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A sympatholytic (sympathoplegic) drug is a medication that opposes the downstream effects of postganglionic nerve firing in effector organs innervated by the sympathetic nervous system (SNS). [1] They are indicated for various functions; for example, they may be used as antihypertensives .
Autonomic drugs are substances that can either inhibit or enhance the functions of the parasympathetic and sympathetic nervous systems. This type of drug can be used to treat a wide range of diseases an disorders, including glaucoma , asthma , and disorders of the urinary , gastrointestinal and circulatory systems.
The mechanisms of sympathomimetic drugs can be direct-acting (direct interaction between drug and receptor), such as α-adrenergic agonists, β-adrenergic agonists, and dopaminergic agonists; or indirect-acting (interaction not between drug and receptor), such as MAOIs, COMT inhibitors, release stimulants, and reuptake inhibitors that increase the levels of endogenous catecholamines.
Alpha 2 receptors are associated with sympatholytic properties. Alpha-adrenergic agonists have the opposite function of alpha blockers. Alpha adrenoreceptor ligands mimic the action of epinephrine and norepinephrine signaling in the heart, smooth muscle and central nervous system, with norepinephrine being the highest affinity.
Propranolol is a highly lipophilic drug achieving high concentrations in the brain. The duration of action of a single oral dose is longer than the half-life and may be up to 12 hours if the single dose is high enough (e.g., 80 mg). [ 72 ]
Adrenergic blocking agents are a class of drugs that exhibit its pharmacological action through inhibiting the action of the sympathetic nervous system [1] in the body. The sympathetic nervous system(SNS) is an autonomic nervous system that we cannot control by will.
Trimetaphan camsilate or trimethaphan camsylate (), trade name Arfonad, is a sympatholytic drug used in rare circumstances to lower blood pressure.. Trimetaphan is a ganglionic blocker: it counteracts cholinergic transmission at a specific type of nicotinic acetylcholine receptors in the autonomic ganglia and therefore blocks both the sympathetic nervous system and the parasympathetic nervous ...
The related drug oxypertine shows high affinity for the serotonin 5-HT 2 and dopamine D 2 receptors (K i = 8.6 nM and 30 nM, respectively) and is also known to act as a catecholamine depleting agent. [ 8 ] [ 9 ] Oxypertine, milipertine, and solypertine all antagonize the behavioral effects of tryptamine , a serotonin receptor agonist , and ...