Ephedra Online

[Nolan Guyz]

TheANS Panel provides a scientific opinion evaluating the safety in use of Ephedra herb and its preparations originating from Ephedra species when used in food, e.g. in food supplements. Ephedra species contain alkaloids of biological relevance: ephedrine, pseudoephedrine, norephedrine, norpseudoephedrine (cathine), methylephedrine and methylpseudoephedrine. They have sympathomimetic activity and some of them are also used as active ingredients in medicinal products for which adverse effects are described. The use of Ephedra herb in food supplements is prohibited in several European countries, however food supplements containing Ephedra herb, also in combination with caffeine, are offered for sale via the internet. The Panel reviewed the available scientific data on a possible association between the intake of Ephedra herb, its preparations or its alkaloids and potential harmful effects on health. There is wide variation in the concentration of the individual ephedra alkaloids in different Ephedra species and in their preparations for use in food. No adequately specified individual preparations of Ephedra herb are known for which sufficient toxicological data for hazard characterisation exist. Due to the absence of adequate data on genotoxicity, short-term, long-term and reproductive and developmental toxicity the Panel could not provide advice on a daily intake of Ephedra herb and its preparations that do not give rise to concerns about harmful effects to health. Ephedra herb and its preparations in food supplements may result in exposure to total ephedra alkaloids or ephedrine which falls within or may exceed the therapeutic dose ranges for the individual ephedra alkaloids or ephedrine, respectively, in medicinal products. Such an exposure could lead to severe adverse effects, which may be enhanced by the combination with caffeine. The Panel concluded that Ephedra herb and its preparations containing ephedra alkaloids used as food supplements were of significant safety concern at the estimated use levels.

Ephedra is an alpha and beta-adrenergic agonist used for the management of respiratory conditions related to bronchial asthma, such as wheezing, shortness of breath, and tightness of chest.

Ephedra is an alkaloid chemical compound traditionally obtained from the plant Ephedra sinica. The sale of ephedra-containing supplements intended to increase muscle weight or promote weight loss was banned in the United States in 2004 due to the risk for adverse effects and a lack of evidence for clinical effectiveness. The drug is still sold in Canada in OTC formulations for respiratory conditions associated with bronchial asthma.

Ephedra is indicated for the temporary relief of shortness of breath, tightness of chest, and wheezing due to bronchial asthma. For the temporary relief of bronchial asthma in over-the-counter formulations.

The alkaloids ephedrine and pseudoephedrine are the active constituents of Ephedra. Pseudoephedrine is used in over-the-counter decongestants. Derivatives of ephedrine are used to treat low blood pressure, but alternatives with reduced cardiovascular risk have replaced it for treating asthma. Ephedrine is also considered a performance-enhancing drug and is prohibited in most competitive sports. 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. 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. Ephedrine's 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 is presumed to have a major role in its mechanism of action.

Ephedrine is a medication used to manage and treat clinically significant hypotension. It is in the sympathomimetic class of drugs. The FDA-approved primary indication for ephedrine is the treatment of clinically significant hypotension perioperatively. Induction of general anesthesia and ongoing anesthesia during operative cases results in vasodilatation and hypotension, requiring treatment with vasopressors. This activity illustrates ephedrine's indications, action, and contraindications in treating clinically significant hypotension. This activity highlights the mechanism of action, administration, contraindications, adverse event profile, and other key factors pertinent to interprofessional healthcare team members involved in caring for patients with clinically significant hypotension and related conditions.

Objectives:Identify the indications for treatment with ephedrine.Recognize common complications of managing clinically significant hypotension intraoperatively with ephedrine.Identify alternative options to treat significant intraoperative hypotension.Apply effective interprofessional team communication to improve outcomes for the patient requiring ephedrine.Access free multiple choice questions on this topic.

