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cholinergic alkaloid used in eyedrops to treat glaucoma

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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2014/02/01 17:27:30」(JST)

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Pilocarpine is a parasympathomimetic alkaloid obtained from the leaves of tropical American shrubs from the genus Pilocarpus. It is a non-selective muscarinic receptor agonist^[2] in the parasympathetic nervous system, which acts therapeutically at the muscarinic acetylcholine receptor M3 due to its topical application,^[3] e.g., in glaucoma and xerostomia.

Uses[edit]

Clinical[edit]

Pilocarpine has been used in the treatment of chronic open-angle glaucoma and acute angle-closure glaucoma for over 100 years.^[4] It acts on a subtype of muscarinic receptor (M₃) found on the iris sphincter muscle, causing the muscle to contract and engage in miosis. Pilocarpine also acts on the ciliary muscle and causes it to contract. When the ciliary muscle contracts, it opens the trabecular meshwork through increased tension on the scleral spur. This action facilitates the rate that aqueous humor leaves the eye to decrease intraocular pressure.

In ophthalmology, pilocarpine is also used to reduce the possibility of glare at night from lights when the patient has undergone implantation of phakic intraocular lenses; the use of pilocarpine would reduce the size of the pupils, relieving these symptoms. The most common concentration for this use is pilocarpine 1%, the weakest concentration.

Pilocarpine is also used to treat dry mouth (xerostomia) which can occur, for example, as a side effect of radiation therapy for head and neck cancers. Pilocarpine stimulates the secretion of large amounts of saliva and sweat.^[5]

Pilocarpine is used to stimulate sweat glands in a sweat test to measure the concentration of chloride and sodium that is excreted in sweat. It is used to diagnose cystic fibrosis (CF).

Preparation[edit]

Plants in the genus Pilocarpus are the only known sources of Pilocarpine, and commercial production is derived entirely from the leaves of Pilocarpus microphyllus (Maranham Jaborandi). This genus grows only in South America, and Pilocarpus microphyllus is native to several states in northern Brazil.^[6]

Pilocarpine is extracted from the powdered leaf material in a multi-step process. First the material is treated with ethanol acidified with hydrochloric acid, and the solvents removed under reduced pressure. The resultant aqueous residue is neutralized with ammonia and put aside until the resin has completely settled. It is then filtered and concentrated by sugar solution to a small volume, made alkaline with ammonia, and finally extracted with chloroform. The solvent is removed under reduced pressure.^{[verification needed]}

Scientific[edit]

Pilocarpine is used to induce chronic epilepsy in rodents, commonly rats, as a means to study the disorder's physiology and to examine different treatments.^[7] Smaller doses may be used to induce salivation in order to collect samples of saliva, for instance, to obtain information about IgA antibodies.

Veterinary[edit]

Pilocarpine is given in moderate doses (about 2 mg) to induce emesis in cats who have ingested foreign plants, foods, or drugs. One feline trial determined it was effective, even though the usual choice of emetic is xylazine.

Trade names[edit]

Pilocarpine is available under several trade names such as: Diocarpine (Dioptic), Isopto Carpine (Alcon), Miocarpine (CIBA Vision), Ocusert Pilo-20 and -40 (Alza), Pilopine HS (Alcon), Salagen (MGI Pharma), Scheinpharm Pilocarpine (Schein Pharmaceutical), and Timpilo (Merck Frosst).

Adverse effects[edit]

Use of pilocarpine may result in a range of adverse effects, most of them related to its non-selective action as a muscarinic receptor agonist. Pilocarpine has been known to cause excessive sweating, excessive salivation, bronchospasm, increased bronchial mucus secretion, bradycardia, vasodilation, brow ache (when used as eye drops) and diarrhea. It can also result in miosis when used chronically as an eye drop. Systemic injection of pilocarpine can compromise the blood brain barrier allowing pilocarpine to gain access to the brain. This can lead to chronic epilepsy.

Epilepsy induced by pilocarpine has been used to develop animal models in rodents in order to study human epilepsy.

