Fentanyl_Citrate: profile and news






Cephalon Reports Outstanding Financial Results for 2005  Feb 14, 2006
In 2005, sales of PROVIGIL(R) (modafinil) Tablets [C-IV] increased 17 percent to $512.8 million; sales of ACTIQ(R) (oral transmucosal fentanyl citrate) [C-II ... - MSN Money

Cephalon Reports Outstanding Financial Results for 2005  Feb 14, 2006
In 2005, sales of PROVIGIL® (modafinil) Tablets [C-IV] increased 17 percent to $512.8 million; sales of ACTIQ® (oral transmucosal fentanyl citrate) [C-II ... - Yahoo! News (press release)

Barr Announces Agreements With Cephalon, Inc. Regarding Settlement ...  Feb 1, 2006
...agreements to settle its pending patent infringement disputes in the United States related to Cephalon's ACTIQ(R) (oral transmucosal fentanyl citrate) [C-II ... - International News Service,

Cephalon, Inc. Announces Agreements With Barr Laboratories, Inc. ...  Feb 1, 2006
...patent infringement disputes in the United States related to PROVIGIL(R) (modafinil) Tablets [C-IV] and ACTIQ(R) (oral transmucosal fentanyl citrate) [C-II]. ... - Black Enterprise,

Cephalon, Inc. Provides Update on Regulatory Status of NUVIGIL(TM)  Feb 1, 2006
...markets four proprietary products in the United States: PROVIGIL, GABITRIL(R) (tiagabine hydrochloride), ACTIQ(R) (oral transmucosal fentanyl citrate) [C-II ... - PR Newswire (press release),

Cephalon, Inc. Provides Update on Regulatory Status of NUVIGIL(TM)  Feb 1, 2006
...markets four proprietary products in the United States: PROVIGIL, GABITRIL® (tiagabine hydrochloride), ACTIQ® (oral transmucosal fentanyl citrate) [C-II] and ... - Yahoo! News (press release)

Barr Announces Agreements With Cephalon, Inc. Regarding Settlement ...  Feb 1, 2006
...agreements to settle its pending patent infringement disputes in the United States related to Cephalon's ACTIQ(R) (oral transmucosal fentanyl citrate) [C-II ... - International News Service,

Cephalon, Inc. Provides Update on Regulatory Status of NUVIGIL  Feb 2, 2006
...markets four proprietary products in the United States: PROVIGIL, GABITRIL(R) (tiagabine hydrochloride), ACTIQ(R) (oral transmucosal fentanyl citrate) [C-II ... - PharmaLive.com (press release),

Studies Confirm Effectiveness Of Fentanyl Lozenges For ' ...  Jan 25, 2006
...medicine. The fentanyl lozenge, known as oral transmucosal fentanyl citrate, or OTFC, is also known by the brand name Actiq. The ... - Medical News Today (press release),

Cephalon, Inc. Announces Agreements With Barr Laboratories, Inc. ...  Feb 1, 2006
...patent infringement disputes in the United States related to PROVIGIL(R) (modafinil) Tablets [C-IV] and ACTIQ(R) (oral transmucosal fentanyl citrate) [C-II]. ... - Black Enterprise,

2d Plymouth paramedic fired  Jan 28, 2006
Police charge that Entenman removed morphine sulfate and fentanyl citrate, both controlled substances, from ambulances and replaced them with a saline solution ... - Philadelphia Inquirer,

Horst Witzel, Dr.-Ing., to Retire From Cephalon Board of Directors  Jan 31, 2006
...products in the United States: PROVIGIL(R) (modafinil) [C-IV], GABITRIL(R) (tiagabine hydrochloride), ACTIQ(R) (oral transmucosal fentanyl citrate) [C-II] and ... - PR Newswire (press release),

Cephalon, Inc. Provides Update on Regulatory Status of SPARLON(TM)  Jan 25, 2006
...markets four proprietary products in the United States: PROVIGIL, GABITRIL® (tiagabine hydrochloride), ACTIQ® (oral transmucosal fentanyl citrate) [C-II] and ... - Yahoo! News (press release)

Horst Witzel, Dr.-Ing., to Retire From Cephalon Board of Directors  Jan 31, 2006
...products in the United States: PROVIGIL® (modafinil) [C-IV], GABITRIL® (tiagabine hydrochloride), ACTIQ® (oral transmucosal fentanyl citrate) [C-II] and ... - Yahoo! News (press release)

