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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
ANALGESIA/EUPHORIA - _______________ will develop - No ____________ effect to analgesia; __________ is the only limiting factor - keep pushing doses until there is a decreased _______________
- TOLERANCE will develop - No CEILING effect to analgesia; TOLERABILITY is the only limiting factor - keep pushing doses until there is a decreased RESPIRATORY DRIVE
26
SEDATION - Requires doses __________ than used for analgesia - Opioids often used for combination _________/_________
- Requires doses HIGHER than used for analgesia | - Opioids often used for combination SEDATION/ANALGESIA
27
ANTITUSSIVE - Opioids can be used as __________________ - Use limited by _____
- Opioids can be used as COUGH SUPPRESSANT | - Use limited by DEA
28
What are 8 adverse effects of opioids?
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)
29
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
- 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
CONSTIPATION - most _________ adverse effect - delay in _________ emptying and slowing ________ - Patients do not develop ____________ to constipation - treat /c ___________ and _____________
- 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
NEUROENDOCRINE - opioids inhibit __________________ hormone and __________ hormone - decreases levels of ______________ and _____________ /c big doses or long-term use - Disturbances in _______________ and ___________ dysfunction
- 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
NAUSEA/VOMITING | - sensitization of chemoreceptors trigger zone via _________ receptors
- sensitization of chemoreceptors trigger zone via MU receptors
33
HYPOTENSION - Result of ______________ vasodilation and inhibition of ___________ reflexes - Result of opioid-induced __________ release (aka morphine itch) - opioids have ________ effects
- Result of PERIPHERAL vasodilation and inhibition of BARORECEPTOR reflexes - Result of opioid-induced HISTAMINE release (aka morphine itch) - opioids have VARYING effects
34
What opioid is the gold standard for moderate to severe pain?
Morphine
35
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
- 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
Use of Morphine should be cautioned /c what two disease states?
1. Acute respiratory depression (ex. COPD, asthma) | 2. Renal failure
37
What are 4 adverse drug reactions of morphine?
1. Respiratory depression /c accumulation and high doses 2. Constipation 3. Histamine release (itching) 4. Orthostatic hypotension
38
HYDROMORPHONE (DILAUDID) - Use in __________ pain - More potent than ___________ - Safer than morphine in _________ failure
- Use in SEVERE pain - More potent than MORPHINE - Safer than morphine in RENAL failure
39
What is the extended-release of Hydromorphone (Dilaudid)? When is it indicated for use?
Exalgo | - use /c opioid tolerant patients /c moderate-severe pain
40
In what 3 populations should Exalgo (extended release hydormorphone) NOT be used?
1. Opioid intolerant 2. Impaired pulmonary function 3. Narrowed or obstructed GI tract
41
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
- 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
FENTANYL PATCH (DURAGESIC) - Useful for management of _____________, moderate to severe pain - designed to provide analgesia for _____ hours - NOT for opioid __________ - do NOT _______ patches
- 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
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
- 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
What is the active metabolite of Meperidine?
Normeperidine
45
Normeperidine (the active metabolite of meperidine) - avoid in ________ dysfunction - What are 4 side effects it can cause?
- avoid in RENAL dysfunction | - 1) anxiety, 2) tremors, 3) myoclonus, and 4) generalized SEIZURES
46
HYDROCODONE - Used in ________ to _______ pain - PO combination: hydrocodone /c _______________ (Norco) --> very dangerous - extended release _________, very potent and should NOT be used
- 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
OXYCODONE - Use in _________ to ________ pain - metabolized to _______________ - oxycodone + acetaminophen = ___________ - oxycodone + aspirin = ______________ - significant _______ potential
- Use in MODERATE to SEVERE pain - metabolized to OXYMORPHONE - oxycodone + acetaminophen = PERCOCET - oxycodone + aspirin = PERCODAN - significant ABUSE potential
48
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
- 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
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
- 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
What are the 3 mechanisms of action for Methadone?
1. Serotonin & NE reuptake inhibition 2. Antagonizes NMDA receptors 3. Agonist at kappa and gamma
51
What are 3 side effects that are unique to Methadone?
1. Prolonged QT interval 2. Torsades de pointes 3. Can cause significant testosterone decrease
52
What 2 patient populations should Methadone be avoided in?
1. those at risk for arrhythmias | 2. those /c numerous drug interactions
53
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
- 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
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
- 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
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 ___________
- 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
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 ________
- 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
NALOXONE (NARCAN) - Competitive opioid receptor ___________ (greatest affinity for _____ receptor) - Used for __________ and ________ dependence/overdose - ________ onset - Poor _____________ - Will cause ___________ syndrome (i.e. pain, anxiety, tachypnea)
- 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
What are 3 symptoms of Acute Withdrawal Syndrome?
1. Pain 2. Anxiety 3. Tachypnea
59
What is the mechanism of action for Mixed Agonists/Antagonsits? what adverse effect does it cause?
agonists at kappa receptor. Hallucinations
60
Why were mixed agonists/antagonists developed?
the desire for analgesics /c less respiratory depression and abuse potential
61
Clinical use of Mixed Agonists/Antagonists is limited: - can precipitate __________ in patients on opioid agonists - limited _______ effects - unique adverse effects = __________, _________ effects, ______ and _____________
- can precipitate WITHDRAWAL in patients on opioid agonists - limited ANALGESIC effects - unique adverse effects = DYSPHORIA, PSYCHOMOTOR effects, HTN and TACHYCARDIA
62
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 _________.
- 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
What are 4 adverse effects of TRAMADOL (ULTRAM, ULTRACET)?
1. Dizziness 2. Constipation 3. Respiratory depression 4. Insomnia or Sedation
64
What drug interactions do you need to watch for /c Tramadol?
1. Anticonvulsants 2. SSRI's 3. TCA's
65
What are the signs/symptoms of a pseudo allergy (3) vs. a true allergy (4)?
Pseudoallergy - Itching - Flushing - Sweating True Allergy - Maculopapular rash - Pustular rash - Bronchospasm - Angioedema
66
Opioid Withdraw - Correlation between opioid __________ and _________ comorbidities - Treatment usually requires long-term ___________ or _________ therapy - can't stop opioids _____________
- Correlation between opioid DEPENDENCE and PSYCHIATRIC comorbidities - Treatment usually requires long-term METHADONE or BUPRENORPHINE therapy - can't stop opioids COLD TURKEY
67
What are the 6 PHYSICAL symptoms of opioid withdrawal?
1. Chills 2. Hypoglycemia 3. Nausea, vomiting, diarrhea 4. Tachycardia 5. Priapism (prolonged erection of the penis w/o arousal) 6. Weakness
68
What are the 6 PSYCHOLOGICAL symptoms of opioid withdrawal?
1. Anxiety 2. Depression 3. Agitation 4. Delirium 5. Paranoia 6. Suicidality
69
Analgesia Ladder — What's step one?
- Acetaminophen, NSAIDs | - adjuvants (substance that enhances the immune system's response to the presence of an antigen)
70
Analgesia Ladder — Step 2
- Opioid for mild to moderate pain | - keep non-opioid
71
Analgesia Ladder — Step 3
- 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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