A ganglionic blocker (or ganglioplegic) is a type of medication that inhibits transmission between

preganglionic In the autonomic nervous system, nerve fibers from the central nervous system to the autonomic ganglion, ganglion are known as preganglionic nerve fibers. All preganglionic fibers, whether they are in the sympathetic nervous system, sympathetic d ...

and

postganglionic In the autonomic nervous system, nerve fibers from the ganglion to the wikt:effector, effector organ are called postganglionic nerve fibers. Neurotransmitters The neurotransmitters of postganglionic fibers differ: * In the parasympathetic div ...

neurons in the

autonomic nervous system The autonomic nervous system (ANS), sometimes called the visceral nervous system and formerly the vegetative nervous system, is a division of the nervous system that operates viscera, internal organs, smooth muscle and glands. The autonomic nervo ...

, often by acting as a nicotinic receptor antagonist. Nicotinic acetylcholine receptors are found on skeletal muscle, but also within the route of transmission for the parasympathetic and sympathetic nervous system (which together comprise the autonomic nervous system). More specifically, nicotinic receptors are found within the ganglia of the autonomic nervous system, allowing outgoing signals to be transmitted from the presynaptic to the postsynaptic cells. Thus, for example, blocking nicotinic acetylcholine receptors blocks both sympathetic (excitatory) and parasympathetic (calming) stimulation of the heart. The nicotinic antagonist hexamethonium, for example, does this by blocking the transmission of outgoing signals across the autonomic ganglia at the postsynaptic nicotinic acetylcholine receptor. Because ganglionic blockers block both the

parasympathetic nervous system The parasympathetic nervous system (PSNS) is one of the three divisions of the autonomic nervous system, the others being the sympathetic nervous system and the enteric nervous system. The autonomic nervous system is responsible for regulat ...

and

sympathetic nervous system The sympathetic nervous system (SNS or SANS, sympathetic autonomic nervous system, to differentiate it from the somatic nervous system) is one of the three divisions of the autonomic nervous system, the others being the parasympathetic nervous sy ...

, the effect of these drugs depends upon the dominant tone in the organ system. The opposite of a ganglionic blocker is referred to as a ganglionic stimulant. Some substances can exhibit both stimulating and blocking effects on autonomic ganglia, depending on dosage and/or duration of action. An example for such a "dual" action is nicotine, which does this via depolarization block (see classification below).

Examples

The first ganglion-blocker to be used clinically was

tetraethylammonium Tetraethylammonium (TEA) is a quaternary ammonium cation with the chemical formula , consisting of four ethyl groups (, denoted Et) attached to a central nitrogen atom. It is a counterion used in the research laboratory to prepare lipophilic salt ...

, although it was soon superseded by better drugs. Nicotinic receptor antagonists: *

hexamethonium Hexamethonium is a non-depolarising ganglionic blocker, a neuronal nicotinic ( nAChR) receptor antagonist that acts in autonomic ganglia by binding mostly in or on the nAChR receptor, and not the acetylcholine binding site itself. It does no ...

* pentolinium * mecamylamine * trimetaphan *

tubocurarine Tubocurarine (also known as ''d''-tubocurarine or DTC) is a toxic benzylisoquinoline alkaloid historically known for its use as an arrow poison. In the mid-1900s, it was used in conjunction with an anesthetic to provide skeletal muscle relaxat ...

* pempidine * benzohexonium * chlorisondamine * pentamine Nicotinic receptor agonists (acting through depolarization block): *

nicotine Nicotine is a natural product, naturally produced alkaloid in the nightshade family of plants (most predominantly in tobacco and ''Duboisia hopwoodii'') and is widely used recreational drug use, recreationally as a stimulant and anxiolytic. As ...

Blocking ACh release in autonomic ganglia (although these have many other actions elsewhere): *

botulinum toxin Botulinum toxin, or botulinum neurotoxin (commonly called botox), is a neurotoxic protein produced by the bacterium ''Clostridium botulinum'' and related species. It prevents the release of the neurotransmitter acetylcholine from axon en ...

