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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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115
Drugs Acting on Cardiovascular System (CVS)
Lidocaine (Xylocaine)
Structure:
H
N
N
CH
3
CH
3
CH
3
CH
3
O
HCl
Chemical name: 2-(Diethylamino)-N-(2,6-dimethylphenyl)-acetamide.
Uses: In the treatment of ventricular tachycardia.
Formulation: Injectable.
Brand names: Xylocard and Gesicard.
Mexiletine
Structure:
O
NH
2
Chemical name: 2-(2-Aminopropoxy)-1,3-dimethylbenzene.
Uses: As an anti-arrhythmic agent.
Formulations: Capsule and Injectables.
Brand name: Mexitil.
Sotalol
Structure:
H
N
N
H
S
H
3
C
O
O
OH
Chemical name: (RS)-N-{4-[1-hydroxy-2-(propan-2-ylamino)-ethyl]-phenyl}-
methanesulfonamide.
Uses: As an anti-arrhythmic agent.
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A Textbook of Pharmaceutical
Chemistry
Formulation: Tablet.
Brand names: Betapace and Sotagard.
Amiodarone
Structure:
I
I
O
N
O
O
Chemical name: (2-{4-[(2-butyl-1-benzofuran-3-yl)-carbonyl]-2,6-diiodophenoxy}ethyl)-
diethylamine.
Uses: To treat ventricular tachycardia, atrial, and ventricular fibrillation.
Formulations: Tablet and Injectables.
Brand names: Nexterone, Aldarone and Eurythmic.
Verapamil
Structure:
N
N
O
O
O
O
Chemical name: (RS)-2-(3,4-Dimethoxyphenyl)-5-{[2-(3,4-dimethoxyphenyl)-ethyl]-
(methyl)amino}-2-prop-2-ylpentanenitrile.
Uses: In the treatment of atrial flutter, hypertension, cardiac arrhythmia, angina pectoris, etc.
Formulations: Tablet and injectables.
Brand name: Calaptin.
117
Drugs Acting on Cardiovascular System (CVS)
Diltiazem
Structure:
O
O
O
O
S
N
N
Chemical name: Cis-(+)-[2-(2-Dimethylaminoethyl)-5-(4-methoxyphenyl)-3-oxo-6-thia-2-
azabicyclo-[5.4.0]-undeca-7,9,11-trien-4yl]-ethanoate.
Uses: In the treatment of atrial flutter, hypertension, cardiac arrhythmia, angina pectoris, etc.
Formulations: Tablet and Injectables.
Brand names: Dilzem and Cardizem.
Lorcainide
Structure:
N
ON
Cl
Chemical name: N-(4-Chlorophenyl)-N-(1-isopropylpiperidin-4-yl)-2-phenyl-acetamide.
Uses: As an anti-arrhythmic agent.
Formulation: Tablet.
Brand name: Remivox.
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A Textbook of Pharmaceutical
Chemistry
Tocainide
Structure:
H
N
NH
2
O
Chemical name: N-(2,6-Dimethylphenyl)-alaninamide.
Uses: As an anti-arrhythmic agent.
Formulation: Tablet.
Brand name: Tonocard.
Approved New Drugs
Ivabradine
Mechanism of action: It acts by selectively inhibiting the "funny" channel pacemaker
current in the sinoatrial node in a dose-dependent fashion, and that is the main advantage of the
drug.
Vyndaqel
Mechanism of action: It acts as a transthyretin stabilizer that selectively binds to
transthyretin, stabilizing the tetramer of the transthyretin transport protein and slowing the
formation of amyloid that causes Cardiomyopathy (ATTR-CM is an underdiagnosed and
potentially fatal disease. It's characterized by deposits of amyloid).
Vyndamax
Mechanism of action: It acts as a transthyretin stabilizer that selectively binds to
transthyretin, stabilizing the tetramer of the transthyretin transport protein and slowing the
formation of amyloid that causes cardiomyopathy.
Rivaroxaban
Mechanism of action: It competitively inhibits free and clot-bound factor Xa. Factor Xa is
needed to activate prothrombin.
Betrixaban
Mechanism of action: It exerts action by preventing thrombin generation without having a
direct effect on platelet aggregation.
Nebivolol
Mechanism of action: It is a selective β1-receptor antagonist.
119
Drugs Acting on Cardiovascular System (CVS)
9.2 ANTIHYPERTENSIVE AGENTS
Antihypertensive agents are used to suppress or lower the increased blood pressure.
Hypertension (HTN or HT), also known as high blood pressure (HBP), is a condition
when blood flows through the blood vessels with a force greater than normal. Hypertension is
a long-term medical condition in which the blood pressure in the arteries remains persistently
elevated. High blood pressure usually does not cause symptoms. Hypertension can strain the heart,
damage blood vessels, and increase the risk of coronary artery disease, heart attack, stroke, vision
loss, kidney problems, and death. Normal blood pressure at rest is within the range of 100–
140 millimeters mercury (mmHg) systolic and 60–90 mmHg diastolic. High blood pressure is
present if the resting blood pressure is persistently at or above 140/90 mmHg for most adults.
Types of Hypertension
Primary Hypertension (Essential Hypertension)
Usually, people with essential hypertension have no symptoms, but you may experience
frequent headaches, tiredness, dizziness or nose bleeds. Although the cause is unknown, it results
from a complex interaction of genes and environmental factors. Numerous common genetic
variants with small effects on blood pressure have been identified as well as some rare genetic
variants with large effects on blood pressure.
Secondary Hypertension
The most common cause of secondary hypertension is an abnormality in the arteries
supplying blood to the kidneys. Other causes include airway obstruction during sleep, diseases
and tumors of the adrenal glands, hormone abnormalities, thyroid disease, and too much salt or
alcohol in the diet. Secondary hypertension results from an identifiable cause. Kidney disease is
the most common secondary cause of hypertension.
