Lesson C1 - Drugs for the Treatment of Angina Pectoris & Congestive Heart Failure Flashcards

1
Q

what are the 3 major classes of antianginal drugs?

A

1) the organic nitrates which include the
short-acting nitroglycerin, and the long-acting isosorbide dinitrate; (2) the β-adrenergic
antagonists of which propranolol is a prototype drug; and (3) the calcium channel blockers of
which nifedipine is a prototype drug

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2
Q

Angina pectoris was first described by the English physician

A

William Heberden in 1768

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3
Q

Angina pectoris (a choking pain in the chest) is usually due to

A

lipid deposits in the coronary

arteries hindering blood flow (atherosclerosis).

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4
Q

The pain arises from

A

diminished blood flow and a diminished oxygen supply to an area of
the heart muscle.

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5
Q

To reduce the pain, one must

A

decrease the oxygen requirement of the heart

and/or increase the oxygen supply to oxygen deficient areas of the heart muscle

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6
Q

Angina pectoris is precipitated by the four “E’s”, namely

A

Eating, Exercise, Excitement, Exposure

to cold.

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7
Q

organic nitrates relax the smooth muscle of blood vessels and exert their
therapeutic effect by

A

Relaxation of large veins, leading to vasodilation and by Dilating large coronary arteries

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8
Q

Nitroglycerin enters blood vessels and is converted in blood vessels into nitric oxide.
Nitroglycerin therefore owes its effectiveness to its conversion into a normal body constituent,

A

nitric oxide.

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9
Q

In endothelial cells lining blood vessels, the enzyme nitric oxide synthase catalyses the
conversion of arginine into

A

citrulline and nitric oxide.

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10
Q

Nitric oxide passes from endothelial cells
into smooth muscle cells where it activates the enzyme guanylyl cyclase and leads through a
series of steps to

A

relaxation of the blood vessel

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11
Q

Therapeutic Uses of GTN

A

For termination of an individual attack, Prevention of individual attack and Chronic prophylaxis

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12
Q

An alternative drug used for chronic prophylaxis of angina pectoris is a

A

β-adrenergic blocking
agent. In order to understand the mechanism of action of β-adrenergic blocking drugs, such as
propranolol, in angina it is necessary to understand that angina is precipitated by factors that
increase sympathetic nervous system (SNS) activity, e.g. stress and exercise.

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13
Q

Increased SNS activity results in an increase in heart rate and an increase in myocardial (heart
muscle) contractility. This in turn leads to an increase in

A

cardiac output and an increase in

myocardial oxygen requirement resulting in the pain of angina.

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14
Q

A β-adrenergic blocking drug such as propranolol will block β receptors in the heart, thereby
decreasing heart rate and myocardial contractility. As a result, cardiac output and myocardial
oxygen requirements will

A

decrease and therefore the pain of angina will be alleviated.

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15
Q

Newer drugs or drugs in development, modify cardiac work load by

A

either slowing the heart

by altering electrical conduction or alter the metabolism of the heart to require less oxygen.

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16
Q

Calcium enters the vascular smooth muscle cell through a

A

Calcium enters the vascular smooth muscle cell through a

17
Q

Calcium enters the vascular smooth muscle cell through a

A

a calcium-calmodulin complex.

18
Q
Cardiac glycosides (digitalis) have a specific and powerful action on the myocardium (heart 
muscle). Digitalis binds specifically to an enzyme sodium, potassium-ATPase, and i
A

inhibits the
extrusion of sodium from cardiac cells. This leads to an increase of calcium in cardiac cells and
to a greater force of contraction of the heart.

19
Q

Therapeutic Uses of Digitalis

A

Congestive heart failure, Treatment of disordered electrical rhythms of the heart

20
Q

Adverse Effects of digitalis

A

Nausea and vomiting, Disordered rhythms in the heart (arrhythmia), Disturbances of vision – often blurred and neurological effects