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Clonidine hydrochloride

Clonidine hydrochloride structure

CAS No:
4205-91-8
Formula:
C9H9Cl2N3.ClH
Chemical Name:
Clonidine hydrochloride
Synonyms:
1H-Imidazol-2-amine,N-(2,6-dichlorophenyl)-4,5-dihydro-,hydrochloride (1:1);2-Imidazoline,2-(2,6-dichloroanilino)-,monohydrochloride;1H-Imidazol-2-amine,N-(2,6-dichlorophenyl)-4,5-dihydro-,monohydrochloride;Catapressan;Catapres;Clonidine hydrochloride;ST 155;2-[(2,6-Dichlorophenyl)amino]-2-imidazoline monohydrochloride;Haemiton;Chlophazolin;2-[(2,6-Dichlorophenyl)amino]-2-imidazoline hydrochloride;Katapresan;Clonidine chloride;Atensina;Capresin;DCAI;Hemiton;Normopresan;Clonidine monohydrochloride;Clofelin;Isoglaucon;2-(2,6-Dichloroanilino)-2-imidazoline hydrochloride;Neuclon;Clopheline;KAPVAY;Dichloranilino imidazolin;7555-15-9;57665-50-6;64638-22-8;66009-47-0;66073-52-7;73121-65-0
Categories:
Active Pharmaceutical Ingredients > Circulatory System Drugs

Description

Clonidine hydrochloride is an agonist of α2-adrenoceptor and potent antihypertensive agent.

Clonidine hydrochloride is a dichlorobenzene.|Clonidine Hydrochloride is the hydrochloride salt form of clonidine, an imidazoline derivate and centrally-acting alpha-adrenergic agonist as well as antagonist with antihypertensive activity. Clonidine hydrochloride binds to and stimulates central alpha-2 adrenergic receptors, thereby decreasing sympathetic outflow to the heart, kidneys, and peripheral vasculature. The reduction in sympathetic outflow, leads to decreased peripheral vascular resistance, decreased blood pressure, and decreased heart rate.|An imidazoline sympatholytic agent that stimulates ALPHA-2 ADRENERGIC RECEPTORS and central IMIDAZOLINE RECEPTORS. It is commonly used in the management of HYPERTENSION.

Clonidine hydrochloride Basic Attributes

Molecular Weight：

266.55

Exact Mass：

264.994019

EC Number：

224-121-5

UNII：

W76I6XXF06

NSC Number：

756699

DSSTox ID：

DTXSID8044670

NCI Thesaurus Code：

C47979

HScode：

2933290090

Characteristics

PSA：

36.4

Appearance：

white

Melting Point：

305 °C

Boiling Point：

319.3°C at 760 mmHg

Flash Point：

146.9ºC

Water Solubility：

soluble in water (50 mg/ml), DMSO (75 mM), methanol, chloroform (slightly), and dehydrated alcohol.

Storage Conditions：

2-8°C

Toxicity：

Oral-Rat LD50: 126 mg/kg; Oral-Mouse LD50: 139 mg/kg

Flammability characteristics：

Flammable; burning produces toxic chloride and nitrogen oxide fumes

Collision Cross Section：

143.3 Å² [M+H]+ [CCS Type: TW, Method: calibrated with polyalanine and drug standards]

Safety Information

Packing level：

III

Hazard category：

6.1(b)

Transport codes：

UN 2811 6.1/PG 1

wgk germany：

hazard class code：

25-26

safety instructions：

22-26-28-36/37/39-45

RTECS Number：

NJ2490000

Marks：

T+

Storage features：

Storehouse ventilated at low temperature and dry; stored separately from oxidants, alkalis, food additives

Precautionary statement(s)：

Missing Phrase - N15.00950417-P260-P304 + P340 + P310-P403 + P233

Hazard Statements：

H301-H330

GHS Classification：

|Danger|H301 (100%): Toxic if swallowed [Danger Acute toxicity, oral]|P260, P264, P270, P271, P284, P301+P310, P304+P340, P310, P320, P321, P330, P403+P233, P405, and P501|Aggregated GHS information provided by 49 companies from 4 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.

Toxicity

Toxicity class：

highly toxic

Drug Information

Drug Indication：

Sedation

MeSH：

Compounds that bind to and activate ADRENERGIC ALPHA-2 RECEPTORS. (See all compounds classified as Adrenergic alpha-2 Receptor Agonists.)|Drugs that inhibit the actions of the sympathetic nervous system by any mechanism. The most common of these are the ADRENERGIC ANTAGONISTS and drugs that deplete norepinephrine or reduce the release of transmitters from adrenergic postganglionic terminals (see ADRENERGIC AGENTS). Drugs that act in the central nervous system to reduce sympathetic activity (e.g., centrally acting alpha-2 adrenergic agonists, see ADRENERGIC ALPHA-AGONISTS) are included here. (See all compounds classified as Sympatholytics.)|Compounds capable of relieving pain without the loss of CONSCIOUSNESS. (See all compounds classified as Analgesics.)|Drugs used in the treatment of acute or chronic vascular HYPERTENSION regardless of pharmacological mechanism. Among the antihypertensive agents are DIURETICS; (especially DIURETICS, THIAZIDE); ADRENERGIC BETA-ANTAGONISTS; ADRENERGIC ALPHA-ANTAGONISTS; ANGIOTENSIN-CONVERTING ENZYME INHIBITORS; CALCIUM CHANNEL BLOCKERS; GANGLIONIC BLOCKERS; and VASODILATOR AGENTS. (See all compounds classified as Antihypertensive Agents.)

