Norepinephrine Releasing Agents
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Norepinephrine Releasing Agents
A norepinephrine releasing agent (NRA), also known as an adrenergic releasing agent, is a catecholaminergic type of drug that induces the synapse, release of norepinephrine (noradrenaline) and epinephrine (adrenaline) from the synapse, pre-synaptic neuron into the synapse. This in turn leads to increased extracellular concentrations of norepinephrine and epinephrine therefore an increase in adrenergic neurotransmission. A closely related type of drug is a norepinephrine reuptake inhibitor (NRI), for instance reboxetine. Another class of drugs that stimulates adrenergic activity is the adrenergic receptor agonist class. Uses and examples NRAs, frequently as norepinephrine–dopamine releasing agents (NDRAs) rather than as binding selectivity, selective NRAs, are used for a variety of clinical indications including the following: * For the treatment of attention deficit hyperactivity disorder (ADHD) — e.g., amphetamine, dextroamphetamine, levoamphetamine, lisdexamfetamine, me ...
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Ephedrine V2
Ephedrine is a central nervous system (CNS) stimulant and sympathomimetic agent that is often used to prevent hypotension, low blood pressure during anesthesia. It has also been used for asthma, narcolepsy, and obesity but is not the preferred treatment. It is of unclear benefit in nasal congestion. It can be taken oral administration, by mouth or by intramuscular, injection into a muscle, intravenous, vein, or subcutaneous injection, just under the skin. Onset with intravenous use is fast, while injection into a muscle can take 20minutes, and by mouth can take an hour for effect. When given by injection, it lasts about an hour, and when taken by mouth, it can last up to four hours. Common side effects include insomnia, trouble sleeping, anxiety, headache, hallucinations, hypertension, high blood pressure, tachycardia, fast heart rate, decreased appetite, loss of appetite, and urinary retention. Serious side effects include stroke and myocardial infarction, heart attack. While ...
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Dextroamphetamine
Dextroamphetamine (international nonproprietary name, INN: dexamfetamine) is a potent central nervous system (CNS) stimulant and enantiomer of amphetamine that is used in the treatment of attention deficit hyperactivity disorder (ADHD) and narcolepsy. It is also used illicitly to enhance Nootropic, cognitive and athletic Performance-enhancing substance, performance, and recreationally as an aphrodisiac and euphoriant. Dextroamphetamine is generally regarded as the prototype drug, prototypical stimulant. The amphetamine molecule exists as two enantiomers, levoamphetamine and dextroamphetamine. Dextroamphetamine is the Levorotation and dextrorotation, dextrorotatory, or 'right-handed', enantiomer and exhibits more pronounced effects on the central nervous system than levoamphetamine. Pharmaceutical dextroamphetamine sulfate is available as both a brand name and generic drug in a variety of dosage forms. Dextroamphetamine is sometimes prescribed as the inactive prodrug lisdexamfet ...
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Nasal Decongestant
A decongestant, or nasal decongestant, is a type of pharmaceutical drug that is used to relieve nasal congestion in the upper respiratory tract. The active ingredient in most decongestants is either pseudoephedrine or phenylephrine (the latter of which has disputed effectiveness). Intranasal corticosteroids can also be used as decongestants and antihistamines can be used to alleviate runny nose, nasal itch, and sneezing. Topical decongestants on topical application as dilute solution (0.05–0.1%) produce local vasoconstriction. Regular use of decongestants for long periods should be avoided because mucosal ciliary function is impaired: atrophic rhinitis and anosmia (loss of the sense of smell) can occur due to persistent vasoconstriction. Decongestants can be absorbed from the nose via an inhaler and produce systemic effects, mainly central nervous system stimulation and rise in blood pressure. These drugs should be used cautiously in hypertensives and in those receiving ...
