Fentanyl resources


DRUG INFO
Fentanyl

Drug Name: Fentanyl

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: DrugBank: Interactions for Fentanyl

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



Fentanyl News
(When available)


Cephalon, Inc. Announces Agreement with Mylan Pharmaceuticals Inc. ...  Jan 10, 2006
PharmaLive.com (press release), The company currently markets four proprietary products in the United States: PROVIGIL, GABITRIL(R) (tiagabine hydrochloride), ACTIQ(R) (oral transmucosal ...

Cephalon CEO readies for 4 new drug launches  Dec 19, 2005
Reuters He anticipates a late 2006 launch of OVF for extreme cancer pain that he believes will more than make up for revenue lost when its pain drug Actiq goes off ...

FDA Issues Approvable Letter for VIVITROL(TM) (Formerly VIVITREX(R ...  Dec 28, 2005
Finanzen.net, ...company currently markets four proprietary products in theUnited States: PROVIGIL(R) (modafinil) (C-IV), GABITRIL(R) (tiagabinehydrochloride), ACTIQ(R) (oral ...

Cephalon, Inc. Completes Acquisition of Zeneus Holdings Limited  Dec 22, 2005
Yahoo! News (press release) ...markets four proprietary products in the United States: PROVIGIL® (modafinil) [C-IV], GABITRIL® (tiagabine hydrochloride), ACTIQ® (oral transmucosal ...

Cephalon, Inc. Completes Acquisition of Zeneus Holdings Limited  Dec 22, 2005
Boursorama, ...company currently markets four proprietary products in the United States: PROVIGIL(R) (modafinil) [C-IV], GABITRIL(R) (tiagabine hydrochloride), ACTIQ(R) (oral ...

Low-level exercise delays heart failure, markedly extends lives ...  15 Jan 2006
Xagena.it, The ) final training intensity was quite low as evidenced by the absence of a training-induced increase in skeletal muscle citrate synthase activity or body ...

Sidnafil Citrate is a medicine, not stimulant warns doctors  Jan 3, 2006
Hindu, ..."These tablets which contain Sidnafil Citrate are specific drugs that are effectively used for the treatment of erectile dysfunction. ...

Gadot Biochemicals seeks to acquire co in US or Europe  Jan 12, 2006
Globes, ...strategy, marking as growth sources several added value products related to the production of citric acid, such as crystalline fructose and Tri-Sodium Citrate. ...

PURE Bioscience Board Elects D. Michael Sitton to its Board of ...  Jan 12, 2006
Business Wire (press release), ...in the Company's growth as I tap the resources in my diverse background to help advance PURE Bioscience's new silver dihydrogen citrate platform technology ...

Tough competition for Pfizer Viagra  Jan 5, 2006
CNN-IBN, Viagra is mainly prescribed for erectile dysfunction. The main ingredient in the magic blue pill is Sildenafil Citrate. Sildenafil ...

Osteoporosis International Publishes Study Showing the 'BEST' Way ...  Dec 20, 2005
PR Newswire (press release), Weight-Bearing Regimen and Calcium Citrate Proven to Increase Bone Mineral Densityin Four-Year Research Study TUCSON, Ariz., Dec. ...

Osteoporosis International Publishes Study Showing the 'BEST' Way ...  Dec 20, 2005
Biotech Intelligence (press release), ...at The University of Arizona which confirmed that a specific regimen of weight-bearing and resistance exercises, combined with calcium citrate supplement over ...

Seek constipation's cause  Dec 27, 2005
Contra Costa Times, Q For several months I have been taking large daily doses of magnesium citrate (1200 mg) in an attempt to deal with my long-term constipation (more than 30 ...

- By Our Correspondent  Dec 21, 2005
The Asian Age, A spokesperson for Ranbaxy India Limited (RIL) said that Pfizer, the original innovator of Viagra (Sildenefil Citrate), has just come into the market and so it ...

