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Opioid Therapy > Opioid Therapy > Flashcards

Opioid Therapy Flashcards

1
Q

Opioid agonists are antagonized by what drug?

A

Naloxone- an opioid antagonist

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2
Q

True or false, the term narcotic should be avoided in clinical context

A

TRUE

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3
Q

Name 3 endogenous opioids

A

Endorphins
Enkephalins
Dynorphin

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4
Q

Opioid receptors belong to a superfamily of what type of receptors?

A

G-protein-coupled receptors

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5
Q

Opioid receptors are found where in the body?

A

In abundance in CNS
Periphery

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6
Q

What are the 3 major types of opioid receptors?

A

1) Mu opioid receptor
2) Kappa opioid receptor
3) delta opioid receptor

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7
Q

What opioid receptor is most responsible for inhibition of nociceptive pathway?

A

Mu opioid receptor (MOR)

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8
Q

Analgesic and psychoactive effects of drugs like morphine as well as the adverse effects of respiratory depression and inhibition of gastric transit are mediated through what receptor?

A

MU (mu opioid receptor)

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9
Q

The inhibitory effects of different types of opioid receptors reflects a set of common mechanisms.

They all include inhibition of a common enzyme ________ and activation of the cellular _____.

A
  1. Adenylate cyclase
  2. Cellular potassium pump
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10
Q

Once activated what do opioid receptors do?

A

Inhibit the transmission of impulses to excitatory pathways (including those that release serotonin, catecholamine and substance P)

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11
Q

What structures of the brain are involved in opioid induced analgesia

A
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12
Q

Define pain:

A

‘An unpleasant sensory or emotional experience associated with actual or potential tissue damage, or described in terms of such damage.’

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13
Q

Other than pain management, activation of MOR can lead to what:

A

Respiratory depression
Sedation
Constipation
Nausea
Vomiting
Reward/euphoria
Dependence/withdrawal

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14
Q

The potential for reinforcement and reward, actions that underlie the development of addiction, is mediated by what opioid receptor?

A

Mu

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15
Q

Activation of what opioid receptors can lead to convulsions?

A

Delta opioid receptor (DOR)

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16
Q

Respiratory depression involves what two opioid receptors?

A

MOR

(Activation in brain stem, pons thalamus, cortical areas, amygdala, lesser extent the periphery in carotid body)

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17
Q

Sedation is caused by what two opioid receptors

A

MOR
KOR

Activated in hypothalamus and locus coeruleus neurons controlling arousal and sleep)

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18
Q

Constiption is mostly mediated through what opioid receptor?

A

MOR in peripheral sensory neurons in GI tract

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19
Q

Nausea and vomiting is mostly mediated through what opioid receptor? And where?

A

MOR

(Medulla, cortex, vestibular apparatus, partially GI tract)

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20
Q

Diuresis results from activation of what opioid receptor?

A

Kappa opioid receptors in hypothalamus

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21
Q

What variant gene is associate with codeine (between 5 and 10% of caucasians possess allelic variants).

A

CYP2D6
(Chromosome 22)

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22
Q

Of the following patient populations: African, Asian or Caucasians who are the poorest metabolizes of codeine?

A

Caucasians 10%

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23
Q

Of the following patient populations who is an ultra-metabolizer?
African
Caucasian
Asian

A

African 20%

Rapid metabolizers can get dangerously high levels of morphine from codeine

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24
Q

Numerous factors affect physiochemical and and pharmacokinetic properties and contribute to the variation in opioid effects observed in the clinical setting.

Name 5

A
  1. Age
  2. Hepatic disease
  3. Renal failure
  4. Obesity
  5. Hypothermia, hypotension and hypovolemia
25
Q

True or false: opioid agonists have no ceiling effect to analgesia

A

True

26
Q

What is a short acting opioid antagonist?

A

Naloxone

Block MOR, DOR and KOR

27
Q

What is a long acting opioid antagonist?

A

Naltrexone
Blocks MOR, DOR, KOR

28
Q

Opioid induced Constipation can be treated with a single agent antagonist drug- the class of drugs is called:

A

Peripherally acting mu opioid receptor antagonists PAMORAs

29
Q

Codeine, morphine, hydromorphone, fentanyl, Oxycodone and methadone are what type of opioid?

A

Pure agonist

30
Q

Codeine (methyl morphine) undergoes biotransformation to morphine by which cytochrome?

A

P450 CYP2D6

31
Q

Approx 7% of caucasians lack CYP2D6 what effect does this have?

A

Lack of efficacy

32
Q

What is the MOA for codeine?

A

Low affinity binding to MOR and biotransformation to morphine by cytochrome P450 CYP2D6

33
Q

What are the metabolites of codeine?

A

Codeine 6 glucuronide
Norcodeine (by enzyme CYP2D6) enzyme CYP3A4)
Morphine 3 glucuronide
Morphine 6 glucuronide

34
Q

Name non-analgesic effects of opioids

A
  1. Reward- the potential for reinforcement and reward, actions that underlie the development of addiction is mediated by MOR.
  2. Sedation- caused by MOR and KOR activation
  3. Respiratory depression- results from activation of MOR in the brainstem medulla and pons, in in cortical areas,
    thalamus and amygdala
  4. Constipation: mostly mediated by MORs in peripheral sensory myenteric and submucosal neurons in the GI tract
  5. Nausea and vomiting- mostly mediated by MORs in the medulla, cortex, vestibular apparatus, and partially in the GI tract
  6. Diuresis- results from activation of the KORs.
35
Q

What 4 opioids are associated with the genetic variant CYP2D6?

