Dugga 3 - cardiovascular

Question 1

What are risk factors for cardiovascular disease?

Answer 1

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

Question 2

Which are important targets for antihypertensive agents?

Answer 2

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

Question 3

What is aliskiren?

Answer 3

An approved renin inhibitor for treating hypertension

Question 4

How are most ACE inhibitors administered?

Answer 4

As prodrugs to lower their polarity and increase absorption

Question 5

What do all ACE inhibitor drugs contain?

Answer 5

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

Question 6

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

Answer 6

Two acidic groups and a hydrophobic substituent

Question 7

What are sartans?

Answer 7

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

Question 8

What are mineralocorticoid receptor antagnists?

Answer 8

They block the effects on aldosterine and have antihypertensive effects

Question 9

What are endothelins?

Answer 9

Endogenous peptides with potent vasoconstrictive properties

Question 10

Are endothelin antagonists hypertensive agents?

Answer 10

Yes

Question 11

What are vasodilators?

Answer 11

They relieve hypertension by dilating blood vessels and reducing blood pressure

Question 12

Which secondary messenger promotes dilation of blood vessels?

Answer 12

Cyclic GMP

Question 13

How can levels of cyclic GMP be increased?

Answer 13

By enhancing the activity of soluble guanylate cyclase

Question 14

How can levels of cyclic GMP be enhanced?

Answer 14

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

Question 15

What are calcium entry blockers?

Answer 15

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

Question 16

What are the 3 structural classes of calcium entry blockers?

Answer 16

Dihydropyridines, phenylalkylamines and benzothiazepines

Question 17

Where do calcium entry blockers bind?

Answer 17

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

Question 18

What are dihydropyridines mainly used for?

Answer 18

To treat hypertension

Question 19

What do dihydropyridines contain?

Answer 19

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

Question 20

What do the phenylalkylamines do?

Answer 20

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

Question 21

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

Answer 21

Diltiazem

Question 22

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

Answer 22

Ivabradine

Question 23

What are statins?

Answer 23

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

Question 24

Do all statins contain the same polar head group?

Answer 24

Yes, and then have differing hydrophobic groups attached

Question 25

What is the most important agent prescribed for lowering cholesterol?

Answer 25

Statins

Question 26

What does the polar head group of statins contain?

Answer 26

Two OH groups and one COOH group

Question 27

What do statins do?

Answer 27

Inhibit the enzyme important in biosynthesis of cholesterol

Question 28

What does the polar head group of statins do?

Answer 28

Mimicks the natural substrate for the target enzyme

Question 29

How do fibrates lower triglyceride levels?

Answer 29

By activating peroxisome proliferator activated alpha receptors in the liver

Question 30

What is mipomersen?

Answer 30

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

Question 31

How does lomitapide lower levels of cholesterol and triglycerides?

Answer 31

By inhibiting a triglyceride transfer protein

Question 32

What are antithrombotic agents?

Answer 32

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

Question 33

What can antithrombotic agents be classified as?

Answer 33

anticoagulent, antiplatelet agents and firbrinolytic agents

Question 34

What do anticoagulents do?

Answer 34

Inhibit the formation of thrombi

Question 35

What is thrombi?

Answer 35

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

Question 36

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

Answer 36

They bind to the enzyme thrombin and inhibit its action

Question 37

What are platelets?

Answer 37

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

Question 38

What is warfarin?

Answer 38

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

Question 39

What is dabigatran

Answer 39

A thrombin inhibitor

Question 40

What is idarucizumab?

Answer 40

a monoclonal antibody that reverses the effect of dabigatran

Question 41

What is a factor Xa inhibitor?

Answer 41

Anticoagulents that block the conversion of prothrombin to thrombin

Question 42

How do antiplatelate agents work?

Answer 42

They block platelet aggregation by binding as antagonists to platelet receptors

Question 43

What are fibrinolytic drugs?

Answer 43

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

Question 44

What is RAAS short for?

Answer 44

Renin Angiotensin Aldosterone System

Question 45

Where is renin formed?

Answer 45

In kidneys

Question 46

What does renin do?

Answer 46

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

Question 47

What does ACE do?

Answer 47

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

Question 48

What are sartans?

Answer 48

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

Question 49

Angiotensin 2 promotes the release of what?

Answer 49

Aldosterone which is a vasoconstrictor

Question 50

What do mineralocorticoid receptor antagonists do?

Answer 50

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