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Investigational Drug Details

Drug ID: D231
Drug Name: Fentanyl
Synonyms:
Type: small molecule
DrugBank ID: DB00813
DrugBank Description: Fentanyl, a potent opioid agonist, was developed in the 1950s to fill a need for strong and rapid analgesia.[A179542] Because of these characteristics, fentanyl is commonly used to treat chronic cancer pain or in anesthesia.[Label,L6598,L6601,L6604,L6607,L922,L6610,L6613] Fentanyl is related to other opioids like [morphine] and [oxycodone]. Fentanyl's high potency has also made it a common adulterant in illicit drugs, especially heroin.[A179542] In 2017, 47600 overdose deaths in the United States involved some opioid (over 2/3 of all overdose deaths).[L6748] Opioid overdoses kill an average of 11 Canadians daily.[L6751] Fentanyl was FDA approved in 1968.[Label,L6598,L6601,L6604,L6607,L922,L6610,L6613]
PubChem ID: 3345
CasNo: 437-38-7
Repositioning for NAFLD: Yes
SMILES: CCC(=O)N(C1CCN(CCC2=CC=CC=C2)CC1)C1=CC=CC=C1
Structure:
InChiKey: PJMPHNIQZUBGLI-UHFFFAOYSA-N
Molecular Weight: 336.4705
DrugBank Targets: Mu-type opioid receptor; Delta-type opioid receptor; Kappa-type opioid receptor; P-glycoprotein 1
DrugBank MoA: Fentanyl binds to opioid receptors, especially the mu opioid receptor, which are coupled to G-proteins.[A179533] Activation of opioid receptors causes GTP to be exchanged for GDP on the G-proteins which in turn down regulates adenylate cyclase, reducing concentrations of cAMP.[A179533] Reduced cAMP decreases cAMP dependant influx of calcium ions into the cell.[A179533] The exchange of GTP for GDP results in hyperpolarization of the cell and inhibition of nerve activity.[A179533]
DrugBank Pharmacology: Fentanyl produces strong analgesia through its activation of opioid receptors.[Label,A179533] It has a duration of action of several hours and a wider therapeutic index as patients develop tolerance to opioids.[Label] Fentanyl is associated with a risk of addiction and abuse and should not be mixed with alcohol or benzodiazepines.[Label,L6598,L6601,L6604,L6607,L922,L6610,L6613]
DrugBank Indication: Fentanyl intravenous or intramuscular injections are indicated for short term analgesia during induction, maintenance, and recovery from general or regional anesthesia.[Label] These injections are also used with a neuroleptic for premedication, induction, and as an adjunct to maintenance of anesthesia.[Label] Finally, fentanyl intravenous or intramuscular injections are used with oxygen for anesthesia in high risk patients.[Label] Fentanyl sublingual tablets, transmucosal lozenges, buccal tablets, sublingual sprays, transdermal systems, and nasal sprays are indicated for the management of breakthrough pain in opioid tolerant cancer patients who require around the clock pain management.[L6598,L6601,L6604,L6607,L922,L6610]
Targets:
Therapeutic Category:
Clinical Trial Progress:
Latest Progress: