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| Formula | C12H30N2 |
| Molar mass | 202.386 g·mol−1 |
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Hexamethonium is a non-depolarisingganglionic blocker, a neuronal nicotinic (nAChR)receptor antagonist[1] that acts inautonomic ganglia by binding mostly in or on thenAChR receptor, and not theacetylcholine binding site itself. It does not have any effect on the muscarinic acetylcholine receptors (mAChR) located on target organs of theparasympathetic nervous system, nor on the nicotinic receptors at the skeletal neuromuscular junction, but acts as antagonist at the nicotinic acetylcholine receptors located in sympathetic and parasympathetic ganglia (nAChR).[2]
By blocking the neuronal nicotinic receptors in autonomic ganglia, which are necessary for transmission in all autonomic ganglia, both the sympathetic and parasympathetic nervous systems are inhibited. Its action on the neuronal nicotinic receptors is primarily through the block of the ion pore, rather than through competition with the binding site for acetylcholine.[3]
Postganglionic sympathetic systems are usually regulated bynorepinephrine (noradrenaline) (adrenergic receptors), whereas parasympathetic systems are acetylcholine-based, and instead rely on muscarinic receptors (some post-ganglionic sympathetic neurons, such as those stimulating sweat glands, release acetylcholine).[citation needed]
The organ system and adverse effects ofganglion blockers are due to the parasympathetic and sympathetic stimuli blockage at preganglionic sites. Side-effects include combinedsympatholytic (e.g.,orthostatic hypotension andsexual dysfunction) andparasympatholytic (e.g., constipation,urinary retention,glaucoma, blurry vision, decreased lacrimal gland secretion, dry mouth (xerostomia) effects.[citation needed]
It was formerly used to treat disorders, such as chronichypertension, of theperipheral nervous system, which is innervated only by thesympathetic nervous system. The non-specificity of this treatment led to discontinuing its use.[4]
The use of inhaled hexamethonium, an unapproved drug, in a normal volunteer during a medical study is believed to have caused or contributed to her death[5][6] in light of the presence of abnormal "ground glass opacities" on her chest X-ray.[needs context]
