Brainscape's Knowledge GenomeTM

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


See full index

Pharm 1 > Opiods Part 2 > Flashcards

Opiods Part 2 Flashcards

1
Q

What is Meperidine (Demerol)?

A

A synthetic opioid agonist at mu and kappa receptors

  • structurally similar to atropine
  • fentanyl products are derived from the base of meperidine
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

How is meperidine metabolized?

A

Extensive hepatic metabolism —> normeperidine —> merperidinic acid, which has toxic effects

  • primarily excreted by kidneys
    • the worse the kidney, the more toxic the effects
  • 1/ life is 3-5 hours
  • 60% protein bound
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

What are the the analgesia and 1/2 life of normeperidine (first mepeperidine metabolite) like?

A

1/2 the analgesic properties of meperidine (still active)
Elimination time is 15 hours
—> >35 hours in renal failure (keeps extending and extending)

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

What are side effects of normeperidine?

A
  • Produces CNS stimulation *
  • CNS stimulation leads to myoclonus and seizures
  • Demerol induced delirium-> confusion, hallucinations,
  • worse in elderly
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

What is meperidine used for now?

A

Too dangerous to use routinely for pain

Mainly used for shivering

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

What are side effects of meperidine?

A
  • increased HR (atropine like effect)
  • orthostatic hypotension- frequent and profound
  • interferes with compensatory SNS
  • large doses decrease myocardial contractility
  • dose dependent ventilatory impairment- worse than morphine
    • Serotonin Syndrome ** especially when given with SSRIs, MAOIs, zyvox and ultram
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

What is Serotonin Syndrome?

A
  • FEVER, HTN, CONFUSION ** hallmark signs (without other sources)
  • tachycardia
  • diaphoresis
  • confusion, agitation
  • hypereflexia
  • coma, seizures
  • coagulopathies
  • metabolic acidosis
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

If planning to give meperidine, zyvox or ultram and your pt is on antidepressants (SSRI,MAOI), what can you do to prevent serotonin syndrome?

A

Hold antidepressant while pt is on zyvox, ultram or meperine

- 7 days for zyvox treatment usually

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

Is there currently a dose ceiling for opioids?

A

No

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

What is the mechanism of action for methadone?

A

Mu agonist with NMDA antagonism

  • CYP metabolism—> inactive metabolites
  • renal and fecal elimination
  • variable 1/2 life (8-60 hours)
  • causes QT prolongation (risk of tornadoes)
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

What are some opioid agonist-antagonists (mixed agents)?

A
  • pentazocine
  • but orphan oil
  • nalbuphine
  • bupresnorphine
  • nalorphine
  • bremazocine
  • dezocine
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

Why are mixed agents important (opioid agonist-antagonist)?

A

Created in response to deaths from respiratory depression in pure opioid agonists

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

What is the mechanism of action for opioid agonist-antagonists?

A

Bind to mu receptors

  • partial agonist produce LIMITED EFFECT AT MU RECEPTOR
  • competitive antagonists produce NO EFFECT at mu receptor
    • may cause partial agonist action at kappa and delta receptors **
  • antagonistic property may effect other opioids
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

What is unique about opioid agonist-antagonists?

A

Glass ceiling: antagonist effect creates a maximum beyond which additional levels have no effect

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

What are the advantages of opioid agonist-antagonists?

A
  • provides analgesia with limited ventilatory depression
  • low potential fro physical dependence
  • should be reserved for pts who cannot tolerate pure opioid agonists *
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

What is true of tolerance and dependence with opioids in general?

A
  • major limitation of all opioids
  • cross tolerance develops between all opioids
  • tolerance can occur without dependence *
  • dependence cannot occur without tolerance
17
Q

What is the structure like in opioid antagonists?

A
  • result from minor changes to structure of opioid agonist

- most commonly, substitution of an alkyl group for a methyl group

18
Q

What are the 3 main opioid antagonists?

A
  • nalaxone
  • naltrexone
  • nalmefene
  • “nals” *
19
Q

How do opioid antagonists work?

A
  • competitive antagonism
    • high affinity for opioid receptor
    • displaces opioid from mu receptor
20
Q

What is nalaxone?

A

Non-selective antagonist at all 3 opioid receptors

- useful in reversal of opioid (in neonates also) and in detecting suspected physical dependence

21
Q

How is nalaxone metabolized?

A

Hepatic enzymes

  • 1/2 life 60-90 minutes ( may need repeated doses for long acting opioids)
  • duration of action = 30-45 minutes
22
Q

What are side effects of naloxone?

A
  • reversal of analgesia/sudden onset of pain
  • N/V related to speed of injection
  • increased SNS activity—> tachycardia, HTN, pulmonary edema, cardiac dysrhythmias
23
Q

What are neuraxial opioids?

A

Opioids in the epidural or subarachnoid space

- mu receptors present in substantia gelatinosa of the spinal cord

24
Q

What is unique regarding neuraxial opioids?

A

Analgesia from neuraxial opioids is NOT associated with:

  • SNS denervation
  • skeletal muscle weakness
  • loss of proprioception (own sense of movement)
25
Q

What is the significance of the epidural space being lipophillic?

A
  • meds here can still absorb systemically (especially if lipophillic-> cell membranes are lipophillic)
  • morphine is ionized and tends to stay in the epidural space
    • vasoconstrictors (epi) given to keep med in
26
Q

Epi is given to prevent epidural med from distributing systemically, but…….

A

It does not effect diffusion into CSF (depending on lipid solubility)

  • coughing/straining causes quicker absorption
  • positioning has no effect
27
Q

When an opioid is given in epidural space there are similar blood/plasma concentrations as when given which other route?

A

I.M.

28
Q

What are the 4 classic side effects on neuraxial morphine administration?

A
  1. ) pruritus
  2. ) N/V
  3. ) urinary retention
  4. ) depression of ventilation
    * * neuraxial opioids can also cause shingles **
29
Q

Which receptors does Ketorolac (toradol) work on and what effects do they have?

A

NSAID, COX 1 and 2 inhibitors

  • COX participate in inflammatory and pain cascade
    • also work on gut and kidneys
  • COX 1 protects layer in GI tract—> NSAID use reduces this layer—> GIB
30
Q

What are side effects of Ketorolac?

A
  • BLACK BOX WARNING: NOR MORE THAN 5 DAYS OF USE DUE TO RISK OF GI BLEEDING*
  • ARF
  • GI
  • CHF
  • platelet malfunction
31
Q

What are some considerations for acetaminophen (Ofirmev: IV)(Tylenol)?

A
  • Hepatotoxicity * cause by metabolite Napqui

Give mucomyst for O.D.

32
Q

What are maximum daily doses for acetaminophen?

A

Liver failure: 2 G daily

Elderly: 3 G daily

33
Q

What is the mechanism of action for Tramadol (Ultram)?

A

Mu agonist, weak SNRI (serotonin norepinephrine reputable inhibitor)

  • CYP metabolism: no active metabolite
  • *contraindicated in seizures **
    • lowers seizure threshold
    • anyone with seizures should never take ultram

Pharm 1 (9 decks)

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