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Medicinal chemistry > Dugga 3 - cardiovascular > Flashcards

Dugga 3 - cardiovascular Flashcards

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1
Q

What are risk factors for cardiovascular disease?

A

Hypertension (high blood pressure), obesity, smoking, diabetes and lack of exercise

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2
Q

Which are important targets for antihypertensive agents?

A

Renin and angiotensin coverting enzyme (ACE) are key enzymes in the RAAS cascade

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3
Q

What is aliskiren?

A

An approved renin inhibitor for treating hypertension

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4
Q

How are most ACE inhibitors administered?

A

As prodrugs to lower their polarity and increase absorption

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5
Q

What do all ACE inhibitor drugs contain?

A

A functional group that binds to the zinc ion cofactor of ACE

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6
Q

What are important binding groups for sartans, and important for activity?

A

Two acidic groups and a hydrophobic substituent

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7
Q

What are sartans?

A

Antihypertensive agents that act on the AT1 receptor as either antagonists or inverse agonists

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8
Q

What are mineralocorticoid receptor antagnists?

A

They block the effects on aldosterine and have antihypertensive effects

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9
Q

What are endothelins?

A

Endogenous peptides with potent vasoconstrictive properties

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10
Q

Are endothelin antagonists hypertensive agents?

A

Yes

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11
Q

What are vasodilators?

A

They relieve hypertension by dilating blood vessels and reducing blood pressure

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12
Q

Which secondary messenger promotes dilation of blood vessels?

A

Cyclic GMP

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13
Q

How can levels of cyclic GMP be increased?

A

By enhancing the activity of soluble guanylate cyclase

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14
Q

How can levels of cyclic GMP be enhanced?

A

By inhibiting phosphodiester type 5 (PDE5) which catalyses the hydrolysis of cyclic GMP

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15
Q

What are calcium entry blockers?

A

Drugs that block voltage gated L type calcium ion channels used to treat hypertension and angina

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16
Q

What are the 3 structural classes of calcium entry blockers?

A

Dihydropyridines, phenylalkylamines and benzothiazepines

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17
Q

Where do calcium entry blockers bind?

A

To distinct binding sites in the alpha 1 subunit of calcium ion channel

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18
Q

What are dihydropyridines mainly used for?

A

To treat hypertension

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19
Q

What do dihydropyridines contain?

A

Five substituents including an aromatic ring and two ester groups. The nitrogen is unsubstituted.

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20
Q

What do the phenylalkylamines do?

A

Bind to calcium ion channel by approaching from the intracellular side of the ion channel. They must cross cell membrane to be effective

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21
Q

What is the name of the only benzothiazepine approved for the clinic?

A

Diltiazem

22
Q

What inhibits the funny ion channel and is approved for treatment of angina?

A

Ivabradine

23
Q

What are statins?

A

Cholesterol lowering agents that block the enzyme involved in the rate-limiting step of cholesterol biosynthesis

24
Q

Do all statins contain the same polar head group?

A

Yes, and then have differing hydrophobic groups attached

25
Q

What is the most important agent prescribed for lowering cholesterol?

A

Statins

26
Q

What does the polar head group of statins contain?

A

Two OH groups and one COOH group

27
Q

What do statins do?

A

Inhibit the enzyme important in biosynthesis of cholesterol

28
Q

What does the polar head group of statins do?

A

Mimicks the natural substrate for the target enzyme

29
Q

How do fibrates lower triglyceride levels?

A

By activating peroxisome proliferator activated alpha receptors in the liver

30
Q

What is mipomersen?

A

An antisense drug that inhibits the translation of apolilpoprotein B, a key component of low density lipoprotein particles

31
Q

How does lomitapide lower levels of cholesterol and triglycerides?

A

By inhibiting a triglyceride transfer protein

32
Q

What are antithrombotic agents?

A

They help to prevent blood clots in the circulatory system to reduce the risk of heart attack and stroke

33
Q

What can antithrombotic agents be classified as?

A

anticoagulent, antiplatelet agents and firbrinolytic agents

34
Q

What do anticoagulents do?

A

Inhibit the formation of thrombi

35
Q

What is thrombi?

A

a blood clot formed in situ within the vascular system of the body and impeding blood flow

36
Q

What are heparins, hirudin and parins and what do they do to the enzyme thrombin?

A

They bind to the enzyme thrombin and inhibit its action

37
Q

What are platelets?

A

Platelets, or thrombocytes, are small, colorless cell fragments in our blood that form clots and stop or prevent bleeding

38
Q

What is warfarin?

A

An oral anticoagulent that inhibits vitamin K epoxide reductase (but low therapeutic window and drug-drug interaction)

39
Q

What is dabigatran

A

A thrombin inhibitor

40
Q

What is idarucizumab?

A

a monoclonal antibody that reverses the effect of dabigatran

41
Q

What is a factor Xa inhibitor?

A

Anticoagulents that block the conversion of prothrombin to thrombin

42
Q

How do antiplatelate agents work?

A

They block platelet aggregation by binding as antagonists to platelet receptors

43
Q

What are fibrinolytic drugs?

A

Enzymes which convert plasminogen to plasmin. Plasmin catalyses the degradation of fibrin leading to the breakdown of thrombus

44
Q

What is RAAS short for?

A

Renin Angiotensin Aldosterone System

45
Q

Where is renin formed?

A

In kidneys

46
Q

What does renin do?

A

catalyses formation of angiotensin 1 which indirectly affects vasoconstriction (vessels becoming narrow)

47
Q

What does ACE do?

A

Converts angiotensin 1 to angiotensin 2
Drugs that act on this are called -prilat or -prill

48
Q

What are sartans?

A

Selective AT1 antagonists bind the receptor AT1 which is responsible for vasoconstriction

49
Q

Angiotensin 2 promotes the release of what?

A

Aldosterone which is a vasoconstrictor

50
Q

What do mineralocorticoid receptor antagonists do?

A

Bind the receptor that aldosterone would have bound and promoted vasoconstriction. Now there will be no constriction

51
Q
A

Medicinal chemistry (10 decks)

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