Scientific Advances on Three Lead Cephalon Oncology Compounds to ...  Dec 8, 2005
...products in the United States: PROVIGIL(R) (modafinil) [C-IV], GABITRIL(R) (tiagabine hydrochloride), ACTIQ(R) (oral transmucosal fentanyl citrate) [C-II] and ... - PR Newswire (press release),

Source: Cephalon, Inc.; Zeneus Holdings Limited  Dec 5, 2005
...products in the United States: PROVIGIL® (modafinil) [C-IV], GABITRIL® (tiagabine hydrochloride), ACTIQ® (oral transmucosal fentanyl citrate) [C-II] and ... - Yahoo! News (press release)

FDA Approvals: Nevanac, Sugar-Free Actiq, Quinine Sulfate  Sep 15, 2005
...suspension for the treatment of pain and inflammation associated with cataract surgery; a sugar-free formulation of oral transmucosal fentanyl citrate for the ... - Medscape (subscription)

Cephalon Receives FDA Approval to Market Sugar-Free Formulation of ...  Sep 12, 2005
...an approval letter from the US Food and Drug Administration (FDA) to market a new sugar-free formulation of ACTIQ(R) (oral transmucosal fentanyl citrate) [C-II ... - PharmaLive.com (press release),

FDA Extends PDUFA Date for VIVITREX(R) to December 30, 2005 ...  Sep 20, 2005
...products in the United States: PROVIGIL(R) (modafinil) (C-IV), GABITRIL(R) (tiagabine hydrochloride), ACTIQ(R) (oral transmucosal fentanyl citrate) (C-II) and ... - Genetic Engineering News,

Cephalon Files New Drug Application for OraVescent(R) Fentanyl for ...  Sep 6, 2005
Cephalon has drawn on its experience with ACTIQ(R) (oral transmucosal fentanyl citrate) [C-II] to develop a comprehensive Risk Minimization Action Plan (RiskMAP ... - PR Newswire (press release),

Cephalon, Inc. Announces Agreement With McNeil Consumer & ...  Sep 1, 2005
...markets four proprietary products in the United States: PROVIGIL, GABITRIL(R) (tiagabine hydrochloride) ACTIQ(R) (oral transmucosal fentanyl citrate) [C-II ... - PR Newswire (press release),

Cephalon Receives Approval to Market Modafinil for Shift Work ...  Aug 30, 2005
...markets four proprietary products in the United States: PROVIGIL(R), GABITRIL(R) (tiagabine hydrochloride), ACTIQ(R) (oral transmucosal fentanyl citrate) [C-II ... - PR Newswire (press release),

Cephalon Board Member Gail Wilensky Appointed to World Health ...  Aug 25, 2005
...products in the United States: PROVIGIL® (modafinil) [C-IV], GABITRIL® (tiagabine hydrochloride), ACTIQ® (oral transmucosal fentanyl citrate) [C-II] and ... - Yahoo News (press release)

Cephalon Board Member Gail Wilensky Appointed to World Health ...  Aug 25, 2005
...products in the United States: PROVIGIL(R) (modafinil) [C-IV], GABITRIL(R) (tiagabine hydrochloride), ACTIQ(R) (oral transmucosal fentanyl citrate) [C-II] and ... - PR Newswire (press release),

Cephalon Receives Approval to Market Modafinil for Shift Work ...  Aug 30, 2005
...markets four proprietary products in the United States: PROVIGIL®, GABITRIL® (tiagabine hydrochloride), ACTIQ® (oral transmucosal fentanyl citrate) [C-II ... - Yahoo News (press release)

New England Journal of Medicine Publishes First Clinical Study of ...  Aug 4, 2005
...markets four proprietary products in the United States: PROVIGIL, GABITRIL(R) (tiagabine hydrochloride), ACTIQ(R) (oral transmucosal fentanyl citrate) [C-II ... - Forbes

New England Journal of Medicine Publishes First Clinical Study of ...  Aug 3, 2005
...markets four proprietary products in the United States: PROVIGIL, GABITRIL® (tiagabine hydrochloride), ACTIQ® (oral transmucosal fentanyl citrate) [C-II] and ... - Yahoo News (press release)

Cephalon Reports Continued Strong Growth in Second Quarter  Aug 2, 2005
Sales of PROVIGIL® (modafinil) Tablets [C-IV] were $129.9 million, a 26 percent increase; sales of ACTIQ® (oral transmucosal fentanyl citrate) [C-II] were ... - Yahoo News (press release)

