Rates of psychostimulant overdose deaths were stable from 2003 to 2010.
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That same year, half of psychostimulant-related overdose fatalities also involved opioid use.
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Between 2010 and 2014, 85-90% of psychostimulant deaths mentioned methamphetamine on the death certificate.
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Between 2010 and 2017, researchers found that psychostimulant-related death rates increased annually by 29%.
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Five times as many children are now prescribed psychostimulant and antipsychotic medications as were in the 1980s.
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Between 2015 and 2016, cocaine-related overdose death rates rose 52% while psychostimulant-related overdose death rates rose 33%.
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Psychostimulant-related overdoses were actually up 200 percent between 2012 and 2017—300 percent if you count cases that include fentanyl.
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The battle to mitigate the effects of meth, currently the world's most popular psychostimulant, may be one of the most important fights there is.
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The Centres for Disease Control and Prevention recorded 4,298 psychostimulant deaths in 2014—up 229% from 2004, at the height of the previous meth epidemic.
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She's referring to a synthetic psychostimulant discovered in 1975 by Alexander "Sasha" Shulgin, a chemist known for creating and testing hundreds of drugs on himself.
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The report notes that from 2012 through 2018, the psychostimulant-induced overdose death rate climbed on average by 30 percent per year to a rate of 3.9 in 2018.
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Before these "psychostimulant medications," most hyperactivity in children was treated with psychotherapy, based on the belief through most of the 20th century that behavioral disorders had no biological basis.
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Lisdexamfetamine (aka Vyvanse in its generic form), a psychostimulant, increases dopamine in the brain, targeting the key imbalance in both attention deficit disorder and binge eating disorder, Kaplan says.
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Adderall, much like Ritalin, is a psychostimulant usually used to treat attention deficit hyperactivity disorder (ADHD), and often abused by anyone that needs to stay concentrated for long periods of time.
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Sergi Ferre, a neurobiologist at the National Institute of Drug Abuse, has co-authored one of the few studies on the subject, and says that he's found caffeine increases the psychostimulant effects of THC.
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Although fentanyl and other synthetic opioids like it were a significant driver of the increase in cocaine-related deaths from 2012 to 2017, opioids were not a significant factor in the of rise psychostimulant-involved deaths from 2010 to 2017.
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Information about current use of medication was available for 1,254, or 103%, of the participants with ADHD: Twenty-seven percent were on psychostimulant medication (methylphenidate or amphetamine) when their brains were scanned, and 47% were not taking medication at scan time.
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As Motherboard found in October last year, a myriad of other previously legal drugs are widely available on the dark web, including Benzo Fury, whose effects resembled ecstasy, and which was first banned in 2013; the psychostimulant ethylphenidate, which attracted the attention of legislators in April 2015; and lisdexamphetamine, which acts as a stimulant and was outlawed in 2014.
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Hexapradol (INN) is a psychostimulant drug which was never marketed.
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GBR-12783 is a psychostimulant which acts as a selective dopamine reuptake inhibitor.
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Fenozolone (Ordinator) was developed by Laboratoires Dausse in the 1960s and is a psychostimulant related to pemoline.
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Fencamine (Altimina, Sicoclor) is a psychostimulant drug of the amphetamine class. It is closely related to fenethylline.
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The RPSGB has identified the most popular products prescribed online as Prozac (an antidepressant), Viagra (for erectile dysfunction), Valium (a tranquiliser), Ritalin (a psychostimulant), Serostim (a synthetic growth hormone) and Provigil (a psychostimulant).RPSGB p.12 A study in the USA has also shown that antibiotics are commonly available online without prescription.
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Mephedrone is often consumed with alcohol. A study in mice investigated the interrelation between these two substances, focusing on the psychostimulant and rewarding properties of mephedrone. It found that at low (non-stimulant) doses alcohol significantly enhanced the psychostimulant effects of mephedrone. This effect was mediated by an increase in synaptic dopamine, as haloperidol, but not ketanserin, was able to block the potentiation by alcohol.
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Bath salts are often consumed concurrently with alcohol. A 2015 study has investigated the interrelation between mephedrone and alcohol, focusing on psychostimulant and rewarding effects. It showed that alcohol, at low (non-stimulant) doses, significantly enhances the psychostimulant effects of mephedrone. This effect is mediated by an increase in synaptic dopamine, as haloperidol, but not ketanserin, was capable of blocking the potentiation by alcohol.
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Lomevactone (INN) (developmental code name DR-250) is a drug described as a psychostimulant and antidepressant which was synthesized and assayed in the 1980s but was never marketed.
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Pimeclone (Karion, Spiractin) is a drug described as either a psychostimulant or a respiratory stimulant (conflicting reports) which is sold in Europe. It was first synthesized in 1927.
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"Neurotoxic profiles of HIV, psychostimulant drugs of abuse, and their concerted effect on the brain: Current status of dopamine system vulnerability in NeuroAIDS". Neuroscience and Biobehavioral Reviews 32(883).
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Levophacetoperane (Lidépran, Phacétoperane) is a psychostimulant developed by Rhône-Poulenc in the 1950s. The drug has been used as an antidepressant and anorectic. It is the reverse ester of methylphenidate.
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Aceglutamide (brand name Neuramina), or aceglutamide aluminum (brand name Glumal), also known as acetylglutamine, is a psychostimulant, nootropic, and antiulcer agent that is marketed in Spain and Japan. It is an acetylated form of the amino acid L-glutamine, the precursor of glutamate in the body and brain. Aceglutamide functions as a prodrug to glutamine with improved potency and stability. Aceglutamide is used as a psychostimulant and nootropic, while aceglutamide aluminum is used in the treatment of ulcers.
