PHARM - Anti-Inflammatory Drugs II: The Arachidonic Acid Pathway and NSAIDS - Week 6 Flashcards

1
Q

Name 5 things that inflammation can occur in response to.

A

Infection
Trauma
Chemicals
Heat
‘Danger’

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2
Q

What three protective mechanisms does inflammation convey?

A

Prevents infection
Clears damaged cells/debris
Facilitates healing

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3
Q

List the two main anti-inflammatory actions of NSAIDs.

A

Inhibition of vascular dilation
Inhibits synergism with other mediators that enhance leakiness

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4
Q

What three conditions can NSAIDs be used as an analgaesic?

A

Headache
Menstrual pain
Musculoskeletal pain

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5
Q

What is often the preferred NSAID for use as an anti-pyretic agent?

A

Paracetamol

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6
Q

List the three major chemical classes of NSAIDs.

A

Salicylates
Propionic acids
Acetic acids

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7
Q

What chemical class of NSAIDs does aspirin fall under?

A

Salicylates

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8
Q

What chemical class of NSAIDs does ibuprofen fall under?

A

Propionic acids

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9
Q

What is the mechanism of action of salicylates?

A

Irreversibly acetylates COX

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10
Q

What are the three main/common uses for aspirin?

A

Analgaesic
Antipyretic
Anti-thrombotic

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11
Q

Name three possible side effects of aspirin.

A

Reyes syndrome
Tinnitus
Uric acid retention

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12
Q

What is the mechanism of action of acetic acids?

A

Potent inhibitors of COX

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13
Q

Which chemical class of NSAIDs is used largely for long-term treatment of inflammatory conditions (like rheumatoid arthritis)?

A

Acetic acids

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14
Q

What is the major adverse effect of NSAIDs and when is it most common?

A

Inhibiting the normal regulatory role of prostanoids, most common when taken at high doses for long periods.

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15
Q

List three adverse effects of inhibiting prostanoids.

A

Increased chance of GI ulceration/bleeding
Increased bleeding time
Renal impairment

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16
Q

Is it more ideal to inhibit COX1 or COX2? Explain why.

A

COX2 because it results in decreased inflammation, while inhibition of COX1 can result in GI disturbances.

17
Q

Define coxibs, what they inhibit, and what symptom it is less likely to induce.

A

Inhibits both COX1 and COX2, but inhibits COX2 far more.
It results in less gastrointestinal adverse effects.

18
Q

Explain why some coxibs increase the risk of cardiovascular deaths and in which patient population COX2 inhibitors should be avoided.

A

COX2 is present in endothelial cells and not platelets, shifting hemostatic balance to pro-coagulation. Platelets have COX1 btw.
COX2 inhibitors should be avoided when patients have, or are at risk of having, cardiovascular disease.

19
Q

Is paracetamol an NSAID?

A

It is a poor inhibitor of COx and is not anti-inflammatory, and is generally not considered to be an NSAID

20
Q

What occurs with a paracetamol overdose?

A

Liver toxicity

21
Q

What are the two major effects of glucocorticoids?

A

Anti-inflammatory
Immunosuppressant

22
Q

What is the mechanism of action for glucocorticoids?

A

Binds to receptors inside the cell to modify gene transcription.

23
Q

Do glucocorticoids affect upregulation or downregulation of genes?

A

Both

24
Q

Name three kinds of anti-rheumatoid drugs.

A

NSAIDs
Glucocorticoids
Disease modifying anti-rheumatic drugs (DMARDs)

25
Q

What class of anti-rheumatoid drug does methotrexate fall under and what is its mechanism of action?

A

Is a non-biological DMARD
Acts as a folate antagonist, inhibiting DNA synthesis

26
Q

How can biological DMARDs be made?

A

Monoclonal antibodies

27
Q

Briefly describe in 3 steps the process of making monoclonal antibodies.

A

An antigen with multiple is introduced to an immune system (ie mouse) and allowed to form B-cells capable of producing antibodies against it.
This B-cell is merged with an immortal myeloma, forming a hybridoma. It is capable of indefinitely providing monoclonal antibodies.

28
Q

Consider monoclonal antibodies taken developed from a non-human line. Describe briefly in 2 steps how it can be humanised.

A

The DNA encoding the V-regions of the antibody can be isolated and cloned.
They are then spliced into human antibody cDNA, and expressed in a new cell line.

29
Q

How do janus ( ͡° ͜ʖ ͡°) kinase inhibitors work (mechanism of action). What are drugs of this class referred to as?

A

Targets multiple cytokines at the cell signalling level. They are called jakinibs.

30
Q

How do NSAIDs act as analgaesics?

A

They target synergistic prostaglandins like PGE2, minimising their hyperalgaesic effect.