FTC chief concerned about drug patent deals  Jan 11, 2006
Reuters The patent settlement challenged in that case involved AstraZeneca's Tamoxifen Citrate, the most widely prescribed drug for breast cancer treatment. ...

Pfizer Introduces RFID Technology to Combat Counterfeiting ...  Jan 8, 2006
MoreRFID (press release), RFID technology is being added to all Viagra(R) (sildenafil citrate) sold in the US to enable pharmacies and wholesalers to verify the unique electronic ...

Cephalon, Inc. Announces Agreement with Mylan Pharmaceuticals Inc. ...  Jan 10, 2006
PharmaLive.com (press release), ...markets four proprietary products in the United States: PROVIGIL, GABITRIL(R) (tiagabine hydrochloride), ACTIQ(R) (oral transmucosal fentanyl citrate) [C-II ...

Pfizer adds radio tags to Viagra to combat fakes  Jan 9, 2006
Pharma Times (subscription), The product to receive the electronic tagging system is erectile dysfunction treatment Viagra (sildenafil citrate), which is one of the most counterfeited ...

Bio/Data Corporation Releases New Control Plasma for vW Testing  Jan 11, 2006
Genetic Engineering News, Bio/Data's other reagents for vW testing include: lyophilized platelets, ristocetin, sodium citrate, tris buffered saline, vW abnormal control plasma and vW ...

Double the Size of Your Portfolio in 60 Days with Enzyte  Jan 10, 2006
I-Newswire.com (press release) ...which usually show the product's trade name ( eg, Viagra ) in big letters and the scientific-sounding chemical name ( eg, sildenafil citrate ) in parentheses ...

VIAGRA: THE WONDER DRUG  Jan 4, 2006
Star of Mysore, ...regain sexual function. Oral tablets like Sildenifil citrate (Viagra), Tadalafil, Yohimbine, etc are routinely used. Injections like ...

Sports and Substance Abuse  Jan 10, 2006
Medscape (subscription) Use of drugs like clomiphene citrate, which masks the androgenic effects of steroids, and diuretics, which decrease the accumulation of fluid weight of these ...

Viagra a medicine, not stimulant  Jan 4, 2006
Newindpress, ...‘‘These tablets which contain sidnafil citrate are specific drugs that are effectively used for the treatment of erectile dysfunction. ...

Erectile Dysfunction: New Agents, New Data  Dec 29, 2005
Medscape (subscription) Sildenafil citrate at a 25- or 50-mg oral daily dose in the morning, or tadalafil at a 5-mg oral dose 3 times weekly in the morning, was administered to 3 men ...

Aspirin Resistance: Fact and Fiction  Dec 27, 2005
Medscape (subscription) It is an in vitro quantitative measurement of platelet adhesion and aggregation that requires whole blood collected in 3.8% sodium citrate. ...

Erectile Dysfunction Drug Viagra Launched In India By Pfizer  Dec 21, 2005
MedIndia, Infact, a generic version of Viagra (Sildenafil Citrate) was available in India much before the launch of the launch of the pill in the US drug market before 7 ...

Is there a quick fertility drug I can use?  Dec 16, 2005
The Monitor, Uganda, ...a woman is found with a problem of ovulation, she is likely to benefit from the so-called fertility drugs of which one common one is called Clomiphene Citrate. ...

Viagra launch could face stiff protest in MP  Dec 23, 2005
Business Standard, ...of Viagra from Pfizer will face stiff protest in Madhya Pradesh, particularly from small-scale sector units that manufacture sildenafil citrate—the main ...

Mumbai not so hard on Viagra  Dec 20, 2005
Mid-Day Mumbai, Sandeep Ashar and Vrushali Lad report. The original sex pill Viagra (sildenafil citrate) for erectile dysfunction among males is finally here. ...

Take this: Real Viagra comes to India!  Dec 20, 2005
Times of India, The original blue pill will cost Rs 594 (Rs 463 for 50 mg) as against Rs 25 or less for the desi or generic version of the drug known as sildenafil citrate. ...