MeSH Entry Terms：

Catapres

Clonidine hydrochloride Use and Manufacturing

Methods of Manufacturing

To a 500 ml reaction flask was added 300 ml of ethanol and 66 g of intermediate 2, and the mixture was heated to reflux with stirring. Remove heat while insolubleAdd 35g of hydrogen chloride-ethanol solution to the filtrate, add dropwise, reflux and stir for 50min, then cool to room temperature naturally, then cool to 0 °C-5 °C and stir and crystallize for 3h, suction filtration, filter cake with a small amount of ethanol to wash, that is Crude hydrochloride hydrochloride.The solid wet product obtained in the above step was added to a 1 L reaction flask, 300 ml of ethyl acetate was added, and the mixture was stirred at room temperature for 1.5 h.After filtration, the cake was washed with a small amount of ethyl acetate and dried to give 51.2 g of white solid.

Uses

In shaving soaps.

Use Classification：

Human drugs -> Rare disease (orphan)|Human Drugs -> EU pediatric investigation plans|Human Drugs -> FDA Approved Drug Products with Therapeutic Equivalence Evaluations (Orange Book) -> Active Ingredients

Computed Properties

Molecular Weight:266.6
Hydrogen Bond Donor Count:3
Hydrogen Bond Acceptor Count:1
Rotatable Bond Count:2
Exact Mass:264.994030
Monoisotopic Mass:264.994030
Topological Polar Surface Area:36.4
Heavy Atom Count:15
Complexity:222
Covalently-Bonded Unit Count:2
Compound Is Canonicalized:Yes

Drug Function and Efficacy

It stimulates the alpha adrenal receptors in the brainstem, reduces the outflow of sympathetic nerves from the central nervous system, and reduces peripheral resistance, renal vascular resistance, heart rate, and blood pressure. It takes effect relatively quickly, and blood pressure reduction begins within 30-60 minutes after oral administration, and the maximum effect is achieved within 2-4 hours. Renal blood flow and glomerular filtration rate remain basically unchanged, and upright symptoms are mild and rare. Acute studies have shown that cardiac output is appropriately reduced (15%-20%) in the supine position, and peripheral resistance remains unchanged; cardiac output is slightly reduced when tilted at 45°, and peripheral resistance is reduced. During long-term treatment, cardiac output tends to return to control values, while peripheral resistance remains reduced.

This ingredient has been used in drugs with the following functions (note: it does not mean that the ingredient itself has the following health functions)

Related Drugs

Clonidine transdermal patch
Ingredients	[2-(2,6-Dichlorophenyl)imino]imidazolidine
Indication	Clonidine may enhance the CNS depressant effects of alcohol, barbiturates, or other sedatives. If a patient taking clonidine hydrochloride is also taking a tricyclic antidepressant, the antihypertensive effect of clonidine may be reduced, thus necessitating an increase in the dose. Patients taking clonidine with drugs that affect sinus node function or AV conduction, such as digoxin, calcium channel blockers, and beta-blockers, should be used with caution because additive effects such as bradycardia and AV block may occur.
Specifications	2.5 mg
Manufacturer	Guoyao Ruifulai Pharmaceutical Co., Ltd.

Zhenju Antihypertensive Tablets
Ingredients	Wild chrysanthemum cream powder Pearl layer powder Clonidine hydrochloride Hydrochlorothiazide Rutin
Indication	Drug interactions may occur if used with other drugs. Please consult your doctor or pharmacist for details.
Specifications	Each tablet weighs 0.26g and contains 0.03mg of clonidine hydrochloride, 5mg of hydrochlorothiazide, and 20mg of rutin

Clonidine Hydrochloride Injection
Ingredients	Clonidine hydrochloride.
Indication	1. When used in combination with central nervous system depressants such as ethanol, barbiturates or sedatives, the central nervous system depressant effect can be enhanced. 2. When used in combination with other antihypertensive drugs, the antihypertensive effect can be enhanced. 3. When used in combination with beta-blockers and then discontinued, the withdrawal syndrome of clonidine can be increased. Therefore, it is advisable to discontinue beta-blockers first and then discontinue clonidine. 4. When used in combination with tricyclic antidepressants, the antihypertensive effect of clonidine is weakened. The dose of clonidine must be increased. 5. When used in combination with nonsteroidal anti-inflammatory drugs, the antihypertensive effect of clonidine is weakened.
Specifications	1ml:0.15mg
Manufacturer	Topfond Pharmaceutical Co., Ltd.

See More Related Drugs

Registered Holders

ENALTEC LABS PRIVATE LTD

United States
Active
ALEMBIC PHARMACEUTICALS LTD

United States
Active
SOCIETA ITALIANA MEDICINALI SCANDICCI SIMS SRL

United States
Active

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