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Glycopyrronium bromide is a medication of the muscarinic anticholinergic group. It does not cross the blood–brain barrier and consequently has no to few central effects. A synthetic quaternary amine, it is available in oral and intravenous (i.v.) forms. It was developed by Sosei and licensed to Novartis in 2005. The cation, which is the active moiety, is also known as glycopyrrolate.^[1]

Pharmacology[edit source | edit]

Glycopyrronium blocks muscarinic receptors,^[2] thus inhibiting cholinergic transmission.

Medical uses[edit source | edit]

In anesthesia, glycopyrronium injection can be used as a preoperative medication in order to reduce salivary, tracheobronchial, and pharyngeal secretions, as well as decreasing the acidity of gastric secretion. It is also used in conjunction with neostigmine, a neuromuscular blocking reversal agent, to prevent neostigmine's muscarinic effects such as bradycardia.

It is also used to reduce excessive saliva (sialorrhea).^[3]^[4]^[5]

It decreases acid secretion in the stomach and so may be used for treating stomach ulcers, in combination with other medications.

Use in treating asthma^[6]^[7] and COPD^[8] has been described.

It has been used topically and orally to treat hyperhidrosis.^[9]^[10]

Side effects[edit source | edit]

Since glycopyrronium reduces the body's sweating ability, it can even cause fever and heat stroke in hot environments. Dry mouth, difficulty urinating, headaches, diarrhea and constipation are also observed side effects of the medication.

The medication also induces drowsiness or blurred vision, an effect exacerbated by the consumption of alcohol.

References[edit source | edit]

^ Bajaj V, Langtry JA (July 2007). "Use of oral glycopyrronium bromide in hyperhidrosis". Br. J. Dermatol. 157 (1): 118–21. doi:10.1111/j.1365-2133.2007.07884.x. PMID 17459043.
^ Haddad EB, Patel H, Keeling JE, Yacoub MH, Barnes PJ, Belvisi MG (May 1999). "Pharmacological characterization of the muscarinic receptor antagonist, glycopyrrolate, in human and guinea-pig airways". Br. J. Pharmacol. 127 (2): 413–20. doi:10.1038/sj.bjp.0702573. PMC 1566042. PMID 10385241.
^ Mier RJ, Bachrach SJ, Lakin RC, Barker T, Childs J, Moran M (December 2000). "Treatment of sialorrhea with glycopyrrolate: A double-blind, dose-ranging study". Arch Pediatr Adolesc Med 154 (12): 1214–8. PMID 11115305.
^ Tscheng DZ (November 2002). "Sialorrhea - therapeutic drug options". Ann Pharmacother 36 (11): 1785–90. doi:10.1345/aph.1C019. PMID 12398577.
^ Olsen AK, Sjøgren P (October 1999). "Oral glycopyrrolate alleviates drooling in a patient with tongue cancer". J Pain Symptom Manage 18 (4): 300–2. doi:10.1016/S0885-3924(99)00080-9. PMID 10534970.
^ Hansel TT, Neighbour H, Erin EM, et al. (October 2005). "Glycopyrrolate causes prolonged bronchoprotection and bronchodilatation in patients with asthma". Chest 128 (4): 1974–9. doi:10.1378/chest.128.4.1974. PMID 16236844.
^ Gilman MJ, Meyer L, Carter J, Slovis C (November 1990). "Comparison of aerosolized glycopyrrolate and metaproterenol in acute asthma". Chest 98 (5): 1095–8. doi:10.1378/chest.98.5.1095. PMID 2225951.
^ Tzelepis G, Komanapolli S, Tyler D, Vega D, Fulambarker A (January 1996). "Comparison of nebulized glycopyrrolate and metaproterenol in chronic obstructive pulmonary disease". Eur. Respir. J. 9 (1): 100–3. doi:10.1183/09031936.96.09010100. PMID 8834341.
^ Kim WO, Kil HK, Yoon DM, Cho MJ (August 2003). "Treatment of compensatory gustatory hyperhidrosis with topical glycopyrrolate" (^{[dead link]}). Yonsei Med. J. 44 (4): 579–82. PMID 12950111.
^ Kim WO, Kil HK, Yoon KB, Yoon DM (May 2008). "Topical glycopyrrolate for patients with facial hyperhidrosis". Br. J. Dermatol. 158 (5): 1094–7. doi:10.1111/j.1365-2133.2008.08476.x. PMID 18294315.

