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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2016/01/30 21:00:31」(JST)

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Trimetaphan camsilate (INN) or trimethaphan camsylate (USAN), trade name Arfonad, is a drug that counteracts cholinergic transmission at the ganglion type of nicotinic receptors of the autonomic ganglia and therefore blocks both the sympathetic nervous system and the parasympathetic nervous system. It acts as a non-depolarizing competitive antagonist at the nicotinic acetylcholine receptor, is short-acting, and is given intravenously.

Effects

Trimetaphan is a sulfonium compound and therefore carries a positive charge. Being charged, it cannot cross lipid cell membranes, such as those that comprise the blood–brain barrier. Due to this, trimethaphan does not have any effect on the central nervous system.

The ciliary muscle of the eye functions to round the lens for accommodation and is controlled mainly by parasympathetic system input. With administration of a ganglion-blocking drug, the ciliary muscle cannot contract (cycloplegia) and the patient loses the ability to focus their eyes.

Trimetaphan has a strong effect on the cardiovascular system. The size of blood vessels is primarily controlled by the sympathetic nervous system. Loss of sympathetic system input to the blood vessels causes them to get larger (vasodilation) which has the effect of lowering blood pressure. Postural hypotension is a common side effect of such drugs. Trimethaphan causes a histamine release which further lowers blood pressure. Effects on the heart include a decreased force of contraction and an increase in heart rate (tachycardia). Reflexive tachycardia can be diminished or undetected because trimetaphan is also blocking the sympathetic ganglia innervating the heart.

The motility of the gastrointestinal tract is regulated by the parasympathetic system, and blockage of this input results in diminished motility and constipation.

Therapeutic uses

The therapeutic uses of trimetaphan are very limited due to the competition from newer drugs that are more selective in their actions and effects produced. It is occasionally used to treat a hypertensive crisis and dissecting aortic aneurysm, to treat pulmonary edema, and to reduce bleeding during neurosurgery

English Journal

Multiple system atrophy: Using clinical pharmacology to reveal pathophysiology.

Jordan J1, Shibao C, Biaggioni I.
Clinical autonomic research : official journal of the Clinical Autonomic Research Society.Clin Auton Res.2015 Feb;25(1):53-9. doi: 10.1007/s10286-015-0271-4. Epub 2015 Mar 11.
Despite similarities in their clinical presentation, patients with multiple system atrophy (MSA) have residual sympathetic tone and intact post-ganglionic noradrenergic fibers, whereas patients with pure autonomic failure (PAF) and Parkinson disease have efferent post-ganglionic autonomic denervatio
PMID 25757803

Preserved functional autonomic phenotype in adult mice overexpressing moderate levels of human alpha-synuclein in oligodendrocytes.

Tank J1, da Costa-Goncalves AC2, Kamer I2, Qadri F2, Ubhi K3, Rockenstein E3, Diedrich A4, Masliah E3, Gross V2, Jordan J1.
Physiological reports.Physiol Rep.2014 Nov 26;2(11). pii: e12209. doi: 10.14814/phy2.12209. Print 2014 Nov 1.
Mice overexpressing human alpha-synuclein in oligodendrocytes (MBP1-α-syn) recapitulate some key functional and neuropathological features of multiple system atrophy (MSA). Whether or not these mice develop severe autonomic failure, which is a key feature of human MSA, remains unknown. We explored
PMID 25428949

Autonomic blockade improves insulin sensitivity in obese subjects.

Gamboa A1, Okamoto LE1, Arnold AC1, Figueroa RA1, Diedrich A1, Raj SR1, Paranjape SY1, Farley G1, Abumrad N1, Biaggioni I2.
Hypertension.Hypertension.2014 Oct;64(4):867-74. doi: 10.1161/HYPERTENSIONAHA.114.03738. Epub 2014 Jul 7.
Obesity is an important risk factor for the development of insulin resistance. Initial compensatory mechanisms include an increase in insulin levels, which are thought to induce sympathetic activation in an attempt to restore energy balance. We have previously shown, however, that sympathetic activi
PMID 25001269

Japanese Journal

Intraoperative Hemodynamic Measurements of the Vertebral Artery and Common Carotid Artery

OKADA Yoshikazu,SHIMA Takeshi,NISHIDA Masahiro,YAMANE Kanji,NAKAGAWA Itsuo,HORI Tomokatsu
Neurologia medico-chirurgica 44(10), 509-515, 2004-10-15
… The effects of changes in the systemic arterial blood pressure (SABP) induced by trimethaphan, phenylephrine, and cervical epidural anesthesia were also investigated. …
NAID 110002283504

ニトロプルシドートリメタファン合剤による低血圧麻酔の血行動態と臓器血流に及ぼす影響:―配合比の検討―

中溝玲恵,武田昭平
昭和医学会雑誌 60(5), 610-617, 2000
雑種成犬21頭を対象として0.87%ハロタン・酸素の麻酔下に3種類の配合比のニトロプルシド (SNP) -トリメタファン (TMP) 合剤による低血圧麻酔 (平均動脈圧60mmHg, 60分間) を施行し, 血行動態, 水素クリアランス法により臓器血流 (腎臓, 肝臓, 膵臓) と筋肉血流に及ぼす影響を比較検討した.SNPの平均投与量は1: 1, 1: 2.5, 1: 5の3種類の配合比で各々6. …
NAID 130001823281

Comparison of prostaglandin E1 and trimethaphan as hypotensive drug under acute isovolemic hemodilution in isoflurane anesthetized dogs

KOBORI M.
J Jpn Soc Auto Blood Trans 11, 313-319, 1998
NAID 50004546499

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「trimetaphan camsilate」

Trimetaphan camsilate
Systematic (IUPAC) name
	3,5-dibenzyl-4-oxo-8λ4-thia-3,5-diazatricyclo[6.3.0.02,6]undecan-8-ylium (7,7-dimethyl-2-oxobicyclo[2.2.1]heptan-1-yl)methanesulfonate
Clinical data
Pregnancy; category	US: D (Evidence of risk); ;
Routes of; administration	Oral, IM, IV
Pharmacokinetic data
Excretion	Renal, mostly unchanged
Identifiers
CAS Number	7187-66-8
ATC code	C02BA01
PubChem	CID 23576
DrugBank	DB01116
UNII	8W556014K9
ChEMBL	CHEMBL1245
Chemical data
Formula	C22H25N2OS (free base)
Molar mass	365.513 g/mol (free base)
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