pancuronium

パンクロニウム

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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2014/07/17 03:28:30」(JST)

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Pancuronium

Systematic (IUPAC) name
[(2S,3S,5S,8R,9S,10S,13S,14S,16S,17R)- 17-acetyloxy-10,13-dimethyl-2,16-bis(1-methyl- 3,4,5,6-tetrahydro-2H-pyridin-1-yl)-2,3,4,5,6,7, 8,9,11,12,14,15,16,17-tetradecahydro-1H- cyclopenta[a]phenanthren-3-yl] acetate
Clinical data
AHFS/Drugs.com	monograph
Pregnancy cat.	B2 (AU) C (US)
Legal status	Prescription Only (S4) (AU) POM (UK) ℞-only (US)
Routes	Intravenous
Pharmacokinetic data
Bioavailability	NA
Protein binding	77 to 91%
Metabolism	Hepatic
Half-life	1.5 to 2.7 hours
Excretion	Renal and biliary
Identifiers
CAS number	16974-53-1 Y 15500-66-0 (bromide)
ATC code	M03AC01
PubChem	CID 441289
IUPHAR ligand	4001
DrugBank	DB01337
ChemSpider	25453 N
UNII	U9LY9Y75X2 N
KEGG	D00492 Y
ChEBI	CHEBI:7908 N
ChEMBL	CHEMBL185073 N
Chemical data
Formula	C35H60N2O4
Mol. mass	572.861 g/mol
InChI InChI=1S/C35H60N2O4.2BrH/c1-24(38)40-32-21-26-13-14-27-28(35(26,4)23-31(32)37(6)19-11-8-12-20-37)15-16-34(3)29(27)22-30(33(34)41-25(2)39)36(5)17-9-7-10-18-36;;/h26-33H,7-23H2,1-6H3;2*1H/q+2;;/p-2/t26-,27+,28-,29-,30-,31-,32-,33-,34-,35-;;/m0../s1 N Key:NPIJXCQZLFKBMV-YTGGZNJNSA-L N
N (what is this?)  (verify)

Pancuronium (trademarked as Pavulon) is a muscle relaxant with various purposes. It is the second of three drugs administered during most lethal injections in the United States.

Mechanism of action

Pancuronium is a typical non-depolarizing curare-mimetic muscle relaxant. It acts as a competitive acetylcholine antagonist on neuromuscular junctions, displacing acetylcholine (hence competitive) from its post-synaptic nicotinic acetylcholine receptors. It is (unlike suxamethonium) a non-depolarizing agent, which means that it causes no spontaneous depolarizations upon association with the nicotinic receptor in neuromuscular junction, thus producing no muscle fasciculations upon administration. Despite being a steroid, pancuronium has no hormonal activity. It exerts slight vagolytic activity (i.e. diminishing activity of the vagus nerve) and no ganglioplegic (i.e. blocking ganglions) activity. Pancuronium is a very potent muscle relaxant/curaremimetic. The ED95 (i.e. the dose that causes 95% depression of muscle twitch response) is only 60 µg/kg body weight administered intravenously. Muscle relaxation suitable for intubation sets in about 90–120 seconds after administration of the drug. Full muscle paralysis for major surgery is achieved about 2–4 minutes after application. Clinical effects (muscle activity lower than 25% of physiological) last for about 100 minutes. The time needed for full (over 90% muscle activity) recovery after single administration is about 120–180 minutes in healthy adults, but can be protracted to more hours in poor health subjects and when concomitantly administered with other long-acting anesthetics (e.g., some opioids, barbiturates, inhalation anesthetics). The effects of pancuronium can be at least partially reversed by anticholinesterasics, such as neostigmine, pyridostigmine, and edrophonium.

Development

Pancuronium is designed to mimic the action of two molecules of acetylcholine with the quaternary nitrogen atoms spaced rigidly apart by the steroid rings at a distance of ten atoms (interonium distance). Decamethonium and suxamethonium also have this same interonium distance.

Uses in medicine

Pancuronium is used with general anaesthesia in surgery for muscle relaxation and as an aid to intubation or ventilation. It does not have sedative or analgesic effects.

Side-effects include moderately raised heart rate and thereby arterial pressure and cardiac output, excessive salivation, apnea and respiratory depression, rashes, flushing, and sweating. The muscular relaxation can be dangerous in the seriously ill and it can accumulate leading to extended weakness. Pancuronium is not preferable in long-term use in ICU-ventilated patients.

In Belgium and the Netherlands, pancuronium is recommended in the protocol for euthanasia. After administering sodium thiopental to induce coma, pancuronium is delivered in order to stop breathing.

