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Fentanyl
drug data and news
Fentanyl 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.
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| Generic name | Fentanyl | ||
| Brand Names/Synonyms | Actiq; CHEMBANK1683; Dea No. 9801; Duragesic; Duragesic-100; Durogesic; F5886; Fentanest; Fentanil; Fentanil [Dcit]; Fentanila; Fentanila [Inn-Spanish]; Fentanyl; Fentanyl Citrate; Fentanyl Citrate Preservative Free; Fentanylum; Fentanylum [Inn-Latin]; HSDB 3329; Pentanyl; Phentanyl; R 4263; Sentonil; Sublimaze; Sublimaze Preservative Free | ||
| Indication | For the treatment of cancer patients with severe pain that breaks through their regular narcotic therapy. | ||
| Sponsored links | Description | Not Available | |
| Pharmacology | Fentanyl is an opioid analgesic. Fentanyl 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, Fentanyl exerts its principal pharmacologic effects on the central nervous system. Its primary actions of therapeutic value are analgesia and sedation. Fentanyl 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. Fentanyl 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. Fentanyl's analgesic activity is, most likely, due to its conversion to morphine. Opioids close N-type voltage-operated calcium channels (OP2-receptor agonist) and open calcium-dependent inwardly rectifying potassium channels (OP3 and OP1 receptor agonist). This results in hyperpolarization and reduced neuronal excitability. | ||
| Fentanyl News (When available) |
Celebrex Lawsuit Set for Trial in Alabama State Court 06 Mar 2006 As trial looms, Celebrex eases Pfizer sales pain Mar 2, 2006 Short-term Celebrex seems safe for osteoarthritis Feb 27, 2006 Celebrex 'doubles risk' of heart attack Mar 2, 2006 Celebrex Doubles Lawsuit Risk Mar 1, 2006 Pfizer's Celebrex raises heart attack risk -study Feb 28, 2006 Study: Pfizer's Celebrex raises heart attack risks Mar 1, 2006 Medsafe stands by Celebrex despite risk study Feb 28, 2006 Analysis: Celebrex ups heart-attack risk Feb 28, 2006 Celebrex Lawsuit Set for Trial in Barbour County Mar 2, 2006 First Celebrex lawsuit going to trial Feb 27, 2006 EDITORIAL - Celebrex not a reason to celebrate Feb 27, 2006 Pfizer Disputes New Zealand Celebrex Heart Attack Link Study ... Mar 2, 2006 Study Finds Celebrex Increases Risk Of Heart Attack Mar 2, 2006 Meta-Analysis Links Celebrex to Doubling of MI Risk Mar 2, 2006 Celebrex safe for osteoarthritis Mar 1, 2006 Why Commercial Breaks During News Broadcasts Are Full Of Celebrex ... Feb 24, 2006 Celebrex Gets Passing Grades for Gastric and Cardiac Safety Feb 23, 2006 Celebrex Lawsuit Set for Trial in Alabama State Court Mar 2, 2006 Date set for first Celebrex trial Feb 28, 2006 Study finds Celebrex doubles heart attack risk Mar 1, 2006 Short spell of Celebrex may be safe for IBD Feb 15, 2006 Further fears over arthritis drug Mar 1, 2006 Study Examines Celebrex and Heart Attacks Mar 1, 2006 Celebrex Doubles Lawsuit Risk Mar 1, 2006 Trial Date for Celebrex Suit Set for June Feb 27, 2006 James Le Fanu on some less than rosy news for arthritis sufferers ... Mar 3, 2006 Arthritis painkiller doubles risk to heart, says study Feb 28, 2006 Pfizer Painkiller’s Bad Data Mar 1, 2006 Study bolsters case against key Pfizer drug Mar 1, 2006 Stock Futures Point to Bounce Mar 1, 2006 Painkiller 'may double risk of heart attacks' Feb 28, 2006 Cutting Through Pharmaceutical Media Spin Mar 2, 2006 Pfizer`s COX 2 may be heart safe Feb 22, 2006 Schaeffer's Midday Options Update Features Pfizer, Sirius ... Mar 1, 2006 New fears of wonder drug link to heart attacks Mar 1, 2006 Options Update: Trading Options on Texas Instruments Mar 1, 2006 Analysis: Pfizer's COX 2 may be heart safe Feb 