Exam 4 - opioid analgesics Flashcards

1
Q

The descending pain modulating system projects via the _____ to the spinal cord ____ ____. Contains high concentrations of endogenous _____ _____. It is activated by _____ analgesics like certain kinds of ____.

A
Medulla
Dorsal horn
Opioid peptides
Opiate
Stress
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2
Q

Opiates produce analgesia by ____ ____ on the CNS

A

Direct action

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3
Q

Name for pain receptors?

A

Nociceptors

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4
Q

How do systemic administration of opiates produce analgesia?

A

By acting at widely distributed sites throughout the CNS

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5
Q

The pain suppression system is controlled by what?

A

Serotonin and also partially enkephalin-mediated

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6
Q

What 4 things is the pain suppression system activated by?

A
  1. Noxious stimuli
  2. Pain
  3. Psychological factors (including placebos)
  4. Opioids
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7
Q

What do opioid analgesics take place?

A

Analgesia system

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8
Q

The analgesia system is mediated by what 3 things?

A
  1. periaqueductal grey matter (midbrain)
  2. nucleus raphe magnus (medulla)
  3. pain inhibitory neurons (dorsal horn)
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9
Q

Proper name for endogenous morphine?

A

Endorphin - opiate like effect

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10
Q

What 5 places are endorphins found?

A
  1. GUT
  2. sns
  3. adrenal medullart chromaffin cells
  4. cns (arcuate nucleus hypothalamus, pituitary/nucleus tractus solitarii, visceral afferents from CN VII, IX, X)
  5. pancreatic islet cells
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11
Q

T/F endorphins are involved in blood pressure regulation, temperature regulation, and food intake.

A

True

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12
Q

What are the 3 precursor molecules of endorphins?

A
  1. proenkephalin A
  2. pro-opiomelanocortin (POMC) = B-endorphin
  3. Proenkephalin B (prodynorphin) = dynorphins
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13
Q

Endorphins act via what receptor in the GI tract?

What side effect does this cause?

A

Mu receptor

Side effect = constipation

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14
Q

_____ mimics opiate activity = weak analgesics

A

Enkephalins

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15
Q

Where are enkephalins found in the body?

A

Widely distributed - NT in many brain areas: PAG, RVM, spinal cord laminea

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16
Q

May be responsible for producing analgesia in placebo responders like _____.

A

Acupuncture

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17
Q

What receptors do enkephalins act through?

A

Mu and delta

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18
Q

What works through the kappa receptors?

A

Dynorphins

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19
Q

What 3 places are dynorphins found?

A
  1. Spinal cord
  2. through out brain
  3. hypothalamus
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20
Q

Opiate effect depends on what?

A

Site of binding - highly specific = STEREOSPECIFIC

Only levo-isomers have biological activity

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21
Q

What receptor is endorphin activated and gives the best pain relief but highest risk for addiction and possible respiratory depression?

A

Mu
(M1- addiction)
(M2 - respiratory depression)

22
Q

Which receptor is enkephalins activated and has an effect on analgesia, emotion, and seizures?

A

Delta

23
Q

Which receptor is dynorphins activated and causes spinal analgesia, miosis, and sedation?

A

kappa

24
Q

What receptor, although no longer classified as an opioid receptor, causes hallucinations, nightmares, anxiety, and tachycardia?

A

Sigma

25
Q

Besides mu, delta, and kappa, what opioid receptor provides analgesia effects?

A

Epsilon

26
Q

Strength of attachment of an opioid drug to its binding site (binding affinity) is proportional to its ______.

A

Potency

27
Q

What happens with continued exposure of tissues to high concentrations of opioid agonists?

A

Tolerance - the potency of the drug declines so that progressively higher concentrations are required to produce the same degree of analgesia
Characteristic of all opioids
Cross tolerance develops as well

28
Q

What are 4 desired clinical effects produced by all opiate drugs?

