Fentanyl: Potent opioid; Indication and pharmacodynamics


Pharmaceutical fentanyl is a synthetic opioid pain reliever, approved for treating severe pain, typically advanced cancer pain. It is 50 to 100 times more potent than morphine. It is prescribed in the form of transdermal patches or lozenges and can be diverted for misuse and abuse in the United States. 

However, most recent cases of fentanyl-related harm, overdose, and death in the U.S. are linked to illegally made fentany. It is sold through illegal drug markets for its heroin-like effect. It is often mixed with heroin and/or cocaine as a combination product—with or without the user’s knowledge—to increase its euphoric effects.
Fentanyl can slow or stop your breathing, and may be habit-forming.

Important Information




Fentanyl can slow or stop your breathing, and may be habit-forming. MISUSE OF NARCOTIC MEDICINE CAN CAUSE ADDICTION, OVERDOSE, OR DEATH, especially in a child or other person using the medicine without a prescription. Using this medicine during pregnancy may cause life-threatening withdrawal symptoms in the newborn. Fatal side effects can occur if you use this medicine with alcohol, or with other drugs that cause drowsiness or slow your breathing.

Indication

Fentanyl is used to treat breakthrough pain (sudden episodes of pain that occur despite round the clock treatment with pain medication) in cancer patients at least 18 years of age (or at least 16 years of age if taking Actiq brand lozenges) who are taking regularly scheduled doses of another narcotic (opiate) pain medication, and who are tolerant (used to the effects of the medication) to narcotic pain medications. Fentanyl is in a class of medications called narcotic (opiate) analgesics. It works by changing the way the brain and nervous system respond to pain.

Pharmacodynamics


Fentanyl provides some of the effects typical of other opioids through its agonism of the opioid receptors. As a Mu-receptor agonist, it binds 50 to 100 times more strongly than morphine.  Fentanyl can also bind to the delta and kappa opioid receptors but with a lower affinity. Its strong potency relative to morphine is largely due to its high lipophilicity, per the Meyer-Overton correlation. Because of this, it can more easily penetrate the central nervous system.

Fentanyl binds to opioid receptors— G-protein coupled receptors (GPCR) which regulate synaptic transmission. Binding of fentanyl activates the GPCR which initiates signalling to result in the inhibition of the release of nociceptive neurotransmitters. This inhibits the ascending pathways in the central nervous system to increase pain threshold by changing the perception of pain; this is mediated by decreasing propagation of nociceptive signals, resulting in analgesic effects




Fentanyl: Potent opioid; Indication and pharmacodynamics Fentanyl: Potent opioid; Indication and pharmacodynamics Reviewed by gafacom on February 05, 2020 Rating: 5

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