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Narcolepsy
Narcolepsy is a chronic neurological disorder that impairs the ability to regulate sleep–wake cycles, and specifically impacts REM (rapid eye movement) sleep. The symptoms of narcolepsy include excessive daytime sleepiness (EDS), sleep-related hallucinations, sleep paralysis, disturbed nocturnal sleep (DNS), and cataplexy. People with narcolepsy typically have poor quality of sleep. There are two recognized forms of narcolepsy, narcolepsy type 1 and type 2. Narcolepsy type 1 (NT1) can be clinically characterized by symptoms of EDS and cataplexy, and/or will have cerebrospinal fluid (CSF) orexin levels of less than 110 pg/ml. Cataplexy are transient episodes of aberrant tone, most typically loss of tone, that can be associated with strong emotion. In pediatric-onset narcolepsy, active motor phenomena are not uncommon. Cataplexy may be mistaken for syncope, tics, or seizures. Narcolepsy type 2 (NT2) does not have features of cataplexy, and CSF orexin levels are normal. ...
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Wakefulness-promoting Agent
A wakefulness-promoting agent (WPA), or wake-promoting agent, is a drug that increases wakefulness and arousal. They are similar to but distinct from psychostimulants, which not only promote wakefulness but also produce other more overt central nervous system effects, such as improved attention span, executive functions, vigilance and motivation. Wakefulness-promoting agents are used to treat narcolepsy and hypersomnia as well as to promote wakefulness and increase performance in healthy people. A variety of different classes of drugs have shown wakefulness-promoting effects, including: * Dopamine reuptake inhibitors like modafinil, armodafinil, mesocarb, phenylpiracetam, and vanoxerine * Norepinephrine–dopamine reuptake inhibitors like methylphenidate, solriamfetol, mazindol, bupropion, nomifensine, and amineptine * Norepinephrine–dopamine releasing agents like amphetamine and methamphetamine * Norepinephrine reuptake inhibitors like atomoxetine and reboxetine * ...
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Aminorex
Aminorex, sold under the brand names Menocil and Apiquel among others, is a weight loss (anorectic) stimulant drug. It was withdrawn from the market after it was found to cause pulmonary hypertension (PPH). In the United States, aminorex is a Schedule I controlled substance. Aminorex, in the 2-amino-5-aryloxazoline group, was developed by McNeil Laboratories in 1962. It is closely related to 4-methylaminorex (4-MAR). Aminorex has been shown to have locomotor-stimulant effects, lying midway between dextroamphetamine and methamphetamine. Aminorex effects have been attributed to the release of catecholamines. It can be produced as a metabolite of the deworming medication levamisole, which is sometimes used as a cutting agent of illicitly produced cocaine. Pharmacology Pharmacodynamics Aminorex is a serotonin–norepinephrine–dopamine releasing agent (SNDRA). Its values for induction of monoamine release are 26.4nM for norepinephrine, 49.4nM for dopamine, and 193nM fo ...
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Phenmetrazine
Phenmetrazine, sold under the brand name Preludin among others, is a stimulant drug first chemical synthesis, synthesized in 1952 and originally used as an appetite suppressant, but withdrawn drug, withdrawn from the market in the 1980s due to widespread drug misuse, misuse. It was initially replaced by its structural analog, analogue phendimetrazine (under the brand name Prelu-2) which functions as a prodrug to phenmetrazine, but now it is rarely prescribed, due to concerns of misuse and drug addiction, addiction. Chemically, phenmetrazine is a substituted amphetamine containing a morpholine ring (chemistry), ring or a substituted phenylmorpholine. Medical uses Phenmetrazine has been used as an appetite suppressant for purposes of weight loss. It was used therapeutically for this indication at a dosage of 25mg two or three times per day (or 50–75mg/day total) in adults. Phenmetrazine has been found to produce similar weight loss to dextroamphetamine in people with obesity. I ...