How Viagra stood up as a product  Dec 20, 2005
Daily News & Analysis, Dr Peter Ellis, executive director, global R&D, recalled the day in September 1993 when Pfizer bosses were ready to abandon research on sildenafil citrate. ...

GTx Reports Positive Phase III Trial Interim Analysis Results  Dec 15, 2005
PR Newswire (press release), ...experienced highly statistically significant increases in bone mineral density (BMD) after one year of treatment with ACAPODENE(R) (toremifene citrate) 80 mg ...

Pfizer to sell Viagra @ Rs 20 in India  Dec 18, 2005
Economic Times, The domestic market is already cluttered with almost a dozen Viagra clones (generic versions containing the active ingredient sildenafil citrate). ...

Wonder pill’s here  Dec 20, 2005
Calcutta Telegraph, In a market flooded with at least seven local brands of sildenafil citrate tablets selling at much cheaper prices, it is difficult to say how much impact Pfizer ...

PURE Bioscience Reports First Quarter Results  Dec 16, 2005
Genetic Engineering News, Michael L. Krall, President and CEO of PURE Bioscience, stated, "We have introduced our silver dihydrogen citrate (SDC) antimicrobial to numerous domestic and ...

Pfizer to launch Viagra in India this week  Dec 12, 2005
Rediff, Pfizer, the inventor of Sildenafil Citrate, is planning to roll out its blockbuster erectile disfunction drug brand, Viagra, in India this week after a long ...

Vaccination drive against filaria  Jan 6, 2006
Hindustan Times, Singh has constituted 25 teams comprising paramedical staff to visit door to door from January 9 to 14 administering diethyl carbamazine citrate tablets to ...

The cost and the claims  Jan 3, 2006
Telegraph.co.uk, Contains: water, glycerol, Vitamin C, Vitamin E, sodium citrate, stabiliser (Xanthan gum), citric acid, sodium chloride (salt), preservative (sorbic acid ...

Manforce rated as No1 erectile dysfunction drug by ORG-IMS  Jan 3, 2006
India Infoline.com, As per ORG-IMS audit dated Oct’2005, the total market for ED related drugs in India is about 95 Crore with a yearly growth of 9%. Sildenafil citrate is the ...

Study: Exercise & Calcium Strengthen Bones  Jan 5, 2006
KOLD-TV, ...to be supplied by their food intake. They took Citracal calcium citrate in the study. The regimen includes six core exercises: Leg ...

Rachel Emrick avoids illness and derives energy from eating right  Dec 31, 2005
Lufkin Daily News, ...system was tweaked as she learned the body's ability to absorb nutrients depended on the supplement's chemical form — like calcium citrate, which cured her ...

Viagra's on the way to India, but there's stiff competition  Dec 21, 2005
Australian, Pfizer had been investigating the cardiovascular effects of sildenafil citrate when it stumbled upon its side effect as an impotence drug. ...

Viagra debuts in India at Rs 463  Dec 20, 2005
Financial Express, MUMBAI, DEC 20: Pfizer India on Tuesday announced the launch of its $1.7 billion erectile dysfunction (ED) drug Viagra (sildenafil citrate) in India, nearly ...

'Viagra misuse might make people go berserk'  Dec 27, 2005
Times of India, Viagra (sildenafil citrate) manufacturer Pfizer is launching the drug in the Indian market this week, seven years after it was introduced in global markets.

Pfizer set to launch Viagra next week  Dec 17, 2005
Sify, ...here. Penegra was the name under which Zydus Cadila launched its version of sildenafil citrate, the active ingredient in Viagra. ...

Counting on the Viagra brand in India  Dec 21, 2005
International Herald Tribune, ...are treatments. One tablet of Viagra, or sildenafil citrate, is sold every six seconds worldwide, according to Pfizer. But Viagra's ...

