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28 Cards in this Set

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morphine; any type of pain, esp dull and continuous; stimulate opiod receptors; no antiinflammatory or antipyretic effects; central site of action; develop tolerance and dependence
aspirin; musculoskeletal pain; inhibition of PG synthesis; both antiinflammatory and antipyretic; central or peripheral action; no tolerance or dependence.
well absorbed by many routes; large first pass effect; large BBB effect; met in liver--glucuronidated and some sulfation; active metabolites excreted in urine; 3 and 6 C's; also demethylation.
opiod receptors
CNS; many in spinal cord in laminae I and II areas; also in areas involved in emotion and respiration
central actions of opiods
analgesia; sedative effects and narcosis; euphoria; respiratory depression; miosis (species specific); muscular rigidity (fentanyl); sickness; anti-tussive; alter thermoregulatory action; multiple neuroendocrine effects
peripheral actions of opiods
GI effects- enteric NS in gut- decreased secretion, increased muscle tone--constipation; morphine constricts sphincter of Oddi in gallbladder; urinary retention; prolongs labor; little effect on CV system (alkaloid character causes some hypotension b/c mast cells release histamine); immunosuppression
mechanism of action
bind to and activate opiod receptors; alter the perception of pain; inhibit synaptic transmission (presynaptically); affect intracellular transduction (inhibit cAMP production and block Ca++ channels).
therapeutic use of morphine
very severe pain; post op; MI pain; sickle cell vaso-occlusive crisis
-chronic pain
usually oral- first pass effect; rectally, spinally, or IV once can't swallow anymore; slow release forms like ms-contin; diarrhea; acute pulmonary edema
side effects of morphine treatment
respiratory depression; nausea and vomiting; constipation; dizziness and mental clouding; dysphoria; hypotention; urinary retention; tolerance and physical dependence; interaction with other drugs; additive with other CNS depressants; enhanced action via antidepressants, amphetamines, antihistamines, etc;
morphine toxicity
coma; pinpoint pupils (may dilate some b/c of CO2); depressed respiration
GIVE NALOXENE to diagnose if heroin overdose or barbiturates
treatment of narcotic addiction
1. substitute another narcotic (methadone)
2. detox
3. narcotic antagonists (naloxene and naltexone)
4. clonidine (not an opiod, but cuts down on withdrawal symptoms)
be careful when...
depressed respiratory reserve; head injury; reduced blood volumes; asthma; biliary colic; renal insufficiency; taking other CNS depressants
morphine derivatives...
1. hydromorphone
2-4x more effective; orally effective; aka dilautid
2. diacetylmorphine (heroin)
acetyl groups on hydroxy groups on carbons 3 and 6; easy to make, much more lipophilic; euphoric effects; abuse
3. codeine (methylmorphine)
methyl on 3 position; less potent and effective orally
4. hydrocodone or oxycodone
components of percodan and percoset; abused; good to treat pain; long term release form is oxycotin
Phenylpiperidine derivatives
1. meperidine
aka Demerol; less potent; normeperidine is toxic metabolite that lowers CNS seizure threshold; interactions with MAOI's and TCA's, etc; short duration of withdrawal
2. fentanyl, sufentanyl, and alfentanyl
much more potent and very lipophilic; fast onset and short duration; effective; maintenance of anesthesia and post op analgesia; fentanyl can cause muscle rigidity in high doses (chest); patch form is slow release and good for chronic pain or radiation patients.
3. diphenoxylate and loperamide
GI drugs to treat diarrhea
Diphenylheptane derivatives
1. methadone
effective orally; long half life active metabolite; more bioavailable; cheap; avoid stigma!
2. propoxyphene
les efficacious than morphine; rough analgesic effect
analgesic and used instead of methadone in treating heroin addicts
similar structure to morphine
- levorphanol- L isomer- 4-5x more potent than morphine and effective orally
-dextomorphan- D isomer- not analgesic but good anti-tussive effects
opiods with mixed agonist and antagonist activities
pentazocine--causes increase in bp and heart rate**; component of "Ts and blues"
nalbuphine--less respiratory depression
buprenorphine--now treats heroin addiction b/c longer retraction of withdrawal symptoms, safe, and more potent
nalorphine--not used much
butorhanol--nasal spray for migraine
opiod antagonists
no analgesic activity; do nothing to normal individuals; precipitate withdrawal symptoms in addicts; naloxone; used in overdose treatment; naltrexone is oral form used in motivated pts
opiod receptors
1. mu- activated by morphine; fentanyl and naloxone are more selective
2. delta- no drugs selective
3. kappa- activated by ketocyclazocine; preferred by pantazocine, butorphanol, and buprenorphine
*receptors in brain, spinal cord, and GI tract; other receptors assoc with opiod action= sigma--phencyline receptor and epsilon--activated by endogenist agonist beta endorphin
endogenous opiods
1. enkephalins- target delta and mu
2. beta endorphin- target delta and epsilon
3. dynorphins- target kappa
4. endomorphin- activated by endomorphins
*no current therapeutic use for opiod peptides