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SRNAPharmacology II > OPIOIDS and NonOP EXAM REVIEW > Flashcards

OPIOIDS and NonOP EXAM REVIEW Flashcards

1
Q

What are some of the causes of Nausea and vomiting associated the use of opioids?
DPG

A
  1. Opioid induced N/V are caused by direct stimulation of the chemoreceptor trigger zone in the floor of the fourth ventricle
  2. Opioids may act as a partial dopamine agonist at
    the chemoreceptor trigger zone
  3. Morphine may also cause N/V by ↑ GI secretions
    and delaying passage of intestinal contents
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2
Q

Which opioid agonist is contraindicated in a patient taking a MAOI?

A

Meperidine

MAOI( phenelzine, Selegine)

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3
Q

How do opioid agonist affect bile duct pressure? Which agents have the greatest/least effect?

A 
• Equal analgesic doses of opioids ↑ bile duct pressure
above pre drug levels 
Greatest effect --> FENTANYL
Intermediate ---> MORPHINE
Least ---> MEPERIDINE
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4
Q

What is the drug of choice to reverse biliary spasms in a patient taking chronic narcotics?

A

Glucagon (2mg IV) may reverse opioid induced biliary

smooth muscle spasm

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5
Q

How are opioid receptors classified? What endogenous neurotransmitter affects each receptor?

A 
OPIOD receptors  (3) 
Mu , Delta, Kappa (ALL G-COUPLED ) antagonize adenylate cyclase, decrease CAMP

Opioid receptors on primary afferent neurons are
activated by 3 endogenous peptide opioid receptor ligands
Endorphins:
Mu 1–> endomorphins and B-endorphins (also morphine itself and synthetic opiods
Mu 2 –> endomorphins and B-endorphins (also morphine itself and synthetic opiods

Enkephalins –> DELTA
Dynorphins –> KAPPA

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6
Q

What endogenous neurotransmitter affect Mu receptors? Think mEN!

A

ENDORPHINS

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7
Q

What endogenous neurotransmitter affect KAPPA receptors? (KevinDurant KD)

A

DYNORPHINS

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8
Q

What endogenous neurotransmitter affect DELTA receptors? DELTA –think DeK

A

ENKEPHALIN

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9
Q

What narcotic is associated with first past lung effect? What concern is this to the clinician?

A

75% of initial fentanyl dose undergoes first pass
pulmonary uptake
Limits the initial amount of drug that reaches the systemic circulation

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10
Q

What is expected with the use of IV induction doses of morphine?

A

DROP in BP and SVR (histamine release)
Exaggerated HYPOTENSION on induction
May prevent drop by giving H1/H2 antagonist.
• Opioids given prior to induction may slow heart rate during exposure to VA with/without surgical stimuli

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11
Q

What is the reversal agent for benzodiazepines?

which part?

A

FLUMANEZIL
Flumenazil only REVERSES the BENZODIAZEPINES COMPONENT OF VENTILATORY DEPRESSION
Does not work for OPIOD ventilatory depression

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12
Q

What is the reversal agent opioid agonist

A

NARCAN

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13
Q

What is the reversal agent for anticholinergics (look it up)?

A

Physostigmine

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14
Q

What opioid agonist has the greatest context sensitive half life?

A

FENTANYL 260 min

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15
Q

Potency of Meperidine

A

1/10th as potent as morphine

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16
Q

Potency of Fentanyl

A

100 times more potent than morphine

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17
Q

Potency of SUFENTANYL

A

• 5-10 times more potent than fentanyl

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18
Q

Hydromorphone potency

A

8 times more potent then morphine

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19
Q

Tramadol Potency

A

5-10 times less potent analgesic than morphine

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20
Q

Alfentanyl Potency

A

1/5-1/10 less potent than fentanyl

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21
Q

Effect equilibration time of each opioid agonist?

