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Pharmacology > Opioids > Flashcards

Opioids Flashcards

1
Q

Opiate

A

drugs derived from opium. Examples include morphine, thebaine, and codeine

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2
Q

Opium

A

Substance derived from the seeds of the opium poppy (Papaver somniferum)

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3
Q

Opioid

A

Term used to describe ALL natural, synthetic, or semi-synthetic compounds that bind to opioid receptors. May be agonists or antagonists. Endogenous peptides may be termed opioids.

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4
Q

Narcotic

A

Derived from the Greek word for stupor. Narcotic has historically been used to describe opioids. May be used to describe any drug that causes dependence (legal or popular press)

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5
Q

Opioid receptors are G-protein-coupled receptors. True or False.

A

True

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6
Q

Location of opioid receptors

A
  • Cerebral cortex, thalamus, PAG, spinal cord, dorsal horn
  • Peripheral sensory neurons in inflammation
  • Non-neurological tissue (immune cells)
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7
Q

Opioid Receptor Effectors

A
  • Receptor dependent potassium channels
  • Voltage-gated calcium channels
  • Inhibit adenylate cyclase (decrease cAMP)
  • Phospholipase C
  • MAP kinase
  • K+
  • Inhibit release of acetylcholine, glutamic acid, dopamine, serotonin, substance P, and norepinephrine
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8
Q

Opioid Receptor Subgroups

µ

A
  • Activated by morphine
    • Miosis, analgesia, sedation, bradycardia, hypothermia, respiratory depression, physical dependence
  • Endomorphins
    • Ednogenous molecules that are produced by the body that react with µ receptors
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9
Q

Opioid Receptor Subgroups:

kappa

A
  • Ketocyclazine
    • Miosis, sedation/psychomimmetic effects, anti-ADH, neuroprotective
  • Spinal, peripheral distribution
  • Dynorphines
    • Endogenous molecules that ineract with Kappa receptors
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10
Q

Opioid receptor subgroups:

Delta

A
  • Central (limbic, cerebral, spinal cord)/pierpheral neurons, smooth muscle, lymphocytes
  • Emotional behavior, immune function, may MODIFY analgesia, ischemic preconditioning, proconvulsant/antidepressants
  • Enkephalins
    • Ednogenous molecule that interacts with delta receptors
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11
Q

Nociceptin Receptor (orphanin FQ receptor)

A
  • High structural homology to µ, kappa, and delta recepotrs
  • Low affinity for traditional opioid agonists
    • Buprenorphine may have some activity
  • Nociceptin/orphanin
    • Endogenuos opioid
    • unique pain modifying and behavioral properties (food intake, memory)
      • Antiopioid (pronociceptive) effects
    • May affect dopamine/GABA mediated transmission
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12
Q

Sigma receptor

A
  • No structural similarity to opioid recepotrs
  • SKF-10,047
    • Mydriasis, tachypnea, tachycardia, hallucinations, mania, vasomotor responses
  • Activated by drugs unrelated to opioids (phencyclidine, haloperidol)
  • Activation not reversed by naloxone or naltrexone
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13
Q

Which drugs reverse opioids?

A
  • Naloxone
  • Diprenorphine
  • Naltraxone
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14
Q

Epsilon receptor

A
  • Opioid growth factor receptor
    • little sequence homology to other opioid receptors
    • Regulation of tissue growth
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15
Q

What are the three endogenous opioid peptides and name their receptors

A
  1. endorphine - µ receptor
  2. dynorphin - kappa receptor
  3. enkephalin - delta receptor
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16
Q

The three endogenous opioid peptides initially identified (endorphines, enkephalines, and dynorphins) are derived from the same precursors. True or False.

A

FALSE - they are derived from three different precurosrs

17
Q

three families of endogenous opioid peptides that were initially identified and described extensively (endorphins, enkephalins, and dynorphins) share what in common?

A

They all share a common amino-terminal sequence: Tyr-Gly-Gly-Phe-(Met or Leu)

18
Q

Endomorphin

A
  • This is another endogenous opioid that do not contain the characteristic opioid AA core sequence
  • High affinity and selectivity for the µ receptor
19
Q

Endogenous Morphine

A
  • Neuroblastoma cells have the ability to synthesize morphine
  • Has been detected in tissues and fluids
20
Q

CNS effects

A
  • Sedation
    • Dysphoria
    • Excitment can occur in the horse and cat
  • Seizures
    • high doses
  • Respiratory depression
  • Stimulate/inhibit chemoreceptor trigger zone (vomiting/nausea)
  • Tolerance/physcial dependence
21
Q

GI effects

A
  • Vomiting/nausea
  • Increased GI tone (nonpropulsive)
    • tends to cause constipation
  • Decreased small intestinal secretion/increased water absorption
    • Loperamide -peripheral agonist
  • Decreased pancreatic biliary secretions
  • Postoperative ileus
22
Q

Side effects on body temp

A

Decreased body temp, except increased in cats

23
Q

opioids are immunosuppressive. True or False.

A

True

24
Q

Opioids increase histamine release/cuase pruritis. True or False.

A

True

25
Q

Opioids increase sphincter tone. True or False.

A

True

26
Q

Enkephalin Pentapeptides

A
  • Precursor: proenkephalin
  • [met]enkephalin
  • [leu]enkephalin
  • High affinity for the delta receptor
  • Low affinity for the kappa receptor
27
Q

Dynorphins

A
  • Precursor: prodynorphin
  • The dynorphins appear to be the endogenous receptor for the kappy recepotr
28
Q

Edorphins

A
  • Precursor: propriomelanocortin
    • Also precuror for adrenocorticotropic hormone, melanocyte-stimulating hormone, and beta-lipotropin
    • Derived from the hypothalamus/neurohypophysis
  • Beta-endorphin
  • Similar affinity for delta and mu receptors and low affinity for kappy receptors
29
Q

Morphine has a high affinity for which receptor?

A

MU

30
Q

Methadone has a high affinity for which receptor?

A

MU

31
Q

Etorphine has a high affinity for which receptors?

A

MU, delta, and kappy

Pharmacology (10 decks)

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