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Encyclopedia > Ephedrine
Ephedrine
Systematic (IUPAC) name
(1R,2S)-2-(methylamino)-1-phenylpropan-1-ol
Identifiers
CAS number 299-42-3
ATC code R01AA03 R03CA02 S01FB02
PubChem 5032
DrugBank nil
Chemical data
Formula C10H15NO 
Mol. mass 165.23
Pharmacokinetic data
Bioavailability 85%
Metabolism minimal hepatic
Half life 3–6 hours
Excretion 22-99% renal
Therapeutic considerations
Pregnancy cat.

A(AU) A(US) Image File history File links Efedryna. ... Image File history File links Size of this preview: 800 × 596 pixelsFull resolution (860 × 641 pixel, file size: 108 KB, MIME type: image/png) File historyClick on a date/time to view the file as it appeared at that time. ... IUPAC nomenclature is a system of naming chemical compounds and of describing the science of chemistry in general. ... CAS registry numbers are unique numerical identifiers for chemical compounds, polymers, biological sequences, mixtures and alloys. ... The Anatomical Therapeutic Chemical Classification System is used for the classification of drugs. ... A section of the Anatomical Therapeutic Chemical Classification System. ... A section of the Anatomical Therapeutic Chemical Classification System. ... A section of the Anatomical Therapeutic Chemical Classification System. ... PubChem is a database of chemical molecules. ... The DrugBank database available at the University of Alberta is a unique bioinformatics and cheminformatics resource that combines detailed drug (i. ... A chemical formula is a concise way of expressing information about the atoms that constitute a particular chemical compound. ... For other uses, see Carbon (disambiguation). ... General Name, Symbol, Number hydrogen, H, 1 Chemical series nonmetals Group, Period, Block 1, 1, s Appearance colorless Atomic mass 1. ... General Name, symbol, number nitrogen, N, 7 Chemical series nonmetals Group, period, block 15, 2, p Appearance colorless gas Standard atomic weight 14. ... General Name, symbol, number oxygen, O, 8 Chemical series nonmetals, chalcogens Group, period, block 16, 2, p Appearance colorless (gas) very pale blue (liquid) Standard atomic weight 15. ... The molecular mass (abbreviated Mr) of a substance, formerly also called molecular weight and abbreviated as MW, is the mass of one molecule of that substance, relative to the unified atomic mass unit u (equal to 1/12 the mass of one atom of carbon-12). ... In pharmacology, bioavailability is used to describe the fraction of an administered dose of unchanged drug that reaches the systemic circulation, one of the principal pharmacokinetic properties of drugs. ... Drug metabolism is the metabolism of drugs, their biochemical modification or degradation, usually through specialized enzymatic systems. ... The liver is an organ in vertebrates including humans. ... It has been suggested that Effective half-life be merged into this article or section. ... The kidneys are important excretory organs in vertebrates. ... Kidneys viewed from behind with spine removed The kidneys are bean-shaped excretory organs in vertebrates. ... The pregnancy category of a pharmaceutical agent is an assessment of the risk of fetal injury due to the pharmaceutical, if it is used as directed by the mother during pregnancy. ... For other uses, see Australia (disambiguation). ... Motto: (Out Of Many, One) (traditional) In God We Trust (1956 to date) Anthem: The Star-Spangled Banner Capital Washington D.C. Largest city New York City None at federal level (English de facto) Government Federal constitutional republic  - President George Walker Bush (R)  - Vice President Dick Cheney (R) Independence from...

