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Pharmacology II: Exam 1 > Pain Management > Flashcards

Pain Management Flashcards

1
Q

Somatic (nociceptive) Pain

A

“Normal pain”

  • originates in skeletal muscle, ligaments, and joints
  • localized and constant (dull, sharp, aching)
  • prostaglandin mediated: typically responds to NSAIDs (and opioids)
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2
Q

Visceral (nociceptive) Pain

A

“Vague, cannot pinpoint”

  • Originates in smooth muscle (solid or hollow organs)
  • Difficult to localize (diffuse, gnawing, crampy)
  • Responds to opioid analgesics
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3
Q

Neuropathic (deafferentiated)

A
  • Peripheral or central nerve injury, not stimulation
  • Burning, tingling, shooting pain
  • Poor response to analgesics- better response to adjuvant Tx
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4
Q

Emerging theme of pain management

A
  • Over excited pain fibers
  • Treat by: Diminishing excitation by hyperpolarizing nerve:
  • -> Reduce influx of Na, Ca
  • -> Increase influx of Cl
  • -> Increase efflux of K
  • Reducing release of pain eliciting neurotransmitters
  • Enhancing inhibition
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5
Q

Opioid Receptor Function

A
  • Found in ascending & descending pain pathways and in portions of the brain
  • Most commonly used opioids are full mu receptor agonists
  • No ceiling effect on analgesia
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6
Q

Mu receptor

A

Analgesia, sedation, respiration depression, constipation, euphoria

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7
Q

Kappa receptor

A

Analgesia, respiratory depression (< mu), sedation, constipation, dysphoria, psychomimetic

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8
Q

Delta receptor

A

Analgesia

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9
Q

Opioid Therapy is First Line for

A
  • Acute severe pain

- Moderate to severe chronic pain related to cancer or other life threatening/limiting illness

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10
Q

Opiate

A 
A drug (i.e morphine, heroin, codeine) containing or derived from opium and tending to induce sleep and to alleviate pain
- From opium poppy
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11
Q

Opioid

A

Possessing some properties characteristic of opiates, but not necessarily derived from opium (fentanyl, methadone)
-Not necessarily from opium poppy

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12
Q

Mu agonist

A
  • Type of opioid

- Relieves pain by binding to the Mu receptor in the nervous system

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13
Q

Mu antagonist

A

Drug that competes with an agonist for opioid receptor binding site (Mu receptor) but has no effect at the site

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14
Q

Mixed agonist/ antagonist

A

A type of opioid that binds to the kappa receptor as an agonist, but to the mu receptor as an antagonist

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15
Q

Partial agonist

A

A compound which possesses affinity for a receptor, but unlike a full agonist, will elicit only a degree of the pharmacological response, even if a high proportion of receptor are occupied by the compound

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16
Q

Route of Administration: Oral

A
  • Significant first pass effect

- IV to PO dose conversions

17
Q

Route of Administration: Parenteral

A

IV, IM, SubQ, PCA

18
Q

Route of Administration: Transdermal

A
  • Compliance benefit

- Disadvantage: cannot rapidly titrate opioid

19
Q

Route of Administration: Neuraxial

A
  • Epidural, intrathecal

- Allow for small doses, longer duration

20
Q

Other routes of administration

A
  • Transmucosal
  • Rectal
  • Topical
  • Intranasal
21
Q

Differences in efficacy between opioids

A
  • No evidence of difference in efficacy of any opioid at equianalgesic doses
  • Onset of action: fentanyl and derivatives quicker IV
  • Duration of action: methadone naturally long acting, most other drugs formulated into long acting oral formulations
22
Q

Mixed agonist- antagonist/ partial agonists

A
  • Lower abuse potential
  • “ceiling” effect on both side effects and analgesia- may not be effective for severe pain
  • High psychotomimetic response due to Kappa stimulation
  • May cause pain or precipitate withdrawal in patients currently receiving full mu opioid agonists
23
Q

Acute opioid induced side effects

A

Common: constipation, cognitive impairment, sedation, nausea, itch
Less common: Sweating, myoclonus, urinary retention, respiratory depression, dry mouth, headache

24
Q

Chronic opioid induced side effects

A

Amenorrhea, sexual dysfunction, immune dysfunction, QTc prolongation (methadone)

25
Q

Treatment for opioid induced side effects

A
  • Most agents treat symptoms (i.e antiemetics for nausea)
  • Opioid antagonists target mechanisms:
  • Respiratory depression
  • Constipation
  • Pruritis
  • Nausea
26
Q

Respiratory Depression

A
  • Opioids have direct effects on respiratory centers and at chemoreceptors
  • Greater risk in patients with COPD, age, sleep apnea, use of additional meds
  • Pain antagonizes respiratory depression
  • Naloxone blocks effects of opioid agonist, reverses respiratory depression
27
Q

Peripherally Acting Antagonists

A
  • Antagonists may reverse side effects but may also reverse analgesia
  • Agents that act peripherally block peripheral adverse effects of opioids without reversing central analgesia
  • Constipation
28
Q

Opioid Induced Hyperalgesia (OIH)

A
  • Increased pain sensitivity
  • Hyperalgesia (increased sensitivity to painful stimuli) and allodynia (pain elicited by non painful stimuli)
  • Abnormal pain often arises from an anatomically distinct region and is of a different quality
29
Q

Tolerance

A

A state of adaptation in which exposure to a drug induces changes that result in a reduction of one or more of the drug’s effects over time

  • The need for a higher dose to achieve the same pharmacological effect
  • Hallmark: Decrease in duration of analgesia per dose
30
Q

Physical Dependence

A

-A state of adaptation that is manifested by a drug class specific withdrawal syndrome that can be produced by abrupt cessation, rapid dose reduction, decreasing blood level of the drug, and/or administration of an antagonist

31
Q

Addiction

A

Primary, chronic disease of the brain reward, motivation, memory and related circuitry. Dysfunction in these circuits leads to characteristic biological, psychological, social, and spiritual manifestations
-Pathologically pursuing reward and/ or relief by substance use and other behaviors

32
Q

Poor Opioid Responsiveness

A

If dose escalation due to tolerance (or disease progression) leads to side effects:

  1. Manage side effects
  2. Pharmacologic strategy to lower opioid requirement:
    - spinal route administration
    - add non opioid or adjuvant analgesic
  3. Non pharmacological strategy to lower opioid requirement
33
Q

Opioid Rotation

A

Opioid rotation involves switching from one opioid to another to optimize analgesia and lessen side effects (or for financial savings or convenience)

34
Q

Incomplete Cross Tolerance

A
  • When switching from one opioid to another at equianalgesic dose a greater response is observed from the new opioid
  • May require a reduction of 33-50% of calculated dose
  • Due to relative selectivity for receptor subtypes or differences in potency or both

Pharmacology II: Exam 1 (3 decks)

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