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