indication

Ephedra is widely used by athletes, despite a lack of evidence that it enhances athletic performance. Ephedra has also been used for weight loss.

mechanism of action

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.

drug interactions

Amitriptyline: The tricyclic antidepressant, amitriptyline, increases the sympathomimetic effect of ephedra.

Amoxapine: The tricyclic antidepressant, amoxapine, increases the sympathomimetic effect of ephedra.

Clomipramine: The tricyclic antidepressant, clomipramine, increases the sympathomimetic effect of ephedra.

Desipramine: The tricyclic antidepressant, desipramine, increases the sympathomimetic effect of ephedra.

Doxepin: The tricyclic antidepressant, doxepin, increases the sympathomimetic effect of ephedra.

Guanethidine: Ephedra may decrease the effect of guanethidine.

Imipramine: The tricyclic antidepressant, imipramine, increases the sympathomimetic effect of ephedra.

Isocarboxazid: Increased arterial pressure

Linezolid: Possible increase of arterial pressure

Methyldopa: Increased arterial pressure

Midodrine: Increased arterial pressure

Moclobemide: Moclobemide increases the sympathomimetic effect of ephedra.

Nortriptyline: The tricyclic antidepressant, nortriptyline, increases the sympathomimetic effect of ephedra.

Phenelzine: Increased arterial pressure

Rasagiline: Increased arterial pressure

Reserpine: Increased arterial pressure

Trandolapril: Ephedra may antagonize the antihypertensive effect of Trandolapril. Monitor Trandolapril efficacy.