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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）』「2019/04/28 02:11:03」(JST)

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Pyridostigmine is a medication used to treat myasthenia gravis.^[1] It is also used together with atropine to end the effects of neuromuscular blocking medication of the non-depolarizing type.^[2] It is typically given by mouth but can also be used by injection.^[2] The effects generally begin within 45 minutes and last up to 6 hours.^[2]

Common side effects include nausea, diarrhea, frequent urination, and abdominal pain.^[2] More severe side effects include low blood pressure, weakness, and allergic reactions.^[2] It is unclear if use in pregnancy is safe for the baby.^[2] Pyridostigmine is an acetylcholinesterase inhibitor in the cholinergic family of medications.^[2] It works by blocking the action of acetylcholinesterase and therefore increases the levels of acetylcholine.^[2]

Pyridostigmine was patented in 1945 and came into medical use in 1955.^[3] It is on the World Health Organization's List of Essential Medicines, the most effective and safe medicines needed in a health system.^[4] Pyridostigmine is available as a generic medication.^[2] The wholesale cost in the developing world is about US$7.17–65.93 a month.^[5] In the United States it costs about US$25–50 per month.^[6]

Medical uses

Pyridostigmine is used to treat muscle weakness in people with myasthenia gravis or forms of congenital myasthenic syndrome and to combat the effects of curariform drug toxicity. Pyridostigmine bromide has been FDA approved for military use during combat situations as an agent to be given prior to exposure to the nerve agent Soman in order to increase survival. Used in particular during the first Gulf War, pyridostigmine bromide has been implicated as a causal factor in Gulf War syndrome.^[7]

Pyridostigmine sometimes is used to treat orthostatic hypotension.^[8] It may also be of benefit in chronic axonal polyneuropathy.^[9]

It is also being prescribed 'off-label' for the postural tachycardia syndrome as well as complications resulting from Ehlers–Danlos syndrome.^[9]^[10]

Contraindications

Pyridostigmine bromide is contraindicated in cases of mechanical intestinal or urinary obstruction and should be used with caution in patients with bronchial asthma.^[11]^[12]

Side effects

Common side effects include:^[11]

Sweating
Diarrhea
Nausea
Vomiting
Abdominal cramps
Increased salivation
Tearing
Increased bronchial secretions
Constricted pupils
Facial flushing due to vasodilation
Erectile dysfunction

Mechanism of action

Pyridostigmine inhibits acetylcholinesterase in the synaptic cleft, thus slowing down the hydrolysis of acetylcholine. It is a quaternary carbamate inhibitor of cholinesterase that does not cross the blood–brain barrier which carbamylates about 30% of peripheral cholinesterase enzyme. The carbamylated enzyme eventually regenerates by natural hydrolysis and excess ACh levels revert to normal.

In a synapse, action potentials are conducted along motor nerves to their terminals where they initiate a Ca²⁺ influx and the release of acetylcholine (ACh). The ACh diffuses across the synaptic cleft and binds to receptors on the post synaptic membrane, causing an influx of Na⁺, resulting in depolarization. If large enough, this depolarization results in an action potential. To prevent constant stimulation once the ACh is released, an enzyme called acetylcholinesterase is present in the endplate membrane close to the receptors on the post synaptic membrane, and quickly hydrolyses ACh.

Names

Pyridostigmine bromide is available under the trade names Mestinon (Valeant Pharmaceuticals), Regonol and Gravitor (SUN Pharma).

