Medicines for Cardiovascular Disease Flashcards

1
Q

What is intramolecular bonding

A

bonding within the same molecule including covalent bonding

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

what is intermolecular bonding

A

bonding between two neighbouring molecules non covalent

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

what type of bonding is involved in drug binding interaction

A

intermolecular

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

what are the main types of intermolecular bonding

A
Electrostatic 
Hydrogen bonding
Van der waals
Dipole - Dipole & ion dipole
Repuslion forces
Pi stacking
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

what is the lock and key hypothesis

A

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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

what is the induced fit model

A

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.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

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

A

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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

what do agonists do

A

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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

when making an agonist what do we need to consider

A

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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

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

A

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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

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

A

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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly