BMI) and obesity in Spain.

OBJECTIVE: To identify the factors associated with geographic variations in Body Mass Index (BMI) and obesity in Spain. DESIGN: Cross-sectional, ecological analysis using data on illiteracy rate (per 1000 population), energy intake (kcal/person/d), sedentary population (%), smoking population (%), alcohol consumption (g/person/d), and percentage of population aged 65 y or over, for Spain's 50 provinces. SUBJECTS: Non-institutionalized population aged 16y or over. MEASUREMENTS: Median BMI and percentage of population with obesity, defined as BMI > 30 kg/m2. RESULTS: There was a clear geographical pattern, with some areas in the south and north-west of the country registering the highest BMI and prevalence of obesity and a north-south pattern on illiteracy per 1000 population. Multivariate regression analysis showed that illiteracy, sedentary lifestyle and energy intake explain 35% and 14% of the variation in BMI and obesity, respectively. Illiteracy proved to be the variable most associated with both BMI (regression coefficient (beta = 0.01; P = 0.005) and obesity (beta = 0.05; P = 0.013). Sedentary lifestyle showed a statistically significant relationship with BMI (beta = 0.01; P = 0.03), but not with obesity (beta = 0.03; P = 0.581). Energy intake exhibited a relationship with BMI (beta < 0.01 P = 0.03) that lost statistical significance when adjusted for age. CONCLUSION: Geographical variations in BMI in Spain are partly explained by illiteracy, sedentary lifestyle and, to a lesser extent, energy intake, whereas regional variations in obesity are related only to the educational level of the population.

Alcohol Drinking↗

PubMed2006

Changes in BMI modulate age-associated changes in sex hormone binding globulin and total testosterone, but not bioavailable testosterone in young adult men: the CARDIA Male Hormone Study.

OBJECTIVES: To compare age-associated 8-year changes in total testosterone, calculated bioavailable testosterone and sex hormone binding globulin (SHBG) across five groups of men stratified according to change in body mass index (BMI) (i.e., BMI stable (+/-0.69 kg/m(2)), decreased (-0.7 kg/m(2)), increased minimally (0.7-1.74 kg/m(2)), increased moderately (1.75-3.19 kg/m(2)) and increased most (> or =3.20 kg/m(2))). DESIGN: Eight-year longitudinal cohort study. SUBJECTS: Four hundred and seventy-four black and 695 white men, aged 24-31 years at the time of the first hormone measurement. MEASUREMENTS: Aging-related changes in serum SHBG, total testosterone and bioavailable testosterone. RESULTS: SHBG significantly increased with age for men whose BMI decreased, and there were progressively smaller increases for men whose BMI was stable, or whose BMI increased minimally or moderately (range 1.1-0.3 nM per year, P< or =0.03, respectively). There was no age relationship with SHBG among men whose BMI increased most. Total testosterone did not change with age for men whose BMI decreased, was stable or increased minimally, but for men whose BMI increased moderately and most there was a graded decrease in total testosterone with age (beta=-0.2 and -0.4 nM per year, respectively, P< or =0.005). However, bioavailable testosterone decreased with age to a similar extent across all groups. CONCLUSIONS: These results suggest that changes in BMI during young adulthood modulate age-related changes in SHBG and total testosterone, but not bioavailable testosterone.

Adult↗

PubMed2006

BMI: new aspects of a classical risk factor for hypertensive disorders in pregnancy.