References

^ WHO Model Formulary 2008 (PDF). World Health Organization. 2009. p. 429. ISBN 9789241547659. Archived (PDF) from the original on 13 December 2016. Retrieved 8 December 2016.
^ ^a ^b ^c ^d ^e ^f ^g ^h ⁱ "Neostigmine Bromide". The American Society of Health-System Pharmacists. Archived from the original on 21 December 2016. Retrieved 8 December 2016.
^ Fischer, Janos; Ganellin, C. Robin (2006). Analogue-based Drug Discovery. John Wiley & Sons. p. 540. ISBN 9783527607495. Archived from the original on 2016-12-20.
^ "WHO Model List of Essential Medicines (19th List)" (PDF). World Health Organization. April 2015. Archived (PDF) from the original on 13 December 2016. Retrieved 8 December 2016.
^ "Pyridostigmine Bromide". International Drug Price Indicator Guide. Retrieved 8 December 2016.
^ Hamilton, Richart (2015). Tarascon Pocket Pharmacopoeia 2015 Deluxe Lab-Coat Edition. Jones & Bartlett Learning. p. 339. ISBN 9781284057560.
^ Golomb BA (March 2008). "Acetylcholinesterase inhibitors and Gulf War illnesses". Proceedings of the National Academy of Sciences of the United States of America. 105 (11): 4295–300. Bibcode:2008PNAS..105.4295G. doi:10.1073/pnas.0711986105. JSTOR 25461411. PMC 2393741. PMID 18332428. Lay summary – Reuters (March 10, 2008).
^ Gales BJ, Gales MA (2007). "Pyridostigmine in the treatment of orthostatic intolerance". Annals of Pharmacotherapy. 41 (2): 314–8. doi:10.1345/aph.1H458. PMID 17284509.
^ ^a ^b Gales BJ, Gales MA (February 2007). "Pyridostigmine in the treatment of orthostatic intolerance". The Annals of Pharmacotherapy. 41 (2): 314–8. doi:10.1345/aph.1H458. PMID 17284509.
^ Kanjwal K, Karabin B, Sheikh M, et al. (June 2011). "Pyridostigmine in the treatment of postural orthostatic tachycardia: a single-center experience". Pacing and Clinical Electrophysiology. 34 (6): 750–5. doi:10.1111/j.1540-8159.2011.03047.x. PMID 21410722.
^ ^a ^b Mestinon | Home Archived 2008-05-13 at the Wayback Machine
^ Mestinon Official FDA information, side effects and uses Archived 2008-05-24 at the Wayback Machine

UpToDate Contents

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1. 重症筋無力症患者に対する麻酔 anesthesia for the patient with myasthenia gravis
2. 重症筋無力症の治療 treatment of myasthenia gravis
3. 起立性低血圧および食後低血圧の治療 treatment of orthostatic and postprandial hypotension
4. 重症筋無力症に対する長期免疫療法 chronic immunomodulating therapies for myasthenia gravis
5. 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

English Journal

Phenotype of a limb-girdle congenital myasthenic syndrome patient carrying a GFPT1 mutation.

Matsumoto C, Mori-Yoshimura M, Noguchi S, Endo Y, Oya Y, Murata M, Nishino I, Takahashi Y.
Brain & development. 2019 May;41(5)470-473.
We report a 38-year-old woman who presented with mild proximal dominant muscle weakness and fatigability that fluctuated during menstruation and treatment with ephedrine-containing medication. The patient had been diagnosed with "congenital myopathy with tubular aggregates" by muscle biopsy at age 1
PMID 30846217

Pyridostigmine bromide and stress interact to impact immune function, cholinergic neurochemistry and behavior in a rat model of Gulf War Illness.

Macht VA, Woodruff JL, Maissy ES, Grillo CA, Wilson MA, Fadel JR, Reagan LP.
Brain, behavior, and immunity. 2019 Apr;().
Gulf War Illness (GWI) is characterized by a constellation of symptoms that include cognitive dysfunction. While the causes for GWI remain unknown, prophylactic use of the acetylcholinesterase inhibitor pyridostigmine bromide (PB) in combination with the stress of deployment has been proposed to be
PMID 30953774

Cholinergic drugs ameliorate endothelial dysfunction by decreasing O-GlcNAcylation via M3 AChR-AMPK-ER stress signaling.