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Amphetamine was first synthesized in 1887 by the Romanian chemist Lazar Edeleano. It has since been used licitly to treat a range of disorders from asthma to ADHD and illicitly for recreational purposes. Amphetamine-type stimulants contain chemical groups including unsubstituted phenyl ring, alphy methyl group, and primary amino group, which accounts for its psychostimulant activities. ATS with multiple substitutions on the phenyl ring has a hallucinogenic effect on top of the psychostimulant effect, and are categorised as the ecstasy-class drugs.
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Many Psychostimulant drugs are known to interact with VMAT, including Amphetamine analogs such as Methamphetamine (METH), Cocaine, and Ecstasy (MDMA). See the Pharmacology section of this article for more information on these drugs' interactions.
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D5 receptor is believed to participate in modulation of psychostimulant-induced locomotion. Mice lacking D5 receptors show increased motor response to administration of methamphetamine than wild type mice, which suggests that these receptors have a role in controlling motor activity.
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Fenmetramide is a drug which was patented as an antidepressant by McNeil Laboratories in the 1960s. The drug was never marketed. It is the 5-ketone derivative of phenmetrazine and would similarly be expected to produce psychostimulant effects, though pharmacological data is lacking.
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Cocaine- and amphetamine-regulated transcript, also known as CART, is a neuropeptide protein that in humans is encoded by the CARTPT gene. CART appears to have roles in reward, feeding, and stress, and it has the functional properties of an endogenous psychostimulant.
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Common stressors used in these paradigms include foot-shock and noiseLu, L., Shepard, J., Hall, F., Shaham, Y. (2003). Effect of Environmental stressors on opiate and psychostimulant reinforcement, reinstatement, and discrimination in rats: a review. Neuroscience and Behavioral Review. 27, 457-491.
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Accordingly, though not known to have been reported in the medical literature, iofetamine likely possesses psychostimulant and possibly entactogenic effects. However, based on structure-activity relationships, it may also be highly neurotoxic to serotonergic and dopaminergic neurons similarly to most other para-halogenated amphetamines.
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As a child, Danko was hyperactive, but was diagnosed in an era before Ritalin became mainstream. Antidepressants were given to children with attention deficit hyperactivity disorder from the late 1940s to the late 1950s because psychostimulant drug weren't handed out to hyperactive children until the early 1960s.
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Fenbutrazate (INN), also known as phenbutrazate (BAN), is a psychostimulant used as an appetite suppressant under the trade names Cafilon, Filon, and Sabacid in Europe, Japan, and Hong Kong. It is a derivative of phenmetrazine and may function as a prodrug due to its similarity to phendimetrazine.
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Trazium (EGYT-3,615) is an antidepressant drug which was never marketed. It has psychostimulant-like effects and its actions appear to be mediated by the dopaminergic and adrenergic systems. It was formulated as a salt with ethanesulfonic acid and given the generic name trazium esilate (INN).
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The psychostimulant effects of bromantane onset gradually within 1.5- to 2-hours and last for 8- to 12-hours. Bromantane is used clinically in doses of 50 mg to 100 mg per day in the treatment of asthenia. The main metabolite of bromantane is 6β-hydroxybromantane.
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Levopropylhexedrine (Eventin) is a psychostimulant used as an anorectic in Germany and patented by Smith Kline & French in 1947.US 2454746 Cyclohexylalkylamines It has also been used in the anticonvulsant preparation barbexaclone in combination with phenobarbital to offset sedation. Levopropylhexedrine is the S-enantiomer of propylhexedrine.
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It has also notably since been used to help alleviate fatigue in multiple sclerosis. With the knowledge of the dopaminergic psychostimulant effects of the adamantane derivatives, bromantane, which is 2-(4-bromophenylamino)adamantane, was developed in the 1980s at the Zakusov State Institute of Pharmacology, Russian Academy of Medical Sciences in Moscow as "a drug having psychoactivating and adaptogen properties under complicated conditions (hypoxia, high environmental temperature, physical overfatigue, emotional stress, etc.)". It was found to produce more marked and prolonged psychostimulant effects than the other adamantanes, and eventually entered use. The drug was notably given to soldiers in the Soviet and Russian militaries to "shorten recovery times after strong physical exertion".
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She set a then-world-leading mark of 67.96 m in February 2011, but subsequently received a six-month suspension for testing positive to methylhexanamine, a banned psychostimulant, and was forced to miss the championships. Discus thrower Vera Begić met the B standard, but was not selected for the World Championships.
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Simmons SJ, Leyrer-Jackson JM, Oliver CF, Hicks C, Muschamp JW, Rawls SM, Olive MF. DARK Classics in Chemical Neuroscience: Cathinone-Derived Psychostimulants. ACS Chem. Neurosci. 2018; 9(10): 2379-2394. Beck O, Bäckberg M, Signell P, Helander A. Intoxications in the STRIDA project involving a panorama of psychostimulant pyrovalerone derivatives, MDPV copycats.
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The psychostimulant MDMA (popularized as ecstasy or XTC) is known to affect serotonergic neurons, but has been shown to inhibit synaptosomal and vesicular uptake of serotonin and dopamine to roughly the same extent in vitro. in vivo studies indicate short-term MDMA exposure causes short-term reduction in VMAT2 activity, which is reversed after 24h.
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Fenethylline (BAN, USAN) is a codrug of amphetamine and theophylline which behaves as a prodrug to both of the aforementioned drugs. It is also spelled phenethylline and fenetylline (INN); other names for it are amphetaminoethyltheophylline and amfetyline. The drug was marketed for use as a psychostimulant under the brand names Captagon, Biocapton, and Fitton.
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Additionally, research on the neurobiological effects of physical exercise suggests that daily aerobic exercise, especially endurance exercise (e.g., marathon running), prevents the development of drug addiction and is an effective adjunct therapy (i.e., a supplemental treatment) for amphetamine addiction. Exercise leads to better treatment outcomes when used as an adjunct treatment, particularly for psychostimulant addictions.