HDP (hypertensive diseases in pregnancy) are one of the leading causes of maternal and fetal mortality and morbidity. BMI (body mass index) is an established risk factor for pre-eclampsia, but its role in HELLP syndrome is unknown. We therefore investigated BMI as a risk factor in the development of HELLP syndrome. At the beginning of pregnancy, BMI was measured in 1067 women with a history of HDP and 1063 controls. Diagnoses of HDP were classified according to ISSHP (International Society for the Study of Hypertension in Pregnancy) and BMI according to WHO (World Health Organization) criteria. After verification of exclusion criteria and matching for confounders, 687 women with hypertensive diseases in pregnancy and 601 controls remained for statistical evaluation by chi(2) test and multiple logistic regressions. As a continuous variable, the increase in BMI was associated with an increase in the development of gestational hypertension {OR (odds ratio), 1.1 [95% CI (confidence interval) 1.062-1.197]} and pre-eclampsia [OR, 1.1 (95% CI, 1.055-1.144)]}, but not for HELLP syndrome. According to WHO definitions, overweight women (BMI > or =25 and <30 kg/m(2)) had a 2-fold (95% CI, 1.365-2.983) risk and obese women (BMI > or =30 kg/m(2)) had a 3.2-fold (95% CI, 1.7-5.909) risk of developing pre-eclampsia when compared with women of normal weight (BMI > or =15.5 and <25 kg/m(2)). Being overweight or having obesity had no effect on the risk of HELLP syndrome. As an increased BMI is correlated with the risk of developing pre-eclampsia but not HELLP syndrome, both diseases have a different risk profile. This finding supports that underlying physiological mechanisms in pre-eclampsia vary from those in HELLP syndrome.

Adult↗

PubMed2004

Relationship between pre-pregnancy BMI and plasma zinc concentrations in early pregnancy.

We previously reported that pregnant women whose plasma Zn concentrations were below the 50th percentile tended to have high pre-pregnancy BMI (kg/m(2)) values. We therefore hypothesized that in pregnant women, plasma Zn concentrations are negatively correlated with BMI. We evaluated the association between BMI values and plasma Zn concentrations in 1474 women whose blood samples were obtained before 15 weeks of gestation. Their mean age was 22.7 years and mean gestational age at blood sampling was 10 weeks. The mean plasma Zn concentration and BMI were 11.6 micromol/l and 26.6 kg/m(2) respectively. Because plasma Zn concentrations decrease as gestational age increases, plasma Zn concentrations were standardized by Z-scores. Z-score distributions were compared among the quartiles of BMI. The highest BMI group had the lowest plasma Zn concentrations, whereas the lowest BMI group had the highest; the differences were significant between the BMI groups (P<0.0001). The interpretation of plasma Zn concentrations to assess Zn nutriture in pregnancy may be complicated not only by the well-established factor of gestational age at blood sampling, but also by a previously unrecognized factor, maternal BMI.

Adult↗

PubMed2005

Effect of body mass index (BMI) on estimation of extracellular volume (ECV) in hemodialysis (HD) patients using segmental and whole body bioimpedance analysis.

The aim of the study was to investigate whether body mass index (BMI) influences the estimation of extracellular volume (ECV) in hemodialysis (HD) patients when using segmental bioimpedance analysis (SBIA) compared to wrist-to-ankle bioimpedance analysis (WBIA) during HD with ultrafiltration (UF). Twenty five HD patients (M:F 19:6,) were studied, and further subdivided into two groups of patients, one group with a high BMI (25 kg m-2) and the other with a low BMI (<25 kg m-2). Segmental (arm, trunk, leg) and wrist-to-ankle bioimpedance measurements on each patient were performed using a modified Xitron 4000B system (Xitron Technologies, San Diego, CA). No differences in extracellular resistance (R(E), ohms) between wrist-to-ankle (R(W)) and sum of segments (R(S)) were noted for either the high BMI (489.2+/-82 ohm versus 491.6+/-82 ohm, p=ns) or low BMI groups (560.8+/-77 ohm versus 557.5+/-75 ohm, p=ns). UF volume (UFV, liters) did not differ significantly between the groups (4.0+/-0.9 L versus 3.3+/-1.0 L, p=ns), but change in ECV (DeltaECV) differed not only between methods: WBIA versus SBIA in the high BMI group (2.74+/-1.1 L versus 3.64+/-1.4 L, p<0.001) and in the low BMI group (1.86+/-0.9 L versus 2.91+/-1.0 L, p<0.05) but also between the high and lower BMI groups with WBIA (2.74+/-1.1 L versus 1.86+/-0.9 L, p<0.01). However, there was no significant difference in SBIA between BMI groups. This study suggests that the segmental bioimpedance approach may more accurately reflect changes in ECV during HD with UF than whole body impedance measurements.

