Beta-blockers

Question 1

What are the two adrenoreceptors???

Answer 1

Alpha and Beta

Question 1

What are the two adrenoreceptors???

Answer 1

Alpha and Beta

Question 2

What are Beta-blockers???

Answer 2

Drugs which prevent the stimulation of the adrenergic receptors. It’s responsible for cardiac action.

Question 3

What are examples of the first generation of beta-blockers???

Answer 3

Propanolol
Isoprinosine
Dichloroisoprenaline
Pronethalol

Question 4

What are examples of the second generation of beta-blockers???

Answer 4

Practolol

Question 5

What is the structure-activity relationship of Aryloxypropanolamines?

Answer 5

The O bond is involved in H bonding to the receptor.
The NH bond is an essential ionic bonding interaction.
The OH bond is an essential H bonding interaction.
Last branch fits hydrophobic pocket.

Question 6

What are the side effects of the synthesis of propranolol?

Answer 6

Fatigue and tiredness owing to reduced cardiac output.
Bronchoconstriction.
CNS effects owing to lipophilicity.
Coldness in extremities.
Heart failure for those on the verge of heart attack.

Question 7

What are the observations of the synthesis of Propranolol?

Answer 7

Variation of the aromatic ring system and heteroaromatic rings is possible.
Substitution of the side-chain methylene increases metabolic stability but lowers activity.
Alcohol group is essential for activity.
Replacing oxygen with S, CH2 or NMe has a detrimental effect.
N-Alkyl substituents longer than isopropyl or t-butyl are less effective.