med chem III quiz 4 analgesics

receptor responsible for analgesia, euphoria, respiratory depression and physical dependence

receptor responsible for mixed-action agonists and analgesia at the level of the spinal cord, sedation and dysphoria

receptor may contribute to analgesia

6 Mu ligands

3 Kappa ligands

4 delta ligands

Kappa receptor mechanism

MU receptor mechanism

delta receptor mechanism

natural phenanthrene
full Mu receptor agonist
ind - analgesic activity and preoperative anesthetic agent

natural phenanthrene
partial agonist of the Mu receptor
effective anti-tussive less analgesic

opium tincture
used to treat diarrhea and as an analgesic

semi-synthetic phenanthrene
full agonist at the Mu receptor
less analgesic and respiratory depression than morphine
used alone for anti-tussive effects

semi-synthetic phenanthrene
full agonist at the Mu receptor
equipotent to morphine

controlled release oxycodone

immediate release oxycodone

combo oxycodone and APAP

combo oxycodone and ASA

semi-synthetic phenanthrene
full agonist at the Mu receptor
equipotent analgesic and respiratory depression but less constipation

extended release hydromorphone

hydromorphone tablet, liquid or injection

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

injection oxymorphone

synthetic phenylpiperidine
ind - support of anesthesia and obstetrical analgesia
less smooth muscle spasms, constipation and depression of the cough reflex
oral and parenteral

synthetic phenylpiperidine
very potent agent
ind - analgesic adjunct in intubated and ventilated patients, major CV or neuro-surgery anesthesia

synthetic phenylpiperidine
adjunct analgesia in incremental dosing
dose individualized not for < 12yo

synthetic phenylpiperidine
very dangerous due to respiratory depression due to high lipid solubility

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

synthetic diphenylheptane
ind - detoxification and maintenance of narcotic addiction (heroin)

opiate agonist/antagonist
ind - mediate morphine like analgesia, euphoria and respiratory and physical depression

partial opiate agonist
equipotent to naloxone

opiate agonist/antagonist
transdermal product

pure opiate antagonist
ind - narcotic overdose
very short duration of action
possible use in alcoholism

what gives opiate a pure antagonist action

opiate agonist/antagonist
first analgesic dosage form approved that can be prescribed in a doctor's office

opiate agonist/antagonist
opiate
ind - nasal spray --> migraines
       injection --> pain management
1/40th activity of naloxone
moa - K agonist, 5X potentcy of morphine

opiate agonist/antagonist
opiate
2nd weakest antagonist

opiate agonist/antagonist
opioid
injection and oral
heroin substitute w/ tripelennamine

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

centeral analgesic
moa - alpha 2 agonist
oral, or epidual for analgesic

ER tab central analgesic foe ADHD

Central analgesic agent
moa - Mu agonist
         inhibit NE reuptake
tablet 18X less potent as morphine

central analgesic agent
antipyretic - inhibits heat regulating center
pain - inhibits prostaglandin synthase in the CNS mainly

IV APAP

used to treat APAP overdose

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

CNS agent for pain relief
ind - postherpetic neuralgia pain
first drug approved for fibromyalgia
binds to alpha2-delta site
structural analog of GABA

pain relief agent
ind - post herpetic neuralgia
moa - binds to VR1