Opioids Flashcards

1
Q

Opioid MOA, class

A
  • 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)
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2
Q

Pain neurotransmitters

A

Substance P
Glutamate
Calcitonin gene peptide

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3
Q

Opioid receptors

A

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

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4
Q

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

A

Mu

Mu = Morphine Agonist

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5
Q

Opioid receptor responsible for dyspnea, dependence, dysphoria

A

Kappa

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6
Q

Full Opioid Agonists

A

Morphine
Fentanyl
Hydromorphone

Codeine
Oxycodone

Methadone
Heroin

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7
Q

Partial Opioid Agonists

A

Buprenorphine

Butorphenal

Suboxone (buprenorphine + Naloxone)

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8
Q

Opioid antagonists

A

Naloxone (Narcan)

Naltrexone

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9
Q

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

A

Schedule II

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10
Q

Schedule III drugs

A

Moderate addiction potential

Hydrocodone, codeine, anaboilc steroids

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11
Q

Schedule IV drugs

A

Low addiction potential

Benzodiazepine,
Meprobamate
Butorphenol
Pentazocine
Propoxyphene
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12
Q

Why opioids can cause pruritus / uriticaria

A

Direct histamine response

Can also cause bronchospasm

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13
Q

Opioid overdose triad

A

Miosis

Loss of consciousness

Respiratory depression

much worse w alcohol or other CNS depressants

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14
Q

Antidote to opioid overdose

A

Naloxone

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15
Q

Half life of morphine

A

2 hours

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16
Q

Morphine drug interactions

A

RARE

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17
Q

Which opioid crosses the BBB

A

Morphine

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18
Q

Codeine is metabolized to

A

Morphine

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19
Q

Potency of Codeine vs Morphine

A

Codeine has 50% potency of morphine

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20
Q

What drugs inhibit effect of codeine and why?

A

2D6!

Buproprion
Cimetidine
Cocaine
Celecoxib

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21
Q

Codeine warning

A

ULTRA METABOLIZERS

esp infants nursing from mothers who take it

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22
Q

3 Kinds of oxycodone

A

Roxicodone
Percocet
Oxycontin

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23
Q

Why is oxycodone such a high potency analgesic?

A

Mu AND Kappa activity

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24
Q

Percocet =

A

Oxycodone + Acetaminophen

25
Q

Most commonly used opioid

A

Hydrocodone

26
Q

Hydrocodone metabolized to _____ by ______

A

HydoMORphone, by 2D6 (just like codeine)

27
Q

Vicodin =

A

Hydrocodone + Acetaminophen

aka Lorcet or Lortab

28
Q

Hydromorphone ex

A

Dilaudid

Exalgo

29
Q

Hydromorphone 1/2 life

A

4 hours

MORE POTENT THAN MORPHINE

30
Q

Which is more potent - morphine of hyrdromorphone

A

HYDROMORPHONE (Dilaudid)

31
Q

How is hydromorphone metabolized and what does that indicated?

A

Metabolized by Glucuronidation

Indicates LIVER activity

32
Q

10x more potent than Morphine

No P450 interactions

A

OXYMORPHONE

aka Opana

33
Q

80x more potent than Morphine

3A4 metabolism

A

FENTANYL

34
Q

Fentanyl administration, onset, half life

A

Transdermal patch

6-12 hr onset for analgesic effect

clearance takes up to 24 hours

35
Q

Fentanyl warnings

A
  1. Dont heat or cut patch - dose dumping

2. Cross reactive w codeine allergy

36
Q

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

A

Demerol

Anticholinergic properties

37
Q

Demerol ADR warnings

A

Neurologic toxicity

Anxiety, tremors, seizures - NOT reversible with naloxone

38
Q

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

A

Methodone

39
Q

Methodone metabolism

A

CYP3A4 and 2D6

Highly lipophilic

40
Q

Methadone ADR warning

A

Cardiotoxicity - Torsades de Pointes

41
Q

Used for heroin / opioid addiction. Has a “ceiling effect”

A

Buprenorphine

Mu agonist
Kappa antagonist

42
Q

Naloxone / Narcan ADRs

A

Headache
Myalgia
Increased BP

—opioid withdrawal

43
Q

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

A

Naltrexone

44
Q

Synthetic codeine analog

A

Tramadol

45
Q

Tramadol MOA

A

Weak Mu receptor agonist

SNRI (inhibits NE and 5HT uptake)

46
Q

Tramadol indications

A

As effective as morphine for mild - moderate pain
- labor

Less effective for severe or chronic pain

47
Q

Tramadol Warnings

A

Seizure risk at increased doses

Suicide risk

Serotonin syndrome risk

48
Q

Serotonin syndrome

A
Agitation
Confusion
High BP, HR
Dilated Pupils
Sweating
Diarrhea
Muscle twitching / rigidity
49
Q

Tramadol drug interactions

A

Carbamazepine
Serotonergic drugs

2D5, 3A4 inhibitor

50
Q

Opioid approved specifically for diabetic neuropathy

A

Tapentadol (Nucynta)

No P450 interactions!

51
Q

Tapentadol CI

A

EToH! Potentially fatal

52
Q

Which antibiotic will increase opioid effects

A

Erythromycin

53
Q

Which group of drugs will decrease the effects of methadone?

A

Rifampin
Phenytoin
Carbamazepine

54
Q

CYD 2D6 inhibitors

Amitriptyline
Bupropion
Cimetidine
Cocaine
Ranitidine
A

Increase TRAMADOL levels

Decrease effect of HYDROCODONE and CODEINE

55
Q

CYP 3A4 Inhibitors

Azoles
Verapamil

A

Increase METHADONE levels

56
Q

CYP 3A4 Inducers

Phenobarb
Phenytoin
Carbamazepine
St. John’s Wort

A

Decrease METHADONE levels

57
Q

Opioid dependence definition

A

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

58
Q

Chronic pain tx guidelines

A

Chronic Pain = lasting > 1 yr

Nonopioid tx preferred

Start w IR opioids, evaulate q 1-4 weeks

Urine drug test before initiating