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Pharmacology > Opioid Analgesics > Flashcards

Opioid Analgesics Flashcards

1
Q

What are the 3 different classifications of pain?

A
  1. Acute pain
  2. Chronic benign pain
  3. Malignant pain
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2
Q

Chasing a euphoric rush/high describes _____________

A

Tolerance

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3
Q

Describe pseudoaddiction

A

patient’s pain is not being treated adequately & person is classified as addict

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4
Q

What drugs act on the same receptors as opium poppy?

A

opioids

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5
Q

What are opioids used for?

A

moderate to severe pain (most people will benefit from using a long-term opioid formulation)

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6
Q

True or False: Opioids have no ceiling effect of analgesia

A

True

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7
Q

What are the 3 opioid receptors?

A
  1. Mu
  2. Delta
  3. Kappa
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8
Q

What are the 6 actions of the Mu receptor?

A
  1. Analgesia
  2. Sedation
  3. Euphoria
  4. Respiratory depression
  5. Physical dependence
  6. Decreased gastric motility
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9
Q

What 5 locations does the Mu receptor act on?

A
  1. Brainstem
  2. Spinal Cord
  3. Limbic Region
  4. Periphery
  5. GI Tract
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10
Q

What are the 2 actions of the Delta receptor?

A
  1. Analgesia

2. Hallucinations

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11
Q

What 3 locations does the Delta receptor act on?

A
  1. Brainstem
  2. Limbic Region
  3. Periphery
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12
Q

What are the 3 actions of the Kappa Receptor?

A
  1. Analgesia
  2. Respiratory depression
  3. Psychomimetic effects
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13
Q

What 3 locations do the kappa receptors act on?

A
  1. Brainstem
  2. Spinal cord
  3. Periphery
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14
Q

What is the mechanism of action of opioids?

A

Opioid receptors impact descending pain signals (endorphins/enkphalins - provide natural pain relief)

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15
Q

What are the 4 PAIN receptors?

A
  1. N-methyl-D-asparate (NMDA)
  2. Serotonin
  3. Norephinephrine
  4. Gamma - aminobutyric acid (GABA)
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16
Q

Which pain receptor when blocked may increase the mu-receptor responsiveness to opiates?

A

N-methyl-D-aspartate (NMDA)

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17
Q

Which 3 pain receptors are good for nerve related pain?

A
  1. Serotonin
  2. Norephinephrine
  3. gamma - aminobutyric acid (GABA)
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18
Q

How are opioids classified? What are the 5 classifications?

A

Classified by their interaction /c opioid receptors

  1. Strong full agonists
  2. Weak full agonists
  3. Partial agonists
  4. Mixed agonists-antagonists
  5. Antagonists
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19
Q

Which opioid receptor is primarily involved in the classification of opioids?

A

Mu receptor

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20
Q

All of these are examples of what classification of opioids

  • Morphine
  • Hydromorphone
  • Oxycodone
  • Oxymorphone
  • Methadone
  • Meperidine
  • Fentanyl
A

Strong Full Agonists

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21
Q

All of these are examples of what classification of opioids

  • Codeine
  • Hydrocodone
  • Propoxyphene
A

Weak Full Agonists

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22
Q

All of these are examples of what classification of opioids

- Buprenophine

A

Partial Agonists

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23
Q

All of these are examples of what classification of opioids

  • Pentazocine
  • Butorphanol
  • Nalbuphine
A

Agonists-Antagonists

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24
Q

What are the 3 pharmacological effects of opioids?

A
  1. Analgesia/Euphoria
  2. Sedation
  3. Antitussive
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25
Q

ANALGESIA/EUPHORIA

  • _______________ will develop
  • No ____________ effect to analgesia; __________ is the only limiting factor
  • keep pushing doses until there is a decreased _______________
A
  • TOLERANCE will develop
  • No CEILING effect to analgesia; TOLERABILITY is the only limiting factor
  • keep pushing doses until there is a decreased RESPIRATORY DRIVE
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26
Q

SEDATION

  • Requires doses __________ than used for analgesia
  • Opioids often used for combination _________/_________
A
  • Requires doses HIGHER than used for analgesia

- Opioids often used for combination SEDATION/ANALGESIA

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27
Q

ANTITUSSIVE

  • Opioids can be used as __________________
  • Use limited by _____
A
  • Opioids can be used as COUGH SUPPRESSANT

- Use limited by DEA

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28
Q

What are 8 adverse effects of opioids?