Which one is fastest

A 
FSAR (6.8,6.2,1.4,1.2)
Fentanyl (6.8)
Sufentanyl (6.2)
Alfentanyl (1.4)
Remifentanyl (1.1)  FASTESt
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22
Q

Which opioid agonist can cause bradycardia? MFAS

A

Morphine
FENTANYL
Alfentanyl
Sufentanyl

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23
Q

Which opioid agonist can cause Tachycardia?

A

MEPERIDINE

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24
Q

What receptor is responsible behind the anti-shivering effects of opioid agonist?

A 
KAPPA RECEPTORS (10% of drugs activity) 
  (Dynorphins goes there FYI)
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25
Q

What area of the spinal cord has the greatest concentration of Mu receptors?

A

substantia gelatinosa (dorsal horn)

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26
Q

Morphine Metabolism

A

LIVER: Principle pathway is conjugation with glucuronic acid in hepatic and extra hepatic sites, MAINLY by the KIDNEYS (renal has significant metabolism)
Principle metabolites
Morphine -3-glucuronide (75-80%)Pharmacologically
inactive

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27
Q

Morphine Metabolite (POTENT)

A

Morphine-6-glucuronide (5-10%)-pharmacologically active more potent and longer duration of action than morphine

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28
Q

MEPERIDINE METABOLISM

A

LIVER:Hepatic metabolism is extensive, 90% metabolized to NORMEPERIDINE (demethylation) and meperidinic acid (hydrolysis)
Better excretion with acidic urine
Decrease renal function, may LEAD TO ACCUMULATION Of Meperidine and metabolites MAY INCREASE RISK OF SEIZURES

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29
Q

FENTANYL METABOLISM

Is metabolites pharmacologically active?

A

LIVER• Metabolized by N-demethylation, producing NORFENTANYL, which is structurally related to normeperidine
• Norfentanyl is excreted in the urine and
detectable for 72 hours after a single IV dose

–>NO

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30
Q

REMIFENTANYL- METABOLISM
Only opiod____________
Not affected by

A

UNIQUE metabolism
–> Only opioid NOT METABOLIZED IN THE LIVER
—> RENAL FAILURE
Ester linkage makes drug susceptible to hydrolysis by nonspecific plasma and tissue esterase’s
UNIQUE METABOLISM results in
1. Brevity of action
2. Rapid onset and short duration of action = precise and titratable effect
3. Non-cumulative effects
4. Rapid recovery after discontinuation of infusion

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31
Q

What are the different chemical groups for the opioid agonist?

A

SEMISYNTHETIC – From modified Morphine molecule: Codeine, Heroin, Hydromorphone, Oxycodone
CHHO

SYNTHETIC OPIOIDS -Contain nucleus of morphine but are manufactured by synthesis - rather than
modified morphine molecule: Fentanyl, Sufentanil, Alfentanil, Remifentanil, Methadone, Meperidine,
Tramadol

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32
Q

What are the different water solubilities of each opioid agonist?
water soluble is MMRCHT
Lipid solule is FAS

A

Morphine, Meperidine, Remifentanyl, Codeine, Hydrocodone, Tramadol, (WATER SOLUBLE)

Fentanyl, Alfentanyl, Sufentanyl (LIPID SOLUBLE)

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33
Q

Match each opioid agonist with the most likely receptor?

A

Mu 1, Mu2 agonist –>Endorphins, Morphine, Synthetic opioids

Meperidine- Demerol – Synthetic opioid agonist at mu & kappa opioid receptors
Morphine, Fentanyl – Mu receptors (1 and 2)
Sufentanil –active at Mu, also binds at delta and kappa
Remifentanil – selective Mu agonist
Tramadol - Centrally acting analgesic with a moderate affinity for mu receptor, weak kappa &
delta opioid receptor affinity

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34
Q

What are risk of naloxone administration?

What decreases risk of N/V?

