OPIOID | Basic Flashcards

1
Q

How long does it take for a fentanyl patch to reach maximum plasma concentration?

A

30 hours

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2
Q

Receptors responsible for RESPIRATORY DEPRESSION

A

mu-2 receptors

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3
Q

O2 dissociation curve in Opioid Administration:

A

curve shift to THE RIGHT

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4
Q

The RESPIRATORY DEPRESSION induced by OPIOID is caused by:

A

INCREASING the CO2 apneic threshold in the MEDULLA

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5
Q

TRUE or FALSE

The context-sensitive halftime for REMIFENTANIL is independent of the duration of infusion.

The context-sensitive halftime of REMIFENTANIL is 4 MINUTES

A

TRUE

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6
Q

One of the clinical effect of Opioid is EPILEPTOGENIC due to Leu-enkephalin and B-endorphin agonism. What receptor is involved in this process?

A

delta receptors

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7
Q

Mu 1 receptors associated side effect?

A

EUPHORIA
Urinary Retention

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8
Q

Mu 2 receptors associated side effects?

A

Hypoventilation
Constipation
Physical Dependence

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9
Q

Kappa receptors associated side effects

A

Dysphoria
Hallucinations

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10
Q

Opioid effect that do not show tolerance

A

MIOSIS

CONSTIPATION

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11
Q

Remifentanil metabolism in infants is faster compared with that of Adults

A

TRUE

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12
Q

Equianalgesic of IV Morphine to PO

A

10mg IV = 30mg PO

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13
Q

Which narcotic has a local anesthetic activity?

A

MEPERIDINE

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14
Q

Narcotic effects that are not REVERSED by NALOXONE

A

Nausea/Vomiting
Constipation
MUSCLE RIGIDITY

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15
Q

PAIN receptor sites in the brain

A

AMYGDALA
PERI-AQUEDUCTAL GRAY
SOMATOSENSORY CORTEX (Locus Ceruleus & Rostral Ventral Medulla)

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16
Q

Dull “Burning” Pain

A

UNmyelinated C Fibers

17
Q

Sharp “Pin prick” Pain

A

MYelinated Au FIBERS

18
Q

Depression of Ventilation is due to what receptor involvement?

A

Mu-2
This is due to the BRAINSTEM involvement at the Mu-2 receptors

19
Q

True of HYDROMORPHONE except:

A. The active metabolite hydromorphone-3-glucuronide has no analgesic properties but may cause neuroexcitation.

B. Peak effect is 15 mins

C. Equianalgesic of IV to PO is 1.5mg to 7.5mg

D. Used as a post-operative pain management due to its very short duration

A

D. Used as a post-operative pain management due to its very short duration

It has a long duration.

20
Q

PURE OPIOID ANTAGNONISTS

A

Naloxone
Naltrexone
Nalmefene

These are ALL pure Mu opioid receptor antagonists with no agonist activity!

Stoelting | 5th Edit

21
Q

True of NALOXONE except:

A. Is a nonselective antagonist at all three opioid receptors
B. Facilitate treatment of deliberate opioid overdose, and detect suspected physical dependence
C. Duration of action of naloxone (30 to 45 minutes) is presumed to be due to its rapid removal from the brain
D. Naloxone cannot easily cross the placenta
E. Administration of naloxone to an opioid-dependent parturient may produce acute withdrawal in the neonate

A

D. Naloxone cannot easily cross the placenta

22
Q

Receives inputs from Ag and C primary afferent fibers

A

LAMINA - I

23
Q

receives input primarily from LARGE diameters AB fibers from skin

A

Lamina IV - V
45

24
Q

AGONIST-ANTAGONIST Opioid

A

Pentazocine
Bremazocine
Dezocine
Maptazinol

Butorphanol
Buprenorphine
Nalorphine
NALBUPHINE

25
Q

OPIOID Full ANTAGONIST

A

Naloxone
Naltrexone
Nalmefene

26
Q

In the brain, opioid receptors are primarily found in:

A

Periaqeuductal gray
Locus Ceruleus
Rostral ventral medulla

27
Q

The effect-site equilibration time(its time to PEAK analgesia) of fentanyl is:

A. 6.8 minutes

B. 3.5 minutes

C. 2.5 minutes

D. 5 minutes

A

The onset of CNS effects of Sulfentanil(effect-site equilibration time of 6.2 minutes is similar to that of 6.8 minutes for fentanyl)

28
Q

Which of the following opioids has the longest context-sensitive halftime?

A. Fentanyl

B. Remifentanil

C. Sulfentanil

D. Alfentanil

A

Fentanyl

FROM LONGEST TO SHORTEST

F>A>S>R

Fentanyl > Alfentanil > Sulfentanil > Remifentanil

29
Q

The effect-site equilibration time(its time to PEAK analgesia) of Alfentanil is:

A. 10 minutes

B. 2.5 minutes

C. 1.4 minutes

D. 5 minutes

A

C. 1.4 minutes

A unique advantage of alfentanil compared
with fentanyl and sufentanil is the more rapid onset of action (rapid effectsite equilibration) after the IV administration of alfentanil.

For example, the effect-site equilibration time for alfentanil is 1.4 minutes compared with 6.8
and 6.2 minutes for fentanyl and sufentanil, respectively.

30
Q

Activation of opioid receptors leads to activation of
which intracellular transduction mechanism?

(A) G proteins
(B) adenylate cyclase
(C) voltage gated calcium channels
(D) voltage gated sodium channels
(E) outward recti ying potassium channels

A

(A) G proteins

G proteins (Gi and/or Go) are activated, as are inward rectifying potassium channels. Adenylate cyclase and voltage-gated calcium channels are inhibited by activation of the opioid receptor.

Voltage-gated sodium channels ARE NOT involved in opioid receptor-activated intracellular transduction mechanisms.

31
Q

Which of the following opioids is the most hydrophilic?

(A) morphine
(B) fentanyl
(C) codeine
(D) methadone
(E) heroin

A

(A) morphine

Morphine has a relatively low lipid solubility.

Fentanyl, codeine, methadone, and heroin are all more lipophilic than morphine.

32
Q

An adult is administered a single dose o entanyl
(100 micrograms intravenously). The clinical effects
of fentanyl are terminated mainly by:

(A) redistribution
(B) hydroxylation
(C) N-dealkylation
(D) conjugation
(E) demethylation

A

(A) redistribution

After a small bolus of fentanyl the plasma and CSF
levels of fentanyl rapidly diminish due to redistribution to muscle and at. Fentanyl undergoes N-dealkylation and hydroxylation in the liver.

33
Q

Which opioid has the longest duration of action
after epidural injection?

(A) alfentanil
(B) fentanyl
(C) hydromorphone
(D) methadone
(E) morphine

A

(E) morphine

Morphine is relatively hydrophilic compared to the
other listed opioids.

This means morphine will remain in the CSF or a longer period of time—up to 24 hours after a single bolus.