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Central nervous system stimulants can be distinguished on the basis of their differential effects in various behavioral tests. There are sufficient differences between these drugs to suggest that one could develop CNS stimulants with more selective behavioral actions.
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BACKGROUND AND OBJECTIVES: Central nervous system (CNS) stimulants may be used to reduce tiredness and increase alertness, competitiveness, and aggression. They are more likely to be used in competition but may be used during training to increase the intensity of the training session. There are several potential dangers involving their misuse in contact sports. This paper reviews the three main CNS stimulants, ephedrine, amfetamine, and cocaine, in relation to misuse in sport. METHODS: Description of the pharmacology, actions, and side effects of amfetamine, cocaine, and ephedrine. RESULTS: CNS stimulants have psychotropic effects that may be perceived to be ergogenic. Some are prescription drugs, such as Ephedra alkaloids, and there are issues regarding their appropriate therapeutic use. Recently attention has been given to their widespread use by athletes, despite the lack of evidence regarding any ergogenic or real performance benefit, and their potentially serious side effects. Recreational drugs, some of which are illegal (cocaine, amfetamines), are commonly used by athletes and cause potential ergolytic effects. Overall, these drugs are important for their frequent use and mention in anti-doping laboratories statistics and the media, and their potentially serious adverse effects. CONCLUSIONS: Doping with CNS stimulants is a real public health problem and all sports authorities should participate in its prevention. Dissemination of information is essential to prevent doping in sport and to provide alternatives. Adequate training and education in this domain should be introduced.
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In an ongoing attempt to develop a model to study the influence of various diseases and drugs on saliva, we studied persons with narcolepsy treated with central nervous system stimulants. The aim was to study the secretion of salivary proteins in narcolepsy in the presence and absence of central nervous system stimulants. For this purpose, two proteins synthesized in acinar cells, acidic proline-rich proteins (PRPs) and statherin, were selected. Persons with narcolepsy treated with central nervous system stimulants only were included, n = 12, ages 14 to 68, seven females. Citric-acid-stimulated parotid and submandibular/sublingual saliva samples were collected from these persons during medication, after a drug-free period of one week, at least two weeks after the drug had been re-introduced, and from a matched healthy control group. PRP and statherin concentrations were determined by means of reversed-phase and anion exchange chromatography, respectively. Both concentration and output of statherins and PRPs were increased in persons with narcolepsy receiving central nervous system stimulants compared with healthy control individuals. When the drug was withdrawn, salivary flow rates were not influenced. In contrast, withdrawal of the drug led to a significantly decreased secretion of PRPs and statherin. The reduced protein secretion may reflect decreased adrenergic activation in narcolepsy, to be reversed by treatment with central nervous system stimulants. It can be concluded that measurements of both salivary fluid and salivary proteins may be necessary for an overall evaluation of the effects of a given drug or disease on salivary secretion.
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Neurostimulator malfunctions must be located and repaired if patients are to receive maximum benefit from central nervous system stimulation. This report lists the problems encountered with the stimulators from four manufacturers. Procedures for locating the source of malfunctions are discussed in some detail.
The objective of this investigation was to evaluate a series of potential pharmacodynamic measures of central nervous system stimulation, including quantitative electroencephalography (EEG) and neuroendocrine, mood, and psychomotor performance measures. The reproducibility and sensitivity of the measures were compared. The study was conducted in two parts. The first part investigated the interindividual and intraindividual variability associated with a series of potential pharmacologic response measures under baseline (i.e., drug-free) conditions. It was an open-label, three-period pilot study in which healthy male volunteers underwent a series of tests (EEG, a visual continuous performance task, a finger tapping task, and self-rated mood scales) repeatedly during each study period. The second part evaluated the sensitivity of a series of potential response measures to detect the effects of dextroamphetamine, and was a double-blind, placebo-controlled, four-period crossover study in nine healthy male volunteers. Subjects received 5 mg, 10 mg, or 20 mg of dextroamphetamine or placebo orally and underwent the same series of tests as in Part I in addition to blood collection for determination of serum prolactin and dextroamphetamine levels. Peripheral response to dextroamphetamine was assessed by heart rate and blood pressure measurement. The greatest variability among days, within days, and among participants was associated with the quantitative electroencephalographic parameters studied. First-session effects were apparent for several of the tests, including EEG. Consistent response on EEG (increased alpha power) to dextroamphetamine was observed only in the three subjects who had a baseline alpha activity greater than 35%. Serum prolactin levels were inversely associated with the amount of dextroamphetamine administered, with the largest decrease in serum prolactin levels observed after the 5-mg dose, and this finding was statistically significant. Mood scales showed that three of nine participants experienced dysphoria after at least one dose level of dextroamphetamine. The effect on mood was generally greater as the dose increased. Doses could not be distinguished based on the results of the performance tests. Serum prolactin concentration was the most sensitive measure of central nervous system stimulation on EEG produced by dextroamphetamine under these study conditions. Cardiovascular measures were more sensitive measures of dextroamphetamine effects than the central nervous system measures.