A

–>N/V appear to be related to rate and dose given
Fortunately vomiting occurs simultaneously with
awakening which allows for pt to protect their
airway
–>Administration over 2-3 minutes

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35
Q

What is the time to peak for morphine IV/IM

A

• IV-15-30 minutes – rapid onset
• IM 45-90 minutes for peak effect
Remifentanil IV = 1.1 min (fastest onset)
Alfentanil: IV = 1.4 min, rapid onset
Sufentanil: IV = 6.2 min
Fentanyl: IV = 6.4-6.8 min (Stoelting says 6.8 min)

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36
Q

Analgesia, euphoria, respiratory depression associated with morphine are probably mediated mainly through this opioid receptor type:

A

Mu receptor

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37
Q

Tolerance develops to analgesia, euphoric, sedative,
depression of ventilation and emetic effects but not to
effects on

A

Miosis and constipation

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38
Q

What are common side effects of neuraxial narcotics?

A
  • Pruritus (MOST COMMON face, neck upper thorax) Cephalad migration into CSF)
  • Nausea/vomiting
  • Urinary retention (most common in young males)
  • Depression of ventilation
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39
Q 
What is a metabolite of meperidine?
Half time?
what about patient with renal failure?
Potency?
What does it cause?
A

NORMEPERIDINE
• Elimination Half time of 15 hours
• Pt with renal failure half life may be >35 hours (can be detect in urine for 3 days)
Normeperidine is ½ as potent as meperidine as an
analgesic
Normeperidine causes CNS stimulation- toxicity manifests
as myoclonus and seizures- most likely during prolonged
meperidine administration as during PCA, especially with
renal function

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40
Q

What is a disadvantage of high dose fentanyl? 2 Ps

A

Possible awareness, postop ventilation depression

41
Q

What are expected cardiovascular effects of morphine?,

BBOH

A
  1. ↓ BP can occur due to morphine induced bradycardia or
    histamine release
  2. Bradycardia due to ↑ activity over vagal nerves, stimulation of vagal nuclei in the medulla, also depressant effect on SA node and slowed conduction through AV node
  3. Opioids given prior to induction may slow heart rate during exposure to VA with/without surgical stimuli
  4. Histamine release and hypotension can be minimized by limiting the rate of administration to 5mg/minute IV,
    maintain pt supine and well hydrate
42
Q

What are expected cardiovascular effects of meperidine?

ROHM?

A

-Rarely causes bradycardia, may ↑ HR- good for pt
with bradycardia
- Orthostatic hypotension
- Hypotension more frequent and more profound
than with morphine
- More ventilatory depression than morphine

43
Q

What are expected cardiovascular effects of Fentanyl? (NCCB)

A

1.No histamine release-no dilation of venous vessels to
cause hypotension
2. Carotid sinus baroreceptor reflex control of heart rate is
depressed by fentanyl
3. Chest wall rigidity
4. BRADYCARDIA more prominent than with morphine

44
Q

What are expected cardiovascular effects of Alfentanyl?

A

Bradycardia

45
Q

What are expected cardiovascular effects of Sufentanyl?

A

Chest wall rigidity, Bradycardia

46
Q

Extra Morphine does not sensitize the heart to catecholamines or predispose to dysrhythmias as long as

A

hypercarbia or arterial hypoxemia doesn’t result from ventilatory depression

47
Q

***Extra Morphine does not sensitize the heart to catecholamines or predispose to dysrhythmias as long as

A

hypercarbia or arterial hypoxemia doesn’t result from ventilatory depression

48
Q

***EXTRA Rapid IV administration of opioids can cause
• Risk greatest with
Sufentanil may cause

A

skeletal muscle rigidity, especially the abdomen and thoracic area- leading to difficult ventilation
Fentanyl than remifentanil, than morphine
laryngospasm & ⇧ difficulty to ventilate

49
Q

EXTRA Very short-acting;

A

REMIFENTANYL

50
Q

eXtRA Principal alkaloid in opium (derived from opium poppy)

A

MORPHINE

51
Q

What are signs symptoms of narcotic overdose

(MHC) ?

