Absorption of Phenoxymethylpenicillin from Mixtures and Tablets in Healthy Volunteers

1983 ◽  
Vol 11 (6) ◽  
pp. 380-384 ◽  
Author(s):  
Kenneth Josefsson ◽  
Lennart Magni

The absorption of the potassium, calcium and benzathine salts of Phenoxymethylpenicillin, given as mixtures, was investigated in twelve healthy volunteers. The potassium salt gave the fas test and highest serum peak levels. Also the relative bioavailability of the potassium salt was greatest, as indicated by the areas under the serum concentration/time curves (AUC). In a second study with twelve other volunteers, the absorption of the mixtures and tablets of the potassium salt was studied. The peak serum levels and AUC were comparable after these preparations. The results in our two studies indicate that, from a pharmacokinetic point of view, the potassium salt of Phenoxymethylpenicillin in mixtures should be preferred in clinical practice. It also appears that the absorption of Phenoxymethylpenicillin from the tablets and mixtures of the potassium salt is comparable, giving the same relative bioavailability.

1977 ◽  
Vol 5 (1) ◽  
pp. 71-76 ◽  
Author(s):  
P J Neuvonen ◽  
E Elonen ◽  
P J Pentikäinen

The effect of food on the absorption of simultaneously ingested ampicillin or pivampicillin was compared in a crossover study in eight healthy volunteers. The absorption of both ampicillin and pivampicillin was delayed by simultaneous food intake as judged by serum concentration and urinary excretion of ampicillin. The total absorption of ampicillin, but not that of pivampicillin was decreased by simultaneous food intake as indicated by the area under the serum ampicillin concentration-time curves and by 24 hours urinary excretion of ampicillin. The excretion of ampicillin into urine was about 30% of the dose when ampicillin was ingested with water into an empty stomach and about 20% when ingested with food. The respective excretion of ampicillin following the ingestion of pivampicillin was about 60% of the dose taken either with or without food.


1994 ◽  
Vol 22 (1) ◽  
pp. 33-39 ◽  
Author(s):  
H Guven ◽  
O Oto ◽  
U Acikel ◽  
S Gidener ◽  
S Apaydin ◽  
...  

The effects of open heart surgery on amikacin concentration time-curves were investigated in eight patients who were scheduled for open heart surgery at a Thoracic and Cardiovascular Surgery Department. A 500 mg single dose of amikacin was administered parenterally to the volunteers pre- and postoperatively and the serum concentration time-curves were compared. Serum amikacin levels after pre-operative intramuscular (IM) administration did not reach therapeutic values. By comparison, preoperative and postoperative IM or intravenously (IV) administration resulted in therapeutic serum amikacin levels. It was concluded that IM administration preoperatively was not appropriate. Serum levels of amikacin were also shown to fall below therapeutic values 8 h after administration. It is recommended that dosing intervals with amikacin should not exceed 8 h.


DICP ◽  
1989 ◽  
Vol 23 (2) ◽  
pp. 153-154
Author(s):  
Joseph M. De Vito ◽  
Brian W. McGuire ◽  
Robert J. De Lap ◽  
Arnold I. Weiss

In a randomized, single-dose, two-way crossover study, 36 male volunteers received 25 mg each of two oral formulations of leucovorin calcium. Reduced serum folate concentrations were determined over the 24 hours after dosing. There were no statistically significant differences in areas under the serum concentration-time curves for total L-tetrahydrofolates, L-leucovorin (L-5–formyltetrahydrofolate), and L-5–methyltetrahydrofolate (the active metabolite of leucovorin and the predominant circulating form of reduced folate after oral administration). The peak serum concentrations and times to peak serum concentrations were also not significantly different. We conclude that the two leucovorin calcium 5 mg tablet formulations are bioequivalent.


Nutrients ◽  
2021 ◽  
Vol 13 (4) ◽  
pp. 1136
Author(s):  
Diana Fiorentini ◽  
Concettina Cappadone ◽  
Giovanna Farruggia ◽  
Cecilia Prata

Magnesium plays an important role in many physiological functions. Habitually low intakes of magnesium and in general the deficiency of this micronutrient induce changes in biochemical pathways that can increase the risk of illness and, in particular, chronic degenerative diseases. The assessment of magnesium status is consequently of great importance, however, its evaluation is difficult. The measurement of serum magnesium concentration is the most commonly used and readily available method for assessing magnesium status, even if serum levels have no reliable correlation with total body magnesium levels or concentrations in specific tissues. Therefore, this review offers an overview of recent insights into magnesium from multiple perspectives. Starting from a biochemical point of view, it aims at highlighting the risk due to insufficient uptake (frequently due to the low content of magnesium in the modern western diet), at suggesting strategies to reach the recommended dietary reference values, and at focusing on the importance of detecting physiological or pathological levels of magnesium in various body districts, in order to counteract the social impact of diseases linked to magnesium deficiency.


2010 ◽  
Vol 14 (3) ◽  
pp. 220-222 ◽  
Author(s):  
Reiji Yoshimura ◽  
Atsuko Sugita-Ikenouchi ◽  
Hikaru Hori ◽  
Wakako Umene-Nakano ◽  
Kenji Hayashi ◽  
...  

