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Pharm > Lecture 6: Analgesics > Flashcards

Lecture 6: Analgesics Flashcards

1
Q

What are drugs that treat inflammation and/or fever?

A

Aspirin and NSAIDs

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2
Q

What are drugs that block sensation?

A

Topical anesthetics

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3
Q

What are drugs that block pain?

A
  • Acetaminophen

* Capsaicin cream

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4
Q

What are the two classes of pharmaceutical drugs?

A
  • Those that are prescription only

* Those are directly available to the consumer

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5
Q

Why is there a huge diversity of products?

A

Because there is only a limited number of approved active ingredients, but they recombine the amounts

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6
Q

What is Analgesics?

A

Pain killing

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7
Q

What are some medications used for Analgesics?

A
  • Tylenol
  • Advil
  • Motrin
  • Robax
  • Anacin
  • Excedrin
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8
Q

What are some typical Decongestants?

A
  • Sudafed
  • Mucinex
  • Coricidin
  • Dristan
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9
Q

What are some common Cough, sleep, allergy medications?

A
  • Buckley’s
  • Benylin
  • Dimetapp
  • Robitussin
  • NyQuil
  • Claritin
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10
Q

What is Efficacy?

A

The ability to evoke a response or produce an effect

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11
Q

What are Primary Afferents?

A

Neurons that detect sensory information in the periphery

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12
Q

Where do Primary Afferents take sensory information?

A

From the periphery to the spinal cord

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13
Q

What do Primary Afferents synapse onto?

A

Secondary afferents in the spinal cord

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14
Q

What do Secondary Afferents do?

A

The carry sensory information from from the spinal cord to the brain

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15
Q

What do Efferent fibers do?

A

Take commands from the brain and send them to the periphery

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16
Q

Which part of the spinal cord do Primary Afferents enter?

A

They enter through the Dorsal horn

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17
Q

What helps to modulate the incoming primary afferents?

A

The descending signals sent by the pain system

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18
Q

What can activate the descending pathway?

A

Opioids and acetaminophen

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19
Q

What is the pathway of the modulating pain Efferents?

A

Parts of the brain synapse at PAG, then RVM, and then to the dorsal horn in the spinal cord

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20
Q

What is pain detected by?

A

Nociceptors

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21
Q

What are Nociceptors?

A

A specific class of primary afferents that detect pain

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22
Q

What are Polymodal Nociceptors?

A

Nociceptors that detect many types of painful stimuli

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23
Q

What are different types of painful stimuli detected by?

A

Specific receptors expressed on polymodal nociceptors

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24
Q

What are the receptors on nociceptors linked to?

A

Intracellular pathways that activate signalling that cause the generation of an action potential into the CNS

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25
Q

What cause the different types of pain sensations perceived?

A

The combination of what signalling gets activated

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26
Q

What are Transient Receptor Potential (TRP) channels?

A

Temperature sensitive ligand-gated ion channels

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27
Q

What are different types of TRP channels tuned to respond to?

A

Very specific temperatures

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28
Q

What is TRPM8 activated by?

A

Temperature below 10ºC

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29
Q

What is TRPV1 activated by?

A

Hot temperatures above 43ºC

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30
Q

Aside from temperature what can TRPV1 and TRPM8 be activated by?

A

Ligands

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31
Q

Which TRP does menthod activate?

A

TRPM8

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32
Q

Which TRP does Capsaicin activate?

A

TRPV1

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33
Q

What do other receptors respond to?

A

Inflammatory molecules

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34
Q

What are inflammatory molecules released from?

A

Surrounding immune cells following tissue injury or infection

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35
Q

What are examples of inflammatory molecules?

A
  • Bradykinin
  • Cytokines
  • Prostaglandins
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36
Q

What is the Axon Reflex?

A

Increased pain sensitivity due to inflammation

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37
Q

What is Hyperalgesia?

A

Increased pain sensitivity in a region

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38
Q

What would aim to such down the increased sensitivity of pain signals?

A
  • Opioids
  • Cannabinoids
  • Noradrenaline
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39
Q

How does Bradykinin work?

A

It bind to the B2 receptor which activates PKC and phosphorylates the TRPV1 channel which enhances the ability of TRPV1 to open and cause depolarization

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40
Q

What is Arachidonic acid?

A

A fatty acid present in phospholipids of cell membranes

41
Q

How is Arachidonic acid freed from the phospholipase molecule?

A

By the enzyme Phospholipase A2

42
Q

What does Phospholipase A2 do?

A

Frees arachidonic acid from the phospholipase molecule

43
Q

What is Arachidonic acid key in?

A

Inflammatory mediation

44
Q

What is Arachidonic acid converted into by COX1 and COX2?

A

Prostandoids

45
Q

What do COX1 and COX2 do to Arachidonic acid?

A

They convert it to Prostanoids

46
Q

What are Prostanoids?

A

A family of signalling molecules

47
Q

What are some Prostanoids?

A
  • Prostaglandins
  • Prostacyclin (PGI2)
  • Thromboxane (TXA2)
48
Q

What are Prostaglandins associated with?

A

Inflammation

49
Q

What is different about COX2?

A

It is the inducible form of the COX enzyme

50
Q

Where does COX2 occur?

A

Only in areas of inflammation

51
Q

When is COX1 expressed?

A

It is constitutively expressed (expressed all the time)

52
Q

Since COX1 is constitutively expressed, what does it do?

A

It facilitates baseline production of certain prostaglandins like PGI2 which protects certain organs and facilitates mucus secretion

53
Q

What is COX2 induced by?