A

Triad of
Miosis
Hypoventilation
Coma should suggest NARCOTIC OVERDOSE

52
Q

What are the TWO principal metabolites of MORPHINE? % and which active/inactive?

A

Morphine -3-glucuronide (75-80%)Pharmacologically
INACTIVE
• Morphine-6-glucuronide (5-10%)-pharmacologically ACTIVE more potent and longer duration of action than morphine

53
Q

What are the principal metabolites of MEPERIDINE? active/inactive?

A

NORMEPERIDINE –> Active

54
Q

What are the principal metabolites of FENTANYL? active/inactive?

A

NORFENTANYL –> Minimal pharmacological activity

55
Q

Extra : Mixed agonist-antagonist:

A

NALBUPHINE

BUTORPHANOL

56
Q

EXTRA Elimination of morphine glucuronide may be

impaired in_______ leading to_______

A

renal failure
accumulation of metabolites and unexpected
respiratory depression with small doses

57
Q

EXTRA How does Meperidine reduce SHIVERING

A

Meperidine, through acting on an alpha type 2 adrenergic receptor, appears most effective among opioid agonists in reducing shivering.

58
Q

EXTRA Repeated administration of this/these opioid may lead to seizures and tremor.

A

MEPERIDINE

59
Q

EXTRA Only________ forms of the opioid exhibit

agonist activity

A

levorotary

60
Q

EXTRA: Opiods Agonist MOA

A

Leads to
⇩intracellular cAMP concentration
⇩ Ca+ + ion influx and inhibits the release of excitatory
neurotransmitters (Glutamate, substance P)
DECREASE cAMP (both presynaptic and post synaptic)

61
Q

EXTRA: All 3 classes of receptors

A

• All 3 classes couple to G proteins and subsequently inhibit adenyl cyclase,
⇩ conductance of voltage gated calcium channels or
open potassium channels

62
Q

EXTRA The principal metabolic pathway associated with morphine metabolism is

A

conjugation (phase II metabolism)

63
Q 
Characteristics of Mu-1 receptors (MUHLE) 
Produces \_\_\_\_\_\_\_(\_\_\_\_and \_\_\_\_\_\_)
A 
Mu1 – produces analgesia(Supraspinal & spinal)
• Miosis 
• Urinary retention
• Hypothermia 
• Low abuse potential
• Euphoria
64
Q

Agonists of Mu1 and Mu2 –> MES

A

Morphine
Endorphins
Synthetic opioids

65
Q

Extra Characteristics of Mu-2 receptors (CHAsP)
Responsible for
Where is analgesia?

A 
Mu2 –responsible for
• Constipation- marked
• Hypoventilation
• Analgesia (spinal)
• Physical dependence (addiction)
66
Q

EXtRA Characteristics of Kappa Receptors
______ (__________and ______)
LADS -MD

A
  • Low abuse potential
  • Analgesia (supraspinal & spinal)
  • Dysphoria
  • Sedation
  • Miosis
  • Diuresis
67
Q

Extra: Agonist of KAPPA is______
cause Inhibition of _________Via -________which resuts in ____
less________ but may cause _____And ______
What may be resistant to the analgesic effect of Kappa receptors?

A

Dynorphins- cause inhibition of neurotransmitter release via type N calcium channels which results in analgesia
•Less respiratory depression, but may cause diuresis and dysphoria
• High intensity painful stimulation may be resistant to the analgesic effect of kappa receptors

68
Q

Extra: Where does Opioid agonist-antagonists often act principally ?

A

on kappa receptors

69
Q

EXTRA Delta Receptors (PAVACU)

Analgesia where?