Several drugs that are utilized primarily for their effects on the central nervous system also affect lower urinary tract function. Most of these effects are produced by the action of these drugs on adrenergic and cholinergic receptors or by direct action of lower urinary tract musculature. Central nervous system stimulants and depressants which are known to affect the storage or evacuation role of the lower urinary tract are discussed.
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The extract of the pericarp of castor bean (Ricinus communis) showed some typical central nervous system stimulant effects when administered to mice. The animals became exophthalmic, presented tremors and clonic seizures and died a few minutes after receiving larger doses of the extract. At lower doses the extract improved memory consolidation and showed some neuroleptic-like properties, such as a decrease in exploratory behavior and catalepsy. The memory-improving effect and the seizure-eliciting properties of the extract were also observed with the administration of ricinine, a neutral alkaloid isolated from the extract. However, the neuroleptic-like properties of the extract were not observed with ricinine. As the therapeutic index of ricinine is of the order of 200, the compound may be considered as a promising cognition-enhancing drug that may be used for the treatment of human amnesias.
Rise in blood pressure and heart rhythm disorders were provoked in rabbits submitted to electrical stimulation of the central nervous system. When injected into the cisterna magna, the hypotensive agent thiamenidine at a single dose of 100 microgram caused a fall in blood pressure and heart rate; this was not the case when the same dose was applied intravenously. Thiamenidine did not hinder the pressor response following stimulation of subthalamic zones, yet a reduction of rhythm disorders was obtained when the drug was administered by either route. The results suggest a central nervous action of thiamenidine.
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A variety of substituted amides of 6,7-dimethoxy-2-hydroxyquinoline-3-carboxylic acid were synthesized. Three of these compounds, tested as potential central nervous system stimulants, showed no marked biological activity.
A survey of patients with Tourette syndrome uncovered 32 who had been exposed to central nervous system stimulants. In 17 (53%) of these patients, symptoms were markedly accentuated by the drugs. Two patients whose Tourette syndrome developed suddenly when methylphenidate was administered are also reported.
BACKGROUND: The Child and Adolescent Unit at Nordland Psychiatric Hospital has conducted a review of the prescription practice in its region with regard to central nervous system stimulants. MATERIAL AND METHODS: Data were collected from the region's pharmacies on the type of drug, the type of medical practitioners prescribing them, and patients's sex, age and community of residence. RESULTS: The total numbers of users of Ritalin/Dexamin (methylphenidate/dextroamphetamine) were 199 children (under 18) and 21 adults (above 18). The male/female ratio was 4:1, boys between 8 and 13 being the largest group. Users in the below-18 group constituted 0.35% of their age group in our region. Prescriptions to children were in 188 out of 199 cases written by child psychiatrists or paediatricians. Prescription patterns in the seven local hospital areas in the region were almost identical, with one area forming an exception. INTERPRETATION: This survey suggest that because of insufficient knowledge of the diagnostic criteria for attention deficit/hyperactivity disorders, many children with this type of problems do not get the treatment they may need. Adequate treatment based on competent diagnostic assessment is assumed to relieve distress and counteract the development of further problems. Similar surveys in other Norwegian regions would enable us to compare prescription practice nation-wide.