Difference between revisions of "Anticholinergic agents"

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Anticholinergics are agents that decrease or block the actions of [[acetylcholine]] on its parasympathetic nervous system receptors on smooth muscle cells, glands and the central nervous system.
== Types of {{PAGENAME}} ==
Cholinergic receptors are usually categorized as nicotinic or muscarinic. Anticholinergics often demonstrate differential antagonism for different receptors types and subtypes, accounting in part for their variety of actions and clinical usefulness for different conditions.
The anticholinergics in clinical use include natural, semisynthetic and synthetic compounds that demonstrate a multitude of actions on smooth muscle cells and the parasympathetic nervous system.
Anticholinergics have antisecretory activities and decrease nasal and bronchial secretions, salivation, lacrimation, sweating and gastric acid production, and can be used to decrease secretions in allergic and inflammatory diseases. Anticholinergics relax smooth muscle in the [[gastrointestinal tract]], bladder and lung and can be used for gastrointestinal, urological or respiratory conditions associated with spasm and dysmotility. Some anticholinergics have antiemetic properties and are used to prevent nausea and vomiting from motion sickness or during the perioperative period. Anticholinergics increase heart rate and can be used to treat [[bradycardia]]. They are also used to reverse cholinergic overstimulation caused by cholinesterase inhibitors and neuromuscular blockers in anesthesia.
The common side effects of anticholinergic agents are largely those of parasympathetic stimulation and include dryness of the mouth and eyes, decreased sweating and [[hyperthermia]], [[headache]], [[visual blurring]], [[constipation]], [[urinary retention]], [[impotence]], [[tachycardia]] and [[palpitations]], [[anxiety]], [[restlessness]] and in some instances [[[[agitation]]]] and [[[[delusions]]]]. Anticholinergics rarely cause liver injury. Their relative safety probably relates to their use in low doses for short periods of time only. Most anticholinergics are metabolized in the liver via the cytochrome P450 system.
Specific anticholinergic agents in clinical use are listed below with common brand name(s), year of approval in the United States, and major use (G=gastrointestinal, N=nausea and motion sickness, R=respiratory, U=urological). General references to the safety and hepatotoxicity of anticholinergics are given at the end of this overview section and are not repeated in the individual drug descriptions.
Anticholinergics used in Parkinson’s disease include benztropine (Cogentin: 1954), biperiden (Akineton: 1959) and trihexyphenidyl (Artane: 1949).
The natural or semisynthetic belladonna alkaloids include [[Atropine]] (generic), hyoscyamine (Anaspaz: U, G) and scopolamine (Scopace, Transderm Scop: 1979, 2001, N).
The synthetic quaternary ammonium derivatives have a bulky ammonium side chain that makes them less likely to cross membranes, including the blood brain barrier, and therefore less likely to have central nervous system effects. Anticholinergic quaternary ammonium derivatives include aclidinium (Tudorza Pressair: 2012, R), clinidium (Quarzan: now withdrawn), darifenacin (Enablex: 2004, U), flavoxate (Urispas: 1970, U), glycopyrrolate (Robinul: 1961, G), ipratropium (Atrovent: 1986, R), mepenzolate (Cantil: 1956, G), methscopolamine (generic), propantheline (Pro-Banthine: 1953, G) and tiotropium (Tiova: R).
The synthetic tertiary anticholinergics include dicyclomine (Bentyl: 1996, G), fesoterodine (Toviaz: 2008, U), hom[[Atropine]] (generic), oxybutynin (Ditropan: 1975, U), solifenacin (VESIcare: 2004, U), tolterodine (Detrol: 1998, U), and trospium (Sanctura: 2004, U).
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Aclidinium is a synthetic anticholinergic agent that is used as an inhalant for treatment of acute bronchospasm due to chronic bronchitis or emphysema. Aclidinium has not been implicated in causing liver enzyme elevations or clinically apparent acute liver injury.
Aclidinium (a" kli din' ee um) is a synthetic quaternary ammonium anticholinergic which inhibits the muscarinic actions of [[acetylcholine]] on autonomic nerve endings, decreasing bronchial smooth muscle contractions and alleviating bronchospasm in patients with chronic obstructive pulmonary disease (COPD). Aclidinium has potent activity against muscarinic [[acetylcholine]] type 3 (M3) receptors which are found in bronchial smooth muscle. Aclidinium is rapidly hydrolyzed in plasma, so that any actively absorbed drug is unlikely to cause major systemic side effects. Its quaternary ammonium structure also decreases its ability to cross lipid membranes such as the blood brain barrier. Aclidinium was approved for use in the United States in 2012 as a respiratory inhalant and indications include maintenance treatment of bronchospasm associated with chronic bronchitis and emphysema. Aclidinium is available in a dry powder inhaler under the brand name Tudorza Pressair. The typically recommended dose in adults is 1 inhalation (400 mcg) twice daily. The common side effects of typical anticholinergic agents (such as dryness of the mouth and eyes, decreased sweating, [[visual blurring]], [[constipation]], [[urinary retention]], [[impotence]], [[tachycardia]] and [[palpitations]], [[anxiety]] and [[restlessness]]) are uncommon in patients treated with aclidinium by inhaler. Aclidinium use can cause paradoxical bronchospasm. Anticholinergic agents can precipitate acute narrow angle glaucoma and acute [[urinary retention]].
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