Legal status

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Routes oral, IV, IM, SC

Ephedrine (EPH) is a sympathomimetic amine similar in structure to the synthetic derivatives amphetamine and methamphetamine. Ephedrine is commonly used as a stimulant, appetite suppressant, concentration aid, decongestant and to treat hypotension associated with regional anaesthesia. Chemically, it is an alkaloid derived from various plants in the genus Ephedra (family Ephedraceae). It is most usually marketed in the hydrochloride and sulfate forms. In pharmacology and toxicology, a route of administration is the path by which a drug, fluid, poison or other substance is brought into contact with the body. ... An intravenous drip in a hospital Intravenous therapy or IV therapy is the administration of liquid substances directly into a vein. ... Intramuscular injection is an injection of a substance directly into a muscle. ... The subcutis is the layer of tissue directly underlying the cutis. ... Sympathomimetics are a class of drugs whose properties mimic those of a stimulated sympathetic nervous system. ... The general structure of an amine Amines are organic compounds and a type of functional group that contain nitrogen as the key atom. ... Amphetamine or Amfetamine(Alpha-Methyl-PHenEThylAMINE), also known as beta-phenyl-isopropylamine and benzedrine, is a prescription stimulant commonly used to treat Attention-deficit hyperactivity disorder (ADHD) in adults and children. ... This article is about the psychostimulant, d-methamphetamine. ... Stimulants are drugs that temporarily increase alertness and wakefulness. ... A decongestant is a broad class of drugs designed to symptomatically treat ailments affecting the respiratory system. ... In physiology and medicine, hypotension refers to an abnormally low blood pressure. ... Chemical structure of ephedrine, a phenethylamine alkaloid An alkaloid is, strictly speaking, a naturally occurring amine produced by a plant,[1] but amines produced by animals and fungi are also called alkaloids. ... Species See text. ... Species See text Ephedra is a genus of gymnosperm shrubs, the only genus in the family Ephedraceae and order Ephedrales. ...


In traditional Chinese medicines, the herb ma huang (Ephedra sinica) contains ephedrine and pseudoephedrine as its principal active constituents. The same is true of other herbal products containing extracts from Ephedra species. Nagayoshi Nagai was the first one to isolate ephedrine from Ephedra vulgaris in 1885. The substance called soma mentioned in old Hindu books such as the Rig Veda, may have been ephedra extract. Binomial name Ephedra sinica Ephedra sinica is a member of the ephedraceae family, native to China. ... Pseudoephedrine (commonly abbreviated as PSE) is a sympathomimetic amine commonly used as a decongestant. ... Nagayoshi Nagai (August 8, 1844 - February 10, 1929) was a notable Japanese chemist, best known for his study of ephedrine. ... Species See text Ephedra vulgaris Rich. ... 1885 (MDCCCLXXXV) is a common year starting on Thursday of the Gregorian calendar (or a common year starting on Saturday of the 12-day slower Julian calendar). ... This article is about the Vedic plant and ritual. ... This article discusses the adherents of Hinduism. ... The Rig Veda ऋग्वेद (Sanskrit ṛc praise + veda knowledge) is the earliest of the four Hindu religious scriptures known as the Vedas. ... Ephedra in medicine. ...


The production of ephedrine in China has become a multi-million dollar export industry. Companies producing for export extract US$13 million worth of ephedrine from 30,000 tons of ephedra annually, 10 times the amount that is used in traditional Chinese medicine.[1]

Contents

Chemistry

Ephedrine exhibits optical isomerism and has two chiral centres. By convention the enantiomers with opposite stereochemistry around the chiral centres are designated ephedrine, while pseudoephedrine has same stereochemistry around the chiral carbons. That is, (1R,2R)- and (1S,2S)-enantiomers are designated pseudoephedrine; while (1R,2S)- and (1S,2R)-enantiomers are designated ephedrine. Optical isomerism is a form of isomerism (specifically stereoisomerism) whereby the different 2 isomers are the same in every way except being non-superimposable mirror images* of each other. ... In chemistry, enantiomers (from the Greek ἐνάντιος, opposite, and μέρος, part or portion) are stereoisomers that are nonsuperimposable complete mirror images of each other, much as ones left and right hands are the same but opposite. ... Pseudoephedrine (commonly abbreviated as PSE) is a sympathomimetic amine commonly used as a decongestant. ...


The isomer which is marketed is (-)-(1R,2S)-ephedrine.[2]


As with other phenylethylamines, it is also somewhat chemically similar to methamphetamine, although the amphetamines are more potent and have additional biological effects. This article is about the psychostimulant, d-methamphetamine. ...


