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Year 1: Patho/Pharm > Pain PHARM > Flashcards

Pain PHARM Flashcards

1
Q

Opioid
Agonist-antagonists
Examples

A

Butorphanol
Nalbuphine
Pentazocine

SE:
cause withdrawal if given with pure opioids
psychotomimetic reactions

MOA:
agonist kappa receptor
antagonist mu receptor

*Exception
Buprenorphine (partial agonist mu, antagonist kappa)

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2
Q

SE Opioids

A

Sedation

Respiratory depression

bradycardia

Hypotension

Urinary retention

*No Tolerance to below:
Constipation
Miosis (pinpoint pupils)

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3
Q

How long does it take to develop physical dependence and tolerance?

A

1-2 weeks

Require wean and WAT-1 score

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3
Q

Example
Pure opioids

A

Strong
Morphine
fentanyl
methadone
hydromorphone, oxymorphone, levorphanol

Moderate
Codiene
Oxycodone
Hydrocodone

MOA

agonist at mu receptors (analgesia, euphoria, sedation, respiratory supression, physical dependence)

Agonist at kappa receptors (analgesia, sedation, psychomimetic effects)

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4
Q

Equianalgesic dose

A

cross tolerance to opioids

dose for different route and/or different opioid

start lower than equianalgesic dosage, cross tolerance is incomplete

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5
Q

Why do you. not prescribe meperidine

A

Toxic metabolite - normeperidine

AE:
Psychogenic - hallucinations, dysphoria, agitation, seizures
serotonin syndrome

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6
Q

Breakthrough dose of opioids

A

1/6 the total daily opioid dose
Q2H PRN

strong opioid, short acting, rapid onset

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7
Q

Decrease SE from opioid

A

reduce dosage by 1/4

opioid rotation

add non opoioid adjuvant

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8
Q

mu receptor
Function

A

sedation

euphoria

respiratory depression

decrease GI motility
- decrease peristalsis
- decreased secretions
- increase rectal sphincter tone

analgesia

physical dependence and tolerance
- decrease receptor number
- decrease receptor activation

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9
Q

kappa receptor
Less agonist activity
Examples

A

sedation

analgesia

Decreased GI motility

psychomimetic effects - hallucinations, nightmares etc.

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10
Q

Pure opioid antagonist
Examples

A

Naloxone
Naltrexone

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11
Q

Morphine MOA

A

binds endogenous opioid receptors
mu agonist
kappa agonist

mu receptor
- respiratory depression, sedation, GI motility decreaes, physical dependence
- sedation, analgesia, euphoria (majority effect)

kappa receptor
- sedaiton
- analgesia
- psychomimetic effects - hallucinations

*receptors exist in the dorsal horn/posterior horn in teh substantia gellatinosa
modulation pain - decrease afferent sensory neurons from sending pain signals to the brain

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12
Q

Morphine SE

A

Respiratory depresion
- caution opoioid naive, swithcing opioid, or increasing dosage

Contradinicated
- pregnancy and breast feeding

SE:
respiraotry depresison
sedation
hallucinations

hypotension
*blunts baroreceptor reflex
*release histamine

bradycardia

urinary retention

constipation
- decrease peristalsis
- increase sphincter tone
- decrease secretions

pruritis
*releases histamine

emesis
- stimulate chemoreceptor trigger zone

physical dependence and tolerance
- decrease receptor number
- decrease receptor activity

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13
Q

Codeine

A

moderate strength opioid
pure opioid
agonist mu and agonist kappa

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14
Q

Codiene
pharmacokinetics

A

Liver converts codiene to morphine (10%)
CYP2D6
ultrametabolizers (higher proportion converted) dangerous (leads to respiratory supression and death)

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15
Q

Codiene contraindications

A

ultra metabolizers

children

pregnancy and breast feeding

16
Q

Codiene ultrametabolizers
Why?

