Opioids And Analgesics Ii

Front 1

why is meperidine a poor first-line option full agonist?

Back 1

-low potency, rapid onset, and short duration of action
-toxic metabolite normeperidine is a CNS stimulant (with high repeated doses or in renal dz it may accumulate and cause seizures)

Front 2

__________ is contraindicated in epilepsy

Back 2

meperidine

Front 3

______________ are not reversed by naloxone

Back 3

seizures

Front 4

meperidine is contraindicated in pts receiving __________

Back 4

MAO inhibitors

Front 5

normeperidine

Back 5

toxic metabolite of meperidine that is a CNS stimulant
-can accumulate and cause seizures

Front 6

why is opioid use contraindicated in pts receiving MAOI?

Back 6

-severe, immediate rxn causing excitation, sweating, hyperpyrexia, HTN, rigidity
-meperidine inhibits reuptake of NE and 5HT; concurrent use with MAOIs causes the serotonin syndrome

Front 7

____________-- has significant antimuscarinic effects and tachycardia

Back 7

meperidine

Front 8

half-life of methadone

Back 8

-longest and most variable half-life

Front 9

duration of analgesia with methadone

Back 9

-duration of analgesia is much shorter than the half-life

Front 10

how long does it take to attain full analgesic effect of methadone?

Back 10

-may not be attained until after 3-5 days

Front 11

what are the characteristics of respiratory depression with methadone use?

Back 11

-peak repiratory depressant effects occur later and persist longer than peak analgesic effects

Front 12

methadone is associated with ____________&__________ since it does delay repolarization

Back 12

QT prolongation and torsades

Front 13

indications for methadone

Back 13

--relief of severe pain
(slower development of tolerance and physical dependence, and milder withdrawal symptoms)
-detoxificatio/temporary maintenance of opiate addiction of opiate addiction
(usually >/= 1yr, but can be indefinitely)

Front 14

what are the major ADR of opioids present in Methadone use for maintenance of opioid addiction?

Back 14

-dulled senses/reflexes, altered mental state, pinpoint pupils, constipation, and drowsiness

Front 15

indication for fentanyl transdermal system

Back 15

-management of chronic pain in pts requiring continuous opioid analgesia
-persistent mod->severe chronic pain in opioid-tolerant pts needing continuous admin for extended time period

Front 16

fentanyl transdermal system is contraindicated in the treatment of?

Back 16

-acute and post-operative pain

Front 17

codiene in pure form is a schedule_____ drug and is used primarily for ________&_______ when other meds fail.

Back 17

1. C-II
2. antitussive and antidiarrheal

Front 18

Codeine used in combo with ASA
1. name of drug
2. schedule
3. use

Back 18

1. Empirin with codiene
2. C-III in AL
3. for moderate pain

Front 19

Codeine used in combo with acetaminophen:
1. name of drug
2. schedule
3. use

Back 19

1. Tylenol #3
2. C-III in AL
3. for moderate pain

Front 20

codeine must be converted to ______ via _________ to exert analgesic effects

Back 20

1. morphine
2. P450 2D6

Front 21

hydrocodone is significantly more________ than codeine with a ______ of action

Back 21

1. potent
2. longer duration

Front 22

__________ is a prodrug that must be converted by 2D6 to hydromorphone for analgesic action

Back 22

hydrocodone

Front 23

buprenorphine is a ______________ that when given IM or IV it is indicated for__________

Back 23

1. partial opioid agonist
2. relief of moderate to severe pain but has ceiling effect for analgesia (this limits its usefulness for severe pain)

Front 24

advantages in using buprenorphine over opiates

Back 24

-much lower abuse potential
-less danger of overdose
-lower intensity of withdrawal Sx upon d/c

Front 25

MOA/characteristics of buprenorphine

Back 25

-partial agonist at mu rec/high affinity/dissociates very slowly
-antagonist at kappa rec
-long duration of action and low physical dependence

Front 26

use of buprenorphine in pts physically dependent on opiates

Back 26

-may result in W/D effects
-cannot be substituted in opiate-dependent addicts due to antagonistic component

Front 27

advantages of buprenorphine use in pts and addicts actively undergoing W/D from opioids

Back 27

-can be used to controlW/D Sx
-safer than methadone in overdose since max intrinsic efficacy is reached at lower doses than those needed to cause significant respiratory depression
-long duration of action(once-daily dosing)
-mild physical dependence/limited W/D Sx so D/C less difficult

Front 28

MOA of buprenorphine use in pts and addicts actively undergoing W/D from opioids

Back 28

-dissociates slowly from the mu receptors
-blockade of euphoric responses from subsequently administered opioids

Front 29

MOA of a mixed opioid agonist-antagonist

Back 29

-agonist at the kappa rec; weaker analgesia compared to mu rec. stimulation, with lower potential for respiratory depression
-antagonist at the mu rec.; lower abuse potentialthanwith full agonists

Front 30

admin of a mixed opioid agonist-antagonist to a pt physically dependent on anopioid agonist at the mu receptor?

Back 30

- can precipitate a withdrawal syndrome

Front 31

will tolerance and dependence occur with continued use of a mixed opioid agonist-antagonist?

Back 31

YES

Front 32

pentazocine

Back 32

-mixed opioid agonist-antagonist
-IM (Talwin)

Front 33

receptor interactions of pentazocine

Back 33

-agonist actions at kappa and sigma rec
-weak antagonist at mu rec; may precipitate W/D Sx in pts physically dependent on opioids
-sedative activity
-psychotomimetic effects

Front 34

pentazocine combined with naloxone taken orally

Back 34

-if taken po the naloxone (a pure antagonist) is inactive; pentazocine is absorbed and exerts analgesic effects

Front 35

pentazocine combined with naloxone

Back 35

-if tablet crushed and efferts made to solubilize the material for injection, the naloxoneis solubilized along with the pentazocine, and antagonizes the opioid effects of pentazocine

Front 36

opioid antagonists (2)

Back 36

-naloxone
-naltrexone

Front 37

MOA of naloxone

Back 37

-competitive antagonism of all opioid receptors with greatest effects at mu rec.
-reverses opioid induced respiratory depression after overdoses
-precipitates withdrawal syndrome in physical dependence

Front 38

indications for naltrexone

Back 38

-management of previously detoxified heroin addicts
-also indicated for tx of alcohol dependence

Front 39

centrally-acting nonopioid analgesics (2)

Back 39

-tramadol
-tapentadol (Nucynta)

Front 40

indications for tramadol

Back 40

-moderate-moderately severe pain

Front 41

MOA of tramadol

Back 41

-actions mediated through an active metabolite formed from 2D6
-not anopiate, but binds to mu oiate rec.

Front 42

tramadol warnings

Back 42

-not recommended for use in opioid dependence
-may enhance seizure risk in pts taking drugs that lower the seizure threshold
-pts with allergic responses to opioids may be at risk

Front 43

___________is a centrally acting analgesic with two mechanisms

Back 43

tapentadol (Nucynta)

Front 44

mechanisms of tapentadol (nucynta)

Back 44

-mu opioid receptor agonist
- NE reuptakeinhibitor; facilitates adrenergic component of the descending analgesia Sx

Front 45

abrupt D/C of tapentadol (Nucynta)

Back 45

-will cause W/D Sx