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Pharmacology Test 3 > Pain Pathway & Opioids (Dr. Garcia) > Flashcards

Pain Pathway & Opioids (Dr. Garcia) Flashcards

1
Q

Opioids method of action

A

Hyperpolarizes cells by potassium channels

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2
Q

Pain

1.

2.

3.

4.

5.

A
  1. From Latin meaning punishment
  2. Sensory and emotional experience assoc. with actual or potential tissue damage
  3. Subjective and genetic
  4. Requires functional CNS
  5. Multiple brain areas
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3
Q

Pain pathway

1.

2.

3.

4.

5.

A
  1. Transduction
  2. Transmission
  3. Modulation
  4. Projection
  5. Perception
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4
Q

Classifications of Pain

Acute vs Chronic

A
  1. Acute: Physiologic purpose
    - short term with easy identifiable cause
    - bodies warning of tissue damage or disease
  2. Chronic pain
    - Persistant pain
    - May be constant or intermittent
    - Outlived usefulness, more difficult to treat
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5
Q
  1. Neuropathic pain
  2. Visceral pain
  3. Somatic pain
A
  1. Generated by the nervous system
  2. Organs…
  3. Skin and muscle
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6
Q
  1. Nociception
  2. Analgesia
  3. Hyperalgesia
  4. Allodynia
A
  1. Nociception
  • ability to perceive/sense pain
  • opiates produce ‘anti-nociception’
  1. Analgesia
  • Loss of sensitivity to pain WITHOUT loss of consciousness
    • opiates => ‘narcotic analgesics’
    • NSAIDs => non-narcotics
  1. Hyperalgesia
    * Inc response to painful stimuli
  2. Allodynia
    * Pain caused by a stimulus that would not normally provoke pain
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7
Q

SIgns of pain

Behavioral Signs

A

Behavioral Signs

  • Vocalization
  • Protective postures
  • Mood changes: aggression
  • Self-mutilation
  • Loss of appetite
  • Shallow/rapid breathing
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8
Q

Signs of Pain

Physiological Changes

A

Physiological Changes

  • General CV activation (inc sympathetic activity)
  • inc stress response (activation of HPA axis)
  • hyperglycemia (inc glycogenolysis & inc lipolysis)
  • reduced GI activity (ileus)
  • reduced immune function (diminished wound healing)
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9
Q

Therapeutic uses of Opioid drugs

A
  1. Anti-Tussive: Codeine and derivatives
    * Butorphanol…?
  2. Emetic: Apomorphine
  • Morphine
  • hydromorphone

*opioids also an anti-emetic…? after repeat doses

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10
Q

Problems

A
  1. Difficulty to assess pain in animals
  2. Specific behavior for each species
  3. Training personell and use validated scales
  4. Time and efficiency
  5. Subjective assessment
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11
Q

Multidimensional scales

A

Scales

  • Glasgow composite

Categories

  • physiologic parameters
  • behavioral responses
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12
Q

Approaches to Alleviate Pain

A
  1. Prevention
  2. Acupuncture
  • May activate endogenous pathways for pain suppression
    • opioid peptides: endorphins, enkephalins
  1. Analgesics
  • drugs that block stimulation of sensory nerve endings (transduction)
    • NSAIDS, Glucocorticoids
  • drugs that block impulse transmission in sensory nerves
    • Local Anesthetics
  • Drugs that block or modulate transmission in spinal / supraspinal pathways or alter the central perception of pain
    • Opioids
    • Alpha-2 Agonists
    • Dissociative Anesthetics (NMDA Antagonists)
    • NSAIDS
    • Local anesthetics
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13
Q

Analgesic Drug Action

CNS Action

A
  1. Alpha-2 agonists
  2. NMDA Antagonists
  3. Opioids
  4. Cannabinoids
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14
Q

Analgesic Drug Action

Epidural Injection

A
  1. Opioids
  2. Local Anesthetics
  3. NMDA Antagonists
  4. Alpha-2 Agonists
  5. NSAIDS
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15
Q

Analgesic Drug Action

Nerve Block

A
  1. Local Anesthetics
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16
Q

Analgesic Drug Action

Peripheral

A
  1. NSAIDs
  2. Corticosteroids
17
Q

DEA-Regulated Opioids

C1-CIV

A

Class 1:

