臭化ヘキサメトニウム

関: C6、hexamethonium

WordNet

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

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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2016/06/14 12:57:27」(JST)

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Hexamethonium is a non-depolarising ganglionic blocker, a nicotinic nACh (N_N) receptor antagonist^[1] that acts in autonomic ganglia by binding mostly in or on the N_N receptor, and not the acetylcholine binding site itself. It does not have any effect on the muscarinic acetylcholine receptors (mAChR) located on target organs of the parasympathetic nervous system but acts as antagonist at the nicotinic acetylcholine receptors located in sympathetic and parasympathetic ganglia (N_N).^[2]

Pharmacology

It can act on receptors at pre-ganglionic sites in both the sympathetic and parasympathetic nervous systems, which are both regulated by nicotinic ligand-gated ionotropic acetylcholine receptors. Postganglionic sympathetic systems are usually regulated by norepinephrine (noradrenaline) (adrenergic receptors), whereas parasympathetic systems are acetylcholine-based, and instead rely on muscarinic receptors (some post-ganglionic sympathetic neurons, such as those stimulating sweat glands, release acetylcholine).

The organ system and adverse effects of ganglion blockers are due to the parasympathetic and sympathetic stimuli blockage at preganglionic sites. Side-effects include combined sympatholytic (e.g., orthostatic hypotension and sexual dysfunction) and parasympatholytic (e.g., constipation, urinary retention, glaucoma, blurry vision, decreased lacrimal gland secretion, dry mouth (xerostomia)) effects.

Uses

It was formerly used to treat disorders, such as chronic hypertension, of the peripheral nervous system, which is innervated only by the sympathetic nervous system. The non-specificity of this treatment led to discontinuing its use.^[3]

The use of inhaled hexamethonium, an unapproved drug, in a normal volunteer during a medical study is believed to have caused or contributed to her death^[4]^[5] in light of the presence of abnormal "ground glass opacities" on her chest X-ray.

References

^ "Hexamethonium - Compound Summary". http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=3604. 2013-06-18. Missing or empty |url= (help)
^ Howland RD, Mycek MJ 2006. Lippincott's illustrated reviews: Pharmacology. 3:d edition, page 47.
^ Hardman et al., Goodman and Gilman's The Pharmacological Basis of Therapeutics, 10th edition, 2001, pp 210-211.
^ "Johns Hopkins’ Tragedy: Could Librarians Have Prevented a Death?". Retrieved 2008-10-06.
^ Savulescu J, Spriggs M (February 2002). "The hexamethonium asthma study and the death of a normal volunteer in research". Journal of Medical Ethics 28 (1): 3–4. doi:10.1136/jme.28.1.3. PMC 1733509. PMID 11834748.

UpToDate Contents

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1. 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
2. 物理性蕁麻疹 physical urticarias
3. 代謝性アシドーシス以外の状況における血清アニオンギャップ serum anion gap in conditions other than metabolic acidosis
4. 12歳未満の小児における慢性喘息：初回評価および診断 asthma in children younger than 12 years rescue treatment for acute symptoms
5. 小児における喘息の急性増悪：救急外来によるマネージメント acute asthma exacerbations in children emergency department management

English Journal

Xenin-25 induces anion secretion by activating non-cholinergic secretomotor neurons in the rat ileum.

Kuwahara A, Kuwahara Y, Kato I, Kawaguchi K, Harata D, Asano S, Inui T, Marunaka Y.
American journal of physiology. Gastrointestinal and liver physiology. 2019 Apr;().
Xenin-25 is a neurotensin-like peptide that is secreted by enteroendocrine cells in the small intestine. Xenin-8 is reported to augment duodenal anion secretion by activating afferent neural pathways. The intrinsic neuronal circuits mediating the Xenin-25-induced anion secretion were characterized u
PMID 30978113

Inhibitory effect of luminal saccharides on glucose absorption from an adjacent jejunal site in rats: a newly described intestinal neural reflex.

Mourad FH, Barada KA, Saade NE.
Pflugers Archiv : European journal of physiology. 2019 Apr;471(4)595-603.
Nutrients in the lumen of the small intestine are sensed by special cells in the epithelial lining. The ensuing neurohumoral reflexes affect gastrointestinal absorption/secretion, motility, and vascular perfusion. To study in vivo the effect of a monosaccharide (glucose) or polysaccharide (starch) p
PMID 30402765

Anti-cholinergics mecamylamine and scopolamine alleviate motion sickness-induced gastrointestinal symptoms through both peripheral and central actions.