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Isopropylamphetamine is a psychostimulant of the substituted amphetamine class. It is an isomer of propylamphetamine and was discovered by a team at Astra Laekemedel AB.CA 1073913 A2 - Amphetamine Derivatives The isopropyl moiety reduces the stimulant activity of the compound but greatly increases the duration of action. For this reason, the compound is not used recreationally.
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Martha Farah is a cognitive neuroscientist from the University of Pennsylvania. She discussed the history of psychostimulant medication, and some of the controversies as well. She mentioned the incorrect belief that medication will make the consumer smarter, and claimed this theory was wrong. Anjan Chatterjee is the chair of neurology of the University of Pennsylvania.
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There is some evidence for the addition of a thyroid hormone, triiodothyronine, in patients with normal thyroid function. Stephen M. Stahl, renowned academician in psychopharmacology, has stated resorting to a dynamic psychostimulant, in particular, d-amphetamine is the "classical augmentation strategy for treatment-refractory depression". However, the use of stimulants in cases of treatment-resistant depression is relatively controversial.
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He performed on a 4-string tenor banjo shortly after entering grade 1. As a child, Danko was hyperactive, but was diagnosed in an era before Ritalin became mainstream. Antidepressants were given to children with attention deficit hyperactivity disorder from the late 1940s to the late 1950s because psychostimulant drug weren't handed out to hyperactive children until the early 1960s.
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Autopsy results released by the Oklahoma State Medical Examiner indicated that Terence Crutcher had "acute phencyclidine (PCP) intoxication" at the time of the shooting. The report stated that Crutcher had 96 nanograms per milliliter of PCP in his blood at the time of death. The report also indicated that tenocyclidine (TCP), a psychostimulant and hallucinogen which is more potent than PCP, was present.
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Clinical and preclinical evidence indicate that consistent aerobic exercise, especially endurance exercise (e.g., marathon running), actually prevents the development of certain drug addictions and is an effective adjunct treatment for drug addiction, and psychostimulant addiction in particular. Consistent aerobic exercise magnitude-dependently (i.e., by duration and intensity) reduces drug addiction risk, which appears to occur through the reversal of drug-induced, addiction- related neuroplasticity.
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Benocyclidine, also known as benzothiophenylcyclohexylpiperidine (BTCP), is a psychoactive recreational drug of the arylcyclohexylamine class which is related to phencyclidine (PCP). It was first described in a patent application naming Marc Caron and colleagues at Duke University in 1997.PCT Patent Application WO199712513 (see also US Patents Nos.5,866,756 and 6,218,595 It acts as a potent and selective dopamine reuptake inhibitor (DRI) and a psychostimulant.
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Within the DMN, functional connectivity is reduced and resting state activity is used to diagnose ADHD in children. Treatment for ADHD, includes psychostimulant medication that directly affects PCC activity. Other studies addressing medication for PCC abnormalities, report that the PCC may only respond to stimulant treatments and the effectiveness of medication can be dependent on motivation levels. Furthermore, ADHD has been associated with the gene SNAP25.
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Maier J, Mayer FP, Luethi D, Holy M, Jäntsch K, Reither H, Hirtler L, Hoener MC, Liechti ME, Pifl C, Brandt SD, Sitte HH. The psychostimulant (±)-cis-4,4'-dimethylaminorex (4,4'-DMAR) interacts with human plasmalemmal and vesicular monoamine transporters. Neuropharmacology. 2018 Aug;138:282-291. A number of related compounds are known, and new derivatives have continued to appear on the designer drug market.
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GBR-13098 is a psychostimulant and selective dopamine uptake inhibitor. Blocking the endogenous striatal dopamine (DA) transporter with GBR-13098 in mice has been shown to prevent damage to the DA nerve terminals caused by malonate. It was suggested that DA transporter inhibitors like GBR-13098 could be used to prevent or treat neurodegenerative disorders caused by the effect of mitochondrial dysfunction on DA homeostasis.
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Cinnamedrine (INN, USAN), also known as N-cinnamylephedrine, is a sympathomimetic drug with similar effects relative to those of ephedrine. It also has some local anesthetic activity. Cinnamedrine was previously used, in combination with analgesics, as an antispasmodic to treat dysmenorrhea in the over-the-counter drug Midol in the 1980s. There is a case report of the drug being abused as a psychostimulant.
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Caffeine's widespread appeal is due primarily to its mild psychostimulant properties, which increase alertness and cognitive arousal and diminish fatigue. Caffeine also produces a wide range of other symptoms, including upregulation of the cardiovascular system, increased global cognitive processing, and improved physical functioning. Cardiovascular effects can range from increased heart rate and reactivity to severe cardiac arrhythmia. The cognitive effects of caffeine include increased performance in memory, attention, and text reading.
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3,3,-Diphenylcyclobutanamine is a psychostimulant drug which was originally prepared as an antidepressant in the late 1970s. It appears to inhibit the reuptake of serotonin, norepinephrine, and dopamine, and may also induce their release as well. The N-methyl and N,N-dimethyl analogues of the compound are also known and are more potent. All three agents produce locomotor stimulation in animal studies, with the tertiary amine being the strongest.
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Tenocyclidine (TCP) was discovered by a team at Parke-Davis in the late 1950s. Heterocyclic compounds and methods for producing the same It is a dissociative anesthetic drug with psychostimulant and hallucinogenic effects. It is similar in effects to phencyclidine (PCP) but is considerably more potent. TCP has slightly different binding properties to PCP, with more affinity for the NMDA receptors, but less affinity for the sigma receptors.
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CREB has a well-documented role in neuronal plasticity and long-term memory formation in the brain. Cocaine- and amphetamine-regulated transcript, also known as CART, is an neuropeptide protein that in humans is encoded by the CARTPT gene. CART appears to have roles in reward, feeding, stress, and it has the functional properties of an endogenous psychostimulant. Taking into account that CART production is upregulated by CREB.
