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The alkaloids ephedrine and pseudoephedrine are the active constituents of Ephedra species. 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.
A sympathetic nerve stimulant resembling adrenaline, its effect on the unstriped muscular fibres is remarkable. It acts promptly in relieving swellings of the mucous membrane. It has valuable antispasmodic properties, acts on the air passages and is of benefit in asthma and hay fever; it is also employed for rheumatism; a 5 to 10 per cent solution has mydriatic properties, prophylactically used for low blood pressure in influenza, pneumonia.
Between 1995 and 1997, the FDA received more than 900 reports of possible ephedra toxicity. Serious adverse events such as stroke, heart attack, and sudden death were reported in 37 cases.
Using ephedra may worsen many health conditions such as cardiovascular disease, kidney disease, and diabetes.
Ephedra may cause seizures in otherwise healthy people as well as in people with seizure disorders.
Taking ephedra can also result in anxiety, difficulty urinating, dry mouth, headache, heart damage, high blood pressure, irregular heart rhythms, irritation of the stomach, kidney stones, nausea, psychosis, restlessness, sleep problems, and tremors.