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Pharmacology 680 > Opioids > Flashcards

Opioids Flashcards

1
Q

drugs which are naturally derived
for opium (extract from the poppy plant);
also refers to synthetically produced drugs
which have opium- or morphine-like
properties

A

opioids

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2
Q

derived from the Greek word
meaning stupor; used interchangeably with
opioid; has negative legal connotation

A

narcotics

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3
Q

4 favorable opioid properties

A
  1. Analgesia
    2.Preservation of blood flow autoregulation
    (CNS, heart, kidneys)
  2. Minimal cardiac depression with
    maintenance of hemodynamics
    4.Blunting of autonomic responses to
    sympathetic stimulation (laryngoscopy,
    surgical stress)
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4
Q

MOA of opioids

A

Opioid agonists bind to opioid receptors at
presynaptic and postsynaptic sites in the
CNS (brainstem and spinal cord) and
peripheral sites (primary afferent neurons).
▪ Opioids act like the endogenous peptides
that normally activate these receptors:
enkephalins, endorphins, and dynorphins

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5
Q

what is the principal effect of opioid receptor activation?

A

decrease in neurotransmission

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6
Q

activation of opioid receptor causes these 2 things:

A

– Closure of voltage-gated Ca2+ channels on presynaptic
nerve terminals to cause a reduction of the release of
neurotransmitters (glutamate, acetylcholine, dopamine,
norepinephrine, serotonin, and substance P)
– Opening K+ channels to hyperpolarize the cell, thus
causing inhibition of the postsynaptic neurons

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7
Q

occurs through activation of opioid receptors in the
medulla, midbrain, and other areas, which causes inhibition of neurons
involved in pain pathways

A

supraspinal analgesia

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8
Q

occurs by activation of presynaptic ORs, which leads to
decreased calcium influx and decreased release of neurotransmitters involved
in nociception (sensory nervous system’s process of handling noxious stimuli)

A

spinal analgesia

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9
Q

explain the steps of the GPCR with opioids

A

– inhibit the activity of adenylate cyclase inside of cells. This results in a
decrease in intracellular cAMP, which decreases conductance of the voltagegated calcium channels (decreased neurotransmitters) and opens potassium
channels (hyperpolarization), resulting in decreased neuronal activity.

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10
Q

opioid analgesic effect 1

A

) directly inhibit the ascending transmission
of nociception information from the spinal
cord dorsal horn

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11
Q

opioid analgesic effect 2

A

activate pain control pathways that
descend from the midbrain, via the rostral
ventromedial medulla to the spinal cord
dorsal horn.

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12
Q 
noxious stimuli (chemical, thermal,
mechanical energy) is converted to an electrical
impulse in sensory nerve endings
A

transduction

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13
Q

– conduction of electrical impulses
(action potential propagation) to the CNS – major
connections for these nerves in dorsal horn of the
spinal cord and thalamus with projections to the
cingulate, insular and somatosensory cortexes
(signal transmitted along myelinated A-delta fibers
and unmyelinated C fibers)

A

transmission

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14
Q

altering pain
transmission – both inhibitory and excitatory
mechanism modulates pain impulse
transmission in peripheral and CNS

A

modulation of pain

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15
Q

occurs at the thalamus
with the cortex important for discrimination
of specific sensory experiences

A

pain perception

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16
Q 
▪ Effect:
– Analgesia (spinal and supraspinal)
– Euphoria
– Miosis
– Bradycardia
– Hypothermia
– Urinary retention
A

MU1 receptor

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17
Q 
Effect:
– Analgesia (spinal)
– Respiratory depression
– Physical dependence
– Constipation (marked)
A

effects at MU2 receptor

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18
Q

what agonists affect mu1 and mu2

A

Endorphins, morphine, synthetic

opioids

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19
Q 
Effects:
– Analgesia (spinal, supraspinal) 
– Sedation
– Dysphoria
– Miosis
– Diuresis
– Respiratory depression
A

effects kappa receptor

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20
Q

what are the agonists of kappa receptors:

A

dynorphins, agonist-antagonists

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21
Q 
▪ Effect:
– Analgesia (spinal, supraspinal)
– Respiratory depression
– Physical dependence
– Urinary retention
– Constipation (mild)
A

effects at delta receptor

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22
Q

what is agonist for delta receptor?

A

enkaphalins

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23
Q

which receptors are present in high concentrations in the dorsal horn of the spinal cord

A

mu, kappa, delta

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24
Q

what 3 areas are receptors found supraspinal

A

▪ Rostral ventral medulla
▪ Locus ceruleus
▪ Midbrain periaqueductal gray area

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25
Q

the dose of a drug required to produce death in 50% of patients receiving the drug. Higher the number, safer it is to administer

A

LD50

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26
Q

what does the decrease in sympathetic tone and stimulation cause cardiovascular wise with opioid admin?

A
  • Venous dilation, pooling
    – Decreased venous return
    – Decreased cardiac output and BP
    – Orthostatic hypotension
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27
Q

what two opioids cause a relax in aortic smooth muscle

A

sufentanil and alfentanil

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28
Q

what causes the decrease in HR with opioids?

A

– due to stimulation of the vagal nucleus in the medulla
– SA node depression, slowed conduction through AV
node
– Opioid-induced bradycardia is responsive to atropine.

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29
Q

what opioid has muscarinic affect and causes tachycardia?

A

meperidine

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30
Q

you will see a synergistic decrease in BP when opioids combined with:

A

benzos (SVR) and nitrous (CO)

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31
Q

what two opioids are cardio protective

A

remifentanil and morphine

32
Q

what receptor causes respiratory depression?

