Narcotics

Question 1

Morphine

Answer 1

C: Opioid
M: Mu-opioid receptor agonist
T: Severe analgesia, mood alteration, antitussive, sedation
SE: Miosis, constipation, respiratory depression** Dry mouth, nausea/vomiting, sedation, sweating; dreams, dysphoria, delerium, myoclonus, seizures, pruritis, urticaria, urinary retention
MISC: 2 major active metabolites: M6 (more potent/active), M3 (little affinity); intraspinal administration possible

Question 2

Codeine

Answer 2

C: Opioid
M: Mu-opioid receptor agonist (low receptor affinity); demethylated to form morphine (10% of oral ingestion, via CYP2D6)
T: Moderate analgesia, antitussive (found in many cough medicines)
SE: Miosis, constipation, respiratory depression** Dry mouth, nausea/vomiting, sedation, sweating; dreams, dysphoria, delerium, myoclonus, seizures, pruritis, urticaria, urinary retention
MISC: 10% of Caucasians unable to convert codeine to morphine (can still experience side effects, though)

Question 3

Tramadol (Ultram)

Answer 3

C:Opioid
M: Mu opioid receptor agonist (weak); some NE/5HT uptake inhibition (leading to analgesia); synthetic codeine analog
T: Moderate (not severe) analgesia
SE: Miosis, constipation, respiratory depression** Dry mouth, nausea/vomiting, sedation, sweating; dreams, dysphoria, delerium, myoclonus, seizures, pruritis, urticaria, urinary retention
MISC: 1 metabolite: demethylated, more potent analgesic

Question 4

Fentanyl (Duragesic)

Answer 4

C: Opioid
M: Mu-opioid receptor agonist (strong); highly lipid-soluble
T: Severe analgesia after identification of dose level via other opiod (e.g., morphine)
SE: Miosis, constipation, respiratory depression** Dry mouth, nausea/vomiting, sedation, sweating; dreams, dysphoria, delerium, myoclonus, seizures, pruritis, urticaria, urinary retention
MISC: IV, transdermal; do not change dose more than 1/week (long half-life); intraspinal administration possible

Question 5

Methadone (Methadose)

Answer 5

C: Opioid
M: Mu-opioid receptor agonist
T: Chronic, severe pain; treatment of heroin and opiod addicts
SE: Miosis, constipation, respiratory depression** Dry mouth, nausea/vomiting, sedation, sweating; dreams, dysphoria, delerium, myoclonus, seizures, pruritis, urticaria, urinary retention
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)

Question 6

Oxycodone

Answer 6

C: Opioid
M: Mu-opioid receptor agonist
T: Moderate to severe analgesia
SE: Miosis, constipation, respiratory depression** Dry mouth, nausea/vomiting, sedation, sweating; dreams, dysphoria, delerium, myoclonus, seizures, pruritis, urticaria, urinary retention
MISC: Oxycontin is extended release

Question 7

Meperidine (Demerol)

Answer 7

C: Opioid
M: Mu-opioid receptor agonist
T: Don't use this
SE: Miosis, constipation, respiratory depression; mental status changes and seizures (normeperidine)** Dry mouth, nausea/vomiting, sedation, sweating; dreams, dysphoria, delerium, myoclonus, seizures, pruritis, urticaria, urinary retention
MISC: 1 metabolite:  normeperidine

Question 8

Propoxyphene (Darvon)

Answer 8

C: Opioid
M: Mu-opioid receptor agonist (weak)
T: Don’t use this
SE: Miosis, constipation, respiratory depression; CNS toxicity (norpropoxyphene)** Dry mouth, nausea/vomiting, sedation, sweating; dreams, dysphoria, delerium, myoclonus, seizures, pruritis, urticaria, urinary retention
MISC: 1 metabolite: norpropoxyphene (has long half-life)

Question 9

Loperamide (Imodium)

Answer 9

C: Opioid
M: Slows peristalsis via opioid receptors in intestine, and possibly decreased GI secretion
T: Diarrhea
SE: Miosis, constipation, respiratory depression** Dry mouth, nausea/vomiting, sedation, sweating; dreams, dysphoria, delerium, myoclonus, seizures, pruritis, urticaria, urinary retention
MISC: Meperidine congener

Question 10

Diphenoxylate (Lomotil)

Answer 10

C: Opioid
M: Slows peristalsis via opioid receptors in intestine, and possibly decreased GI secretion
T: Diarrhea
SE: Miosis, constipation, respiratory depression** Dry mouth, nausea/vomiting, sedation, sweating; dreams, dysphoria, delerium, myoclonus, seizures, pruritis, urticaria, urinary retention
MISC: Meperidine congener

Question 11

Naloxone (Narcan)

Answer 11

C: Opioid antagonist
M: Competitive mu-, delta-, and kappa-opioid receptor antagonist
T: Acute opioid toxicity (depressed RR best predicts reponse)
SE: 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

Question 12

Naltrexone (Revia)

Answer 12

C: Opioid antagonist
M: Mu-opioid receptor antagonist
T: Alcoholism
SE: May produce a prolonged withdrawal state (nausea, vomiting, piloerection, yawning)
MISC: --