Isolated Systolic Hypertension
Blood pressure is recorded in two numbers: The upper or first number is the systolic
pressure which is the pressure exerted during the heartbeat; the lower or second number is the
diastolic pressure which is the pressure as the heart is resting between beats. Normal blood
pressure is considered 140/90 mm of Hg. With isolated systolic hypertension, the systolic
pressure rises above 140 while the lower number stays near the normal range below 90. This type
of hypertension is most common in people over the age of 65 and is caused by the loss of
elasticity of the arteries. Systolic pressure is much more important than diastolic pressure when it
comes to the risk of cardiovascular disease for an older person.
Malignant Hypertension
This type occurs in only about one percent of people with hypertension. It is more common
in younger adults, African-American men, and women who have pregnancy toxemia. Malignant
hypertension occurs when your blood pressure rises extremely quickly. If your diastolic pressure
goes over 130, you may have malignant hypertension. This is a medical emergency and should be
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A Textbook of Pharmaceutical
Chemistry
treated in a hospital. Symptoms include numbness in the arms and legs, blurred vision, confusion,
chest pain and headache.
Resistant Hypertension
If three different types of antihypertensive medications are prescribed to the patient and
blood pressure is still too high, it may have resistant hypertension. Resistant hypertension may
occur in 20 to 30 percent of high blood pressure cases. Resistant hypertension may have a genetic
component and is more common in people who are older, obese and female, or have an
underlying illness such as diabetes or kidney disease.
Complications of High Blood Pressure
When blood pressure stays high over time, it can damage the body and cause complications.
Some common complications and their signs and symptoms include:
Aneurysms
Formation of an abnormal bulge in the wall of an artery. Aneurysms develop and grow for
years without causing signs or symptoms until they rupture, grow large enough to press on nearby
body parts, or block blood flow. The signs and symptoms that develop depend on the location of
the aneurysm.
Chronic Kidney Disease
Narrowing of blood vessels in the kidneys possibly causes kidney failure.
Cognitive Changes
Research shows that over a while, higher blood pressure numbers can lead to cognitive
changes. Signs and symptoms include memory loss, difficulty finding words, and losing focus
during conversations.
Eye Damage
When blood vessels in the eyes burst or bleed. Signs and symptoms include vision changes
or blindness.
Antihypertensive agents are classified as follows:
(a) Angiotensin-converting Enzyme Inhibitors
Captopril
Enalapril
Lisinopril
Ramipril
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Drugs Acting on Cardiovascular System (CVS)
Fosinopril
Quinapril
(b) Angiotensin (AT-1) Receptor Blockers
Losartan
Candesartan
Valsartan
Telmisartan
Olmesartan
(c) Renin-inhibitors
Aliskiren
(d) Sympathetic Inhibitors
(i)
-receptor blockers
Prazosin
Terazosin
Doxazocin
Phentolamine
Phenoxybenzamine
(ii) β-receptor blockers
Propranolol
Metoprolol
Atenolol
α + β blockers
Labetalol
Carvedilol
(e) Central sympatholytics drugs
Clonidine
Methyldopa
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A Textbook of Pharmaceutical
Chemistry
(f) Calcium channel blockers
(i) Phenyl alkyl amines
Verapamil
(ii) Benzothiazepine
Diltiazem
(iii) Dihydropyridines
Nifedipine
Amlodipine
Felodipine
(g) Vasodilators
(i) Arteriolar dialators
Hydralazine
Minoxidil
Diazoxide
(ii) Arteriolar + venodialators
Sodium nitroprusside
(h) Natural antihypertensive
Reserpine
Propranolol
Structure:
HO
N
H
O
Chemical name: (RS)-1-(1-Methylethylamino)-3-(1-naphthyloxy)-propan-2-ol.
Uses: As an antihypertensive agent.
123
Drugs Acting on Cardiovascular System (CVS)
Formulations: Tablet and Injectable.
Brand name: Inderal.
Captopril
Structure:
N
O
HS
CH
3
COOH
Chemical name: (2S)-1-[(2S)-2-methyl-3-sulfanylpropanoyl]-pyrrolidine-2-carboxylic acid.
Uses: As an antihypertensive agent.
Formulation: Tablet.
Brand names: Capotril and Capoten.
Lisinopril
Structure:
H
N
HO
O
N
NH
2
O
OH
O
Chemical name: (2S)-1-[(2S)-6-amino-2-{[(1S)-1-carboxy-3-phenylpropyl)-amino]-
hexanoyl}-pyrrolidine-2-carboxylic acid.
Uses: As an antihypertensive agent.
Formulation: Tablet.
Brand names: Listril, Zestril and Lisoril.
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A Textbook of Pharmaceutical
Chemistry
Enalapril
Structure:
H
N
O
O
N
O
OH
O
Chemical name: (2S)-1-[(2S)-2-{[(2S)-1-ethoxy-1-oxo-4-phenylbutan-2-yl]-amino}-
propanoyl)-Pyrrolidine-2-carboxylic acid.
Uses: As an antihypertensive agent.
Formulation: Tablet.
Brand names: Enam, Renitec and Vasotec.
Benazepril
Structure:
H
N
O
O
N
O
OH
O
Chemical name: 2-[(3S0-3-{[(2S)-1-ethoxy-1-oxo-4phenylbutan-2-yl]-amino}-2-oxo-4,5-
dihydro-3H-1-benzazepin-1-yl]-acetic acid.
Uses: As an antihypertensive agent.
Formulation: Tablet.
Brand names: Lotensin and Benace
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