References[edit]

^ Mervyn Gornitsky, George Shenouda, Khalil Sultanem, Howard Katz, Michael Hier, Martin Black, Ana M Velly (2004). "Double-blind randomized, placebo-controlled study of pilocarpine to salvage salivary gland function during radiotherapy of patients with head and neck cancer". Oral Surgery, Oral Medicine, Oral Pathology, Oral Radiology and Endodontology 98 (1): 45–52.
^ Spalding et al. 2002.
^ Pharmacology, (Rang, Dale, Ritter & Moore, ISBN 0-443-07145-4, 5:th ed., Churchill Livingstone 2003) Page 144.
^ Rosin, A. (1991). "Pilocarpine. A miotic of choice in the treatment of glaucoma has passed 110 years of use". Oftalmologia (Romania) 35 (1): 53–55. PMID 1811739.
^ "Pilocarpine".
^ De Abreu, Ilka Nacif; Sawaya, Alexandra Cristine H. F.; Eberlin, Marcos Nogueira; Mazzafera, Paulo (November–December 2005). "Production of Pilocarpine in Callus of Jaborandi (Pilocarpus microphyllus Stapf)". In Vitro Cellular & Developmental Biology. Plant (Society for In Vitro Biology) 41 (6): 806–811.
^ Morimoto, K; Fahnestock, M, Racine, RJ (May 2004). "Kindling and status epilepticus models of epilepsy: rewiring the brain.". Progress in neurobiology 73 (1): 1–60. doi:10.1016/j.pneurobio.2004.03.009. PMID 15193778. Cite uses deprecated parameters (help)

External links[edit]

U.S. National Library of Medicine: Drug Information Portal - Pilocarpine

UpToDate Contents

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1. シェーグレン症候群における口内乾燥およびその他の非眼結膜炎症状の治療 treatment of dry mouth and other non ocular sicca symptoms in sjogrens syndrome
2. 頭頚部癌の後期合併症のマネージメントおよびその治療 management of late complications of head and neck cancer and its treatment
3. 閉塞隅角緑内障 angle closure glaucoma
4. 緊張性瞳孔 tonic pupil
5. シェーグレン症候群におけるドライアイの治療 treatment of dry eyes in sjogrens syndrome

English Journal

Upregulation of dysbindin in temporal lobe epileptic foci of human and experimental animals.

Zhang Y, Xu Y, Zhu Q, Zhao F, Luo J, Zhang X, Wang X.SourceDepartment of Neurology, The First Affiliated Hospital of Chongqing Medical University, Chongqing Key Laboratory of Neurology, Chongqing 400016, China.
Synapse (New York, N.Y.).Synapse.2012 Jul;66(7):622-9. doi: 10.1002/syn.21548. Epub 2012 Mar 30.
The gene encoding dystrobrevin-binding-protein-1 (dysbindin) is expressed in many areas of the central nervous system and plays a role in intracellular vesicle trafficking, synaptic vesicle trafficking, and neurotransmitter release. At a cellular level, dysbindin is thought to mediate presynaptic gl
PMID 22337344

Glutamate carboxypeptidase II (GCPII) inhibitor displays anti-glutamate and anti-cocaine effects in an invertebrate assay.

Tallarida C, Song K, Raffa RB, Rawls SM.SourceDepartment of Pharmaceutical Sciences, Temple University Health Sciences Center, 3307 North Broad Street, Philadelphia, PA, 19140, USA.
Amino acids.Amino Acids.2012 Jun;42(6):2521-4. Epub 2011 Aug 18.
Glutamate carboxypeptidase II (GCPII) inhibitors are promising anti-glutamatergic and anti-addictive agents. We hypothesized that a GCPII inhibitor 2 (phosphonomethyl) pentanedioic acid (2-PMPA) would display anti-stereotypical activity in planarians. Experiments revealed that 2-PMPA displayed no ov
PMID 21850438

Japanese Journal

ドライアイに対する内服ピロカルピン塩酸塩の効果の検討 (特集第64回日本臨床眼科学会講演集(3))

高野朋子,白石敦,山口昌彦 [他]
臨床眼科 65(5), 617-620, 2011-05
NAID 40018862506

Upregulation of STREX splice variant of the large conductance Ca^<2+>-activated potassium (BK) channel in a rat model of mesial temporal lobe epilepsy

