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Junior - Pharm II - 1 > 3 - Opioids > Flashcards

3 - Opioids Flashcards

1
Q

What are Mu1 receptors responsible for:

A

Analgesia

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2
Q

What are Mu2 receptors responsible for:

A

Respiratory depression, miosis, reduced gastric motility, sedation, euphoria, pruritis, urinary retention, PHYSICAL DEPENDENCE

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3
Q

What are Kappa receptors responsible for?

A

Contribute to analgesic properties (but Mu1 is responsible for most of the analgesia)

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4
Q

What is the Delta receptor responsible for?

A

Located in the periphery and selective for enkephalins

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5
Q

Which is more hydrophilic - morphine or fentanyl?

A

Morphine

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6
Q

Which is more lipophilic - morphine or fentanyl?

A

Fentanyl

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7
Q

What causes tolerance?

A

Down-regulation of opioid receptors

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8
Q

What is opioid-induced hyperalgia?

A

Increased pain or pain sensitivity without a change in medical condition

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9
Q

Desensitization is the result of:

A

Down-regulation

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10
Q

Which opioid is associated with the greatest histamine release and thus “itching” sensation?

A

Morphine

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11
Q

Morphine - MOA?

A

High affinity for Mu1 and Mu2

Weak affinity for Delta/Kappa

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12
Q

Morphine - pharmacokinetics:

A

Significant first pass effect if oral

Least lipophilic - only a small amount crosses BBB -> less euphoria than fentanyl or heroin

Will cross placenta

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13
Q

Heroin is __ times more potent than morphine

A

6

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14
Q

Presence of morphine in urine could indicate exposure to:

A

Morphine
Heroin
Codeine

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15
Q

Morphine - AE’s?

A

Increases ICP (caution in head injury)

Respiratory depression

N/V

Pruritus

HOTN

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16
Q

Hydromorphone (Dilaudid) - MOA:

A

Mu receptor agonist

Metabolite of morphine

More lipophilic than morphine

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17
Q

Hydromorphone (Dilaudid) - note on extended release form:

A

Requires provider training q 2 yrs - Risk Evaluation and Mitigation Strategy (REMS) drug

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18
Q

Hydrocodone ER (Zohydro ER) - MOA:

A

Less binding affinity than morphine

Metabolizes to hydromorphone

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19
Q

Oxycodone (OxyContin) - MOA:

A

Mu receptor agonist - low binding affinity

Metabolizes to noroxycodone and oxymorphone (active metabolites)

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20
Q

Oxymorphone (Numorphan) - MOA:

A

Semi-synthetic Mu receptor agonist

Greater analgesic profile than morphine

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21
Q

Codeine - MOA:

A

PRODRUG (no analgesic activity)

Metabolized to morphine

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22
Q

Codeine - clinical use:

A

Mild to moderate pain

Antitussive

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23
Q

Codeine - box warning:

A

Death delated to ultra-rapid metabolism of codeine to morphine

Not recommended for peds <12

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24
Q

What is the CYP enzyme responsible for converting codeine to morphine?

A

CYP2D6

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25
Q

If Codeine is single ingredient, what schedule?

A

II

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26
Q

If codeine combined with another analgesic (i.e. APAP), what schedule?

A

III

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27
Q

If Codeine combined with Guaifenesin (cough medicine), what schedule?

28
Q

Buprenorphine (Buprenex) C-III - MOA:

A

Mixed agonist/antagonist

Partial Mu agonist and Kappa ANTagonist

29
Q

Buprenorphine (Buprenex) - clinical use?

A

Opioid detoxification

As effective as methadone

Resistant to naloxone d/t long duration of action

30
Q

Butorphanol (Stadol) C-IV - MOA?

A

Partial Mu and Kappa agonist

31
Q

Butorphanol (Stadol) C-IV - clinical use:

A

Pain management

Pain during labor (if epidural is not possible)

32
Q

Butorphanol (Stadol) C-IV - AE’s?

A

Can produce unwanted dysphoria

33
Q

Nalbuphine (Nubain) - MOA:

A

Not controlled

Partial Mu antagonist

Strong Kappa agonist

34
Q

Nalbuphine (Nubain) - clinical use:

A

Sedation with minimal respiratory depression

Used to reverse ventilatory depression in opioid overdose WHILE MAINTAINING some alalgesia

Think “Nubain” is the kinder Narcan

35
Q

Meperidine (Demerol) C-II - MOA:

A

Strong Mu and Kappa agonist

Anticholinergic effects

36
Q

Meperidine (Demerol) C-II - clinical use:

A

ACUTE DOSING ONLY

Relief of moderate to severe pain

SHIVERING AND RIGORS

USE NOT GENERALLY RECOMMENDED

37
Q

Meperidine (Demerol) C-II - CI’s?

