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Файл:Ординатура / Хирургия / Библиотека им академика М.И. Перельмана / Книга_5282_Библиотеки_им_академика_М_И_Перельмана
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125
Drugs Acting on Cardiovascular System (CVS)
Quinapril
Structure:
H
N
O
O
N
O
O OH
Chemical name: (3S)-2-{[(2S)-1-ethoxy-1-oxo-4-phenylbutan-2-yl]-amino}-propanoyl]-
3,4-dihydro-1H-isoquinoline-3-carboxylic acid.
Uses: As an antihypertensive agent
Formulation: Tablet.
Brand name: Accupril.
Clonidine
Structure:
C
l
H
N
N
H
N
Cl
Chemical name: N-(2,6-Dichlorophenyl)-4,5-dihydro-1H-imidazol-2-amine.
Uses: As an antihypertensive agent.
Formulation: Tablet.
Brand names: Catapres, Kapvay and Nexiclon.
126
A Textbook of Pharmaceutical
Chemistry
Methyldopa
Structure:
HO
H
O
OH
O
H
2
N
Chemical name: (S)-2-amino-3-(3,4-dihydroxyphenyl)-2-methyl-propanoic acid.
Uses: As an antihypertensive agent and in gestational hypertension.
Formulations: Tablet and Injectable.
Brand names: Aldomet, Aldoril and Emdopa.
Nifedipine
Structure:
O
N
O
O
N
+
O
-
O
O
Chemical name: 3,5-Dimethyl-2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-
dicarboxylate.
Uses: As an antihypertensive agent, in Raynaud’s syndrome.
Formulations: Tablet and Topical.
Brand names: Adalat, Depin, and Depin-R.
127
Drugs Acting on Cardiovascular System (CVS)
Hydralazine
Structure:
N
N
HN
NH
2
Chemical name: 1-Hydrazinylphthalazine.
Uses: As an antihypertensive agent.
Formulation: Tablet.
Brand names: Nepresol and Apresoline
9.3 ANTIANGINAL AGENTS
Drugs used in the treatment of angina pectoris are called antianginal agents.
The word ‘angina’ (Greek word meaning to choke) is used to describe cardiac pain. Angina
is caused by the coronary artery constriction which prevents blood flow to cardiac muscles. It is
generally manifested by sudden, severe pain which radiates to the left shoulder.
It often occurs when the heart muscle itself needs more blood than it is getting, for example
during times of physical activity or strong emotions.
Types of Angina Pectoris
(a) Classical angina: This type of anginal attack occurs mainly due to physical exertion or
mental stress and hence it is also known as angina of efforts.
(b) Unstable angina: In this type, the prominent cause is atherosclerotic coronary artery
disease.
(c) Variant or Prinzmetal’s angina: This type of attack may be seen at rest, usually in the
morning. This is an example of an anginal attack seen in patients who are free from
atherosclerotic coronary stenosis.
Signs and Symptoms
Common symptoms reported by patients with angina include the following:
Retrosternal chest discomfort (pressure, heaviness, squeezing, burning, or choking
sensation) as opposed to frank pain.
Pain localized primarily in the epigastrium, back, neck, jaw, or shoulders.
128
A Textbook of Pharmaceutical
Chemistry
Pain precipitated by exertion, eating, exposure to cold or emotional stress lasting for
about 1-5 minutes and relieved by rest.
Pain intensity does not change with respiration, coughs, or changes in position.
Possible triggers of stable angina include:
Emotional stress
Exposure to very hot or cold temperatures
Smoking
Antianginal agents are classified as follows:
(a) Nitrates
(i) Short-acting nitrates
Glyceryl trinitrate (GTN)/nitroglycerine
Isosorbide dinitrate (sublingual)
(ii) Long-acting nitrates
Isosorbide dinitrate
Isosorbide mononitrate
(b) Potasium channel opener
Nicorandil
Isosorbide Dinitrate
Structure:
O
H
H
O
N
+
O
O
O
-
N
+
O
O
-
O
Chemical name: 1,4:3,6-Dianhydro-2,5-di-o-nitro-D-glucitol.
Uses: As an antianginal agent.
Formulation: Tablet.
Brand names: ISORDIL and DITRATE.
129
Drugs Acting on Cardiovascular System (CVS)
Nitroglycerine (GTN)
Structure:
N
O O O
O
N
O
O
N
O
O
Chemical name: Propane-1,2,3-triyl trinitrate.
Uses: As an antianginal agent.
Formulations: Tablet and Spray (Aerosol).