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Thozalinone (USAN) (brand name Stimsen; former developmental code name CL-39808) is a psychostimulant that has been used as an antidepressant in Europe. It has also been trialed as an anorectic. Thozalinone is described as a "dopaminergic stimulant", and likely acts via inducing the release of dopamine and to a minimal extent norepinephrine; similar to analogue pemoline, it is seemingly devoid of abuse potential unlike common psychostimulants that increase catecholamines.
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In particular, aerobic exercise decreases psychostimulant self-administration, reduces the reinstatement (i.e., relapse) of drug-seeking, and induces increased dopamine receptor D2 (DRD2) density in the striatum. This is the opposite of pathological stimulant use, which induces decreased striatal DRD2 density. One review noted that exercise may also prevent the development of a drug addiction by altering ΔFosB or immunoreactivity in the striatum or other parts of the reward system.
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"Brother's Little Helper" is the second episode of The Simpsons' eleventh season. It first aired on the Fox network in the United States on October 3, 1999. In the episode, Bart floods the school gymnasium and the schoolyard, which prompts the school's principal Seymour Skinner to diagnose Bart with ADHD. Bart is prescribed a psychostimulant drug called Focusyn (a parody of Ritalin), and initially starts paying more attention to his studies.
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Adapromine is an antiviral drug of the adamantane group related to amantadine (1-aminoadamantane), rimantadine (1-(1-aminoethyl)adamantane), and memantine (1-amino-3,5-dimethyladamantane) that is marketed in Russia for the treatment and prevention of influenza. It is an alkyl analogue of rimantadine and is similar to rimantadine in its antiviral activity but possesses a broader spectrum of action, being effective against influenza viruses of both type A and B. Strains of type A influenza virus with resistance to adapromine and rimantadine and the related drug deitiforine were encountered in Mongolia and the Soviet Union in the 1980s. Electroencephalography (EEG) studies of animals suggest that adapromine and related adamantanes including amantadine, bromantane (1-amino-2-bromophenyladamantane), and memantine have psychostimulant-like and possibly antidepressant-like effects, and that these effects may be mediated via catecholaminergic processes. These psychostimulant effects differ qualitatively from those of conventional psychostimulants like amphetamine however, and the adamantane derivatives have been described contrarily as "adaptogens" and as "actoprotectors".
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Methylphenidate has shown some benefits as a replacement therapy for individuals who are addicted to and dependent upon methamphetamine. Methylphenidate and amphetamine have been investigated as a chemical replacement for the treatment of cocaine addiction in the same way that methadone is used as a replacement drug for physical dependence upon heroin. Its effectiveness in treatment of cocaine or psychostimulant addiction, or psychological dependence has not been proven and further research is needed.
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Some medications, such as seizure and ulcer medications and antibiotics containing erythromycin, can interfere with the way theophylline works. Coffee, tea, colas, cigarette-smoking, and viral illnesses can all affect the action of theophylline and change its effectiveness. A physician should monitor dosage levels to meet each patient's profile and needs. Additionally some psychostimulant drugs that have an amphetamine like mode of action, such as amphetamine,Amphetamine is listed as having medical uses as bronchodilator.
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Continuous exercise can produce a transient state of euphoria – a positively-valenced affective state involving the experience of pleasure and feelings of profound contentment, elation, and well-being – which is colloquially known as a "runner's high" in distance running or a "rower's high" in rowing. Current medical reviews indicate that several endogenous euphoriants are responsible for producing exercise-related euphoria, specifically phenethylamine (an endogenous psychostimulant), (an endogenous opioid), and anandamide (an endogenous cannabinoid).
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IAD may be associated with a co-morbidity, so treating a related disorder may also help in the treatment of IAD. When addicts were treated with certain anti-depressants it reduced time online by 65% and also reduced cravings of being online. The anti-depressants that have been most successful are selective serotonin reuptake inhibitors such as escitalopram and a heterocyclic atypical anti-depressant called bupropion. A psychostimulant, methylphenidate has also shown beneficial effects.
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A serotonin–norepinephrine-dopamine releasing agent (SNDRA), also known as a triple releasing agent (TRA), is a type of drug which induces the release of serotonin, norepinephrine/epinephrine, and dopamine in the brain and body. SNDRAs produce euphoriant, entactogen, and psychostimulant effects, and are almost exclusively encountered as recreational drugs. A closely related type of drug is a serotonin–norepinephrine–dopamine reuptake inhibitor (SNDRI). Stahl uses the term "Trimonoaminergic Modulators" (TMM) in his work.
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Additionally, many drugs of abuse such as cocaine and methylphenidate possess NRI activity, though it is important to mention that NRIs without combined dopamine reuptake inhibitor (DRI) properties are not significantly rewarding and hence are considered to have a negligible abuse potential. However, norepinephrine has been implicated as acting synergistically with dopamine when actions on the two neurotransmitters are combined (e.g., in the case of NDRIs) to produce rewarding effects in psychostimulant drugs of abuse.
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Bromantane is described primarily as a mild psychostimulant and anxiolytic. It is also said to possess antiasthenic properties. Bromantane is reported to improve physical and mental performance, and hence could be considered a performance-enhancing drug. Bromantane has been found to lower the levels of pro-inflammatory cytokines IL-6, IL-17 and IL-4 and to normalize behavior in animal models of depression, and may possess clinical efficacy as an antidepressant.
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In 2004, it was discovered that amantadine and memantine bind to and act as agonists of the σ1 receptor (Ki = 7.44 μM and 2.60 μM, respectively) and that activation of the σ1 receptor is involved in the dopaminergic effects of amantadine at therapeutically relevant concentrations. These findings might also extend to the other adamantanes such as adapromine, rimantadine, and bromantane and could explain the psychostimulant-like effects of this family of compounds.