A
  1. Codeine
  2. Hydrocodone
  3. Oxycodone
  4. Tramadol
36
Q

Most opioid metabolism occurs in the _____ (phase 1 and 2 reactions) and the hydrophilic metabolites are predominately excreted ______.

A
  1. liver
  2. renally
37
Q

Outline the WHO pain ladder.

A
  1. STEP 1: Non-opioid +/- adjuvant (mild pain)
  2. STEP 2: Weak opioid +/- non opioid +/-adjuvant (generally moderate, or mild pain that has not responded to step 1)
  3. STEP 3: Strong opioid +/- non opioid +/- adjuvant (severe pain, and those with pain of lesser intensity but have not responded to step 2 analgesia.)
  4. STEP 4 Interventional (blocks, spinal medications, spinal cord stimulation, surgical)
38
Q

Examples of drugs that are conventionally used for moderate pain?

A
  1. Codeine (pure mu-agonist)
  2. Tramadol (mixed mechanism opioid
  3. Buprenorphrine (partial agonist)
39
Q

Which potent opioid is on the Essential drug List?

A

Morphine

40
Q

MOA of morphine

A

Potent Mu agonist drug
Absorbed in upper small bowel
Extensive presystemic elimination of the drug by the liver

About 90% of morphine is converted into metabolites

Morphine is metabolized by demethylation and glucuronidation

Glucuronidation is the predominate mode of metabolism producing: M6G and M3G

Demethylation produces: normorphine

Excreted by kidney

41
Q

Hydromorphone is largely excreted unchanged in the kidneys; it is partially metabolized in the liver to _____

A

3-glucuronide
which is then excreted by the kidneys

42
Q

Fentanyl is a semisynthetic opioid and is a highly selective mu agonist. What makes it different from hydromorphone and morphine (aside from potency).

A

Fentanyl is lipophylic (and extensively taken up into fatty tissue).
Hydromorphone and morphine are hydrophilic

43
Q

Methadone is a synthetic drug.
It is a mu opioid agonist and NMDA receptor antagonist.
Inhibition of what cytochrome will lead to reduced methadone metabolism and put the patient at increased risk for sedation/resp depression?

A

Cytochrome CYP3A

44
Q

What are examples of drugs that will inhibit cytochrome CYP3A? (which effectively reduces the metabolism of methadone)

A

Fluconazole
Ciprofloxacin
Erythromycin
Grapefruit juice

45
Q

What are examples of drugs the induce cytochrome CYP3A4? (effectively accelerate methadone metabolism and cause increased pain or possibly even withdrawal.

A

Rifampin (antibiotic)
phenobarbitol (GABA agonist)
Phenytoin (voltage gated Na channel blocker)
Carbamezapine (Na channel blocker)

46
Q

Methadone can lead to QT prolongation and can cause Torsade de pointes. What drugs do you need to be careful co-adminstering?

A

Haldol
Olanzapine
Ondansetron
Tricyclic antidepressants
Citalopram (SSRI)

47
Q

Other than QT prolongation, what does methadone tend to exacerbate for people?

A

Obstructive and central sleep apnea

(and is further exacerbated by coadministration of a benzo)

48
Q

Buprenorphine is characterized as a __________

A

partial mu opioid receptor agonist

(it is also a KOR antagonist)

49
Q

Why do opioids lead to bladder spasm, urinary retention?

A

There is increase in smooth muscle tone

*Tolerance can develop rapidly

50
Q

What adverse effects of opioids can develop tolerance?

A

Sedation
Nausea and vomiting
Urinary retention
Respiratory depression?

51
Q

Paradoxical worsening of pain with escalation of opioid dose is known as what?

A

Opioid induced hyperalgesia

52
Q

How would you counsel a patient about driving while using opioids?

A

Not to drive when initiating
Not to drive when making changes to dose
Do not drive if feeling drowsy
Critical self assessment of their fitness to drive on moment to moment basis

Should the physician feel they are not capable of driving this should be forcefully communicated. If they continue to drive then requires physician to report to MOT.

53
Q

Name 7 factors which could increase a patients risk of addiction, or misuse of opioids.

A
  1. Personal or family hx of drug or etoh abuse
  2. Hx of major psychiatric d/o
  3. Hx of addiction
  4. Age (younger age puts you at moderate risk)
  5. Social - involvement of others engaging in drug abuse inc risk
  6. Smoking
  7. Hx of sexual or physical abuse
54
Q

What is the best scale that predicts risk of an aberrant drug behavior

Validated tool

A

Screener and opioid assessment for patients with pain
SOAPP-R

55
Q

In addition to its agonist effect on opioid receptors, tramadol has an additional mechanism of action which is thought to contribute to its analgesic effect. What is the MOA.

A

Opioid receptor agonist and serotonin norepinephrine reuptake inhibitor (SNRI)

56
Q

Which opioid undergoes extensive first pass metabolism?

A

Fentanyl

57
Q

Fentanyl, oxycodone, methadone and tramadol all of ______ effect; caution use in patients taking SSRI or SNRI antidepressants.

A

serotonergic effect

58
Q

Where should a fentanyl patch be placed?

A

Above the heart
Location that has not been radiated
No scar
No hair
No moles
No open sores
Alternate between left and right deltoid or subclavian region

Opioid Therapy (2 decks)

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