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Clinical Pharmacology > Opioid analgesics > Flashcards

Opioid analgesics Flashcards

1
Q

What is an opiate?

A

drug derived from opium poppy

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2
Q

What is the persistent, compulsive continuation of a behavior or use of a chemical substance despite its adverse effects?

A

addiction

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3
Q

What is a decreased drug response to a drug w/ continued administration that can be overcome with increasing the dose?

A

drug tolerance

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4
Q

What is the continued need of a user to take a drug?

A

drug dependence

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5
Q

What’s the class of natural endogenous peptides that bind to human mu delta, and kappa opiod receptors?

A

endogenous opioid peptides

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6
Q

How much do chronic pain syndromes cost the country?

A

65-70bill annually

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7
Q

What’s the difference between acute and chronic pain?

A

acute is related to an event and resolves and not requiring long term medication, while chronic is not always identified and includes multiple types of pain, prolonged durations

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8
Q

What type of pain has direct simulation, transmission along normal nerves, with tissue injury apparent, and source is from somatic or visceral stimulants?

A

nociceptive

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9
Q

What type of pain is caused by disordered peripheral or central nerves which can exceed observable injury and can be described as burning, tingling, shooting, stabbing, or electrical?

A

neuropathic

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10
Q

What is the function of the mu opioid receptor subtype?

A

supraspinal and spinal analgesia, sedation, inhibition of respiration, slowed GI transit, modulation of hormone and neurotransmitter release

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11
Q

What is the function of the delta receptor subtype?

A

supraspinal and spinal analgesia, development of tolerance

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12
Q

What is the function of the kappa receptor subtype?

A

supraspinal and spinal analgesia, sedative actions, slowed GI tract

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13
Q

How do opiods act?

A

by binding to the receptors, modifies sensory to pain

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14
Q

What are the advantages of opiods?

A

multiple routes of administration, ease of titration, reliable, effective

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15
Q

What are some opioid agonists?

A

codeine, fentanyl, hydrocodone, hydromorphone, methadone, morphine, oxycodone

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16
Q

What are some weak agonists/reuptake inhibitors?

A

tapentadol and tramadol

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17
Q

What are some weak agonist-antagonists?

A

buprenorphine

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18
Q

What are some antagonists?

A

naloxone, naltrexone, methylnaltrexone, naloxegol

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19
Q

What’s the opioid MOA?

A

close channels on PREsynaptic nerve and inhibit POSTsynpatic inhibing transmission of signal

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20
Q

What opioids are metabolized by cytochrome CYP2D6 to active metabolites?

A

Codeine –> morphine
oxycodone –> oxymorphone
hydrocodone -> hydromorphone

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21
Q

What route is preferred?

A

oral, but can take 45 minutes, with IV reserved for severe pain

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22
Q

How do most opioid agonists metabolize?

A

hepatically with eliminaton by kidneys

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23
Q

How is morphine different?

A

undergoes glucuronidation to metabolite similar

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24
Q

What are opioid agonist ADRs?

A

drowsiness and sedation, N/V with ambulation, cough suppressant/CO2 levels rise, pupillary constriction (except meperidine)
pinpoint pupils, constipation, urinary retention, flushing, pruritus, diaphoresis

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25
Q

How is mereperidine different?

A

can cause tachycardia instead of bradychardia and can have high histamine release

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26
Q

histamine release

A

natural>semi-synthetic>synthetic

merpiridine, codeine, morphine > hydrocodone, oxycodone > hydromorphone, fetanyl

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27
Q

The more ____ the opioid, the ___ histamine release

A

potent, less

28
Q

How can you manage opioid ADRs?

A

bowel regimen, decrease dose, take w/ food, antihistamine or consider other drugs

29
Q

How can you manage mood changes?

A

decrease dose, consider longer acting

30
Q

How do you manage urinary retention?

A

catheter, more non-opioids

31
Q

What class cannot be refilled

A

class 2

32
Q

What class can only be refilled with a 6 month limit?

A

3

33
Q

What do you counsel the patient with?

A

can cause drowsiness, do not operate machinery, night vision may be affected, do not share, do not chew or crush

avoid alcohol and caution w/ CNS depressants, and prescribe laxatives like bisacodyl/docusate and PEG

34
Q

What signifies an allergic reaction to an opioid?