Algorithms↗

PubMed2026

Unveiling the BMI Risk Threshold for Osteoarthritis: Multi-Database Causal and Nonlinear Evidence.

OBJECTIVE: To characterize the nonlinear relationship between BMI and osteoarthritis (OA), and to identify BMI thresholds that inform precise prevention strategies. METHODS: This multi-database study integrated Global burden of disease 2021, National Health and Nutrition Examination Survey 2007-2018, and Genome-Wide Association Studies. A generalized additive model was performed to visualize the BMI-OA relationship, adjusting for multiple confounders. We applied segmented logistic regression models to identify potential threshold effects and used Mendelian randomization to estimate the causal effects of BMI on OA subtypes. RESULTS: From 1990 to 2021, the age-standardized prevalence and years lived with disability rates for OA were highest in regions with high SDI. OA prevalence rose nonlinearly with BMI, with breakpoints at 24.00 and 41.58 kg/m2. Each unit increase in BMI was associated with higher odds of OA between 24.00 and 41.58 kg/m2 (OR = 1.022, 95% CI: 1.003-1.041) and above 41.58 kg/m2 (OR = 1.055, 95% CI: 1.022-1.090). Women and individuals aged ≥ 45 years exhibited a higher susceptibility to knee osteoarthritis. BMI was causally associated with knee osteoarthritis (OR = 1.63, 95% CI 1.50-1.77) and hip osteoarthritis (OR = 1.54, 95% CI 1.40-1.70). CONCLUSIONS: These findings suggest that OA risk awareness and weight-management strategies should begin before BMI reaches the high range, particularly among individuals with BMI exceeding 24.00 kg/m2.

Humans↗

PubMed1992

The pharmacology of a novel topical retinoid, BMY 30123: comparison with tretinoin.

Preclinical studies pertaining to the pharmacology and toxicology of BMY 30123 (4-acetamidophenyl retinoate) are reported. BMY 30123 is a novel compound which has topical retinoid activity. This compound exhibits lower toxicity, both local and systemic, than other clinically used topical retinoids such as tretinoin (all-trans retinoic acid) in animal models. BMY 30123 is effective in a number of retinoid sensitive skin models including the rhino mouse utriculi reduction assay, the mouse epidermal hyperplasia model and in the suppression of DNA synthesis in mouse skin stimulated with phorbol ester. BMY 30123 was equipotent with tretinoin in these topical models. In the rhino mouse model the ED30 values for BMY 30123 and tretinoin were 0.037 and 0.015 mM, respectively. In addition, BMY 30123 was active in the UVB-induced photodamaged mouse model, another retinoid sensitive model. One of the problems associated with topically applied tretinoin is local irritation. Therefore, for topical therapy to be optimal, it is important to reduce or minimize local irritation. Repeated applications of BMY 30123 to rabbit skin resulted in low skin irritation. The first perceptible signs of skin irritation produced by BMY 30123 occurred at a dose 10 times higher than that observed for tretinoin. BMY 30123 also exhibits low retinoid activity after oral or i.p. administration in mice and produced no signs of hypervitaminosis A-related toxicity at twenty times the no effect dose of tretinoin. Because retinoids are effective modulators of epidermal growth and differentiation, this compound should be useful for the treatment of cutaneous disorders that exhibit altered epidermal differentiation such as acne, psoriasis, ichthyosis and epithelial tumours.(ABSTRACT TRUNCATED AT 250 WORDS)

Acetaminophen↗

PubMed1985

Evaluation of the in vitro activity of BMY-28142, a new broad-spectrum cephalosporin.