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Decreased PEA metabolism has been linked to schizophrenia, a logical finding considering excess PEA would result in over-activation of TAAR1 and prevention of monoamine transporter function. Mutations in region q23.1 of human chromosome 6 – the same chromosome that codes for TAAR1 – have been linked to schizophrenia. Medical reviews from February 2015 and 2016 noted that TAAR1-selective ligands have significant therapeutic potential for treating psychostimulant addictions (e.g., cocaine, amphetamine, methamphetamine, etc.).
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Propylhexedrine, sold under the brand names Benzedrex and Obesin among others, is a nasal decongestant, appetite suppressant, and psychostimulant medication. It is used medicinally for relief of congestion due to colds, allergies and allergic rhinitis and recreationally for its euphoric effects. The effects are similar to those of methamphetamine, though the duration of propylhexedrine is much shorter. Propylhexedrine differs from methamphetamine only in that it has a saturated cyclohexane ring where methamphetamine has a phenyl ring.
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In zebrafish and in humans, loss of GRK5 function has been associated with heart defects due to heterotaxy, a series of developmental defects arising from improper left-right laterality during organogenesis. In the mouse, GRK6 regulation of D2 dopamine receptors in the striatum region of the brain alters sensitivity to psychostimulant drugs that act through dopamine, and GRK6 has been implicated in Parkinson’s disease and in the dyskinesia side effects of anti-parkinson therapy with the drug L-DOPA.
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Methamphetamine (contracted from ) is a potent psychostimulant of the phenethylamine and amphetamine classes that is used to treat attention deficit hyperactivity disorder (ADHD) and obesity. Methamphetamine exists as two enantiomers, dextrorotary and levorotary. Dextromethamphetamine is a stronger CNS stimulant than levomethamphetamine; however, both are addictive and produce the same toxicity symptoms at high doses. Although rarely prescribed due to the potential risks, methamphetamine hydrochloride is approved by the United States Food and Drug Administration (USFDA) under the trade name Desoxyn.
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There is evidence that dopamine receptors play a central role in the behavioral responses of animals to cocaine, amphetamines, and other psychostimulant drugs. One action causes the dopamine molecules to be released from inside the vesicles into the cytoplasm of the nerve terminal, which are then transported outside by the mesolimbic dopamine pathway to the nucleus accumbens. This plays a key role in the rewarding and reinforcing effects of cocaine and amphetamine in animals, and is the primary mechanism for amphetamine dependence.
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A meta-analytic review on the efficacy of various behavioral therapies for treating drug and behavioral addictions found that cognitive behavioral therapy (e.g., relapse prevention and contingency management), motivational interviewing, and a community reinforcement approach were effective interventions with moderate effect sizes. Clinical and preclinical evidence indicate that consistent aerobic exercise, especially endurance exercise (e.g., marathon running), actually prevents the development of certain drug addictions and is an effective adjunct treatment for drug addiction, and for psychostimulant addiction in particular.
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In June 2011 it was announced that Perković had failed two doping tests conducted in the month before at the Diamond League meetings in Rome and Shanghai. She tested positive for methylhexanamine, a psychostimulant banned by the World Anti-Doping Agency since 2010. Perković stated that the positive results were due to Nox Pump, an American-made energy drink product she had been using without knowing it contained banned substances. She did not request an analysis of her B-sample.
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The mode of antidepressant action of isoniazid is still unclear. It is speculated that its effect is due to the inhibition of diamine oxidase, coupled with a weak inhibition of monoamine oxidase A. Selikoff and Robitzek also experimented with another anti-tuberculosis drug, iproniazid; it showed a greater psychostimulant effect, but more pronounced toxicity. Later, Jackson Smith, Gordon Kamman, George E. Crane, and Frank Ayd, described the psychiatric applications of iproniazid. Ernst Zeller found iproniazid to be a potent monoamine oxidase inhibitor.
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Bromantane is a stimulant drug with anxiolytic properties developed in Russia during the late 1980s. Bromantane acts mainly by facilitating the biosynthesis of dopamine, through indirect genomic upregulation of relevant enzymes (tyrosine hydroxylase (TH) and aromatic L-amino acid decarboxylase (AAAD), a.k.a. DOPA decarboxylase), although at very high doses bromantane also has anticholinergic effects. Study results suggest that the combination of psychostimulant and anxiolytic actions in the spectrum of psychotropic activity of bromantane is effective in treating asthenic disorders compared to placebo.
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One review noted that exercise may prevent the development of drug addiction by altering ΔFosB or c-Fos immunoreactivity in the striatum or other parts of the reward system. Moreover, aerobic exercise decreases psychostimulant self-administration, reduces the reinstatement (i.e., relapse) of drug-seeking, and induces opposite effects on striatal dopamine receptor D2 (DRD2) signaling (increased DRD2 density) to those induced by pathological stimulant use (decreased DRD2 density). Consequently, consistent aerobic exercise may lead to better treatment outcomes when used as an adjunct treatment for drug addiction.
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Norepinephrine reuptake inhibitors (NRIs or NERIs) are a type of drug that acts as a reuptake inhibitor for the neurotransmitter norepinephrine (noradrenaline) by blocking the action of the norepinephrine transporter (NET). This in turn leads to increased extracellular concentrations of norepinephrine. NRIs are commonly used in the treatment of conditions like ADHD and narcolepsy due to their psychostimulant effects and in obesity due to their appetite suppressant effects. They are also frequently used as antidepressants for the treatment of major depressive disorder, anxiety and panic disorder.
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The therapeutic effects of bromantane in asthenia are said to onset within 1- to 3-days. It has been proposed that the combination of psychostimulant and anxiolytic activity may give bromantane special efficacy in the treatment of asthenia. In a large-scale, multi-center clinical trial of 728 patients diagnosed with asthenia, bromantane was given for 28 days at a daily dose of 50 mg or 100 mg. The impressiveness were 76.0% on the CGI-S and 90.8% on the CGI-I, indicating broadly-applicable, high effectiveness.