Ephedrine may also be referred to as: (αR)-α-[(1S)-1-(methylamino)ethyl]benzenemethanol, α-[1-(methylamino)ethyl]benzyl alcohol, or L-erythro-2-(methylamino)-1-phenylpropan-1-ol. Ephedrine hydrochloride has a melting point of 187-188°C.[3]


Mode of action

Ephedrine is a sympathomimetic amine - that is, its principal mechanism of action relies on its direct and indirect actions on the adrenergic receptor system, which is part of the sympathetic nervous system or SNS. Central nervous system or CNS involvement is present, but the predominant clinical effects are caused by involvement with the sympathetic segment of the peripheral nervous system due to the fact that while ephedrine does cross the blood-brain barrier, it doesn't do this very efficiently (efficient crossers with similar modes of action would include amphetamine and methamphetamine). Epinephrine Norepinephrine The adrenergic receptors (or adrenoceptors) are a class of G protein-coupled receptors that are targets of the catecholamines. ... The Sympathetic Nervous System (SNS) is a branch of the autonomic nervous system. ...


Ephedrine increases post-synaptic noradrenergic receptor activity by (weakly) directly activating post-synaptic α-receptors and β-receptors, but the bulk of its effect comes from the pre-synaptic neuron being unable to distinguish between real adrenaline or noradrenaline from ephedrine. The ephedrine, mixed with noradrenaline, is transported through the noradrenaline reuptake complex and packaged (along with real noradrenaline) into vesicles that reside at the terminal button of a nerve cell.


As an alkaloid, having some small amount of ephedrine within a noradrenaline vesicle reduces the overall pH of the vesicle. This has the effect of increasing likelihood that the affected vesicle will be released during any subsequent action potential the nerve cell experiences. The nerve cells in question generally fire at some regular baseline rate; the effect of adding ephedrine is to increase the number of vesicles released during each action potential and possibly to extend the time during which noradrenaline has an opportunity to have an effect on the post-synaptic neuron by virtue of the fact that the reuptake complex has to process both noradrenaline AND ephedrine, presumably a longer process.


Ephedrine's mechanism of action on neurotransmission in the brain is wide. Its action as an agonist at most major noradrenaline receptors and its ability to increase the release of both dopamine and to a lesser extent, serotonin by the same mechanism as explained above for norepinephrine, is presumed to have a major role in its mechanism of action. For other uses, see Dopamine (disambiguation). ... Serotonin (pronounced ) (5-hydroxytryptamine, or 5-HT) is a monoamine neurotransmitter synthesized in serotonergic neurons in the central nervous system (CNS) and enterochromaffin cells in the gastrointestinal tract of animals including humans. ...


Because of ephedrine's ability to potentiate dopamine neurotransmission it is thought to have addictive properties by some researchers. The ability to potentiate serotonin and noradrenergic activity is clinically relevant, but is not thought to contribute to the potential for abuse. For other uses, see Dopamine (disambiguation). ...


While ephedrine's role in the serotonin system is less understood there is preliminary documentation of clinically significant agonism at excitory serotonin receptors, perhaps as a downstream response to the large release of norepinephrine in the nucleus accumbens (commonly referred to as the "pleasure center" of the brain). In mice, stereotypical behaviour was both easily induced by administration of ephedrine and it's primary alkaloids and reversed when serotonin antagonists were administered. The nucleus accumbens (NAcc), also known as the accumbens nucleus or as the nucleus accumbens septi (Latin for nucleus leaning against the septum), is a collection of neurons located where the head of the caudate and the anterior portion of the putamen meet just lateral to the septum pellucidum. ...


Clinical use

Ephedrine Sulphate (1932) Ephedrine Compound (1932) and Swan-Myers Ephedrine Inhalant No. 66 (ca. 1940)
Ephedrine Sulphate (1932) Ephedrine Compound (1932) and Swan-Myers Ephedrine Inhalant No. 66 (ca. 1940)

ephedrine In 1887 Nagajoshi Nagai (1845­1929), a Japanese researcher working in Germany, isolated ephedrine as the active ingredient of ma huang but found the substance to be highly toxic. ... ephedrine In 1887 Nagajoshi Nagai (1845­1929), a Japanese researcher working in Germany, isolated ephedrine as the active ingredient of ma huang but found the substance to be highly toxic. ...

Indications

Ephedrine was once widely used as a topical decongestant and as a bronchodilator in the treatment for asthma. It continues to be used for these indications, although its popularity is waning due to the availability of more effective agents for these indications which exhibit fewer adverse effects.[4] The role in nasal congestion has largely been replaced by more potent α-adrenergic receptor agonists (e.g. oxymetazoline). Similarly the role of ephedrine in asthma has been almost entirely replaced by β2-adrenergic receptor agonists (e.g. salbutamol). Ephedrine continues to be used intravenously in the reversal of hypotension from spinal/epidural anaesthesia.[4] It is also used in other hypotensive states, including overdose with ganglionic blocking agents, antiadrenergic agents, or other medications that lower blood pressure.[5] It can be used in narcolepsy and nocturnal enuresis. Topical decongestants are decongestants applied directly to the nasal cavity. ... A bronchodilator is a medication intended to improve bronchial airflow. ... Oxymetazoline is a topical decongestant used, in the form of Oxymetazoline hydrochloride, in products such as Nasivion, Vicks Sinex and Afrin. ... Salbutamol (INN) or albuterol (USAN) is a short-acting β2-adrenergic receptor agonist used for the relief of bronchospasm in conditions such as asthma and COPD. Salbutamol sulphate is usually given by the inhaled route for direct effect on bronchial smooth muscle. ... An intravenous drip in a hospital Intravenous therapy or IV therapy is the administration of liquid substances directly into a vein. ... In physiology and medicine, hypotension refers to an abnormally low blood pressure. ... The epidural space is a part of the human spine which is very close to the spinal cord, lying just outside the dura mater. ... A muscle relaxant is a drug which decreases the tone of a muscle. ... For other uses, see Narcolepsy (disambiguation). ... Bedwetting (or enuresis) is involuntary urination while asleep in bed. ...


In traditional Chinese medicine, ephedrine has been used in the treatment of asthma and bronchitis for centuries.[6]


An ECA stack is a component found in thermogenic weight loss pills, composed of ephedrine, caffeine and aspirin (many supplement manufacturers include salicin instead of aspirin) working to speed up the metabolism and thus cause food energy to burn faster. The ECA stack is a popular supplement taken by body builders before workouts due to the increased amount of energy and alertness. The ECA stack is a popular drug combination for use as an energy booster and in weight loss. ... Salicylic acid is a colorless, crystalline organic carboxylic acid. ... Food energy is the amount of energy in food that is available through digestion. ... Professional Bodybuilder Gustavo Badell posing Bodybuilding is the process of maximizing muscle hypertrophy through the combination of weight training, sufficient caloric intake, and rest. ...


For many years, the US Coast Guard recommended ephedrine together with an equal 25 mg dose of promethazine to its sailors to combat seasickness. Promethazine manages nausea and ephedrine fights the ensuing drowsiness. Commonly referred to as the Coast Guard cocktail, ephedrine may still be available for prescription for this purpose. Promethazine is a first-generation H1 receptor antagonist antihistamine and antiemetic medication. ... Seasickness is hazardous for scuba divers Seasickness is the feeling of nausea and, in extreme cases, vertigo experienced after spending time on a craft on water. ...


Adverse effects

Adverse drug reactions (ADRs) are more common with systemic administration (e.g. injection or oral administration) compared to topical administration (e.g. nasal instillations). ADRs associated with ephedrine therapy include:[4] An adverse drug reaction (abbreviated ADR) is a term to describe the unwanted, negative consequences sometimes associated with the use of medications. ...

The approved maximum daily dosage of ephedrine for use as a bronchodilator is 150mg, as specified on the packaging of the bronchodilator and expectorant combination, Bronkaid, made by Bayer pharmaceuticals. This article or section does not cite any references or sources. ... A cardiac arrhythmia, also called cardiac dysrhythmia, is a disturbance in the regular rhythm of the heartbeat. ... The blood vessels are part of the circulatory system and function to transport blood throughout the body. ... For other forms of hypertension, see Hypertension (disambiguation). ... Dermatology (from Greek δερμα, skin) is a branch of medicine dealing with the skin and its appendages (hair, ass, sweat glands etc). ... Upper and Lower gastrointestinal tract The gastrointestinal tract (GI tract), also called the digestive tract, or the alimentary canal, is the system of organs within multicellular animals that takes in food, digests it to extract energy and nutrients, and expels the remaining waste. ... In anatomy, the genitourinary system is the organ system of all the reproductive organs and the urinary system. ... The nervous system of an animal coordinates the activity of the muscles, monitors the organs, constructs and also stops input from the senses, and initiates actions. ... Look up Confusion in Wiktionary, the free dictionary Confusion can have the following meanings: Unclarity or puzzlement, e. ... This article is about the sleeping disorder. ... This article is an expansion of a section entitled Mania from within the main article Bipolar disorder. ... A hallucination is a false sensory perception in the absence of an external stimulus, as distinct from an illusion, which is a misperception of an external stimulus. ... A delusion is commonly defined as a false belief, and is used in everyday language to describe a belief that is either false, fanciful or derived from deception. ... Formication is a tactile hallucination that insects or snakes are crawling over or under the skin. ... For other senses of this word, see paranoia (disambiguation). ... Anger is a term for the emotional aspect of aggression, as a basic aspect of the stress response in animals whereby a perceived aggravating stimulus provokes a counterresponse which is likewise aggravating and threatening of violence. ... Panic is the primal urge to run and hide in the face of imminent danger. ... Agitation may have the following special meanings Agitation, an emotional state Agitation, putting into motion (by shaking or stirring) Agitation, a term from the lexicon of Communists: political activities aimed at urging people to do something This is a disambiguation page — a navigational aid which lists other pages that... The Respiratory System Among four-legged animals, the respiratory system generally includes tubes, such as the bronchi, used to carry air to the lungs, where gas exchange takes place. ... Dyspnea (R06. ... Hyperglycemia or High Blood Sugar is a condition in which an excessive amount of glucose circulates in the blood plasma. ...


Overdose can lead to death, although the approved dose is not likely to cause severe reactions when used as directed.


Ephedrine can also lead to damage of the brain receptors over a period of high usage; this is because of its constant action on the neurochemicals. It also leads to high increase in blood pressure which over time can lead to damage in the blood vessels.


Contraindications

Ephedrine should not be used in conjunction with certain antidepressants, namely SNRIs (Selective norepinephrine re-uptake inhibitors), as this increases the risk of the above symptoms due to excessive serum levels of norepinephrine. Serotonin norepinephrine reuptake inhibitors (SNRIs) are a class of antidepressant used in the treatment of clinical depression and other affective disorders. ...


Wellbutrin is an example of an antidepressant with an amphetamine-like structure similar to ephedrine. It has a similar action but also releases serotonin from presynaptic clefts. It should not be used with ephedrine as it may increase the likelihood of the above side effects. Bupropion (amfebutamone) is an antidepressant of the aminoketone class, chemically unrelated to tricyclics or SSRIs. ...


Ephedrine should be used with caution in patients with inadequate fluid replacement, impaired adrenal function, hypoxia, hypercapnia, acidosis, hypertension, hyperthyroidism, prostatic hypertrophy, diabetes mellitus, cardiovascular disease, during delivery if maternal BP > 130/80 mmHg, and lactation.[7] Hypoxia is a pathological condition in which the body as a whole (generalised hypoxia) or region of the body (tissue hypoxia) is deprived of adequate oxygen supply. ... // Hypercapnia (from the Greek hyper = above and kapnos = smoke), also known as CO2 Poisoning, is a condition where there is too much carbon dioxide (CO2) in the blood. ... Acidosis is an increased acidity (i. ... For other forms of hypertension, see Hypertension (disambiguation). ... Hyperthyroidism (or overactive thyroid gland) is the clinical syndrome caused by an excess of circulating free thyroxine (T4) or free triiodothyronine (T3), or both. ... BPH redirects here, It can also refer to the Break Permitted Here character in the C1 control code set. ... For the disease characterized by excretion of large amounts of very dilute urine, see diabetes insipidus. ... The circulatory system or cardiovascular system is the organ system which circulates blood around the body of most animals. ...


Contraindications for the use of ephedrine include: closed angle glaucoma, phaeochromocytoma, asymmetric septal hypertrophy (idiopathic hypertrophic subaortic stenosis), concomitant or recent (previous 14 days) monoamine oxidase inhibitor (MAOI) therapy, general anaesthesia with halogenated hydrocarbons (particularly cyclopropane or halothane), tachyarrhythmias or ventricular fibrillation, hypersensitivity to ephedrine or other stimulants. Ephedrine should NOT be used at any time during pregnancy unless specifically indicated by a qualified physician and ONLY when other options are unavailable.[7] Human eye cross-sectional view. ... A pheochromocytoma (also phaeochromocytoma, English spelling) is a tumor in the medulla of the adrenal glands (or, rarely, the ganglia of the sympathetic nervous system) which secretes excessive amounts of catecholamines, usually epinephrine and norepinephrine. ... This article does not cite any references or sources. ... Anesthesia (AE), also anaesthesia (BE), is the process of blocking the perception of pain and other sensations. ...