Brand names: Angised and Nitrolingual.
Amyl nitrite
Structure:
H
3
C
CH
3
O
N
O
Chemical name: (3-Methylbutyl)-nitrite/3-Methyl-1-nitrosooxybutane.
Uses: As an antianginal agent.
Formulation: Tablet.
Brand name: Vaporole.
General Information
130
Chapter
Diuretics
Diuretics are the drugs that promote diuresis, that is, increased production of urine. Diuretics
are very useful in treating hypertension, edema, fluid retention, etc.
The history of diuretics goes back a long way. It is believed that paleolithic man discovered
caffeine-containing plants. Beverages containing caffeine were prepared from the seeds and bark
of different plants. Xanthine derivatives and osmotic diuretics were also used due to their
clinically important diuretic effects before the emergence of modern diuretics.
Modern drugs initiate the diuresis by mobilization of the edema fluid. In diuresis, increased
urine is due to the increased excretion of Na
+
, H
+
, Cl
–
, HPO
4–
and Ca
++
ions. This may result in
hypokalemia, hyperglycemia, and hyperuricemia.
There are many pathological conditions that stress the need of using diuretics. Monitoring
the dosing schedule is necessary to avoid dehydration and electrolyte imbalance.
Diuretics are classified as follows:
(a) High ceiling diuretics (Loop diuretics)
This type of diuretics acts on the ascending limb of the loop of Henle of the nephron.
Furosemide
Bumatenide
Torasemide
(b) Thiazides (Calcium sparing diuretics)
This type of diuretics acts on the proximal-distal tubule of the nephron.
Chlorthalidone
Hydrochlorthiazide
Benzthiazide
10
131
Diuretics
Xipamide
Clopamide
Indapamide
(c) Potassium-sparing diuretics
(i) Aldosterone antagonist
Spironolactone
Eplerenone
(ii) Sodium channel inhibitors
Amiloride
Triamterene
(d) Carbonic anhydrase inhibitors
This type of diuretics inhibits the enzyme carbonic anhydrase.
Acetazolamide
(e) Osmotic diuretics
Isosorbide
Mannitol
Glycerol
Furosemide
Structure:
O
HO
S
O
H
2
N
O
Cl
NH
O
Chemical name: 4-Chloro-2-[(furan-2-ylmethyl)amino]-5-sulfamoylbenzoic acid.
Uses: As a diuretic agent.
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A Textbook of Pharmaceutical
Chemistry
Formulations: Tablet and Injectable.
Brand names: Lasix and Salinex.
Bumetanide
Structure:
O
H
O
H
2
NO
2
S
O
H
N
Chemical name: 3-Butylamino-4-phenoxy-5-sulfamoyl benzoic acid.
Uses: As a diuretic agent.
Formulations: Tablet and Injectable.
Brand names: Bumet and Bumex.
Acetazolamide
Structure:
H
N
N
N
SH
2
N
O
O
S
O
Chemical name: N-(5-sulfamoyl-1,3,4-thiadiazol-2-yl)acetamide
Uses: As a diuretic agent.
Formulations: Tablet and Capsule.
Brand names: Diamox and Synomax.
133
Diuretics
Xipamide
Structure:
OHCl
S
H
N
O
CH
3
H
3
C
O
O
NH
2
Chemical name: 4-chloro-N-(2,6-dimethylphenyl)-2-hydroxy-5-sulfamoylbenzamide
Uses: As a diuretic agent.
Formulation: Tablet.
Brand names: Xipamad and Aquaphor.
Spironolactone (Steroidal Diuretic)
Structure:
H
O
S
O
H
H
O
O
Chemical name: S-[(7R, 8R, 9S, 10R, 13S, 14S, 17R)-10, 13-Dimethl-3, 5’-dioxospiro [2, 6,
7, 8, 9, 11, 12, 14, 15, 16-decahydro-1H-cyclopenta[a]phenanthrene-17,2’-oxolane]-7-yl]-
ethanethioate.
Uses: As a diuretic agent.
Formulation: Tablet.
Brand names: Aldactone and Spiromide.
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A Textbook of Pharmaceutical
Chemistry
Benzthiazide
Structure:
O
SS
H
2
N
O
O
Cl N
S
NH
O
Chemical name: 6-Chloro-1, 1-dioxo-3-(phenylmethylsulfanylmethyl)-4H-benzo[e][1, 2,
4]thiadiazine-7-sulfonamide.
Uses: As a diuretic agent.
Formulations: Tablet and Capsule.
Brand names: Aquatag, Dihydrex and Diucen.
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