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MD2002 > NSAIDS > Flashcards

NSAIDS Flashcards

1
Q

List the main actions of NSAIDs.

A

Anti-inflammatory
Analgesic
Anti-pyretic

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2
Q

What do NSAIDs do?

A

INHIBIT PROSTAGLANDIN BIOSYNTHESIS BY DIRECT INHIBITION OF CYCLO-OXYGENASE (COX)

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3
Q

What are the two main mechanisms used by NSAIDs to inhibit COX?

A

Irreversible, time dependant inhibition of COX

A rapid, reversible competitive inhibition of COX

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4
Q

Give an example of a NSAID that inhibits the COX enzyme irreversibly.

A

Aspirin

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5
Q

Describe the mechanism of action of aspirin.

A

Acetylates the alpha-amino group of the terminal serine of the enzyme forming a covenant bond, thus inhibiting it

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6
Q

Give an example of a NSAID that inhibits the COX enzyme reversibly.

A

Ibuprofen

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7
Q

Describe the mechanism of action of ibuprofen.

A

Bind reversibly with COX, competing for its active site with the natural substrate, arachidonic acid

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8
Q

What are prostaglandins?

A

Family of cyclic fatty acids which have hormone-like effects on the body

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9
Q

What is the difference between autocrine and paracrine cell signalling?

A

Autocrine has an effect on the cell that secreted the chemical signal
Paracrine has an effect on a more distant area, but still in the vicinity of the cell secreting the chemical signal

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10
Q

What two substances combine to produce prostaglandins?

A

COX (cyclo-oxygenase)

Arachidonic acid

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11
Q

Name three substances that are all products of arachidonic acid metabolism.

A

Thromboxanes
Prostaglandins
Leukotrienes

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12
Q

What is the function of COX-1?

A

Constitutive (i.e. is produced continuously in the body regardless of the needs of cells
Important in maintaining GI tract integrity

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13
Q

What is the difference in structure between COX-1 & COX-2 and what does this mean with regard to inhibition?

A

COX-2 has a ‘side pocket’ in its structure (additional ring)

This means that inhibitors have to be specific to either COX-1 or COX-2

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14
Q

What is the function of COX-2?

A

Inducible (i.e. brought about when needed)
Involved in inflammatory response
Implicated in cancer development

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15
Q

What specifically, when considering this topic, is released upon inflammation?

A

Prostaglandins:
Predominantly PGE2
Also PGI2
PGD2 from mast cells

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16
Q

What is the function of these specific prostaglandins in an inflammatory response?

A

Potent vasodilators
Have combined effects with other inflammatory mediators, e.g. histamine & bradykinin
Potentiate histamine & bradykinin actions on post-capillary venue permeability & pain sensory nerves

17
Q

What is the primary function of NSAIDs?

A

To reduce many of the local signs and symptoms of inflammation, i.e. redness, heat, swelling, pain

18
Q

Run through the anti-pyretic (anti-feverish) effect that NSAIDs have.

A

Bacterial endotoxins cause release of factors such as INTERLEUKIN 1 from macrophages
Interleukin 1 causes generation of prostaglandins in the hypothalamus (PGEs)
PGE prostaglandins increase the set point of temperature —> fever.
HOWEVER, NSAIDs prevent the formation of these prostaglandins, preventing rise in temperature

19
Q

Describe the analgesic (pain relieving) effect NSAIDs have.

A

Inflamed regions painful due to histamine & bradykinin release (activate nociceptors)
Prostaglandins sensitise nociceptive nerves to histamine & bradykinin
NSAIDs prevent prostaglandin production —> no pain

20
Q

What are the salicylates?

A

The aspirin family

21
Q

What is aspirin a pro-drug to?

A

Acetylsalicylic acid

22
Q

What can aspirin also be metabolised to and what metabolises it to this compound?

A

Salicylic acid

By plasma & tissue esterases

23
Q

How long does it take for salicylate to appear in the plasma and after what time do they peak in plasma concentration?

A

Appear after 30 minutes

Peak within 1-2 hours

24
Q

List some side effects of salicylate.

A

Stomach - bleeding, ulcers
Systemic - tinnitus, dizziness, impaired hearing, nausea, vomiting, hypersensitivity
Metabolic changes - acid/base balance affected
Haemostasis - blood coagulation affected through action on platelets
CNS - initial stimulation, ultimately coma & respiratory depression
Renal - insufficiency with chronic use & OD

25
Q

What category of drugs do ibuprofen and naproxen fall under?

A

Propionic acids

26
Q

Give an example of a fenamate.

A

Mefenamic acid

27
Q

List some advantages paracetamol has.

A

Good analgesic & antipyretic activity
Well tolerated in GI tract
Given orally (convenient) and well absorbed
Fewer side effects than other NSAIDs

28
Q

After how long does paracetamol reach its peak plasma concentration?

A

30-60 minutes

Half life 2-4 hours for therapeutic doses

29
Q

List some disadvantages paracetamol has.

A

Poor anti-inflammatory

Weak COX inhibitor (& may be specific to COX-3)

30
Q

What is a major issue associated with paracetamol overdose?

A

Hepatotoxicity —> hepatic necrosis (due to saturation of liver inactivation enzymes)

31
Q

What is the name given to selective COX-2 inhibitors?

A

Coxibs

32
Q

Give an example of a selective COX-2 inhibitor.

A

Celecoxib

33
Q

What are selective COX-2 inhibitors used to treat?

A

To treat osteoarthritis & rheumatoid arthritis

34
Q

When are COX-2 inhibitors generally used?

A

When the traditional NSAIDs produce too severe GI tract side effects

35
Q

List some cases in which NSAIDs would be used.

A 
Headache
Dysmenorrhea (painful menstruation)
Backache
Bony metastases of cancers
Postoperative pain
Anti-inflammatory action
Anti-pyretic action
36
Q

Which NSAIDs are used in cases of SHORT term analgesia?

A

ASPIRIN
PARACETAMOL
IBUPROFEN

37
Q

Which NSAIDs are used in cases of LONGER lasting chronic analgesia?

A

NAPROXEN

DICLOFENAC

38
Q

Why is important that the NSAID of choice for treating chronic inflammatory disorders has a low incidence of side effects?

A

Dosage for chronic inflammatory disorders is high

MD2002 (27 decks)

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