Recreational and illicit use

Ephedrine tablets
Ephedrine tablets

Anecdotal reports have suggested that ephedrine helps studying, thinking, or concentrating to a greater extent than caffeine. Some students and some white-collar workers have used ephedrine (or Ephedra-containing herbal supplements) for this purpose, as well as some professional athletes and weightlifters. It is common for many athletes to use stimulants while exercising. Such use of ephedrine has been associated with stimulant dependence, as well as deaths from heatstroke in athletes and circulatory problems such as aortic aneurysm in weightlifters, though these side effects are rare.[verification needed] Image File history File links Download high-resolution version (1060x784, 126 KB) (Turkeyphant, Template:Ephedrine) I, the creator of this work, hereby grant the permission to copy, distribute and/or modify this document under the terms of the GNU Free Documentation License, Version 1. ... Image File history File links Download high-resolution version (1060x784, 126 KB) (Turkeyphant, Template:Ephedrine) I, the creator of this work, hereby grant the permission to copy, distribute and/or modify this document under the terms of the GNU Free Documentation License, Version 1. ... To meet Wikipedias quality standards, this article or section may require cleanup. ... Drug addiction, or dependency is the compulsive use of drugs, to the point where the user has no effective choice but to continue use. ... This article does not cite any references or sources. ... An aortic aneurysm is a general term for any swelling (dilatation or aneurysm) of the aorta, usually representing an underlying weakness in the wall of the aorta at that location. ...


As a phenylethylamine, ephedrine has a similar chemical structure to amphetamines. Ephedrine can be used in the synthesis of methamphetamine by chemical reduction; this has made ephedrine a highly sought-after chemical precursor in the illicit manufacture of methamphetamine. The most popular method for reducing ephedrine to methamphetamine is similar to the Birch reduction, in that it uses anhydrous ammonia and lithium metal in the reaction. The second most popular method uses red phosphorus, iodine, and ephedrine in the reaction. Phenethylamine is an alkaloid and monoamine. ... Amphetamine or Amfetamine(Alpha-Methyl-PHenEThylAMINE), also known as beta-phenyl-isopropylamine and benzedrine, is a prescription stimulant commonly used to treat Attention-deficit hyperactivity disorder (ADHD) in adults and children. ... Clandestine chemistry generally refers to chemistry carried out in illegal drug laboratories, but can include any kind of laboratory operation carried on in secret. ... This article is about the psychostimulant, d-methamphetamine. ... The Birch reduction is the organic reduction of aromatic rings by sodium in liquid ammonia invented by Arthur Birch. ... Ammonia is a chemical compound with the formula NH3. ... This article is about the chemical element named Lithium. ... For other uses, see Chemical reaction (disambiguation). ... General Name, symbol, number phosphorus, P, 15 Chemical series nonmetals Group, period, block 15, 3, p Appearance waxy white/ red/ black/ colorless Standard atomic weight 30. ... For the record label, see Iodine Recordings. ...


Through oxidation, ephedrine can be easily synthesized into methcathinone. Ephedrine is listed as a Table I precursor under the United Nations Convention Against Illicit Traffic in Narcotic Drugs and Psychotropic Substances.[8] The most fundamental reactions in chemistry are the redox processes. ... This article or section is not written in the formal tone expected of an encyclopedia article. ... United Nations Convention Against Illicit Traffic in Narcotic Drugs and Psychotropic Substances Opened for signature December 20, 1988[1] at Vienna Entered into force November 11, 1990[2] Conditions for entry into force 20 ratifications Parties 170[3] The 1988 United Nations Convention Against Illicit Traffic in Narcotic Drugs and...


Ephedrine has been reported to cause both physical and psychological dependence after excessive long-term use.[citation needed] This is particularly true with oral forms of ephedrine, since parenteral administration is unlikely to occur over long periods. With many majore diet review websites such as *[Celebritydietsonline.com] talking about ephedrine and the fact that it has become accesable via the internet ephedrine has become an acceptable form of weight loss according to many.[7]


Neurotoxicity of Ephedrine

As a sympathomimetic agent similar in structure and activity to amphetamines, there has been a dispute over whether ephedrine produces any neurodegenerative effects. It has not been shown clinically that certain amphetamines (namely (d)-amphetamine and (d)-methamphetamine) can cause varying levels of long-term dopamine depletion in dopamine-rich brain and nervous centers such as the putamen and the basal ganglia.


