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302 - Content > CVD Drugs - Chemistry > Flashcards

CVD Drugs - Chemistry Flashcards

1
Q

What converts angiotensinogen in angiotensin I

~ antihypertensives

A

Renin

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2
Q

What converts angiotensin I to angiotensin II?

A

ACE (angiotensin converting enzyme)

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3
Q

What are the effects of angiotensin II?

A

• vasoconstriction
• activation of sympathetic nervous system
• ADH release from posterior pituitary to increase water absorption
• aldosterone secretion - promotes reaborbtion of Na and water. Promoting K secretion

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4
Q

Which drug classes target RAAS and give examples

A

ACEI - Ramipril
Renin inhibitors - Aliskiren
Angiotensin receptor blockers - Lostran
Aldosterone inhibitors - Spiractalone & Elerenone

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5
Q

Angiotensin promotes the release of aldosterone. Why does the release of aldosterone cause an increase in BP

A

Aldosterone promotes the reabsortbtion of fluid in kidneys, increasing blood volume, thus increasing BP

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6
Q

Which reaction occurs to convert angiotensin I to angiotensin II

A

ACE catalysis hydrolysis of the linkage peptide

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7
Q

ARBs bind to which receptors and which areas are they’re receptors located

A

They bind (block) to AT1 receptors found in the heart, kidneys and blood vessels

They are antagonist or inverse agonist

Prevent angiotensin II from binding to AT1

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8
Q

Lostran is a PRO drug, how it is metabolised?

Hydrolysis, reduction or oxidation

A

Oxidation

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9
Q

Regarding RAAS, which is a hormone potent in vasoconstriction

A

Angiotensin II

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10
Q

What are the main 2 target and enzymes (in RAAS) for antihypertensive agents

A

Renin and ACE

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11
Q

Which drug class inhibits angiotensin I synthesis

A

Renin inhibitors - aliskren

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12
Q

ACEI are products to decrease and increase what?

A

Decrease polarity
Increase absorption

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13
Q

Do antihypertensives block the action of endogenous or exdogenous hormones with vasoconstriction properties?

A

Endogenous hormones

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14
Q

Beta blockers

A
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15
Q

BB act on b1 adrenoreceptors, where are they main located

A

Heart

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16
Q

B1 adrenoreceptors are…

A

• found in the heart
• G-coupled protein receptors

17
Q

What happens when b1 adrenoreceptors are activated

A

Cardiac muscle contraction

18
Q

BB act on the heart to…

A

Reduce cardiac output

19
Q

BB act on the CNS to….

A

Decrease activity of the sympathetic nervous system

20
Q

BB act on the kidneys to…

A

Decrease renin release

21
Q

Give an example of a 1st gen beta blocker and their selectivity?

A

Propranolol (aka aryloxypropanolamine)
Non selective - act on both b1 and b2

22
Q

Give an example of a 2st gen beta blocker and their selectivity?

A

Bisporolol
B1 selective - cardio selective

23
Q

Why should propranolol not be given in asthmatics

A

It blocks b2 adrenoreceptors in lungs, constricting airways

24
Q

Vasodilators

A
25
Q

What is cyclic GMP

A

Secondary messenger

26
Q

cGMP is converted into GMP via

A

PDE5

27
Q

What is an example of a PDE5 inhibitor

A

Slidinafil - vasodilator in the penis

28
Q

Levels of cGMP can be increased by

A

PDE5 inhibitors - increases half life of cGMP and this action of vasodilation

29
Q

CCBs

A
30
Q

Which subunit do CCB bind to ?

A

a1 subunit

31
Q

What are the 3 classes of CCB

A

• dihydropyradines
• benzothiazepines
• phenylalkylamines

32
Q

All these classes of drug bind to different areas of the a1 subunit, but are very close - making them allosterically linked. What does allosterically linked mean?

A

When one drug bind, it will affect the bind of another near by drug

33
Q

Are dihydropyradines hydrophilic or hydrophobic

A

Hydrophobic

34
Q

Statins

A
35
Q

What is the role of NDAP?

A

Reducing agent

36
Q

Give an example of type 1 and type 2 statin

A

Type 1 - simvastatin

Type 2 - Atorvastatin, rosuvastatin, fluvastatin

37
Q

From type 1 or type 2, which has the most ADRs

A

Type 1

38
Q

Which type is harder to synthesis

A

Type 1 - due to the number of chiral circles

302 - Content (44 decks)

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