9. Pharm: Opioids Flashcards
What are the most common drugs involved in prescription opioid OD deaths?
- Methadone
- Oxycodone
- Hydrocodone
Who is more likely to OD on opioids?
- 25 - 54 YO
- M
- Whites & American-Indian or Alaskan Natives
Opioid AGO (9)
- Morphine
- Hydromorphine
- Methadone
- Oxycodone
- Hydrocodone
- Fentanyl
- Codeine
- Propoxyphene
- Meperidine
Opioid Partial AGO (Mixed AGO/ANT)
- Buprenorphine
- Nalbuphine
- Butorphanol
- Pentazocine
Opioid ANT
- Naloxone
- Naltrexone
General MOA of opioid analgesics
- 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
- Inhibiting ascending pain pathways
- Decrease response and pain perception (nociception)
- CNS depression
What is the general onset of action of opioid drugs?
- Depends on the patient: dosing must be individualized
- Oral (immediate release) => work in 30 minutes
- IV => work in 5 - 10 minutes
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
- Suppository
- 3- 5 hours
- 8 - 24 hours
- 1 dose lasts up to 24 hours
- 3 -7 hours
Black Box Warning for Opioids
- 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.
Opioid AE
- CNS depression
- Constipation: problematic in ppl with [unstable angine or post-MI], so consider preventative measures to decrease possib of constiptation (stool softner or fiber)
-
HypOtension: can cause severe hypOtension (including orthostatic hypotension and syncope); use with caution in ppl with
- hypovolemia/shock
- CV disease
- Drugs that worsen hypotensive effects (phenothiasinzes or general anesthetics)
What opioid is the most potent?
fentanyl > buprenorphine
Indications for Opioids
Manage pain and acute/chronic pain in patients with
- MI
- Sickle cell crisis
- Post-op
- Trauma/cancer
- Back pain
- Kidney stones
- General anesthesia/epidural anesthesia
- Palliative care
- Antitussive
- Anti-diarrheal (Loperamide)
Types of opioid receptors
1. Mu (u)
2. Delta
3. Kappa
Mu receptors respond best to what endogenous opioid peptides?
endorphins > enkaphalins > dysnorphins
Delta receptors respond best to what endogenous opioid peptides?
Enkephalins > [endorphins and dysnorphins]
Kappa receptors respond best to what endogenous opioid peptides?
Dysnorphins >>> endorphins and enkephalins
MOA of Methadone
Mu opiod receptor full AGO

Treats: opioid addiction
MOA of Buprenorphine
Mu, kappa and delta partial AGO.
Treats: opioid addiction

MOA of Naltrexone
Mu-R ANT and kappa partial AGO.
Treat: alcohol and opioid addiction
MOA of Nalmefene
Mu-R ANT and Kappa-R partial AGO.
Treat: alcohol addiction
High degree of tolerance may develop to what effects of opioids?
- Analgesia
- Euphoria, dysphoria
- Mental clouding
- Sedation
- Respiratory depression
- Antidiuresis/N/V
- Cough suppression
Moderate degree of tolerance may develop to what effects of opioids?
- Bradycardia
Minimal/no degree of tolerance may develop to what effects of opioids?
- Miosis
- Constipation
- Convulsions
AE of Chronic Opioid Use
- Hypogonadism
- Immunosupression
- Increased feeding
- Withdrawal, tolerance/dependence
- Abuse/addiction
- Hyperalgesia
Opioid Drug Interactions
- Sedative-Hyponotics: ↑ CNS depressions (resp depression)
- Antipsychotic agents: ↑ sedation, worsen CV effects (antimuscarinic and a-blocking actions)
- MAO-I: relative CI to all opioids d/t ↑ incidence of hyperpyrexic coma
Morphine Sulfate
- Indication
- CI
- Warnings and precautions***
- Adverse reactions***
- Opioid AGO used to manage pain that does NOT respond to non-narcotic analgesics
-
CI:
- Hypersensitive/allergy to morphine;
- Bronchial asthma or UA obstruction, respiratory depression WO resuscitative equipment
-
Warnings and precautions
- Dosing errors: pay atn to confusion in dosing concentrations (mg vs m:)
- Respiratory depression
- CNS depressants: increase risk of resp depression
- CNS toxicity
-
AE:
- Sedation, lightheadedness/dizziness, N/V, constipation
Buprenophine
- Indication
- Warnings and precautions
- Drug interactions****
- Treat opioid addiction and preferred for induction
-
Warnings and precautions
- Can be abused: monitor stability of pt
- Resp depression and death can occur, esp when taking via IV with benzos and CNS depressants
- Drug interactions
- Broken down in liver by CYP3A4: Monitor patients starting/ending CYP3A4 inhibitors/inducers to prevent over/underdosing
Naloxone
- MOA
- Indication
- Warnings and precautions
- MOA: Pure opioid competitive ANT that displaces opioid receptor sites
-
Indication: Opioid OD (suspected or known)
- Completely or partially reverses opioid depression (& respiratory depression) caused _by natural/synthetic opioid_s (propoxyphene, methadone, nalbuphine, butorphanol, pentazocine)
- SUSPECTED/ known acute opioid OD
-
Warnings and precaution:
- Acute opioid withdrawal: giving nalaxone in chronic opioid users => release of catecholamines => acute withdrawal or unmask pain
Naltrexone
- MOA
- Indication
- Warnings and precautions
- 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
- Accidental opioid overdose: respond to lower opioid doses than before => life-threatening opioid intoxication
- Acute opioid withdrawal: cause withdrawal in pts dependent on opioids: pain, HTN, sweating, agitiation and withdrwaral; in neonates: shrill cry, failure to feed.
Addicts who cant get opioids OD on what?
Treatment for OD?
- 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.