Brainscape's Knowledge GenomeTM

Browse over 1 million classes created by top students, professors, publishers, and experts.


See full index

Mo and Mik > m and m 10 - analges agents > Flashcards

m and m 10 - analges agents Flashcards

1
Q

4 types of opioid receptors are

A

mu
kappa
delta
sigma

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

second messengers associated with opioid receptor activation are (2)

A
  • inhibition of adenylyl cyclase (decrease intracellular AMP)
  • activation of phospholipase C
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

two ion channels affected by opioids are?

A

inhibit voltage gated ion channels

activated inwardly rectifying potassium channels

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

Four examples of opioid agonists / antagonists are?

A

nalbuphine
nalorphine
butorphanol
pentazocine

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

True or false - opioids cause the release of presynaptic neurotransmitters?

A

False, they Inhibit release of these NTs

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

True or false - opioids are also located on the peripheral NS?

A

True, think receptors in the GI tract that cause constipation

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

What are the two isomers possible for opioids and which are more potent?

A

Levorotary and Dextrorotary - levorotary are more potent

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

Maximal effects of IM hydromorphone, morphine and meperidine after how long?

A

20-60 minutes

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

What property(s) of fentanyl favor transdermal absorption?

A

Low molecular weight, hight Lipid solubility

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

Why Is transdermal fentanyl not Instantaneously effective?

A

It takes time for local skin to establish a reservoir that allows for effective serum concentrations

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

Amount of time for steady state after a fentanyl patch? Steady state can persist for how long?

A

SS in 14-24 hrs, persists for up to 72 hours

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

Morphine, meperidine, fentanyl, sufentanyl, alfentanil and remifentanil. Which is least lipid soluble?

A

Morphine

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

Morphine, meperidine, fentanyl, sufentanyl, alfentanil and remifentanil. Which is most lipid soluble? (2)

A

Fentanyl and sufentanil

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

Morphine, meperidine, fentanyl, sufentanyl, alfentanil and remifentanil. Which has the least protein binding?

A

Morphine

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

Morphine, meperidine, fentanyl, sufentanyl, alfentanil and remifentanil. Which has the most protein binding? (2)

A

Sufentanil and alfentanil

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

Morphine, meperidine, fentanyl, sufentanyl, alfentanil and remifentanil. Which has the most non-ionized fraction?

A

Fentanyl and meperidine

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

What properties of fentanyl and alfentanil hasten onset and decrease duration of action?

A

High lipid solubility

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
18
Q

Alfentanil is less lipid soluble than fentanyl, but it has a more rapid onset and shorter duration of action. Why?

A

It has a high non-ionized fraction and lower volume of distribution, therefore more (percentage) of the drug is available for receptor binding

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
19
Q

What major organ system can serve as reservoir for opioids?

A

Lungs

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
20
Q

What characteristics decrease opioid binding in the lungs?

A

Tobacco use

Prior accumulation of other drugs

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
21
Q

What terminates the effects of lipid soluble opioids (fentayl, sufentanil) drugs at lower doses? Higher doses?

A

Lower doses? Redistribution

Higher doses? Biotransformation

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
22
Q

The time required for fentanyl and sufentanil concentrations to decrease by half is context sensitive. Why?

A

Because the half life depends on what amount of drug was administered, varies based on high or low dose

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
23
Q

What is the major site of Metabolism of opioids? What drug is the exception?

A

Liver, by cytochrome C

Exception is remifentanil

24
Q

Opioids have a [high/low] hepatic extraction ratio, therefore their clearance depends on ____.

A

High hepatic extraction ratio, Therefore clearance depends on blood flow to the liver.

25
Q

What are the hepatic metabolic products of morphine (2)and hydromorphone (1)?

A

Morphine 3-glucuronide, Morphine 6 glucuronide and hydromorphone 3-glucuronide

26
Q

What is the biotransformation product of meperidine and what is its significance?

A

Normeperidine, associated with seizures

27
Q

True or false, the metabolic products of fentanyl, alfentanil and sufentanil are active?

A

False, these are inactive

28
Q

What is the significance of norfentanyl?

A

Metabolic product of fentanyl, present in the urine long after fentanyl use, can be used to detect fentanyl abuse (chronic)

29
Q

What do codeine and tramadol have in common re: hepatic metabolism?

