Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C13H16N2.ClH |
Molecular Weight | 236.74 |
Optical Activity | ( + ) |
Defined Stereocenters | 1 / 1 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
Cl.C[C@H](C1=CN=CN1)C2=C(C)C(C)=CC=C2
InChI
InChIKey=VPNGEIHDPSLNMU-MERQFXBCSA-N
InChI=1S/C13H16N2.ClH/c1-9-5-4-6-12(10(9)2)11(3)13-7-14-8-15-13;/h4-8,11H,1-3H3,(H,14,15);1H/t11-;/m0./s1
DescriptionSources: https://www.ncbi.nlm.nih.gov/pubmed/16369581Curator's Comment: description was created based on several sources, including http://www.accessdata.fda.gov/drugsatfda_docs/label/2016/021038s027lbl.pdf
Sources: https://www.ncbi.nlm.nih.gov/pubmed/16369581
Curator's Comment: description was created based on several sources, including http://www.accessdata.fda.gov/drugsatfda_docs/label/2016/021038s027lbl.pdf
Dexmedetomide (biologically active dextroisomer of medetomidine) is an alpha2-adrenergic agonist which was approved by FDA for the sedation purposes. Upon administration the drug activates the alpha2 receptors thus inhibiting the release of norepinephrine and terminating the propagation of pain signals. Also it inhibits sympathetic activity and thus can decrease blood pressure and heart rate.
CNS Activity
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
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Target ID: CHEMBL2095158 |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
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Preventing | PRECEDEX Approved UseDexmedetomidine hydrochloride injection is a relatively selective alpha2-adrenergic agonist indicated for: 1) Sedation of initially intubated and mechanically ventilated patients during treatment in an intensive care setting. Administer Precedex by continuous infusion not to exceed 24 hours. 2) Sedation of non-intubated patients prior to and/or during surgical and other procedures. Launch Date1999 |
PubMed
Title | Date | PubMed |
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Noradrenergic regulation of hippocampal place cells. | 2001 |
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Dextromethorphan and dexmedetomidine: new agents for the control of perioperative pain. | 2001 Aug |
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[Medetomidine-butorphanol combination anesthesia in the dog]. | 2001 Dec |
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alpha2A-adrenoceptor stimulation reduces capsaicin-induced glutamate release from spinal cord synaptosomes. | 2001 Dec |
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Effects of reduced sympathetic activity on myocardial metaiodobenzylguanidine (MIBG) washout. | 2001 Jun |
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Comparison between dexmedetomidine and propofol for sedation in the intensive care unit: patient and clinician perceptions. | 2001 Nov |
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Dexmedetomidine: a real innovation or more of the same? | 2001 Nov |
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Effect of medetomidine on electroencephalography and use of a quantitative electroencephalograph for evaluating sedation levels in dogs. | 2001 Nov |
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Cardiopulmonary effects of three different anaesthesia protocols in cats. | 2001 Nov |
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Cardiopulmonary evaluation of the use of medetomidine hydrochloride in cats. | 2001 Nov |
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Dexmedetomidine decreases extracellular dopamine concentrations in the rat nucleus accumbens. | 2001 Nov 16 |
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Optimization of intraperitoneal injection anesthesia in mice: drugs, dosages, adverse effects, and anesthesia depth. | 2001 Oct |
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New agents for sedation in the intensive care unit. | 2001 Oct |
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Use of propofol and other nonbenzodiazepine sedatives in the intensive care unit. | 2001 Oct |
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Benzodiazepines in the intensive care unit. | 2001 Oct |
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Dexmedetomidine infusion and somatosensory evoked potentials. | 2001 Oct |
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Clinical comparison of preanaesthetic intramuscular medetomidine and dexmedetomidine in domestic sheep. | 2001 Oct |
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Controlled hypotension in children: a critical review of available agents. | 2002 |
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Interactions between cutaneous afferent inputs to a withdrawal reflex in the decerebrated rabbit and their control by descending and segmental systems. | 2002 |
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Anesthesia of boma-captured Lichtenstein's hartebeest (Sigmoceros lichtensteinii) with a combination of thiafentanil, medetomidine, and ketamine. | 2002 Apr |
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Down-regulation of the alpha-2C adrenergic receptor: involvement of a serine/threonine motif in the third cytoplasmic loop. | 2002 Apr 2 |
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Activation of the peroxisome proliferator-activated receptor alpha protects against myocardial ischaemic injury and improves endothelial vasodilatation. | 2002 Apr 9 |
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Initial experience with dexmedetomidine in paediatric-aged patients. | 2002 Feb |
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Some factors influencing the level of clinical sedation induced by medetomidine in rabbits. | 2002 Feb |
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The use of alpha2-agonists during off-pump coronary artery bypass and the effects of hypothermia. | 2002 Feb |
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Alpha 2-adrenoceptors in the enteric nervous system: a study in alpha 2A-adrenoceptor-deficient mice. | 2002 Feb |
