9. Pharm: Opioids Flashcards

1
Q

What are the most common drugs involved in prescription opioid OD deaths?

A
  1. Methadone
  2. Oxycodone
  3. Hydrocodone
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2
Q

Who is more likely to OD on opioids?

A
  1. 25 - 54 YO
  2. M
  3. Whites & American-Indian or Alaskan Natives
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3
Q

Opioid AGO (9)

A
  1. Morphine
  2. Hydromorphine
  3. Methadone
  4. Oxycodone
  5. Hydrocodone
  6. Fentanyl
  7. Codeine
  8. Propoxyphene
  9. Meperidine
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4
Q

Opioid Partial AGO (Mixed AGO/ANT)

A
  1. Buprenorphine
  2. Nalbuphine
  3. Butorphanol
  4. Pentazocine
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5
Q

Opioid ANT

A
  1. Naloxone
  2. Naltrexone
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6
Q

General MOA of opioid analgesics

A
  1. Binds to opioid receptor in the CNS: close presynaptic Ca2+ channels; open post-synpatic K+ channel => ↓ synaptic transmission => inhibit release of ACh, NE, 5HT, glutamate and substance P
    1. Inhibiting ascending pain pathways
    2. Decrease response and pain perception (nociception)
    3. CNS depression
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7
Q

What is the general onset of action of opioid drugs?

A
  • Depends on the patient: dosing must be individualized
    • Oral (immediate release) => work in 30 minutes
    • IV => work in 5 - 10 minutes
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8
Q

What is the general duration of pain relief of

  • 1. Immediate release opioids (tablet, oral solution or injection)
  • 2. Extended release capsule and tablet
  • 3. Epidural or intrathecal
    1. Suppository
A
  1. 3- 5 hours
  2. 8 - 24 hours
  3. 1 dose lasts up to 24 hours
  4. 3 -7 hours
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9
Q

Black Box Warning for Opioids

A
  • Can cause respiratory depression: watch closely, especially when initiating or increasing dose.
    • CO2 retention from opioid-induced respiratory depression can worsen sedating effects of opiods.
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10
Q

Opioid AE

A
  1. CNS depression
  2. Constipation: problematic in ppl with [unstable angine or post-MI], so consider preventative measures to decrease possib of constiptation (stool softner or fiber)
  3. HypOtension: can cause severe hypOtension (including orthostatic hypotension and syncope); use with caution in ppl with
    1. hypovolemia/shock
    2. CV disease
    3. Drugs that worsen hypotensive effects (phenothiasinzes or general anesthetics)
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11
Q

What opioid is the most potent?

A

fentanyl > buprenorphine

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12
Q

Indications for Opioids

A

Manage pain and acute/chronic pain in patients with

  1. MI
  2. Sickle cell crisis
  3. Post-op
  4. Trauma/cancer
  5. Back pain
  6. Kidney stones
  7. General anesthesia/epidural anesthesia
  8. Palliative care
  9. Antitussive
  10. Anti-diarrheal (Loperamide)
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13
Q

Types of opioid receptors

A

1. Mu (u)

2. Delta

3. Kappa

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14
Q

Mu receptors respond best to what endogenous opioid peptides?

A

endorphins > enkaphalins > dysnorphins

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15
Q

Delta receptors respond best to what endogenous opioid peptides?

A

Enkephalins > [endorphins and dysnorphins]

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16
Q

Kappa receptors respond best to what endogenous opioid peptides?

A

Dysnorphins >>> endorphins and enkephalins

17
Q

MOA of Methadone

A

Mu opiod receptor full AGO

Treats: opioid addiction

18
Q

MOA of Buprenorphine

A

Mu, kappa and delta partial AGO.

Treats: opioid addiction

19
Q

MOA of Naltrexone

A

Mu-R ANT and kappa partial AGO.

Treat: alcohol and opioid addiction

20
Q

MOA of Nalmefene

A

Mu-R ANT and Kappa-R partial AGO.

