Medicines for Cardiovascular Disease

Question 1

What is intramolecular bonding

Answer 1

bonding within the same molecule including covalent bonding

Question 2

what is intermolecular bonding

Answer 2

bonding between two neighbouring molecules non covalent

Question 3

what type of bonding is involved in drug binding interaction

Answer 3

intermolecular

Question 4

what are the main types of intermolecular bonding

Answer 4

Electrostatic 
Hydrogen bonding
Van der waals
Dipole - Dipole & ion dipole
Repuslion forces
Pi stacking

Question 5

what is the lock and key hypothesis

Answer 5

rigid structure and the substrate + active site of enzyme are complementary in shape however does not explain multiple substrates

Question 6

what is the induced fit model

Answer 6

substrate and enzyme NOT complementary but similar in shape, as the substrate makes contact with the active site it undergoes a conformational change to become complementary to the substrate.

This change is driven by maximisation of intermolecular binding. Binding interaction must be strong enough to hold substrate but must allow release of products or neurotransmitter.

Question 7

what are the main structural requirements for selective binding ot the alpha 1 subunit of L type calcium channel for amlodipine

Answer 7

chloro group on the aromatic ring lock the ring perpendicular to dihydropyridine

worth noting that the terminal amino group is important for formulation and ionic interaction in membranes

protonation at physiological pH allows formulation as the maleate salt

Question 8

what do agonists do

Answer 8

mimic the natural messenger and need to bind to the receptor in such a way to activate it.

Question 9

when making an agonist what do we need to consider

Answer 9

drug must have correct binding groups
binding groups must be in the correct position
drug must be correct size for binding site

Question 10

why would we give a patient salbutamol to alieve the symptom of bronchospasm due to an overdose of atenolol

Answer 10

atentolol is a adrenergic receptor antagonist whilst salbutamol is a beta 2 receptor agonist.

bronchospasm due to excessive action from atenolol on beta 1 and 2 receptors, adding an agonist will return normal levels of activity

Question 11

why is atenolol an antagonist and salbutomal an agonist for the same receptor

Answer 11

agonists are smaller maximizing induced fit.

Similar placement of h bonding group but have same binding interactions but means that these are in a slightly different position for atenolol reducing induced fit

tert butyl group on salbutamol could be advantageous