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Pharamacology > Drug enzyme targets > Flashcards

Drug enzyme targets Flashcards

1
Q

What are the 3 types of AChE inhibitors (anti-cholinesterases)?

A

short-acting
medium duration
irreversible

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2
Q

Give an example of a short-acting AChE inhibitor?

A

Edrophonium

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3
Q

What is edrophonium used for?

A

diagnostic test for myasthenia gravis

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4
Q

What is Myasthenia Gravis?

A

body’s own immune system destroys ACh receptors on cells, resulting in muscle weakness

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5
Q

Give 3 examples of medium duration anticholinesterases?

A

Pyridostigmine
Neostigmine
Physostigmine

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6
Q

What are 2 advantages of pyridostigmine over Neostigmine?

A
  • Better absorbed

- Longer lasting

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7
Q

What is Pyridostigmine used for?

A

treatment for Myasthenia Gravis

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8
Q

What is Physostigmine used for ?

A

used in eye drops to treat glaucoma

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9
Q

Give 2 examples of irreversible anticholinesterases?

A

Dyflos and Ecothiophate

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10
Q

What are the 2 most common ACE inhibitors?

A

Enalaprilat

Captopril

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11
Q

How is Enalaprilat a prodrug?

A

Converted from Enalapril in the liver to Enalaprilat

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12
Q

What is the function of Angiotensin II?

A

Potent vasoconstrictor

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13
Q

What are the clinical uses of ACE inhibitors?

A

Hypertension

Congestive Heart failure

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14
Q

What is the common drug group used to target the COX-1 and COX-2 enzymes?

A

NSAIDs

Non Steroidal Anti-Inflammatory Drugs

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15
Q

How do NSAIDs exhibit their anti-inflammatory effect?

A

Decrease prostaglandin E2 and Prostacyclin production which reduced vasodilation

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16
Q

How do NSAIDs exhibit their anti-pyretic effect?

A

Prevent IL-1 releasing prostaglandins in CNS that increase the hypothalamic set point for temperature

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17
Q

What sort of pain are NSAIDs ideal for managing?

A

Inflammation and tissue damage

18
Q

How do NSAIDs exhibit their analgesic effect?

A

decrease the production of prostaglandins that sensitise nociceptors

19
Q

what are nociceptors?

A

sensory neurones that respond to damaging stimuli

20
Q

What are some of the unwanted effects of NSAIDs?

A

GI disturbances
skin reactions
CV side effects

21
Q

Give an example of an unwanted side effect of a NSAID

A

Aspirin- anti platelet action

other NSAIDs don’t

22
Q

How do DPP IV inhibitors work?

A

prevent the DPP IV enzyme breaking down incretins, thereby increasing incretin levels and lowering blood glucose

23
Q

In what 2 ways do DPP IV inhibitors lower blood glucose?

A

Inhibit glucagon release

Trigger insulin release

24
Q

Give 2 examples of DPP IV inhibitors?

A

Sitagliptin

Ildagliptin

25
Q

What are the clinical uses for DPP IV inhibitors?

A

Obesity

Diabetes

26
Q

What are the 3 main examples of irreversible MAO inhibitors?

A

Phenelzine
Tranylcypromine
Iproniazid

27
Q

Which molecular form of MAO is the preferred target for MAO inhibitors?

A

MAO-A

28
Q

What does MAO-A have a substrate preference for?

A

serotonin (5-HT)

29
Q

What does MAO-B have a substrate preference for?

A

Dopamine and phenylethylamine

30
Q

What drug selectively inhibits MAO-B preventing the breakdown of dopamine?

A

selegiline (used to treat Parkinsons)

31
Q

What are the clinical uses of MAO inhibitors?

A

Depression and Anxiety

32
Q

Give 2 examples of PDE V inhibtors?

A

Sildenafil (viagra)

Tadalafil (longer acting)

33
Q

How is PDE V used to treat Erectile dysfunction?

A

prevents the cGMP being converted to an inactive product

Instead it activates protein kinase G resulting in vasodilation and improved blood flow

34
Q

What other clinical use can PDE V inhibitors be applied to?

A

Pulmonary Hypertension

35
Q

Give an example of an XO inhibitor?

A

Allopurinol

36
Q

How does Allopurinol decrease uric acid synthesis?

A

Converted to Alloxanthine (by XO)

Which is a non- competitive inhibitor of XO (remains in tissues for long time)

37
Q

What is the clinical use of XO inhibitors?

A

Gout

38
Q

What is Gout?

A

a metabolic disease that causes urate crystals to be deposited into tissues

39
Q

What is chloroquine?

A

Anti-malarial Haem Polymerase Inhibitor

40
Q

What does Haem Polymerase do?

A

converts FP IX to non-toxic haemozoin

41
Q

in what 2 ways do haem polymerase inhibitors cause toxicity?

A
  1. Cause build up of FP IX

2. Form chloroquine-haem complexes that generate free radicals

Pharamacology (7 decks)

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