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Pharm 2 > Test 4: Opioid Agonists specific drugs to know > Flashcards

Test 4: Opioid Agonists specific drugs to know Flashcards

1
Q

What is the Onset and Peak time of Morphine?

A

-IV Onset = 20 minutes
-Peak = 30-60 minutes
Variable per patient

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2
Q

What is the distribution of Morphine?

A

-35% Protein bound
-Vd 2.8 L/kg
-DOA 4-5 hours

LEAST lipophillic of the opioids (very hydrophillic)
-reason why delayed onset and longer DOA.
-Less accumulation in lipid membranes or fatty tissues.

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3
Q

What is the metabolism of Morphine?

A

-Liver via Phase 2
-Active Metabolites: issue with chronic administration or patients in renal failure (decreased clearance)

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4
Q

What Morphine’s active metabolite, and why is it a concern?

A

-Morphine-6-glucuronide (M6G)
-More potent than the parent drug in the CNS
-However, M6G is more hydrophillic than parent drug (morphine), which impedes its passage into the CNS. But, with chronic administration or in renal failure patients, M6G can enter the CNS.
-Doesn’t readily cross the BBB, but high plasma levels can increase CNS penetration
-Causes prolonged effect/excessive sedation in renal failure patients

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5
Q

What is the 1/2 life of Morphine in adults and neonates?

A

-Adults: 3-5 hours
-Neonates: 4-13 hours

Pediatrics have more TBW, so 1/2 life is longer.
-Concern for respiratory depression in kids due to extended DOA and late side effects.

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6
Q

What is the MOA of Morphine?

A

-Natural opioid agonist
-Causes inhibition of ascending pain pathways
-Alters the perception and response to pain

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7
Q

What are the CNS effects of Morphine?

A

-Sedation, then analgesia (sedation does NOT mean adequate analgesic coverage)
-Generalized CNS depression

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8
Q

What are the Respiratory effects of Morphine?

A

-Dose dependent respiratory depression
-Later sign

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9
Q

What are the Cardiovascular effects of Morphine?

A

-Palpitations
-Hypotension: r/t histamine release and vasodilation
-Bradycardia (should this be tachycardia?)

Large histamine release = dec SVR, dec BP, and inc HR

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10
Q

How does Morphine cause pruritus?

A

Centrally mediated effect via Mu receptors.

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11
Q

What are the local effects of Histamine release from Morphine?

A

Local itching, redness, or hives near the site of IV injection.

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12
Q

Is Morphine a common choice for intra-op pain?

A

No, fentanyls are more common.
-Morphine has a slow onset and slow peak effect
-Also has a large patient variability
-So much more common post op than intra-op.

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13
Q

What are the Onset and Peak times of Hydromorphone?

A

-IV onset: 15-30 minutes
-Peak: 30-90 minutes
Used at the end of the case, helps create a steady state (can give 0.2 mg q 15-30 minutes to create a steady state)

7-8xs more potent than Morphine. Less hydrophillic = faster onset.

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14
Q

What is the distribution of Hydromorphone?

A

-20% Protein bound
-Vd = 4 L/kg
-DOA = 4-5 hours

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15
Q

What is the metabolism of Hydromorphone?

A

-Liver metabolism
-No active metabolites
-Safe for renal patients.

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16
Q

What is the 1/2 life of Hydromorphone?

A

1-3 hours

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17
Q

What is the usual dose of Hydromorphone?

A

0.2 - 2 mg
-Risk of tolerance

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18
Q

What is the MOA of Hydromorphone?

A

Treatment of moderate to severe pain.
-Semisynthetic opioid agonist
-Causes inhibition of ascending pain pathways
-Alters the perception and response to pain

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19
Q

What are the CNS effects of Hydromorphone?

A

Generalized CNS depression
Can cause N/V

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20
Q

What are the respiratory effects of Hydromorphone?

A

-Cough suppression via direct action in the medulla
-Respiratory depression

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21
Q

What are the cardiovascular effects of Hydromorphone?