A
  1. Respiratory depression
  2. Constipation
  3. Neuroendocrine
  4. Nausea/vomiting
  5. Hypotension
  6. Urticaria/pruritis (dermatological condition)
  7. Urinary retention
  8. Miosis (constriction of pupils)
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29
Q

RESPIRATORY DEPRESSION

  • most ___________ adverse effect
  • Same __________ of ___________ opioids leads to the same degree of respiratory depression
  • ___________ will develop
  • Consider ___________ for reversal if respiratory rate is < 8
A
  • most SERIOUS adverse effect
  • Same DOSAGE of DIFFERENT opioids leads to the same degree of respiratory depression
  • TOLERANCE will develop
  • Consider NALOXONE (NARCAN) for reversal if respiratory rate is < 8
30
Q

CONSTIPATION

  • most _________ adverse effect
  • delay in _________ emptying and slowing ________
  • Patients do not develop ____________ to constipation
  • treat /c ___________ and _____________
A
  • most COMMON adverse effect
  • delay in GASTRIC emptying and slowing MOTILITY
  • Patients do not develop TOLERANCE to constipation
  • treat /c STIMULANT and STOOL SOFTENER
31
Q

NEUROENDOCRINE

  • opioids inhibit __________________ hormone and __________ hormone
  • decreases levels of ______________ and _____________ /c big doses or long-term use
  • Disturbances in _______________ and ___________ dysfunction
A
  • opioids inhibit GONADOTROPIN RELEASING hormone and CORTICOTROPIN RELEASING hormone
  • decreases levels of TESTOSTERONE and CORTISOL /c big doses or long-term use
  • Disturbances in MENSTRUATION and SEXUAL dysfunction
32
Q

NAUSEA/VOMITING

- sensitization of chemoreceptors trigger zone via _________ receptors

A
  • sensitization of chemoreceptors trigger zone via MU receptors
33
Q

HYPOTENSION

  • Result of ______________ vasodilation and inhibition of ___________ reflexes
  • Result of opioid-induced __________ release (aka morphine itch)
  • opioids have ________ effects
A
  • Result of PERIPHERAL vasodilation and inhibition of BARORECEPTOR reflexes
  • Result of opioid-induced HISTAMINE release (aka morphine itch)
  • opioids have VARYING effects
34
Q

What opioid is the gold standard for moderate to severe pain?

A

Morphine

35
Q

MORPHINE

  • ________ opioid agonist
  • _______ receptor selective; moderate _______ and weak ________ receptor selectivity
  • Metabolized by the _________, but excreted in the __________. (can accumulate in ________ dysfunction)
  • Extensive ________ metabolism
  • only small amounts cross the blood-brain barrier; Lipid ____________, extensive __________ binding
  • Dosing is largely dependent on ___________, __________, and __________ function
A
  • STRONG opioid agonist
  • MU receptor selective; moderate KAPPA and weak DELTA receptor selectivity
  • Metabolized by the LIVER, but excreted in the URINE. (can accumulate in RENAL dysfunction)
  • Extensive FIRST PASS metabolism
  • only small amounts cross the blood-brain barrier; Lipid INSOLUBLE, extensive PROTEIN binding
  • Dosing is largely dependent on TOLERANCE, PAIN, and RENAL function
36
Q

Use of Morphine should be cautioned /c what two disease states?

A
  1. Acute respiratory depression (ex. COPD, asthma)

2. Renal failure

37
Q

What are 4 adverse drug reactions of morphine?

