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PMCOL 200 - Introduction to Pharmacology > Lecture 10 - Over the Counter Drugs - Analgesics > Flashcards

Lecture 10 - Over the Counter Drugs - Analgesics Flashcards

1
Q

Neurons that detect sensory information in the periphery are called:

A

primary afferents

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2
Q

Primary afferent synapse onto ____ afferents in the ____ which passes sensory information up to the brain.

A

secondary; spinal cord

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3
Q

____ efferents take ____ commands from the brain and send them to the periphery (muscles or glands)

A

motor;motor

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4
Q

Pain is detected by a specific class of primary afferents called ____.

A

nociceptors

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5
Q

Where are nociceptors located?

A
  • embedded in the epidermis.
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6
Q

Which channels are temperature sensitive ligand-gated ion channels?

A

TRP (transient receptor potential)

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7
Q
  • TRPM8 is activated at what temperatures and give an example of a medication?
  • TRPV1 is activated at what temperatures and give an example of a medication?
A

TRPM8 is for temperatures below 10 degrees and menthol
TRPV1 is for temperatures above 43 degrees and capsaicin

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8
Q

Other receptors respond to inflammatory molecules such as:

hint- there are 3, bcp

A
  • Bradykinin
  • Cytokines
  • Prostaglandins
  • these are released from immune cells following tissue injury or infection
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9
Q

Chronic use of capsiacin leads to excess calcium activation causing desensitization and ____ of ____ nociceptors.

A

loss of TRPV1

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10
Q

____ acid is a fatty acid present in phospholipids of cell membranes and is freed from the phospholipid molecule by the enzyme ____ A2.

A

Arachidonic; phospholipase

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11
Q

Which enzymes metabolize arachidonic acid into prostaglandins(PG) and thromboxanes (TX)?

A

Cyclooxygenase 1 and 2; COX 1 and COX 2

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12
Q

COX1 and COX2 metabolize arachidonic acid into what 2 components?

A

Prostaglandins (PG) and Thromboxanes (TX)

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13
Q

Which of the following are functions of prostaglandins?
1. Inflammation
2. Vasodilator
3. Pyrogenic
4. Leuokatactic
5. Gastric mucosa production (mainting low pH)
6. Platelet aggregation
7. Vasoconstriction

A

1-5

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14
Q

What are the 2 functions of Thromboxanes?

A

Platelet aggregation and vasoconstriction

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15
Q

Potent vasodilators lead to vasodilation of blood vessels and is also associated with ____ and ____.

A

swelling;redness

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16
Q

What does a pyrogenic molecule do?

A

associated with elevation in body temperature; fever.

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17
Q

Which prostagladin is associated with inflammation?

A

Prostaglandin E2

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18
Q

What signals the platelets to form a clot, causing vasoconstriction?

A

thromboxane A2

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19
Q

Arachidonic acid ia converted to ____ within blood vessels

A

thromboxane A2

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20
Q

COX _ is primarily expressed in non-imglammatory cells such as blood vessels, platelets and gastric mucosa. It is Constitutive (always on)

A

1

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21
Q

COX _ is primarily expressed in inflammatory cells such as macrophages. It is constitutive and inducible (must be activated by stimulus)

A

2

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22
Q

What is NSAIDs?

A

Non-Steroidal Anti-Inflammatory drugs.

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23
Q

NSAIDs inhibit ____ and ____.

A

COX1 and COX2

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24
Q

As NSAIDs inhibit COX1 and COX2, it results in a decreased production of what?

A

Prostaglandin and Thromboxanes.

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25
Q

Decreasing prostaglandin production inhibits inflammation and reduces ____.

A

Pain; aspirin reduces the production of PGH2 so its not binding to nociceptors so you don’t feel as much pain.

26
Q

NSAIDs also suppress prostaglandin synthesis in the brain that is stimulated by pyrogens and reduce ____ (antipyretic action)

A

fever

27
Q

Example of a NSAID?

A

aspirin

28
Q

Most NSAIDs inhibit the ____ site of COX enzymes (where arachidonic acid binds).

A

catalytic

29
Q

Acetylsalicylic acid (____) is a ________, ________ inhibitor. It permanenetly binds to the catalytic site of COX enzymes through ____ bonds.

A

aspirin; non-competitive, irreversible; covelent

30
Q

Why does aspirin have a long half life?

A

due to its permanent binding to the catalytic site.