A

Both have to be metabolized by CYP enzymes to become active compounds, morphine and O-desmethyltramadol, respectively

30
Q

What makes remifentanil unique re: metabolism? Site?

A

Ester structure makes it suceptible to hydrolysis by non-specific esterases in RBCs and tissues. Half life of less than 10 minutes

31
Q

True or false, a dose adjustment is needed for patients with a pseudocholinesterase deficiency if treatment with remifentanil (or even esmolol) is desired.

A

False. These drugs are metabolized by non-specific plasma esterases, not pseudocholine esterases

32
Q

Significance of renal dysfunction on morphine and meperidine use?

A

Metabolites are excreted in urine. morphine 6 glucuronide is even more potent than morphine, therefore more chance of narcosis if renal failure is present, Accumulation of normeperidine is associated with seizures

33
Q

True or false, seizures from normeperidine can be prevented / reversed with naloxone?

A

False

34
Q

What opioid is unique in being able to cause tachycardia? Why?

A

Meperidine, structurally similar to atropine

35
Q

Opioids [do/don’t] directly depress cardiac contractility?

A

Opioids do not depress contractility

36
Q

Opioids [do/don’t] cause brady cardia?

A

Opioids cause brady cardia by stimulation of the vagus nerve

37
Q

True or false, opioids can cause decreased BP?

A

True, usually from brady cardia, venodilation and depressed sympathetic reflexes

38
Q

What class of drugs, when administered with opioids, are most likely to cause profound drop in BP?

A

Benzos

39
Q

What 3 opioids are associated with histamine release? Significance?

A

Meperidine, morphine and hydromorphone, This can cause significant drop in SVR

40
Q

True or false, large boluses of opioids can cause HTN? What is the reason?

A

True, this is typically attributed to not enough anesthetic depth

41
Q

What are the mechanisms by which opioids depress ventilation?

A

Increase partial pressure of CO2 (PaCO2) and blunt the response to increasing CO2. This increases the apneic threshold (the greatest Paco2 at which pt remains apneic) and decreases hypoxic drive

42
Q

What opioids are associated with bronchospasm? mechanism?

A

Morphine and meperidine. Mechanism is histamine induced bronchospasm

43
Q

Rapids administration of what 4 opioids are associated with chest wall rigidity? How is this treated? centrally or peripherally mediated?

A

Fentanyl, alfent, sufent and reminfent
Treatment is neuromuscular blockers
Centrally mediated

44
Q

What is the overall effect of opioids on intracranial pressure? cerebral perfusion? cerebral oxygen consumption?

A

Decreases all these parameters

45
Q

What is the effect of opioids on EEG?

A

No effect

46
Q

True or False, large doses of remifentanil Intraoperatively can produce acute tolerance?

A

True - will subsequently require larger doses of opioids to achieve the same effect

47
Q

Best opioid for post op shivering is?

A

Meperidine

48
Q

Opioids can cause biliary colic by causing contraction of ____ structure. What is the treatment?

A

Sphincter of oddi

Treatment is naloxone or glucagon

49
Q

Chronic opioid use will result in tolerance to most side effects except? What are 2 drugs used to treat this side effect?

A

Constipation

Methylnaltrexone and almivopan

50
Q

Why avoid NSAIDs in certain types of surgeries?

A

Bleeding risk Is the major issue.

51
Q

Cox-1 and Cox-2, which is constitutive and which is induced?

A

Cox-2 is induced, Cox-1 is constitutive

52
Q

Why is it possible to have cox-2 specific drugs, but generally speaking not cox-1?

A

Cox-2 binding site is larger, can accomodate larger molecules that cannot bind cox-1

53
Q

True or false, acetaminophen acts as a cox-2 blocker?

A

True

54
Q

Most Cox inhibitors are well absorbed orally. What is the exception?

A

Ketorolac

55
Q

True or false, Cox inhibitors are lipid soluble?

A

True, This is how they centrally mediate analgesia and antipyresis

56
Q

What is the major organ for biotransformation of the COx inhibitors?

A

Liver

Mo and Mik (9 decks)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2024 Bold Learning Solutions. Terms and Conditions