In 2007, Dr Michael Munro, a Scottish neonatologist at Aberdeen Maternity Hospital, was cleared of malpractice by the GMC Fitness to Practice panel after giving 23 times the standard dose of pancuronium to two dying neonates. In the final minutes of life, each baby was suffering from agonal gasping and violent body spasms, which was highly distressing for the parents to witness. Dr Munro then administered pancuronium to the babies after advising the parents that this would ease their suffering, but could also hasten death. It is on record that neither of the children's parents was unhappy with Dr Munro's treatment of their babies.

Uses in execution

Procedure

It is also used as one component of a lethal injection in administration of the death penalty in some parts of the United States.

Controversy

Pancuronium bromide has no hypnotic effects, and, if the anaesthetic agent used in lethal injection is ineffective, the individual may never achieve unconsciousness, and thus be able to feel all of the pain associated with the procedure, but unable to cry out or move due to the pancuronium's complete paralytic action. There have also been several high-profile civil lawsuits alleging similar failures to achieve analgesia or unconsciousness prior to general surgical procedures. These, too, have been blamed largely on improper or insufficient dosages of anaesthetic in concert with normal dosages of pancuronium bromide.

Echoing this sentiment, Amnesty International has objected to its use in lethal injections on the grounds that it "may mask the condemned prisoner's suffering during the execution," thereby leading observers to conclude that lethal injection is painless, or less cruel than other forms of execution.

In September 2007, the US Supreme Court agreed to hear their first case of whether or not the use of lethal injection does in fact violate the US Constitution's Eighth Amendment's ban on cruel and unusual punishment. On April 16, 2008, the court upheld the constitutionality of Kentucky's lethal injection practices.

Uses in crime

Pancuronium is the compound that was used in Efren Saldivar's killing spree. It was also used by the Skin Hunters to kill patients in the Polish city of Łódź. Pavulon was also used by Richard Angelo in 1987 to kill at least 10 patients under his care at the Good Samaritan Hospital in New York.

References

External links

• (French) "Pavulon – Information professionnelle [prescribing information]" (PDF). Compendium Suisse des Médicaments. December 12, 2005. Retrieved 2011-01-23. 

UpToDate Contents

全文を閲覧するには購読必要です。 To read the full text you will need to subscribe.

• 1. 重症患者における神経筋遮断剤の使用 use of neuromuscular blocking medications in critically ill patients
• 2. 小児に対する急速挿管法（RSI） rapid sequence intubation rsi in children
• 3. 成人における迅速導入気管挿管のための神経筋遮断剤（NMBA） neuromuscular blocking agents nmba for rapid sequence intubation in adults
• 4. 周術期アナフィラキシー：再発反応の評価および予防 perioperative anaphylaxis evaluation and prevention of recurrent reactions
• 5. 術後肺合併症を減少させるための戦略 strategies to reduce postoperative pulmonary complications

English Journal

• Variability in the Muscle Composition of Rat Esophagus and Neural Pathway of Lower Esophageal Sphincter Relaxation.

• Jiang Y, Bhargava V, Lal HA, Mittal RK.Source1University of California San Diego.
• American journal of physiology. Gastrointestinal and liver physiology.Am J Physiol Gastrointest Liver Physiol.2011 Sep 1. [Epub ahead of print]
• Introduction and Aims: Several studies from our laboratory show that axial stretch of the lower esophageal sphincter (LES) in an oral direction causes neurally mediated LES relaxation. Under physiological conditions, axial stretch of the LES is caused by longitudinal muscle contraction (LMC) of the
• PMID 21885684

• Intact internal dynamics of the neocortex in acutely paralyzed mice.

• Minamisawa G, Funayama K, Matsuki N, Ikegaya Y.SourceLaboratory of Chemical Pharmacology, Graduate School of Pharmaceutical Sciences, The University of Tokyo, Japan.
• The journal of physiological sciences : JPS.J Physiol Sci.2011 Jul;61(4):343-8. doi: 10.1007/s12576-011-0155-x. Epub 2011 Jun 3.
• Animals collect sensory information through self-generated movements. Muscle movements drive active feedback of sensory information and determine large parts of the sensory inputs the animal receives; however, little is known about how this active feedback process modulates the ongoing dynamics of t
• PMID 21633910

Japanese Journal

• 家兎摘出灌流肺におけるベクロニウムおよびパンクロニウムの肺循環への影響

• 舩木 一美
• 米子医学雑誌 62(1), 21-30, 2011-01
• NAID 40018707632

• Flow Injection Potentiometric Determination of Pancuronium Bromide in Pharmaceutical Preparation and Urine Samples Using Modified Carbon Paste Electrodes