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Effect of the alpha2-agonist dexmedetomidine on cerebral neurotransmitter concentrations during cerebral ischemia in rats. | 2002 Feb |
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Neurohormonal and metabolic effects of medetomidine compared with xylazine in beagle dogs. | 2002 Jan |
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Effects of alpha(2)-adrenoceptor agonists on perinatal excitotoxic brain injury: comparison of clonidine and dexmedetomidine. | 2002 Jan |
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alpha(2C)-Adrenergic receptors mediate spinal analgesia and adrenergic-opioid synergy. | 2002 Jan |
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Reliability of goniometry in Labrador Retrievers. | 2002 Jul |
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Evaluation of the perioperative stress response in dogs administered medetomidine or acepromazine as part of the preanesthetic medication. | 2002 Jul |
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Effects of medetomidine-midazolam, midazolambutorphanol, or acepromazine-butorphanol as premedicants for mask induction of anesthesia with sevoflurane in dogs. | 2002 Jul |
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Effect of synthesis parameters of the sol-gel-processed spray-dried silica gel microparticles on the release rate of dexmedetomidine. | 2002 Jul |
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In vivo regulation of dopamine and noradrenaline release by alpha2A-adrenoceptors in the mouse prefrontal cortex. | 2002 Jun |
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Dual alpha(2)-adrenergic agonist and alpha(1)-adrenergic antagonist actions of dexmedetomidine on human isolated endothelium-denuded gastroepiploic arteries. | 2002 Jun |
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Hemodynamics of anesthetized ventilated mouse models: aspects of anesthetics, fluid support, and strain. | 2002 Jun |
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Use of medetomidine for capture and restraint of cassowaries (Casuarius casuaris). | 2002 Mar |
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Dexmedetomidine may be effective, but is it safe? | 2002 Mar |
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Infusion of alpha-2-adrenergic agents into the paraventricular and arcuate nuclei of the hypothalamus in the Siberian hamster: opposing effects on basal prolactin. | 2002 Mar |
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N-Glucuronidation of some 4-arylalkyl-1H-imidazoles by rat, dog, and human liver microsomes. | 2002 Mar |
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Postoperative pain control in cats: clinical trials with medetomidine and butorphanol. | 2002 Mar-Apr |
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Quantitative electroencephalography of medetomidine, medetomidine-midazolam and medetomidine-midazolam-butorphanol in dogs. | 2002 May |
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Pharmacokinetics of dexmedetomidine infusions for sedation of postoperative patients requiring intensive caret. | 2002 May |
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Altered presynaptic function in monoaminergic neurons of monoamine oxidase-A knockout mice. | 2002 May |
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New agents, new monitors, same unanswered questions. | 2002 May |
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Bispectral index-guided sedation with dexmedetomidine in intensive care: a prospective, randomized, double blind, placebo-controlled phase II study. | 2002 May |
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alpha(2B)-Adrenergic receptors activate MAPK and modulate proliferation of primary cultured proximal tubule cells. | 2002 May |
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Cardiopulmonary effects of a medetomidine-ketamine combination administered intravenously in gopher tortoises. | 2002 May 15 |
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alpha 2B-adrenergic receptor activates MAPK via a pathway involving arachidonic acid metabolism, matrix metalloproteinases, and epidermal growth factor receptor transactivation. | 2002 May 31 |
Patents
Sample Use Guides
For Adult Intensive Care Unit Sedation: Generally initiate at one mcg/kg over 10 minutes, followed by a maintenance infusion of 0.2 to 0.7 mcg/kg/hour. For Adult Procedural Sedation: Generally initiate at one mcg/kg over 10 minutes, followed by a maintenance infusion initiated at 0.6 mcg/kg/hour and titrated to achieve desired clinical effect with doses ranging from 0.2 to 1 mcg/kg/hour.
Route of Administration:
Intravenous
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/15795144
Strips of pregnant human myometrium obtained from six individuals at elective caesarean section were incubated with dexmedetomidine (1x10(-11) to 1x10(-6) g/mL) and the in vitro effect was studied as the drug may be used in obstetric anaesthesia
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EMA VETERINARY ASSESSMENT REPORTS |
SEDADEX [AUTHORIZED]
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CEPEDEX (AUTHORISED)
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SEDADEX [AUTHORIZED]
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SILEO [AUTHORIZED]
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DEXDOMITOR (AUTHORISED)
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EMA ASSESSMENT REPORTS |
DEXDOR (AUTHORIZED: CONSCIOUS SEDATION)
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NCI_THESAURUS |
C29709
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DEXDOMITOR (AUTHORISED)
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CEPEDEX (AUTHORISED)
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LL-19
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ACTIVE MOIETY
SUBSTANCE RECORD