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1Fall24 PoA II > Acute Pain & OFA pt2 > Flashcards

Acute Pain & OFA pt2 Flashcards

1
Q

Codeine metabolism is variable due to more than ____ polymorphisms resulting in analgesic variability.

A

50

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2
Q

What is the adult dose and max of codeine?

A

15 - 60 mg q4

360mg max per day

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3
Q

What is the pediatric dose and max of codeine?

A

0.5 - 1 mg/kg/dose

60mg max per day

should be avoided in children?

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3
Q

60mg of codeine (maximal dose) is equivalent to how much aspirin?

A

650mg

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4
Q

What drugs does codeine have interactions with? (3)

A

Opioids, EtOH, and Anticholinergics

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5
Q

What drug is described by the following?

A

Tramadol

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6
Q

Where does the + enantiomer of tramadol have affinity and what does it do? (3)

A

Centrally acting opioid agonist:
- μ → moderate affinity
- K & δ → weak affinity
- Opposes serotonin reuptake

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7
Q

What does the - entantiomer of tramadol do? (2)

A
  • Inhibits NE reuptake
  • Stimulates α2 receptors
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8
Q

What is tramadol metabolized into and what is the relevance of its metabolite?

A

Tramadol → CYP3A4 & 2D6 → O-desmethyltramadol (2-4 times more potent)

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9
Q

What is tramadol’s potency compared to morphine?

A

1/5 to 1/10

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10
Q

What is the oral onset for tramadol?

A

1-2 hours

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11
Q

What is the half life of tramadol?

A

6.3 hours

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12
Q

When is tramadol contraindicated? (2)

A
  • Seizure Disorders
  • PONV
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13
Q

What are the benefits of tramadol vs other opioids? (3)

A
  • Minimal respiratory depression
  • Minimal-none addiction
  • Minimal constipation
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14
Q

Oral morphine dose is ____ times the IM or IV route.

A

3

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15
Q

What receptors are primary affected by morphine?

A

μ-1 and μ-2

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16
Q

What are the two principle active metabolites of morphine? (also list effects)

A
  • Morphine-6-glucuronide → analgesia
  • Morphine-3-glucuronide → neurotoxicity & hyperalgesia
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17
Q

How is morphine metabolized?

A
  • Hepatic: conjugation w/ glucuronic acid
  • Kidneys
18
Q

What factors contribute to morphine’s minimal CNS absorption?

A
  • ↓ lipid solubility
  • ↑ protein binding
  • ↑ Ionization at normal bodily pH
19
Q

What is the IV/IM onset and peak of action for morphine?

A

Onset: 15-30 min
Peak: 45-90 min

20
Q

What differences does morphine exhibit in women vs men?

A

In women:
↑ analgesic potency
↓ speed of offset

21
Q

What is the protein binding of morphine?
What about the half-time?

A

35% protein binding
1.7 - 3.3 hours

22
Q

What is released from morphine administration?
What is the result?

A

Histamine → vasodilation and hypotension

23
Q

Morphine should be avoided in patients with ____ impairment as the metabolite morphine–6-glucuronide can accumulate and lead to _________ ________.

A

Renal impairment : respiratory depression

24
Q

What drug is a semisynthetic derivative of thebaine and is the most used opioid worldwide?

A

Oxycodone

25
Q

What are the metabolites of oxycodone?

A

Oxymorphone (active)
Noroxycodone (inactive)

Oxycodone is primarily a prodrug.

26
Q

What is the site of action of oxycodone?

A

μ and κ receptors of the CNS

27
Q

What are the two types of PO oxycodone?

A

IR = Immediate release
CR = Controlled release

28
Q

What is the dose of oxycodone?

A

10 - 15mg (equivalence with 10 mg morphine)

29
Q

What is the onset of action of oxycodone?

A

< 1 hour

30
Q

Opioids (in general) exhibit an ____ effect with other drugs that are CNS depressants

A

additive

31
Q

Why is methadone used for opioid addiction maintenance? (3)

A
  • 60-95% oral bioavailability
  • High potency
  • Long duration of action
32
Q

What should be known about methadone’s half life?

A

Very long and unpredictable (up to 36 hours)
Can accumulate w/ repeated doses

33
Q

What various receptors affinities does methadone have? (4)

A
  • Weak noncompetitive NMDA antagonist
  • Serotonin reuptake inhibitor
  • Monoamine reuptake inhibitor
  • High μ receptor affinity
34
Q

What would occur with concurrent methadone and carbamazepine use?

A

Carbamazepine is a CYP450 inducer thus methadone will be metabolized faster.

35
Q

What agents can inhibit the metabolism of methadone?

A

CYP450 Inhibitors:

  • Antiretrovirals
  • Grapefruit juice
36
Q

How much is methadone clearance affected by hepatic and renal impairment?

A

Not much

37
Q

What is the dose of methadone?

A

2.5 - 10 mg PO/IM/SC q4-12 hours

38
Q

Why are standardized simple dosing guidelines unachievable for methadone?

A

High variable half life (8-80 hours)

39
Q

What is the worst med interaction associated with methadone?

A

MAOI’s

40
Q

What drugs are known to increase the concentration/effects of methadone? (3)

A
  • Cipro
  • Diazepam
  • Acute EtOH
41
Q

What drugs are known to decrease concentration/effects of methadone? (5)

A
  • Anti-retrovirals
  • Phenobarbital
  • Phenytoin
  • Rifampin
  • MAOI’s
42
Q

What cardiac complication can occur in rare cases with methadone usage?

A

Pause dependent dysrhythmia

43
Q

What is the half life of codeine?

A

3-3.5 hours

1Fall24 PoA II (30 decks)

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