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Pain Medicine > Pharmacology > Flashcards

Pharmacology Flashcards

1
Q

Name the opioid receptor(s) each opioid acts at.

  1. Methadone
  2. morphine
  3. fentanyl
  4. sufentanil
  5. nalbuphine
  6. buprenorphine
A
  1. mu +++
  2. mu +++, kappa +
  3. mu +++
  4. mu +++, delta +, kappa +
  5. kappa ++
  6. partial mu +
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2
Q

Morphine pharmacology:

A
  1. 40% bioavailability
  2. 30% protein bound
  3. major pathway of metabolism of glucuronidation
  4. metabolized to morphine-6-glucuronide and morpine-3-glucuronide
  5. converted to hydromorphine
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3
Q

Name 4 opioids in the class of phenylpiperidines?

A
  • Fentanyl
  • Remifentanil
  • Sufentanil
  • Meperidine
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4
Q

Methadone pharmacology

A
  • synthetic
  • mu receptor preferential binding
  • noncompetitive antagonist at NMDAR
  • bioavaliability 50% (41-99%) oral or rectal
  • reaches peak plasma levels at 4hrs
  • onset to analgesia 30-60min orally
  • 90% protein bound
  • half life alpha 2-3 hours, beta 15-60 hours
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5
Q

Hydromorphone pharmacology

A
  • semisynthetic
  • 5X potency to morphine
  • SC route is 80% bioavailable
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6
Q

Oxycodone pharmacology

A
  • semisynthetic
  • mu and kappa agonist
  • peak plasma levels at 2 hours
  • oral bioavailability 60-87%
  • half-life 3-5.7 hours
  • metabolized by 2D6 and 3A4
  • metabolized to oxymorphone and noroxycodone
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7
Q

sufentanil pharmacology

A
  • 10X more potent than fentanyl
  • 1000X more potent than morphine
  • peak effect is 5min when given IV
  • rapid onset of respiratory depression
  • highly liophilic
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8
Q

fentanyl pharmacology

A
  • synthetic phenylpiperidine
  • 100X more potent than morphine
  • IV duration of action is 30-60min
  • patch - steady state at 12-24 hours after application; after patch removal 50% decline in plasma levels in 17 hours
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9
Q

codeine pharmacology

A
  • 10% converted to morphine
  • codeine itself has very low affinity for mu receptors
  • half-life 2-4 hours
  • metabolism is primarily by CYP2D6
  • 10% of caucasians cannot convert codeine to morphine
  • 1-2% are ultrarapid metabolizers
  • contraindicated in children undergoing tonsillectomy and adenoidectomy and children and adolescents for pain and cough management
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10
Q

tramadol pharmacology

A
  • synthetic codeine analog
  • SNRI + weak mu agonist
  • analgesia within one hour and peak effect in 2-3 hours
  • can lower seizure threshold
  • metabolism is primarily by CYP2D6
  • 1-2% are ultrarapid metabolizers
  • 10% of caucasians cannot convert codeine to morphine
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11
Q

Acetaminophen sites of action?

A
  • spinal cord

- cerebral cortex

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12
Q

Through what two pathways does acetaminophen exert its analgesic action?

A
  • weak central inhibition through prostaglandin synthetase

- inhibition of nitric oxide pathway (mediated by NMDA, Sub P)

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13
Q

What are side effects of acetaminophen?

A
  • liver toxicity
  • cholestatic jaundice
  • acute pancreatitis
  • thromocytopenia
  • agranulocytosis
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14
Q

MOA of NSAIDs?

A
  • inhibition PG production from AA by inhibiting COX-1/COX-2
  • direct action on spinal nociceptive processing
  • Goal is to COX-2 and not COX-1
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15
Q

Side effects of NSAIDs?

A
  • GIB
  • GI ulceration
  • disturbance of platelet function
  • sodium and water retention
  • nephrotoxicity
  • hypersensitivity reactions
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16
Q

Name common drugs that interact with NSAIDs

A
  • antacids
  • warfarin/anticoagulants
  • RA drugs (azothiaprine, gold compounds, methotrexate)
  • corticosteroids
  • diuretics
  • lithium
  • oral hypogylcemics
  • phenytoin
  • probenacid
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17
Q

MOA of calcium channel blockers?

