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Biology > Anti-inflammatories > Flashcards

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

A

Valine

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
Q

What is a suicide inhibitor

A

A drug that covalently binds to its target to cause a permanent inactivation of its target

26
Q

Side effects of NSAIDS

A

Gut issues, renal function issues, liver damage, bronchospasms and skin rashes

27
Q

advantages of drugs to target COX1

A

Beneficial for people at risks of strokes - antithrombotic

28
Q

What can inhibition of COX2 lead to

A

An increase in blood pressure and salt retention

29
Q

What does arthritis involve

A

Swelling around the synovium of the joints

30
Q

Symptoms of arthritis

A

pain, poor sleep, morning stiffness, swelling in affected joints

31
Q

How is the inflammatory response activated in arthritis

A

t cells activate macrophages which release mediators

32
Q

What are the two mediators involved in arthritis

A

Cytokines known as IL1 and TNF alpha

33
Q

Which drugs limit the inflammatory response in arthritis

A

Methotrexate folic acid and DIMARDS

34
Q

What does methotrexate do

A

Works as an antagonist for folic acid. It’s effective at low concentrations

35
Q

What do DIMARDS stand for

A

Disease modifying anti- rheumatoid drugs

36
Q

Examples of last resort drugs for arthritis

A

Cyclosporin’s and glucocorticoids

37
Q

How do cyclosporins work

A

Binds to calcanewin and inhibits the function of NF Kabba B, limiting the production of cytokines

38
Q

Example of glucocorticoid

A

Prednisolone

39
Q

How do glucocorticoids work

A

Work directly on the level of transcription by binding to the DNA. They act as repressors, inhbiting the genes that make cytockines

40
Q

Example of biopharmaceutical which treats arthritis

A

Adalmumab

41
Q

What does Adalmumab do

A

It recognises and binds to TNF alpha so it can no longer bind to its receptors

42
Q

Advantages and costs of Adalmumab

A

Its a single injection which lasts 3 months, has much lower side effects but is expensive

43
Q

Issues with biological drugs

A

They are expensive and have a limited pattern time

44
Q

Examples of inflammatory respiratory diseases

A

COPD and asthma

45
Q

What is COPD

A

A progressive disease driven by macrophages

46
Q

Symptoms of asthma

A

Shortness of breath, coughing and wheezing

47
Q

What does asthma involve

A

Inflammation of the airways and involves bronchial-hyper reactivity

48
Q

How to treat asthma

A

Avoid the allergen, give salbutamol, steroid drugs administered through an inhaler

49
Q

How does salbutamol work

A

Its an agonist for the beta adreno receptors found in smooth muscle airways. These receptors relax once activated

50
Q

Two phases of asthma

A

Early phase: mediated by mast cells secreting histamine
Late phase reactions: cytokines forcing an inappropriate inflammatory response to take place in the lungs

51
Q

What is asthma driven by

A

T cells

52
Q

What do steroid drugs do for asthma

A

Dampen down the production of cytokines and therefore control the response

53
Q

What are the unwanted side effects of steroid use

A

Crushing’s syndrome

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