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UpToDate Contents

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1. 原発性局所多汗症 primary focal hyperhidrosis
2. 慢性閉塞性肺疾患（COPD）における抗コリン療法の役割 role of anticholinergic therapy in copd
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English Journal

Novel relaxant effects of RPL554 on guinea pig tracheal smooth muscle contractility.

Venkatasamy R1, Spina D1.
British journal of pharmacology.Br J Pharmacol.2016 Aug;173(15):2335-51. doi: 10.1111/bph.13512. Epub 2016 Jul 7.
BACKGROUND AND PURPOSE: We investigated the effectiveness of RPL554, a dual PDE3 and 4 enzyme inhibitor, on airway smooth muscle relaxation and compared it with that induced by salbutamol, ipratropium bromide, glycopyrrolate or their combination on bronchomotor tone induced by different spasmogenic
PMID 27174172

Topical glycopyrrolate reduces axillary hyperhidrosis.

Baker DM1.
Journal of the European Academy of Dermatology and Venereology : JEADV.J Eur Acad Dermatol Venereol.2016 Jul 13. doi: 10.1111/jdv.13745. [Epub ahead of print]
INTRODUCTION: Oral anti-cholinergic medications reduce generalized hyperhidrosis, but the effectiveness of topical anticholinergic solutions on axillary hyperhidrosis is unclear. This study determines the initial effectiveness of 1% and 2% topical glycopyrrolate spray and compares this with Botulinu
PMID 27406319

Plantar Hyperhidrosis: An Overview.

Vlahovic TC1.
Clinics in podiatric medicine and surgery.Clin Podiatr Med Surg.2016 Jul;33(3):441-51. doi: 10.1016/j.cpm.2016.02.010. Epub 2016 Mar 26.
Plantar hyperhidrosis, excessive sweating on the soles of feet, can have a significant impact on patients' quality of life and emotional well-being. Hyperhidrosis is divided into primary and secondary categories, depending on the cause of the sweating, with plantar hyperhidrosis typically being prim
PMID 27215162

Japanese Journal

慢性閉塞性肺疾患に対するチオトロピウムとインダカテロールの併用療法からグリコピロニウム/インダカテロール配合剤への切り替えの検討 : 単施設での自己対照比較研究

呼吸器内科 = Respiratory medicine 28(3), 256-262, 2015-09
NAID 40020599206

臨床新薬レビューグリコピロニウム臭化物/インダカテロールマレイン酸塩 Glycopyrronium Bromide/Indacaterol Maleate ウルティブロ吸入用カプセルノバルティスファーマ

MD : medical doctor : 明日を創る医療総合誌 11(6), 27-29, 2014-06
NAID 40020113738

新しいCOPD治療の選択肢 : 長時間作用性抗コリン薬，グリコピロニウム

日本薬理學雜誌 = Folia pharmacologica Japonica 142(4), 190-199, 2013-10-01
NAID 10031202974

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リンク元	「グリコピロニウム」
拡張検索	「glycopyrronium bromide」

「グリコピロニウム」

Glycopyrronium
Systematic (IUPAC) name
	3-(2-cyclopentyl-2-hydroxy-2-phenylacetoxy)-1,1-dimethylpyrrolidinium
Clinical data
AHFS/Drugs.com	monograph
MedlinePlus	a602014
Pregnancy cat.	B
Legal status	?
Routes	oral, IV
Pharmacokinetic data
Half-life	0.6–1.2 hours
Excretion	85% renal, unknown amount in the bile
Identifiers
CAS number	596-51-0
ATC code	A03AB02 R03BB06
PubChem	CID 3494
DrugBank	DB00986
ChemSpider	11201
UNII	V92SO9WP2I
KEGG	D00540
ChEMBL	CHEMBL1201335
Chemical data
Formula	C19H28NO3+
Mol. mass	318.431 g/mol
	SMILES [Br-].O=C(OC1CC[N+](C)(C)C1)C(O)(c2ccccc2)C3CCCC3;
	InChI InChI=1S/C19H28NO3.BrH/c1-20(2)13-12-17(14-20)23-18(21)19(22,16-10-6-7-11-16)15-8-4-3-5-9-15;/h3-5,8-9,16-17,22H,6-7,10-14H2,1-2H3;1H/q+1;/p-1 ; Key:VPNYRYCIDCJBOM-UHFFFAOYSA-M ;
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　　[★]

