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Pharm > Opioid Agonist/Antagonist > Flashcards

Opioid Agonist/Antagonist Flashcards

1
Q

What is the name of the fibers that send a fast signal of sharp, well localized pain?

A

A delta fibers

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2
Q

What is the name of the fibers that send a slow signal of dull, poorly localized pain?

A

C fibers

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3
Q

A pain signal travels up 3 neurons to make the ______ tract

A

spinothalmic

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4
Q

The first order neuron is from the ____ to the _____.

A

Periphery to the dorsal horn.

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5
Q

The second order neuron is from the ____ to the _____.

A

dorsal horn to the thalamus

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6
Q

The third order neuron is from the ____ to the _____.

A

thalamus to the cerebral cortex

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7
Q

What is transduction?

A

The tissue is injured and chemicals are released that causes activation of peripheral nerves and immune cells. The chemicals are transduced into an action potential by nerves and then interpreted by the brain

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8
Q

What is transmission?

A

The signal from transduction is the electrically relayed up the spinothalmic tract to the brain

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9
Q

What is modulation?

A

The inhibition of signals down the decending pathyway from the release of GABA and glycine in the brain/spinal cord and norepinephrine, 5-HT (serotonin), and endorphins. Regulates the amount of pain we feel.

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10
Q

What is the most important site for pain modulation?

A

substantia gelatinosa

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11
Q

What is perception?

A

The processing of the signals in the cerebral cortex and limbic system. Subjective to each person. Can be influenced by many factors.

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12
Q

What are the 3 types of opioid analgesic chemical classes?

A

Phenanthrenes, phenylpiperidines, phenylhepatones

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13
Q

What are 3 meds that are phenanthrenes (an opium class)

A

Morphine, Codeine, Thebaine

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14
Q

What are 2 meds that are benzylisoquinolines? (an opium class that lacks opioid activity?

A

papavarine, noscapine

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15
Q

What is the name of the class of synthetic opioids?

A

Phenylpiperidine derivatives

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16
Q

What medications are phenylpiperidine derivatives? (5)

A 
meperidine
fentanyl
sufentanil
alfentanil
remifentanil
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17
Q

What are 3 types of endogenous substances that act as natural pain killers?

A

Endorphins
Enkephlins
Dynorphins

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18
Q

What substances are released in response to tissue injury?

A

COX-2 and prostaglandins

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19
Q

Which ion decreases after an opioid binds to a receptor? Which one increases?

A

Ca++ movement inward decreases, K+ outward movement increases

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20
Q

What effect does the movement of potassium have to an opioid receptor

A

It hyperpolarizes the post-synaptic neuron, the trigger potential moves further away from the resting membrane potential, makes it more resistant to stimulation.

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21
Q

What are the 3 types of opioid receptors?

A

Mu, delta, kappa

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22
Q

What are the side effects of activating the Mu receptors?

A

euphoria, miosis, hypothermia, bradycardia, urinary retention, pruritis, hypoventilation, physical dependence, constipation

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23
Q

What are the cardiovascular side effects of opioids?

A

Minimal effect in healthy patients, bradycardia, dose dependent vasodilation
Morphine and Demerol-histamine release

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24
Q

What are the ventilation effects of opioids?

A

decreased rate, prolonged inspiration and delayed expiration, increased CO2, decreased response to rising CO2, decreased minute ventilation

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25
Q

What are the symptoms of Serotonin Syndrome?

A

Sweating, tachycardia, agitation, hypertension, clonus, diarrhea, tremor, hyperrflexia

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26
Q

What is hyperalgesia?

A

a decrease in pain threshold in an area of inflammation. Low stimuli causes pain.

27
Q

Place in order from most to least potency:

Alfentanil
Remifentanil
Sufentanil
Fentanyl
Hydromorphone
Demerol
Morphine
A

Sufentanil>Fentany=Remifentanyl>Alfentanil>Hydromorphone>Morphine>Meperidine

28
Q

What is a critical side effect of Morphine?