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In the 1960s, the adamantane derivative amantadine (1-aminoadamantane) was developed as an antiviral drug for the treatment of influenza. Other adamantane antivirals subsequently followed, such as rimantadine (1-(1-aminoethyl)adamantane) and adapromine (1-(1-aminopropyl)adamantane). It was serendipitously discovered in 1969 that amantadine possesses central dopaminergic psychostimulant-like properties, and subsequent investigation revealed that rimantadine and adapromine also possess such properties. Amantadine was then developed and introduced for the treatment of Parkinson's disease due to its ability to increase dopamine levels in the brain.
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Chlorphentermine (trade names Apsedon, Desopimon, Lucofen) is a serotonergic appetite suppressant of the amphetamine family. Developed in 1962, it is the 4-chloro derivative of the better known appetite suppressant phentermine, which is still in current use. Chlorphentermine acts as a highly selective serotonin releasing agent (SRA). It is not a psychostimulant and has little or no abuse potential, but is classed as a Schedule III drug in the USA due mainly to its similarity to other appetite suppressants such as diethylpropion which have been more widely abused.
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The field of monoamine transporter research began roughly five decades ago with Julius Axelrod's research on NETs. Axelrod eventually received his Nobel Prize for this research, which led to the discovery of DATs and SERTs as well as consequences associated with antidepressant and psychostimulant interactions with MAT proteins. Since Axelrod's initial studies, understanding the pharmacological and functional properties of MAT proteins have been essential in the discovery of therapeutic treatment of many mental disorders. During the 1990s various cloning techniques using MATs have elucidated the genetic structure of these proteins.
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It appears to be an anticholinergic (specifically at alpha-7 nicotinic receptors) like the similar pharmaceutical memantine. In 2004, it was discovered that amantadine and memantine bind to and act as agonists of the σ1 receptor (Ki = 7.44 μM and 2.60 μM, respectively), and that activation of the σ1 receptor is involved in the dopaminergic effects of amantadine at therapeutically relevant concentrations. These findings may also extend to the other adamantanes such as adapromine, rimantadine, and bromantane, and could explain the psychostimulant-like effects of this family of compounds.
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Bromantane, sold under the brand name Ladasten, is an atypical psychostimulant and anxiolytic drug of the adamantane family related to amantadine and memantine which is used in Russia in the treatment of neurasthenia. Although the effects of the bromantane have been determined to be dependent on the dopaminergic and possibly serotonergic neurotransmitter systems, its exact mechanism of action is unknown, and it is distinct in its properties relative to typical psychostimulants such as amphetamine. Because of its unique aspects, bromantane has sometimes been described instead as an adaptogen and actoprotector.
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Monoamine releasing agents can have a wide variety of effects depending upon their selectivity for monoamines. Selective serotonin releasing agents such as fenfluramine and related compounds are described as dysphoric and lethargic in lower doses, and in higher doses some hallucinogenic effects have been reported. Less selective serotonergic agents that stimulate an efflux in dopamine, such as MDMA are described as more pleasant, increasing energy, sociability and elevating mood. Dopamine releasing agents, usually selective for both norepinephrine and dopamine have psychostimulant effect, causing an increase in energy, and elevated mood.
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Additionally, many drugs of abuse such as cocaine and methylphenidate possess NRI activity, though it is important to mention that NRIs without combined dopamine reuptake inhibitor (DRI) properties are not significantly rewarding and hence are considered to have a negligible abuse potential. However, norepinephrine has been implicated as acting synergistically with dopamine when actions on the two neurotransmitters are combined (e.g., in the case of NDRIs) to produce rewarding effects in psychostimulant drugs of abuse. A meta analysis published in BMJ in 2011 concluded that the selective NRI reboxetine is indistinguishable from placebo in the treatment of depression.
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Azacyclonol (trade names Ataractan, Calmeran, Frenoton, Frenquel, Psychosan), also known as γ-pipradrol, is a drug which is an ataractive; an agent which diminishes hallucinations in psychotic individuals. It has also been called a tranquilizer and antipsychotic, though these definitions are not accurate as it does not actually possess such properties. Despite being a positional isomer of pipradrol, it is not a psychostimulant, and instead has mild depressant effects. The drug was introduced in Europe in the mid-1950s for the treatment of schizophrenia likely because it was found to attenuate the subjective psychedelic effects of LSD and mescaline in humans.
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A dopamine reuptake inhibitor (DRI) is a class of drug which acts as a reuptake inhibitor of the monoamine neurotransmitter dopamine by blocking the action of the dopamine transporter (DAT). Reuptake inhibition is achieved when extracellular dopamine not absorbed by the postsynaptic neuron is blocked from re-entering the presynaptic neuron. This results in increased extracellular concentrations of dopamine and increase in dopaminergic neurotransmission. DRIs are used in the treatment of attention-deficit hyperactivity disorder (ADHD) and narcolepsy for their psychostimulant effects, and in the treatment of obesity and binge eating disorder for their appetite suppressant effects.
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Because of its high affinity for the PCP site of the NMDA receptor complex, the 3H radiolabelled form of TCP is widely used in research into NMDA receptors. TCP acts primarily as an NMDA receptor antagonist which blocks the activity of the NMDA receptor, however its increased psychostimulant effects compared to PCP suggests it also has relatively greater activity as a dopamine reuptake inhibitor (DRI). Due to its similarity in effects to PCP, TCP was placed into the Schedule I list of illegal drugs in the 1970s, although it was only briefly used in the 1970s and 1980s and is now little known.
