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PHRM 845 Exam 5 > Barker's lecture 2 part 2 > Flashcards

Barker's lecture 2 part 2 Flashcards

1
Q

PK of Morphine/Phenanthrenes

A

Metabolism
-readily absorbed
-first pass metabolism
-bioavailability 25%

Hepatic
-CYP2D6, CYP3A4
-genetic differences
-elimination T1/2 increased with liver disease

Glucuronidation at 3’ and 6’

Morphine-6-glucuronide
still potent

Excretion
-glomerular filtration
-90% excreted in 24h

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2
Q

Some opioid metabolites are still active

A

Heroin, codeine, tramadol=prodrugs

Fentanyl and methadone do not produce active metabolites

Onset/duration influenced by lipophilicity

Morphine: low lipophilicity, slower passage across BBB, prolonged duration of action

Fentanyl: high lipophilicity, rapid onset, short duration

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3
Q

CYP3A4 (FOUR)–> MAKES OPIOIDS STARTING WITH NOR

A

Codeine–CYP2D6–>Morphine

CYP3A4–>NOR metabolites which is less active

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4
Q

Fentanyl is a very potent opioid

A

100x potent over morphine

50x potent over heroin

Used for palliative care, breakthrough pain

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5
Q

Sufentanil, remifentanil, alfentanil

A

agonists

anesthesia/sedation

breakthrough by plasma esterases due to ester linkage

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6
Q

Hydromorphone, oxymorphone

A

agonists

no opioid-active metabolites

IV, oral liquid, PCA

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7
Q

Morphine

A

agonist

ER

Long-acting, lower rush

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8
Q

Hydrocodone, oxycodone

A

agonist

pre/peri/post procedure pain

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9
Q

Tramadol

A

Mild opioid analgesic

Has SNRI properties

5-HT/NE reuptake inhibitor, stimulate 5HT release

Management of mild neuropathic pain

Painkiller used when you don’t want to prescribe a stronger opioid

Schedule 4

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10
Q

Meperidine

A

Used to treat rigors

Has toxic metabolite normeperidine that causes nervousness, tremors, twitches, seizures

Renally excreted

Not recommended without good justification

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11
Q

Methadone

A

Primarily used for opioid dependence

Long duration of action/long half life

Prolonged QTc
NMDA antagonist
Chronic pain

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12
Q

Why would antagonism at NMDA receptors be useful?

A

block pain signal that is coming in

may help with analgesia effect

secondary function

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13
Q

Codeine

A

cough/antitussive

Schedule 2

Schedule 5 in certain formulations

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14
Q

Dextromethorphan

A

enantiomer of levomethorphan

limited opioid activity

at high doses acts as SSRI, NMDA antagonist

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15
Q

Diphenoxylate with atropine

A

schedule 5

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16
Q

Loperamide

A

strong p-gp substrate–low BBB

scheduled 5/decontrolled OTC

17
Q

Eluxadoline

A

mu/kappa agonist

delta antagonist

scheduled 4

18
Q

Pentazocine and Butorphanol

A

schedule 4

K agonist, partial agonist/antagonism at mu

SE: less dysphoria, hallucinations, increase BP and HR

19
Q

Nalbuphine

A

schedule 4

Full agonist at K, antagonist at mu

antagonism produces withdrawal

20
Q

Buprenorphine

A

partial mu agonist, weak K agonist and delta antagonist

opioid replacement therapy

21
Q

Opioid-induced hyperalgesia

A

prolonged exposure to opiates

secondary pain pathway that kicks in

changes in glutamate pathways

22
Q

Methadone the full agonist

A

cross tolerance

Provide relief from withdrawal

slow acting

Slow PK: accumulates with repeated soe

Elimination half-life (8-50hrs)

NMDA antagonist

23
Q

Buprenorphine partial agonist

A

ceiling effect

block full agonist effect
antagonist
use 4 hrs after last heroin dose

Provides some activation
agonist
less withdrawal

24
Q

Naltrexone the antagonist

A

decent oral bioavailability

will cause withdrawal

works better if patient has been drug free for 1 month or more

PO

25
Q

Naloxone

A

IV or nasal spray

limited or bioavailability

rapid onset

short half-life

26
Q

Neonatal abstinence syndrome

A

Symptoms: tremor, yawning, poor feeding, sweating

Onset: symptoms may begin 24-48 hours after birth or as late as 5-10 days

Heroin and other opiates including methadone

Cause serious withdrawal in the baby

Some symptoms can last as long as 4-6 months

Seizures can also occur

27
Q

Treatment of neonatal abstinence syndrome

A

Pharmacological:

Morphine sulfate–>oral morphine diluted to 0.4mg/ml

SL buprenorphine

Methadone

Morphine and buprenorphine linked with shorter hospital stay than methadone

Clonidine

PHRM 845 Exam 5 (13 decks)

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