Guanethidine

Các tên gọi khác (10 ) :

(2-(Octahydro-1-azocinyl)ethyl)guanidine
2-(1-N,N-Heptamethyleneimino)ethylguanidine
2-(1'-Azacyclooctyl)ethylguanidine
Azocine, 1-(2-guanidinoethyl)octahydro-
Guanethidine
Guanethidinum
Guanetidina
Guanidine, (2-(hexahydro-1(2H)-azocinyl)ethyl)-
Heptamethylenimine, 1-(2-guanidinoethyl)-
N-(2-Perhydroazocin-1-ylethyl)guanidine

antihypertensive agents, adrenergic agents, sympatholytics

Thuốc Gốc

Small Molecule

CAS: 645-43-2

ATC: C02CC02, S01EX01

ĐG : Novartis AG , http://www.novartis.com

CTHH: C₁₀H₂₂N₄

PTK: 198.3085

An antihypertensive agent that acts by inhibiting selectively transmission in post-ganglionic adrenergic nerves. It is believed to act mainly by preventing the release of norepinephrine at nerve endings and causes depletion of norepinephrine in peripheral sympathetic nerve terminals as well as in tissues. [PubChem]

Nhận Dạng Quốc Tế & Đặc Tính Hóa Học

Công thức hóa học

C₁₀H₂₂N₄

Phân tử khối

198.3085

Monoisotopic mass

198.184446724

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)

InChI Key

InChIKey=ACGDKVXYNVEAGU-UHFFFAOYSA-N

IUPAC Name

2-[2-(azocan-1-yl)ethyl]guanidine

Traditional IUPAC Name

guanethidine

SMILES

NC(N)=NCCN1CCCCCCC1

Độ tan chảy

276-281

Độ hòa tan

Very soluble

logP

0.8

logS

-1.9

pKa (Strongest Basic)

11.77

PSA

67.64 Å²

Refractivity

59.7 m³·mol^-1

Polarizability

23.67 Å³

Rotatable Bond Count

H Bond Acceptor Count

H Bond Donor Count

Physiological Charge

Number of Rings

Bioavailability

Rule of Five

true

Ghose Filter

true

Dược Lực Học : High blood pressure can cause the heart and arteries to not function properly. This can damage the blood vessels of the brain, heart, and kidneys, resulting in a stroke, heart failure, or kidney failure. High blood pressure may also increase the risk of heart attacks. These problems may be less likely to occur if blood pressure is controlled. Guanethidine works by decreasing the heart rate and relaxing the blood vessels so that blood can flow more easily through the body, thereby reducing these risks. It is a postganglionic sympathetic nerve terminal blocker that prevents the release of norepinephrine from nerve terminals.

Cơ Chế Tác Dụng : An antihypertensive agent that acts by inhibiting selectively transmission in post-ganglionic adrenergic nerves. It is believed to act mainly by preventing the release of norepinephrine at nerve endings and causes depletion of norepinephrine in peripheral sympathetic nerve terminals as well as in tissues. [PubChem] Guanethidine acts at the sympathetic neuroeffector junction by inhibiting or interfering with the release and/or distribution of norepinephrine, rather than acting at the effector cell by inhibiting the association of norepinephrine with its receptors. It is taken up by norepinephrine transporters. It becomes concentrated in NE transmitter vesicles, replacing NE in these vesicles. This leads to a gradual depletion of NE stores in the nerve endings. Once inside the terminal it blocks the release of noradrenaline in response to arrival of an action potential. In contrast to ganglionic blocking agents, Guanethidine suppresses equally the responses mediated by alpha-and beta-adrenergic receptors but does not produce parasympathetic blockade. Since sympathetic blockade results in modest decreases in peripheral resistance and cardiac output, Guanethidine lowers blood pressure in the supine position. It further reduces blood pressure by decreasing the degree of vasoconstriction that normally results from reflex sympathetic nervous activity upon assumption of the upright posture, thus reducing venous return and cardiac output more.

Dược Động Học :

▧ Absorption :
3-30% of oral dose (poor and highly variable)
▧ Metabolism :
Guanethidine is converted by the liver to three metabolites, which are excreted in the urine. The metabolites are pharmacologically less active than the parent compound.
▧ Route of Elimination :
Ismelin is converted by the liver to three metabolites, which are excreted in the urine.
▧ Half Life :
1.5 days
▧ Clearance :
* Renal cl=56 ml/min

Độc Tính : Side effects include drowsiness, dizziness, tiredness or confusion. LD₅₀=1000 mg/kg (mouse, oral)

Chỉ Định : For the treatment of moderate and severe hypertension, either alone or as an adjunct, and for the treatment of renal hypertension.

