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Ephedrine is a central nervous system (CNS) stimulant and sympathomimetic agent that is often used to prevent low blood pressure during anesthesia.[13] It has also been used for asthma, narcolepsy, and obesity but is not the preferred treatment.[13] It is of unclear benefit in nasal congestion.[13] It can be taken by mouth or by injection into a muscle, vein, or just under the skin.[13] Onset with intravenous use is fast, while injection into a muscle can take 20 minutes, and by mouth can take an hour for effect.[13] When given by injection, it lasts about an hour, and when taken by mouth, it can last up to four hours.[13]
Common side effects include trouble sleeping, anxiety, headache, hallucinations, high blood pressure, fast heart rate, loss of appetite, and urinary retention.[13] Serious side effects include stroke and heart attack.[13] While probably safe in pregnancy, its use in this population is poorly studied.[14][15] Use during breastfeeding is not recommended.[15] Ephedrine works by inducing the release of norepinephrine and hence indirectly activating the α- and β-adrenergic receptors.[13] Chemically, ephedrine is a substituted amphetamine and is the (1R,2S)-enantiomer of β-hydroxy-N-methylamphetamine.[16]
Ephedrine was first isolated in 1885 and came into commercial use in 1926.[17][18] It is on the World Health Organization’s List of Essential Medicines.[19] It is available as a generic medication.[13] It can normally be found in plants of the Ephedra genus.[13][20] Over-the-counter dietary supplements containing ephedrine are illegal in the United States,[13] with the exception of those used in traditional Chinese medicine, where its presence is noted by má huáng.[13][20]
Medical uses
Ephedrine is a non-catecholamine sympathomimetic with cardiovascular effects similar to those of adrenaline (epinephrine): increased blood pressure, heart rate, and contractility. Like pseudoephedrine, it is a bronchodilator, with pseudoephedrine having considerably less effect.[21][22]
Ephedrine may decrease motion sickness, but it has mainly been used to decrease the sedating effects of other medications used for motion sickness.[23][24]
Ephedrine is also found to have quick and long-lasting responsiveness in congenital myasthenic syndrome in early childhood and also even in adults with a novel COLQ mutation.[25]
Ephedrine is administered by intravenous boluses. Redosing usually requires increased doses to offset the development of tachyphylaxis, which is attributed to the depletion of catecholamine stores. Buy Ephedrine Powder Cas 299-42-3
Weight loss
Ephedrine promotes modest short-term weight loss,[26] specifically fat loss, but its long-term effects are unknown.[27] In mice, ephedrine is known to stimulate thermogenesis in the brown adipose tissue, but because adult humans have only small amounts of brown fat, thermogenesis is assumed to take place mostly in the skeletal muscle. Ephedrine also decreases gastric emptying. Methylxanthines such as caffeine and theophylline have a synergistic effect with ephedrine for weight loss. This led to the creation and marketing of compound products.[28] One of them, known as the ECA stack, contains ephedrine with caffeine and aspirin. It is a popular supplement taken by bodybuilders seeking to cut body fat before a competition.[29] A 2021 systematic review found that ephedrine taken in doses from 60 mg to 150mg, with or without caffeine, for 4 to 24 weeks led to a 2 kilograms (4.4 lb) weight loss greater than placebo, raised heart rate, and reduced LDL and raised HDL, with no statistically significant difference in blood pressure.[30]
Available forms
Ephedrine is available as a prescription-only pharmaceutical drug in the form of an intravenous solution, under brand names including Akovaz, Corphedra, Emerphed, and Rezipres as well as in generic forms, in the United States.[31][32] It is also available over-the-counter in the form of 12.5 and 25 mg oral tablets for use as a bronchodilator and as a 0.5% concentration nasal spray for use as a decongestant.[32] The drug is additionally available in combination with guaifenesin in the form of oral tablets and liquids.[32] Ephedrine is provided as the hydrochloride or sulfate salt in pharmaceutical formulations.[31][32]
Contraindications
Ephedrine should not be used in conjunction with certain antidepressants, namely norepinephrine–dopamine reuptake inhibitors (NDRIs), as this increases the risk of symptoms due to excessive serum levels of norepinephrine.[citation needed]
Bupropion is an example of an antidepressant with an amphetamine-like structure similar to ephedrine, and it is an NDRI. Its action 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 side effects.[citation needed]
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 blood pressure is >130/80 mmHg, and during lactation.[33]
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 anesthesia with halogenated hydrocarbons (particularly halothane), tachyarrhythmias or ventricular fibrillation, or hypersensitivity to ephedrine or other stimulants.[citation needed]
Ephedrine should not be used at any time during pregnancy unless specifically indicated by a qualified physician and only when other options are unavailable.[33]
Side effects
Ephedrine is a potentially dangerous natural compound; as of 2004 the US Food and Drug Administration (FDA) had received over 18,000 reports of adverse effects in people using it.[34]
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 [35]
- Cardiovascular: tachycardia, cardiac arrhythmias, angina pectoris, vasoconstriction with hypertension
- Dermatological: flushing, sweating, acne vulgaris
- Gastrointestinal: nausea
- Genitourinary: decreased urination due to vasoconstriction of renal arteries, 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, agitation
- Respiratory: dyspnea, pulmonary edema
- Miscellaneous: dizziness, headache, tremor, hyperglycemic reactions, dry mouth
Overdose
Overdose of ephedrine may result in sympathomimetic symptoms like tachycardia and hypertension
Ephedrine Cas 299-42-3 Market Research Scope and Coverage
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