A
  1. Respiratory depression /c accumulation and high doses
  2. Constipation
  3. Histamine release (itching)
  4. Orthostatic hypotension
38
Q

HYDROMORPHONE (DILAUDID)

  • Use in __________ pain
  • More potent than ___________
  • Safer than morphine in _________ failure
A
  • Use in SEVERE pain
  • More potent than MORPHINE
  • Safer than morphine in RENAL failure
39
Q

What is the extended-release of Hydromorphone (Dilaudid)? When is it indicated for use?

A

Exalgo

- use /c opioid tolerant patients /c moderate-severe pain

40
Q

In what 3 populations should Exalgo (extended release hydormorphone) NOT be used?

A
  1. Opioid intolerant
  2. Impaired pulmonary function
  3. Narrowed or obstructed GI tract
41
Q

FENTANYL

  • Use for _________ pain
  • Extremely ___________
  • Unique opioid properties — __________ on/off, no release of __________, minimal myocardial __________ effects, no active ____________.
  • Metabolized ___________
  • Highly ______ soluble (aka penetrates brain immediately)
  • Drug of choice in _______ setting and _______ failure
A
  • Use for SEVERE pain
  • Extremely POTENT
  • Unique opioid properties — QUICK on/off, no release of HISTAMINE, minimal myocardial DEPRESSANT effects, no active METABOLITES.
  • Metabolized HEPATICALLY
  • Highly LIPID soluble (aka penetrates brain immediately)
  • Drug of choice in ICU setting and RENAL failure
42
Q

FENTANYL PATCH (DURAGESIC)

  • Useful for management of _____________, moderate to severe pain
  • designed to provide analgesia for _____ hours
  • NOT for opioid __________
  • do NOT _______ patches
A
  • Useful for management of PERSISTENT, moderate to severe pain
  • designed to provide analgesia for 72 hours
  • NOT for opioid NAIVE
  • do NOT CUT patches
43
Q

MEPERIDINE (DEMEROL)

  • Major use is for post-anesthesia __________
  • Pharmacologically similar to morphine but not as ____________, ___________ analgesic duration, and greater __________
  • metabolized in the _________ (= drug interactions)
  • avoid use longer than _____ hours
A
  • Major use is for post-anesthesia SHIVERING
  • Pharmacologically similar to morphine but not as POTENT, SHORTER analgesic duration, and greater TOXICITY
  • metabolized in the LIVER (= drug interactions)
  • avoid use longer than 48 hours
44
Q

What is the active metabolite of Meperidine?

A

Normeperidine

45
Q

Normeperidine (the active metabolite of meperidine)

  • avoid in ________ dysfunction
  • What are 4 side effects it can cause?
A
  • avoid in RENAL dysfunction

- 1) anxiety, 2) tremors, 3) myoclonus, and 4) generalized SEIZURES

46
Q

HYDROCODONE

  • Used in ________ to _______ pain
  • PO combination: hydrocodone /c _______________ (Norco) –> very dangerous
  • extended release _________, very potent and should NOT be used
A
  • Used in MODERATE to SEVERE pain
  • PO combination: hydrocodone /c ACETAMINOPHEN (Norco) –> very dangerous
  • extended release ZOHYDRO, very potent and should NOT be used
47
Q

OXYCODONE

  • Use in _________ to ________ pain
  • metabolized to _______________
  • oxycodone + acetaminophen = ___________
  • oxycodone + aspirin = ______________
  • significant _______ potential
A
  • Use in MODERATE to SEVERE pain
  • metabolized to OXYMORPHONE
  • oxycodone + acetaminophen = PERCOCET
  • oxycodone + aspirin = PERCODAN
  • significant ABUSE potential
48
Q

CODINE

  • Indicated for ______ to _______ pain
  • Codeine/acetaminophen amount indicated by number (Tylenol # _____ is most common)
  • _________ opioid activity
  • often used as an _____________
  • Codine metabolized by _________ to morphine
A
  • Indicated for MILD to MODERATE pain
  • Codeine/acetaminophen amount indicated by number (Tylenol # 3 is most common)
  • WEAK opioid activity
  • often used as an ANTI-TUSSIVE
  • Codine metabolized by CYP 2D6 to morphine
49
Q

