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65 Cards in this Set

  • Front
  • Back
What is pain?
An unpleasant sensory or emotional experience usually associated w/ actual or potential tissue dmg
What is analgesia?
A state in which no pain is felt despite the presence of a stimulus which is normally painful.
What are Analgesics?
Drugs that alleviate pain without impairing other sensory modalities.
What are pain receptors called?
Nociceptors
What nerve fibers mediate
-Sharp localized pain
-Dull, diffuse, ache/burn
Sharp = A-delta fibers

Dull = C fibers
Where in the spinal cord dorsal horn do they terminate:
-Adelta fibers
-C fibers
Adelta = in lamina I
C fibers = in lamina II
What is the pain mediated by Adelta and Cfibers called, and what NT is used in the spinal cord laminae I/II?
Adelta: Somatic - Glutamate

Cfiber: Visceral - Glutamate and Substance P
After the primary synapse of Adelta and Cfibers in the dorsal horn of the SC, where do the 2ndary neurons project?
To the thalamus
What are the ascending 2ndary neurons that mediate pain to the thalamus called?
Spinothalamic tracts
To what 3 sites do the pain sensations project after the thalamus?
-Limbic system
-Sensory/association cortex
What other tracts are involved in pain?
Descending tracts
Where do the descending pathways originate?
-Periaqueductal gray region of the midbrain
-Nuclei of rostro-ventral medulla
Where do the descending pathways synapse in the spinal cord? What is the tract in the SC called?
-Dorsolateral funiculus
-Terminates in the dorsal horn on ascending pain pathways
What do the descending pathways release, and what is their effect on ascending pain pathways?
-RElease NE, 5HT, Enkephalin
-Inhibit ascending pain
So what is the NT released by Adelta or C fibers when they synapse in the laminae I/II?
Glutamate - excitatory
What is the effect of serotonin release by descending fibers?
Excitatory - stimulates Enkephalin release
What effect do Enkephalin, Serotonin, and Norepinephrine all have on the ascending pain pathway activity?
Inhibitory
Where do the majority of narcotic analgesics work?
At descending pain pathways to inhibit pain perception
What are the 3 basic families of ENDOGENOUS opioid peptides?
-Enkephalin
-B-Endorphin
-Dynorphin
What is the Enkephalin precursor?
Proenkephalin
Where are Enkephalins distributed?
Widely throughout the CNS especially in interneurons associated with pain pathways
What is the Endorphin precursor?
Proopiomelanocorton (pomc)
Where are B-endorphins distributed?
-Hypothalamus
-NTS
-Anterior pituitary
How do the B-endorphins in the anterior pituitary behave?
Co-released with ACTH in response to stress
What is the Dynorphin precursor?
Prodynorphin
Where are longerchain dynorphins located?
-Colocalized with Vasopressin in hypothal and posterior pituitary
Where are shorter chain dynorphins located?
In CNS pain pathways in the spinal cord
How many opioid receptors are there, and to what superfamily do they all belong?
THREE - all are GPCR's
What are the 3 opioid receptor classes?
-Mu
-Kappa
-Delta
What is the G protein coupled to all 3 of the opioid receptors?
Gi
What are the 3 opioid receptors?
-Mu
-Delta
-Kappa
Where are Mu and Delta receptors located? What might this be responsible for?
In limbic areas - may be responsible for drug dependence
Where are Kappa receptors located? What might this be involved in?
In limbic areas - may be involved in dysphoria
What is the natural endogenous ligand of Mu receptors?
-B-endorphin especially
-Enkephalins also
What is the natural endogenous ligand of Kappa receptors?
Dynorphin
What is the natural endogenous ligand of Delta receptors?
-Enkephalins mostly
-B-endorphin also
How many drugs are agonists of the Mu receptor? What acronym is for them?
7 - MMMFOCH
What is MMMFOCH
-Morphine
-Methadone
-Meperidine
-Fentanyl
-Oxycodone
-Codeine
-Heroin
What are the 2 antagonists of the mu receptor?
-Naloxone
-Naltrexone
What is the main Kappa receptor drug to know?
Nalbuphine
Where is the Delta receptor well known for being localized in addition to limbic areas?
Vas deferens
What is the drug ligand of the delta receptor?
There are none
What does the term "Narcotic" refer to?
-Morphine like drugs
-Some other abused substances
What effects do narcotics produce as drugs?
-Stuporous sleeplike state
-May or may not be analgesic
What is a better term than Narcotic, why?
Opiate - because these are what there are actually receptors to - there are no "narcotic" receptors
What are Opiates?
Drugs derived from opium or have a morphine-like pharmacologic profile
What is the definition of Opioid?
Referring to ALL opiates, agonist-antagonists, and endogenous peptides.
How are opioids administered?
Can be parenteral or oral based on how much FPE they are subject to
What 2 opioids particularly undergo extensive FPE?
-Morphine
-Naloxone
How much lower is the oral potency of Morphine and Naloxone due to their high FPE?
1/3 that of parenteral potency
How do you overcome the low oral potency and bioavailability of Morphine and Naloxone?
just give MORE
What IS morphine?
Opioid agonist of Mu receptor
What IS naloxone?
Opioid antagonist of Mu
What is the onset of action of opioids determined by?
Their lipophilicity
Which has higher lipophilicity; heroin or morphine?
Heroin!
What 2 factors determine the duration of action of opioids?
-Lipophilicity
-Rate of elimination
How does lipophilicity affect duration of drug action?
The more lipophilic, the faster it will redistribute away from its active site.
What is important to remember about the metabolism of some of the opioids?
Metabolism will produce active drugs
What are 2 opioids that are converted to active drugs by metabolism?
-Codeine
-Heroin
What is the structure of Heroin and its active metabolite?
Heroine = Diacetylmorphine
Metabolite = monoacetylmorph
What is the mechanism by which the opioids are metabolized?
Common mechanisms - to increase polarity and decrease activity
How many effects do the opioid agonists have? Acronym?
NINE - ScARE SPENC
What are the nine effects of the Opioid agonists?
-Suppress cough
-Analgesia
-Respiratory depression
-Euphoria
-Sedation
-Pupil constriction
-Endocrine effects
-Nausea
-Constipation
What are 2 ways in which the opioid agonists are analgesic?
-Decrease pain perception
-Decrease appreciation of pain
What type of pain do the opioids alleviate?
Nociceptive - NOT neuropathic