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Pharmacology > Enzyme inibitors > Flashcards

Enzyme inibitors Flashcards

1
Q

what are some important drug targets for inhibiting enzymes?

A

AchE, ACE, COX, DPP IV, MAO, PDE, XO

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2
Q

AchE

A

acetylcholine esterase

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3
Q

COX

A

cycloxygenase

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4
Q

DPP IV

A

dipeptidyl peptidase

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5
Q

MAO

A

monoamine oxidase

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6
Q

XO

A

xanthine oxidase

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7
Q

what does ACE do?

A

convert angiotensin I to angiotensin II

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8
Q

what are some examples of ACE inhibitors?

A

captopril, enalapril (prodrug)

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9
Q

what do all ACE inhibitors end in?

A

-pril

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10
Q

what are ACE inhibitors used in clinically?

A

heart failure and hypertension

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11
Q

angiotensin II is a potent

A

vasoconstrictor

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12
Q

what does catopril work on?

A

the binding site one angiotensin I

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13
Q

what does angiotensin II do?

A

increase sympathetic activity
increase tubular Na+ and Cl- reabsorption
promote release of aldosterone from gland on kidney
arteriolar vasoconstriction
increase ADH secretion from pituitary gland (increasing collecting ducts H2O absorption)

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14
Q

what does the prodrug enalapril originate from?

A

enalaprilat

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15
Q

what are the clinical uses for acetylcholine esterase inhibitors?

A

Myasthenia gravis, glaucoma,

Alzheimer’s disease

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16
Q

what is an example of AchE inhibitor?

A

Physostigmine

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17
Q

what are the clinical uses for COX enzyme inhibitors?

A

Acute/chronic inflammation,

oedema, swelling & fever

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18
Q

which class of drug inhibits COX enzymes?

A

NSAIDs

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19
Q

what are prostaglandins synthesised from?

A

arachidonic acid

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20
Q

what do COX enzymes do in the synthesis of prostaglandins?

A

cut arachadonate into cycloendoperoxides (prostaglandins G and H)

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21
Q

what are coxs more selective for?

A

COX2 enzymes

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22
Q

example of NSAIDs

A

ibuprofen, aspin, diclofenac, naproxin

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23
Q

what does TXA2 do?

A

thromboxane - platelets - vasoconstrictor, Gaq signalling, Promotes clotting and vasodilation

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24
Q

what does PGF2a do?

A

vasoconstrictor, Gaq signalling

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25
Q

what does PGD2 do?

A

works in smooth muscle, vasodilator, Gas signalling

26
Q

PGI2 - does?

A

vascular endothelium

- vasodilator, Gas signalling, increases pain sensitivity

27
Q

why do NSAIDs lead to GI bleeding?

A

Prostaglandins that are made in the stomach – inhibit the production of acid, protect the mucosa, protects the GI tract

28
Q

what are TX, PGI2, PGF2, PGD?

A

prostanoids

29
Q

which enzyme synthesises leukotrienes from arachondonate?

A

5-lipoxygenase

30
Q

what do leukotrienes do?

A

broncho-constricters - asthma

increase vascular complement

31
Q

example of COX-2 selective inhibiter?

A

rofecoxib

32
Q

which COX enzymes are expressed when?

A

COX1 – expressed at all times

COX2 - when there is pain and inflamation

33
Q

what is the clinical use for Xanthine Oxidase?

A

gout - formation of painful crystals of uric acid

34
Q

how does XO cause gout?

A

convert purines (aa’s) into uric acid - the painful crystals

35
Q

what drug inhibits xanthine oxidase?

A

allopurinol (and oxipurinol)

36
Q

how many distinct phosphodiesterase are there?

A

14

37
Q

what does PDE do?

A

inactivates the second messenger cAMP - breaks it down

38
Q

what are the 4 groups of PDEs?

A

non-specific, PDE III, PDE IV, PDE V

39
Q

examples of non specific PDE inhibitors?

A

caffeine and theophylline (asthma)

40
Q

examples of PDE III inhibitors?

A

arminone (CHF), cilostazol (intermittent claudication)

41
Q

examples of PDE IV inhibitors?

A

Apremilast (psoriasis)

Roflumilast (COPD

42
Q

examples of PDE V inhibitors?

A

sidenifil for erectile disfunction

43
Q

what does sexual stimulation cause the smooth muscle cells in the walls of the arteries to do? result?

A

relax

- more blood flows into the sinusoids and so volume increase - erect penis

44
Q

flaccid to erect penis

A
  • sexual stimulation
  • production of NO
  • activation of guanlyl cyclase
  • cGMP
  • relaxation of smooth muscle of corpus cavenosum
  • inc. blood flow
  • errection
45
Q

flaccid to erect penis

A
  • sexual stimulation
  • production of NO
  • activation of guanlyl cyclase
  • cGMP
  • relaxation of smooth muscle of corpus cavenosum
  • inc. blood flow
  • errection
46
Q

what are the clinical uses for monoamine oxidase inhibitors?

A

depression, anxiety, parkinson disease

47
Q

what does monoamine oxidase do?

A

responsible for removing the neurotransmitters norepinephrine, serotonin and dopamine from the neurone/brain.

48
Q

what do monoamine oxidases look like?

A

adreneline

49
Q

what is the cheese reaction?

A

when people are taking monoamine oxidase inhibitors and they eat cheese and have an adverse reaction

50
Q

where are the inactive metabolites formed by the monoamine oxidase get excreted?

A

in the urine

51
Q

MAO non specific inhibitor?

A

phenalzine

52
Q

MAOa inhibitor

A

moclobemide

53
Q

MAOb inhibitor

A

selegiline

54
Q

what dose dipeptidyl peptidase 4 do?

A

inactivates the incretin

55
Q

what do incretin hormones do?

A

lower blood glucose by increasing insulin secretion, suppressing glucagon and slowing gastric emptying

56
Q

what do DPP 4 inhibitors do?

A

prolong incretin activity and lower blood glucose levels

57
Q

what are the clinical uses for DPP4 inhibitors?

A

diabetes and obesity

58
Q

examples of incretin hormones?

A

GLP-1, GIT

59
Q

examples of DPP4 inhibitors

A

gliptins (block incretin breakdown) - sitagliptin, ildagliptin

60
Q

what does exenatide do?

A

GLP-1 mimetic - mimics the incretin that lower blood glucose

Pharmacology (18 decks)

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