A
  • bind to pre-synaptic alpha2 delta subunit of L(N)-type VGCC
  • reduces release of Sub P, glutamate and NE
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18
Q

Sites of action of gabapentinoids?

A

Central:

  • spinal dorsal horn
  • brainstem/forebrain (descending pathways)
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19
Q

Side effects of gabapentinoids?

A
  • fatigue
  • sedation
  • tremor
  • ataxia
  • peripheral edema
  • hallucinations
  • suicidal ideation
  • gastroretentive gabapentin (OD dosing) has lower incidence of side effects than regular gabapentin
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20
Q

Name common drugs that interact with gabapentinoids?

A
  • hydrocodone
  • morphine
  • naproxen
  • antacids
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21
Q

What is ziconatide?

A
  • inhibits presynaptic N-type calcium channel; thereby inhibits excitatory NT release (Glutamate and Sub P)
  • given intrathecally
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22
Q

Indications for ziconatide?

A
  • Chronic cancer pain
  • HIV neuropathy
  • neuropathic pain
23
Q

MOA of cannabinoids?

A
  • THC is agonist at CB1-R which inhibits DA neurons mainly by pre-synaptic inhibition.
  • CB2-R in CNS but CB1 more in brain.
  • CBD stimulates the vanilloid receptor type 1 (VR1)
  • Both are G-protein coupled receptors
24
Q

What are the indications for cannabinoids?

A
  • 3rd line for neuropathic pain
  • 2nd line for MS related pain
  • Chemotherapy induced nausea/vomiting
  • HIV-related neuropathy
  • HIV-related weight loss
  • MS or SCI related spasticity (not first line)
  • possible epilepsy
25
Q

MOA of NMDAR antagonists?

A
  • NMDA-R is a type of ionotropic glutamate receptor (other AMPA, KA).
  • Blocks excitatory neurotransmitters
  • Helps to decrease OIH through dampen central sensitization by decreasing NMDA-R hyperexcitability.
26
Q

What are examples of drugs that are NMDAR antagonists?

A
  • methadone
  • ketamine
  • memantine
27
Q

What are the side effects of methadone?

A

sedation, QTc prolongation, constipation, drug-drug interactions and all other general opioid side effects

28
Q

What are the side effects of ketamine?

A
  • increased BP
  • tachycardia
  • N/V
  • blurred vision
  • nystagmus, dissociation
  • altered MS
  • hepatotoxicity
  • ketamine induced cystitis.
29
Q

MOA of sodium channel blockers?

A
  • inhibits development and propagation of ectopic discharges

- block normally conducting non-nociceptive nerves

30
Q

What drugs are included in the category of sodium channel blockers?

A
  • antiepileptics
  • anticonvulsants
  • local anesthetics
  • TCAs
  • antiarrhythmics
31
Q

what are the max doses of:
Lidocaine
Bupivicaine
Ropivicaine

A

Lidocaine 4.5 (7 with epi)
Bupivicaine 2.5 (3 with epi)
Ropivicaine 2-3

32
Q

Side effects of sodium channel blockers?

A
  • delayed urinary retention
  • paresthesia
  • paresis/gait impairment
  • orthostatic hypotension
  • dyspnea
  • lidocaine
    • dizziness, blurred vision, seizure, bradycardia.. cardiac arrest
33
Q

What p450 enzyme metabolizes oxycodone?

A
  • 2D6

* 10% of Caucasian population are poor metabolizers and do not get good analgesic effects from oxycodone

34
Q

Opioid receptors are what type of receptors?

A
  • g-protein coupled receptors
35
Q

Opioid receptors act where (cellularly)?

A
  • presynaptic (decrease calcium influx and subsequent NT release
  • post-synaptically through opening of K channels and subsequent hyperpolarization
36
Q

Opioid receptors act where (anatomically)?

A
  • PAG - activate descending projections that involve NE and 5-HT and modulate excitability of dorsal raphe and locus coeruleus which project limbic/forebrain (emotional strcutures)
  • selectively depress the discharge of dorsal horn neurons
37
Q

What are two different strategies for opioid rotation as per Canadian guidelines?

