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GUANETHIDINE SULFATE

GUANETHIDINE SULFATE
GUANETHIDINE SULFATE structure
CAS No.
645-43-2
Chemical Name:
GUANETHIDINE SULFATE
Synonyms
uanethidine MonosuL;Guanethidine Sulphae;GUANETHIDINE SULFATE;Guanethidine MonosuL;GUANETHIDINE MONOSULFATE;GUANETHIDINEMONOSULFATE,USP;GUANETHIDINE MONOSULFATE (1:1);GUANETHIDINE SULFATE USP/EP/BP;Guanethidine Monosulfate (200 mg);1-(2-Guanidinoethyl)octahydroazocine
CBNumber:
CB3200665
Molecular Formula:
C10H24N4O4S
Formula Weight:
296.39
MOL File:
645-43-2.mol

GUANETHIDINE SULFATE Properties

Melting point:
276-281 °C
storage temp. 
2-8°C
solubility 
Freely soluble in water, practically insoluble in ethanol (96 per cent)
InChIKey
YUFWAVFNITUSHI-UHFFFAOYSA-N
CAS DataBase Reference
645-43-2(CAS DataBase Reference)
FDA UNII
8AQ60474G9
SAFETY
  • Risk and Safety Statements
Symbol(GHS) 
GHS07
Signal word  Warning
Hazard statements  H302
Precautionary statements  P301+P312+P330
Hazard Codes  Xn
Risk Statements  22
Safety Statements  25-36
RTECS  MF3150000
HS Code  2933999552

GUANETHIDINE SULFATE price More Price(6)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Sigma-Aldrich BP181 Guanethidine monosulfate British Pharmacopoeia (BP) Reference Standard 645-43-2 bp181 $220 2020-08-18 Buy
Sigma-Aldrich BP181 Guanethidine monosulfate British Pharmacopoeia (BP) Reference Standard 645-43-2 $220 2021-03-22 Buy
Sigma-Aldrich 1301801 Guanethidine monosulfate United States Pharmacopeia (USP) Reference Standard 645-43-2 200mg $350 2021-03-22 Buy
Cayman Chemical 16217 Guanethidine (sulfate) ≥95% 645-43-2 100mg $45 2021-03-22 Buy
Cayman Chemical 16217 Guanethidine (sulfate) ≥95% 645-43-2 1g $198 2021-03-22 Buy

GUANETHIDINE SULFATE Chemical Properties,Uses,Production

Chemical Properties

GUANETHIDINE SULFATE is colourless, crystalline powder

Originator

Ismelin,Ciba,US,1960

Uses

Antihypertensive.

Definition

ChEBI: A organic sulfate salt obtained from guanethidine and sulfuric acid in a 1:1 ratio.

Manufacturing Process

13.6 grams of chloroacetyl guanide is added while stirring to a solution of 22.6 grams of heptamethylene imine in 200 ml of benzene. After warming for 1 hour, and then cooling, the solution is filtered and the filtrate concentrated under reduced pressure. The residue, containing the 2-(1-N,N-heptamethylene-imino)-aceticacid guanide, is suspended in tetrahydrofuran and added to a refluxing solution of 6 grams of lithium aluminum hydride in tetrahydrofuran. After completion of the reaction, the excess of lithium aluminum hydride is decomposed by adding water, then aqueous sodium hydroxide. The solid material is filtered off, the filtrate is acidified with sulfuric acid and the 2-(1-N,N-heptamethylene-imino)-ethyl-guanidine sulfate can be recovered and recrystallized from aqueous ethanol, MP 276° to 281°C (with decomposition).

brand name

Ismelin (Novartis).

Therapeutic Function

Antihypertensive

General Description

Guanethidinemonosulfate, [2-(hexahydro-1 (2H)-azocinyl)ethyl]guanidinesulfate (Ismelin sulfate), is a white, crystalline materialthat is very soluble in water. It was one of a series ofguanidine compounds prepared in the search for potent antitrypanosomalagents. There is an absence of CNS effects,such as depression, because the drug is highly polar anddoes not easily cross the blood-brain barrier. Guanethidinemonosulfate produces a gradual, prolonged fall in bloodpressure. Usually, 2 to 7 days of therapy are required beforethe peak effect is reached, and usually, this peak effectis maintained for 3 or 4 days. Then, if the drug is discontinued,the blood pressure returns to pretreatment levelsover a period of 1 to 3 weeks. Because of this slow onsetand prolonged duration of action, only a single daily doseis needed.

Mechanism of action

Guanethidine is an adrenergic neuronal blocking agent that produces a selective block of peripheral sympathetic pathways by replacing and depleting norepinephrine stores from adrenergic nerve endings, but not from the adrenal medulla. It prevents the release of norepinephrine from adrenergic nerve endings in response to sympathetic nerve stimulation. The chronic administration of guanethidine results in an increased sensitivity of these effector cells to catecholamines. Following the oral administration of usual doses of guanethidine, depletion of the catecholamine stores from adrenergic nerve endings occurs at a very slow rate, producing a more gradual and prolonged fall in systolic blood pressure than in diastolic pressure. Associated with the decrease in blood pressure is an increase in sodium and water retention and expansion of plasma volume (edema). If a diuretic is not administered concurrently with guanethidine, tolerance to the antihypertensive effect of the guanethidine during prolonged therapy can result.

