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S2 Case 4 - Hypertension Monitoring > Beta Blockers > Flashcards

Beta Blockers Flashcards

1
Q

Which 2 types of NS does the peripheral NS utilise?

A

Cholinergic
Adrenergic

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2
Q

What does the cholinergic use?

A

Ach

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3
Q

What does adrenergic use?

A

Adrenaline + noradrenaline

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4
Q

What is adrenaline?

A

Hormone

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5
Q

What are noradrenaline + Ach?

A

Neurotransmitters

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6
Q

What are the 2 types of adrenoreceptors?
G-protein coupled receptors

A

Alpha - 1,2
Beta - 1,2,3

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7
Q

Describe beta receptor

A

7TM receptor
G protein linked to adenyl cyclase
= ATP to cAMP
Protein phosphorylation drives response

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8
Q

What are the structures of adrenaline + noradrenaline?

A

Small + simple molecules
Catechol ring
Alkylamine chain
Stereogenic centre

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9
Q

Describe the adrenergic binding sites

A

Pi-Pi stacking of Van der Waals
H bonding
Catechol H bonding
Hydrophobic interactions

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10
Q

What are the important binding groups?

A

OH
Ring
NHR2

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11
Q

Why should it be a R stereoisomer?

A

More reactive than S
= orientation different

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12
Q

What does it mean if the R2 is larger on the NH?

A

Larger = increased beta selectivity

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13
Q

What are molecules that won’t bind?

A

Tyramine = missing OH
Amphetamine = CH3 pushed NH2 too far out

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14
Q

What was pronethalol found to do?

A

Block beta receptors + partial agonist

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15
Q

Why was pronethalol withdrawn?

A

Toxicology concerns

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16
Q

Describe propranolol structure

A

Linking group
Dual benzene ring

17
Q

What are epoxides?

A

Strained 3-membered rings
Strong Nu under basic conditions

18
Q

What is epichlorohydrin?

A

“Special” epoxide for providing a 1,2,3-substituted compound

19
Q

What were the side effects of 1st generation beta blockers?

A

Crossed BBB = dizziness/sedation
Bronchoconstriction = asthmatics
Lowered CO

20
Q

What were the issues with propranolol?

A

High logP
= hydrophobic
= BBB penetration

21
Q

How to fix propranolol?

A

Reduce logP
= take out 1 aromatic ring

22
Q

What was the 2nd generation?

A

Practolol
= not as potent BUT more selective

23
Q

Why was practolol withdrawn?

A

Rashes, eye problems + peritonitis

24
Q

How were 2nd generation modified?

A

Contained extended para substituent

25
Q

How were short-acting beta blockers created?

A

Amides resistant to hydrolysis
So ester instead
= esmolol

26
Q

How were 3rd generation created?

A

Incorporate + extend amine substituent with proposal interact with another part of beta 1 receptor

27
Q

What are examples of 3rd generation?

A

Primidolol
Epanolol

28
Q

What are examples of 2nd generation?

A

Atenolol
Betaxolol

S2 Case 4 - Hypertension Monitoring (12 decks)

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