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JT- PHARM > Opiods 4-7 > Flashcards

Opiods 4-7 Flashcards

1
Q

What are opiates?

A

derived from opium (morphine, codeine, and variety of related alkaloids)

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2
Q

What are opioid?

A

all agonists and antagonists that have alkaloid structures in addition to naturally occurring and synthetic peptides that bind to opioid receptors

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3
Q

What are narcotics?

A

any drug that induces sleep; then used to describe strong opiate analgesics; and now wide variety of opioid and nonopioid abused substances

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4
Q

What are the opioid binding sites in the CNS?

A

Mu, kappa, delta

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5
Q

What kinda protein are opioid receptors ?

A

They are coupled G proteins.

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6
Q

What do opioid receptors inhibit?

A

Adenylyl cyclases.

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7
Q

What is the effect of inhibiting adenylyl cyclases?

A

It turns off the production of ATPs and puts the cell to sleep.

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8
Q

What is decreased by opioid receptors?

A

Conduction of Ca channels.

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9
Q

What is inhibited from primary afferent sensory neurons in the spinal cord?

A

Substance P release.

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10
Q

What channels do opioids open to lead to hyperpolarization?

A

K channels.

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11
Q

What does hyperpolarization prevent?

A

Excitation or propagation of action potentials.

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12
Q

What is the interaction between NMDA receptors and mu receptors?

A

Mu receptors appear to block NMDA receptors.

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13
Q

What are roles of opioid receptors?

A
  • They are coupled G protein.
  • When they are activated –> they inhibit adenylyl cyclase –> decrease cAMP –> decrease conduction of Ca channels –> impair AP and neurotransmitter release –> inhibit substance P from being released from primary afferent sensory neurons in the spinal cord and peripheral terminals –> reduce perception of pain.
  • Open K channels –> hyperpolarization –> decrease AP
  • Block NMDA receptors (by mu receptors)
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14
Q

What cause desensitization in the context of opioids?

A

Prolonged activation

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15
Q

What is internalization regarding opioid receptors?

A

Removal of receptors from the cell membrane without reduction in total number of receptors.

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16
Q

What does recycled/downregulation refer to?

A

Reduction in total number of receptors.

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17
Q

What is tolerance in relation to opioids?

A

Loss of effectiveness due to reduced receptor synthesis and altered drug metabolism.

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18
Q

What are the properties of chronic opioid users?

A
  • Desensitization
  • Internalization
  • Downregulation/recycled
  • Tolerance
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19
Q

What are endomorphines?

A

Endogenous opioid ligands that act on mu receptors.

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20
Q

What endogenous opioid ligands that act on mu receptors?

A

Endomorphines
E-endorphin

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21
Q

What endogenous opioid ligands that act on kappa receptors?

A

Dynorphin-A

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22
Q

What endogenous opioid ligands that act on delta receptors?

A
  • Methionine-enkephalin
  • leucine-enkephalin
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23
Q

What are the effects of mu receptors?

A

Mu1 (analgesia) and Mu2 (side effects) - Analgesia, respiratory depression, sedation, reward, euphoria, physical dependence, constipation, bradycardia, hypothermia, urinary retention.

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24
Q

What are the effects of kappa receptors?