A

difficulty breathing, severe drop in BP, rash, swelling, use agent in different class

35
Q

If you have an allergy to morphine, codeine, hydrocodone, hydromorphone, or oxycodone, what do you use?

A

fetanyl, meperidine, methadone, tramadol, or tapentadol

36
Q

What are examples of group 1 opiates?

A

morphine, codeine, thebaine, natural, group 1

37
Q

What are examples of semi-synthetics?

A

hydrocodone, oxycodone, hydromorphone, oxymorphone, buprenorphine, group 2

38
Q

What are examples of synthetics?

A

fetanyl, methadone, tramadol, propoxyphene, meperidine, group 3 and CAN be used with an allergy to others

39
Q

What are some strong opioids?

A

morhpine, hydromorphone (dialudid), meperidine (demerol), fentanyl, methadone

40
Q

What are some moderate opioid agonists?

A

oxycodone (oxycontin, percodan, percocet), hydrocodone (lortab, norco, vicodin, vicoprofen), codeine (tylenol w/ codeine)

41
Q

When should you avoid morphine?

A

renal dysfunction

42
Q

How is codeine usually prescribed?

A

in combo with APAP or promethazine (antitussive)
CYP2D6 = ultra–rapid metabolizers
avoid in peds

43
Q

When should you use caution with hydrocodone?

A

with APAP products

44
Q

When should you avoid using oxycodone?

A

with CYP3A4 inhibitors

45
Q

When should you use caution using hydromorphine?

A

with CYP3A4 (use low doses) and very potent!

46
Q

How is fetanyl used?

A

only for chronic pain and can be a patch, IV, lollipop, and also caution with CYP3A4 inhibitors

47
Q

How is meperidine (demerol_ used?

A

sometimes for shivering post-op, can increase risk of serotonin syndrome, AVOID using as an analgesic, and can accumulate with renal failure and cause CNS toxicity

48
Q

How is methadone used?

A

treatment of patients addicted to narcotics, Wide variability in half life, risk of QT prolongation, with MANY drug interactions

49
Q

What opioids should you avoid in hepatic impairment?

A

codeine, meperidine

50
Q

What opioids should you use with caution in hepatic impairment?

A

oxycodone, hydrocodone, morphine, fetanyl

51
Q

What opioids should you avoid in renal impairment?

A

morphine, codeine, meperidine, tramadol

all others use cautiously

52
Q

What’s tramadols moa?

A

agonist/reuptake inhib, weak mu agonist, serotonin/nore reuptake inhibitor

53
Q

what are ADRs of tramadol?

A

lowers seizure threshold and serotonin syndrome, nausea

54
Q

When can you not use tramadol?

A

mao-i use within 14 days, Hx of epilepsy

55
Q

What is the MOA of tapentadol?

A

agonist/reuptake inhib, moderate mu agonist, strong NE reuptake inhibitor, weak 5-HT inhibitor

56
Q

What are ADRS of tapentadol?

A

seizures and serotonin syndrome

57
Q

Is tapentadol effective?

A

as effective as oxycodone with lower GI effects

58
Q

What’s the MOA of buprenorphine?

A

mixed agonist-antagonist, partial Mu agonist, kappa antagonist, for moderate pain or opioid use abuse

59
Q

Is buprenorphine oral bioavailable?

A

no, need to give sublingually

60
Q

Why is naloxone added to buprenorphine?

A

to prevent abuse, Suboxone

61
Q

What are signs/symptoms of opioid overdose?

A

somnolence/difficulty to arouse, respiratory depression, cold/clammy skin, constricted pupils

62
Q

What are warnings w/ naloxone?

A

will cause withdrawal and repeat doses may be needed

63
Q

Does methylnaltrexone and naloxegol have an effect on analgesia and enter CNS?

A

no

64
Q

What can methylnaltrexone and naloxegol cause?

A

severe diarrhea, GI perf do not use with GI obstruction and strong 3A4 inhibitors (naloxegol)

65
Q

What can you switch a patient to for less itching?

A

hydromorphone and fetanyl are lowest

Clinical Pharmacology (14 decks)

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