A

S/Sx can differ depending on patient.
-Palpitations
-Hypotension
-Peripheral vasodilation
-Tachycardia
-Bradycardia
-Flushing
Less anaphylactic profile compared to morphine. No histamine release.

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22
Q

What are the Onset and Peak times of Fentanyl?

A

-IV Onset = 2-5 minutes
-Peak = 20-30 minutes

Highly lipophillic!

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23
Q

What is the distribution of Fentanyl?

A

-84% Protein bound
-Vd = 4 L/kg
-DOA = 0.5 - 1 hour

24
Q

What is the metabolism of Fentanyl?

A

-First pass uptake in the lungs with temporary accumulation before release into the periphery!! (Unique to fentanyl and its derivatives)
-Liver via N-dealkylation & hydroxylation to inactive metabolites
-Clearance dependent on hepatic blood flow
-Eliminated in urine & bile
-Elimination is prolonged in elderly and neonates.

25
Q

What is the 1/2 life of Fentanyl?

A

-2-4 hrs
-single dose actions terminated by redistribution
-continuous infusion actions terminated by elimination

26
Q

What is the usual dose of Fentanyl?

A

-Induction = up to 1-2 mcg/kg
-Maintenance = 25-100mcg

27
Q

What are the Phenylpiperidines?

A

-Fentanyl
-Alfentanil
-Sufentanil
-Remifentanil

28
Q

What is the MOA of Fentanyl?

A

-80 to 100 xs more potent than Morphine
-Synthetic opioid agonist
-Increases the pain threshold
-Inhibits ascending pain pathways
-Phenylpiperidine

29
Q

What are the CNS effects of Fentanyl?

A

-Profound dose dependent analgesia & sedation
-Drowsiness
-Confusion

Implicated in N/V

30
Q

What are the Respiratory effects of Fentanyl?

A

-Dose dependent depression
-Muscle rigidity/chest wall rigidity (loss of compliance in chest wall)

31
Q

What are the Cardiovascular effects of Fentanyl?

A

Overall, pretty stable with CV.
-Bradycardia (transient)
-Hypotension
-Peripheral vasodilation

32
Q

What are the routes of administration for Fentanyl?

A

-IV, PCA, Transdermal patch
-Intrathecal & epidural
-Transnasal or Transpulmonary (mucosal absorption)

33
Q

What are the Onset and Peak times of Remifentanil?

A

-IV Onset = 1 min
-Peak = 1 min

Moderately lipophillic.

34
Q

What is the distribution of Remifentanil?

A

-58% protein bound
-Vd = 0.39 L/kg (smallest Vd)
-DOA = 5-10 minutes

35
Q

What is the metabolism of Remifentanil?

A

-Rapidly metabolized in the blood by tissue esterases
-Via hydrolysis catalyzed by general esterase enzymes to a less active compound (Succ metabolism does not influence Remi’s metabolism)

Doses are non-cumulative. Rapid recovery occurs after stopping infusion.

36
Q

What is the 1/2 life of Remifentanil?

A

9 minutes (8-20 min)

37
Q

What is the dose of Remifentanil?

A

-Comes in a powder that has to be reconstituted.
-If in drip format, start at low dose and see how patient responds.
0.2 - 2 mcg/kg/min.

38
Q

What is the MOA of Remifentanil?

A

100-200xs more potent than Morphine
-Synthetic opioid agonist
-Phenylpiperidine with an ester link
-Increases the pain threshold & alters pain perception
-Inhibits ascending pain pathways

39
Q

What are the CNS effects of Remifentanil?

A

Occur in <10% of patients.
-Dizziness
- HA
- Agitation
- Fever

Also N/V

40
Q

What are the CV & Resp effects of Remifentanil?

A

CV: Dose dependent hypotension & bradycardia
Resp: Depression
Muscle rigidity/truncal rigidity (same as with Fentanyl)

41
Q

Can you use Remifentanil for post op pain control?