A

Renal impairment

MAOI’s

Hepatic impairment

Elderly (caution)

38
Q

Meperidine (Demerol) C-II - AE’s?

A

Anticholinergic effects (can cause tachycardia and mydriasis)

HOTN, delirium, seizures

Severe withdrawal

GENERALLY - AVOID THIS DRUG

39
Q

Fentanyl C-II - MOA:

A

Mu receptor agonist

Synthetic

75 to 125 time more potent than morphine

More lipophilic (easily crosses BBB leading to more euphoria)

Rapid onset/shorter duration than morphine

40
Q

Fentanyl - pharmacokinetics:

A

Renal excretion

Easy distribution in tissues due to high lipohilicity

41
Q

Fentanyl - clinical use?

A

Moderate to severe pain (acute)

Moderate to severe pain (chronic)(patches)

42
Q

Fentanyl - transdermal onset of action:

A

12 to 24 hours

43
Q

What is the TIRF REMS program?

A

Transmucosal Immediate Release Fentanyl Risk Evaluation and Mitigation Strategy

Mitigate the misuse, addiction, overdose, and serious complications due to medication errors with the use of TIRF medicines

44
Q

Which Fentanyl derivative has the fastest peak effect, duration and elimination?

A

Remifentanil (think “r” revved up)

45
Q

What do Alfentanil, Sufentanil, and Remifentanil all have in common?

A

They don’t accumulate when infused

46
Q

Methadone - MOA:

A

Potent agonist of Mu, Kappa, Delta

Antagonist of NMDA receptor

Inhibits serotonin and norepi reuptake

47
Q

Methadone - clinical use:

A

Chronic pain syndrome (CA, non-CA, neuropathic)

Detoxification of opioid addiction

48
Q

Methadone half-life?

A

Unpredictable - 8 to 59 hours

Difficult to titrate

Analgesia duration is SHORTER than t1/2, toxicity d/t accumulation can occur

49
Q

Methadone - cardiac AE’s?

A

Arrhythmias can occur - prolonged QT interval

50
Q

Pentazocine (Talwin) C-IV - MOA:

A

Partial Mu agonist

Full kappa agonist

51
Q

Pentazocine (Talwin) C-IV - clinical use:

A

Moderate to severe pain

Labor when epidural is not possible

52
Q

Pentazocine (Talwin) C-IV - AE’s:

A 
HTN
Hallucinations
Dysphoria
Dizziness
Tachycardia
53
Q

Tramadol (Utlram) C-IV: MOA:

A

Partial Mu receptor agonist

Serotonin and norepinephrine reuptake inhibitor

54
Q

Tramadol (Ultram) - metabolism:

A

Majority of therapeutic activity depends on metabolism

Ultra-rapid metabolizers -> significant respiratory depression

55
Q

Tramadol (Ultram) C-IV- AE’s:

A

SEROTONIN SYNDROME

Seizures reported at recommended doses

56
Q

Tapentadol (Nucynta) C-II - MOA:

A

Chemically similar to tramadol

Mu agonist, norepi reuptake inhibitor

57
Q

Tapentadol (Nucynta) C-II - clinical use?

A

Diabetic peripheral neuropathy (ONLY OPIOID WITH THIS INDICATION)

58
Q

What is the only indication for oral Naloxone?

A

Opioid-induced constipation

59
Q

Naltrexone - MOA:

A

Mu receptor competitive antagonist

Competes but does not displace opioids

60
Q

Naltrexone - clinical use:

A

Longer duration of action (10 hrs)

Tx of ETOH and opioid dependence

61
Q

Naltrexone can be combined with ___ for weight management:

62
Q

Nalaxone (Narcan) - MOA:

A

Competitive antagonist of Mu receptors - displaces opioids

63
Q

Nalaxone (Narcan) - clinical use:

A

Reversal of opiate overdose

64
Q

Naloxone can be given every ___ to ___ minutes:

65
Q

When tapering off opioids, what percentage deduction in amount of drug (for non-addicted patients):

A

20 to 50 percent (of original dose) per week

Junior - Pharm II - 1 (6 decks)

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