A

mu2

33
Q

a decrease in responsiveness to PaCO2 causes

A

a right shift in the co2 curve which means a higher co2 is needed to stimulate breath

34
Q

what medication can reverse respiratory depression without reversing analgesia?

A

physostigmine (using this because of decrease ACh release)

35
Q

what type of patients do not tolerate a increase in paCO2 i.e: careful when giving opioids

A

– Patients with increased intracranial pressure

– Asthma, COPD, or cor pulmonale

36
Q

what is cause of death of opioids

A

respiratory depression (mu2)

37
Q

Mobilization of opioid from skeletal muscle following

rewarming, increased blood flow, and movement

A

re-narcotization (redistribution)

38
Q

respirations are tied to …. during procedures

A

stimulation

39
Q

what type of pain are opioids most effective with

A

visceral continuous dull pain

40
Q

Can opioids be used as an anesthetic

A

NO THEY DO NOT CAUSE AMNESIA

41
Q

when hypercarbia is avoided, opioids cause:

A

cerebral vasoconstriction,
a decrease in cerebral blood flow, and a decrease
in ICP

42
Q

do opioids increase or decrease cerebral o2 consumption

A

decrease

43
Q

what four reasons should you be careful when administering opioids to head trauma patients

A

– Sedative effects make neuro checks difficult
– Pupillary effects – miosis
– Hypoventilation effects – increased PaCO2 causes
vasodilation, increased ICP
– Increased sensitivity to opioids if blood-brain barrier is not intact

44
Q

how do opioids cause miosis

A

excitatory action on the autonomic nervous

system.

45
Q

an intensification of tone of large
muscles of the thorax and abdomen, “Stiff Chest
Syndrome, reduces compliance to ventilate

A

Trunchal rigidity

46
Q

what is trunchal rigidity associated with

A

rapid administration of large doses of highly lipidsoluble opioids (fentanyl, sufentanil, alfentanil, remifentanil)

47
Q

moa of trunchal rigidity

A

inhibited release of GABA in the muscles and increased dopamine production

48
Q

how is trunchal rigidity prevented and treated

A

– Prevented with slow administration, avoidance of nitrous oxide
during induction
– Relieved with antagonist (Narcan) or relaxed with neuromuscular blockers

49
Q

what medication causes closure of vocal cords

A

sufentanil (crap opioid to use for induction)

50
Q

N/V is caused by

A

direct stimulation of the chemoreceptor trigger zone
floor of the fourth ventricle

reflect the effect of increased gastric secretions and
delayed emptying

51
Q

what opioid depresses vomiting center in medulla

A

morphine

52
Q

types of patients more at risk for n/v

A

ambulatory patients (especially young female gyn)
epidural
pca

53
Q

what do you give if you want to diagnose biliary spasm (sphincter of oddi) vs angina pectoris

A

glucagon (1) , narcan, nitro

54
Q

can opioids cross placenta

A

yes, be careful in use during delivery. safe for non-delivery procedures

55
Q

Histamine release, urticaria, or a local

reaction more common with

A

morphine and meperidine

56
Q

Reflex cough often seen with

A

administration of fentanyl-type on induction -

57
Q

▪ No tolerance to these two effects

A

miosis

constipation

58
Q 
Opioid receptor desensitization*
– Down-regulation of receptors
– Up-regulation of the cAMP system
– NOT due to enzyme induction (increase in the
rate of metabolism of opioids occurs.)
– Activation of NMDA receptors and
downregulation of spinal glutamate transporters
(treatment with small doses of NMDA
antagonist, ketamine, to treat
A

theories of what causes opioid tolerance

59
Q

4 withdrawal symptoms of opioids listed

A

– Yawning
– Diaphoresis
– Lacrimation
– Coryza – severe nasal congestion

60
Q

what med is effective in hiding withdrawal signs

A

clonidine

61
Q

effect opioids have on Hypothalamic-pituitary-adrenal axis

A

decreased plasma cortisol levels

62
Q

Hypothalamic-pituitary-gonadal axis affects what 5 hormones

A

prolactin (increases)
decreases
-estrogen, d luteinizing hormone, follicle stimulating
hormone, testosterone

63
Q

how does opioid exposure affect immune system

A

Alter the development, differentiation, and
function of bone marrow progenitor cells,
macrophages, T cells

64
Q

triad of opioid overdose

A

miosis, hypoventilation, coma

65
Q

overdose symptoms

A

Respiratory depression – principal symptom
▪ Pupils symmetric and constricted (if hypoxemia,
mydriasis)
▪ Muscles flaccid
▪ Likely airway obstruction

66
Q

how to treat overdose

A

mechanical ventilation with O2
administration of opioid antagonist (naloxone,
Narcan), which may cause acute withdrawals

67
Q

what organ plays significant role in first pass uptake

A

lungs

68
Q

how much sufentanil is found in lungs immediately after injections

A

50%

69
Q

Amount of uptake by the lungs is influenced by

A

▪ Prior accumulation of another drug (decreases)
▪ Smokers (increases)
▪ Inhalation anesthetic administration (decreases)

70
Q

the effect of small doses of opioids is terminated by

A

redistribution

71
Q

large doses of opioids are terminated by

A

metabolism

72
Q

Most opioids are chiefly metabolized by the

A

liver (except for remifentanil)

73
Q

what are the two metabolites of morphine?

A

morphine 3-glucuronide and

morphine 6-glucuronide

74
Q

how are opioids excreted

A

kidneys!! different than metabolization

75
Q

metabolite of meperidine

A

normeperidine (causes seizures)

76
Q

When used in conjunction with propofol for
TIVA (total intravenous anesthesia),
clinically useful doses of propofol inhibit the
degradation of alfentanil and sufentanil by

A

50-60% and up to 90% with higher propofol

doses.

Pharmacology 680 (19 decks)

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