Drug Action And Binding Energies

Question 1

Give examples of drug targets

Answer 1

Lipids
Carbohydrates
Proteins
Nucleic acids

Question 2

Why are amides relatively inert chemically?

Answer 2

Because the N lone pair is delocalised into the carbonyl group

Question 3

What is physiological pH?

Answer 3

7.4

Question 4

Why are dipole-dipole interactions important at drug targets?

Answer 4

Because they attract the drug to the binding site, as well as orienting the molecule in the correct manner

Question 5

What are the most important drug interactions?

Answer 5

Reversible interactions

Question 6

What drives hydrophobic drug interactions?

Answer 6

An increase in entropy of the surrounding water, as the system becomes more disordered when two hydrophobic molecules interact - straying from the ordered water molecules solvating the two hydrophobic regions

This causes ∆G to become more negative as ∆G = ∆H - T∆S

Question 7

When are covalent bonds used for drug interactions?

Answer 7

Used in chemotherapy, and glaucoma - Dyflos, though only used when other drugs fail due to persistent drug action and side effects

Question 8

What is the MOA of penicillin?

Answer 8

Penicillin inhibits bacterial cell wall synthesis - transpeptidase - causing holes in the bacterial cell wall leading to content leakage and death

Penicillin is bactericidal

Question 9

What’re the desirable properties of penicillin?

Answer 9

Active against gram positive and some gram negative bacteria
Not toxic and very selective - among safest drugs found

Question 10

What’re the undesirable properties of penicillin?

Answer 10

Not active over a wide range (spectrum) of bacteria

Ineffective when taken orally

Sensitive to all known ß-lactamases