Several studies have recently compared the quantities of such neurotransmitters as serotonin, dopamine, glutamate, and epinephrine after concurrent administration of ephedrine and various amphetamine-like agents. The results showed that ephedrine has no neurotoxic effect nor has amphetamine counterparts.


Ephedrine increases serum dopamine levels minimally in comparison with an equivalent dose of dextroamphetamine (Dexedrine®). Dextromethamphetamine (Desoxyn®) raises dopamine levels dramatically (more than two times that of an equivalent dose of dextroamphetamine). This supports the general consensus that ephedrine has more of a peripheral action on the sympathetic nervous system, whereas amphetamines appear to cross the blood brain barrier more freely and tend to have a stronger central action. The fact that dopamine is believed to play a major role in the addiction response has been used in recent years as justification for controlling the distribution of dextroamphetamine and dextromethamphetamine, along with various other amphetamines.[9]


Legality in USA

Ephedrine itself has never been illegal in the United States. In 1997, the FDA proposed a regulation on ephedra (the herb from which ephedrine is obtained), which limited an ephedra dose to 8 mg (of active ephedrine) with no more than 24 mg per day.[1] This proposed rule was withdrawn in part in 2000 because of "concerns regarding the agency's basis for proposing a certain dietary ingredient level and a duration of use limit for these products."[2] In 2004, the FDA created a ban on ephedrine alkaloids that are marketed for reasons other than asthma, colds, allergies, other disease, or traditional Asian use.[3] On April 14, 2005, the U.S. District Court for the District of Utah ruled that the FDA did not have proper evidence that low dosages of ephedrine alkaloids are actually unsafe,[4] but on August 17, 2006, the U.S. Court of Appeals for the Tenth Circuit in Denver upheld the FDA's final rule declaring all dietary supplements containing ephedrine alkaloids adulterated, and therefore illegal for marketing in the United States.[5] Ephedrine is, however, still legal in many applications outside of dietary supplements. However, purchasing is currently limited and monitored, with specifics varying from state to state. “FDA” redirects here. ... April 14 is the 104th day of the year (105th in leap years) in the Gregorian calendar, with 261 days remaining. ... Year 2005 (MMV) was a common year starting on Saturday (link displays full calendar) of the Gregorian calendar. ... The United States District Court for the District of Utah is the Federal district court whose jurisdiction is the state of Utah. ... is the 229th day of the year (230th in leap years) in the Gregorian calendar. ... Year 2006 (MMVI) was a common year starting on Sunday of the Gregorian calendar. ... The United States Court of Appeals for the Tenth Circuit is a federal court with appellate jurisdiction over the following United States district courts: District of Colorado District of Kansas District of New Mexico Eastern, Northern, and Western Districts of Oklahoma District of Utah District of Wyoming These districts were...


The House passed the Combat Methamphetamine Epidemic Act of 2005 as an amendment to the renewal of the USA PATRIOT Act. Signed into law by president George W. Bush on March 6, 2006, the act amended the US Code (21 USC 830) concerning the sale of ephedrine-containing products. The federal statute included the following requirements for merchants who sell these products: Type Bicameral Speaker of the House of Representatives House Majority Leader Nancy Pelosi, (D) since January 4, 2007 Steny Hoyer, (D) since January 4, 2007 House Minority Leader John Boehner, (R) since January 4, 2007 Members 435 plus 4 Delegates and 1 Resident Commissioner Political groups Democratic Party Republican Party... The Combat Methamphetamine Epidemic Act of 2005 (CMEA) was signed into United States law on March 9, 2006 to regulate, among other things, retail over-the-counter sales of ephedrine, pseudoephedrine, and phenylpropanolamine products. ... The Uniting and Strengthening America by Providing Appropriate Tools Required to Intercept and Obstruct Terrorism Act of 2001 (Public Law 107-56), known as the USA PATRIOT Act or simply the Patriot Act, is an Act of Congress which U.S. President George W. Bush signed into law on October... George Walker Bush (born July 6, 1946) is the 43rd and current President of the United States, inaugurated on January 20, 2001. ... The United States Code (U.S.C.) is the general and permanent federal Law of the United States. ...

