Opioids Flashcards
Morphine
MOA: Impairs ascending pain signals in spinal cord by enhancing K+ conductance and impairing Ca2+ conductance; activate descending 5-HT pathways from raphe nucleus
Use: severe pain, anesthesia
Abuse: euphoria, sedation
Toxicity: miosis, respiratory depression (decreased CO2 sensitivity and rigidity of trunk muscles); increased prolactin and ADH release, N/V, constipation, prolonged labor during birth
**miosis and constipation do not develop tolerance
PK: acetylation yields heroin
Methadone
MOA: Impairs ascending pain signals in spinal cord by enhancing K+ conductance and impairing Ca2+ conductance; activate descending 5-HT pathways from raphe nucleus
Use: severe pain, opioid depression in neonates
Abuse: euphoria, sedation
Toxicity: miosis, respiratory depression (decreased CO2 sensitivity and rigidity of trunk muscles); increased prolactin and ADH release, N/V, constipation, prolonged labor during birth
**miosis and constipation do not develop tolerance
PK: long half life
Meperidine
MOA: Impairs ascending pain signals in spinal cord by enhancing K+ conductance and impairing Ca2+ conductance; activate descending 5-HT pathways from raphe nucleus
Use: severe pain, anesthesia
Abuse: euphoria, sedation
Toxicity: miosis, respiratory depression (decreased CO2 sensitivity and rigidity of trunk muscles); increased prolactin and ADH release, N/V, constipation, prolonged labor during birth
**miosis and constipation do not develop tolerance
PK: cleared rapidly
CI: SSRIs due to serotonin syndrome
Fentanyl
MOA: Impairs ascending pain signals in spinal cord by enhancing K+ conductance and impairing Ca2+ conductance; activate descending 5-HT pathways from raphe nucleus
Use: breakthrough pain, anesthesia
Abuse: euphoria, sedation
Toxicity: miosis, respiratory depression (decreased CO2 sensitivity and rigidity of trunk muscles); increased prolactin and ADH release, N/V, constipation, prolonged labor during birth
**miosis and constipation do not develop tolerance
PK: useful in patients with impaired renal clearance
Hydromorphone
MOA: Impairs ascending pain signals in spinal cord by enhancing K+ conductance and impairing Ca2+ conductance; activate descending 5-HT pathways from raphe nucleus
Use: severe pain, anesthesia
Abuse: euphoria, sedation
Toxicity: miosis, respiratory depression (decreased CO2 sensitivity and rigidity of trunk muscles); increased prolactin and ADH release, N/V, constipation, prolonged labor during birth
**miosis and constipation do not develop tolerance
Codeine
MOA: metabolized into morphine
Use: mild pain (dental procedures)
Abuse: euphoria, sedation
Tox: miosis, respiratory depression, constipation, N/V
Hydrocodone (Vicodin)
MOA: metabolized into morphine
Use: mild pain (dental procedures)
Abuse: euphoria, sedation
Tox: miosis, respiratory depression, constipation, N/V
Oxycodone (Percocet)
MOA: metabolized into morphine
Use: mild pain (dental procedures)
Abuse: euphoria, sedation
Tox: miosis, respiratory depression, constipation, N/V
PK: useful in patients with impaired renal clearance
Nalbuphine
MOA: some opioid activity, but inhibit the effects of full agonists when given together
Use: sedation/pain in patients with respiratory dysfunction
Pentazocine
MOA: some opioid activity, but inhibit the effects of full agonists when given together
Use: sedation/pain in patients with respiratory dysfunction
Buprenorphine
MOA: some opioid activity, but inhibit the effects of full agonists when given together
Use: given to minimize opioid withdrawal symptoms
Tramadol
MOA: inhibits opioid, 5-HT, and NE uptake
Use: Neuropathic pain
Loperamide (Imodium)
MOA: CNS inactive opioid, decreases GI motility
Use: Diarrhea
Dextromethorphan (Robitussin DM)
MOA: CNA inactive opioid
Use: cough suppressant
Naloxone
MOA: opioid receptor antagonist
Use: acute opioid overdone
PK: short half-life
