Comparative evaluation of some pharmacological properties and side effects of d-glucitol hexanicotinate (sorbinicate) and nicotinic acid correlated with the plasma concentration of nicotinic acid

1980 ◽  
Vol 36 (1) ◽  
pp. 135-148 ◽  
Author(s):  
A. Subissi ◽  
P. Schiantarelli ◽  
M. Biagi ◽  
G. Sardelli
1969 ◽  
Vol 21 (02) ◽  
pp. 320-324 ◽  
Author(s):  
K Seiler ◽  
F Duckert

SummaryA case of severe Marcoumar intoxication is described. Eleven hours after the intake a plasma concentration of 15.75 µg/ml was found which corresponds approximately to the 5-fold therapeutic concentration. Repeated administration of vitamin K1 made it possible to avoid extreme lowering of the activity of the clotting factors II, VII and X and to prevent bleeding. Side effects were not observed. The biologic half-life of Phenprocoumon has been found to be shortened at high plasma concentration (3.7 instead of 5.9 days). It is probable that in extreme concentration the drug is less strongly bound to the plasma proteins.


2020 ◽  
Vol 24 (5) ◽  
pp. 473-486 ◽  
Author(s):  
Ligia S. da Silveira Pinto ◽  
Thatyana R. Alves Vasconcelos ◽  
Claudia Regina B. Gomes ◽  
Marcus Vinícius N. de Souza

Azetidin-2-ones (β-lactams) and its derivatives are an important group of heterocyclic compounds that exhibit a wide range of pharmacological properties such as antibacterial, anticancer, anti-diabetic, anti-inflammatory and anticonvulsant. Efforts have been made over the years to develop novel congeners with superior biological activities and minimal potential for undesirable side effects. The present review aimed to highlight some recent discoveries (2013-2019) on the development of novel azetidin-2-one-based compounds as potential anticancer agents.


2014 ◽  
Vol 1 (1) ◽  
pp. 1 ◽  
Author(s):  
Ahmet Aslan ◽  
Ahmet Özmeriç ◽  
Ökkeş Bilal ◽  
Fatih Doğar ◽  
Zübeyde Özkaya ◽  
...  

2019 ◽  
Vol 144 (04) ◽  
pp. 264-275
Author(s):  
Niels Voigt ◽  
Katharina Ort ◽  
Samuel Sossalla

AbstractDrug-drug interactions (DDI) represent a significant problem in modern medicine. The number of patients with multi-morbidity, who take multiple drugs, is constantly increasing (polypharmacy). The related exponential increase in potential DDI is almost incomprehensible. In this article, we review pharmacodynamic DDI and provide clinically relevant examples. In addition, we extensively review pharmakokinetic DDI (e. g. through the cytochrome P450-system or p-glycoproteins) that can modify the plasma concentration of many compounds, thereby also increasing the likelihood of unwanted side effects. Finally we provide tools, which may help clinicians in their daily practice to identify and avoid potential DDI. In the context of an ageing society receiving polypharmacy, a better awareness of DDI and of strategies to prevent them is expected to reduce mortality and morbidity.


1971 ◽  
Vol 118 (546) ◽  
pp. 523-524 ◽  
Author(s):  
M. Y. Ekdawi

Dibenzepin hydrochloride is a new tricyclic antidepressant drug with pharmacological properties midway between those of imipramine and amitriptyline. In a double-blind comparative trial, J. M. Fielding (Med. J. Australia, 1969, 1, 614) found no significant difference in the speed of the effect of the two drugs in depressed patients. He reported that side-effects rated subjectively by patients were maximal before starting on the drugs and tended to decrease with time. The following trial was accordingly staged.


2020 ◽  
Vol 6 (1) ◽  
Author(s):  
Abdullahi Bello Umar ◽  
Adamu Uzairu ◽  
Gideon Adamu Shallangwa ◽  
Sani Uba

Abstract Background The resistance of V600E-BRAF to the vemurafenib and the side effects of the identified inhibitors trigger the research for a novel and more potent anti-melanoma agents. In this study, virtual docking screening along with pharmacokinetics ADMET and drug-likeness predictions were combined to evaluate some 4-(quinolin-2-yl)pyrimidin-2-amine derivatives as potent V600E-BRAF inhibitors. Results Some of the selected compounds exhibited better binding scores and favorable interaction with the V600E-BRAF enzyme. Out of the screened compounds, two most potent (5 and 9) having good Rerank scores (− 128.011 and − 126.258) emerged as effective and potent V600E-BRAF inhibitors that outperformed the FDA-approved V600E-BRAF inhibitor (vemurafenib, − 118.607). Thus, the molecular docking studies revealed that the studied compounds showed competing for inhibition of V600E-BRAF with vemurafenib at the binding site and possessed better pharmacological parameters based on the drug-likeness rules filters for the oral bioavailability, and ADMET risk parameters. Conclusion The docking analysis, drug-likeness rules filters, and ADMET study identified compounds (5 and 9) as the best hits against V600E-BRAF kinase with enhanced pharmacological properties. This recommends that these compounds may be developed as potent anti-melanoma agents.


1996 ◽  
Vol 9 (2) ◽  
pp. 118-129 ◽  
Author(s):  
Deanna M. Guith

Clozapine (Clozaril®, Sandoz, East Hanover, NJ), an atypical antipsychotic agent with pharmacological properties considerably different from standard neuroleptics, has been found to be of great benefit especially to patients with treatment-resistant psychotic disorders. However, it is these unique pharmacological properties that have also been associated with mul tiple side effects ranging from the relatively benign (ie, sialorrhea during sleep, dizziness) to the potentially fatal (ie, agranulocytosis, seizures, and respiratory depression) which have limited its use. These untoward side effects are particularly problematic in the elderly population who often have concomitant medi cal illnesses requiring multiple medication regimens, including psychotropics that may interact with cloza pine (ie, benzodiazepines, cimetidine, fluoxetine). Because even the most benign of side effects has the potential of becoming fatal in certain circumstances if left unaddressed, it is imperative for patients, clinicians, pharmacists, and all health care professionals to be aware of adverse reactions and possible complica tions of clozapine therapy to prevent significant morbidity and mortality. Copyright © 1996 by W.B. Saunders Company


1977 ◽  
Vol 5 (4) ◽  
pp. 390-392
Author(s):  
J Gravesen

The acidimetric method for the determination of nicotinic acid (NA) using Lactobacillus plantarum ATCC 8014 (Lactobacillus arabinosus 17-5) has been simplified and thus made less time consuming, and the sensitivity has been increased fivefold by replacement of the titration by a pH determination. As the regression of the decrease in pH on the amount of NA was found linear within a range of 1 to 4 ng of NA per ml, the calculations were performed according to the slope-ratio principle. The NA concentration of plasma was determined with a coefficient of variation of 5 to 7%, which rose to about 10% at low NA concentrations. Assays of fasting plasma samples from 13 hyperlipidemic male patients showed a group mean NA concentration of 80 +/- 55 ng/ml (mean +/- 2 standard deviation), before treatment, and 705 +/- 544 ng/ml (mean +/- 2 standard deviation) during therapy with sustained release NA preparations, of which a single dose, ingested during steady-state conditions, doubled or tripled the plasma concentration within 1 to 3 h.


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