Pharmacokinetics

Guanethidine is incompletely absorbed from the GI tract and is metabolized in the liver to several metabolites, including guanethidine N-oxide (from flavin mononucleotide). These metabolites of guanethidine are excreted in the urine and have less than 10% of its hypotensive activity. The amount of drug that reaches the systemic circulation after oral administration is highly variable from patient to patient and may range from 3 to 50% of a dose. Guanethidine accumulates in the neurons with an elimination half-life of 5 days.

Clinical Use

Guanethidine monosulfate is metabolized by microsomalenzymes to 2-(6-carboxyhexylamino)ethylguanidine andguanethidine N-oxide . Both metabolites havevery weak antihypertensive properties. Guanethidine monosulfateis taken up by the amine pump located on theneuronal membrane and retained in the nerve, displacingnorepinephrine from its storage sites in the neuronal granules.The displaced norepinephrine is metabolized to homovanillicacid by mitochondrial MAO, depleting the nerveending of the neurotransmitter. The usefulness of guanethidinemonosulfate also resides in the fact that once it is takenup by the nerve, it produces a sympathetic blockade by inhibitingrelease of nonepinephrine that would occur on neuronalmembrane response to stimulation29 by the nerveaction potential. Guanethidine monosulfate stored in thegranules is released by the nerve action potential but hasvery low intrinsic activity for the adrenergic receptors on thepostjunctional membrane. Moderate doses for a prolongedperiod or large doses may produce undesirable side effectsby causing neuromuscular blockade and adrenergic nerveconduction blockade.

Side effects

Adverse effects of guanethidine frequently are dose related, including dizziness, weakness, lassitude, and syncope resulting from postural or postexercise hypotension. A hot environment (i.e., a hot bath) may aggravate postural hypotension. Patients should be warned about possible orthostatic hypotension and about the effect of rapid postural changes on blood pressure (e.g., arising in the morning) that may cause fainting, especially during the initial period of dosage adjustment. Sodium retention (edema) usually is controlled by the coadministration of a diuretic.

Drug interactions

Diuretics and other hypotensive drugs can potentiate the hypotensive effects of guanethidine. Reportedly, MAO inhibitors antagonize the hypotensive effect of guanethidine. Oral sympathomimetic, nasal decongestants, and other vasopressor agents should be used cautiously in patients receiving guanethidine, because guanethidine may potentiate their pressor effects. The mydriatic response to ophthalmic administration of phenylephrine is markedly increased in patients receiving guanethidine either ophthalmically or orally.
Tricyclic antidepressants and some phenothiazines block the uptake of guanethidine into adrenergic neurons and, thus, prevent the hypotensive activity of guanethidine. Orthostatic hypotension may be increased by concomitant administration of alcohol with guanethidine, and patients receiving guanethidine should be cautioned to limit alcohol intake.

GUANETHIDINE SULFATE Preparation Products And Raw materials

Raw materials

Preparation Products


GUANETHIDINE SULFATE Suppliers

Global( 97)Suppliers
Supplier Tel Fax Email Country ProdList Advantage
career henan chemical co
+86-371-86658258
sales@coreychem.com CHINA 29960 58
Hebei Guanlang Biotechnology Co., Ltd.
+8619930503282
sales3@crovellbio.com China 5460 58
Chongqing Chemdad Co.,Ltd
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BOC Sciences
1-631-485-4226
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Chongqing Chemdad Co., Ltd
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HENAN BON INDUSTRIAL CO.,LTD
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Shaanxi Dideu Medichem Co. Ltd
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SHANGHAI T&W PHARMACEUTICAL CO., LTD.
86-021-61999440
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Target Molecule Corp
18019718960 781-999-5354
marketing@targetmol.com United States 19232 58
Hefei TNJ Chemical Industry Co.,Ltd.
0551-65418671
0551-65418697 sales@tnjchem.com CHINA 37441 58

View Lastest Price from GUANETHIDINE SULFATE manufacturers

Image Release date Product Price Min. Order Purity Supply Ability Manufacturer
2021-08-12 GUANETHIDINE SULFATE
645-43-2
US $9.90 / KG 1KG 99% 10 mt Hebei Guanlang Biotechnology Co., Ltd.
2021-08-11 GUANETHIDINE SULFATE USP/EP/BP
645-43-2
US $1.10 / g 1g 99.9% 100 Tons min Dideu Industries Group Limited
2021-07-02 guanethidine monosulfate
645-43-2
US $15.00-10.00 / KG 1KG 99%+ HPLC Monthly supply of 1 ton Zhuozhou Wenxi import and Export Co., Ltd

GUANETHIDINE SULFATE Spectrum


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