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Modafinil acid (code name CRL-40467), also known as modafinilic acid or modafinil carboxylate, is the major metabolite of modafinil, and one of the two major metabolites of modafinil – the other being modafinil sulfone. Modafinil acid is also a metabolite of the modafinil prodrug, adrafinil, and the (R)-(–)-enantiomer is a metabolite of armodafinil, the (R)-(–)-enantiomer of modafinil. Modafinil acid seems to be inactive, and similarly to modafinil sulfone, does not appear to contribute to the wakefulness- promoting/psychostimulant effects of modafinil. In the breakdown process of modafinil, modafinil is primarily hydrolyzed by an esterase or amidase enzyme into modafinil acid.
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Cypenamine (INN, BAN), or cypenamine hydrochloride (USAN), also known as 2-phenylcyclopentylamine, is a psychostimulant drug which was developed by a group at the William S. Merrell Chemical Company in the 1940s. It is currently known only in scientific research and has never been developed for market use. Cypenamine is currently legal throughout the entire world, and though its chemical structure has a vague similarity to certain controlled stimulants like fencamfamine, it is likely that it is too distant for it to be considered an illicit analogue under the United States Federal Analogue Act of the Controlled Substances Act.
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Cocaine is a powerful psychostimulant and known to be one of the most widely abused substances. Cocaine is a nonselective, reuptake inhibitor of the norepinephrine, serotonin, and dopamine transporters. This thwarts the absorption of these chemicals into the presynaptic terminal and allows a large concentration of dopamine, serotonin and norepinephrine to build up in the synaptic cleft. The potential for cocaine addiction is thought to be a result of its effects on dopamine transporters in the CNS, while it has been suggested that the life- threatening cardiovascular effects of cocaine may involve the inhibition of NETs at sympathetic and CNS autonomic synapses.
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Norepinephrine Epinephrine A norepinephrine reuptake inhibitor (NRI, NERI) or noradrenaline reuptake inhibitor or adrenergic reuptake inhibitor (ARI), is a type of drug that acts as a reuptake inhibitor for the neurotransmitters norepinephrine (noradrenaline) and epinephrine (adrenaline) by blocking the action of the norepinephrine transporter (NET). This in turn leads to increased extracellular concentrations of norepinephrine and epinephrine and therefore can increase adrenergic neurotransmission. NRIs are commonly used in the treatment of conditions like ADHD and narcolepsy due to their psychostimulant effects and in obesity due to their appetite suppressant effects. They are also frequently used as antidepressants for the treatment of major depressive disorder, anxiety and panic disorder.
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Methylphenidate has been the subject of controversy in relation to its use in the treatment of ADHD. The prescription of psychostimulant medication to children to reduce ADHD symptoms has been a major point of criticism. The contention that methylphenidate acts as a gateway drug has been discredited by multiple sources, according to which abuse is statistically very low and "stimulant therapy in childhood does not increase the risk for subsequent drug and alcohol abuse disorders later in life". A study found that ADHD medication was not associated with increased risk of cigarette use, and in fact stimulant treatments such as Ritalin seemed to lower this risk.
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3,4-Dichloromethylphenidate (or 3,4-DCMP) is a stimulant drug related to methylphenidate. Dichloromethylphenidate is a potent psychostimulant that acts as both a dopamine reuptake inhibitor and norepinephrine reuptake inhibitor, meaning it effectively boosts the levels of the norepinephrine and dopamine neurotransmitters in the brain, by binding to, and partially blocking the transporter proteins that normally remove those monoamines from the synaptic cleft. 3,4-DCMP, the threo-diastereomer, is approximately seven times more potent than methylphenidate in animal studies, but has weaker reinforcing effects due to its slower onset of action. However, H. M. Deutsch's discrimination ratio implies it to be more reinforcing than cocaine.
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Perković culminated her successful junior career by winning gold at the 2009 European Junior Championships with a new national record. A month later, she made the final of the World Championships as the youngest discus thrower in the field. In her first year of senior competition she won gold at the 2010 European Championships, becoming the youngest ever European champion in women's discus throw. A six-month doping suspension after testing positive for a banned psychostimulant kept her out of competition for most of the 2011 season, including the World Championships, but she returned in strong form in 2012 and successfully defended her title in the European Championships.
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3,4-Methylenedioxyamphetamine (MDA), is an empathogen-entactogen, psychostimulant, and psychedelic drug of the amphetamine family that is encountered mainly as a recreational drug. In terms of pharmacology, MDA acts most importantly as a serotonin-norepinephrine-dopamine releasing agent (SNDRA). In most countries, the drug is a controlled substance and its possession and sale are illegal. MDA is rarely sought after as a recreational drug compared to other drugs in the amphetamine family; however, it remains an important and widely used drug due to it being a primary metabolite, the product of hepatic N-dealkylation, of MDMA (ecstasy), In addition, it is common to find MDA as an adulterant of illicitly produced MDMA.
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Bromantane was once thought to act as a reuptake inhibitor of serotonin and dopamine. Indeed, bromantane does inhibit the reuptake of serotonin, dopamine, and to a lesser extent norepinephrine in vitro in rat brain tissue. However, the concentrations required to do so are extremely high (50–500 μM) and likely not clinically relevant. (Although one study found an IC50 for dopamine transport of 3.56 μM, relative to 28.66 nM for mesocarb; neither drug affected serotonin transport at the tested concentrations, in contrast.) In any case, the lack of typical psychostimulant-like effects and adverse effects seen with bromantane supports the notion that it is not acting significantly as a monoamine reuptake inhibitor, but rather via enhancement of dopamine synthesis.
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Unlike methamphetamine, the psychostimulant cocaine interacts with VMAT2 in such a way that mobilizes VMAT2-expressing vesicles, causing a shift in VMAT2 protein from a plasmalemmal (synaptosomal) membrane fraction to a vesicle-enriched fraction that is not associated with the synaptosomal membrane and not retained in synaptosomal preparations. The drug methylphenidate (branded Ritalin and Concerta) is believed to interact with VMAT2 in a similar fashion. In addition to mobilizing VMAT2-expressing vesicles, cocaine has been shown to increase Vmax of VMAT2 for dopamine, and to increase the number of DTBZ binding sites. Cocaine has also been shown to mobilize a synapsin-dependent reserve pool of dopamine-containing synaptic vesicles, thereby interacting with the vesicular trafficking cycle to increase dopamine release.
