Pharm 3 Cont.

Front 1

OPIOIDS

Front 3

what are the CNS actions of morphine (5)?

Back 3

analgesia, respiratory depression, miosis, antitussive, nausea

Front 4

what are the peripheral actions of morphine?

Back 4

analgesia, anti-diarrheal, increased smooth muscle tone

Front 5

what is meant by the term potency?

Back 5

relative amount of drug needed to achieve half of maximum effect

Front 6

what are the effects of opiods at the cellular level (3)?

Back 6

1) decrease cAMP by inhibiting adenylate cyclase; 2) increase K current; 3) decrease Ca++ influx; last two effects decrease cell excitability

Front 7

where are all types of opioid receptors found?

Back 7

peripheral nervous system, GI, cortex, striatum, hippocampus, dorsal horn

Front 8

where are only delta receptors found?

Back 8

amygdala

Front 9

where are only mu and kappa receptors found?

Back 9

periaqueductal grey

Front 10

which endogenous opioid agonists are co-released with ACTH in the pituitary, and tie in with HPA stress axis?

Back 10

endorphins

Front 11

what endogenous opioids are present in inhibitory circuits, and found in brain/spinal cord, and what receptors do they prefer?

Back 11

enkephalins - prefer deltareceptor

Front 12

which endogenous opioids are found in pitiuitary, hypothalamus, midbrain, and striatum?

Back 12

dynorphins

Front 13

what receptors do dynorphins prefer, and what action are they involved in?

Back 13

brain region-dependent precursor processing - prefer kappa receptor

Front 14

what is an opioid antagonist that is used to counteract opioid overdose, and what does it do in normal healthy adults vs. post-surgery?

Back 14

naloxone - raises LH and FSH in normal adults, does not alter pain threshold in normal adults, but is hyperalgesic in post-surgery patients

Front 15

what are the three opioid drug classes?

Back 15

phenanthrene, phenylpiperidine, phenylheptanone

Front 16

which class only has two drugs in it, and what are they?

Back 16

phenylhepatone (methadone, propoxyphene)

Front 17

what class are morphine, codeine, hydrocodone, hydromorphone, hydrocodeine, oxycodone, dihydrocodeine, diacethylmorphine in?

Back 17

phenanthrene

Front 18

what drugs are phenylpiperidine?

Back 18

meperadine, fentanyl, alfentanil, sufentanil, femifentanil

Front 19

what type of pain is morphine best against?

Back 19

continuous, dull pain

Front 20

what effect of morphine occurs at sub-algesic/respiratory depressing doses?

Back 20

antitussive (anti-cough)

Front 21

what can morphine cause that can interfere with ventilation in surgery?

Back 21

truncal rigidity

Front 22

what effects of morphine do tolerance not develop for?

Back 22

miosis, diarrhea

Front 23

in what ways does morphine depress respiration?

Back 23

1) depress CO2 blood tension sensitivity in BS; 2) depress medullary/pontine centers that regulate frequency

Front 24

what is the effect of prolonged exposure to morphine on N/V?

Back 24

nearly completely prevents stimulation of CTZ and blocks emesis via other agents (but early exposure to opiates stimulates CTZ)

Front 25

what are GI effects of morphine?

Back 25

increased SM tone, muscle spasms can increase pain, decreases secretions, decreased motility - antidiarrheal/constipating effect

Front 26

what does morphine do to SM tone at therapeutic doses?

Back 26

insignificant increase in tone at therapeutic doses - but at higher doses, increases tone, aggravating asthma, causing urinary retention, and prolonging labor

Front 27

what does morphine do to the CV system at therapeutic doses?

Back 27

minimal effects - decreased BP, stimulate histamine release, orthostatic hypotension

Front 28

what is morphine effective in treating due to these CV effects?

Back 28

pulmonary edema

Front 29

why are morphine and similar opiates good for pain asociated with inflammation?

Back 29

opioid receptors are upregulated at nociceptors due to local inflammation/injury - exogenously applied opioid takes advantage of increased receptor #

Front 30

why is oral morphine not as effective as IV?

Back 30

first pass effect (1/3 to 1/6 as potent)

Front 31

how is morphine excreted, and how fast?