A

Histamine release

29
Q

What is the active metabolite of Morphine?

A

moprhine-6 glucuronide

30
Q

Elimination of morphine may be impaired in patients with _____. This can cause an accumulation of active metabolites and cause _______.

A

Renal disease, respiratory depression

31
Q

Which opioid is least potent?

A

Demerol

32
Q

What is Demerol used for in the PACU?

A

Post-op shivering

33
Q

Is Demerol mostly ionized or unionized?

A

Ionized (93%)

34
Q

Demerol and MAOI’s or SSRI’s can cause _____.

A

Serotonin Syndrome

35
Q

What are some side effects of Demerol?

A

Tachycardia, decreased contractility, orthostatic hypotension, histamine release, delirium and seizures with prolonged use

36
Q

Demerol is 90% metabolized by the _____ enzyme

A

CYP450

37
Q

The active metabolite of Demerol is_____.

A

Normeperidine

38
Q 
Fentanyl:
Onset:
DOA:
Half-life
Ionized or nonionized?
A

Onset: 2-5 min
DOA: 30min-1hr
Half-life: 2-4 hrs
Highly Ionized

39
Q

What are side effects of Fentanyl?

A

Respiratory depression, bradycardia, decreased SVR, muscle rigidity

40
Q

Sufentanyl:
Onset:
DOA:
Half-life:

A

Onset: 1-3 min
DOA: dose dependent
Half-life: 6hrs

41
Q

What are some side effects of Sufentanyl?

A

Significant bradycardia-can cause decreased cardiac output and then decreased blood pressure

42
Q

What are two benefits of Sufentanyl?

A

Decreased cerebral metabolic O2 demand, longer period of analgesia with less respiratory depression

43
Q

Alfentanil:
Onset:
DOA:
Half-life:

A

Onset: Immediate
DOA: brief, rapid redistribution
Half-life: 1.5hrs

44
Q

What are side effects of Alfentanil?

A

Bradycardia and hypotension

45
Q

What makes Alfentanil work so quickly?

A

The pka is a base (6.4) It is non-ionized, then when added to the circulation, you get more non-ionized portion of the drug.

46
Q

How is Alfentanil metabolized?

A

CYP450

47
Q

Remifentanil:
Onset:
DOA:
Half-life:

A

Onset: 1 min
DOA: 5-10 min
Half-life: not listed

48
Q

How is Remifentanil broken down?

A

hydrolysis by plasma esterases

49
Q

What are side effects of Remifentanil?

A

Muscle rigidity, hypotension, hyperalgesia

50
Q

What does Remifentanil do to the MAC and propofol needs?

A

Reduces it by 50%

51
Q

How do you calculate a dose of Remifentanil for an obese person?

A

use ideal body weight plus 25%

52
Q

How much should you reduce a Remifentanil dose by for the elderly?

A

50-70% reduction

53
Q

Hydromorphone (Dilaudid)
Onset:
DOA:
Half-life:

A

Onset: 15-30min
DOA: 4-5hr
Half-life: 1-3hr

54
Q

Oxymorphone is a result of an addition of a ______ group to hydromorphone

A

Hydroxyl

55
Q

About _____% of Codeine is metabolized or changed to _____ in the liver.

A

10%, morphine

56
Q

What is a side effect of Codeine?

A

constipation

57
Q

What is a use for Methadone?

A

Suppression of withdrawal symptoms in a physically dependent person

58
Q

Methadone is a ____ receptor AGONIST and a _____ receptor ANTAGONIST

A

Mu, NMDA

59
Q

Methadone can increase the ____ interval.

A

QT

60
Q

What does Nubain do?

A

Reverses respiratory depression from Fentanyl but maintains analgesia

61
Q

What are 3 opioid agonist/antagonists?

A

Nalbuphine (Nubain), Butorphanol (Stadol), Buprenorphine (Tawin)

62
Q

What do opioid antagonists do?

A

Take away all analgesia on board

63
Q

What are 2 opioid antagonists?

A

Naloxone and Naltrexone

Pharm (12 decks)

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