Pharmacology - T2 C. Opioid Analgesics

Front 1

what is the difference between the 3 opioid receptor types?

p87

Back 1

Mu - most significant (activate: analgesia, euphoria, respiratory depression, GI mobility change)
kappa - analgesia (spinal cord level), dysphoria (anxiety)
Delta R's - associated with analgesia and positive reinforcement effects

Front 2

which is not endogenous opioid member?
a. enkephalin
b. endorphine
c. fentanyl
d. dynorphines
p88

Back 2

c.
endo opioids act as neurotransmitters, neuromodulators and neurohormones. physiological role not well understood.

Front 3

Morphine (opioid), alalgesia
dorsal horn: how effect neurotransmitters?

p88

Back 3

block release of neurotransmitters from terminals of primary afferent neurons via presynaptic receptors. postsynaptically inhibit output from interneurons and ascending neurons of spinothalamic tract that carry nociceptive info up

Front 4

activation of descending aminergic inhibitory system via morphine:
a. stim. or inhib. PAG (midbrain)?
b. NRPC?
c. NRM?

Back 4

a. stimulates periaqeductal gray and nucleus reticularis paragigantocellularis, leads to activation of inhibitory neurons fo nucleus raphe magnus = which project to dorsal horn interneurons inhibiting activity of spinothalamic neurons

Front 5

opioid R in ventral tegmentum leads to the _____ area of the brain, diminishes and dissociates the emotional suffering associated with pain. mech unclear
p89

Back 5

"reward area" of the brain

Front 6

euphoria uses what receptors?

p89

Back 6

opioids euphoria gives false sense of well being and considerable positive reinforcement, consequence of M- and D- receptor stimulation

Front 7

most common reason for opioid death with OD?

p90

Back 7

respiratory arrest.
medullary respiration ctr EXQuisitelY sensitive to morphine.

Front 8

how does morphine depress respiration?

p90

Back 8

reduces brainstem respiratory centers to CO2.
pontine and medullary ctr's that regulate rhymicity

Front 9

heroin atics dont caugh. what about morphine and apnea?

p90

Back 9

hypoxic drive to respiration is resistant to morphine effects. be ready to administer O2 via positive pressure if respiration fails

Front 10

most common reason for opioid death with OD?

p90

Back 10

respiratory arrest.
medullary respiration ctr EXQuisitelY sensitive to morphine.

Front 11

how does morphine depress respiration?

p90

Back 11

reduces brainstem respiratory centers to CO2.
pontine and medullary ctr's that regulate rhymicity

Front 12

Define Wellness.

Back 12

The aspects of wellness include exercise, nutrition, managing your weight and stress, not smoking, keeping current on immunizations and physical check ups.

Front 13

projectile vomiting is because stimulation of area postrema in medulla called
a. PAG
b. NMR
c. CTZ
d. NRPG
p090

Back 13

c.
CTZ - the chemoreceptor trigger zone

Front 14

GI effects from morphine?

p91

Back 14

yes. constipation. propulsive waves in sm/lg intestines decreased. nonpropulsive waves in sm/lg increased. anal/pyloric sphincters increase tone. get concretions

Front 15

any route absorbs opoids, only 30% protein bound. difficult crossing BBB, what's 1st pass metabolism (related to morphine)?
p92

Back 15

1st pass metabolism - undergoes extensive biotransformation (75%) first time through liver

Front 16

morphine - 6 - glucuronide, where's this come from?

p92

Back 16

made via bioactivation, a mj. metabolite, mor potent analgesic than morphine (but doesnt pass BBB)

Front 17

so, opioids are drugs of abuse?
if chronically taken?
withdrawl peak time?
p92

Back 17

no. tolerance and speed of development depends on physiological action being considered. cross tolerance b/w all opioids.
withdrawl peaks 36-72 hrs. supress withdrawl by decreasing dose 50% every few days

Front 18

what's up Codeine?
type:
unique:
p93`

Back 18

Codeine: (pure agonist) analgeisia via M- Receptor
unique: 60% availible (orally talken), 10% turns Morphine (good for analgesia)
less sedation, Potent histamine Release
Schedule II (abuse potential)

Front 19

what's up Hydromorphone (DILAUDID)
type:
unique:
p. 93

Back 19

what's up Hydromorphone (DILAUDID)
type: strong analgesic, orally effective
unique: schedule II. Junkies lining up (heroin substitute) DONT USE
p. 93

Front 20

what's up METHADONE (Dolophine)
type:
unique:
p. 93

Back 20

METHADONE (Dolophine)
type: pure agonist
unique: first synthetic opioid. schedule II, weak, used in rehab
p. 93

Front 21

what's up PROPOXYPHENE (Darvon)
type:
unique:
p. 93

Back 21

PROPOXYPHENE (Darvon)
type: pure agonist
unique: aspirin level analgesia "MOST dangerous drug in USA", yet schedule IV. no use in dentistry

Front 22

what's up Meperidine (DEMEROL)
type:
unique:
p. 94

Back 22

Meperidine (DEMEROL)
type: pure agonist
unique: synthetic. strong alangesic parenterally, 1/2 orally. short duration, Antimuscarinic proterties
schedule II (high class drug of abuse, used by dentists, zb)

Front 23

what's up FENTANYL (SUBLIMAZE)
type:
unique:
p. 94

Back 23

FENTANYL (SUBLIMAZE)
type: synthetic with strong alagesic properties, a PURE agonist
unique: 80 fold more potent than Morphine, short duration. IV only, good in oral surgery.
schedule II, base for "designer drugs", ie china blue

Front 24

whats the difference b/w opioid and non-opioid analgesic, and how is this manipulated?

p94

Back 24

poioids act on central mechanisms and nonopioids act on peripheral mech's, combine and you get additive analgesia, greater than either alone

Front 25

what's up OXYCODONE products
type:
unique:
p. 94

Back 25

OXYCODONE products
type: combo - PERCODAN has aspirin, TYLOX has acetaminophen
unique: schedule II (street drug), orally effective, moderate (+) analgesic

Front 26

HYDROCOCONE products
type:
unique:
p. 95

Back 26

HYDROCOCONE products
type: combo - AZDONE has aspirin
LORTAB & VICODIN have acetaminophen & VICOPROFEN has ibProfen
not as effective as oxycodone (analgesic). heavily detailed in dentstry
schedule III

unique:

Front 27

CODEINE products
type:
unique:
p95

Back 27

CODEINE products
type: combo - EMPIRIN#3 - has aspirin, tylenol #3 has acetaminophen
unique: schedule III. less than hydrocodone

Front 28

what do you call a group of drugs that produce analgesia, primarily by stimulating K receptors, while at same time competitive pharmacological antagonists at M receptor sites (partial agonists) ?
p95

Back 28

these are
MIXED Agonist/ Antagonist Agents
advantage: limited respiratory effects and 2. little abuse potential (some uncontrolled even)

Front 29

what's up PENTAZOCINE (TALWIN)
type:
unique:
p95

Back 29

PENTAZOCINE (TALWIN)
type: mixed agonist/ antagonist agent
unique: schedule IV drug. Tal Nx has M-receptor antagonist even. Moderate analgesic, less GI effects than morphine. increase HR/BP. psychotomimetic effects have been reported

Front 30

TRAMADOL (ULTRAM)
type:
unique:
p96

Back 30

TRAMADOL (ULTRAM)
type: mixed agonist
unique: more nausea and sweating. 1 hr onset (slow), not a scheduled drug

Front 31

3 disease states that require caution?

p96

Back 31

emphysema. contraindicated in all copd's even agonist/antagonist agents.
bronchial asthma (b/c histamine released by opioids)
Recent head injury - respiratory depression, vasodilation, pressure

Front 32

what do you call something that binds to opioid receptors but have no efficacy at therapeutic doses?

p96

Back 32

an opioid antagonist

Front 33

whats up NALOXONE (NARCAN)
type:
unique:
p96

Back 33

NALOXONE (NARCAN)
type: "opioid antagonist"
analogue of oxymorphine, parenteral route only
unique: first of "pure" antagonists. nonspecific pharmacological anagonist

