Exam 4 - opioid analgesics Flashcards Preview

Pharmacology > Exam 4 - opioid analgesics > Flashcards

Flashcards in Exam 4 - opioid analgesics Deck (50):
1

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 ____.

Medulla
Dorsal horn
Opioid peptides
Opiate
Stress

2

Opiates produce analgesia by ____ ____ on the CNS

Direct action

3

Name for pain receptors?

Nociceptors

4

How do systemic administration of opiates produce analgesia?

By acting at widely distributed sites throughout the CNS

5

The pain suppression system is controlled by what?

Serotonin and also partially enkephalin-mediated

6

What 4 things is the pain suppression system activated by?

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

7

What do opioid analgesics take place?

Analgesia system

8

The analgesia system is mediated by what 3 things?

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

9

Proper name for endogenous morphine?

Endorphin - opiate like effect

10

What 5 places are endorphins found?

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

11

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

True

12

What are the 3 precursor molecules of endorphins?

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

13

Endorphins act via what receptor in the GI tract?
What side effect does this cause?

Mu receptor
Side effect = constipation

14

_____ mimics opiate activity = weak analgesics

Enkephalins

15

Where are enkephalins found in the body?

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

16

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

Acupuncture

17

What receptors do enkephalins act through?

Mu and delta

18

What works through the kappa receptors?

Dynorphins

19

What 3 places are dynorphins found?

1. Spinal cord
2. through out brain
3. hypothalamus

20

Opiate effect depends on what?

Site of binding - highly specific = STEREOSPECIFIC
(Only levo-isomers have biological activity)

21

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

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

22

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

Delta

23

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

kappa

24

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

Sigma

25

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

Epsilon

26

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

Potency

27

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

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

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

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

29

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

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

What are some side effects of withdrawal?

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

31

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

Respiratory depression

32

What are the 2 opiate antagonists?

1. naltrexone (Depade, ReVia, Vivitrol) - oral or IM
2. naloxone (Narcan) - IV to reverse OD

33

Where is opium from?

Dried juice obtained from unripe seed capsules of poppy plant

34

What are 2 common derivatives of opium used in dentistry?

1. morphine
2. codeine

35

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

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

What is the optimum dose of codeine?

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

37

What is the most widely prescribed codeine product in dentistry?

Tylenol 3 (3 =30 mg codeine)

38

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

Cough suppression

39

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

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

40

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

Norco
10 mg hydrocodone with 325 mg acetaminophen

41

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

No use OTC to supplement

42

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

oxycodone - schedule 2
1. Percocet
2. Tylox
3. Percodan
4. Roxicet

43

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

hydrocodone with acetaminophen
Vicodin or Lorcet

44

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

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

In dentistry, when would you use fentanyl?

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

46

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?

tramadol (Ultram)

47

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.

ketorolac (Toradol) - NSAID

48

Why are NSAIDs preferred to an opiate for pain management?

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

49

When would you prescribe someone meperidine (demerol)?

For patients with a history of codeine allergy

50

What opioid drugs are almost never prescribed by dentists?

morphine and hydromorphone (Dilaudid)