opioid analgesics / Benzodiazepines / Barbiturates / Nonbenzodiazepine hypnotics Flashcards
opioid analgesics - drugs
- Morphine 2. fentanyl 3. codeine
- lorepamide 5. methadone
- meperidine 7. dextromethorphan
- diphenoxylate 9. pentazocine
opioid receptors
μ=morphine, δ=enkephalin, κ=dynorphin
opioid analgesics - mechanism of action
act as agonists at opioid receptors to modulate synaptic transmission –> open K+ channels, close Ca2+ channels –> decrease synaptic transmission. Inhibit release of Ach, norepinephrine, 5-HT, glutamate, substance P
opioid analgesics - Inhibit release of
Ach, norepinephrine, 5-HT, glutamate, substance P
opioid analgesics - clinical use (and which drugs, if specific)
- pain controle 2. cough suppressor (dextromethorphan)
- diarrhea (loperamide, diphenoxylate)
- acute pulmonary edema
- maintenance programs for heroin addicts (methadone, buprenorphine + naloxone)
maintenance programs for heroin addicts - drugs
methadone, buprenorphine + naloxone
opioid analgesics - toxicity
- addiction
- respiratory depression
- constipation (no tolerance)
- miosis (pinpoint pupils) (no tolerance) (except meperidine –> mydriasis)
- addictive CNS depression with other drugs
- opioid withdrawal syndrome
- suppressed gag reflex
opioid analgesics - toxicity - tolerance does not develop to
miosis and constipation
opioid analgesics toxicity treated with
opioid receptor antagonists (naloxone or natrexone)
buprenorphine - mechanism of action
- agonistic effects at μ δ opioid receptors
- antagonist effect at κ opioid receptors
butorphanol - mechanism of action
- κ-opioid receptor agonist
- μ-opioid receptor partial agonist
butorphanol - clinical use
severe pain (migraine, labor)
butorphanol vs full opioids agonists according to side effects
butorphenol causes less respiratory depression than full opioid agonists
butorphanol - toxicity
- can cause opioid withdrawal symptoms if patient is also taking full opiod agoinsts (competition for opioid receptor)
- overdose not easily reversed with naloxone
- less respiratory depression than full opioid agonists
butorphenol - antidote
overdose not easily reversed with naloxone
tramadol - mechanism of action
very weak opioid agonist
also inhibits 5-HT and norepinephrine reuptake
tramadol - clinical use
chronic pain
tramadol toxicity
- similar to opioid
- decreases seizure threshold
- serotonin syndrome
dextromethorphan + seretonergic agents –>
seretonin syndrome
barbiturates - drugs
(-BARBITAL + THIOPENTAL)
- phenobarbital
- pentobarbital
- secobarbital
- thiopental