L47 - L48: Opioids Flashcards

Question

Methadone

Answer 1

Similar to morphine: analgesia, sedation, respiratory depression, miosis, constipation, antitussive effects Good oral absorption Duration: single dose - 6 hours; repeated doses - 16 to 20 hours (long acting) Used as replacement for heroin in "methadone treatment" of addition - potent; orally effective; high persistent effect when given repeatedly (unlike morphine) even though single dose has same duration of action; can be used as single daily dosage to suppress withdrawal symptoms Useful for treatment of chronic pain

Answer 2

Sublimaze of china white Potent analgesic with relatively short durations of actions: 80 - 100x more potent than morphine; more lipid soluble than morphine, which accounts for more rapid onset and shorter duration of action; onset = 5 min; duration = 0.5 to 1 hour Intravenous supplements to general anesthesia and induction of anesthesia Major advantage - cardiovascular stability Highly absued (china white is street name) bc of immediate rush; there is a lot of mixing a little bit of fentanyl w/ heroin

Answer 3

Fentanyl patch Delivers fentanyl for ~3 days: used only for severe pain, not treated by less potent drugs

Answer 4

Lomotil Therapeutic use: antidiarrheal Not an analgesic, not an anti-tussive CNS depression action, some euphoric effects Lomotil is combination w/ atropine; diphenoxylate is potentially addictive, but atropine makes abuse unlikely (if you try to up the dose, atropine kicks in and makes you sick so you'll stop)

Answer 5

Synthetic codeine analog Weak mu receptor agonist Also acts as norepinephrine and serotonin uptake inhibitor Used for moderate to moderately severe pain Side effects may include seizures

Answer 6

Strong kappa receptor agonist, mu receptor antagonist Used for moderate to severe pain May have 'ceiling' to respiratory depression But may be additive with some mu receptor agonists at lower doses

Answer 7

Partial mu receptor agonist and antagonist Less euphoria and respitaroy depression than heroine or methadone At moderate doses reach 'ceiling' effect Injected: Rapid onset 2 - 3 min, 15 min IM Analgesic duration 3 - 6 hours (pretty long-lasting) Very slow release from receptor (which is why, at high doses, is an antagonist) Use in 'methadone' opiate replacement therapy

Answer 8

Perfect antagonist - no action or cross-antagonism Requires IV admin Almost immediate onset: 1 - 2 min for response Relatively short duration of action (b/w 1 -4 hours); have to re-inject Once stabilized, use naltrexone

Answer 9

Effective orally Remarkably long duration of action Single oral dose blocks opioid agonists for 48 - 72 hours Can't use for acute toxicity if need rapid onset Very useful for treating morphine overdose - patient does not need to be monitored for relapse of respiratory depression Reduces alcohol and opioid cravings - probably by acting on pleasure centers in hypothalamus

Answer 10

Co-packaging to prevent abuse Taken orally, agonist works as pain medication Injected, nalaxone prevents agonist action (E.g. oxycodone and naloxone) Taken orally, naloxone has no effect Crushed and injected, naloxone blocks receptors