Week 11: Opioids and Cannabinoids Flashcards

1
Q

Naturally occurring opioids

A
  • Morphine (Extract from opium resin)
  • Codeine
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2
Q

Semisynthetic opioids

A
  • Semisynthetic: Synthesized w/ naturally occurring opioid as base
  • Bureprenorphine Diacetlymorphine (Heroin)
  • Hydrocodone (Vicodin)
  • Oxycodone (Oxycontin)
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3
Q

Fully synthetic

A
  • Fully synthetic: Fully synthesized in lab (no structural similarity w/ naturally occurring/completely independent from morphine/codeine)
  • Significant contribution to opioid epidemic
  • Fentanyl
  • Levacetylmethadyl (LAAM)
  • Methadone (Dolophine)
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4
Q

Opioids and the BBB

A
  • Morphine and heroin easily cross the BBB
  • Heroin > morphine
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5
Q

Opioid absorption

A
  • Differ in lipid solubility
  • Primarily metabolized in liver, often producing metabolites that have bio effects
  • Active metabolites depend on parent compound
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6
Q

Main metabolites

A
  • Morphine –> Morphine-6-glucuronide
  • Codeine –> Morphine –> Morphine 6 glucuronide
  • Heroin –> Monoacetylmorphine –> Morphine –> Morphine-6-glucoronide
  • Acetylcodeine –> Codeine –> Morphine –> Morphine-6-glucoronide
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7
Q

Opioid elimination

A
  • Elimination rate of opioids varies from drug to drug
  • Methadone takes up receptor heroin uses, weakening heroine effects
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8
Q

Endogenous opioid system

A
  • Neuropeptide NTS: System includes opioid NTs and receptors
  • Propeptide: Large chain of amino acids; propeptides for eventual neuropeptide
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9
Q

Common effect in opioid receptors

A

Analgesia (help respond to pain & inflammation)

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10
Q

Opioid receptors

A
  • G-protein-coupled metabotropic receptors
  • Reduce metabollic activity within neurons
  • Inhibitory mechanism = activation of inwardly rectifying K+ channels (support maintenance of cell at baseline)
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11
Q

Where are opioid-synthesizing neurons located in the CNS?

A
  • Cerebral cortex
  • Stratum
  • Arcuate nucleus
  • Nucleus of solitary tract
  • Rosffal ventromedial medulla
  • Dorsal hor
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12
Q

Where are opioid receptors located in the CNS?

A
  • Thalamus
  • Nucleus accumbens
  • Amygdala
  • Hippocampa formation
  • Hypothalamus
  • Periaqueductal gray
  • VTA
  • Locus ceruleus
  • Nucleus ambiguus
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13
Q

Opioid effects in reward circuitry

A
  1. Decreases/inhibits GABA release in VTA
  2. Increases Dopamine neuroactivity along dopamine neuron to NA
  3. Increased dopamine lvls = increased reinforcement effects
  4. Less GABA activity = more reinforcing effects
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14
Q

Pain system

A

Nociceptors —> dorsal horn –> spinothalamic tract –> thalamus –> somatosensory cortex/limbic system

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15
Q

Where do input and output pain signals meet?

A

Dorsal horn (come into brain and come out of spinal cord into PNS)

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16
Q

Most of the opioid drugs used act on ____ opioid receptors

A
  • mu (symbol)
  • Psychoactive effects depend on this
17
Q

Pure opioid receptor agonists

A
  • Produce full agonist actions at mu receptor
  • Enhances mu activation
  • Ex. Fentanyl and morphone
18
Q

Partial opioid recept agonists

A
  • Produce partial agonist actions at mu opioid receptors
  • Enhances mu activation
  • Ex. Buprenorphine
19
Q

Pure opioid receptor antagonists

A
  • Act as full-receptor antagonists at mu receptor
  • Fails to activate mu
  • Ex. Naloxone and naltrexone
20
Q

Mixed opioid receptor agonist-antagonists

A

Exhibit agonist actions at some receptors and antagonist actions at others (ex. Pentazocine)

21
Q

Subjective effects of opioid agonists

A
  • Rush: Initial & rapid onset of euphoria
  • High: Feelings of joy & ease
  • Nod: Calm, disinterest, unaware
  • Straight: Normalcy b/w craving opioid and feeling euphoric/other positive effecfts
22
Q

Conditioned place preference

A
  • Demonstrate a preference for the compartment they previously received an injection of heroin, demonstrating its reinforcing and associative properties
  • Strongly prefer place they experienced morphine
23
Q

____ ____ receptors prevented morphine-induced CPP

A
  • Blocking NMDA
  • Also exhibit w/ NMDA inhibition
24
Q

Opioid overdose

A
  • Sever respiratory depression, weakness, weak pulse, bluish colour to lips and skin, inability to talk, and potentially, unconsciousness
  • Respiratory depression from inhibitory effects in the medulla
  • More severe than w/ ethanol b/c of dosage/concentration required
25
Q
A