Treat: alcohol addiction

21
Q

High degree of tolerance may develop to what effects of opioids?

A
  1. Analgesia
  2. Euphoria, dysphoria
  3. Mental clouding
  4. Sedation
  5. Respiratory depression
  6. Antidiuresis/N/V
  7. Cough suppression
22
Q

Moderate degree of tolerance may develop to what effects of opioids?

A
  1. Bradycardia
23
Q

Minimal/no degree of tolerance may develop to what effects of opioids?

A
  1. Miosis
  2. Constipation
  3. Convulsions
24
Q

AE of Chronic Opioid Use

A
  1. Hypogonadism
  2. Immunosupression
  3. Increased feeding
  4. Withdrawal, tolerance/dependence
  5. Abuse/addiction
  6. Hyperalgesia
25
Q

Opioid Drug Interactions

A
  1. Sedative-Hyponotics: ↑ CNS depressions (resp depression)
  2. Antipsychotic agents: ↑ sedation, worsen CV effects (antimuscarinic and a-blocking actions)
  3. MAO-I: relative CI to all opioids d/t ↑ incidence of hyperpyrexic coma
26
Q

Morphine Sulfate

  1. Indication
  2. CI
  3. Warnings and precautions***
  4. Adverse reactions***
A
  1. Opioid AGO used to manage pain that does NOT respond to non-narcotic analgesics
  2. CI:
    1. Hypersensitive/allergy to morphine;
    2. Bronchial asthma or UA obstruction, respiratory depression WO resuscitative equipment
  3. Warnings and precautions
    1. Dosing errors: pay atn to confusion in dosing concentrations (mg vs m:)
    2. Respiratory depression
    3. CNS depressants: increase risk of resp depression
    4. CNS toxicity
  4. AE:
    1. Sedation, lightheadedness/dizziness, N/V, constipation
27
Q

Buprenophine

  1. Indication
  2. Warnings and precautions
  3. Drug interactions****
A
  1. Treat opioid addiction and preferred for induction
  2. Warnings and precautions
    1. Can be abused: monitor stability of pt
    2. Resp depression and death can occur, esp when taking via IV with benzos and CNS depressants
  3. ​​Drug interactions
    1. Broken down in liver by CYP3A4: Monitor patients starting/ending CYP3A4 inhibitors/inducers to prevent over/underdosing
28
Q

Naloxone

  1. MOA
  2. Indication
  3. Warnings and precautions
A
  1. MOA: Pure opioid competitive ANT that displaces opioid receptor sites
  2. Indication: Opioid OD (suspected or known)
    1. Completely or partially reverses opioid depression (& respiratory depression) caused _by natural/synthetic opioid_s (propoxyphene, methadone, nalbuphine, butorphanol, pentazocine)
    2. SUSPECTED/ known acute opioid OD
  3. Warnings and precaution:
    1. ​Acute opioid withdrawal: giving nalaxone in chronic opioid users => release of catecholamines => acute withdrawal or unmask pain
29
Q

Naltrexone

  • MOA
  • Indication
  • Warnings and precautions
A
  • MOA
    • _Pure Opioid blocker (_mu competitive ANT), with highest affinity for mu receptors.
  • Indication:
    • ​1. Alcohol use disorder: prevents intoxication, euphoria and cravings
    • 2. Opioid dependence: blocks effects of exogenous opioids; must withdraw first
  • Warnings and precaustions
    1. Accidental opioid overdose: respond to lower opioid doses than before => life-threatening opioid intoxication
    2. Acute opioid withdrawal: cause withdrawal in pts dependent on opioids: pain, HTN, sweating, agitiation and withdrwaral; in neonates: shrill cry, failure to feed.
30
Q

Addicts who cant get opioids OD on what?

Treatment for OD?

A
  • Diarrhea drugs (Loperamide) => tx diarrhea adn decrease drainage in ps with ostomies. Safe at recommeded doses.
  • Tx for OD = Naloxone: monitor vitals for at least 24 hours after last dose.