Back 31

almost all gone in 24h in urine

Front 32

what is the triad of symptoms that should make one highly suspicious of opioid toxicity?

Back 32

miosis, decreased respiration, and coma

Front 33

why must naloxene be monitored/readministered?

Back 33

shorter t1/2 than toxicant

Front 34

what is morphine metabolized to in the first pass?

Back 34

morphine-6-glucuronide and morphine-3-glucuronide, which are active metabolites, one excitotoxic, and one analgesic - these build up in blood over long term

Front 35

what induces morphine dependence?

Back 35

only withdrawal of drug

Front 36

what is the active analgesic when codeine is administered, and how is it metabolized to this?

Back 36

10% metabolized by CYP2D6 to morphine

Front 37

what should be used to treat severe pain with an inflammatory sourec?

Back 37

both an opioid and an anti-inflammatory

Front 38

what are three semi-synthetic modified versions of molecules found in the opium poppy, that are used as with codeine (3)?

Back 38

1) dihydrocodeine (in synalgos); 2) oxycodone (in percocet); 3) hydrocodone (in vicodin)

Front 39

what drugs are completely synthetic and structurally dissimilar than morphine that we must know, but have similar actions and side effects (3)?

Back 39

1) meperidine (demerol); 2) methadone; 3) fentanyl (and family)

Front 40

what is the DOC for outpatient anesthesia, and why?

Back 40

alfentanil - fentanyl family - repeated doses do not accumulate, and recovery is rapid

Front 41

which of these synthetics was said to have high abuse potential?

Back 41

meperidine (demerol) - as hard to kick as heroin -

Front 42

what is potency of meperidine like compared to morphine, and what is it used in?

Back 42

used in labor and delivery - 1/10 morphine's potency

Front 43

what AE's are reduced with meperidine compared to morphine?

Back 43

retains atropine-like functions - reduced biliary spasm and miosis

Front 44

what is the AE of meperidine we must know?

Back 44

CNS excitation/tremors/convulsions

Front 45

what is the potency of methadone compared to morphine, and how does it differ in pharmacokinetics?

Back 45

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

Front 46

what group of people is methadone used for?

Back 46

heroin addicts

Front 47

what is fentanyl like in potency and pharmacokinetics?

Back 47

100x as potent as morphine, short duration, lipophilic (lollipop preparations for addult breakthrough pain)

Front 48

in what situation is fentanyl (and family) used in anesthesia, besdies outpatient anesthesia, and for what reasons?

Back 48

used as IV analgesic in balanced anesthesia (especially cardiac surgery) because of improved cardiac stability (post-surgical reaction)

Front 49

what function does it lack when used in surgery, and what should be used concomitantly?

Back 49

lacks anesthetic activity - people open eyes, dilate pupils, move during surgery - should use concomitant muscle relaxers for truncal rigidity

Front 50

what opioid antagonists must we know, what is the duration of each, and which is available orally?

Back 50

naloxone and naltrexone, naloxone has 1-4 hour duration and is NOT available orally, naltrexone has 48-72 hour duration and is available orally

Front 51

what drug is used as an antitussive, why is it used, and what is it like chemically?

Back 51

dextromethorphan - D-isomer of codeine analog methorphan - no analgesic/addictive properties - D-isomer of codeine analog methorphan

Front 52

what is the MOA of dextromethorphan?

Back 52

acts via non-opioid receptors, centrally, to elevate coughing threshold - not reversed by naloxone

Front 53

what is the brand name for OTC dextromethorphan and how can it be abused?

Back 53

cough syrup - robitussin - "roboing" is when it antagonizes NMDA receptors at high doses, for hallucination

Front 54

what type of side effects are caused by increased dosage in long-term use of mixed agents?

Back 54

dysphoric side effects

Front 55

will addiction develop after long term use?

Back 55

no evidence of addiction per se developing, but physical dependence will

Front 56

what is the most likely cause of flushed feeling and itchiness when opioids are given?

Back 56

morphine triggers histamine release

Front 57

what can help itching and N/V from morphine?

Back 57

concomitant antihistamine

Front 58

in addition to normal pain medication, what should cancer patients always be given?

Back 58

a rapid onset drug for reakthrough pain

Front 59

when should opioids be used for chronic non-malignant pain?

Back 59

only after other analgesics have been tried and failed