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N524 Summer Pharm > Opioids > Flashcards

Opioids Flashcards

1
Q

Which opioid is naturally occurring? Semisynthetic opioids?

A

Natural: Morphine
Semisynthetic: Heroin, hydromorphone, codeine

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2
Q

Opioid structures: phenanthrene vs. benzylisoquinolines?

A

Phenanthrene: contains benzene rings
Benzylisoquinoline: from alkaloid plant

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3
Q

What are the four types of exogenous synthetic opioids?

A
  1. Morphinan derivatives: levorphenol, butorphenol
  2. Diphenyl derivatives: methadone
  3. Benzomorphans: phenazoncine, pentazocine
  4. Phenylpiperidines: meperidine, fentanyl, alfentanil, sufentanil, remifentanil
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4
Q

Opioid partial agonist vs. mixed agonist/antagonist?

A

Agonist: buprenorphine, regardless of dose, it can’t produce full mu receptor effects like morphine
Mixed agonist/antagonist: nalbuphine, agonist at kappa receptor and antagonist at mu reversing respiratory depression (good for chronic pain patients)

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5
Q

What acts on Mu-1 receptor? What are the effects?

A 
ALL endogenous and synthetic opioid agonists 
Analgesia, euphoria, sedation
SUPRASPINAL analgesia (and some spinal)
Miosis (pupil constriction)
Bradycardia
Urinary retention
Prolactin release, hypothermia
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6
Q

What acts on Mu-2 receptor? What are the effects?

A 
ALL endogenous and synthetic opioid agonists
Hypoventilation (resp depression)
Physical dependence
SPINAL analgesia
Constipation, N/V, urinary retention
Bradycardia
Miosis
Pruritis
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7
Q

What acts on the Kappa receptor? What are the effects?

A 
DYNORPHINS act on kappa receptors
SUPRASPINAL and SPINAL analgesia
Dysphoria
Sedation
Miosis
Diuresis
Psych reactions (hallucinations, delirium)
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8
Q

What acts on the delta receptor? What are the effects?

A 
ENKEPHALINS act on delta receptors
SUPRASPINAL and SPINAL analgesia
Hypoventilation (resp depression)
Physical dependence
Constipation
Urinary retention
Pruritis
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9
Q

Which two receptors (Mu1/2, kappa, or delta) are responsible for physical dependence?

A

Mu-2 and Delta receptors

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10
Q

What G-coupled reactions occur when an opioid acts on an opioid receptor?

A
  1. MAPK cascade -> phospholipase A2 producing prostaglandins and leukotrienes
  2. K influx
  3. Ca channel inactivation -> suppression of neurotransmitter (substance P) release
  4. Dec adenylate cyclase, less cAMP
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11
Q

Are opioids strong or weak, acid or base?

A

WEAK BASES

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12
Q

Someone acidotic needs ____ (more/less) opioid

A

MORE

Because more ionization occurs

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13
Q

The higher % unionized, the higher diffusible fraction, and ____ (faster/slower) the onset
The higher unbound, the ____ (faster/slower) the onset

A

The higher % unionized, the higher diffusible fraction, and FASTER the onset
The higher unbound, the FASTER the onset

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14
Q

Which opioids are highly ionized vs non-ionized?

Morphine, meperidine, fentanyl, sufentanil, alfentanil, remifentanil

A

Non-ionized: alfentanil 89%, remifentanil 58%
The rest are highly ionized, the percents nonionized is..
Morphine 23%, meperidine 7%, fentanyl 8.5%, sufentanil 20%

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15
Q

List opioids in order of % protein binding.

Morphine, meperidine, fentanyl, sufentanil, alfentanil, remifentanil

A 
Morphine 35% (LOW)
Meperidine 70%
Fentanyl 84%
Alfentanil 92%
Remifentanil 66-93%
Sufentanil 93%
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16
Q

List opioids in order of clearance.

Morphine, meperidine, fentanyl, sufentanil, alfentanil, remifentanil

A 
Alfentanil 238 mL/min
Sufentanil 900
Meperidine 1020
Morphine 1050
Fent 1530
Remi 4000
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17
Q

List opioids in order of volume of distribution.

Morphine, meperidine, fentanyl, sufentanil, alfentanil, remifentanil

A 
Alf 27
Remi 30
Suf 123
Morphine 224
Meperidine 305
Fent 335
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18
Q

What is the partition coefficient (how much it penetrates the tissues)?
(Morphine, meperidine, fentanyl, sufentanil, alfentanil, remifentanil)

A 
Remi (no data)
Morphine 1
Meperidine 32
Alfentanil 129
Fent 955
Suf 1727
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19
Q

Do young and old patients need more or less opioids? Why?

A

LESS
Neonates have dec rate of elimination due to immature CP450
Elderly have more sensitivity to the drug

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20
Q

Are opioids dosed based on current weight or ideal body weight?

A

Ideal weight (lean body mass) not actual body weight

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21
Q

What area produces spinal analgesic effects?