A

Method 1: Decrease the total daily dose of the current opioid by 25–50% and convert to new opioid equivalent dose
Method 2. Decrease the total daily dose of the current oral opioid 10-30% while starting the new oral opioid at the lowest total daily dose for the formulation
OR
decrease the total daily dose of the current opioid 10-25% per week while titrating up the total daily dose of the new opioid weekly by 10-20% with a goal of switching over 3-4 weeks

38
Q

What three main treatment approaches available to clinicians managing patients with opioid-induced sleep disordered breathing?

A
  1. Reduce opioid dose without specific treatment for sleep apnea
  2. Don’t change the opioid dose but provide specific sleep apnea treatment (CPAP, MRD, etc.)
  3. Reduce opioid dose and provide specific treatment for apnea.
39
Q

What are long-term consequences of opioid therapy?

A
  • OIH
  • Sleep apnea
  • hypogonadism
40
Q

What are three strategies for opioid tapering as per Canadian guidelines?

A
  1. Gradually reduce dose by 5–10% of morphine equivalent dose every 2–4 weeks with frequent follow-up.
  2. Switching from immediate release to controlled
    release opioids on a fixed dosing schedule may assist some patients in adhering to the withdrawal plan.
  3. Switch opioid to methadone or buprenorphine/naloxone preparations and then gradually taper
    * Reduce the opioid dose rapidly over a few days/weeks or immediately but must be carried out in a medically supervised withdrawal centre.
41
Q

How do you taper fentanyl patch?

A
  • Consider reducing fentanyl by 12–25 μg/h patches every 2–4 weeks
  • Consider adding immediate release oral opioid for pain relief (e.g. morphine IR 5 mg q 4–6 h prn)
  • Once fentanyl is at the lowest available dose (e.g. 12 μg/h every 72 hours), stop the fentanyl transdermal patch and only use the immediate release oral opioid for pain relief
42
Q

When does opioid tolerance become clearly evident?

A
  • 3 months

* a reasonable opioid trial is 3-6 months

43
Q

What are common acute side of opioids?

A
  • sedation
  • constipation (most common)
  • urinary retention
  • nausea
  • pruritis
44
Q

What are four opioids that would theoretically be useful for treating neuropathic pain?

A
  • methadone
  • tramadol
  • tapentadol
45
Q

What opioids are in the the class named phenanthrenes?

A

All the morphines - heroin, hydromorphone, naloxone, oxycodone, morphine, buprenorphine

46
Q

Which opioids do not show up on UDS?

A

synthetics (fentanyl, methadone) and semisynthetics (oxycodone, hydromorphone, hydrocodone)

47
Q

What are the pharmacological properties of antidepressants?

A
  • monoamine transmission
  • cholinergic transmission
  • glutamatergic
  • opioid receptor
  • sigma receptors
  • neurokinin receptors
  • corticotrophin releasing factor receptors
48
Q

Pharmacological mechanisms of antidepressants in nociception?

A
  • descending inhibition
  • monoamine modulation
  • glutamatergic neurotransmission (NMDA suppression)
  • opioid interactions (stimulate endogenous opioid release, decreased opioid utilization, synergistic effects)
    Miscellaneous:
  • through adenosine
  • ion channels (Na channels, Ca and K channels)
  • TCAs can decrease inflammatory responses
49
Q

Antidepressants with the best evidence for pain control?

A
  • TCAs
  • Venlafaxine
  • Duloxetine
  • Milnacipran
50
Q

Side effects of TCAs?

A
  • sedation
  • orthostatic hypotension
  • urinary retention
  • dry mouth
  • falls
  • confusion
51
Q

tapentadol pharmacology?

A
  • opioid agonist and NE reuptake inhibitor
  • works at both ascending and descending pathways
  • metabolized primarily by glucuronidation
  • 3.3mg of tapentadol = 1mg morphine
  • lower incidence of nausea and constipation
  • can result in serotonin syndrome through indirect effects
52
Q

tapentadol indications?

A
  • moderate to severe acute pain
  • acute low back pain and radicular pain
  • OA
  • post-op pain
  • ER formulation approved for severe DPN
  • moderate to severe cancer pain
53
Q

How to do a rotation to Tapentadol?

A
  • D/C all other long-acting opioids, and initiate tapentadol ER at 50% of oral morphine equivalents

Pain Medicine (14 decks)

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