Experimental pharmacokinetics of carphedon

Spektor, S. S.; Berlyand, A. S.

doi:10.1007/bf02334630

Cited by 3 publications

(4 citation statements)

References 0 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…For the laboratories involved, the identification of a previously unknown doping agent and the hearing procedures were interesting experiences from which one could benefit later. As for some other examples of the disclosure of “new” doping agents, such as bromantan, tetrahydrogestrinone (THG), hydroxyethyl starch (HES), and carphedon (fonturacetam) there were few adverse findings later on. The latest statistics from the World Anti‐Doping Agency (WADA) on global laboratory findings in 2017 showed six adverse findings for probenecid, which only represents 1% of all adverse findings in the doping class S 5 Diuretics and other Masking Agents .…”

Section: Resultsmentioning

confidence: 99%

The Probenecid‐story – A success in the fight against doping through out‐of‐competition testing

Hemmersbach

2020

Drug Testing and Analysis

View full text Add to dashboard Cite

The effectiveness of doping control in sport has been improved continuously during the past 50 years. One of the major steps forward was the introduction of unannounced and targeted out-of-competition testing in order to control the misuse of anabolic-androgenic steroids (AAS), mainly during the end of the 1980s. It also led to the misuse of masking agents in case a surprise control was performed. Athletes tried to be "prepared", when the doping control officer showed up. The disclosure of the masking agent probenecid in 1987 is a perfect example of a memorable finding, of a suspected and purported case of performance manipulation. Probenecid and its metabolites were identified in five urine samples collected from Norwegian athletes in an out-of-competition test, while they were staying and training in the USA. Probenecid is a drug that reduces the urinary excretion of AAS from the body. It was the first time that it had showed up in a doping control sample. The athletes were sanctioned for hampering the analysis of their urine sample, although probenecid was not yet specified on the Prohibited List. Its detection was the result of a successful collaboration of laboratories and investigative diligence and enthusiasm following up suspicious observations in the actual samples. Immediately afterwards probenecid was added to the Prohibited List for 1988 as well as including the manipulation of doping control samples. K E Y W O R D Sdoping, probenecid, sample manipulation, target testing

show abstract

Section: Resultsmentioning

confidence: 99%

The Probenecid‐story – A success in the fight against doping through out‐of‐competition testing

Hemmersbach

2020

Drug Testing and Analysis

View full text Add to dashboard Cite

show abstract

“…In the previous article, the sensitivity of the analysis was 0.2 mg ml 21 using the LLE method. 1 The relative standard deviation (RSD) of the slopes from the calibration curve was no greater than 5.2%. The validation data are shown in Table 1.…”

Section: Validation Of the Methodsmentioning

confidence: 94%

“…Carphedon [(2-oxo-4-phenylpyrroline)acetamide] was synthesized in Russia at the beginning of the 1990s. [1][2][3][4][5] It is a phenylethylamide derivative chemically related to nootropil as well as an analogue of pemoline and is described as a psycho stimulant and stress protector. Several members of these classes possess analgesic properties, which are comparable to that of morphine.…”

Section: Introductionmentioning

confidence: 99%

See 1 more Smart Citation

Determination of carphedon in human urine by solid-phase microextraction using capillary gas chromatography with nitrogen–phosphorus detection

Kim¹,

Park²,

Myung³

et al. 1999

Analyst

View full text Add to dashboard Cite

Carphedon is a phenyl derivative of nootropil and is effective in increasing physical endurance and cold resistance, and is used for amnesia treatment. Carphedon was extracted from human urine samples by solid-phase microextraction with a 65 microns carbowax-divinylbenzene-coated fiber. This analysis was performed by using capillary gas chromatography with nitrogen-phosphorus detection and optimized at pH 9.6, 30% NaCl, immersion time 10 min and desorption in the GC injector at 250 degrees C for 3 min. The regression equation for carphedon showed good linearity in the range from 0.1 to 10 micrograms ml-1 for human urine samples. The limit of detection was 0.01 microgram ml-1. The developed method is more sensitive and simpler in sample preparation than liquid-liquid extraction and can be applied to doping analysis for stimulants.

show abstract

Piracetam and Piracetam-Like Drugs

Malykh¹,

Sadaie²

2010

Drugs

221

View full text Add to dashboard Cite

There is an increasing interest in nootropic drugs for the treatment of CNS disorders. Since the last meta-analysis of the clinical efficacy of piracetam, more information has accumulated. The primary objective of this systematic survey is to evaluate the clinical outcomes as well as the scientific literature relating to the pharmacology, pharmacokinetics/pharmacodynamics, mechanism of action, dosing, toxicology and adverse effects of marketed and investigational drugs. The major focus of the literature search was on articles demonstrating evidence-based clinical investigations during the past 10 years for the following therapeutic categories of CNS disorders: (i) cognition/memory; (ii) epilepsy and seizure; (iii) neurodegenerative diseases; (iv) stroke/ischaemia; and (v) stress and anxiety. In this article, piracetam-like compounds are divided into three subgroups based on their chemical structures, known efficacy and intended clinical uses. Subgroup 1 drugs include piracetam, oxiracetam, aniracetam, pramiracetam and phenylpiracetam, which have been used in humans and some of which are available as dietary supplements. Of these, oxiracetam and aniracetam are no longer in clinical use. Pramiracetam reportedly improved cognitive deficits associated with traumatic brain injuries. Although piracetam exhibited no long-term benefits for the treatment of mild cognitive impairments, recent studies demonstrated its neuroprotective effect when used during coronary bypass surgery. It was also effective in the treatment of cognitive disorders of cerebrovascular and traumatic origins; however, its overall effect on lowering depression and anxiety was higher than improving memory. As add-on therapy, it appears to benefit individuals with myoclonus epilepsy and tardive dyskinesia. Phenylpiracetam is more potent than piracetam and is used for a wider range of indications. In combination with a vasodilator drug, piracetam appeared to have an additive beneficial effect on various cognitive disabilities. Subgroup 2 drugs include levetiracetam, seletracetam and brivaracetam, which demonstrate antiepileptic activity, although their cognitive effects are unclear. Subgroup 3 includes piracetam derivatives with unknown clinical efficacies, and of these nefiracetam failed to improve cognition in post-stroke patients and rolipram is currently in clinical trials as an antidepressant. The remaining compounds of this subgroup are at various preclinical stages of research. The modes of action of piracetam and most of its derivatives remain an enigma. Differential effects on subtypes of glutamate receptors, but not the GABAergic actions, have been implicated. Piracetam seems to activate calcium influx into neuronal cells; however, this function is questionable in the light of findings that a persistent calcium inflow may have deleterious impact on neuronal cells. Although subgroup 2 compounds act via binding to another neuronal receptor (synaptic vesicle 2A), some of the subgroup 3 compounds, such as nefiracetam, are similar to those of subgr...

show abstract

Experimental pharmacokinetics of carphedon

Cited by 3 publications

References 0 publications

The Probenecid‐story – A success in the fight against doping through out‐of‐competition testing

The Probenecid‐story – A success in the fight against doping through out‐of‐competition testing

Determination of carphedon in human urine by solid-phase microextraction using capillary gas chromatography with nitrogen–phosphorus detection

Piracetam and Piracetam-Like Drugs

Contact Info

Product

Resources

About