A

Inflammation

54
Q

What is the site of Aspirin and NSAIDs?

A

COX1 and COX2 enzymes

55
Q

What does the Prostanoid pathway do generally?

A

It is either inflammatory (COX2) or it is protective

56
Q

What does the enzyme 5-lipoxygenase (LOX) do to arachidonic acid?

A

It metabolizes arachidonic acid into various leukotrienes

57
Q

How do Prostaglandins and Leukotrienes drive inflammation?

A

They are vasodilators, pyrogenic (fever inducing) and attract immune cells

58
Q

Where are Prostaglandins and leukotrienes especially pyrogenic?

A

When they reach the thalamus

59
Q

What happens with immune cells once they are attracted by prostaglandins?

A

They can be induced to attract COX2

60
Q

Where is COX1 primarily expressed?

A

In non-inflammatory cells (blood vessels, platelets, gastric mucosa)

61
Q

Where is COX2 mainly expressed?

A

In inflammatory cells

62
Q

What do non-selective NSAIDs target?

A

Both COX pathways

63
Q

What do COX2 specific NSAIDs target?

A

The COX2 pathway

64
Q

Where are the cells that express the inducible COX2 pathway found?

A

Cells that respond to inflammatory stress like macrophages, synoviocytes, endothelial cells, kidneys

65
Q

What do Aspirin and other non-selective NSAIDs do?

A

Inhibit both COX isoforms

66
Q

What happens when aspirin and nsaids inhibits both COX isoforms?

A

Prostaglandin production decreases, inhibiting inflammation and reducing pain and fever

67
Q

How do Aspirin and other NSAIDs reduce fever?

A

By inhibiting the COX pathway they suppress prostaglandin synthesis in the brain that is stimulated by pyrogens

68
Q

Which COX pathway would it be bad to inhibit?

A

COX1 because it is supposed to be constitutively active

69
Q

Why are Non-selective NSAIDs associated with gastric toxicity?

A

Because they inhibit COX1 which is supposed to constitutively active and produce mucus in the stomach, bicarbonate, and blood flow

70
Q

What can chronic use of non-specific NSAIDs do?

A

Cause gastric toxicity like gastric ulceration, upper GI bleeding and renal failure

70
Q

What can chronic use of non-specific NSAIDs do?

A

Cause gastric toxicity like gastric ulceration, upper GI bleeding and renal failure

70
Q

What can chronic use of non-specific NSAIDs do?

A

Cause gastric toxicity like gastric ulceration, upper GI bleeding and renal failure

71
Q

How can the gastric toxicity due to non-specific NSAIDs be bypassed?

A

Specific COX2 inhibitors have been developed

72
Q

What do COX2 inhibitors do?

A

They reduce inflammation in chronic inflammatory diseases, but are less effective at treating acute pain

73
Q

What are specific COX2 inhibitors also associated with?

A

Higher risk of Cardiovascular toxicity

74
Q

What does Acetaminophen inhibit?

A

COX3

75
Q

Where is COX3 found most abundantly?

A

In the cerebral cortex

76
Q

What is the difference between the effects of acetaminophen and NSAIDs?

A

Acetaminophen lacks the anti-inflammatory effects

77
Q

What are the effects of Acetaminophen?

A

It is an analgesic and antipyretic agent

78
Q

Which enzymes does Acetaminophen block?

A

COX1 and COX3

79
Q

How can Acetaminophen be toxic?

A

When taking by overdose in patients it can lead to liver damage and death

80
Q

What are the most widely used topical anesthetics?

A
  • Procaine
  • Lidocaine
  • Bupivacaine
81
Q

What do most local anesthetics contain?

A
  • Hydrophobic (aromatic) moiety
  • A linker region
  • Substituted amine (hydrophilic region)
82
Q

What is the hydrophilic region of a topical anesthetic?

A

The substituted amine

83
Q

What does the nature of the linker region of a topical anesthetic do?

A

Determine pharmacological properties

84
Q

What does an ester linker region mean?

A

Because they are hydrolyzed easily they are able to get rid of in the body so they have a shorter affect

85
Q

What is the effector mechanism of local anesthetics?

A

They bind reversibly to an intracellular site within the pore of sodium channels and block ion movement through the pore

86
Q

What must anesthetics do in order to block a pore?

A

They must cross the cell membrane

87
Q

Why does hydrophobicity increase the potency and duration of action of an anesthetic?

A

Because the Na+ channel binding pocket it hydrophobic and anesthetic must cross the hydrophobic cell membrane

88
Q

What do all local anesthetics do?

A

Block all sensation and can cause motor paralysis

89
Q

What do local anesthetics have higher affinity for?

A

The open conformation of the sodium channel, so they preferentially block neurons that are active (nociceptors when there is pain)

90
Q

What are different types of painful stimuli detected by?

A

Specific receptors on polymodal nociceptors

91
Q

What is the active ingredient in chilli pepper?

A

Capsaicin

92
Q

What is Capsaicin an agonist for?

A

The TRPV1 receptor

93
Q

What does capsaicin do to TRPV1 receptors?

A

It activates normal signalling TRPV1

94
Q

What does initial application of Capsaicin do?

A

Gives a sense of burning

95
Q

What does chronic activation of TRPV1 induced by capsaicin do?

A

Cause desensitization of TRPV1 which blocks its ability to transmit afferent information. Basically blocks its function to signal for pain leading to analgesia

95
Q

What does chronic activation of TRPV1 induced by capsaicin do?

A

Cause desensitization of TRPV1 which blocks its ability to transmit afferent information. Basically blocks its function to signal for pain leading to analgesia

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