A
  • Analgesia
  • dysphoria
  • aversion
  • diuresis
  • miosis
  • low abuse potential.
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25
What are the effects of delta receptors?
* Analgesia * respiratory depression * constipation * urinary retention.
26
What are the receptor sites for opioids in the CNS?
Spinal cord, dorsal root ganglia, brain stem, midbrain, cortex (specifically Periaqueductal gray (PAG), Locus ceruleus, and Rostral ventral medulla (RMS))
27
What are the receptor sites for opioids in the peripheral nervous system?
* Primary afferent neurons (increased in inflammation with limited tolerance), * neuroendocrine, immune, and ectodermal tissues
28
What are the short-term clinical effects of opioids?
* Analgesia * Respiratory depression * Sedation * Euphoria * Vasodilation * Bradycardia * Cough suppression * Miosis * Nausea/vomiting * Skeletal muscle hypertonus * Constipation * Urinary retention * Biliary spasm
29
What are the long-term clinical effects of opioids?
* Tolerance to effects * Physical and psychological dependence
30
What receptors are most clinically useful opioids selective for?
mu receptors. They are similar in analgesia and respiratory depression, but differ in histamine release, presence of active metabolites, onset, and duration of action.
31
What receptor agonist causes significant dysphoria?
Selective kappa receptor agonist (arylacetamide)
32
How do opioids differ in their effects?
They differ in histamine release, presence of active metabolites, onset, and duration of action.
33
What type of pain are opioids most effective for?
Opioids are most effective for visceral or burning pain; less effective for sharp pain and least effective for neuropathic pain.
34
What is the opioid effect on nociception?
Opioid effect is selective for nociception leading to a change in the effective response to pain, dissociation from pain and mood elevation
35
What should we do to dose and concentration in the increase of intensity of acute pain?
Increase the dose and concentration. Since they are reduced in intensity of acute pain.
36
What is required for optimal opioid effect?
Opioids need to be titrated for optimal effect.
37
What surrogate markers are useful for intraoperative use?
Blood pressure, heart rate, and movement are useful surrogate markers.
38
What variable factors affect opioid efficacy?
* Location and intensity of pain * psychological factors (previous positive or negative experience) * drug interactions: Coadministration of NSAIDs, alpha2 agonist, or certain sedative (hydroxyzine) may enhance analgesia; others may actually increase toxicity (alcohol, benzos, and barbs) * age: Elderly are more sensitive, but some may require higher doses * pathologic disease *Hypothyroidism or pre-existing CNS disease can cause increased sensitivity *Asthmatics and patients with h/o COPD may be more at risk of toxicity (increased secretions and bronchospasm) *Hepatic or renal disease * sex * genetic differences –Poor metabolizers at CYP2D6 have inability to convert codeine to morphine (10% of whites and most Chinese) –Colombian Indians are more sensitive than white or Latino patients to respiratory depressive effects of morphine.
39
How can drug interactions affect analgesia?
Coadministration of NSAIDs, alpha2 agonist, or certain sedatives may enhance analgesia; others may increase toxicity.
40
How does age affect opioid sensitivity?
Elderly patients are more sensitive, but some may require higher doses.
41
What pathologic diseases can increase opioid sensitivity?
Hypothyroidism or pre-existing CNS disease can cause increased sensitivity.
42
What risk do asthmatics and COPD patients face with opioids?
They may be more at risk of toxicity due to increased secretions and bronchospasm.
43
Why do hepatic or renal diseases affect opioid use?
Hepatic or renal disease can affect opioid metabolism and sensitivity.
44
What genetic differences affect opioid metabolism?
Poor metabolizers at CYP2D6 cannot convert codeine to morphine; this affects 10% of whites and most Chinese.
45
Which population is more sensitive to morphine's respiratory depressive effects?
Colombian Indians are more sensitive than white or Latino patients.
46
What is the absorption characteristic of opioids after oral administration?
Rapidly absorbed via oral but undergo significant first pass effect ## Footnote First pass effect refers to the metabolism of a drug before it reaches systemic circulation.
47
What form is becoming more popular to circumvent short duration of opioid effects?
Delayed release formulations ## Footnote These formulations allow for a slower onset and prolonged duration of action.
48
How does the lipophilicity of fentanyl compare to morphine?
Fentanyl is much more lipophilic than morphine ## Footnote This property allows fentanyl to be delivered via lollipops and patches.
49
What opioid can be aerosolized?
Morphine can be aerosolized and achieve 60% bioavailability ## Footnote Aerosolization is a method that enhances the absorption of morphine.
50
What is the distribution characteristic of opioids in the body?
Rapid and extensive throughout the body ## Footnote This distribution is critical for the onset of therapeutic effects.
51
What does the difference in onset and duration of opioids relate to?
Lipophilicity ## Footnote More lipophilic opioids tend to have a faster onset and shorter duration.
52
What happens to lipophilic opioids like fentanyl after neuraxial administration?
They move quickly into the CNS and effects are terminated by redistribution (rapid onset of highly segmental block, rapid redistribution and offset of effect)
53
How different is epidural or intrathecal morphine?
*Long duration of effect *CSF circulates slowly (6 or more hours from lumbar cistern to brain for water soluble opioids) *Rostral spread can lead to delayed respiratory depression or thoracic analgesia after lumbar epidural. ## Footnote This is in contrast to lipophilic opioids which have shorter durations.
54
How long does it take for CSF to circulate from the lumbar cistern to the brain for water soluble opioids?
6 or more hours ## Footnote This slow circulation can affect the timing of opioid effects.
55
What can rostral spread of morphine after lumbar epidural lead to?
Delayed respiratory depression or thoracic analgesia ## Footnote This is due to the slow circulation of CSF in the body.
56
What is the primary route of metabolism for most opioids?
Extensive hepatic metabolism to polar metabolites that are excreted in urine.
57
How is Remifentanil uniquely metabolized?
It is hydrolyzed by esterases in plasma and peripheral tissues.
58
What are the active metabolites of Morphine?
Morphine-3- and -6-glucuronide.
59
What effects do the active metabolites of Morphine have?
Prolonged effects, especially in renal patients.
60
What opioids undergo oxidation by CYP450?
meperidine and fentanyl
61
What is Meperidine metabolized to, and what are its properties?
N-demethylated to normeperidine, which has analgesic and convulsive properties.
62
In which patients should caution be exercised when administering Meperidine?
Renal patients or others with compromised renal function (e.g., elderly).
63
What clinical effects of opioid in terms of CNS?
* Sedation and sleep often accompany pain relief, but as a rule opioids are poor hypnotics. * Agitation and dysphoria can occur. * Convulsant effects (generally only with high doses) *Increased intracranial pressure by causing hypercarbia. * Modest direct cerebral vasodilation

JT- PHARM (8 decks)

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