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Pharmacology > Enzymes as drug targets > Flashcards

Enzymes as drug targets Flashcards

1
Q

Example and use of ACE inhibitors

A

Captopril, rampiril in high BP, HF and chronic renal insufficiency

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2
Q

What is Km?

A

Substrate conc where reaction rate reaches half of Vmax

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3
Q

Competitive inhibitor?

A

Competes with substrate for active site

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4
Q

Reversible inhibitor

A

Overcome by increase in substrate, Km up but Vmax same

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5
Q

Irreversible inhibitor

A

Covalent binding, renders active site unusable, decreases Vmax

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6
Q

Example of irreversible inhibitor

A

Selegiline, irreversible inhibitor of MAO B

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7
Q

What does a false substrate do plus example?

A

Produces false transmitter, alpha methyl dopa

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8
Q

Example of pro drug

A

L-DOPA in Parkinson’s

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9
Q

Drugs acting on Ach

A

Neostigmine and echothiopate

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10
Q

Drug that acts on Choline acetyl transferase

A

Hemicholinum (f5)

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11
Q

Drug acting on bacteirial transpeptidases

A

Penicillin

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12
Q

Drug acting on Xanthine Oxidase

A

Allopurinol

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13
Q

Drugs acting on MAO

A

Selegiline, ipronazid

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14
Q

Drug acting on dihydrofolate synthase

A

Sulphonamides

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15
Q

Drugs acting on dihydrofolate reductase

A

Methotrexate

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16
Q

Drugs acting on dopa decarboxylase

A

Carbidopa, alpha methyl dopa

17
Q

Drugs acting on reverse transcriptase

A

Zidovudine

18
Q

Drugs acting on thymidine kinase

A

Aciclovir

19
Q

How does Cox 1 work

A

Constitutive, concerts arachidonate to cyclic endoperoxidases -> prostanoids inc thromboxane and prostaglandin

20
Q

How does cox 2 work

A

Inducible by injury or inflammation

21
Q

What do NSAIDs inhibit

A

Cox 1 and 2, lasts until new enzyme synthesised

22
Q

How do sulphonamides work?

A

Compete with PABA for uptake in bacteria, prevent DNA synthesis by inhibiting dihydrofolate synthase

23
Q

Example and use of HMG CoA reductase inhibitor

A

Pravastatin in hypercholesterolaemia

Pharmacology (4 decks)

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