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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2016/12/03 23:12:50」(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 Glycopyrronium.^[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]

It is used to treat Ménière's disease.^[10]

Side effects

Since glycopyrronium reduces the body's sweating ability, it can even cause hyperthermia 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,^[11] 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.^[12]

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. doi:10.3349/ymj.2003.44.4.579. 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.
^ Maria, Sammartano Azia; Claudia, Cassandro; Pamela, Giordano; Andrea, Canale; Roberto, Albera (1 December 2012). "Medical therapy in Ménière's disease". Audiological Medicine. 10 (4): 171–177. doi:10.3109/1651386X.2012.718413 – via Taylor and Francis+NEJM.
^ 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

Pharmacological interventions for treating sialorrhea associated with neurological disorders: A mixed treatment network meta-analysis of randomized controlled trials.

Sridharan K1, Sivaramakrishnan G2.
Journal of clinical neuroscience : official journal of the Neurosurgical Society of Australasia.J Clin Neurosci.2018 May;51:12-17. doi: 10.1016/j.jocn.2018.02.011. Epub 2018 Feb 21.
PMID 29475576

Nebulized glycopyrrolate (Lonhala Magnair) for COPD.

[No authors listed]
The Medical letter on drugs and therapeutics.Med Lett Drugs Ther.2018 Apr 23;60(1543):72.
PMID 29667949

Stability of regularly prescribed oral liquids formulated with SyrSpend^® SF.

Uriel M, Gómez-Rincón C, Marro D.
Die Pharmazie.Pharmazie.2018 Apr 2;73(4):196-201. doi: 10.1691/ph.2018.7008.
The purpose of this research was to evaluate the stability of 12 oral liquid formulations frequently compounded in hospital and community settings formulated in a specific vehicle: SyrSpend® SF. The stability of melatonin, glycopyrrolate, ciclosporin, chloral hydrate, flecainide acetate, tiagabine
PMID 29609685

Japanese Journal

Comparative Characterization of Lung Muscarinic Receptor Binding After Intratracheal Administration of Tiotropium, Ipratropium, and Glycopyrrolate

OGODA Masaki,NIIYA Ryo,KOSHIKA Tadatsura,YAMADA Shizuo
Journal of pharmacological sciences 115(3), 374-382, 2011-03-20
… The aim of the current study was to characterize comparatively the binding of muscarinic receptor in the lung of rats intratracheally administered anticholinergic agents (tiotropium, ipratropium, glycopyrrolate) used clinically to treat chronic obstructive pulmonary disease (COPD) and asthma. …
NAID 10029892778

Effects of premedication on salivary secretion in the rat submandibular gland

Taniwa Satoko,Uchihashi Kenji,Kotani Junichiro,Nishikawa Yasuo
Journal of Osaka Dental University 43(1), 119-127, 2009-04
… The effects of muscarinic antagonists (pirenzepine, methoctramine, 4-diphenylacetoxy-N-dimethylpiperidinium (4-DAMP) and glycopyrrolate) were examined on secretion from the submandibular gland evoked by acetylcholine in pentobarbital-anesthetized rats. … Glycopyrrolate caused less elevation in heart rate than the other anticholinergics. … 4-DAMP and glycopyrrolate markedly inhibited the acetylcholine-evoked fluid responses. …
NAID 110007160618

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拡張検索	「glycopyrrolate bromide」

「glycopyrrolate bromide」

Glycopyrronium
Clinical data
AHFS/Drugs.com	Monograph
MedlinePlus	a602014
Pregnancy; category	US: B (No risk in non-human studies); ;
Routes of; administration	oral, IV
ATC code	A03AB02 (WHO) R03BB06 (WHO)
Legal status
Legal status	US: ℞-only;
Pharmacokinetic data
Biological half-life	0.6–1.2 hours
Excretion	85% renal, unknown amount in the bile
Identifiers
	IUPAC name: 3-(2-Cyclopentyl-2-hydroxy-2-phenylacetoxy)-1,1-dimethylpyrrolidinium
CAS Number	596-51-0
PubChem (CID)	3494
IUPHAR/BPS	7459
DrugBank	DB00986
ChemSpider	3374
UNII	V92SO9WP2I
KEGG	D00540
ChEMBL	CHEMBL1201335
Chemical and physical data
Formula	C19H28NO3+
Molar mass	318.431 g/mol
3D model (Jmol)	Interactive image
	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 ;
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Glycopyrronium bromide
Clinical data
Pregnancy; category	US: B (No risk in non-human studies); ;
ATC code	A03AB02 (WHO) R03BB06 (WHO)
Legal status
Legal status	US: ℞-only;
Identifiers
	IUPAC name: 3-[2-Cyclopentyl(hydroxy)phenylacetoxy]-1,1-dimethylpyrrolidinium bromide
CAS Number	51186-83-5
PubChem (CID)	11693
ChemSpider	11201
UNII	V92SO9WP2I
Chemical and physical data
Formula	C19H28BrNO3
Molar mass	398.335 g/mol
3D model (Jmol)	Interactive image
	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 ;

　　[★] 臭化グリコピロレート

[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. doi:10.3349/ymj.2003.44.4.579. 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.

[10] Maria, Sammartano Azia; Claudia, Cassandro; Pamela, Giordano; Andrea, Canale; Roberto, Albera (1 December 2012). "Medical therapy in Ménière's disease". Audiological Medicine. 10 (4): 171–177. doi:10.3109/1651386X.2012.718413 – via Taylor and Francis+NEJM.

[pmid10385241-11] 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.

[12] 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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glycopyrrolate