Cephalon Reports Continued Strong Growth in Second Quarter  Aug 2, 2005
Sales of PROVIGIL(R) (modafinil) Tablets [C-IV] were $129.9 million, a 26 percent increase; sales of ACTIQ(R) (oral transmucosal fentanyl citrate) [C-II] were ... - PharmaLive.com (press release)

Cephalon, Inc. Completes Acquisition of TRISENOX From Cell ...  Jul 19, 2005
...products in the United States: PROVIGIL(R) (modafinil) [C-IV], GABITRIL(R) (tiagabine hydrochloride), ACTIQ(R) (oral transmucosal fentanyl citrate) [C-II] and ... - PharmaLive.com (press release)

Cephalon, Inc. Completes Acquisition of TRISENOX(R) From Cell ...  Jul 19, 2005
...products in the United States: PROVIGIL® (modafinil) [C-IV], GABITRIL® (tiagabine hydrochloride), ACTIQ® (oral transmucosal fentanyl citrate) [C-II] and ... - Yahoo News (press release)

Cephalon, Inc. Accepts Notes Tendered Pursuant to Offer for 2-1/2 ...  Jul 12, 2005
...in the United States: PROVIGIL(R) (modafinil) Tablets [C-IV], GABITRIL(R) (tiagabine hydrochloride) and ACTIQ(R) (oral transmucosal fentanyl citrate) [C-II ... - PharmaLive.com (press release) <**results**>

Cephalon Announces Exercise of $120 Million Over-allotment Option ...  Jul 1, 2005
...products in the United States: PROVIGIL® (modafinil) [C-IV], GABITRIL® (tiagabine hydrochloride) and ACTIQ® (oral transmucosal fentanyl citrate) [C-II] and ... - Yahoo News (press release)

Cephalon Announces Exercise of $120 Million Over-allotment Option ...  Jul 1, 2005
...products in the United States: PROVIGIL(R) (modafinil) [C-IV], GABITRIL(R) (tiagabine hydrochloride) and ACTIQ(R) (oral transmucosal fentanyl citrate) [C-II ... - PharmaLive.com (press release)

Cephalon, Inc. Announces Acquisition of TRISENOX(R) from Cell  Jun 13, 2005
...in the United States: PROVIGIL(R) (modafinil) Tablets [C-IV], GABITRIL(R) (tiagabine hydrochloride), and ACTIQ(R) (oral transmucosal fentanyl citrate) [C-II ... - APA OTS (Pressemitteilung)

Cephalon and Alkermes Announce Agreement for the Commercialization ...  Jun 24, 2005
...products in the United States: PROVIGIL®(modafinil) Tablets [C-IV], GABITRIL® (tiagabine hydrochloride) and ACTIQ®(oral transmucosal fentanyl citrate) [C-II ... - Yahoo News (press release)

Cephalon and Alkermes Announce Agreement for the Commercialization ...  Jun 24, 2005
...in the United States: PROVIGIL(R)(modafinil) Tablets (C-IV), GABITRIL(R) (tiagabine hydrochloride) and ACTIQ(R)(oral transmucosal fentanyl citrate) (C-II), and ... - Business Wire (press release)

Cephalon, Inc. Announces Acquisition of TRISENOX(R) from Cell ...  Jun 13, 2005
...in the United States: PROVIGIL® (modafinil) Tablets [C-IV], GABITRIL® (tiagabine hydrochloride), and ACTIQ® (oral transmucosal fentanyl citrate) [C-II], and ... - Yahoo News (press release)


Other information


Indication
For the treatment of cancer patients with severe pain that breaks through their regular narcotic therapy.

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.

Drug Category
Anesthetics; Narcotics; Adjuvants; Analgesics; Opiate Agonists; ATC:N01AH01; ATC:N02AB03

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

Dosage Forms
DISC (SUSTAINED-RELEASE); LIQUID; SOLUTION

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.

--> 


Chemical IUPAC Name
N-(1-phenethyl-4-piperidyl)-N-phenyl-propanamide

Chemical Formula
C22H28N2O

Half Life
7 (range 3-12) hours

Drug Type
Approved Drug

# Accession No
APRD00347

CAS Registry Number
437-38-7

Home | About | Cancers | Treatment | Medications
Copyright onconews.org 2005.
All Rights Reserved.
Google
 
Web onconews.org