Sympathomimetic drug
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.
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[edit] Mechanisms of action
The mechanisms of sympathomimetic drugs can be direct-acting, such as α-adrenergic agonists, β-adrenergic agonists, and dopaminergic agonists; or indirect-acting, such as MAOIs, COMT inhibitors, release stimulants, and reuptake inhibitors.[edit] Direct-acting
[edit] Adrenergic receptor agonists
[edit] Dopaminergic agonists
Stimulation of the D1 receptor by dopaminergic agonists such as fenoldopam is used intravenously to treat hypertensive crisis.[edit] Indirect-acting
[edit] 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.[edit] 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 inhibitorCOMT inhibitors can also decrease metabolism of norepinephrine and epinephrine. (MAOI) drugs can induce such effects.[edit] Cross-reactivity
Substances like cocaine also affect dopamine, and some substances like MDMA affect serotonin.Norepinephrine is synthesized by the body into epinephrine, causing central nervous system stimulation. Thus, all sympathomimetic amines fall into the larger group of stimulants (see psychoactive drug chart). Many of these stimulants have therepeutic use and abuse potential, can induce tolerance, and possibly physical dependence.
[edit] Comparison
"Parasympatholytic" and "sympathomimetic" are similar, but not identical. For example, both cause mydriasis, but parasympatholytics reduce accommodation (cycloplegia) while sympathomimetics do not.[edit] Examples
- ephedrine (found in Ephedra)
- pseudoephedrine (also found in Ephedra species)
- amphetamine
- methamphetamine
- 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)