Carbachol 742666 204201400 2008-04-08T12:42:43Z Thijs!bot 1392310 robot Adding: [[es:Carbacol]] {{Drugbox| |IUPAC_name = 2-carbamoyloxyethyl-trimethyl-azanium | image=Carbachol.png | CAS_number=51-83-2 | ATC_prefix=N07 | ATC_suffix=AB01 | ATC_supplemental= | PubChem=2551 | DrugBank=APRD00845 | C=6 | H=15 | N=2 | O=2 | charge=+ | molecular_weight = 147.196 g/mol | bioavailability= ? | metabolism = ? | elimination_half-life= ? | excretion = ? | pregnancy_US = C | legal_status = ? | routes_of_administration= Tablet, liquid }} '''Carbachol''', also known as '''carbamylcholine''' (marketed under the brand names '''Carbastat''', '''Carboptic''', '''Isopto Carbachol''', '''Miostat'''), is a [[drug]] that binds and activates the [[acetylcholine receptor]]. Thus it is classified as a [[cholinergic agonist|cholinergic]] [[agonist]]. It is primarily used for various ophthalmic purposes, such as for treating [[glaucoma]], or for use during ophthalmic surgery. It is generally administered as an [[ophthalmic]] solution (i.e. [[eyedrop]]). ==Chemistry and pharmacology== Carbachol is a [[choline]] [[ester]] and a positively charged quaternary ammonium compound. It is not well absorbed in the [[gastro-intestinal tract]] and does not cross the [[blood-brain barrier]]. It is usually administered topical ocular or through intraocular injection. Carbachol is not easily metabolized by [[cholinesterase]], it has a two to 5 minute onset of action and its duration of action is 4 to 8 hours with topical administration and 24 hours for intraocular administration. Since carbachol is poorly absorbed through topical administration, [[benzalkonium chloride]] is mixed in to promote absorption. Carbachol is a [[parasympathomimetic]] that [[agonist|stimulates]] both [[muscarinic acetylcholine receptor|muscarinic]] and [[nicotinic acetylcholine receptor|nicotinic]] receptors. In topical ocular and intraocular administration its principal effects are [[miosis]] and increased [[aqueous humour]] outflow. In the [[cat]] and [[rat]], carbachol is well-known for its ability to induce [[Rapid eye movement sleep|rapid eye movement]] (REM) sleep when microinjected into the [[pons|pontine reticular]] formation. Carbachol elicits this REM sleep-like state via activation of postsynaptic muscarinic [[acetylcholine|cholinergic]] receptors (mAChRs). ==Indications== Carbachol is primarily used in the treatment of [[glaucoma]], but it is also used during ophthalmic surgery. Carbachol eyedrops are used to decrease the pressure in the eye for people with glaucoma. It is sometimes used to constrict the pupils during [[cataract]] surgery. Topical occular administration is used to decrease intraocular pressure in people with primary open-angle [[glaucoma]]. Intraocular administration is used to produce miosis after lens implantation during cataract surgery. Carbachol can also be used to stimulate bladder emptying if the normal emptying mechanism is not working properly. In most countries carbachol is only available by prescription. ==Contraindications== Use of carbachol, as well as all other muscarinic receptor agonists, is contraindicated in patients with asthma, coronary insufficiency, gastroduodenal ulcers, and incontinence. The [[parasympathomimetic]] action of this drug will exacerbate the symptoms of these disorders. ==Overdose== The effects of a systemic overdose on a cholinergic will probably be similar to the effects of a [[nerve agent]], but weaker.{{Fact|date=February 2007}} However, when administered ocularly there is probably little risk of such effects.{{Fact|date=February 2007}} ==External links== * [http://www.rxlist.com/cgi/generic2/carbachol.htm RxList.com - Carbachol] ==References== * Brenner, G. M. (2000). ''Pharmacology.'' Philadelphia, PA: W.B. Saunders Company. ISBN 0-7216-7757-6 * Canadian Pharmacists Association (2000). ''Compendium of pharmaceuticals and specialties'' (25th ed.). Toronto, ON: Webcom. ISBN 0-919115-76-4 * Carbachol (1998). ''MedlinePlus''. Retrieved June 27, 2004, from http://www.nlm.nih.gov/medlineplus/druginfo/uspdi/202110.html * Carbachol (2003). ''RxList''. Retrieved June 27, 2004, from http://www.rxlist.com/cgi/generic2/carbachol.htm * National Institute for Occupational Safety and Health. (2002). Choline, chloride, carbamate. In ''The registry of toxic effects of chemical substances.'' Retrieved June 27, 2004, from http://www.cdc.gov/niosh/rtecs/gad59f8.html * Carbachol Chloride (2004). ''Hazardous Substances Data Bank''. Retrieved July 16, 2004, from http://toxnet.nlm.nih.gov/cgi-bin/sis/htmlgen?hsdbb.htm (search carbachol). {{Parasympathomimetics}} {{Antiglaucoma preparations and miotics}} [[Category:Quaternary ammonium compounds]] [[Category:Choline esters]] [[Category:Carbamates]] [[de:Carbachol]] [[es:Carbacol]] [[ja:カルバコール]]