ephedrine
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ephedrine
EphedrineSystematic (IUPAC) name(1R,2S)-2-(methylamino)-1-phenylpropan-1-olIdentifiersCAS number299-42-3ATC codeR01AA03 R03CA02 S01FB02PubChem5032DrugBankDB01364ChemSpider8935Chemical dataFormulaC10H15NO Mol. mass165.23Pharmacokinetic dataBioavailability85%Metabolismminimal hepaticHalf life3–6 hoursExcretion22-99% renalTherapeutic considerationsPregnancy cat.A(AU) A(US)Legal statusPrescription Only (S4)(AU) Schedule VI(CA) P(UK) OTC(US)Routesoral, IV, IM, SCEphedrine (EPH) is a sympathomimetic amine commonly used as a stimulant, appetite suppressant, concentration aid, decongestant, and to treat hypotension associated with anaesthesia. Ephedrine is similar in structure to the synthetic derivatives amphetamine and methamphetamine. 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 traditional Chinese medicines, the herb má huáng (麻黄, 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 distachya (syn. Ephedra vulgaris) in 1885. The substance called soma mentioned in old Hindu books such as the Rig Veda, may have been ephedra extract. This, however, is disputed, as the identity of soma.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.// ChemistryEphedrine 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.The isomer which is marketed is (-)-(1R,2S)-ephedrine.As with other phenylethylamines, it is also somewhat chemically similar to methamphetamine, although the amphetamines are more potent and have additional biological effects.Ephedrine may also be referred to as: (αR)-α-benzenemethanol, α-benzyl alcohol, or L-erythro-2-(methylamino)-1-phenylpropan-1-ol. Ephedrine hydrochloride has a melting point of 187-188°C. Mode of actionEphedrine is a sympathomimetic amine, the principal mechanism of its 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 because 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).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 increases 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.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.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 its primary alkaloids and reversed when serotonin antagonists were administered. Clinical use IndicationsEphedrine 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. 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. It is also used in other hypotensive states, including overdose with ganglionic blocking agents, antiadrenergic agents, or other medications that lower blood pressure. It can be used in narcolepsy and nocturnal enuresis. It also remains the only drug available to treat the symptoms of certain types of Congenital Myasthenia.In traditional Chinese medicine, ephedrine has been used in the treatment of asthma and bronchitis for centuries.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.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. Adverse effectsAdverse 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:Cardiovascular: tachycardia, cardiac arrhythmias, Angina pectoris, vasoconstriction with hypertensionDermatological: flushing, sweating, acne vulgarisGastrointestinal: nausea, appetite lossGenitourinary: increased urine output due to increased blood flow (difficulty urinating is not uncommon, as alpha-agonists such as ephedrine constrict the internal urethral sphincter, mimicking the effects of sympathetic nervous system stimulation)Nervous system: restlessness, confusion, insomnia, mild euphoria, mania/hallucinations (rare except in previously existing psychiatric conditions), delusions, formication (may be possible, but lacks documented evidence) paranoia, hostility, panic, agitationRespiratory: dyspnea, pulmonary edemaMiscellaneous: dizziness, headache, tremor, hyperglycemic reactionsThe approved maximum daily dosage of ephedrine for use as a bronchodilator is 150 mg, as specified on the packaging of the bronchodilator and expectorant combination, Bronkaid, made by Bayer pharmaceuticals.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. ContraindicationsEphedrine should not be used in conjunction with certain antidepressants, namely SNRIs (serotonin-norepinephrine re-uptake inhibitors), as this increases the risk of the above symptoms due to excessive serum levels of norepinephrine.Bupropion is an example of an antidepressant with an amphetamine-like structure similar to ephedrine, and it is known as an NDRI (norepinephrine-dopamine re-uptake inhibitor). It has an action which bears more resemblance to amphetamine than to fluoxetine in that its primary mode of therapeutic action involves norepinephrine and to a lesser degree dopamine, but it also releases some serotonin from presynaptic clefts. It should not be used with ephedrine as it may increase the likelihood of the above side effects.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.Contra
Ephedrine or any alpha/beta agonist are dangerous compounds that should not be abused. In a recent issue of IronMan magazine a columnist wrote about a âthermogenicâ dietary supplement that is said to provide more calorie burning than the famous E/C/A (âEphedrine / Caffeine / Aspirinâ) stack.1. Liest sich sehr easy und ist vollgestopft mit tollen Infos.Licensed ephedrine products are now being sold on the net.Traditional forms of weight loss are changing fast. Most other companies' products varied from 3-6% L-ephedrine. They should NOT be used if proper research is not done. Our overseas factory has always standardized our ephedra extract to 10% ephedrine group alkaloids, with a minimum of 8.comI have used an ECA stack in the past but like Dumboâs Feather (which if you remember helped him to fly) I think it had more of a placebo effect. An article about Ephedrine and Clenbuterol, two drugs found in effective diet pills. If FORZA is shrewd they will keep this up and continue to build our trust.Licenced Ephedrine Products.0]hept-3-ene-3-carboxylate(2R)-2-[(4-Ethyl-2,3-dioxopiperazinyl)carbonylamino]-2-(4-hydroxyphenyl)acetic acid(2R)-2-[(4-Ethyl-2,3-dioxopiperBurn Fat Fast And Feel Great Again.. It seems that we havenât got the time to plan what we eat and instead a turning our attention to diet pills. They have side
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ephedrine
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Ephedrine (EPH) is a sympathomimetic amine commonly used as a stimulant, appetite suppressant, concentration aid, decongestant, and to treat hypotension associated with anaesthesia ...
Ephedrine - Wikipedia, the free encyclopedia
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