ERMOLINSKY Boris S.,SKINNER Frank,GARCIA Ileana,ARSHADMANSAB Massoud F.,PACHECO OTALORA Luis F.,ZAREI Masoud M.,GARRIDO-SANABRIA Emilio R.
Neuroscience research : the official journal of the Japan Neuroscience Society 69(1), 73-80, 2011-01-01
NAID 10028190294

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★リンクテーブル★

リンク元	「ピロカルピン」
拡張検索	「pilocarpine instillation test」

「ピロカルピン」

Pilocarpine
Systematic (IUPAC) name
	(3S,4R)-3-Ethyl-4-((1-methyl-1H-imidazol-5-yl)methyl)dihydrofuran-2(3H)-one
Clinical data
Trade names	Salagen
AHFS/Drugs.com	monograph
MedlinePlus	a608039
Pregnancy cat.	C
Legal status	℞-only (US)
Routes	gtts, p.o.
Pharmacokinetic data
Half-life	0.76 hours (5 mg), 1.35 hours (10 mg)
Excretion	urine
Identifiers
CAS number	92-13-7 ; 54-71-7 (hydrochloride)
ATC code	N07AX01 S01EB01
PubChem	CID 5910
IUPHAR ligand	305
DrugBank	DB01085
ChemSpider	5699
UNII	01MI4Q9DI3
KEGG	D00525
ChEBI	CHEBI:8207
ChEMBL	CHEMBL550
Chemical data
Formula	C11H16N2O2
Mol. mass	208.257 g/mol
	SMILES O=C2OC[C@H](Cc1n(cnc1)C)[C@@H]2CC;
	InChI InChI=1S/C11H16N2O2/c1-3-10-8(6-15-11(10)14)4-9-5-12-7-13(9)2/h5,7-8,10H,3-4,6H2,1-2H3/t8-,10-/m0/s1 ; Key:QCHFTSOMWOSFHM-WPRPVWTQSA-N ;
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　　[★]

英: pilocarpine
化: 塩酸ピロカルピン pilocarpine hydrochloride
商: アドソルボカルピン、サラジェン、サンピロ、ピロリナ
関: ムスカリン受容体

muscarinic receptor agonist
アルカロイド
シェーグレン症候群や放射線照射後のxerostomia(dry mouse)に対する治療薬として用いられる(PPC.121)

「pilocarpine instillation test」

　　[★] ピロカルピン点眼試験

[1] Mervyn Gornitsky, George Shenouda, Khalil Sultanem, Howard Katz, Michael Hier, Martin Black, Ana M Velly (2004). "Double-blind randomized, placebo-controlled study of pilocarpine to salvage salivary gland function during radiotherapy of patients with head and neck cancer". Oral Surgery, Oral Medicine, Oral Pathology, Oral Radiology and Endodontology 98 (1): 45–52.

[2] Spalding et al. 2002.

[Rang-3] Pharmacology, (Rang, Dale, Ritter & Moore, ISBN 0-443-07145-4, 5:th ed., Churchill Livingstone 2003) Page 144.

[4] Rosin, A. (1991). "Pilocarpine. A miotic of choice in the treatment of glaucoma has passed 110 years of use". Oftalmologia (Romania) 35 (1): 53–55. PMID 1811739.

[5] "Pilocarpine".

[ivcdb-6] De Abreu, Ilka Nacif; Sawaya, Alexandra Cristine H. F.; Eberlin, Marcos Nogueira; Mazzafera, Paulo (November–December 2005). "Production of Pilocarpine in Callus of Jaborandi (Pilocarpus microphyllus Stapf)". In Vitro Cellular & Developmental Biology. Plant (Society for In Vitro Biology) 41 (6): 806–811.

[7] Morimoto, K; Fahnestock, M, Racine, RJ (May 2004). "Kindling and status epilepticus models of epilepsy: rewiring the brain.". Progress in neurobiology 73 (1): 1–60. doi:10.1016/j.pneurobio.2004.03.009. PMID 15193778. Cite uses deprecated parameters (help)

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pilocarpine