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GRK6 exists in three splice variants that differ in the carboxyl terminal region that regulates membrane association: one form is palmitoylated, another contains a lipid-binding polybasic domain, and the third is truncated and has neither. In the mouse, GRK6 regulates the D2 dopamine receptor in the striatum region of the brain, and loss of GRK6 leads to increased sensitivity to psychostimulant drugs that act through dopamine. Overexpression of GRK6 in the striatum in a rat model of Parkinson’s disease improves drug-induced movement disorder (tardive dyskinesia) symptoms arising from L-DOPA therapy. In mouse immune cells, GRK6 is important for chemotaxis of B-lymphocytes and T-lymphocytes in response to the chemoattractant CXCL12, and of neutrophils to sites of injury in response to leukotriene B4.
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Take Your Pills is an hour-long American documentary from 2018, directed by Alison Klayman and produced by Motto Pictures and Netflix Studios. The documentary explores the positives and negatives of taking psychostimulant medications, such as Adderall—the main focus of the documentary. The film is a series of interviews with college students and working adults who are prescribed stimulants for attention deficit hyperactivity disorder (ADHD), along with parents who touch on the difficulties raising children with ADHD and interviews with professionals commenting on the use of stimulants. Those interviewed include former player for the NFL's Jacksonville Jaguars Eben Britton, and neuroscientist Anjan Chatterjee. The film’s executive producers were Maria Shriver and Christina Schwarzenegger; its world premiere was at the SXSW film festival in 2018.
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Subsequent studies of the racemates showed that the central stimulant activity is associated with the threo racemate and were focused on the separation and interconversion of the erythro isomer into the more active threo isomer.Leandro Panizzon et al Pyridine and piperdjine compounds Issue date: 16 May 1950Rudolf Rouietscji et al Process for the conversion of Issue date: 10 June 1958Rudolf Rouietscji et alProcess for the conversion of Issue date: 25 October 1960 Methylphenidate was first used to allay barbiturate- induced coma, narcolepsy and depression. It was later used to treat memory deficits in the elderly. Beginning in the 1960s, it was used to treat children with ADHD based on earlier work starting with the studies by American psychiatrist Charles Bradley on the use of psychostimulant drugs, such as Benzedrine, with then called "maladjusted children".
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Pseudophenmetrazine is a psychostimulant compound of the morpholine class. It is the N-demethylated and cis-configured analogue of phendimetrazine as well as the cis-configured stereoisomer of phenmetrazine. In addition, along with phenmetrazine, it is believed to be one of the active metabolites of phendimetrazine, which itself is inactive and behaves merely as a prodrug. Relative to phenmetrazine, pseudophenmetrazine is of fairly low potency, acting as a modest releasing agent of norepinephrine (EC50 = 514 nM), while its (+)-enantiomer is a weak releaser of dopamine (EC50 = 1,457 nM) whereas its (−)-enantiomer is a weak reuptake inhibitor of dopamine (Ki = 2,691 nM); together as a racemic mixture with the two enantiomers combined, pseudophenmetrazine behaves overall more as a dopamine reuptake inhibitor (Ki = 2,630 nM), possibly due to the (+)-enantiomer blocking the uptake of the (−)-enantiomer into dopaminergic neurons and thus preventing it from inducing dopamine release.
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Ethylphenidate (EPH) is a psychostimulant and a close analog of methylphenidate. Ethylphenidate acts as both a dopamine reuptake inhibitor and norepinephrine reuptake inhibitor, meaning it effectively boosts the levels of the norepinephrine and dopamine neurotransmitters in the brain, by binding to, and partially blocking the transporter proteins that normally remove those monoamines from the synaptic cleft. However, considering the close similarities between ethylphenidate and methylphenidate and the fact that methylphenidate, like cocaine, actually does not primarily act as a "classical" reuptake inhibitor, but rather as an "inverse agonist at the DAT" (also called a "negative allosteric modulator at the DAT"), it is at least very likely that ethylphenidate also primarily acts as an inverse DAT agonist instead of (or at least only secondarily) as a classical reuptake inhibitor (which could be called a "competitive antagonist at the DAT" using a similar terminology as "negative allosteric modulator at the DAT", which per definition means that its mechanism is non-competitive). There have been anecdotal reports of a perforated septum resulting from even just a few uses of ethylphenidate by insufflation (snorting).
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While caffeine does not directly bind to any dopamine receptors, it influences the binding activity of dopamine at its receptors in the striatum by binding to adenosine receptors that have formed GPCR heteromers with dopamine receptors, specifically the A1–D1 receptor heterodimer (this is a receptor complex with 1 adenosine A1 receptor and 1 dopamine D1 receptor) and the A2A–D2 receptor heterotetramer (this is a receptor complex with 2 adenosine A2A receptors and 2 dopamine D2 receptors). The A2A–D2 receptor heterotetramer has been identified as a primary pharmacological target of caffeine, primarily because it mediates some of its psychostimulant effects and its pharmacodynamic interactions with dopaminergic psychostimulants. Caffeine also causes the release of dopamine in the dorsal striatum and nucleus accumbens core (a substructure within the ventral striatum), but not the nucleus accumbens shell, by antagonizing A1 receptors in the axon terminal of dopamine neurons and A1–A2A heterodimers (a receptor complex composed of 1 adenosine A1 receptor and 1 adenosine A2A receptor) in the axon terminal of glutamate neurons. During chronic caffeine use, caffeine-induced dopamine release within the nucleus accumbens core is markedly reduced due to drug tolerance.
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