A
  • Physical dependence
  • Analgesia (supraspinal & spinal)
  • Ventilatory depression
  • Antidepressant effects
  • Constipation- minimal
  • Urinary retention
70
Q

EXTRA -Inhibits release of excitatory neurotransmitters

A

Endorphins

71
Q

FY*I Spinal cord ends at

A

L-1

72
Q

Relieve PRURITIS with

A

Can relieve with opioid antagonist

73
Q

EXTRA Risk of ventilatory depression with opiods increase with __________intrathoracic pressure

A

Increased intrathoracic pressure

74
Q

EPIDURAL MORPHINE SHOULD BE

A

PRESERVATIVE FREE

75
Q

Morphine is better for _____than ____pain

A

dull pain; sharp pain

76
Q

X_TRA: MORPHINE Respiratory acidosis(hypoventilation) will decrease the

A

non ionized portion but may lead to
higher CNS concentrations due to ↑ cerebral blood
flow due to the ↑ carbon dioxide levels

77
Q

Morphine vs Fentanyl

Morphine accumulates rapidly in the (3) and unlike fentanyl does

A

kidneys, liver and skeletal muscles

not undergo significant first pass effect into the lungs

78
Q

XTRA important• CV- high doses (_______)to supine
normovolemic patient is UNlikely to cause a_________
• Change from supine to standing may cause
• Caused by impairment of______
• Decrease in vasomotor tone leads to ________ ,_______ and ________

A

(1mg/kg IV)
direct myocardial depression or hypotension
hypotension and syncope
compensatory sympathetic nervous system response
decreased preload,
cardiac output and blood pressure

79
Q

eXTRA • Ventilatory depression can result in the baby as a
result of giving mom opioids- so give ________
• Morphine causes greater neonatal depression in
the neonate then Meperidine
• May be a result of an____________
• Chronic opioid use by the mom may result in__________________

A

give after delivery

immature BBBphysical dependence (intrauterine addiction)

80
Q

• Administration of naloxone may cause life

threatening

A

neonatal abstinence syndrome

81
Q

Initial symptoms of withdrawal include (IRDYL)

•

A 
Insomnia
Restlessness 
Diaphoresis
Yawning
Lacrimation, or coryza
82
Q

Prevention of Withdrawal

A

CLONIDINE

83
Q

Best suited for providing analgesia especially for short surgical procedure and also when rapid recovery is beneficial.

A

REMIFENTANYL

84
Q

OPIODS OD and eyes

A

MIOSIS

Unless hypoxemia –> MYDRIASIS

85
Q

Narcan dose

A

Naloxone 0.4-2mg every 2-3 minutes as needed

86
Q

____ , ____,____,_____are analogues of Meperidine (FARS)

A

Fentanyl
Alfentanil
Remifentanil
Sufentanil

87
Q

• Principally for analgesia during labor and delivery

and after surgery

A

MEPERIDINE

88
Q

Fentanyl

A

Single IV dose-more rapid onset and shorter
duration of action than morphine due to its rapid
redistribution to inactive tissues ( fat, skeletal
muscle)

89
Q

Low dose fentanyl

A

• Low dose 1-2 mcg/kg

90
Q

High dose fentanyl

A

50-150mcg/kg SURGICAL ANESTHESIA

91
Q

Doses of SUFENTANYL

A

0.1-0.4 mcg/kg

92
Q

Metabolism of this opioid is dependent neither on liver metabolism or renal excretion:

A

REMIFENTANYL

93
Q

FASTER ONSET Of activity

A

REMIFENTANYL

94
Q

Inappropriate for POST OP analgesia control

A

REMIFENTANYL

95
Q

REMIFENTANYL Anesthesia induced with_______over 60-90 seconds or with gradual initiation of infusion at________
for about 10 minutes, before a hypnotic prior to tracheal
intubation

A

1mcg/kg IV ;0.5-1.0 mcg/kg IV

96
Q

Meperidine causes

A

Mydriasis and elevated HR

97
Q

What is the reason there is rapid effect site equilibration of ALFENTANYL?

A

due to low pKa90% of drug is non-ionized at physiologic pH

98
Q

Effect equilibration time of Alfentanyl

A

1.4 min

99
Q

Opioid more susceptible to CYP450 function

A

Alfentanyl

SRNAPharmacology II (32 decks)

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