Uses

Ganglionic blockers are used less frequently now than they were in the past, because antihypertensives with fewer side effects are now available.

Hexamethonium Hexamethonium is a non-depolarising ganglionic blocker, a neuronal nicotinic ( nAChR) receptor antagonist that acts in autonomic ganglia by binding mostly in or on the nAChR receptor, and not the acetylcholine binding site itself. It does no ...

has been described as the "first effective antihypertensive drug". However, they are still used in some emergency situations, such as

aortic dissection Aortic dissection (AD) occurs when an injury to the innermost layer of the aorta allows blood to flow between the layers of the aortic wall, forcing the layers apart. In most cases, this is associated with a sudden onset of agonizing ches ...

autonomic dysreflexia Autonomic dysreflexia (AD) is a life-threatening medical emergency characterized by hypertension and cardiac arrhythmias. This condition is sometimes referred to as autonomic hyperreflexia. Most cases of AD occur in individuals with spinal cord ...

Side effects

* Cardiovascular:

Orthostatic hypotension Orthostatic hypotension, also known as postural hypotension, is a medical condition wherein a person's blood pressure drops when they are standing up ( orthostasis) or sitting down. Primary orthostatic hypotension is also often referred to as ne ...

with or without reflex

tachycardia Tachycardia, also called tachyarrhythmia, is a heart rate that exceeds the normal resting rate. In general, a resting heart rate over 100 beats per minute is accepted as tachycardia in adults. Heart rates above the resting rate may be normal ...

* ENT/glands:

xerostomia Xerostomia, also known as dry mouth, is a subjective complaint of dryness in the mouth, which may be associated with a change in the composition of saliva, reduced salivary flow, or have no identifiable cause. This symptom is very common and is o ...

, dry eyes, blurred vision, reduced bronchial secretion,

hypohidrosis Hypohidrosis is a medical condition in which a person exhibits diminished sweating in response to appropriate stimuli. In contrast with hyperhidrosis, which is a socially troubling yet often benign condition, the consequences of untreated hypohidr ...

* GIT:

gastroparesis Gastroparesis (gastro- from Ancient Greek – gaster, "stomach"; and -paresis, πάρεσις – "partial paralysis") is a medical disorder of ineffective neuromuscular contractions (peristalsis) of the stomach, resulting in food and l ...

constipation Constipation is a bowel dysfunction that makes bowel movements infrequent or hard to pass. The Human feces, stool is often hard and dry. Other symptoms may include abdominal pain, bloating, and feeling as if one has not completely passed the ...

urinary retention Urinary retention is an inability to completely empty the bladder. Onset can be sudden or gradual. When of sudden onset, symptoms include an inability to urinate and lower abdominal pain. When of gradual onset, symptoms may include urinary incont ...

* Sexual dysfunction: failure of

erection An erection (clinically: penile erection or penile tumescence) is a Physiology, physiological phenomenon in which the penis becomes firm, engorged, and enlarged. Penile erection is the result of a complex interaction of psychological, neural, ...

and

ejaculation Ejaculation is the discharge of semen (the ''ejaculate''; normally containing sperm) from the penis through the urethra. It is the final stage and natural objective of male sexual stimulation, and an essential component of natural conception. ...

* in overdose risk of peripheral

circulatory collapse Shock is the state of insufficient blood flow to the tissues of the body as a result of problems with the circulatory system. Initial symptoms of shock may include weakness, tachycardia, hyperventilation, sweating, anxiety, and increased thirst. ...

(shock) and paralytic

ileus Ileus is a disruption of the normal propulsive ability of the intestine. It can be caused by lack of peristalsis or by mechanical obstruction. The word 'ileus' derives . The term 'subileus' refers to a partial obstruction. Signs and symptoms S ...

References

{{Acetylcholine metabolism and transport modulators Neuropharmacology Nicotinic antagonists

Examples

Uses

Side effects

See also

References