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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2017/08/26 08:31:58」(JST)

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Guanethidine is an antihypertensive drug that reduces the release of catecholamines, such as norepinephrine. Guanethidine is transported across the sympathetic nerve membrane by the same mechanism that transports norepinephrine itself (NET, uptake 1), and uptake is essential for the drug's action. Once guanethidine has entered the nerve, it is concentrated in transmitter vesicles, where it replaces norepinephrine. It may also inhibit the release of granules by decreasing norepinephrine.

Side effects

Side effects include orthostatic and exercise hypotension, sexual dysfunction (delayed or retrograde ejaculation), and diarrhea.

Pharmacology

Guanethidine is transported by uptake 1 into the presynaptic terminal transported by norepinephrine transporter (NET). (In this it competes with norepinephrine so can potentiate exogenously applied norepinephrine.) It becomes concentrated in norepinephrine transmitter vesicles, replacing norepinephrine in these vesicles. This leads to a gradual depletion of norepinephrine stores in the nerve endings. Once inside the terminal it blocks the release of norepinephrine in response to arrival of an action potential. Spontaneous release is not affected.

Uses

Guanethidine was once a mainstay for hypertension resistant to other agents, and was often used safely during pregnancy, but it is no longer used in the US due to lack of availability. It is still licensed in some countries, e.g., UK, for the rapid control of blood pressure in a hypertensive emergency.

Intravenous nerve block (Bier block) using guanethidine has been used to treat chronic pain caused by complex regional pain syndrome.^[1]

References

^ Joyce PI, Rizzi D, Caló G, Rowbotham DJ, Lambert DG (November 2002). "The effect of guanethidine and local anesthetics on the electrically stimulated mouse vas deferens". Anesth. Analg. 95 (5): 1339–43, table of contents. PMID 12401623. doi:10.1097/00000539-200211000-00045.

UpToDate Contents

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1. 成人における複合性局所疼痛症候群の予防およびマネージメント prevention and management of complex regional pain syndrome in adults
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English Journal

Characterization of the role of endogenous nitric oxide in myogenic vascular oscillations during cooling-evoked hemodynamic perturbations of rats.

Lin YH1,2, Liu YP3, Lin YC1, Lee PL4, Tung CS1.
Canadian journal of physiology and pharmacology.Can J Physiol Pharmacol.2017 Jul;95(7):803-810. doi: 10.1139/cjpp-2016-0476. Epub 2017 Mar 9.
PMID 28278384

Physiological approaches to assess diminished sympathetic activity in the conscious rat.

Zahner MR1, Liu CN2, Bernardo V2, Northcott C2, Tyszkiewicz C2, Okerberg C2, Boucher M2, Pardo I2, Somps CJ2.
Journal of pharmacological and toxicological methods.J Pharmacol Toxicol Methods.2017 Jun 25. pii: S1056-8719(17)30013-8. doi: 10.1016/j.vascn.2017.06.002. [Epub ahead of print]
PMID 28658603

Local chemical sympathectomy of rat bone marrow and its effect on marrow cell composition.

Dubový P1, Klusáková I2, Kučera L3, Osičková J4, Chovancová J4, Loja T4, Mayer J4, Doubek M4, Joukal M2.
Autonomic neuroscience : basic & clinical.Auton Neurosci.2017 Jun 23. pii: S1566-0702(16)30259-4. doi: 10.1016/j.autneu.2017.06.003. [Epub ahead of print]
PMID 28688831

Japanese Journal

Adrenergic Stimulation-Released Histamine Taken-up in Adrenergic Nerves Induces Endothelium-Dependent Vasodilation in Rat Mesenteric Resistance Arteries

Haruki Yuto,Takatori Shingo,Hattori Sayo [他],ZAMAMI Yoshito,KOYAMA Toshihiro,TANGSUCHARIT Panot,KAWASAKI Hiromu
Journal of pharmacological sciences 118(4), 537-542, 2012-04-20
… Chlorpheniramine, guanethidine, combination of histamine and desipramine, and endothelium-removal abolished PNS-induced vasodilation in histamine-treated preparations. …
NAID 10030572277

Endothelium-Derived Relaxing Factor-Mediated Vasodilation in Mouse Mesenteric Vascular Beds

Fujiwara Hiroki,Wake Yoshihiro,Hashikawa-Hobara Narumi [他],MAKINO Kento,TAKATORI Shingo,ZAMAMI Yoshito,KITAMURA Yoshihisa,KAWASAKI Hiromu
Journal of pharmacological sciences 118(3), 373-381, 2012-03-20
… In preparations with active tone produced by methoxamine in the presence of guanethidine, injections of acetylcholine, A23187, and sodium nitroprusside (SNP) caused a concentration-dependent decrease in perfusion pressure due to vasodilation. …
NAID 10030455705

Neurogenic Vascular Responses in Male Mouse Mesenteric Vascular Beds

Fujiwara Hiroki,Hashikawa-Hobara Narumi,Wake Yoshihiro [他],Takatori Shingo,Goda Mitsuhiro,Higuchi Hiroshi,Zamami Yoshito,Tangsucharit Panot,Kawasaki Hiromu
Journal of Pharmacological Sciences 119(3), 260-270, 2012
… PNS-induced vasoconstriction was abolished by tetrodotoxin (neurotoxin) and guanethidine (adrenergic neuron blocker) and blunted by prazosin (<I>α</I><SUB>1</SUB>-adrenoceptor antagonist). …
NAID 130001889286

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リンク元

「グアネチジン」

Guanethidine
Clinical data
AHFS/Drugs.com	Micromedex Detailed Consumer Information
MedlinePlus	a600027
ATC code	C02CC02 (WHO) S01EX01 (WHO);
Pharmacokinetic data
Biological half-life	1.5 days
Identifiers
	IUPAC name 2-[2-(azocan-1-yl)ethyl]guanidine;
CAS Number	645-43-2 ;
PubChem CID	3518;
IUPHAR/BPS	7194;
DrugBank	DB01170 ;
ChemSpider	3398 ;
UNII	5UBY8Y002G;
KEGG	D08030 ;
ChEBI	CHEBI:5557 ;
ChEMBL	CHEMBL765 ;
ECHA InfoCard	100.010.403
Chemical and physical data
Formula	C10H22N4
Molar mass	198.309 g/mol
3D model (JSmol)	Interactive image;
	SMILES N(=C(\N)N)\CCN1CCCCCCC1 ;
	InChI InChI=1S/C10H22N4/c11-10(12)13-6-9-14-7-4-2-1-3-5-8-14/h1-9H2,(H4,11,12,13) ; Key:ACGDKVXYNVEAGU-UHFFFAOYSA-N ;
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英: guanethidine
化: 硫酸グアネチジン guanethidine sulfate
商: イスメリン Ismelin
関: 降圧薬

[pmid12401623-1] Joyce PI, Rizzi D, Caló G, Rowbotham DJ, Lambert DG (November 2002). "The effect of guanethidine and local anesthetics on the electrically stimulated mouse vas deferens". Anesth. Analg. 95 (5): 1339–43, table of contents. PMID 12401623. doi:10.1097/00000539-200211000-00045.

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guanethidine