Qi R, Su Y, Pan L, Mao Y, Liang L, Dai Z, Wang J, Cai Y.
Neuropharmacology. 2019 Mar;146()252-263.
Enhanced cholinergic activity contributes to the production of complex autonomic manifestations of motion sickness (MS). However, whether anti-cholinergics exert their anti-MS effects through central or peripheral actions remained unclarified. In the present study, we investigated the effects of mec
PMID 30543811

Japanese Journal

タウリン・オルニチン・グリシンのラット小腸吸収に対するカプサイシンの作用

田中竜介,井上晋一,杉浦義正 [他]
医学と生物学 155(10), 682-690, 2011-10
NAID 40019018648

V1 Receptor Activation Induced by Hemorrhage and Sympathoinhibition in the Mesentery and Hindquarters of Spontaneously Hypertensive Rats

Xing Chi Hong,Teranishi Yasuhiro
Hiroshima Journal of Medical Sciences 54(4), 93-99, 2005-12
… The combination of a non-hypotensive hemorrhage (0.3 ml/100 g weight) and ganglionic blockade with hexamethonium bromide (C6; …
NAID 120005617623

動脈圧の低振動成分に介在する交感神経活動に及ぼす一酸化窒素の血行力学的効果

飯田紀子
日本生理学会大会発表要旨集 2004(0), S97-S97, 2004
… Ganglion blocker hexamethonium bromide (C6), N<sup>ω</sup>-nitro-L-arginine methyl ester (L-NAME), and L-arginine (L-Arg) were used to examine the hemodynamic effects of the NO system and the sympathetic nervous system on mean arterial pressure (MAP), mean heart rate (MHR), arterial pressure variability (APV) and heart rate variability (HRV). …
NAID 130005447362

「臭化ヘキサメトニウム」

Hexamethonium
Systematic (IUPAC) name
	N,N,N,N',N',N'-hexamethylhexane-1,6-diaminium
Clinical data
Pregnancy; category	D;
Legal status
Legal status	℞ (Prescription only);
Identifiers
CAS Number	60-26-4
PubChem	CID 3604
IUPHAR/BPS	3963
DrugBank	DB08960
ChemSpider	3478
UNII	3C9PSP36Z2
ChEMBL	CHEMBL105608
Chemical data
Formula	C12H30N2
Molar mass	202.38 g/mol
	SMILES C(CCCC[N+](C)(C)C)C[N+](C)(C)C ;
	InChI InChI=1S/C12H30N2/c1-13(2,3)11-9-7-8-10-12-14(4,5)6/h7-12H2,1-6H3/q+2 ; Key:VZJFGSRCJCXDSG-UHFFFAOYSA-N ;
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　　[★]

英: hexamethonium bromide
関: ヘキサメソニウム、ヘキサメトニウム

「bromide」

　　[★]

n.

臭化物、ブロム剤

「bromides」

　　[★]

n.

臭化物、ブロム剤

[1] "Hexamethonium - Compound Summary". http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=3604. 2013-06-18. Missing or empty |url= (help)

[2] Howland RD, Mycek MJ 2006. Lippincott's illustrated reviews: Pharmacology. 3:d edition, page 47.

[3] Hardman et al., Goodman and Gilman's The Pharmacological Basis of Therapeutics, 10th edition, 2001, pp 210-211.

[urlJohns_Hopkins.E2.80.99_Tragedy:_Could_Librarians_Have_Prevented_a_Death.3F-4] "Johns Hopkins’ Tragedy: Could Librarians Have Prevented a Death?". Retrieved 2008-10-06.

[pmid11834748-5] Savulescu J, Spriggs M (February 2002). "The hexamethonium asthma study and the death of a normal volunteer in research". Journal of Medical Ethics 28 (1): 3–4. doi:10.1136/jme.28.1.3. PMC 1733509. PMID 11834748.

リンク元	「臭化ヘキサメトニウム」
関連記事	「bromide」「bromides」

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案内

hexamethonium bromide