Sufentanil drug data and news

Sufentanil 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 Sufentanil
Brand Names/Synonyms Chronogesic; Dea No. 9740; HSDB 6760; R-30730; Sufenta; Sufentanil; Sufentanil Base; Sufentanil Citrate; Sufentanil [Usan:Ban:Inn]; Sufentanilum [Inn-Latin]; Sufentanyl; Sulfentanil Citrate
Indication Used as an analgesic adjunct in anesthesia and as a primary anesthetic drug in procedures requiring assisted ventilation and in the relief of pain.
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Description Not Available
Pharmacology Sufentanil is a synthetic opioid analgesic. Sufentanil interacts predominately with the opioid mu-receptor. These mu-binding sites are discretely distributed in the human brain, spinal cord, and other tissues. In clinical settings, sufentanil exerts its principal pharmacologic effects on the central nervous system. Its primary actions of therapeutic value are analgesia and sedation. Sufentanil may increase the patient's tolerance for pain and decrease the perception of suffering, although the presence of the pain itself may still be recognized. In addition to analgesia, alterations in mood, euphoria and dysphoria, and drowsiness commonly occur. Sufentanil depresses the respiratory centers, depresses the cough reflex, and constricts the pupils.
Mechanism Of Action Opiate receptors are coupled with G-protein receptors and function as both positive and negative regulators of synaptic transmission via G-proteins that activate effector proteins. Binding of the opiate stimulates the exchange of GTP for GDP on the G-protein complex. As the effector system is adenylate cyclase and cAMP located at the inner surface of the plasma membrane, opioids decrease intracellular cAMP by inhibiting adenylate cyclase. Subsequently, the release of nociceptive neurotransmitters such as substance P, GABA, dopamine, acetylcholine and noradrenaline is inhibited. Opioids also inhibit the release of vasopressin, somatostatin, insulin and glucagon. Sufentanil's analgesic activity is, most likely, due to its conversion to morphine. Opioids open calcium-dependent inwardly rectifying potassium channels (OP1 receptor agonist). This results in hyperpolarization and reduced neuronal excitability.
Sufentanil News
(When available)

Endo Pharmaceuticals Reports First Quarter 2006 Financial Results  Apr 20, 2006
Add: Stock compensation expense related to SFAS 123R 2,323 - Add: Topical ketoprofen patch upfront payment - 10,000 Add: Transdermal sufentanil patch upfront ... - PR Newswire (press release),

Dosage Forms LIQUID; SOLUTION
Drug_Category Anesthetics, Intravenous; Narcotics; Adjuvants, Anesthesia; Analgesics, Opioid; Opiate Agonists; ATC:N01AH03
Absorption Not Available
Interactions Interactions for Sufentanil:
May interact with the following: any other medicine, prescription or nonprescription (over-the-counter [OTC]), or street drugs, such as amphetamines, barbiturates, cocaine, marijuana, phencyclidine, and heroin or other narcotics (serious side effects may occur if anyone gives you an anesthetic without knowing that you have taken another medicine), benzodiazepines, central nervous system (CNS) depressants (the CNS depressant and other effects of either these medicines or the narcotic analgesics may be increased), buprenorphine or similar medicines (the narcotic analgesics may not work if you are taking buprenorphine or other similar medicines), cimetidine, erythromycin (increased chance of side effects with some narcotic analgesics), and naltrexone (the narcotic analgesics will not work if you are taking naltrexone).
Toxicity Intravenous, mouse LD50: 18.7 mg/kg
Organisms Affected Humans and other mammals
Chemical IUPAC Name N-[4-(methoxymethyl)-1-(2-thiophen-2-ylethyl)-4-piperidyl]-N-phenyl-propanamide
Chemical Formula C22H30N2O2S
Molecular Weight 386.552 g/mol
Smiles String CCC(=O)N(C1=CC=CC=C1)C2(CCN(CC2)CCC3=CC=CS3)COC
Melting Point 97 °C
Water Solubility 76 mg/L
State Solid (white granules or powder)
LogP/Hphobicity 3.382
Isoelectric Point Not Available
Biotransformation Not Available
Half Life 265 minutes
Protein Binding [%] Not Available
RxList Link Not Available>RXlist
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Drug Reference http://www.drugs.com/cons/Sufentanil.html
Drug Type Approved Drug
Accession No APRD00671
CAS Registry Number 56030-54-7
KEGG Compound ID C08022
PubChem ID SID:10222
PharmGKB ID PA451527
SwissProt ID Not Available
GenBank ID Not Available
Drug ID Number [DIN] 2244147

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