1. DRUGS AFFECTING THE
CARDIOVASCULAR SYSTEM
Lec. No. 10

2. Cardiovascular agents
affect the action of the
circulatory system.
Most of these agents are
highly specialized.

3. 1-Antihypertensive drugs
 A. Diuretics
a) Thiazide diuretics: initial therapy in most cases,
used in mild to moderate hypertension.
b) Loop diuretics: in sever and resistant hypertension
and hypertension of renal failure.
c) K-sparing diuretics: in hyperaldosteronism.
 B. Beta blockers
Nonselective: propranolol, timolol, pindolol.
Cardio selective (β1 selective): atenolol, esmolol,
metoprolol

4.  C. Calcium channel blockers (CCBs)
a) More selective on heart: Verapamil & Diltiazem
b) More selective on blood vessels: Nifedipine
 D. Drugs affecting angiotensin system
1. Angiotensin converting enzyme inhibitors
(ACE Is):
 E.g.: Captopril, Alcepril, Enalapril, Lisinopril
2. Angiotensin-1 receptors antagonists (AT-1
antagonists):
 E.g.: Saralasin, Losartan

5. ACE-i. Mechanism of Action
VASOCONSTRICTION
ALDOSTERONE
VASOPRESSIN
SYMPATHETIC
VASODILATATION
PROSTAGLANDINS
Kininogen
tPA
Kallikrein
Angiotensinogen
RENIN
Angiotensin I
A.C.E.
ANGIOTENSIN II
Inhibitor
BRADYKININ
Kininase II
Inactive Fragments

6. Angiotensin II Receptor Blockers (ARB)
RENIN
Angiotensinogen
Other pathways
AT1
Receptor
Blockers
AT1
Vasoconstriction
Angiotensin I
ACE
ANGIOTENSIN II
RECEPTORS
Proliferative
Action
AT2
Vasodilatation
Antiproliferative
Action

7.  E. Direct acting vasodilators
Nitroprosside
Minoxidil
Hydralazine
Diazoxide

8.  F. α1 adrenergic blockers:
eg. Prazosin HCl
 Angina
 Heart failure
 Diabetes

9. Possible combinations between some classes of antihypertensive
drugs
Thiazide diuretics
β-blockers
Angiotensin
receptor
antagonists
α- blockers
Calcium
antagonists
ACE inhibitors
The preferred combinations in the general hypertensive population are represented as thick lines.
The frames indicate classes of agents proven to be beneficial in controlled intervention trials

10. These include:
 hypertensive encephalopathy,
 cerebral stroke,
 severe renal failure.
Patient should be hospitalized and reduction of blood
pressure should be in hours and not in minutes.
Drugs that can be used:

11. 1. Sublingual nifedipine or captopril
2. Parentral therapy
Diuretics (furosemide, bumetanide) I.V.
Diazoxid 300 mg I.V. very rapidly.
Nitroprusside infusion 2-5mcg/kg/min.
according to blood pressure.
Beta blocker (propranolol) l-2mg I.V. slowly
diluted
Nefedipine I.V. diluted


12. 2- Drugs used in the treatment of
congestive heart failure (CHF)
Cardiac glycosides
a- Calcium channel blockers e.g amlodipine
b- Angiotensin converting enzyme inhibitors
e.g.:(Captopril, enalapril )
c- Other vasodilators e.g.:(hydralazine, nitroprusside)

13.  Cardiac Glycoside
 Digitoxin
 Digoxin(lanoxin)

14. 3- Drugs used in the treatment of
Arrhythmia
Impulse formation,
impulse conduction,
or a combination

15. Quinidine. Lidocaine (I.V)
Propranolol, Atenolol, Sotalol
Amiodarone, Bretylium
Verapamil, Diltiazem.
Adenosine, Digoxin, Atropine, Adrenalin &
Isoprenaline

16. 4- Drugs used in treatment of
Angina:
is an acute chest pain that
occurs when
blood flow
is
to supply
the oxygen required by
the heart.

17.  Short acting Nitrates:
1. Glyceryl Trinitrate (Nitroglycerin)
[sublingual /I.V /infusion]
2. Amyl nitrite [inhalation]
3. Isosorbide dinitrate [sublingual]

18. 1. Long acting Nitrates
Isosorbide mononitrate, Isosorbide dinitrate
[oral]
2. Beta adrenergic blockers
3. Calcium channel blockers
4. Antiplatelets
(aspirin, dipyridamol):
used to ↓↓ incidence of coronary
thrombosis.

19. Tolerance for the vasodilating action
may develop
with continuous exposure to Nitrates
without interruption.

20. 5- Drugs used in the treatment of hyperlipidemia
is a condition of high levels
of
,

21. prevent cholesterol synthesis
or
promote the breakdown of internal
cholesterol.

22. e.g. cholestyramine, colestipol
e.g. lovastatin, simvastatin
e.g. gemfibrozil, clofibrate

23. 6- Thrombolytic drugs
e.g.: Streptokinase

24. 7- Anticoagulants
.
Heparin
Warfarin (Caumadin®)