The FDA-approved primary indication for ephedrine is the treatment of clinically significant hypotension perioperatively. Induction of general and ongoing anesthesia during operative cases results in vasodilatation and hypotension, requiring treatment with vasopressors.[1]

It is also frequently the agent of choice for hypotension induced by spinal or epidural anesthesia. In obstetrics, sympathectomy during spinal anesthetics results in hypotension in 80% of patients.[2] Although phenylephrine selection is due to fewer effects on umbilical arterial acidity, ephedrine is a frequent choice due to less alpha-adrenergic action on the uterine vasculature, which preserves uterine blood flow.[3]

It is sometimes given intramuscularly to achieve a longer-lasting effect.[4] According to the American Society of Anesthesiologists Committee Task Force on obstetric anesthesia, ephedrine or phenylephrine can be utilized to treat hypotension during neuraxial anesthesia. However, in the absence of maternal bradycardia, phenylephrine is preferred.[5]

Since ephedrine results in both alpha and beta-adrenoreceptor stimulation, it is most beneficial in the setting of hypotension along with bradycardia or a low-normal heart rate, and caution is necessary for patients with hypotension and coexisting tachycardia. Most vasopressors used during anesthesia should be viewed as a temporizing measure while determining and addressing the source of hypotension.

Another notable indication of ephedrine is for allergy relief. Due to the constriction of smooth muscle via alpha receptor binding and bronchi dilation due to beta-2 receptor agonism, most sympathomimetics, including ephedrine, work effectively to decrease allergic symptoms.[6]

Oral formulations of ephedrine have been used historically to treat asthma via pulmonary vasoconstriction and reduction in airway edema along with beta-induced bronchodilation, but it is rarely used for this purpose in modern medicine due to unwanted cardiac effects and availability of more selective beta-agonists such as albuterol. Ephedrine is also available in a fixed-dose combination with guaifenesin to temporarily relieve mild asthma symptoms with an expectorant.[7]

Other off-label indications include bronchoconstriction, myasthenia gravis, and weight loss(in the past). In the early 2000s, the drug became very popular among over-the-counter supplements because it was found to work synergistically with caffeine to promote weight loss by stimulating metabolism.[8] However, ephedrine lost favor as a supplement after research established links to ventricular arrhythmias, nausea, and psychiatric issues with use.[9]

Patients with myasthenia gravis may also benefit from treatment with ephedrine; however, evidence for its specific mechanism of action and benefit in this disease has not come from randomized controlled trials, and only observational and non-randomized trials are currently available.[10] Lastly, case reports demonstrate using ephedrine to alleviate bronchoconstriction during induction for patients on beta-blocker maintenance therapy.[11]

Ephedrine, a stereoisomer to better-known pseudoephedrine, is a sympathomimetic amine with unique effects due to its indirect mechanism than other sympathomimetic agents like pseudoephedrine and phenylephrine.[12] Ephedrine acts as both a direct and indirect sympathomimetic. It binds directly to both alpha and beta receptors; however, its primary mode of action is indirectly achieved by inhibiting neuronal norepinephrine reuptake and displacing more norepinephrine from storage vesicles.[13] This action allows norepinephrine to remain in the synapse longer to bind postsynaptic alpha and beta receptors.[14]

Stimulation of alpha-1-adrenergic smooth muscle receptors within vasculature results in a rise in systemic vascular resistance and, consequently, systolic and diastolic blood pressure. Direct stimulation of beta-1 receptors by ephedrine and norepinephrine increases cardiac chronotropy and inotropy. Finally, beta-2-adrenergic receptor stimulation in the lungs results in bronchodilation with ephedrine administration, though it is not as pronounced as its cardiovascular effects.[15]

Elimination: Limited clinical data after intravenous administration of ephedrine endorses similar observations of urinary excretion. The plasma elimination half-life of ephedrine after oral administration is approximately 6 hours. The urinary excretion of ephedrine is increased in acidic urine.[17] nephrolithiasis induced by an excessive dose of ephedrine has been treated with urinary alkalinization.[18][17]

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