Human trials for new Viagra uses begin  Dec 21, 2005
Financial Express, MUMBAI, DEC 21: Pfizer India has commenced clinical trials in India on certain new uses of sildenafil citrate, the active ingredient in its blockbuster ...

Pfizer to bring products from global portfolio  Dec 22, 2005
Business Standard, The drug, sildenafil citrate, with serious contraindications is being launched in select cities as it is structured to be sold on the prescription of a ...

FDA Issues Approvable Letter for VIVITROL(TM) (Formerly VIVITREX(R ...  Dec 28, 2005
Finanzen.net, ...products in theUnited States: PROVIGIL(R) (modafinil) (C-IV), GABITRIL(R) (tiagabinehydrochloride), ACTIQ(R) (oral transmucosal fentanyl citrate) (C-II)and ...

Pfizer launches Viagra in India  Dec 20, 2005
Webindia123, Pfizer today announced the launch of VIAGRA (sildenafil citrate), their breakthrough treatment for Erectile Dysfunction (ED), in the Indian market. ...

Jharkhand Chemists to Boycott Viagra  Dec 30, 2005
MedIndia, Association (JCDA). The manufacturer of Viagra, which is chemically sildenafil citrate, is launching the product in India next week. Sinha ...

Druglords descend on R&D haven  Dec 25, 2005
Calcutta Telegraph, Similarly, Pfizer India, which launched the Viagra only last week, is also conducting human clinical trials on new uses of sildenafil citrate, the compound ...

Cephalon, Inc. Completes Acquisition of Zeneus Holdings Limited  Dec 22, 2005
Yahoo! News (press release) ...products in the United States: PROVIGIL® (modafinil) [C-IV], GABITRIL® (tiagabine hydrochloride), ACTIQ® (oral transmucosal fentanyl citrate) [C-II] and ...

Cephalon, Inc. Completes Acquisition of Zeneus Holdings Limited  Dec 22, 2005
Boursorama, ...products in the United States: PROVIGIL(R) (modafinil) [C-IV], GABITRIL(R) (tiagabine hydrochloride), ACTIQ(R) (oral transmucosal fentanyl citrate) [C-II] and ...

MGI PHARMA Provides Update on Aquavan(R) Injection Program; Top ...  Dec 21, 2005
Business Wire (press release), ...of four different initial bolus doses of Aquavan Injection (2.0, 5.0, 6.5, or 8.0 mg/kg) or midazolam (0.02 mg/kg) following pretreatment with fentanyl citrate ...

TAMIFLU: DANGEROUS AND INEFFECTIVE?  Dec 26, 2005
Free Market News Network, The oral suspension liquid, meanwhile, contains: oseltamivir; saccharin sodium (E954); sodium benzoate (E211); sodium dihydrogen citrate (E331 (a)); sorbitol ...

The many functions of calcium  Dec 26, 2005
New Straits Times, ...consider a calcium supplement. Calcium supplements are available in many forms and the citrate form is found to be better absorbed.

Cephalon, Inc. Announces Agreement with Ranbaxy Laboratories ...  Dec 22, 2005
Yahoo! News (press release) ...markets four proprietary products in the United States: PROVIGIL, GABITRIL® (tiagabine hydrochloride), ACTIQ® (oral transmucosal fentanyl citrate) [C-II] and ...

Preventing bone loss is best protection  Dec 13, 2005
Newsday, ...them at night. Calcium citrate is a better choice, in my opinion, but bone health is not really about the calcium. It's about the ...

Why Viagra Spam Floods Your Email  Dec 13, 2005
Emediawire (press release), ...product associated with spammers. Many overseas pharmacies are selling sildenafil citrate, the ingredient in Viagra. The product they ...

The Strong Connection Between Viagra and Spam  Dec 13, 2005
Cheap Web Hosting Directory, The strong connection between spam and Viagra may be as follows: Many overseas pharmacies are selling sildenafil citrate, the ingredient in Viagra. ...

