Pain Opioids 3 Flashcards

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1
Q

How does hydromorphone compare to morphine regarding

  • lipid solubility
  • Onset of action
  • Potency
A

More lipid soluble
Faster onset
5X more potent

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2
Q

What are the 2 metabolites of hydromorphone? How does the active metabolite compare to morphine-6-glucuronide

A

Hydromorphone-6-glucuronide
Hydromorphone-3-glucuronide
Hydromorphone-6-glucuronide less active at receptor than morphine-6-glucuronide

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3
Q

What is the product of hydrocodone metabolism? What is the enzyme responsible?

A

Hydromorphone

CYP2D6

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4
Q

When hydrocodone is combined with acetamenophen, you get _ (2)

A

Vicodin

Lortab

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5
Q

What is oxycodone metabolized to? What us the enzyme responsible?

A

Oxymorphone

CYP2D6

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6
Q

How is codeine related to morphine? What enzyme metabolizes codeine?

A

It is a prodrug that is demethylated to yield morphine

CYP2D6

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7
Q

How is heroin related to morphine? What property makes it a drug of abuse?

A

It is converted to monoacetyl morphine, then into morphine in the brain
Euphoria, Lipid soluble, fast onset

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8
Q

How is methadone administered? What makes it unique? What is it used for (2)?

A

Orally
Ultra long lasting (half life or 15-60 hrs)
Opioid addiction, pain management

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9
Q

How does meperidine compare to morphine with regards to:

  • Lipid solubility
  • Potency
A

More lipid soluble

1/10 X potency

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10
Q

What is the metabolic product of meperidine? Where does this occur? What are 2 potential side effects of this metabolite?

A

nor-meperidine
Liver
CNS stimulation, convulsions

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11
Q

What patient subpopulation may be at risk for serious meperidine side effects?

A

Patients with renal failure, not cleared as needed

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12
Q

What are the components of the serotonin syndrome triad?

A

Neuromuscular hyperactivity
Autonomic hyperactivity
Altered mental status

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13
Q

What mu opioid agonist is associated with serotonin syndrome? This is especially true when combined with _ (2)

A

Meperidine

SSRIs or MAOs

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14
Q

What is the activity of tramadol at the mu receptor? What other receptor does it function at?

A

Partial agonist

Inhibitor of the monoamine reuptake inhibitor

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15
Q

What is ultracet? What enzymes metabolize tramadol / ultracet? Which gives its active metabolite?

A

Utracet = Tramadol + acetamenophen
CYP2D6 and CYP3A4
CYP2D6

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16
Q

What is tapentadol? What enzyme metabolizes it? What advantage does it have over tramadol?

A

Partial mu agonist and inhibitor of the monoamine reuptake inhibitor
CYP2C9 and CYP2C19
Less pharmacogenetic variability

17
Q

What is the receptor activity profile for pentazocine, butorphanol and nalbuphine? What are these drugs used for (2)?

A

Kappa agonists, mu partial agonists or antagonists

Acute short term pain and to manage side effects

18
Q

What is the receptor activity profile for buprenorphine? How does its affinity for the mu receptor affect its clinical use? What can it be used for?

A
  • Partial mu agonist, full kappa agonist
  • Very high affinity at mu receptor, hard to displace, therefore hard to provide analgesia for surgical patients
  • Drug abuse and addiction
19
Q

Regarding pharmacokinetics, where are majority of phase 1 enzymes found? (2)

A

Gut

Liver

20
Q

How can a clinician account for the variability of opioid activity from patient to patient?

A

Titrate to effect

21
Q

What are 2 mu agonists that can be used to treat diarrhea? What are their unique properties?

A

Diphenoxylate
Loperamine
Poorly / Not absorbed

22
Q

What are the 4 examples of opioid antagonists provided?

A

Naloxone
Naltrexone
Almivopan
Methylnaltrexone

23
Q

How do naloxone and naltrexone compare regarding duration of action and administration?

A

Naloxone is administered IV , naltrexone is oral

Naltrexone is also very long lasting

24
Q

A poorly absorbed orally active opioid antagonist that antagonizes the GI side effects of opioids. This describes _

A

Almivopan

25
Q

Quaternary ammonium derivative that is positively charged. IV peripherally restricted opioid antagonist for
constipation. This describes _

A

Methylnaltrexone

26
Q

2 opioid formulations designed to provide pain relief by be resistant to abuse is _

A

ER morphine with sequestered naloxone

Oxycodone-naloxone

27
Q

A prodrug for oxymorphone is _. The enzyme responsible for metabolism is _

A

Oxycodone

CYP2D6

28
Q

Why is acetaminophen, and not NSAIDs, combined with opioids?

A

Acetaminophen safer than NSAIDs, less side effects, therefore patient can use more of drug without problems. If patient stops an opioid combined with NSAIDs, can get withdrawal

29
Q

CYP2D6 is involved in the metabolism of a lot of opioids. What is a drug where its pharmacogenomic variability is actually clinically significant?

A

Dosing of codeine

30
Q

What is an advantage of the fentanyl patch? What is an advantage of oral fentanyl? Another use for fentanyl beyond pain relief is _

A
  • Hard to abuse patch
  • Rapid onset and potent orally
  • Sedation
31
Q

What are 3 plausible explanations for variable responses to opioids between patients?

A

Mu receptor polymorphisms
Drug metabolisms differences
Increased drug efflux from tissues
** All related to pharamcogenetics **