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any of the salts of hydrobromic acid; formerly used as a sedative but now generally replaced by safer drugs

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〈U〉臭化物(鎮静剤・睡眠剤として用いる) / 〈C〉《話》陳腐なことば

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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2015/12/20 19:33:06」(JST)

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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]

Medical uses

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).^[2]^[3]^[4]

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^[5]^[6] and COPD^[7] has been described.

It has been used topically and orally to treat hyperhidrosis, in particular, gustatory hyperhidrosis.^[8]^[9]

Side effects

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.

Pharmacology

Glycopyrronium blocks muscarinic receptors,^[10] thus inhibiting cholinergic transmission.

Pharmacokinetics

Glycopyrronium bromide affects the gastrointestinal tracts, liver and kidney but has a very limited effect on the brain and the central nervous system. In horse studies, after a single intravenous infusion, the tendency of glycopyrronium followed a tri-exponential equation, followed by rapid disappearance from the blood followed by a prolonged terminal phase. Excretion was mainly in urine and in the form of an unchanged drug. Glycopyrronium has a relatively slow diffusion rate, and in a standard comparison to atropine, is more resistant to penetration through the blood-brain barrier and placenta.^[11]

References

^ 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.
^ 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. doi:10.1001/archpedi.154.12.1214. 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". 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.
^ 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.
^ Rumpler, M.J.; Colahan, P.; Sams, R.A. (2014). "The pharmacokinetics of glycopyrrolate in Standardbred horses". J. Vet Pharmacol Ther. 3 (37): 260–8. doi:10.1111/jvp.12085. PMID 24325462.

UpToDate Contents

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1. 麻酔後回復室（PACU）における心血管の障害 cardiovascular problems in the post anesthesia care unit pacu
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
3. 眼の待機手術に対する麻酔 anesthesia for elective eye surgery
4. 脊髄麻酔：手技 spinal anesthesia technique
5. 重症筋無力症患者に対する麻酔 anesthesia for the patient with myasthenia gravis

English Journal

Effects of sugammadex vs. pyridostigmine-glycopyrrolate on post-operative nausea and vomiting: propensity score matching.

Lee OH1, Choi GJ1, Kang H1, Baek CW1, Jung YH1, Woo YC1, Oh J1, Park YH1.
Acta anaesthesiologica Scandinavica.Acta Anaesthesiol Scand.2017 Jan;61(1):39-45. doi: 10.1111/aas.12813. Epub 2016 Oct 2.
BACKGROUND: Sugammadex is a new agent that reverses neuromuscular blockade by aminosteroid neuromuscular blocker. This retrospective study compared the effects of sugammadex on post-operative nausea and vomiting (PONV) with those of a pyridostigmine-glycopyrrolate mixture.METHODS: We reviewed the el
PMID 27696339

Drug updates and approvals: 2016 in review.

Meadowcraft L1, Mospan G, Morrisette T, Smart K, Janis M.
The Nurse practitioner.Nurse Pract.2016 Dec 16;41(12):20-27.
In 2016, the FDA approved several new drugs for use in primary care. These drugs include amphetamine extended-release orally disintegrating tablets (Adzenys XR-ODT), elbasvir and grazoprevir (Zepatier), emtricitabine and tenofovir alafenamide (Descovy), glycopyrrolate and formoterol (Bevespi Aerosph
PMID 27861265

Efficacy and Safety of Glycopyrrolate/Formoterol MDI Formulated using Co-Suspension™ Delivery Technology in Patients with COPD.

Martinez FJ1, Rabe KF2, Ferguson GT3, Fabbri LM4, Rennard S5, Feldman GJ6, Sethi S7, Spangenthal S8, Gottschlich GM9, Rodriguez-Roisin R10, Arora S11, Siler TM12, Siddiqui S13, Darken P14, Fischer T15, Maes A14, Golden M15, Orevillo C14, Reisner C14.
Chest.Chest.2016 Dec 1. pii: S0012-3692(16)62551-5. doi: 10.1016/j.chest.2016.11.028. [Epub ahead of print]
BACKGROUND: Long-acting muscarinic antagonist (LAMA)/long-acting β2-agonist (LABA) combinations are a treatment option for patients with chronic obstructive pulmonary disease (COPD) who continue to have symptoms despite treatment with a LAMA or LABA alone.OBJECTIVES: The PINNACLE-1 (NCT01854645) an
PMID 27916620

Japanese Journal

高齢者における周術期管理 : Glycopyrronium bromide 投与時の脳波定量分析

岩田修
日本手術医学会誌 = Journal of Japanese Association for Operating Room Technology 18(4), 429-437, 1997-11-30
NAID 10011343264

抗コリン剤Glycopyrronium bromideのreserpine潰瘍に対する効果--殊に脈管の立場から

村井俊介 [他]
臨牀と研究 54(7), p2365-2374, 1977-07
NAID 40003783335

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★リンクテーブル★

リンク元	「グリコピロニウム」
関連記事	「bromide」「bromides」

「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; category	US: B (No risk in non-human studies); ;
Legal status	US: ℞-only;
Routes of; administration	oral, IV
Pharmacokinetic data
Biological 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
IUPHAR/BPS	7459
DrugBank	DB00986
ChemSpider	3374
UNII	V92SO9WP2I
KEGG	D00540
ChEMBL	CHEMBL1201335
Chemical data
Formula	C19H28NO3+
Molecular mass	318.431 g/mol
	SMILES C[N+]1(CCC(C1)OC(=O)C(C2CCCC2)(C3=CC=CC=C3)O)C ;
	InChI InChI=1S/C19H28NO3/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/q+1 ; Key:ANGKOCUUWGHLCE-UHFFFAOYSA-N ;
(what is this?) (verify)

Glycopyrronium bromide
Systematic (IUPAC) name
	3-[2-Cyclopentyl(hydroxy)phenylacetoxy]-1,1-dimethylpyrrolidinium bromide
Clinical data
Pregnancy; category	US: B (No risk in non-human studies); ;
Legal status	US: ℞-only;
Identifiers
ATC code	A03AB02 R03BB06
PubChem	CID: 11693
ChemSpider	11201
Chemical data
Formula	C19H28BrNO3
Molecular mass	398.335 g/mol
	SMILES C[N+]1(CCC(C1)OC(=O)C(C2CCCC2)(C3=CC=CC=C3)O)C.[Br-] ;
	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 ;

　　[★]

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

「bromide」

　　[★]

n.

臭化物、ブロム剤

「bromides」

　　[★]

n.

臭化物、ブロム剤

[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.

[pmid11115305-2] 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. doi:10.1001/archpedi.154.12.1214. PMID 11115305.

[pmid12398577-3] Tscheng DZ (November 2002). "Sialorrhea - therapeutic drug options". Ann Pharmacother 36 (11): 1785–90. doi:10.1345/aph.1C019. PMID 12398577.

[pmid10534970-4] 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.

[pmid16236844-5] 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.

[pmid2225951-6] 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.

[pmid8834341-7] 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.

[pmid12950111-8] Kim WO, Kil HK, Yoon DM, Cho MJ (August 2003). "Treatment of compensatory gustatory hyperhidrosis with topical glycopyrrolate". Yonsei Med. J. 44 (4): 579–82. PMID 12950111.

[pmid18294315-9] 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.

[pmid10385241-10] 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.

[11] Rumpler, M.J.; Colahan, P.; Sams, R.A. (2014). "The pharmacokinetics of glycopyrrolate in Standardbred horses". J. Vet Pharmacol Ther. 3 (37): 260–8. doi:10.1111/jvp.12085. PMID 24325462.

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案内

glycopyrronium bromide