Sympathomimetic Drug

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Sympathomimetic drug

Sympathomimetic drugs are substances that mimic the effects of the sympathetic nervous system, such as catecholamines, epinephrine (adrenaline), norepinephrine (noradrenaline), dopamine, etc. Such drugs are used to treat cardiac arrest and low blood pressure, or even delay premature labor, among other things. These drugs act at the postganglionic sympathetic terminal,[1] either directly activating postsynaptic receptors, blocking breakdown and reuptake, or stimulating production and release of catecholamines.

 Mechanisms of action
The mechanisms of sympathomimetic drugs can be direct-acting, such as -adrenergic agonists, adrenergic agonists, and dopaminergic agonists; or indirect-acting, such as MAOIs, COMT inhibitors, release stimulants, and reuptake inhibitors.

y Direct-acting

Adrenergic receptor agonists


Direct stimulation of the - and -adrenergic receptors can produce sympathomimetic effects. Salbutamol is a very commonly used direct-acting 2-agonist. Other examples include phenylephrine, isoproterenol, and dobutamine.

Dopaminergic agonists
Stimulation of the D1 receptor by dopaminergic agonists such as fenoldopam is used intravenously to treat hypertensive crisis.

y Indirect-acting

Norepinephrine transporter blockade


Classical sympathomimetic drugs are amphetamines (including MDMA), ephedrine, and cocaine, which act by blocking and reversing norepinephrine transporter (NET) activity. NET is a transport protein expressed on the surface of some cells that clears noradrenaline and adrenaline from the extracellular space and into cells, terminating the signaling effects.

Inhibition of epinephrine and norepinephrine metabolism


Inhibition of norepinephrine or epinephrine metabolism can produce sympathomimetic effects. Both are metabolized mainly by the enzyme monoamine oxidase (MAO), thus the monoamine oxidase inhibitor (MAOI) drugs can induce such effects. COMT inhibitors can also decrease metabolism of norepinephrine and epinephrine.

 Examples
y y y y

ephedrine (found in Ephedra) pseudoephedrine (also found in Ephedra species) amphetamine methamphetamine

y y y y y y y y y y y y

methylphenidate (Ritalin) lisdexamfetamine (Vyvanse) cocaine (found in Erythroxylum coca, Coca) cathinone (found in Catha edulis, Khat) cathine (also found in Catha edulis) methcathinone benzylpiperazine (BZP) methylenedioxypyrovalerone (MDPV) 4-methylaminorex pemoline (Cylert) phenmetrazine (Preludin) propylhexedrine (Benzedrex)

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