A

Receptor activation in the spinal cord and dorsal root ganglia, substantia gelatinosa

22
Q

What area produces supra spinal analgesia?

A

Receptor activation in the periaquaductal/periventricular gray matter of the brain

23
Q

Opioid perioperative CNS effects?

A 
Analgesia, euphoria
Drowsy, sleep
Miosis
Nausea (chemoreceptor trigger zone)
Dec CBF, ICP (neuro stability)
24
Q

Opioid perioperative CV effects?

A

CV stable
Dose dependent bradycardia, dec CO/BP
Vasodilation
Meredine- tachycardia, myocardial depression

25
Q

Opioid perioperative ventilatory effects?

A

Respiratory depression (dose dependent)
Decrease compliance in chest wall, constricted pharyngeal and laryngeal muscles (inhibition of GABA, increase in dopamine)
Hypercarbia, hypoxia
Dec RR, inc Vt (dec Vt in high doses)
Dec hypoxic ventilatory drive
Vent response curve reduced and shifted to R

26
Q

Opioid perioperative renal/GI/liver effects?

A 
Increase peristalsis and tone of ureters
Urgency
Block catecholamine and cortisol release
Sphincter of Oddi spasm (inc biliary pressure)
Constipation, dec GI motility 
Prolonged gastric emptying
27
Q

When giving neuraxial block, cephalic movement of opioid depends lipid solubility, the more lipid solubility will cause what?

A

More lipid solubility causes limited migration (fentanyl)

Less lipid solubility causes more cephalad movement in CSF (morphine)

28
Q

Side effects of neuraxial opioids?

A

Pruritis
N/V
Urinary retention
Ventilatory depression (delayed in morphine)

29
Q

Morphine: solubility, protein binding, ionization?

A

Poor lipid solubility
Low PB 35%
Highly ionized (low nonionization 23%)

30
Q

Which two opioids are histamine releasers?

A

Morphine
Meperedine
This may be the mechanism causing pruritus

31
Q

Morphine peak? DOA?

A

Peak: 15-30 min
DOA: 4 h

32
Q

Morphine metabolism?

A

ACTIVE metabolite: M6G - morphine-6-glucuronide

Metabolized by liver, kidneys also play a role

33
Q

Meperidine is structurally similar to what drug?

A

Atropine, giving it muscarinic effects

Also similar to local anesthetics, it blocks Na channels

34
Q

Meperidine metabolism?

A

ACTIVE metabolite: normeperidine lasts 3 days, half as potent, can cause seizures

35
Q

How does hydromorphone compare to morphine?

A

5x more potent
Derivative of morphine
Q4h dosing needed
More sedation but less euphoria than morphine

36
Q

Fentanyl is _____x more potent than morphine

A

100x

37
Q

Meperidine is ____ as potent as morphine

A

1/10

38
Q

Sufentanil is _____x more potent than morphine

A

1,000x

39
Q

Sufentanil metabolism?

A

ACTIVE metabolite: desmethylsufentanil
Rapidly metabolized in liver
Undergoes first pass pulmonary uptake

40
Q

Alfentanil is ____x more potent than morphine

A

10-20x

41
Q

Remifentanil metabolism?

A

Metabolized by tissue/plasma esterases

42
Q

Remifentanil is _____x more potent than morphine

A

100 (similar to fentanyl, but slightly more potent than fentanyl)

43
Q

List the order of potency of opioids.

Morphine, meperedine, fentanyl, sufentanil, alfentanil, remifentanil, dilaudid

A 
Sufentanil (most potent)
Remifentanil
Fentanyl
Alfentanil
Dilaudid
Morphine
Demerol/meperidine
"She ran far away down main drive"
From least to most: "Dad made dinner again from ramen soup"
44
Q

What receptors are opioid Agonist-Antagonists hitting?

A

Mu- antagonist
Kappa- partial agonist
(Note: kappa receptors may cause dysphoria)

45
Q

Nalbuphine (nubain) MOA?

A

Works at kappa and sigma receptors to antagonize opioid induced respiratory depression while maintaining analgesia

46
Q

Nalbuphine (nubain) pros/cons?

A

Pro: no adverse CV problems, reverses sphincter of Oddi spasm (used instead of glucagon), analgesic response equal to morphine
Con: dyseuphoria (kappa receptor), hypotension can occur

47
Q

Butorphenol (stadol) acts as an agonist at ____ receptor and a weak antagonist at ____ receptor and is ____ x more potent than morphine

A

Agonist at kappa
Weak antagonist at mu
5x more potent than morphine

48
Q

Naloxone class of drug and MOA?

A

Opioid antagonist

Competitively blocks receptor sites (mu, kappa, delta) and reverses respiratory depression and analgesia

49
Q

Naloxone DOA, onset?

A 
Short DOA (less than most opioids)
Onset 1-2 min
50
Q

Naloxone side effects?

A

Tachycardia, HTN, vent dysrhythmias
Severe pain
Pulmonary edema (due to catecholamine release)

N524 Summer Pharm (8 decks)

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