  • heroin
  • bufotenine

Class 2

  • morphine
  • fetanyl
  • opium

Class 3

  • buprenorphine

Class 4

  • butorphanol
18
Q

Opioid Receptors

A

mu

kappa

delta

19
Q

Required Drugs

Morphine =>

Butorphanol =>

Buprenorphine =>

Naloxone =>

A

Morphine => full agonist

-limiting factor is side-effects

Butorphanol => agonist-antagonist

  • will eventually reach full analgesia
  • ceiling effect (and will reverse itself at high doses I think)

Buprenorphine => partial agonist

-ceiling effect (and will reverse itself at high doses I think)

Naloxone => antagonist

20
Q

mu receptor

A

Most effective opioid recepter (most potent analgesic)

Has the most side effects

21
Q

Pharmacological Actions of Opioids

A

Depresses

  • CNS
    • analgesia
    • mood alteration
    • sedation
    • nausea/vomiting (dogs)
    • depressed breathing (change)
  • GI
    • contipation (dec propulsive activity)
  • CV
    • bradycardia hypotension (histamine release)
22
Q

Opioid Analgesia

Effect and levels of action

A

Effect involves at least two levels of action

Spinal Cord (modulation)

  • dec substance P release from sensory afferents
  • dec postsynaptic actions of substance P

Supraspinal Level (perception)

  • dec affective response to pain
  • dec fear / anxiety associated with pain
23
Q

Opioid Sedation

A
  1. Variable degree of sedation depending on species, age and demeanor
  2. Additive depression with other CNS depressants
    * reduces overall anesthetic requirement in most animals
  3. Dopinergic decrease
  4. Opioids can cause excitement as a premed
24
Q

Ventilatory Depression in opioid

A
  1. Depresses PCO2 sensitivity of brainstem repiratory center neurons
  • reversible with naloxone
  • most common cause of death in humans in opioid overdose
25
Q

Opioid Nausea & Emesis

A
  1. Caused by stimulation of brainstem chemoreceptor trigger zone (CTZ)
  • apomorphine is extremely effective
  • reduced by phenothiazines and other dopamine antagonists
    • Anti-emetic after first dose
    • Effect of Vomiting Center
26
Q

Opioid cough suppression

A

Butorphanol

27
Q

Opioid pupillary Effect

A

Species specific

28
Q

GI Actions of Opioids

A
  1. Inhibit most indices of GI activity
  2. GI effects local and CNS actions
  • dec propulsive movements (peristalsis)
  • dec secretion
  • inc segmental contractions (tone, intragastric pressure)
29
Q

Cardiovascular actions of Opioids

A

Cause

  • dec heart rate
  • dec blood pressure if: histamine release

Reversed by anti-cholinergic agents

30
Q

Morphine

A
  1. Moderate lipid solubility, mod ability to penetrate blood-brain barrier
    * ideal for epidural administration
  2. High first pass metabolism
  3. Metabolized via glucuronic conjugation
  4. Active metabolites
  • morphine-6-glucuronide (M6G)
  • morphine-3-glucoronide (M3G)
  1. Potency 1 (related to dose, 1 not very potent)
31
Q

Fentanyl

A
  1. Potent synthetic opioid agonist
    * 100X more potent than morphine for most indications
  2. Good analgesic in dogs, cats and horses
  3. Less cardiovascular impact than morphine
    * less histamine release
  4. fairly short half life (rapid liver metabolism
32
Q

Meperidine

A
  1. Good sedative in young / geriatric patients
  2. Structure similar to atropine
    * only opioid to cause inc in heart rate
  3. Give IM because of histamine release
33
Q

Buprenorphine

A
  1. Mild-moderate analgesic
  2. given SC, IM, IV,
    * sublingual in cats
34
Q

Butorphanol

A
  1. Mu antagonist / kappa agonist
    * Can use to reverse some of effects of Mu agonists while providing analgesia via kappa
  2. Minimal side effects
  3. Mild analgesic in dogs, cats
  • less CV and respiratory depression
  • effective anti-tussive in dogs and cats
  1. Good analgesia in Horses and ruminants
35
Q

Naloxone

A
  1. Full antagonist
  2. Shorter half-life than most opioids
  3. opioid intoxication reverseral
36
Q

Neuroleptanalgesia

A
  1. animal unresponsive to sensory stimuli and no response to pain but not completely unconscious
  2. Combination of an analgesic with a sedative
  • penothiazines
  • alpha-2 agonists

Pharmacology Test 3 (12 decks)

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