Narcotics Flashcards
Morphine
Class: Opioid
Mech: Mu-opioid receptor agonist
Thera: Severe analgesia, mood alteration, antitussive, sedation
Tox: Miosis, constipation, respiratory depression
Dry mouth, nausea/vomiting, sedation, sweating; dreams, dysphoria, delerium, myoclonus, seizures, pruritis, urticaria, urinary incontinence
Misc: 2 major active metabolites: M6 (more potent/active), M3 (little affinity); intraspinal administration possible
Codeine
Class: Opioid
Mech: Mu-opioid receptor agonist (low receptor affinity); demethylated to form morphine (10% of oral ingestion, via CYP2D6)
Thera: Moderate analgesia, antitussive (found in many cough medicines)
Tox: Miosis, constipation, respiratory depression
Dry mouth, nausea/vomiting, sedation, sweating; dreams, dysphoria, delerium, myoclonus, seizures, pruritis, urticaria, urinary incontinence
Misc: 10% of Caucasians unable to convert codeine to morphine (can still experience side effects, though)
Tramadol
Class: Opioid
Mech: Mu opioid receptor agonist (weak); some NE/5HT uptake inhibition (leading to analgesia); synthetic codeine analog
Thera: Moderate (not severe) analgesia
Tox: Miosis, constipation, respiratory depression
Dry mouth, nausea/vomiting, sedation, sweating; dreams, dysphoria, delerium, myoclonus, seizures, pruritis, urticaria, urinary incontinence
Misc: 1 metabolite: demethylated, more potent analgesic
Fentanyl
Class: Opioid
Mech: Mu-opioid receptor agonist (strong); highly lipid-soluble
Thera: Severe analgesia after identification of dose level via other opiod (e.g., morphine)
Tox: Miosis, constipation, respiratory depression
Dry mouth, nausea/vomiting, sedation, sweating; dreams, dysphoria, delerium, myoclonus, seizures, pruritis, urticaria, urinary incontinence
Misc: IV, transdermal; do not change dose more than 1/week (long half-life); intraspinal administration possible
Methadone
Class: Opioid
Mech: Mu-opioid receptor agonist
Thera: Chronic, severe pain; treatment of heroin and opioid addicts
Tox: Miosis, constipation, respiratory depression
Dry mouth, nausea/vomiting, sedation, sweating; dreams, dysphoria, delerium, myoclonus, seizures, pruritis, urticaria, urinary incontinence
Misc: 90% bound to plasma protein, accumulates in tissues (thus, extended duration of action); do not change dose more than 1/week (long half-life)
Oxycodone
Class: Opioid
Mech: Mu-opioid receptor agonist
Thera: Moderate to severe analgesia
Tox: Miosis, constipation, respiratory depression
Dry mouth, nausea/vomiting, sedation, sweating; dreams, dysphoria, delerium, myoclonus, seizures, pruritis, urticaria, urinary incontinence
Misc: Oxycontin is extended release
Meperidine
Class: Opioid
Mech: Mu-opioid receptor agonist
Thera: Don’t use this
Tox: Miosis, constipation, respiratory depression; mental status changes and seizures (normeperidine)
Dry mouth, nausea/vomiting, sedation, sweating; dreams, dysphoria, delerium, myoclonus, seizures, pruritis, urticaria, urinary incontinence
Misc: 1 metabolite: normeperidine
Propoxyphene
Class: Opioid
Mech: Mu-opioid receptor agonist (weak)
Thera: Don’t use this
Tox: Miosis, constipation, respiratory depression; CNS toxicity (norpropoxyphene)
Dry mouth, nausea/vomiting, sedation, sweating; dreams, dysphoria, delerium, myoclonus, seizures, pruritis, urticaria, urinary incontinence
Misc: 1 metabolite: norpropoxyphene (has long half-life)
Naloxone
Class: Opioid antagonist
Mech: Competitive mu-, delta-, and kappa-opioid receptor antagonist
Thera: Acute opioid toxicity (depressed RR best predicts reponse)
Tox: Can precipitate withdrawal (flu-like symptoms of nausea, vomiting, diarrhea; piloerection, yawning, irritability)
Misc: Continuous parenteral infusion, as lasts only 15-30 minutes (oral almost completely metabolized by liver); patient has normal mental status
Natrexone
Class: Opioid antagonist
Mech: Mu-opioid receptor antagonist
Thera: Alcoholism
Tox: May produce a prolonged withdrawal state (nausea, vomiting, piloerection, yawning)
Loperamide
Class: Opioid
Mech: Slows peristalsis via opioid receptors in intestine, and possibly decreased GI secretion
Thera: Diarrhea
Tox: Miosis, constipation, respiratory depression
Dry mouth, nausea/vomiting, sedation, sweating; dreams, dysphoria, delerium, myoclonus, seizures, pruritis, urticaria, urinary incontinence
Misc: Meperidine congener
Diphenoxylate
Class: Opioid
Mech: Slows peristalsis via opioid receptors in intestine, and possibly decreased GI secretion
Thera: Diarrhea
Tox: Miosis, constipation, respiratory depression
Dry mouth, nausea/vomiting, sedation, sweating; dreams, dysphoria, delerium, myoclonus, seizures, pruritis, urticaria, urinary incontinence
Misc: Meperidine congener