英: glycopyrronium
同: グリコピロレート
化: 臭化グリコピロニウム glycopyrronium bromide、臭化グリコピロレート glycopyrrolate bromide
商: シーブリ

抗コリン薬、四級アンモニウム系、胃腸機能改善

「glycopyrronium bromide」

　　[★] 臭化グリコピロニウム

[pmid17459043-1] Bajaj V, Langtry JA (July 2007). "Use of oral glycopyrronium bromide in hyperhidrosis". Br. J. Dermatol. 157 (1): 118–21. doi:10.1111/j.1365-2133.2007.07884.x. PMID 17459043.

[pmid10385241-2] Haddad EB, Patel H, Keeling JE, Yacoub MH, Barnes PJ, Belvisi MG (May 1999). "Pharmacological characterization of the muscarinic receptor antagonist, glycopyrrolate, in human and guinea-pig airways". Br. J. Pharmacol. 127 (2): 413–20. doi:10.1038/sj.bjp.0702573. PMC 1566042. PMID 10385241.

[pmid11115305-3] Mier RJ, Bachrach SJ, Lakin RC, Barker T, Childs J, Moran M (December 2000). "Treatment of sialorrhea with glycopyrrolate: A double-blind, dose-ranging study". Arch Pediatr Adolesc Med 154 (12): 1214–8. PMID 11115305.

[pmid12398577-4] Tscheng DZ (November 2002). "Sialorrhea - therapeutic drug options". Ann Pharmacother 36 (11): 1785–90. doi:10.1345/aph.1C019. PMID 12398577.

[pmid10534970-5] Olsen AK, Sjøgren P (October 1999). "Oral glycopyrrolate alleviates drooling in a patient with tongue cancer". J Pain Symptom Manage 18 (4): 300–2. doi:10.1016/S0885-3924(99)00080-9. PMID 10534970.

[pmid16236844-6] Hansel TT, Neighbour H, Erin EM, et al. (October 2005). "Glycopyrrolate causes prolonged bronchoprotection and bronchodilatation in patients with asthma". Chest 128 (4): 1974–9. doi:10.1378/chest.128.4.1974. PMID 16236844.

[pmid2225951-7] Gilman MJ, Meyer L, Carter J, Slovis C (November 1990). "Comparison of aerosolized glycopyrrolate and metaproterenol in acute asthma". Chest 98 (5): 1095–8. doi:10.1378/chest.98.5.1095. PMID 2225951.

[pmid8834341-8] Tzelepis G, Komanapolli S, Tyler D, Vega D, Fulambarker A (January 1996). "Comparison of nebulized glycopyrrolate and metaproterenol in chronic obstructive pulmonary disease". Eur. Respir. J. 9 (1): 100–3. doi:10.1183/09031936.96.09010100. PMID 8834341.

[pmid12950111-9] Kim WO, Kil HK, Yoon DM, Cho MJ (August 2003). "Treatment of compensatory gustatory hyperhidrosis with topical glycopyrrolate" (^{[dead link]}). Yonsei Med. J. 44 (4): 579–82. PMID 12950111.

[pmid18294315-10] Kim WO, Kil HK, Yoon KB, Yoon DM (May 2008). "Topical glycopyrrolate for patients with facial hyperhidrosis". Br. J. Dermatol. 158 (5): 1094–7. doi:10.1111/j.1365-2133.2008.08476.x. PMID 18294315.

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glycopyrronium