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Benzphetamine
Benzphetamine, sold under the brand name Didrex among others, is an amphetamine-type stimulant and appetite suppressant used short-term for weight loss along with a doctor-approved, reduced-calorie diet, exercise, and behavioral program. It is prescribed for obesity to people who have been unable to lose weight through exercise and dieting alone. It is a prodrug of dextromethamphetamine and dextroamphetamine. Mechanism of Action Benzphetamine promotes weight loss by reducing appetite and slightly increasing metabolism. It is the parent compound of clobenzorex, the latter of which is not subject to the Federal Analogue Act, nor scheduled per the Controlled Substances Act of 1970. Contraindications Benzphetamine is contraindicated in patients with advanced arteriosclerosis, symptomatic cardiovascular disease, moderate to severe hypertension, hyperthyroidism, known hypersensitivity or idiosyncrasy to sympathomimetic amines, and glaucoma, or who have recently used a monoami ...
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Phentermine
Phentermine, sold under the brand name Adipex-P among others, is a medication used together with diet and exercise to treat obesity. It is available by itself or as the combination phentermine/topiramate. Phentermine is taken by mouth. Common side effects include a fast heart beat, high blood pressure, trouble sleeping, dizziness, and restlessness. Serious side effects may include abuse, but do not include pulmonary hypertension or valvular heart disease, as the latter complications were caused by the fenfluramine component of the " fen-phen" combination. Phentermine is a norepinephrine and dopamine releasing agent (NDRA) and produces stimulant, rewarding, and appetite suppressant effects. Chemically, it is a substituted amphetamine. Phentermine was approved for medical use in the United States in 1959. It is available as a generic medication. In 2022, it was the 149th most commonly prescribed medication in the United States, with more than 3million prescriptions. Ph ...
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Binge-eating Disorder
Binge eating disorder (BED) is an eating disorder characterized by frequent and recurrent binge eating episodes with associated negative psychological and social problems, but without the compensatory behaviors common to bulimia nervosa, OSFED, or the binge-purge subtype of anorexia nervosa. BED is a recently described condition, which was introduced to distinguish binge eating similar to that seen in bulimia nervosa but without characteristic purging. Individuals who are diagnosed with bulimia nervosa or binge eating disorder exhibit similar patterns of compulsive overeating, neurobiological features such as dysfunctional cognitive control and food addiction, and biological and environmental risk factors. Some professionals consider BED to be a milder form of bulimia, with the two conditions on the same spectrum. Binge eating is one of the most prevalent eating disorders among adults, though it receives less media coverage and research about the disorder compared to anorexia n ...
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Obesity
Obesity is a medical condition, considered by multiple organizations to be a disease, in which excess Adipose tissue, body fat has accumulated to such an extent that it can potentially have negative effects on health. People are classified as obese when their body mass index (BMI)—a person's weight divided by the square of the person's height—is over ; the range is defined as overweight. Some East Asian countries use lower values to calculate obesity. Obesity is a major cause of disability and is Obesity-associated morbidity, correlated with various diseases and conditions, particularly cardiovascular diseases, type 2 diabetes, obstructive sleep apnea, certain types of cancer, and osteoarthritis. Obesity has individual, socioeconomic, and environmental causes. Some known causes are Western pattern diet, diet, low physical activity, automation, urbanization, quantitative trait locus, genetic susceptibility, medications, mental disorders, Economic policy, economic pol ...
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Anorectic
An anorectic is a drug that reduces appetite, resulting in lower food consumption, leading to weight loss. These substances work by affecting the central nervous system or certain neurotransmitters to create a feeling of fullness or reduce the desire to eat. The understanding of anorexiant effects is crucial in the development of interventions for weight management, eating disorders, and related health concerns. The anorexiant effect can be induced through diverse mechanisms, ranging from hormonal regulation to neural signaling. Ghrelin, leptin, and peptide YY are among the hormones involved in appetite control. Additionally, neurotransmitters such as serotonin and dopamine in the central nervous system contribute significantly to the regulation of food intake. By contrast, an appetite stimulant is referred to as orexigenic. The term is (from the Greek and ), and such drugs are also known as anorexigenic, anorexiant, or appetite suppressant. History Used on a short-term ...
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