Pentolinium is a ganglionic blocking agent which acts as a

nicotinic acetylcholine receptor Nicotinic acetylcholine receptors, or nAChRs, are receptor polypeptides that respond to the neurotransmitter acetylcholine. Nicotinic receptors also respond to drugs such as the agonist nicotine. They are found in the central and peripheral ner ...

antagonist. Formulated as the pentolinium tartrate

salt Salt is a mineral composed primarily of sodium chloride (NaCl), a chemical compound belonging to the larger class of salts; salt in the form of a natural crystalline mineral is known as rock salt or halite. Salt is present in vast quant ...

, it is also known as Ansolysen. It can be used as an

antihypertensive Antihypertensives are a class of drugs that are used to treat hypertension (high blood pressure). Antihypertensive therapy seeks to prevent the complications of high blood pressure, such as stroke and myocardial infarction. Evidence suggests tha ...

drug during surgery or to control hypertensive crises. It works by binding to the acetylcholine

receptor Receptor may refer to: * Sensory receptor, in physiology, any structure which, on receiving environmental stimuli, produces an informative nerve impulse *Receptor (biochemistry), in biochemistry, a protein molecule that receives and responds to a ...

of adrenergic nerves and thereby inhibiting the release of

noradrenaline Norepinephrine (NE), also called noradrenaline (NA) or noradrenalin, is an organic chemical in the catecholamine family that functions in the brain and body as both a hormone and neurotransmitter. The name "noradrenaline" (from Latin '' ad'', ...

and

adrenaline Adrenaline, also known as epinephrine, is a hormone and medication which is involved in regulating visceral functions (e.g., respiration). It appears as a white microcrystalline granule. Adrenaline is normally produced by the adrenal glands an ...

. Blocking this receptor leads to smooth muscle relaxation and

vasodilation Vasodilation is the widening of blood vessels. It results from relaxation of smooth muscle cells within the vessel walls, in particular in the large veins, large arteries, and smaller arterioles. The process is the opposite of vasoconstrictio ...

Route of administration and dose

Pentolinium can be given orally (20mg three times a day), injected intramuscularly, or administered

intravenously Intravenous therapy (abbreviated as IV therapy) is a medical technique that administers fluids, medications and nutrients directly into a person's vein. The intravenous route of administration is commonly used for rehydration or to provide nutrie ...

Use

Pentolinium and

hexamethonium Hexamethonium is a non-depolarising ganglionic blocker, a 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 not have a ...

combined with ''

Rauvolfia ''Rauvolfia'' (sometimes spelled ''Rauwolfia'') is a genus of evergreen trees and shrubs, commonly known as devil peppers, in the family Apocynaceae. The genus is named to honor Leonhard Rauwolf. The genus can mainly be found in tropical reg ...

'' was reported in 1955 to be effective in the outpatient management of moderate to severe hypertension, with satisfactory orthostatic reduction in blood pressure but there are significant untoward effects attributable to the use of the hexamethonium. Pentolinium has been reported to offer more prolonged ganglionic blockade and has less severe untoward effects than hexamethonium.

References

External links

DrugBank: Pentolinium
{{Nicotinic acetylcholine receptor modulators Antihypertensive agents Nicotinic antagonists Pyrrolidines Quaternary ammonium compounds