Families sue over alleged pain patch deaths  Dec 31, 2005
Provo Daily Herald, ...of receiving them. The Duragesic patch is designed to deliver the pain killer fentanyl in controlled doses. Both lawsuits claim ...

Kin file suits over pain patch deaths  Dec 28, 2005
Salt Lake City Deseret News, ...the patch for two different medical conditions, but both were found dead in their homes within one or two days of receiving the Duragesic patch, which was ...

Family sues over Rx drug  Dec 14, 2005
Salt Lake City Deseret News, ...using to control pain. Duragesic distributor, ALZA Corp., is being sued by the family of Marilyn Titus, who died Dec. 14, 2003, at ...

DURECT Announces Positive Preliminary Results from Transdermal ...  Dec 26, 2005
PR Newswire (press release), The top-line preliminary results of this study showed that patients can be converted from the Duragesic(R) product to the TRANSDUR-Sufentanil product safely ...

Drug business making Johnson & Johnson sluggish  Dec 18, 2005
Chicago Tribune, Big seller Procrit is losing share to Amgen's competing anemia drugs, and new generic challengers have emerged for such products as the Duragesic patch for ...

Endo submits new studies to FDA on painkillers  Dec 22, 2005
philly.com, New versions would help the company compete in the $4.2 billion market for strong painkillers, which include OxyContin, Duragesic, and Avinza. ...

Hearing set for woman charged in death  Dec 21, 2005
The Southern, ...$1 million. According to information filed by federal prosecutors, Krieger allegedly provided a Duragesic gel patch on Nov. 22 containing ...

Police beat: Dec. 21  Dec 21, 2005
Annapolis Capital, There they found evidence linking her to the fake prescriptions for the Duragesic patches, which deliver an opioid painkiller through the skin. ...

Business Briefing  Dec 24, 2005
Sun-Sentinel.com, In September, the FDA rejected Noven's copy of Johnson & Johnson's Duragesic pain patch, based on concerns about possible overdoses. ...

Cephalon, Inc. Announces Agreement with Mylan Pharmaceuticals Inc. ...  Jan 10, 2006
PharmaLive.com (press release), ...markets four proprietary products in the United States: PROVIGIL, GABITRIL(R) (tiagabine hydrochloride), ACTIQ(R) (oral transmucosal fentanyl citrate) [C-II ...

FDA Issues Approvable Letter for VIVITROL(TM) (Formerly VIVITREX(R ...  Dec 28, 2005
Finanzen.net, ...products in theUnited States: PROVIGIL(R) (modafinil) (C-IV), GABITRIL(R) (tiagabinehydrochloride), ACTIQ(R) (oral transmucosal fentanyl citrate) (C-II)and ...

Cephalon, Inc. Completes Acquisition of Zeneus Holdings Limited  Dec 22, 2005
Yahoo! News (press release) ...products in the United States: PROVIGIL® (modafinil) [C-IV], GABITRIL® (tiagabine hydrochloride), ACTIQ® (oral transmucosal fentanyl citrate) [C-II] and ...

Cephalon, Inc. Completes Acquisition of Zeneus Holdings Limited  Dec 22, 2005
Boursorama, ...products in the United States: PROVIGIL(R) (modafinil) [C-IV], GABITRIL(R) (tiagabine hydrochloride), ACTIQ(R) (oral transmucosal fentanyl citrate) [C-II] and ...

MGI PHARMA Provides Update on Aquavan(R) Injection Program; Top ...  Dec 21, 2005
Business Wire (press release), ...of four different initial bolus doses of Aquavan Injection (2.0, 5.0, 6.5, or 8.0 mg/kg) or midazolam (0.02 mg/kg) following pretreatment with fentanyl citrate ...

Cephalon, Inc. Announces Agreement with Ranbaxy Laboratories ...  Dec 22, 2005
Yahoo! News (press release) ...markets four proprietary products in the United States: PROVIGIL, GABITRIL® (tiagabine hydrochloride), ACTIQ® (oral transmucosal fentanyl citrate) [C-II] and ...


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