• Zayed Sayed Imam Mohamed
• Chemical and Pharmaceutical Bulletin 59(2), 254-259, 2011
• … Carbon paste electrodes for pancuronium bromide was prepared based on ion association complexes of pancuronium bromide with sodium tetraphenylborate (NaTPB) or ammonium reineckate using dibutyl phthalate as solvent mediator and tetradodecylammonium tetrakis-(4-chlorophenyl)borate (ETH 500) as lipophilic additive. …
• NAID 130000405524

• Presynaptic M1, M2, and A1 receptors play roles in tetanic fade induced by pancuronium or cisatracurium

• BORNIA ELAINE CAMPANA SANCHES,BANDO ERIKA,MACHINSKI MIGUEL Jr,PEREIRA MONALISA WOLSKI,ALVES-DO-PRADO WILSON
• Journal of anesthesia 23(4), 513-519, 2009-11-20
• NAID 10027264734

Related Links

• Pancuronium, What isPancuronium? About its Science ...

Find out about the science and chemistry of Pancuronium (Pavulon, Lethal injection, Euthanasia), see colourful images of Pancuronium and explore interactive 3D molecules of Pancuronium ... Pancuronium is used with general ...

• Pancuronium - Scribd

Pancuronium - Read online for free.

Related Pictures

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★リンクテーブル★

リンク元	「薬理学」「パンクロニウム」
拡張検索	「pancuronium bromide」

「薬理学」

　　[★]

英

pharmacology

関

drug entries

定義

• 生物系と化学物質の選択的な相互作用を研究する学問 (SPC.2)

生物系と薬の相互作用

• 薬の生物系に対する相互作用：薬理作用 <-化学の視点
• 生物系の薬に対する相互作用：薬物動態 <-生物の視点

関連分野

• 薬物学 materia medica
• 生薬学
• 実験薬理学
• 臨床薬理学
• 動物薬理学
• 人体薬理学
• 比較薬理学
• 薬理作用学(薬力学)
• 薬物動態学
• 中毒学、毒科学
• 薬物治療学
• 処方学

薬品の命名

Ending of the drug name	Category	Example
～afil	Erectile dysfunction	sildenafil
～ane	Inhalatinal general anesthetic	halothane
～azepam	Benzodiaizepine	diazepam
～azine	Phenothiazine (neuroleptic, antiemetic)	chlorpromazine
～azole	Ailtifungal	ketoconazole
～barbital	Barbiturate	phenobarbital
～caine	Local anesthetic	lidocaine
～cillin	Penicillin	methicillin
～cycline	Antibiotic, protein syntlesis inhibitor	tetracycline
～ipramine	TCA	iimipramine
～navir	Protease inhibitor	saquinavir
～olol	β-antagonist	propranolol
～operidol	Butyrophenone ( neuroleptic )	haloperidol
～oxin	Cardiac glycoside ( inotropic agent )	digoxin
～phylline	Methylxanthine	theophylline
～pril	ACE inhibitor	captopril
～terol	β2 agonist	albuterol
～tidine	H2 antagonist	cimtidine
～triptyline	TCA	amitriptyline
～tropine	Pituitary hormone	somatotropine
～zosin	a1 antagonist	prazosin

薬一覧

神経筋接合部遮断薬(筋弛緩薬)

• 非脱分極性筋弛緩薬 競合的筋弛緩薬

• ベクロニウム vecuronium
• パンクロニウム pancuronium
• アトラクリウム atracurium
• d-ツボクラリン tubocurarine

• 脱分極性筋弛緩薬

• スキサメトニウム suxamethonium
• デカメトニウム decamethonium

交感神経作動薬

→アドレナリン受容体

交感神経遮断薬

→アドレナリン受容体

副交感神経作動薬

→アセチルコリン受容体

副交感神経遮断薬

→アセチルコリン受容体

甲状腺関連物質

• 甲状腺ホルモン製剤

• レボチロキシン levothyroxine
• リオチニシン liothyronine

• 抗甲状腺薬

• プロピルチオウラシル propylthiouracil
• チアマゾール thiamazole

痛風治療薬

• 痛風発作予防薬

• コルヒチン colchicine

• 尿酸排泄促進薬

• ベンズブロマロン benzbromarone
• プロベネシド probenecid

• 尿酸生成抑制薬

• アロプリノール allopurinol

「パンクロニウム」

　　[★]

英

pancuronium

化

臭化パンクロニウム パンクロニウム臭化物 pancuronium bromide

商

Pavulon、ミオブロック

「pancuronium bromide」

　　[★]

• 臭化パンクロニウム

関

pancuronium