METHADONE

  • Used mainly for _________ and ________ addiction
  • Causes less ________ than other opioids, while relieving signs and symptoms of _________
  • Not routinely used for _________
  • Many former heroin users treated /c oral methadone show virtually no overt _______ effects
A
  • Used mainly for OPIOID and HEROIN addiction
  • Causes less EUPHORIA than other opioids, while relieving signs and symptoms of WITHDRAWAL
  • Not routinely used for ANALGESIA
  • Many former heroin users treated /c oral methadone show virtually no overt BEHAVIORAL effects
50
Q

What are the 3 mechanisms of action for Methadone?

A
  1. Serotonin & NE reuptake inhibition
  2. Antagonizes NMDA receptors
  3. Agonist at kappa and gamma
51
Q

What are 3 side effects that are unique to Methadone?

A
  1. Prolonged QT interval
  2. Torsades de pointes
  3. Can cause significant testosterone decrease
52
Q

What 2 patient populations should Methadone be avoided in?

A
  1. those at risk for arrhythmias

2. those /c numerous drug interactions

53
Q

Initial Dosing

  • long acting formulations NOT recommended for __________ patients
  • short acting formulations should be ___________ in opioid naive patients. Once stable, patients can be transitioned to __________ formulations
  • Use _________ effective dose
A
  • long acting formulations NOT recommended for OPIOID NAIVE patients
  • short acting formulations should be INITIATED in opioid naive patients. Once stable, patients can be transitioned to LONG ACTING formulations
  • Use LOWEST effective dose
54
Q

Chronic Opioid Therapy

  • Most patients will benefit from combination of long-acting opioid. Eliminates need for patients to take __________ around the clock. Ensures analgesia throughout the ________. Avoids _________ and __________ of pain relief.
  • short acting opioid use for ___________ pain
A
  • Most patients will benefit from combination of long-acting opioid. Eliminates need for patients to take MEDICATIONS around the clock. Ensures analgesia throughout the NIGHT. Avoids PEAKS and TROUGHS of pain relief.
  • short acting opioid use for BREAKTHROUGH pain
55
Q

Breakthrough Pain

  • Total daily dose of long acting opioid should be ____________. Short acting opioid should be ______% of long acting dose.
  • short acting opioid should be ______ product as long action opioid
  • dose short acting ___________
A
  • Total daily dose of long acting opioid should be CALCULATED. Short acting opioid should be 10 - 15% of long acting dose.
  • short acting opioid should be SAME product as long action opioid
  • dose short acting AS NEEDED (PRN)
56
Q

BUPRENORPHINE/NALOXONE (SUBOXONE)

  • Used for treatment of opioid ______________
  • Buprenorphine = prevents _______ and ________ rush. Partial _____ receptor agonist and antagonist at _______ receptor
  • Naloxone = Antagonist at ____ receptor. No ________ rush from opioid
  • Requires special ________ for prescribers
  • Reduces __________ symptoms and ________ effects. Does not completely reverse __________.
  • Alternative to ________
A
  • Used for treatment of opioid DEPENDENCE
  • Buprenorphine = prevents WITHDRAWAL and EUPHORIC rush. Partial MU receptor agonist and antagonist at KAPPA receptor
  • Naloxone = Antagonist at MU receptor. No EUPHORIC rush from opioid
  • Requires special CERTIFICATION for prescribers
  • Reduces WITHDRAWALS symptoms and RESPIRATORY effects. Does not completely reverse ANALGESIA.
  • Alternative to METHADONE
57
Q

NALOXONE (NARCAN)

  • Competitive opioid receptor ___________ (greatest affinity for _____ receptor)
  • Used for __________ and ________ dependence/overdose
  • ________ onset
  • Poor _____________
  • Will cause ___________ syndrome (i.e. pain, anxiety, tachypnea)
A
  • Competitive opioid receptor ANTAGONIST (greatest affinity for MU receptor)
  • Used for ALCOHOLISM and OPIOID dependence/overdose
  • RAPID onset
  • Poor BIOAVAILABILITY
  • Will cause ACUTE WITHDRAWAL syndrome (i.e. pain, anxiety, tachypnea)
58
Q

What are 3 symptoms of Acute Withdrawal Syndrome?

