Dexmedetomidine drug data and news

Dexmedetomidine drug data, resources, and news articles (when available). Onconews.org provides news on cancer research. This section, which includes profiles on medicines that may or not be cancer-related is in beta form. If things run smoothly we will be releasing a new format late in the summer of 2006.

Generic name Dexmedetomidine
Brand Names/Synonyms Dexmedetomidine; Medetomidina [Spanish]; Medetomidine; Medetomidinum [Latin]; PRECEDEX; Precedex
Indication For sedation of initially intubated and mechanically ventilated patients during treatment in an intensive care setting, also used in pain relief; anxiety reduction and analgesia
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Description Not Available
Pharmacology Dexmedetomidine activates 2-adrenoceptors, and causes the decrease of sympathetic tone, with attenuation of the neuroendocrine and hemodynamic responses to anesthesia and surgery; it reduces anesthetic and opioid requirements; and causes sedation and analgesia.
Mechanism Of Action Dexmedetomidine is a specific and selective alpha-2 adrenoceptor agonist. By binding to the presynaptic alpha-2 adrenoceptors, it inhibits the release if norepinephrine, therefore, terminate the propagation of pain signals. Avtivation of the postsynaptic alpha-2 adrenoceptors inhibits the sympathetic activity decreases blood pressure and heart rate.
Dexmedetomidine News
(When available)
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Dosage Forms Not Available
Drug_Category Adrenergic alpha-Agonists; Analgesics; Hypnotics and Sedatives; ATC:C02A
Absorption Not Available
Interactions -->Interactions for Dexmedetomidine:

General

In vitro studies in human liver microsomes demonstrated no evidence of cytochrome P450-mediated drug interactions that are likely to be of clinical relevance.

Anesthetics/Sedatives/Hypnotics/Opioids

Co-administration of PRECEDEX with anesthetics, sedatives, hypnotics, and opioids is likely to lead to an enhancement of effects. Specific studies have confirmed these effects with sevoflurane, isoflurane, propofol, alfentanil, and midazolam. No pharmacokinetic interactions between dexmedetomidine and isoflurane, propofol, alfentanil, and midazolam have been demonstrated. However, due to possible pharmacodynamic interactions, when co-administered with PRECEDEX, a reduction in dosage of PRECEDEX on the concomitant anesthetic, sedative, hypnotic or opioid may be required.

Neuromuscular Blockers

In one study of 10 healthy volunteers, administration of PRECEDEX for 45 minutes at a plasma concentration of 1 (one) ng/mL resulted in no clinically meaningful increases in the magnitude or neuromuscular blockade associated with rocuronium administration.

Toxicity Not Available
Organisms Affected Humans and other mammals
Chemical IUPAC Name 4-[1-(2,3-dimethylphenyl)ethyl]-3H-imidazole
Chemical Formula C13H16N2
Molecular Weight 200.28 g/mol
Smiles String CC1=C(C(=CC=C1)C(C)C2=CN=CN2)C
Melting Point Not Available
Water Solubility Freely soluble in water
State Solid
LogP/Hphobicity 3.001
Isoelectric Point 7.1
Biotransformation Hepatic
Half Life 2 hours
Protein Binding [%] 94%
RxList Link RXlist
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Drug Reference http://www.rxlist.com/cgi/generic/precedex.htm
http://www.pharmgkb.org/views/index.jsp?objId=
Drug Type Approved Drug
Accession No APRD00578
CAS Registry Number 113775-47-6
KEGG Compound ID C07450
PubChem ID SID:9653
PharmGKB ID PA449256
SwissProt ID Not Available
GenBank ID Not Available
Drug ID Number [DIN] Not Available

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