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receptor responsible for analgesia, euphoria, respiratory depression and physical dependence
Mu
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receptor responsible for mixed-action agonists and analgesia at the level of the spinal cord, sedation and dysphoria
Kappa
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receptor may contribute to analgesia
Delta
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6 Mu ligands
- endorphins
- enkephalins
- morphine
- fentanyl
- methadone
- meperidiine
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3 Kappa ligands
- dynorphins
- pentazocine
- butorphanol
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4 delta ligands
- enkephalins
- endorphins
- morphine
- codiene
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Kappa receptor mechanism
decreased Ca2+ conductance
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MU receptor mechanism
increased K+ conductance
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delta receptor mechanism
increased K+ conductance
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natural phenanthrene
full Mu receptor agonist
ind - analgesic activity and preoperative anesthetic agent
morphine - avinza
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natural phenanthrene
partial agonist of the Mu receptor
effective anti-tussive less analgesic
codeine
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opium tincture
used to treat diarrhea and as an analgesic
codeine
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semi-synthetic phenanthrene
full agonist at the Mu receptor
less analgesic and respiratory depression than morphine
used alone for anti-tussive effects
hydrocodone - lortab
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semi-synthetic phenanthrene
full agonist at the Mu receptor
equipotent to morphine
oxycodone
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controlled release oxycodone
oxycontin
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immediate release oxycodone
oxecta
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combo oxycodone and APAP
roxicet
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combo oxycodone and ASA
percodan
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semi-synthetic phenanthrene
full agonist at the Mu receptor
equipotent analgesic and respiratory depression but less constipation
hydromorphone
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extended release hydromorphone
exalgo
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hydromorphone tablet, liquid or injection
dilaudid
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semi-synthetic phenanthrene
full agonist at the Mu receptor
10X as potent as morphine IV
weakest anti-tussive agent
most potent respiratory depression and intense physical dependence of all agents
don't us in pts < 18 yo or hepatic failure
oxymorphone
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injection oxymorphone
opana
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synthetic phenylpiperidine
ind - support of anesthesia and obstetrical analgesia
less smooth muscle spasms, constipation and depression of the cough reflex
oral and parenteral
meperidine - demerol
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synthetic phenylpiperidine
very potent agent
ind - analgesic adjunct in intubated and ventilated patients, major CV or neuro-surgery anesthesia
sufentanil - sufenta
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synthetic phenylpiperidine
adjunct analgesia in incremental dosing
dose individualized not for < 12yo
alfentanil - alfenta
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synthetic phenylpiperidine
very dangerous due to respiratory depression due to high lipid solubility
fentanyl
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synthetic phenylpiperidine
extremely potent analgesic agent
ind - induction of anesthesia
watch for interuption during infusion
do no administer into same IV line as blood products
remifentanil - ultiva
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synthetic diphenylheptane
ind - detoxification and maintenance of narcotic addiction (heroin)
methadone - dolophine, methadose
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opiate agonist/antagonist
ind - mediate morphine like analgesia, euphoria and respiratory and physical depression
buprenorphine - buprenex
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partial opiate agonist
equipotent to naloxone
buprenorphiine - buprenex
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opiate agonist/antagonist
transdermal product
buprenorphine - butrans
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pure opiate antagonist
ind - narcotic overdose
very short duration of action
possible use in alcoholism
naloxone - narcan
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what gives opiate a pure antagonist action
N-allyl substituition
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opiate agonist/antagonist
first analgesic dosage form approved that can be prescribed in a doctor's office
buprenorphine & naloxone - suboxone
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opiate agonist/antagonist
opiate
ind - nasal spray --> migraines
injection --> pain management
1/40th activity of naloxone
moa - K agonist, 5X potentcy of morphine
butorphanol tartrate - stadol
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opiate agonist/antagonist
opiate
2nd weakest antagonist
nalbuphine
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opiate agonist/antagonist
opioid
injection and oral
heroin substitute w/ tripelennamine
pentazocine lactate - talwin
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non-schedule agent with narcotic agonistic activity
opioid
moa - binds Mu and prevents NE and 5HT reuptake in the CNS
modify dose for CrCl < 30
metabolized by CYP2D6
tramadol - ultram
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centeral analgesic
moa - alpha 2 agonist
oral, or epidual for analgesic
clonidine - duraclon
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ER tab central analgesic foe ADHD
clonidine - Kapvay
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Central analgesic agent
moa - Mu agonist
inhibit NE reuptake
tablet 18X less potent as morphine
tapentadol - nucynta
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central analgesic agent
antipyretic - inhibits heat regulating center
pain - inhibits prostaglandin synthase in the CNS mainly
acetaminophen
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used to treat APAP overdose
N-Acetylcysteine
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conopeptides or conotoxin
derived form snail
moa - binds to N type Ca2+ (A-delta and C)
induces decreased GI motility but not respiratory depression
CI in psychosis pts
zirconitide - prialt
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CNS agent for pain relief
ind - postherpetic neuralgia pain
first drug approved for fibromyalgia
binds to alpha2-delta site
structural analog of GABA
pregabalin - lyrica
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pain relief agent
ind - post herpetic neuralgia
moa - binds to VR1
capsaicin - qutenza
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