2004 ◽  
Vol 48 (11) ◽  
pp. 4144-4147 ◽  
Author(s):  
D. Tarragó ◽  
L. Aguilar ◽  
M. J. Giménez ◽  
A. Fenoll ◽  
J. Casal

ABSTRACT A model of mouse sepsis caused by a serotype 6B Streptococcus pneumoniae strain (amoxicillin MIC of 8 μg/ml) was developed to investigate the therapeutic effect of an amoxicillin dose (3.12 mg/kg of body weight three times daily for 48 h) producing, over the whole treatment period, subinhibitory concentrations in serum (peak concentration [C max]: 6.1 μg/ml) in animals that prior to infection had been passively immunized with a 6B or 23F hyperimmune serum (obtained by immunization with a whole-cell heat-inactivated inoculum and diluted to produce no protective effect by itself). Mortality in nonimmunized animals treated with antibiotic (3.12 mg/kg) was 90%, and mortality in animals immunized but not treated with the antibiotic was 100%. Antibiotic treatment in immunized animals produced mortality rates ≤20% when the hyperimmune serum was used, thus showing cross-protection and synergism (defined as the situation in which there is no response to the single agents [no differences versus placebo] while the combination exhibits significant activity) with subinhibitory concentrations of the antibiotic. The presence of antipneumococcal antibodies allowed antibiotic efficacy with negligible values of pharmacodynamic parameters (C max/MIC ratio of <1 and thus a null value for the time that serum levels exceed the MIC). This in vivo synergism offers a potential therapeutic strategy against resistant strains.


Oncology ◽  
2007 ◽  
Vol 72 (5-6) ◽  
pp. 371-380 ◽  
Author(s):  
Naohide Oue ◽  
Hiroki Kuniyasu ◽  
Tsuyoshi Noguchi ◽  
Kazuhiro Sentani ◽  
Masanori Ito ◽  
...  

2011 ◽  
Vol 55 (5) ◽  
pp. 2290-2296 ◽  
Author(s):  
Thomas N. Kakuda ◽  
Samantha Abel ◽  
John Davis ◽  
Julia Hamlin ◽  
Monika Schöller-Gyüre ◽  
...  

ABSTRACTThe effects of darunavir-ritonavir at 600 and 100 mg twice daily (b.i.d.) alone, 200 mg of etravirine b.i.d. alone, or 600 and 100 mg of darunavir-ritonavir b.i.d. with 200 mg etravirine b.i.d. at steady state on the steady-state pharmacokinetics of maraviroc, and vice versa, in healthy volunteers were investigated in two phase I, randomized, two-period crossover studies. Safety and tolerability were also assessed. Coadministration of 150 mg maraviroc b.i.d. with darunavir-ritonavir increased the area under the plasma concentration-time curve from 0 to 12 h (AUC12) for maraviroc 4.05-fold relative to 150 mg of maraviroc b.i.d. alone. Coadministration of 300 mg maraviroc b.i.d. with etravirine decreased the maraviroc AUC12by 53% relative to 300 mg maraviroc b.i.d. alone. Coadministration of 150 mg maraviroc b.i.d. with etravirine-darunavir-ritonavir increased the maraviroc AUC123.10-fold relative to 150 mg maraviroc b.i.d. alone. Maraviroc did not significantly affect the pharmacokinetics of etravirine, darunavir, or ritonavir. Short-term coadministration of maraviroc with darunavir-ritonavir, etravirine, or both was generally well tolerated, with no safety issues reported in either trial. Maraviroc can be coadministered with darunavir-ritonavir, etravirine, or etravirine-darunavir-ritonavir. Maraviroc should be dosed at 600 mg b.i.d. with etravirine in the absence of a potent inhibitor of cytochrome P450 3A (CYP3A) (i.e., a boosted protease inhibitor) or at 150 mg b.i.d. when coadministered with darunavir-ritonavir with or without etravirine.


2014 ◽  
Vol 2014 ◽  
pp. 1-8 ◽  
Author(s):  
Yuan-Lin Guo ◽  
Rui-Xia Xu ◽  
Cheng-Gang Zhu ◽  
Na-Qiong Wu ◽  
Zhi-Ping Cui ◽  
...  

Objective. Statin treatment alone has been demonstrated to significantly increase plasma proprotein convertase subtilisin/kexin type 9 (PCSK9) levels. The effect of policosanol combined with statin on PCSK9 is unknown.Methods. Protocol I: 26 patients with atherosclerosis were randomly assigned to receive either atorvastatin 20 mg/d or policosanol 20 mg/d + atorvastatin 20 mg/d for 8 weeks. Protocol II: 15 healthy volunteers were randomly assigned to either policosanol 20 mg/d or a control group for 12 weeks. Serum levels of PCSK9 were determined at day 0 and the end of each protocol.Results. Protocol I: atorvastatin 20 mg/d significantly increased serum PCSK9 level by 39.4% (256 ± 84 ng/mL versus 357 ± 101 ng/mL,P=0.002). However, policosanol 20 mg/d + atorvastatin 20 mg/d increased serum PCSK9 level by only 17.4% without statistical significance (264 ± 60 ng/mL versus 310 ± 86 ng/mL,P=0.184). Protocol II: there was a trend toward decreasing serum PCSK9 levels in the policosanol group (289 ± 71 ng/mL versus 235 ± 46 ng/mL,P=0.069).Conclusion. Policosanol combined with statin attenuated the statin-induced increase in serum PCSK9 levels. This finding indicates that policosanol might have a modest effect of lowering serum PCSK9 levels.


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