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Fentanyl treats severe, ongoing pain that cannot be controlled with other medicines. This medicine is a narcotic pain reliever.
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Fentanyl for sale was first made by Paul Janssen in 1960, following the medical inception of pethidine (also known as meperidine, marketed as Demerol) several years earlier. Janssen developed fentanyl by assaying analogues of the structurally related drug pethidine for opioid activity. The widespread use of fentanyl triggered the production of fentanyl citrate (the salt formed by combining fentanyl and citric acid in a 1:1 stoichiometry), which entered medical use as a general anaesthetic under the trade name Sublimaze in the 1960s. Following this, many other fentanyl analogues were developed and introduced into medical practice, including sufentanil, alfentanil, remifentanil, and lofentanil.
Fentanyl is a synthetic, lipophilic phenylpiperidine opioid agonist with analgesic and anesthetic properties. Fentanyl selectively binds to and activates the mu-receptor in the central nervous system (CNS) thereby mimicking the effects of endogenous opiates. Activation of the mu-subtype opioid receptor stimulates the exchange of GTP for GDP on the G-protein complex and subsequently inhibits adenylate cyclase. This causes a decrease in intracellular cAMP which inhibits cAMP-mediated calcium influx into the cell via the calcium channels and thereby results in hyperpolarization and reduced neuronal excitability.
fentanyl citrateThe citrate salt of fentanyl, a synthetic opioid related to the phenylpiperidines with analgesic and anesthetic properties. Fentanyl exerts its analgesic effect by selectively binding to the mu-opioid receptor in the central nervous system (CNS), thereby mimicking the effects of endogenous opiates. Additional pharmacological effects of fentanyl include anxiolysis, euphoria, feelings of relaxation, respiratory depression, constipation, miosis, and cough suppression. Check for active clinical trials using this agent. (NCI Thesaurus)
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