A
  1. Potent analgesia
  2. Sedation and euphoria
  3. Cough suppression
  4. GI effects (increase smooth muscle tone -> constipation, used as diarrhea tx)
29
Q

There are 15 common adverse effects produced by all opiate drugs. What are they?
(Severity of side effect is proportional to efficacy)

A
  1. Physical addiction
  2. Respiratory depression
  3. Nausea/vomiting
  4. Constipation
  5. Miosis
  6. Urinary retention
  7. CNS effects - anxiety, restlessness, nervousness, dysphoria
  8. Cardiovascular - postural hypotension, bradycardia
  9. Biliary tract constriction - biliary colic
  10. Histamine release
  11. Pregnancy/lactation - prolong labor, depress fetal respiration, cross breast milk
  12. Develop tolerance
  13. May cause an adverse reaction
  14. Overdoes
  15. Withdrawal
30
Q

What are some side effects of withdrawal?

A

yawning, lacrimation, perspiration, rhinorrhea, gooseflesh/piloerection, irritability, nausea, vomiting, tachycardia, tremors, chills

31
Q

Identify the life-threatening adverse event associated with opiate overdose.

A

Respiratory depression

32
Q

What are the 2 opiate antagonists?

A
  1. naltrexone (Depade, ReVia, Vivitrol) - oral or IM

2. naloxone (Narcan) - IV to reverse OD

33
Q

Where is opium from?

A

Dried juice obtained from unripe seed capsules of poppy plant

34
Q

What are 2 common derivatives of opium used in dentistry?

A
  1. morphine

2. codeine

35
Q

Arrange these common opioids according to potency, highest to lowest.
meperidine, codeine, dihydrocodeine, fentanyl, morohine, hydrocodone.

A
  1. fentanyl = 100x more potent than morphine and 500x more than meperidine
  2. morphine = oxycodone
  3. meperidine
  4. hydrocodone = 3x more than codeine
  5. codeine
  6. dihydrocodeine = codeine (same efficacy/potency)
36
Q

What is the optimum dose of codeine?

A

60 mg - no increased effect after this, but increased adverse events

37
Q

What is the most widely prescribed codeine product in dentistry?

A

Tylenol 3 (3 =30 mg codeine)

38
Q

Codeine is used for moderate to moderately severe pain and what else?

A

Cough suppression

39
Q

hydrocodone is 3x more potent than codeine, what are 2 examples with acetaminophen?

A
  1. Viodin (5/500 or 7.5/500)

2. Lorcet/Lortab (5/500 or 7.5/500)

40
Q

What drug uses a lower dose of acetaminophen but is still a strong opiate dose?

A

Norco

10 mg hydrocodone with 325 mg acetaminophen

41
Q

Does hydrocodone with ibuprofen have enough enough ibuprofen for an anti-inflammatory response?

A

No use OTC to supplement

42
Q

Which opioid is highly addictive, as potent as morphine, more potent than codeine, has more side effects, and used to treat severe pain? Know the 4 brand names

A

oxycodone - schedule 2

  1. Percocet
  2. Tylox
  3. Percodan
  4. Roxicet
43
Q

What is the most widely used hydrocodone preparation used by dentists?

A

hydrocodone with acetaminophen

Vicodin or Lorcet

44
Q

In dentistry, when would you use meperidine (Demerol)?

A

IV conscious sedation or orally for moderate to severe pain. Not as potent as fentanyl so less risk of respiratory depression but may cause nausea

45
Q

In dentistry, when would you use fentanyl?

A

Conscious sedation only! Given through IV, transdermal, and lollipop

46
Q

What drug is used for short term acute dental pain (less than 5 days), it inhibits the reuptake of norepinephrine and serotonin, and associated with seizures?

A

tramadol (Ultram)

47
Q

What drug is used for short term acute dental pain (less than 5 days), is not an opioid but gives relief at that level. Watch for bleeding and GI complications.

A

ketorolac (Toradol) - NSAID

48
Q

Why are NSAIDs preferred to an opiate for pain management?

A

Opiates do not reduce inflammation and treating inflammation will decrease pain
All opiates have adverse side effects - especially nausea and constipaiton

49
Q

When would you prescribe someone meperidine (demerol)?

A

For patients with a history of codeine allergy

50
Q

What opioid drugs are almost never prescribed by dentists?

A

morphine and hydromorphone (Dilaudid)