The in vitro activity of BMY-28142, a new cephalosporin, was tested by a broth microdilution system and compared with those of cefotaxime, ceftazidime, cefoperazone, moxalactam, and HR 810 against 747 bacterial isolates, one-third of which were resistant to one or more third-generation cephalosporins. BMY-28142 was the most active drug tested against 326 Enterobacteriaceae with an MIC for 90% of the organisms tested (MIC90) of 1.0 micrograms/ml. Against these Enterobacteriaceae the relative activities were: BMY-28142 greater than HR 810 greater than moxalactam and ceftazidime greater than cefotaxime greater than cefoperazone. For cefotaxime- and cefoperazone-resistant strains, the MIC90 of BMY-28142 was 4.0 micrograms/ml (compared with 0.13 micrograms/ml for susceptible strains). BMY-28142, with an MIC90 of 8.0 micrograms/ml for Pseudomonas aeruginosa, was about half as active as ceftazidime. The relative activities against P. aeruginosa were: ceftazidime greater than BMY-28142 greater than HR 810 greater than cefoperazone greater than moxalactam and cefotaxime. The MIC90 of BMY-28142 against staphylococci was 2.0 micrograms/ml, which was fourfold less active than HR 810, slightly less active than cefotaxime and cefoperazone, and fourfold more active than ceftazidime and moxalactam. BMY-28142 was very active against beta-lactamase-positive and -negative Haemophilus influenzae (MIC90, 0.06 micrograms/ml), Neisseria gonorrhoeae (MIC90, 0.015 micrograms/ml),aand nonenterococcal streptococci. Its activity against Streptococcus faecalis was poor (MIC90, 64 micrograms/ml). BMY-28142 was stable against the several beta-lactamases tested but exhibited little beta-lactamase inhibitory effect.

Bacteria↗

PubMed1989

In vitro and in vivo evaluations of a new broad-spectrum oral cephalosporin, BMY-28232, and its prodrug esters.

The in vitro activity of a new cephalosporin, BMY-28232 (7-[(Z)-2-(2-aminothiazol-4-yl)-2-hydroxyiminoacetamido]-3-[ (Z)-1- propenyl]-3-cephem-4-carboxylic acid), was compared with those of cefuroxime and BMY-28488, the 3-vinyl congener of BMY-28232, against 899 bacteria including strains resistant to newer cephalosporins. BMY-28232 displayed potent, broad-spectrum antibacterial activity with high stability to various types of beta-lactamase. Its acetoxyethyl ester (BMY-28271) and pivaloyloxymethyl ester (BMY-28257) were well absorbed after oral administration to mice and rats. Both esters were metabolized to BMY-28232 and mainly excreted in urine. Oral bioavailability of both prodrug esters (60 to 70%) was better than that of cefuroxime axetil (46%) and gave excellent therapeutic efficacy against gram-positive- and gram-negative-bacterial infections in mice. Oral 50% protective doses (in milligrams per kilogram of body weight) of 0.65 and 0.72 for Staphylococcus aureus Smith, 0.9 and 1.2 for Escherichia coli Juhl, 1.6 and 1.6 for Proteus vulgaris, and 18.9 and 14.3 for Enterobacter cloacae were obtained for BMY-28271 and BMY-28257, respectively.

Animals↗

PubMed1990

Antimicrobial activity and stability to beta-lactamase of BMY-28271, a new oral cephalosporin ester.

BMY-28271, the acetoxyethyl ester of BMY-28232, 7-[(Z)-2-(2-aminothiazol-4-yl)-2-hydroxyiminoacetamido]-3(Z) -propen-1-yl-3- cephem-4-carboxylic acid, is a new oral cephalosporin. BMY-28232 has a widely expanded spectrum with high activity against gram-positive and gram-negative bacteria. BMY-28232 is far more active than cefixime or cefteram against Staphylococcus aureus and Staphylococcus epidermidis. Against gram-negative bacteria, the activity of BMY-28232 was comparable to or somewhat weaker than that of cefixime or cefteram. BMY-28232 was a poor substrate for various beta-lactamases. Orally administered BMY-28271 had a good therapeutic effect on systemic infections with S. aureus and some gram-negative bacteria in mice. Oral BMY-28271 was efficacious against S. aureus Smith infection: the efficacy of BMY-28271 was 80 to 90 times higher than that of cefixime or cefteram.

Administration, Oral↗