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Pharmacology of Analgesics
Biochemical and Molecular Principles of Drug Action Biochemical and Molecular Principles of Drug Action
23
Pharmacology
Professional
04/10/2012

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Term
Pain
Definition
the end perceptual consequence of the neural processing of particular sensory information.
Pain serves a protective function by alerting a person to presence of health problems
Typically arises in periphery and is transferred under multiple controls through sensory relays in the CNS to cortex
Term
Nociceptors
Definition
primary sensory neurons because they respond to noxious stimuli, are “high threshold” because they require strong potentially tissue damaging stimulus to depolarize their terminals
Term
Vanilloid receptor 1 and 2
Definition
heat response
Na/Ca influx
Term
Nociceptor Neurons
Definition
Nociceptor neurons respond to thermal, mechanical and multiple chemical activator
Chemical ligands that evoke somatosensory responses: protons, potassium ions, ATP, amines, cytokines, chemokines, nerve growth factor, bradykinin
ASICs- acid sensitive ion channels
Term
Fentanyl
Definition
synthetic opioid; binds particularly μ- receptor; 100x more potent than morphine; short duration of action 15-30min
Term
Buprenorphine
Definition
classified as partial agonist at μ- receptors; acts like morphine in naïve patients but precipitates withdrawal in morphine users
Major use is opioid detoxification; but less severe and shorter duration than methadone
Term
Naloxone
Definition
antagonist to μ-, κ-, δ- receptors; 10-fold higher affinity μ-, κ- receptors reveres the effects of agonists; will precipitate symptoms of opiate withdrawal
Used to reverse coma and respiratory depression of opioid overdose (within 30 seconds of iv)
Produces no pharmacological effects on normal individuals
Term
Naltrexone
Definition
antagonist to μ-, κ-, δ- receptors; 10-fold higher affinity μ-, κ- receptors reveres the effects of agonists; will precipitate symptoms of opiate withdrawal
Used to reverse coma and respiratory depression of opioid overdose (within 30 seconds of iv)
Produces no pharmacological effects on normal individuals
Term
Morphine Mechanism of Actions
Definition
high affinity at the μ-receptor; acts at the κ-receptor in laminae I and II in the dorsal horn of spinal cord; decreases release of substance P; inhibits release of many excitatory neurotransmitters carrying nociceptive painful stimuli
Term
Therapeutic Uses of Morphine
Definition
Analgesia
Treatment of Diarrhea
Relief of Cough: codeine and dextromethorphan more commonly used
Treatment of Pulmonary Edema: iv morphine relieves dyspnea caused by pulmonary edema associated with left ventricular failure, possibly by vasodilation effect
Term
Adverse Effects of Morphine
Definition
Respiratory depression
Tolerance and physical dependence: repeated use
Drug interactions: rare but depressant actions of morphine are enhanced by phenothiazines (anti-psychotics), MAOIs, and tricyclic anti-depressants
Vomiting
Histamine-enhanced hypotensive effects
Elevated intracranial pressure
Urinary retention
Term
Meperidine
Definition
synthetic opioid; binds particularly μ- and κ- receptor.
Used for acute pain
Causes respiratory depression but no significant cardiovascular action.  peripheral resistance and an  blood flow.
Dilates cerebral blood vessels,  CSF pressure
Uses
Analgesia
Not used for treatment of diarrhea
Toxic metabolite causes neurotoxic properties
Adverse effects
Anxiety, tremors, muscle twitches, rarely convulsions
Term
Methadone
Definition
synthetic opioid, binds μ- receptor; less euphoria and longer DOA than morphine; NMDA antagonist
Uses
Neurogenic pain (is that which arises from a primary disorder, trauma, or dysfunction of neural afferent structures)
Control withdrawal of dependent abusers from heroin and morphine (milder and more protracted than other opioids)
Adverse effects
Can produce physical dependence like morphine but less neurotoxicity
Can cause torsades de pointes
Term
Morphine
Definition
Term
Oxycodone
Definition
Term
Hydrocodone
Definition
Term
Methadone
Definition
Term
Fentanyl
Definition
Term
Meperidine
Definition
Term
Butorphanol
Definition
Term
Burenorphine
Definition
Term
Naloxone
Definition
Term
Naltrexone
Definition
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