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60 Cards in this Set

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OPIOIDS
what are the CNS actions of morphine (5)?
analgesia, respiratory depression, miosis, antitussive, nausea
what are the peripheral actions of morphine?
analgesia, anti-diarrheal, increased smooth muscle tone
what is meant by the term potency?
relative amount of drug needed to achieve half of maximum effect
what are the effects of opiods at the cellular level (3)?
1) decrease cAMP by inhibiting adenylate cyclase; 2) increase K current; 3) decrease Ca++ influx; last two effects decrease cell excitability
where are all types of opioid receptors found?
peripheral nervous system, GI, cortex, striatum, hippocampus, dorsal horn
where are only delta receptors found?
amygdala
where are only mu and kappa receptors found?
periaqueductal grey
which endogenous opioid agonists are co-released with ACTH in the pituitary, and tie in with HPA stress axis?
endorphins
what endogenous opioids are present in inhibitory circuits, and found in brain/spinal cord, and what receptors do they prefer?
enkephalins - prefer deltareceptor
which endogenous opioids are found in pitiuitary, hypothalamus, midbrain, and striatum?
dynorphins
what receptors do dynorphins prefer, and what action are they involved in?
brain region-dependent precursor processing - prefer kappa receptor
what is an opioid antagonist that is used to counteract opioid overdose, and what does it do in normal healthy adults vs. post-surgery?
naloxone - raises LH and FSH in normal adults, does not alter pain threshold in normal adults, but is hyperalgesic in post-surgery patients
what are the three opioid drug classes?
phenanthrene, phenylpiperidine, phenylheptanone
which class only has two drugs in it, and what are they?
phenylhepatone (methadone, propoxyphene)
what class are morphine, codeine, hydrocodone, hydromorphone, hydrocodeine, oxycodone, dihydrocodeine, diacethylmorphine in?
phenanthrene
what drugs are phenylpiperidine?
meperadine, fentanyl, alfentanil, sufentanil, femifentanil
what type of pain is morphine best against?
continuous, dull pain
what effect of morphine occurs at sub-algesic/respiratory depressing doses?
antitussive (anti-cough)
what can morphine cause that can interfere with ventilation in surgery?
truncal rigidity
what effects of morphine do tolerance not develop for?
miosis, diarrhea
in what ways does morphine depress respiration?
1) depress CO2 blood tension sensitivity in BS; 2) depress medullary/pontine centers that regulate frequency
what is the effect of prolonged exposure to morphine on N/V?
nearly completely prevents stimulation of CTZ and blocks emesis via other agents (but early exposure to opiates stimulates CTZ)
what are GI effects of morphine?
increased SM tone, muscle spasms can increase pain, decreases secretions, decreased motility - antidiarrheal/constipating effect
what does morphine do to SM tone at therapeutic doses?
insignificant increase in tone at therapeutic doses - but at higher doses, increases tone, aggravating asthma, causing urinary retention, and prolonging labor
what does morphine do to the CV system at therapeutic doses?
minimal effects - decreased BP, stimulate histamine release, orthostatic hypotension
what is morphine effective in treating due to these CV effects?
pulmonary edema
why are morphine and similar opiates good for pain asociated with inflammation?
opioid receptors are upregulated at nociceptors due to local inflammation/injury - exogenously applied opioid takes advantage of increased receptor #
why is oral morphine not as effective as IV?
first pass effect (1/3 to 1/6 as potent)
how is morphine excreted, and how fast?
almost all gone in 24h in urine
what is the triad of symptoms that should make one highly suspicious of opioid toxicity?
miosis, decreased respiration, and coma
why must naloxene be monitored/readministered?
shorter t1/2 than toxicant
what is morphine metabolized to in the first pass?
morphine-6-glucuronide and morphine-3-glucuronide, which are active metabolites, one excitotoxic, and one analgesic - these build up in blood over long term
what induces morphine dependence?
only withdrawal of drug
what is the active analgesic when codeine is administered, and how is it metabolized to this?
10% metabolized by CYP2D6 to morphine
what should be used to treat severe pain with an inflammatory sourec?
both an opioid and an anti-inflammatory
what are three semi-synthetic modified versions of molecules found in the opium poppy, that are used as with codeine (3)?
1) dihydrocodeine (in synalgos); 2) oxycodone (in percocet); 3) hydrocodone (in vicodin)
what drugs are completely synthetic and structurally dissimilar than morphine that we must know, but have similar actions and side effects (3)?
1) meperidine (demerol); 2) methadone; 3) fentanyl (and family)
what is the DOC for outpatient anesthesia, and why?
alfentanil - fentanyl family - repeated doses do not accumulate, and recovery is rapid
which of these synthetics was said to have high abuse potential?
meperidine (demerol) - as hard to kick as heroin -
what is potency of meperidine like compared to morphine, and what is it used in?
used in labor and delivery - 1/10 morphine's potency
what AE's are reduced with meperidine compared to morphine?
retains atropine-like functions - reduced biliary spasm and miosis
what is the AE of meperidine we must know?
CNS excitation/tremors/convulsions
what is the potency of methadone compared to morphine, and how does it differ in pharmacokinetics?
equipotent with morphine, high bioavailability - repeated dosage causes longer-lasting effects - can use orally for once daily dosing - functions as pure agonist, and does not block opioid actions
what group of people is methadone used for?
heroin addicts
what is fentanyl like in potency and pharmacokinetics?
100x as potent as morphine, short duration, lipophilic (lollipop preparations for addult breakthrough pain)
in what situation is fentanyl (and family) used in anesthesia, besdies outpatient anesthesia, and for what reasons?
used as IV analgesic in balanced anesthesia (especially cardiac surgery) because of improved cardiac stability (post-surgical reaction)
what function does it lack when used in surgery, and what should be used concomitantly?
lacks anesthetic activity - people open eyes, dilate pupils, move during surgery - should use concomitant muscle relaxers for truncal rigidity
what opioid antagonists must we know, what is the duration of each, and which is available orally?
naloxone and naltrexone, naloxone has 1-4 hour duration and is NOT available orally, naltrexone has 48-72 hour duration and is available orally
what drug is used as an antitussive, why is it used, and what is it like chemically?
dextromethorphan - D-isomer of codeine analog methorphan - no analgesic/addictive properties - D-isomer of codeine analog methorphan
what is the MOA of dextromethorphan?
acts via non-opioid receptors, centrally, to elevate coughing threshold - not reversed by naloxone
what is the brand name for OTC dextromethorphan and how can it be abused?
cough syrup - robitussin - "roboing" is when it antagonizes NMDA receptors at high doses, for hallucination
what type of side effects are caused by increased dosage in long-term use of mixed agents?
dysphoric side effects
will addiction develop after long term use?
no evidence of addiction per se developing, but physical dependence will
what is the most likely cause of flushed feeling and itchiness when opioids are given?
morphine triggers histamine release
what can help itching and N/V from morphine?
concomitant antihistamine
in addition to normal pain medication, what should cancer patients always be given?
a rapid onset drug for reakthrough pain
when should opioids be used for chronic non-malignant pain?
only after other analgesics have been tried and failed