Cui YL, Xue RQ, Xi He , Ming Zhao , Yu XJ, Liu LZ, Wu Q, Si Yang , Li DL, Zang WJ.
Life sciences. 2019 Apr;222()1-12.
Obesity is associated with increased cardiovascular morbidity and mortality. It is accompanied by augmented O-linked β-N-acetylglucosamine (O-GlcNAc) modification of proteins via increasing hexosamine biosynthetic pathway (HBP) flux. However, the changes and regulation of the O-GlcNAc levels induce
PMID 30786250

Japanese Journal

眼症状を初発とし，クリーゼをきたした全身型重症筋無力症の2例

大野新一郎,坂井摩耶,坂口美華,上床希久,原英夫,江内田寛
神経眼科 35(3), 330-336, 2018
眼症状を初発とし，精査中，治療開始後にクリーゼをきたした高齢者の全身型重症筋無力症（MG）2例の報告．症例1は左眼の眼瞼下垂，滑車神経麻痺にて発症した．AChR抗体陽性で，頸筋の筋力低下をきたし，全身型MGの診断にて，ピリドスチグミン臭化物内服開始となった．内服開始から3日目に呼吸困難をきたし，クリーゼを発症，救急外来受診し緊急入院となった．ステロイド療法，免疫抑制剤，免疫グロブリン静注療法，単純 …
NAID 130007497120

The Long-Lasting Enhancing Effect of Distigmine on Acetylcholine-Induced Contraction of Guinea Pig Detrusor Smooth Muscle Correlates with Its Anticholinesterase Activity

Obara Keisuke,Ogawa Tsukasa,Chino Daisuke,Tanaka Yoshio
Ｂｉｏｌｏｇｉｃａｌ　＆　Ｐｈａｒｍａｃｅｕｔｉｃａｌ　Ｂｕｌｌｅｔｉｎ 40(7), 1092-1100, 2017
… Distigmine bromide (distigmine), a reversible, long-lasting cholinesterase (ChE) inhibitor, is used for the treatment of underactive bladder in Japan and has been shown to potentiate urinary bladder (UB) contractility. … We studied the duration of distigmine's potentiating effects on acetylcholine (ACh)-induced UB contraction and its inhibitory effects on ChE activity, and compared that with those of other ChE inhibitors (neostigmine, pyridostigmine, and ambenonium). …
NAID 130006846428

Long-Lasting Inhibitory Effects of Distigmine on Recombinant Human Acetylcholinesterase Activity

Obara Keisuke,Chino Daisuke,Tanaka Yoshio
Ｂｉｏｌｏｇｉｃａｌ　＆　Ｐｈａｒｍａｃｅｕｔｉｃａｌ　Ｂｕｌｌｅｔｉｎ 40(10), 1739-1746, 2017
… Cholinesterase (ChE) inhibitors, distigmine, pyridostigmine, neostigmine, and ambenonium, were tested. … Within 2–4 h after removing pyridostigmine, neostigmine, or ambenonium, the rhAChE activity was restored to the control levels. … values for pyridostigmine, neostigmine, and ambenonium were calculated to be 0.51±0.05, 0.66±0.03, and 1.41±0.08 h−1, and the t1/2 …
NAID 130006110566

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リンク元	「ピリドスチグミン」
関連記事	「bromide」「pyridostigmine」「bromides」

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Pyridostigmine
Clinical data
Trade names	Mestinon, others
AHFS/Drugs.com	Monograph
MedlinePlus	a682229
Pregnancy; category	AU: C ; US: C (Risk not ruled out) ; ;
Routes of; administration	by mouth, intravenous
ATC code	N07AA02 (WHO) ;
Legal status
Legal status	UK: POM (Prescription only) ; US: ℞-only ;
Pharmacokinetic data
Bioavailability	7.6 +/- 2.4%
Elimination half-life	1.78 +/- 0.24hrs
Excretion	kidney
Identifiers
	IUPAC name 3-[(dimethylcarbamoyl)oxy]-1-methylpyridinium;
CAS Number	155-97-5 ;
PubChem CID	4991;
DrugBank	DB00545 ;
ChemSpider	4817 ;
UNII	19QM69HH21;
KEGG	D00487 ;
ChEMBL	ChEMBL1115 ;
CompTox Dashboard (EPA)	DTXSID20165786 ;
Chemical and physical data
Formula	C9H13N2O2
Molar mass	181.212 g/mol g·mol−1
3D model (JSmol)	Interactive image;
	SMILES O=C(Oc1ccc[n+](c1)C)N(C)C;
	InChI InChI=1S/C9H13N2O2/c1-10(2)9(12)13-8-5-4-6-11(3)7-8/h4-7H,1-3H3/q+1 ; Key:RVOLLAQWKVFTGE-UHFFFAOYSA-N ;
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