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Pharmacology > Lecture 8 - Pharmacology of Analgesia > Flashcards

Lecture 8 - Pharmacology of Analgesia Flashcards

1
Q

Define

Nociception

A

Pain perception

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2
Q

Nociceptive terminal

Chemical receptors

A

ASIC, P2X, P2Y
Beta-1, Beta-2

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3
Q

Nociceptive Terminal

Mechanical receptors

A

Mechanosensitive ion channel

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4
Q

Nociceptive terminal

Thermal receptors

A

TRPV1, TRPV2, TM8

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5
Q

General signal cascade in nociceptive terminal

A

Chemical, mechanical, and/or thermal recpetor activation –> Na+/Ca2+ influx –> membrane deploarization –> reach voltage-gated Na+ hannel threshold –> Action potential

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6
Q

Classsification of nerve fibers

A-alpha nerve fibers

A
  • somatic motor
  • propioception; muscle spindle (Ia), golgi tendon organ (Ib)
  • Myelinated
  • largest diameter and velocity
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7
Q

Classification of nerve fibers

A-beta nerve fibers

A
  • touch, pressure (II)
  • myelinated
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8
Q

Classification of nerve fibers

A-gamma nerve fibers

A
  • motor to muscle spindle
  • myelinated
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9
Q

Classification of nerve fibers

A-delta nerve fibers

A
  • Pain (fast), cold, touch (III)
  • myelinated
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10
Q

Classification of nerve fibers

B nerve fibers

A
  • Preganglionic sympathetic
  • myelinated
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11
Q

Classification of nerve fibers

C nerve fibers

A
  • Dorsal root - pain (slow), heat, mechanoreceptors, reflex (IV)
  • Sympathetic postganglionic
  • Most numerous
  • smallest diameter and velocity
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12
Q

Define

Hyperanalgesia

A

Peripheral sensitization such as inflammation of tissue injury which leads to over-response to normal stimuli or increased sensitivity to pain

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13
Q

Process of inflammation

What substances are released to cause inflammation?

A

Histamines, prostaglandins, bradykinin, serotonin

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14
Q

What is the result of of inflammation?

A
  • Redness, swelling, warmth, pain, and loss of function
  • Promotion of healing
  • pain receptors stimulated
  • nerves sensitized
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14
Q

What are the key mediators of inflammation?

A
  • Prostaglandins (PG): made in cell membranes
  • Cyclooxygenase (COX): required to make prostaglandin from arachidonic acid
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15
Q

Prostaglandin production

What blocks phospholipase A2 from synthesizing arachidonic acid from the cell membrane?

A

Anti-inflammatory steroids, cortisol, hydrocortisone, and prednisone

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16
Q

Prostaglandin production

Arachidonic acid + liopgenase = ?

A

Leukotrienes - mediators for asthma and allergy

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17
Q

Prostaglandin production

Arachidonic acid + COX1 or COX2 = ?

Reaction blokced by NSAIDs

A
  • Prostacyclin
  • Prostaglandin –> PGF2, PGE2
  • Thromboxane –> Platelet plug (blocked by aspirin)
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18
Q

Describe the prostanoid backbone

A

20-carbon carboxylic acid with cyclopentane ring and a 15-hydroxyl group (all prostaglandins, prostacyclins, and thromboxanes)

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19
Q

What are ecosanoids and where do they bind?

A
  • Prostaglandins, thromboxanes, lipoxins, leukotrienes
  • Bind to GCPRs
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20
Q

Ecosanoids involved in vasocontriction

A

PGF2-alpha, TxA2, LTC4, LTD4, LTE4

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21
Q

Stages of inflammation

Ecosanoids involved in vasodilation (erythemia)

A

PGI2, PGE1,PGE2, PGD2, LXA4, LXB4, LTB4

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22
Q

Stages of inflammation

Ecosanoids involved in edema (swelling)