  • A retrievable record of all purchases identifying the name and address of each party to be kept for two years.
  • Required verification of proof of identity of all purchasers
  • Required protection and disclosure methods in the collection of personal information
  • Reports to the Attorney General of any suspicious payments or disappearances of the regulated products
  • Non-liquid dose form of regulated product may only be sold in unit dose blister packs
  • Regulated products are to be sold behind the counter or in a locked cabinet in such a way as to restrict access
  • Daily sales of regulated products not to exceed 3.6 grams without regard to the number of transactions
  • Monthly sales not to exceed 9 grams of pseudoephedrine base in regulated products

The law gives similar regulations to mail-order purchases, except the monthly sales limit is only 7.5 grams. In most common law jurisdictions, the Attorney General is the main legal adviser to the government, and in some jurisdictions may in addition have executive responsibility for law enforcement or responsibility for public prosecutions. ...


References

  1. ^ Long, Professor. http://www.chinadialogue.net/article/show/single/en/692-Chinese-medicine-s-great-waste-of-resources
  2. ^ (1989) in Edited by Reynolds JEF: Martindale: The complete drug reference, 29th edition, London: Pharmaceutical Press. ISBN 0-85369-210-6. 
  3. ^ Budavari S, editor. The Merck Index: An encyclopedia of chemicals, drugs, and biologicals, 12th edition. Whitehouse Station: Merck
  4. ^ a b c Joint Formulary Committee. British National Formulary, 47th edition. London: British Medical Association and Royal Pharmaceutical Society of Great Britain; 2004. ISBN 0853695873
  5. ^ Bicopoulos D, editor. AusDI: Drug information for the healthcare professional, 2nd edition. Castle Hill: Pharmaceutical Care Information Services; 2002.
  6. ^ Ford MD, Delaney KA, Ling LJ, Erickson T, editors. Clinical Toxicology. Philadelphia: WB Saunders; 2001. ISBN 0-7216-5485-1 Research Laboratories; 1996. ISBN 0-911910-12-3
  7. ^ a b c Mayne Pharma. Ephedrine sulfate injection DBL (Approved Product Information). Melbourne: Mayne Pharma; 2004
  8. ^ http://www.incb.org/pdf/e/list/red.pdf
  9. ^ Txsci.oxfordjournals

Otherwise known as the doctors prescribing Bible the British National Formulary (BNF) contains a wide spectrum of information on prescribing and pharmacology, among others indications, side effects and costs of the prescription of all medication drugs available on the National Health Service. ...

See also

Phenethylamine, or β-Phenylethylamine, is an alkaloid and monoamine. ... Pseudoephedrine (commonly abbreviated as PSE) is a sympathomimetic amine commonly used as a decongestant. ... Synephrine Synephrine is a dietary supplement aimed at encouraging fat loss. ... This article is about the psychostimulant, d-methamphetamine. ... This article or section is not written in the formal tone expected of an encyclopedia article. ... The ECA stack is a popular drug combination for use as an energy booster and in weight loss. ... This article is about the Vedic plant and ritual. ...

External links


  Results from FactBites:
 
Ephedrine (2191 words)
Ephedrine is a sympathomimetic that acts directly and indirectly on the sympathetic nerves.
The second case appears to be one of significant long-term abuse; the high consumption of ephedrine over 23 years was a likely cause of the case's predisposition to stroke and the eventual fatality.
While it was possible that her stroke was precipitated by the vasoconstricting and hypertensive effect of ephedrine, it is difficult to determine with any confidence.
:: ForsLean - Sabinsa Corporation :: (791 words)
40% of the thermogenic activity of ephedrine is reported to be due to the activation of the b3 adrenoreceptors in the adipose tissues2.
Ephedrine is referred to as a mixed-acting drug because it activates adrenergic receptors by direct and indirect mechanisms.
Ephedrine use is therefore contraindicated in people prone to hypertension, heart disease, hyperglycemia, hyper- thyroidism, prostate disease and related conditions and in those taking prescription medications3,6.
  More results at FactBites »

 
 

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