31
Q

Why do immune cells (half life of 6-8hrs) recover faster than platelets (~96hrs)?

A

Platelets are anucleated and they make new proteins very slowly but immune cells are nucleated and they divide/recover much more quickly.

32
Q

Non-selective NSAIDs are associated with ____ toxicity due to inhibiton of COX 1 enzymes in ____ mucosa.

A

Gastric

33
Q

Chronic use of aspirin can result in gastric ____ and upper GI ____ and renal ____.

A

ulcers; bleeding; failure

34
Q

Ketoralac (____) is a highly efficacious non-selective NSAID (comparable to morphine) which blocks COX ____ more effectively than COX ____.

A

Toradol; 1 and 2

35
Q

Non-selective NSAIDs inhibit COX ____ more than COX ____.

A

1 and 2

36
Q

CHronic use of Toradol results in ____ issues; recommeded for short-term use.

A

gastric.

37
Q

To bypass gastric toxicity caused by the inhibition of COX 1 enzyme, specific ____ inhibitors are developed.

A

COX 2

38
Q

Specific COX2 inhibitors are also associated with a higher risk of ____ toxicity.

A

cardiovascular toxicity such as abnormal heart rate; lethal arrythmias.

39
Q

An example a specific COX2 inhbitor is:

A

celecoxib.

40
Q

____ is a weak and reversible COX1 and COX2 inhibitor, so it doesnt work like other NSAIDs

A

Acetominophen

41
Q

Besides COX1 and COX2, what else does acetominophen inhibit that is found in the cerebral cortex?

A

COX3

42
Q

COX3 interfers with ____ processing and ____ synthesis.

A

nociceptive; prostaglandin

43
Q

Which drug is an analgesic and antipyretic agent that lacks anti-inflammatory effects and does not effect the COX2 emxyme found in immune cells?

A

Acetaminophen.

44
Q

Acetominophen will not block ____ and ____ but will reduce fever and block pain.

A

swelling and redness.

45
Q

Acetominophen can lead to ____ damage/death if overdosed. It saturates the normal ____ enzymes that breakdown the drugs.

A

liver; liver

46
Q

What was the first local anesthetic discovered in the late 19th century and was used as a topical anesthetic for ophthalmological surgery?

A

Cocaine.

47
Q

What are the 3 examples of the most widely used topical anesthetics?

Hint: PIB

A

Procain, lidocaine and bupivivaine.

48
Q

The most local anesthetics contain 3 regions, what are they?

A
  • hydrophobic (aromatic)
  • A linker region
  • A substituted amine (hydrophilic)
49
Q

Which region is hydrophobic, the linker region, the aromatic or the substituted amine?

A

aromatic

50
Q

Which region is hydrophilic, the linker region, the aromatic or the substituted amine?

A

substiuted amine.

51
Q

Procaine is really vulnerable to plasma ____ meaning it breaks down really quickly; it would also have a much shorter half-life than lidocaine or bupivicaine due to the ester connection in the linker.

A

Esterase.

52
Q

Identify the following topical Anesthetics

A
53
Q

Local anesthetics bind ____ to a specific site within the pore of ____ channels and block ion movement through the pore; inhibits the ability of the neurons to fire upon ____ channels blocking.

A

Reversibily; Na+

54
Q

The site to which anesthetics bind is only accesible ____ (must cross the cell membrane).

A

intracellularly

55
Q

Hydrophobicity ____ both the potency and duration of action because the Na+ channels binding pocket is hydrophobic and anesthetics must cross the hydrophobic cell membrane.

A

increases

56
Q

More hydrophobic = more ____, longer ____

A

potent; action.

57
Q

All neurons (sensory, motor) require which channels for action potential progapgation?

A

Sodium channels

58
Q

Local anesthetics block all sensation and can cause ____ paralysis in the area.

A

motor

59
Q

Local anesthetics have ____ affinity for the open conformation of the ____ channels so they prefentially block neurons that are active (i.e., nociceptors when there’s pain)

A

higher; sodium

60
Q

When the voltage-gated Na+is closed is there increased or decreased anesthetic binding?

A

decreased

61
Q

When the voltage-gated Na+is open is there increased or decreased anesthetic binding?

A

increased

62
Q

Capsaicin is an ____ for the ____ receptor

A

agonist; TRPV1

PMCOL 200 - Introduction to Pharmacology (12 decks)

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