Front 34

whens NALOXONE (NARCAN) used in a dental setting?

p96

Back 34

used to reverse respiratory depression inpt who has received an opioid analgesic. will antagonize opioid effects only. help precipitate cold turkey withdrawal in dependent individuals

Front 35

ok, i have noticalbe change in daily routine, difficulty falling asleep at night
a. mild pian
b. moderate pain
c. severe pain
p97

Back 35

b. moderate pain
mild - little change in daily routine, no problem falling asleep at night
severe - departure from daily routine, interrupts sleep

Front 36

examples of mild moderate and sever pain

p97

Back 36

mild - root planning, scaling
moderate - gingivectomy
severe - extraction of 3rd's, bone recontouring

Front 37

the highest degree of pain relief achievable by agent is called what?

p97

Back 37

the ceiling analgesic effect

Front 38

the smallest dose of a drug that can produce its ceiling analgesic effect is called what?
p98

Back 38

ceiling analgesic dose

Front 39

the component in comination products that provides the bulk of analgesia in situations of dental pain is called what?
p101

Back 39

the NONOPIOID agent

Front 40

aspirin + opioids = ?

p 101

Back 40

nausea and vomitting

Front 41

what's up ULTRACET
type:
unique:

Back 41

ULTRACET
type: comination analgesic
unique: tramadol and acetimophen, 2 tabs daily

Front 42

COMBUNOX
type:
unique:

Back 42

COMBUNOX
type: combination analgesic
unique: ibuprofen and oxycodone, 1 tab daily

Front 43

considering combination analgesics, what would be the best combo?

p 102

Back 43

NSAID + acetaminophen. fewer adverse effects too. recommend 600 mg IBUPROFEN and 1000 mg acetaminophen
biologic variation: trial error for best NSAID

Front 44

upper limit for
ibuprofen
acetaminophen
p102

Back 44

ibuprofen 2400 mg/day

4000 mg acetaminophen/day

Front 45

when would one pretreat with NSAIDS?
p102

Back 45

where treatment involves surgical technques that lead to tissue trauma, ie oral surgery, endo

Front 46

why pretreat with NSAIDS for surgery?

p102

Back 46

blocking COX before trauna occurs less PGs will be made. this limits nociceptor sensitization and DELAY onset of post op pain and REDUCE magnitude of pain.
acetaminophen and opioids NOT effective.
pretreatmnt = les post op meds

Front 47

rigid dosing vs. PRN

p103

Back 47

first 24 hrs, rigid, after go
PRN (pro rae nata). first 24 give most intense pain, keep control and less discomfort later on

Front 48

long lasting local anesthetics:
used when?
effects ?
p103

Back 48

used when there's considerable tissue trauma. long lasting local anesthetic can reduce amnt of post op analgesics. it inhibits nociceptive sensiticzation in few hours.
Good adjunct to pretreamnt and rigid dosing
ie. artican - longer lasting

Front 49

explain Total Dose

p103

Back 49

after 2 days, most postop sensitivity with adequate alangeisc products, pt should be able to control discomfort well with OTC prodcuts

Front 50

EXTRA strength, explain

p103

Back 50

combination products often, which have higher dose of opioid (not good for dentsitry), will see a minimum increase in efficacy that is often overshadowed by a significant increase in adverse side effects

Front 51

EXTENDED release products, explain

p104

Back 51

not ideally suited for dentistry. SLOW onset and lower blood levels of analgesic, poor recipe for dealing with acute pain

Front 52

what is the Oral Dosing Protocol?

p104

Back 52

administer on an empty stomach. drink 8oz fluid
let gravity do it's job

Front 53

protocol for pts on 81 mg aspirin/day.

p104

Back 53

NSAID should be taken 1 hr After asprin or 6 HR's before aspirin.
the NSAID competes with aspirin for inhibiton of COX 1 in platelets. Aspirin must bin dto COX 1 first because its irreversible