Tương Tác Thuốc :

Acetophenazine Acetophenazine may decrease the effect of guanethidine.
Alimemazine Trimeprazine may decrease the effect of guanethidine.
Amitriptyline The tricyclic antidepressant, amitriptyline, decreases the effect of guanethidine.
Amoxapine The tricyclic antidepressant, amoxapine, decreases the effect of guanethidine.
Amphetamine Amphetamine may decrease the effect of guanethidine.
Benzphetamine Benzphetamine may decrease the effect of guanethidine.
Chlorpromazine Chlorpromazine may decrease the effect of guanethidine.
Chlorprothixene Chlorprothixene may decrease the effect of guanethidine.
Clomipramine The tricyclic antidepressant, clomipramine, decreases the effect of guanethidine.
Desipramine The tricyclic antidepressant, desipramine, decreases the effect of guanethidine.
Dexfenfluramine Dexfenfluramine may decrease the effect of guanethidine.
Dextroamphetamine Dextroamphetamine may decrease the effect of guanethidine.
Diethylpropion Diethylpropion may decrease the effect of guanethidine.
Dobutamine Dobutamine may decrease the effect of guanethidine.
Dopamine Dopamine may decrease the effect of guanethidine.
Doxepin The tricyclic antidepressant, doxepin, decreases the effect of guanethidine.
Ephedra Ephedra may decrease the effect of guanethidine.
Ephedrine Ephedrine may decrease the effect of guanethidine.
Epinephrine Epinephrine may decrease the effect of guanethidine.
Ethopropazine Ethopropazine may decrease the effect of guanethidine.
Fenfluramine Fenfluramine may decrease the effect of guanethidine.
Fluphenazine Fluphenazine may decrease the effect of guanethidine.
Haloperidol Haloperidol may decrease the effect of guanethidine.
Imipramine The tricyclic antidepressant, imipramine, may increase the sympathomimetic effect of guanethidine.
Isocarboxazid Isocarboxazid may decrease the effect of guanethidine.
Mazindol Mazindol may decrease the effect of guanethidine.
Mesoridazine Mesoridazine may decrease the effect of guanethidine.
Metaraminol Metaraminol may decrease the effect of guanethidine.
Methamphetamine Methamphetamine may decrease the effect of guanethidine.
Methdilazine Methdilazine may decrease the effect of guanethidine.
Methotrimeprazine Methotrimeprazine may decrease the effect of guanethidine.
Methoxamine Methoxamine may decrease the effect of guanethidine.
Methylphenidate Methylphenidate may decrease the effect of guanethidine.
Norepinephrine Norepinephrine may decrease the effect of guanethidine.
Nortriptyline The tricyclic antidepressant, nortriptyline, decreases the effect of guanethidine.
Pargyline Pargyline may decrease the effect of guanethidine.
Perphenazine Perphenazine may decrease the effect of guanethidine.
Phendimetrazine Phendimetrazine may decrease the effect of guanethidine.
Phenelzine Phenelzine may decrease the effect of guanethidine.
Phenmetrazine Phenmetrazine may decrease the effect of guanethidine.
Phentermine Phentermine may decrease the effect of guanethidine.
Phenylephrine Phenylephrine may decrease the effect of guanethidine.
Phenylpropanolamine Phenylpropanolamine may decrease the effect of guanethidine.
Prochlorperazine Prochlorperazine may decrease the effect of guanethidine.
Promazine Promazine may decrease the effect of guanethidine.
Promethazine Promethazine may decrease the effect of guanethidine.
Propericiazine Propericiazine may decrease the effect of guanethidine.
Propiomazine Propiomazine may decrease the effect of guanethidine.
Protriptyline The tricyclic antidepressant, protriptyline, decreases the effect of guanethidine.
Pseudoephedrine Pseudoephedrine may decrease the effect of guanethidine.
Thiethylperazine Thiethylperazine may decrease the effect of guanethidine.
Thioridazine Thioridazine may decrease the effect of guanethidine.
Thiothixene Thiothixene may decrease the effect of guanethidine.
Tranylcypromine Tranylcypromine may decrease the effect of guanethidine.
Trifluoperazine Trifluoperazine may decrease the effect of guanethidine.
Triflupromazine Triflupromazine may decrease the effect of guanethidine.
Trimipramine The tricyclic antidepressant, trimipramine, decreases the effect of guanethidine.

Liều Lượng & Cách Dùng : Tablet - Oral

Dữ Kiện Thương Mại

Giá thị trường

Biệt dược thương mại : Guanethidine monosulf powder

Giá bán buôn : USD >102.0

Đơn vị tính : g

Nhà Sản Xuất

Công ty : Chen Ho

Sản phẩm biệt dược : Ismedine
Công ty : Amdipharm

Sản phẩm biệt dược : Ismelin

Đóng gói

Công ty : Novartis AG

Website : http://www.novartis.com
Công ty : Professional Co.

Tài Liệu Tham Khảo Thêm

drugbank

http://www.drugbank.ca/drugs/DB01170

PubChem Compound

http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=3518

PubChem Substance

http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46507567

KEGG Drug

http://www.genome.jp/dbget-bin/www_bget?drug:D02237

ChemSpider

http://www.chemspider.com/Chemical-Structure.3398.html

National Drug Code Directory

http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0083-0049-30

PharmGKB

http://www.pharmgkb.org/drug/PA449823

Wikipedia

http://en.wikipedia.org/wiki/Guanethidine

RxList

http://www.rxlist.com/cgi/generic3/guanethidine.htm

Drugs.com

http://www.drugs.com/mtm/guanethidine.html

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