A

PGE2, LTB4, LTC4, LTD4, LTE4

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23
Q

Stages of inflammation

Ecosanoids involved in chemotaxis and leukocyte adhesion

A

LTB4, HETE, LXA4, LXB4

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24
# Stages of inflammation Ecosanoids involved in increased vascular permeability
LTC4, LTD4, LTE4
25
# Stages of inflammation Ecosanoids involved in pain and hyperanalgesia
PGE2, PGI2, LTB4
26
# Stages of inflammation Ecosanoids involved in local heat and systemic fever
PGE2, PGI2, LXA4
27
# Major physiological function of prostaglandins Activation of inflammatory response
- produces pain and fever - tissue damage --> WBCs to site --> prostaglandins produced
28
# Major physiological function of prostaglandins Blood clots form when blood vessel is damaged
Thromboxane - stimulates constriction and clotting of platelets
29
# Major physiological function of prostaglandins Induction of labor
- Other reproductive processes - PGE2 causes uterine contractions and has been used to induce labor
30
# Major physiological function of prostaglandins Other effects
- Inhibits acid synthesis and increases secretion of protective mucus in the GI tract - Increased blood flow to the kidneys - Leukotrienes and prostaglandins promote vasoconstriction of bronchi
31
Thromboxane functions
- vasoconstrictor - potent hypertensive agent - facilitates platelet aggregation
32
Prostacyclin function
- Inhibits platelet activation - vasodilator
33
How do nonsterioidal anti-inflammatory drugs (NSAIDs) decrease inflammation?
Inhibits prostaglandin sythesis
34
NSAID groups
- Original NSAIDs - salicylates and aspirin - Synthetic NSAIDs - ibuprofen and celecoxib
35
Salicylate functions (aspirin, salicyclic acid, methyl salicylate)
- Antipresis (reduces fever) - Blocks prostaglandin stimulation of the CNS - Prevents heart disease and formation of thromboemboli
36
Cinical indications of NSAIDs
- Headache dental extraction, soft tissue injury, sunburn, musculoskeletal, joint overexcertion, and strain - Chronic treatment of dsmenorrhea - Tendinitis, bursitis, osteoarthritis, and rheumatoid arthritis (visceral pain caused by inflammation)
36
# Actions of NSAIDs Analgesics, anti-inflammatory, antipyretics
- Inhibits syhtesis of prostaglandinsand prevent bradykinin from stimulating pain receptors - inhibits pain centrally and peripherally
37
Systemic effects of NSAIDs in Peptic Ulcer Disease
- Inhibition of COX --> decrease in prostaglandins --> increase in gastric acid secretion, decrease in bicarbonate/mucus production and blood flow - increaded expression of intracellular adhesion, molecules in gastric vascular endothelium --> increased neutrophil adherence to vascular endothelial cells --> mucousal damage
38
Celecoxib
Selective COX-2 inhibitor
39
Acetaminophen (Tylenol)
- Analgesic and antipyretic - direct action on hypothalamus to reduce body temp - NOT a NSAID - metabolites can cause liver toxicity
40
# Opiod Analgesics How is PREsynaptic inhibition regulated?
Reduced activity of voltage sensitive calcium ion channels
41
# Opiod Analgesics How is POSTsynaptic inhibition regulated?
Enhanced chloride influx and potassium efflux (supresses pain perception)
42
# Opiod Analgesics Opioid mechanism of action
Opioid receptors (GiPCRs) decrease cAMP in neurons, inhibit Ca2+ channel, and activate K+ channel
43
# Define Endorphin
- Endogenous peptide hormone released from the pituitary gland - modifies pain perception and mood, regulates cardiovascular, respiratory, and GI function
44
Clinical Indications of opioid agonists
- Analgesia, sedation, cough, diarrhea - first-line therapy for pain associated with procedures, trauma or cancer - Releaves moderate to severe acute or chronic pain - sedatives co-administered with anaesthetics
45
Sources of opioid analgesics
- Naturally occuring - morphine and codeine (poppy plant) - Synthetic chemicals - Fentanyl
46
Where do centerally acting analgesics act?
Acts in the spinal cord and brain (does not impair the functions of peripheral nerves)
47
What are the major side effects of opioid analgesics?
- Tolerance - Physical dependence - Drug abuse - Respiratory depression - Constipation
48
Morphine
- Full mu agonist - high risk of respiratory depression - high abuse potential
49
Fentanyl
- full mu agonist - 100x more potent than morphine - Very high risk of respiratory depression - very high abuse potential
50
Butorphanol
- weak mu antagonist - 5x more potent than morphine - Moderate risk of respiratory depression - Lower abuse potential
51
Buprenorphine
- Partial mu antagonist - 30x more potent than morphine - moderate risk of respiratory depression - moderate abuse potential
52
Opioid antagonists
- Displace the analgesics and rapidly reverse respiratory depression - Naloxone and methylnaltrexone (MNTX) (competitive binding)
53
Partial opioid agonists
- Produces respiratory depression in normal individuals but reverses it in the case of acute opioid poisoning - butorphanol, nalbuphine, and pentazocine
54
Ziconotide
- A-typical pain relief agent - blocks calcium channels in the synapses - peptide - toxin found in some fish
55
# NSAIDs vs Opioids Type of pain relief
NSAIDs - mild to moderate pain associated with inflammation Opioids - severe and sharp pain by regulating neural transmission
56
# NSAIDs vs Opioids Major side effects
NSAIDs - Does not affect consciousness or mental function Opioids - Can lead to respiratory suppression, tolerance, addiction, and constipation
57
# NSAIDs vs Opioids How is analgesia produced?
NSAIDs - targets central and peripheral Opioids - Only targets central neurons
58
# NSAIDs vs Opioids Drug targets
NSAIDs - COX 1 and COX 2 Opioids - GPCRs

Pharmacology (23 decks)

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