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79 Cards in this Set

  • Front
  • Back
agent derived from opium
all agents acting on morphine receptors, including antagonists
opioid receptors
1) mu
2) delta
3) kappa
4) sigma
5) epsilon
opioid receptors all belong to what?
G protein-coupled class of receptors
What are endogenous ligands for opioid receptors?
peptides (with varying affinities for each receptor type)
opioid receptor activity
1) inhibitory
2) decreasing intracellular cAMP
3) excitatory (very low doses)
excitation of G stimulatory protein will cause what?
1) increase activity of AC (adenylyl cyclase) and cAMP
2) increase protein kinase A
3) decrease K conductance
4) increase Ca conductance
5) increase action potential
6) increase transmitter release
7) excitatory effects
inhibition of G(i)
decrease the activity of adenylyl cyclase/cAMP
inhibition of G(o)
1) increase K conductance
2) decrease Ca conductance
3) decrease action potential
4) decrease transmitter release
5) inhibitory effects
1) mu receptor
1) analgesia
2) resp. depression
3) euphoria
4) miosis
5) physical dependence
6) decreased GI motility
2) kappa receptor
1) supraspinal analgesia
2) sedation
3) dysphoria (psychoses)
3) delta receptor
analgesia (spinal?)
4) sigma receptor
1) dysphoria
2) hallucinations
1) mu receptor locations
1) brainstem
2) medial thalamus
3) some in spinal cord
2) kappa receptor locations
1) mainly in the dorsal horn of the SC
2) some in the brainstem medullary reticular formation
3) delta receptor locations
mainly in the limbic system
4) sigma receptor locations
mainly in the hippocampus and amygdala of the limbic system
endogenous opioids derived from what?
precursor polypeptides
polypeptides include:
1) endorphines
2) dynorphines
3) enkephalins
polypeptides deffer in chain length, but share:
same first few AA's (61-65)
Is endomorphine polypeptide?
No, it is TETRApeptide
newly discovered
mu receptor selective
endogenous opioids act as:
1) NTM
2) neuromodulators
3) neurohormones
4) body's pain modulators
~65% of opioid receptor homology exists among:
1) mu
2) delta
3) kappa
analgesia mediated via receptors located in the:
1) dorsal horn of SC
2) periaqueductal gray matter
3) thalamus
ventral brainstem receptors mediate effects on:
1) coughing
2) vomiting
3) respiration
4) pupillary diameter
hypothalamus controls what?
neuroendocrine functions
limbic system controls what?
mood and behavioral effects
peripheral mu receptors associated with:
GI tract
4 primary interaction of opioid ligands with opioid receptors:
1) agonist
2) antagonist
3) partial agonist
4) mixed agonist/antagonist
partial agonist
binds to the receptor, but produces less than maximal response
mixed agonist/antagonist
binds to more than one type of opioid receptor, acting as an agonist at one, and an antagonist at others
central opioid effects
1) neuronal activity - <
2) analgesia
3) resp. depression
4) mood alteration
5) sedation
6) miosis
7) N/V
8) antitussive
9) endocrine (inhibits LHRH secretion)
peripheral opioid effects
1) histamine release
2) venous dilation
3) smooth muscle contraction
4) inhibition of Ach release
common opioid uses:
1) analgesia
2) pre-op sedation
3) anesthesia
4) epidural
5) diarrhea
6) cough suppression
7) opioid addiction withdrawal
8) opioid overdose (antagonist)
major opioid SE
1) resp. depression
2) N/V
3) hypothermia
4) constipation
5) histamine release
6) muscular rigidity
muscular regidity is due to:
inhibition of dopamine release in the striatum (Parkinson-like)
ADME of the opioids
1) most are well absorbed from GI tract
2) large 1st-pass metabolism (PO)
3) most distributes well
4) most cross placenta well
excretion of the opioids mainly via:
renal and biliary mechanisms of metabolized forms
opioid agonists #1
1) morphine (MS contin)
2) hydromorphone (Dilaudid)
3) Oxymorphone (Numorphan)
4) Codeine (Tylenol with Codeine)
5) Hydrocodone (Vicodine)
6) Oxycodone (Oxycontin)
opioid agonists #2
1) Heroin
2) Levorphanol (Levo-Deomoran)
3) Dextromethophan (Dimetane)
4) Meperidine (Demerol)
5) Methadone (Dolophine)
6) Propoxyphene (Darvon)
opioid agonists #3
1) Fentanyl (Sublimaze)
2) Sufentanil (Sufenta)
3) Alfentanil (Alfenta)
morhine is natural alkaloid from:
Papaver somniferum
morphine acts primarily at:
mu receptors (some kappa)
morphine develop
rapid tolerance
1) diacetylmorohine
2) semisynthetic
3) easily prepared from morphine
4) twice as potent as morphine
5) enters CNS rapidly, cause euphoria
6) not approved for clinical use
1) 1/10 potency of morphine
2) little risk of addiction or resp. depression
3) partially converted to morphine in the body
4) potent antitussive
Oxycodone (Oxycontin)
1) twice as potent as morphine
2) high euphoric liability
3) 160 mg, extended release tab. - widely abused (Hillbilly Heroin)
4) many deaths linked to chewing the extended release form
Levorphanol (Levo-Dromoran)
1) very potent synthetic morphine analgesic congener (5X)
2) less constipating
3) longer lasting
Dextromethorphan (Dimetane)
1) a dextro-rotary isomer
2) no analgesic activity
3) effective antitussive
Meperidine (Demerol)
1) most widely used synthetic congener
2) 1/10 as potent as MS
3) shorter duration
Why Meperidine frequently abused?