22, 2006 Arthritis drug increases risk of heart attacks: study Feb 28, 2006 Doc defends pain supplements, slams study Feb 23, 2006 Drug linked to heart attack risk Feb 28, 2006 US stocks set to rebound from prior-session losses Mar 1, 2006 Glucosamine-Chondroitin Sulfate Can Ease Severe Pain Feb 22, 2006 Scientist urges rethink after secondarthritis drug found to be ... Feb 28, 2006 Ease joint pain without blockbuster drugs Feb 28, 2006 US stocks set for modest rebound after selloff Mar 1, 2006 Bextra - What Did Pfizer Know? - Everything Mar 5, 2006 Study: Supplements fail to ease arthritis Feb 22, 2006 | ||
| Dosage Forms | DISC (SUSTAINED-RELEASE); LIQUID; SOLUTION | ||
| Drug_Category | Anesthetics; Narcotics; Adjuvants; Analgesics; Opiate Agonists; ATC:N01AH01; ATC:N02AB03 | ||
| Absorption | Not Available | ||
| Interactions |
Interactions for Fentanyl: Agents Affecting Cytochrome P450 3A4 Isoenzyme System Fentanyl is metabolized mainly via the human cytochrome P450 3A4 isoenzyme system (CYP3A4), therefore potential interactions may occur when DURAGESIC® is given concurrently with agents that affect CYP3A4 activity. Coadminstration with agents that induce 3A4 activity may reduce the efficacy of DURAGESIC®. The concomitant use of transdermal fentanyl with ritonavir or other potent 3A4 inhibitors such as ketoconazole, itraconazole, troleandomycin, clarithromycin, nelfinavir, and nefazadone may result in an increase in fentanyl plasma concentrations. The concomitant use of other CYP3A4 inhibitors such as diltiazem and erythromycin with transdermal fentanyl may also result in an increase in fentanyl plasma concentrations, which could increase or prolong adverse drug effects and may cause serious respiratory depression. In this situation, special patient care and observation are appropriate. Central Nervous System Depressants The concomitant use of DURAGESIC® (fentanyl transdermal system) with other central nervous system depressants, including but not limited to other opioids, sedatives, hypnotics, tranquilizers (e.g., benzodiazepines), general anesthetics, phenothiazines, skeletal muscle relaxants, and alcohol, may cause respiratory depression, hypotension, and profound sedation, or potentially result in coma or death. When such combined therapy is contemplated, the dose of one or both agents should be significantly reduced. MAO Inhibitors DURAGESIC® is not recommended for use in patients who have received MAOI within 14 days because severe and unpredictable potentiation by MAO inhibitors has been reported with opioid analgesics. --> | ||
| Toxicity | Not Available | ||
| Organisms Affected | Humans and other mammals | ||
| Chemical IUPAC Name | N-(1-phenethyl-4-piperidyl)-N-phenyl-propanamide | ||
| Chemical Formula | C22H28N2O | ||
| Molecular Weight | 336.471 g/mol | ||
| Smiles String | CCC(=O)N(C1CCN(CC1)CCC2=CC=CC=C2)C3=CC=CC=C3 | ||
| Melting Point | 87.5 °C | ||
| Water Solubility | 200 mg/L | ||
| State | Solid | ||
| LogP/Hphobicity | 4.144 | ||
| Isoelectric Point | Not Available | ||
| Biotransformation | Fentanyl is metabolized primarily via human cytochrome P450 3A4 isoenzyme system. | ||
| Half Life | 7 (range 3-12) hours | ||
| Protein Binding [%] | 13 and 21% | ||
| RxList Link | RXlist | ||
| Sponsored links | |||
| Drug Reference |
http://www.drugs.com/cons/Fentanyl.html http://www.rxlist.com/cgi/generic2/fentanyl.htm | ||
| Drug Type | Approved Drug | ||
| Accession No | APRD00347 | ||
| CAS Registry Number | 437-38-7 | ||
| KEGG Compound ID | C06998 | ||
| PubChem ID | SID:373581 | ||
| PharmGKB ID | PA449599 | ||
| SwissProt ID | Not Available | ||
| GenBank ID | Not Available | ||
| Drug ID Number [DIN] | 2240434 |
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