A

No: Need a plan for management of post-op pain (Blue Box)

Risk for OIH: Opioid Induced Hyperalgesia. Need a longer acting agent on board before a short acting agent is metabolized away.

42
Q

Can you bolus Remifentanil pre-op or post-op?

A

No, due to risk of respiratory depression

43
Q

Why can you NOT give Remifentanil Intrathecally or Epidurally?

A

-Commercial preparation is as a powder and needs to be reconstituted (1mg, 2mg or 5 mg vials)
-Water-soluble lyophilized (freeze-dried) powder that contains a free base + glycine (transport vehicle)
-Potential for glycine neurotoxicity = DO NOT USE INTRATHECALLY OR EPIDURALLY

44
Q

What are the Onset and Peak times of Sufentanil?

A

-IV Onset = 1-3 minutes
-Peak = unknown. Maybe less than 5 minutes?
-Highly lipophillic

45
Q

What is the distribution of Sufentanil?

A

-93% Protein bound
-Vd = 2 L/kg
-Dec Vd in elderly
-DOA is dose dependent

46
Q

What is the metabolism of Sufentanil?

A

Hepatic via O-demethylation and N-dealkylation.
-1/2 life = 6 hours

47
Q

What is the dose of Sufentanil?

A

-Infusion 0.05 – 0.5 mcg/kg/hour
-Bolus 0.1 – 2 mcg/kg (1-2 mcg/kg if used for induction)
-D/C 30-60 min prior to emergence if you want them to breathe on their own.

Can be mixed into Spinal or Epidural.

48
Q

What is the MOA of Sufentanil?

A

5-10 xs more potent than Fentanyl (which was 80-100xs more potent than Morphine).
-Synthetic opioid agonist
-Increases the pain threshold
-Inhibits ascending pain pathways
-Phenylpiperidine

49
Q

List the Phenylpiperidines in order of most to least potent.

A

Sufentanil > Fentanyl = Remifentanil > Alfentanil

50
Q

When is Sufentanil used?

A

Used where profound and often long term anesthesia/analgesia is required.
-Cardiac
-Chronic Pain
-Free tissue transfers (flaps)

51
Q

What are the CNS effects of Sufentanil?

A

-Dose dependent sedation & depression

N/V

52
Q

What are the CV & Resp effects of Sufentanil?

A

CV: Bradycardia & hypotension
Resp: Dose-dependent respiratory depression (inc incidence of depression in the elderly due to dec Vd).

53
Q

What is Context-Sensitive Half Time?

A

The time required for plasma concentrations of a drug to decrease by 50% after discontinuation of an infusion.
-Cannot be predicted by elimination half-life
-Depends on drug distribution
-Explains the duration of action of a drug infusion after the infusion has stopped

Reflects several pharmacokinetic principles
1) As a drug infuses into the body it accumulates in the body’s tissues
-The longer the infusion(context) the more accumulation in the tissues until saturation
-Once the infusion is D/C the stored drug will redistribute back into plasma and maintain the effects
2) Each drug accumulates at a different rate and to a different extent based on its physiochemical properties
3) Drugs are removed from the blood through two major mechanisms
-Distribution – where the drug moves from the blood to the tissues
-Excretion – where the drug is metabolized or excreted unchanged. Does the drug have an active metabolite?

54
Q

What is the CS 1/2 time of Remifentanil?

A

Short, stable and wears of very quickly after stopping the infusion.

Remi is pretty static. Turn it off and it’s gone.
-To drop it 50% after 1 hour is 1-2 minutes. To drop it 75% after 1 hour is 7-8 minutes.
-Wears off quickly no matter how long you ran it.

55
Q

What is the CS 1/2 time of Fentanyl?

A

Variable, take much longer to wear off and is less predictable.
-Takes a long time for concentration to drop. Why we don’t use fentanyl drips. Plasma concentration stays very high, takes longer to wear off.

56
Q

What is unique about the CS 1/2 time of Morphine?

A

Morphine has active metabolite: 10% of metabolized morphine becomes M6G - increasing DOA.

Pharm 2 (40 decks)

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