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845 > Opioid Analgesics Part I (Mechanisms/General Information) > Flashcards

Opioid Analgesics Part I (Mechanisms/General Information) Flashcards

1
Q

Placebo Meta-analytic Review

A
  • Placebo associated with decrease in self=reported pain
  • Hidden/blind injection of naloxone reverse placebo-induced analgesia
  • Nucleus accumbens DA release account for 25% of placebo analgesic effects
  • Placebos may NOT be an adequate negative control
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2
Q

Opium

A

Dried powdered mixture of 20 alkaloids obtained from unripe seed capsules of the poppy plant

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3
Q

Opiate

A
  • Drugs from opium

- Morphine (10%) and codeine (0.5%)

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4
Q

Opioid

A
  • All substances with morphine-like properties
  • Exogenous or endogenous
  • Generic term for this class of drugs
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5
Q

Analgesia

A

Without pain

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6
Q

Allodynia

A

Feels pain from non-painful stimuli (ex: touch)

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7
Q

Hypoalgesia

A

Reduced pain perception

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8
Q

Hyperalgesia

A

Increased pain perception

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9
Q

Narcotic

A

Induces sleep (narcosis)

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10
Q

Endorphins

A
  • Endogenous opioid peptide

- In spinal cord interneurons produce analgesia

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11
Q

Enkephalins

A
  • Endogenous opioid peptide

- In spinal cord interneurons produce analgesia

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12
Q

Nociceptive Pain

A

Pain receptors and transmission over intact nerves

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13
Q

Neuropathic Pain

A

Caused by damaged neural structures, doesn’t respond well to opioids

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14
Q

Integumental Pain

A
  • Skin, mucosa, muscles/joints, headache

- Controlled by NSAIDs and may be combined with narcotics

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15
Q

General NSAID MoA

A
  • Decrease synthesis of prostaglandins and release of bradykinin
  • Peripheral MoA
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16
Q

Visceral Pain

A
  • Within body cavities (thorax, abdomen)
  • Diffuse, hard to localize, referred to other sites
  • Best treated with opioids
  • Main action is on spinal cord and in upper CNS
  • NSAIDs aren’t as effective unless pain is associated with inflammation
17
Q

Pain/Neurogenic Inflammation

A
  • Components of tissue injury lower pain threshold by producing inflammation and hyperalgesia
  • Serotonin, histamine, bradykinin, and prostaglandins all contribute to inflammation
18
Q

Local Anesthetics MoA

A
  • Inhibit axonal action potential propagation

- Peripheral MoA

19
Q

Opioid Analgesics MoA

A
  • Work on CNS
  • Raise pain perception threshold and alter emotional response
  • No other sense are affected
20
Q

Ascending Pain Pathways

A
  • Perception

- Localization and discrimination of pain

21
Q

Descending Pain Pathways

A
  • Upper brain and brainstem

- Use descending serotonin and NE neruons to reduce pain transmission through dorsal horn of the spinal cord

22
Q

Opioid Site of Action

A
  • Glutamate and neuropeptides trasmit pain signal in dorsal horn of spine’
  • Mu opioid receptors are activated by enkephalins to decrease Ca++ influx in presynaptic neuron, which decreases glutamate release
  • Also causes an increase in K+ efflux to hyperpolarize the postsynaptic neuron
  • NE and 5HT activate presynaptic alpha2 and 5HT1A receptors to decrease calcium influx
23
Q

Specific Opioid Peptides

A
  1. Leu-/Met-enkephalins: amino acids found in brain, spinal cord, and adrenal medulla with NE and EPI
  2. Beta endorphin: amino acids found in pituitary and hypothalamus, released with ACTH in response to stress
  3. Dynorphins: amino acids found in neurons with diffuse projects (neuromodulators)
  4. Nociceptin/Orphanin FQ: amino acids resembling dynorphin, doesn’t act at classic opioid receptors
24
Q

Opioid Peptides Characteristics

A
  • Stores in vesicles and release by exocytosis
  • Requires energy, calcium, and an intact cytoskeleton to release
  • Polar, soluble in aqueous solvents
  • Circulate unbound in blood and tend to have a short half life
  • Can’t be given orally, only injection or through a mucous membrane if the peptides are small
  • Interacts with cell membrane receptors (can’t cross membranes)
25
Q

Mu Receptors

A

-u1 and u2

u1

  • Prototypic drug: most endogenous, natural or synthetic opioids
  • Proposed actions: supraspinal analgesia

u2

  • Prototypic drug: morphine
  • Proposed actions: respiratory depression and CV effects
26
Q

Delta Receptors

A
  • Prototypic drug: enkephalins

- Proposed actions: spinal analgesia

27
Q

Kappa Receptors

A
  • Prototypic drug: dynorphin

- Proposed actions: spinal analgesia, sedation, and miosis

28
Q

Sigma Receptors

A
  • Prototypic drug: N-allylnormetazocine

- Proposed actions: psycotomimetic effects

29
Q

Opium contains….

A
  • Morphine - analgesic**
  • Codeine - mild analgesic/cough suppressant**
  • Noscapine
  • Papaverine
  • Thebaine**
30
Q

Thebaine

A
  • No analgesic effect
  • Used in production of semisynthetic opioid morphine/codeine analogues
  • Includes oxycodone, hydrocodone, oxymorphone, buprenorphine, naloxone, naltrexone

845 (24 decks)

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