A

They have multiple copies of teh CYP2D6 gene
they convert way more than 10% to morphine
leads to respiratory supression and death

17
Q

Fentanyl
Indications, SE, duration action

A

INdications
- chronic pain, cancer pain
- Severe pain

MOA
- 100x affinity for mu and kappa receptors compared to morphine

SE
- severe respiratory sedation and death
- same as morphine

Duraiton action
- transdermal patch
- 24 hours reach peak
- 48 hours duraiton

Contraindications
- children < 18 years
- weight < 110lbs
- post operative pain/perioperative pain
- CYP3A4 inhibitors (results in toxicity)

18
Q

Pharmakokinetics
Fentanyl

A

100x affinity for mu and kappa receptors

metabolized by CYP3A4
- inhibitors result in toxicity (respiratory depresison and death)

19
Q

Methadone
Indication, SE, contraindications

A

Indication
- chronic pain
- long acting strong opioid
- duration 72 hours

SE
- QT prolonged interval, torsades de pointes
- respiratory depression if combined with CNS depressant (black box warning)

Contraindications
- do not combine with CNS depressant
- QT interval prolonged

20
Q

Prescribing considerations
Methadone

A

ECG baseline, 1 month, anually
- looking for prolonged QT interval

Do not prescribe iwth CNS depressants
- toxicity, respiratory depresison and death

21
Q

Moderate Opioids
Examples
Multi-modal therapy

A

Percocet
- tylenol + oxycodone

Perdocan
- ASA + oxycodone

Vicodin
- Hydromorphone + tylenol

*risk abuse potential when crushed
increases onset
rapid onset = addiction

22
Q

Tramadol
MOA, SE, contraindications

A

MOA
- synthetic opioid
- codiene analog

  1. weak agonist mu receptor
  2. inhibits reuptake of NE and serotonin
  • neurmodulation of pain in the dorsal horn/posterior horn
  • inhibit release excitatory NT
  • promote release inhibitory NT
  • promote activation inhiitory interneurons

SE
- HTN crisis (combined with MAO innhibitor)
- serotonin syndrome (MAOi, SSRI, SNRI, TCA, triptan etc.)

Contraindications
- banned from prescription in canada
- CLass I opioid

DEATH WHEN COMBINED WITH CNS DEPRESSANT

23
Q

Opioid tolerance
pathophysiology

A

decreased number receptors
decreased intrinsic activity of receptors

24
Q

opioid physical dependence

A

high dose
long duraiton therapy 1-2 weeks
will develop physical dependence and abstenience syndrome when withdrawal

25
Q

Buphrenorphine
MOA, Indication, SE

A

MOA
- partial mu agonist
- kappa antagonist

Indication
- opioid withdrawal
- addiction

SE
- naloxone/naltrexone does not work
- binds too tightly to the mu receptor
- there is no reversal agent
- renal or hepatic disease (too much drug in system)
- prolonged QT interval (similar to methadone)

26
Q

Saboxone
Example

A

Saboxone = buphrenorphine + naloxone

used in withdrawl/detoxification opioids
induction agent to stablize withdrawal

  1. naloxone to kick off opioid
  2. buphrenorphine to partially antagonize the mu receptors (binds tightly)
27
Q

Embeda
Example

A

morphine + naltrexone
PO formulae
prevents abuse - naltrexone will block euphoria if it is crushed

28
Q

Opioids that prolong the QT interval

A
  1. methadone
  2. buphrenorphine
  3. saboxone
29
Q

opioids that result in toxicity with CYP

A
  1. fentanyl
    - CYP3A4 inhibitors result in toxicity
  2. Codiene
    - CYP2D6 ultrametabolizers increase amount converted to morphine > 10%
30
Q

Neuropathic pain
Adjuvants

A

SNRI
- venlafaxine
- duloxetine

SSRI
- paroxetine
- fluoxetine
- citalopram

TCA
- amytriptyline
- nortriptyline

AED
- topiramate
- divalproex (VPA)
- gabapentin
- pregabalin
- carbamazepine

31
Q

Trigeminal neuralgia
Treatment

A

Carbamazepine

SE
- neuro: diplopia, nystagmus, blurred, ataxia, sedation
- bone: bone marrow supression, bleeding
- liver/kidney: hepatitis, kidney disease
- teratogenic
- hyponatremia and water retention
- Skin: TENS, DRESS, SJS (HLA1502 asian)

32
Q

Cannabinoid examples

A

Nabilone = THC
Sativex (nabiximol) = THC + cannabidiol
Marinol = Dronabinol = THC
Medical Marijuana

33
Q

Cannabinoid
MOA, SE

A

bind endogenous cannabinoid receptors
release endogenous opioids

34
Q

Capsaicin cream

A

block C fibre transmission

35
Q
A

Year 1: Patho/Pharm (39 decks)

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