Anti-inflammatories Flashcards

1
Q

What do NSAIDS stand for

A

Non-steroidal anti-inflammatory drugs

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2
Q

What did Felix Hoffmann add to salicylic acid to improve its properties

A

An acetyl group

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3
Q

What was one of the first synthetic drugs created

A

Aspirin

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4
Q

Benefits of aspirin

A

Less gut effects

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5
Q

Examples of NSAIDS

A

Aspirin, Paracetamol, Ibuprofen

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6
Q

What do NSAIDS target

A

Prostaglandins and thromboxane’s

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7
Q

What do Phospholipase a2 generate

A

The precursors required for the synthesis of everything else (arachidonate)

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8
Q

What is arachidonate converted into

A

Other mediators by cyclo-oxygenase

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9
Q

What is PGF important for

A

Initiation of labour

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10
Q

What is PDG needed for

A

Platelet aggregation

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11
Q

What is PGE needed for

A

Blood vessel relaxation (Hyperalgesia)

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12
Q

What do prostaglandins attract

A

Immune cells known as chemo attractants

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13
Q

What are NSAIDS

A

Anti-inflammatory, analgesic anti-pyretic

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14
Q

What does analgesic mean

A

Decreases pain

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15
Q

What does anti-pyretic mean

A

Lowers raised temperature

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16
Q

What is the COX1 enzyme responsible for

A

Constant constitutive synthesis of prostaglandins, has many homeostatic functions for maintaining health

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17
Q

What is COX2 responsible for

A

It’s an inducible enzyme in response to inflammation

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18
Q

Where is COX3 found

A

In the brain and kidneys

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19
Q

What is COX made of

A

Two identical subunits

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20
Q

What’s the difference between COX1 and COX2

A

The structure of the little pore where the arachidonic acid has to go up is smaller in COX2

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21
Q

Which amino acid does COX1 have

A

Isoleucine

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22
Q

Which amino acid does COX2 have

23
Q

Why does aspirin cause GI issues

A

Because prostaglandins maintain the mucus layer surrounding the stomach

24
Q

What do prostaglandins maintain

A

Blood flow in the kidneys

25
What is a suicide inhibitor
A drug that covalently binds to its target to cause a permanent inactivation of its target
26
Side effects of NSAIDS
Gut issues, renal function issues, liver damage, bronchospasms and skin rashes
27
advantages of drugs to target COX1
Beneficial for people at risks of strokes - antithrombotic
28
What can inhibition of COX2 lead to
An increase in blood pressure and salt retention
29
What does arthritis involve
Swelling around the synovium of the joints
30
Symptoms of arthritis
pain, poor sleep, morning stiffness, swelling in affected joints
31
How is the inflammatory response activated in arthritis
t cells activate macrophages which release mediators
32
What are the two mediators involved in arthritis
Cytokines known as IL1 and TNF alpha
33
Which drugs limit the inflammatory response in arthritis
Methotrexate folic acid and DIMARDS
34
What does methotrexate do
Works as an antagonist for folic acid. It's effective at low concentrations
35
What do DIMARDS stand for
Disease modifying anti- rheumatoid drugs
36
Examples of last resort drugs for arthritis
Cyclosporin's and glucocorticoids
37
How do cyclosporins work
Binds to calcanewin and inhibits the function of NF Kabba B, limiting the production of cytokines
38
Example of glucocorticoid
Prednisolone
39
How do glucocorticoids work
Work directly on the level of transcription by binding to the DNA. They act as repressors, inhbiting the genes that make cytockines
40
Example of biopharmaceutical which treats arthritis
Adalmumab
41
What does Adalmumab do
It recognises and binds to TNF alpha so it can no longer bind to its receptors
42
Advantages and costs of Adalmumab
Its a single injection which lasts 3 months, has much lower side effects but is expensive
43
Issues with biological drugs
They are expensive and have a limited pattern time
44
Examples of inflammatory respiratory diseases
COPD and asthma
45
What is COPD
A progressive disease driven by macrophages
46
Symptoms of asthma
Shortness of breath, coughing and wheezing
47
What does asthma involve
Inflammation of the airways and involves bronchial-hyper reactivity
48
How to treat asthma
Avoid the allergen, give salbutamol, steroid drugs administered through an inhaler
49
How does salbutamol work
Its an agonist for the beta adreno receptors found in smooth muscle airways. These receptors relax once activated
50
Two phases of asthma
Early phase: mediated by mast cells secreting histamine Late phase reactions: cytokines forcing an inappropriate inflammatory response to take place in the lungs
51
What is asthma driven by
T cells
52
What do steroid drugs do for asthma
Dampen down the production of cytokines and therefore control the response
53
What are the unwanted side effects of steroid use
Crushing's syndrome