CLONIDINE

CLONIDINE Basic information
Product Name:CLONIDINE
Synonyms:CLONIDINE (200 MG);clonidine (amino form);clonidine (imino form);2-((2,6-dichlorophenyl)amino)-2-imidazoline;2-(2,6-dichloroanilino)-1,3-diazacyclopentene-(2);2-(2,6-dichloroanilino)-2-imidazolin;2-(2,6-dichloroanilino)-2-imidazoline;2-(2,6-Dichlorophenylamino)-2-imidazoline
CAS:4205-90-7
MF:C9H9Cl2N3
MW:230.09
EINECS:224-119-4
Product Categories:
Mol File:4205-90-7.mol
CLONIDINE Structure
CLONIDINE Chemical Properties
Melting point 141-142℃
Boiling point 369.21°C (rough estimate)
density 1.3946 (rough estimate)
refractive index 1.6300 (estimate)
Fp 9℃
storage temp. -20°C
solubility DMSO:100.0(Max Conc. mg/mL);434.61(Max Conc. mM)
pka8.10±0.50(Predicted)
form Solid
color White to Off-White
CAS DataBase Reference4205-90-7(CAS DataBase Reference)
EPA Substance Registry System1H-Imidazol-2-amine, N-(2,6-dichlorophenyl)-4,5-dihydro- (4205-90-7)
Safety Information
Hazard Codes F,T
Risk Statements 11-23/24/25-39/23/24/25
Safety Statements 16-36/37-45
RIDADR UN1230 - class 3 - PG 2 - Methanol, solution
WGK Germany 1
HS Code 2933290000
Hazardous Substances Data4205-90-7(Hazardous Substances Data)
ToxicityLD50 oral in rat: 67300ug/kg
MSDS Information
CLONIDINE Usage And Synthesis
UsesAntihypertensive.
UsesClonidine may be useful in the treatment of acute opioid withdrawal. Epidural clonidine 1–2μgkg –1 increases the duration and potency of analgesia provided by epidural opioid or local anaesthetic drugs.
DefinitionChEBI: A clonidine that is 4,5-dihydro-1H-imidazol-2-amine in which one of the amino hydrogens is replaced by a 2,6-dichlorophenyl group.
Brand nameCatapres (Boehringer Ingelheim).
PharmacokineticsClonidine is lipid soluble and rapidly absorbed after oral administration, with a peak plasma concentration occurring in 60–90min. O ral, intravenous and intramuscular routes may be used for sedation or analgesia. I n addition, epidural and intrathecal clonidine is used to augment regional anaesthesia, but perineural administration is of limited or no effect. The elimination halflife is 9–13h and is prolonged in renal failure. Fifty percent of an administered dose is excreted unchanged by the kidneys, and 50% is metabolised in the liver to inactive metabolites.
Physiological effectsClonidine has some effects at α1-receptors (α2/ α1 > 200 : 1). Clonidine reduces the MA C of inhalational anaesthetic agents by up to 50%. I t has a synergistic analgesic effect with opioids which may be partly pharmacokinetic because the elimination half-life of opioids is also increased.
Physiological effectsCNS effects
Clonidine produces sedation, anxiolysis and analgesia. I t also has a MA Csparing effect, but there is a ceiling to the reduction because of the potential for activity at α1 receptors when used at higher doses.
CVS effects
The cardiovascular effects of clonidine probably involve α1 receptors and imidazoline receptors as with dexmedetomidine. Clonidine lowers the set point around which arterial pressure is regulated.
Respiratory effects
Clonidine has minor respiratory effects, causing only a small reduction in minute ventilation.
Metabolic pathwayClonidine is well absorbed orally, with peak plasma concentrations after 60–90min. I t is highly lipid soluble, and approximately 50% is metabolised in the liver to inactive metabolites; the rest is excreted unchanged via the kidneys, with an elimination half-life of 9–12h.
CLONIDINE Preparation Products And Raw materials
Raw materials2,6-Dichloroaniline-->Clonidine Hydrochloride Chloride
Mecamylamine hydrochloride Labetalol guanethidine Clonidine hydrochloride 2,6-Dichloroaniline

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