A
  1. Pain
  2. Anxiety
  3. Tachypnea
59
Q

What is the mechanism of action for Mixed Agonists/Antagonsits? what adverse effect does it cause?

A

agonists at kappa receptor. Hallucinations

60
Q

Why were mixed agonists/antagonists developed?

A

the desire for analgesics /c less respiratory depression and abuse potential

61
Q

Clinical use of Mixed Agonists/Antagonists is limited:

  • can precipitate __________ in patients on opioid agonists
  • limited _______ effects
  • unique adverse effects = __________, _________ effects, ______ and _____________
A
  • can precipitate WITHDRAWAL in patients on opioid agonists
  • limited ANALGESIC effects
  • unique adverse effects = DYSPHORIA, PSYCHOMOTOR effects, HTN and TACHYCARDIA
62
Q

TRAMADOL (ULTRAM, ULTRACET)

  • Used in ________ pain
  • ________ mechanism: ____ opioid agonist, __________ and _____________ reuptake inhibition
  • contraindicated in __________ function compromise (CrCl < 30 mL/min)
  • Requires conversion by CYP 2D6. Metabolite O-desmethyltramadol has 200x Mu receptor affinity of tramadol. Won’t work if on _________.
A
  • Used in MODERATE pain
  • DUAL mechanism: MU opioid agonist, NOREPINEPHRINE and SEROTONIN reuptake inhibition
  • contraindicated in RENAL function compromise (CrCl < 30 mL/min)
  • Requires conversion by CYP 2D6. Metabolite O-desmethyltramadol has 200x Mu receptor affinity of tramadol. Won’t work if on SSRI.
63
Q

What are 4 adverse effects of TRAMADOL (ULTRAM, ULTRACET)?

A
  1. Dizziness
  2. Constipation
  3. Respiratory depression
  4. Insomnia or Sedation
64
Q

What drug interactions do you need to watch for /c Tramadol?

A
  1. Anticonvulsants
  2. SSRI’s
  3. TCA’s
65
Q

What are the signs/symptoms of a pseudo allergy (3) vs. a true allergy (4)?

A

Pseudoallergy

  • Itching
  • Flushing
  • Sweating

True Allergy

  • Maculopapular rash
  • Pustular rash
  • Bronchospasm
  • Angioedema
66
Q

Opioid Withdraw

  • Correlation between opioid __________ and _________ comorbidities
  • Treatment usually requires long-term ___________ or _________ therapy
  • can’t stop opioids _____________
A
  • Correlation between opioid DEPENDENCE and PSYCHIATRIC comorbidities
  • Treatment usually requires long-term METHADONE or BUPRENORPHINE therapy
  • can’t stop opioids COLD TURKEY
67
Q

What are the 6 PHYSICAL symptoms of opioid withdrawal?

A
  1. Chills
  2. Hypoglycemia
  3. Nausea, vomiting, diarrhea
  4. Tachycardia
  5. Priapism (prolonged erection of the penis w/o arousal)
  6. Weakness
68
Q

What are the 6 PSYCHOLOGICAL symptoms of opioid withdrawal?

A
  1. Anxiety
  2. Depression
  3. Agitation
  4. Delirium
  5. Paranoia
  6. Suicidality
69
Q

Analgesia Ladder — What’s step one?

A
  • Acetaminophen, NSAIDs

- adjuvants (substance that enhances the immune system’s response to the presence of an antigen)

70
Q

Analgesia Ladder — Step 2

A
  • Opioid for mild to moderate pain

- keep non-opioid

71
Q

Analgesia Ladder — Step 3

A
  • Opioid for moderate severe pain

- plus or minus non-opioid/adjuvant (substance that enhances the immune system’s response to the presence of an antigen)

Pharmacology (10 decks)

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