because it does not cause miosis, hard to detect
Meperidine are metabolized to :
1) CNS stimulant
2) potential Sz with renal pt
Meperidine are contraindicated with:
MAOI therapy
Methadone (Dolophine)
1) same potency as MS
2) less sedation than MS
3) longer duration of action (slower elimination)
4) used to counter withdrawal symptoms
Propoxyphene (Darvon)
1) structurally r/t MS
2) less than 1/10 as potent as MS
3) properties similar to other opioid
concern for Propoxyohen (Darvon)
questions have been raised concerning it's benefit in dose strengths found in most products
Fentanyl (Sublimaze)
1) chemically r/t meperidine
2) ~80X as potent as MS
3) continuous epidural
4) transdermal analgesia
advantage of Fentanyl is:
it's short half-life of redistribution (12.5 min)
potency of Fentanyl
1) Sufentanil (800X)
2) Fentanyl (80X)
2) Remifentanil (80X)
4) Alfentanil (20X)
Remifentanil (Ultiva)
selective mu-receptor agonist
(almost 100 % at mu-receptor)
Remifentanil differs from other Fentamyl derivatives by having:
an ester-linkage
1) short duration due to hydrolysis by non-spe. esterases
2) rapid recovery
opioid antagonists act by blocking:
mu receptors mainly (some kappa blockade)
opioid antagonists block:
1) analgesic
2) respiratory
3) euphoric
4) miosis
5) hypotension
6) smooth muscle actions of opioids
7) endogenous beta-endorphine
8) enkephalins
clinical use of opioid antagonists:
to reverse opioid-induced resp. depression and in the Tx of "addicts"
Naltrexone (Trexan)
Nalmefene (Revex)
1) similar with Narcan
2) longer half-life
3) given orally
Buprenorphine (Buprenex)
1) partial opioid agonist
2) shares structural components of Codeine and Naltrexone
3) binds to mu receptors, and elicits a weaker maximal response
use of Buprenorphine
1) less abuse potential
2) to conteract Heroin and Morphine addiction without causeing fullblown withdrawal symptoms
1) Nallorphine (Nalline)
2) Levallorphan (Lorfan)
1)mixed opioid agonist/antagonists
2) mu receptor antagonists
3) kappa receptor weak agonists
1) Nallorphine (Nalline)
2) Levallorphan (Lorfan)
block mu receptor mediated analgesia and euphoria
1) Nallorphine (Nalline)
2) Levallorphan (Lorfan)
kappa induced analgesia and sedation
large doses of Nallorphine and Levallorphan may cause:
dysphoria and hallucinations
Pentazocine (Talwin) and Nalbuphine (Nubain)
have similar actions, but are stronger kappa mediated analgesics
Tramadol (Ultram)
1) newer analgesices
2) structural similarities to opioids and NSAIDs
3) analgesic strength similar to Codeine-Acetaminophen agents
Tramadol (Ultram) acts to block re-uptake of:
serotonin and NE in central synapses, which then decreases pain info transmission in the brain
both the parent compound and an active metabolite of Tramadol have:
weak affinity for mu receptors, but their analgesic effect is not entirely reversed by Naloxone
Tramadol (Ultram) can cause:
1) dizziness
2) sedation
3) Sz
4) hallucinations
neuroleptic anesthesia: Butyrophenone
1) Droperidol - D2 blocker with antiemetic
2) Opioid (ex. Fentanyl)
3) N2O
4) used in dental office
New therapeutic possibilities
1) use of peptide-type receptor agonists for pain relief (designed to target specific receptor sub-types)
2) transplantation of adrenal medullary chromaffin cells into the spinal subarachnoid space
transplantation of adrenal medullary chromaffin cells
1) secrete opioid peptides
2) to provide long-term pain relief to chronic pain sufferes w/o exogenous opioid SE's