Opioids Flashcards Preview

PHARM II, QUIZ 4 > Opioids > Flashcards

Flashcards in Opioids Deck (58):
1

Opioid MOA, class

- Opioid receptor agonist

- Blocks release of pain neurotransmitters from nociceptive fibers

- Inhibits GABA release so that dopamine fire more vigorously and can accumulate in the gap ( = pleasure)

2

Pain neurotransmitters

Substance P
Glutamate
Calcitonin gene peptide

3

Opioid receptors

Mu - brainstem and medial thalamus
Kappa - limbic, spinal cord
Delta - brain, not well studied

4

Opioid receptor responsible for analgesia, respiratory depression, euphoria, sedation, decreased GI motility, addiction

Mu

(Mu = Morphine Agonist)

5

Opioid receptor responsible for dyspnea, dependence, dysphoria

Kappa

6

Full Opioid Agonists

Morphine
Fentanyl
Hydromorphone

Codeine
Oxycodone

Methadone
Heroin

7

Partial Opioid Agonists

Buprenorphine

Butorphenal

Suboxone (buprenorphine + Naloxone)

8

Opioid antagonists

Naloxone (Narcan)

Naltrexone

9

Morphine, oxycodone, methadone, fentanyl, amphetamine - what schedule?

Schedule II

10

Schedule III drugs

Moderate addiction potential

Hydrocodone, codeine, anaboilc steroids

11

Schedule IV drugs

Low addiction potential

Benzodiazepine,
Meprobamate
Butorphenol
Pentazocine
Propoxyphene

12

Why opioids can cause pruritus / uriticaria

Direct histamine response

Can also cause bronchospasm

13

Opioid overdose triad

Miosis

Loss of consciousness

Respiratory depression

**much worse w alcohol or other CNS depressants**

14

Antidote to opioid overdose

Naloxone

15

Half life of morphine

2 hours

16

Morphine drug interactions

RARE

17

Which opioid crosses the BBB

Morphine

18

Codeine is metabolized to

Morphine

19

Potency of Codeine vs Morphine

Codeine has 50% potency of morphine

20

What drugs inhibit effect of codeine and why?

2D6!

Buproprion
Cimetidine
Cocaine
Celecoxib

21

Codeine warning

ULTRA METABOLIZERS

esp infants nursing from mothers who take it

22

3 Kinds of oxycodone

Roxicodone
Percocet
Oxycontin

23

Why is oxycodone such a high potency analgesic?

Mu AND Kappa activity

24

Percocet =

Oxycodone + Acetaminophen

25

Most commonly used opioid

Hydrocodone

26

Hydrocodone metabolized to _____ by ______

HydoMORphone, by 2D6 (just like codeine)

27

Vicodin =

Hydrocodone + Acetaminophen

aka Lorcet or Lortab

28

Hydromorphone ex

Dilaudid

Exalgo

29

Hydromorphone 1/2 life

4 hours

MORE POTENT THAN MORPHINE

30

Which is more potent - morphine of hyrdromorphone

HYDROMORPHONE (Dilaudid)

31

How is hydromorphone metabolized and what does that indicated?

Metabolized by Glucuronidation

Indicates LIVER activity

32

10x more potent than Morphine

No P450 interactions

OXYMORPHONE

aka Opana

33

80x more potent than Morphine

3A4 metabolism

FENTANYL

34

Fentanyl administration, onset, half life

Transdermal patch

6-12 hr onset for analgesic effect

clearance takes up to 24 hours

35

Fentanyl warnings

1. Dont heat or cut patch - dose dumping

2. Cross reactive w codeine allergy

36

Opioid to avoid w elderly and with MAO-I's

Demerol

Anticholinergic properties

37

Demerol ADR warnings

Neurologic toxicity

Anxiety, tremors, seizures - NOT reversible with naloxone

38

Opioid that can also be used for neuropathic pain and is a SNRI

Methodone

39

Methodone metabolism

CYP3A4 and 2D6

Highly lipophilic

40

Methadone ADR warning

Cardiotoxicity - Torsades de Pointes

41

Used for heroin / opioid addiction. Has a "ceiling effect"

Buprenorphine

Mu agonist
Kappa antagonist

42

Naloxone / Narcan ADRs

Headache
Myalgia
Increased BP

---opioid withdrawal

43

Opioid receptor antagonist used for opioid addiction. CI in patients using opioids / alcohol

Naltrexone

44

Synthetic codeine analog

Tramadol

45

Tramadol MOA

Weak Mu receptor agonist

SNRI (inhibits NE and 5HT uptake)

46

Tramadol indications

As effective as morphine for mild - moderate pain
- labor

Less effective for severe or chronic pain

47

Tramadol Warnings

Seizure risk at increased doses

Suicide risk

Serotonin syndrome risk

48

Serotonin syndrome

Agitation
Confusion
High BP, HR
Dilated Pupils
Sweating
Diarrhea
Muscle twitching / rigidity

49

Tramadol drug interactions

Carbamazepine
Serotonergic drugs

2D5, 3A4 inhibitor

50

Opioid approved specifically for diabetic neuropathy

Tapentadol (Nucynta)

No P450 interactions!

51

Tapentadol CI

EToH! Potentially fatal

52

Which antibiotic will increase opioid effects

Erythromycin

53

Which group of drugs will decrease the effects of methadone?

Rifampin
Phenytoin
Carbamazepine

54

CYD 2D6 inhibitors

Amitriptyline
Bupropion
Cimetidine
Cocaine
Ranitidine

Increase TRAMADOL levels

Decrease effect of HYDROCODONE and CODEINE

55

CYP 3A4 Inhibitors

Azoles
Verapamil

Increase METHADONE levels

56

CYP 3A4 Inducers

Phenobarb
Phenytoin
Carbamazepine
St. John's Wort

Decrease METHADONE levels

57

Opioid dependence definition

3 or more of the "addiction behaviors" within a 12 month period

58

Chronic pain tx guidelines

Chronic Pain = lasting > 1 yr

Nonopioid tx preferred

Start w IR opioids, evaulate q 1-4 weeks

Urine drug test before initiating