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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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85
Drugs Acting on Autonomic Nervous System (ANS)
Dopamine
A compound is present in the body as a neurotransmitter and a precursor of other substances
including adrenaline.
Structure:
NH
2
HO
HO
Chemical name: 4-(2-Aminoethyl)-benzene-1,2-diol.
Uses: It is useful in the treatment of Parkinson’s disorder which is a long-term degenerative
disorder of the central nervous system that mainly affects the motor system.
Formulation: Injectable.
Brand names: Dopamine and Dopacard.
Ephedrine
Structure:
OH
NH
Chemical name: (R,S)-2-(methylamino)-1-phenylpropan-1-ol.
Uses: It is useful in the treatment of hypertension and as a bronchodilator.
Formulations: Injectable and Nasal drop.
Brand names: Sufidrin and Enorine.
Phenylephrine
Structure:
OH
OH
H
N
Chemical name: (R)-3-[1-Hydroxy-2-(methylamino)-ethyl]-phenol.
86
A Textbook of Pharmaceutical
Chemistry
Uses: It is useful as a decongestant and acts as a vasopressor agent. Hemorrhoids (swollen
veins in the lowest part of rectum and anus). Priapism (A medical condition in which the erect
penis does not return to its flaccid state). It is also used as a mydriatic (Pupil dilation).
Formulations: Injectable, Nasal spray, Eye drop, and Tablet.
Brand names: Sinarest, Decold and Fenox.
Oxymetazoline
Structure:
HO
N
H
N
Chemical name:3-(4,5-Dihydro-1H-imidazol-2-yl-methyl)-2,4-dimethyl-6-tert-butyl-phenol.
Uses: It is useful as a decongestant and acts as a vasopressor agent. It is useful as a mydriatic
(Pupil dilation).
Formulations: Injectable, Nasal spray, Eye drop, and Tablet.
Brand names: Afrin and Drixine.
Naphazoline
Structure:
N
H
N
Chemical name: 2-(Naphthalen-1-yl-methyl)-4,5-dihydro-1H-imidazole.
Uses: It is used as a decongestant and acts as a vasopressor agent.
Formulations: Nasal spray and Nasal drops.
Brand names: Naphcon-A and Privine.
87
Drugs Acting on Autonomic Nervous System (ANS)
Pseudoephedrine
Structure:
OH
NH
Chemical name: (S,S)-2-Methylamino-1-phenylpropan-1-ol.
Uses: It is used as a nasal/sinus decongestant and stimulant.
Formulations: Syrup and Tablet.
Brand names: Sudafed and Sinutab.
Propylhexadrine
Structure:
HN
Chemical name: 1-Cyclohexyl-N-methylpropan-2-amine.
Uses: It is used as a nasal decongestant (for relief of congestion due to colds, allergies and
allergic rhinitis).
Formulations: Syrup and Tablet.
Brand names: Benzedrex and Obesin.
Metaraminol
Structure:
HO
HO
NH
2
H
3
C
H
H
Chemical name: (1R,2S)-3-[2-Amino-1-hydroxypropyl]-phenol.
Uses: It is used in the prevention and treatment of acute hypotensive state occurring with
spinal anesthesia.
88
A Textbook of Pharmaceutical
Chemistry
Formulation: Injectable.
Brand names: Aramine, Metaramin, and Pressonex.
Salbutamol
Structure:
H
N
OH
O
H
OH
Chemical name: (RS)-4-[2-(tert-Butylamino)-1-hydroxyethyl]-2-(hydroxymethyl)-phenol.
Uses: It is useful in the symptomatic treatment of asthma attacks and symptoms relief of
conditions associated with reversible airways obstruction.
Prevention of bronchospasm (tightening of the windpipe causing difficulty in breathing)
due to exercise or by unavoidable exposure to a known allergen. It is useful in delaying delivery
in women undergoing premature labor.
Formulations: Tablet, Inhalation, and Injectable.
Brand names: Ventolin, Proventil, and Accuneb.
Salmeterol
Structure:
HO
N
H
O
OH
OH
Chemical name: (RS)-2-(Hydroxymethyl)-4-{1-hydroxy-2-[6-(4-phenylbutoxy)-
hexylamino]-ethyl}-phenol.
Uses: It is useful in the treatment of asthma in combination with another long-term asthma-
control medicine (e.g., inhaled corticosteroids). It is used to prevent breathing problems in certain
patients, including patients with nighttime asthma or breathing problems caused by exercise. It is
also used for the long-term treatment of Chronic Obstructive Pulmonary Disease (COPD).
89
Drugs Acting on Autonomic Nervous System (ANS)
Formulations: Tablet, Inhalation, and Injectable.
Brand name: Serevent.
8.2 SYMPATHOLYTICS (ADRENERGIC ANTAGONIST)
Sympatholytic drugs block the sympathetic adrenergic system. Adrenergic antagonists are
the agents that act to inhibit the action of catecholamines (adrenaline) at the adrenergic receptors.
Sympatholytic agents are classified as follows.
(a) Beta ()-haloalkylamine
Phenoxybenzamine
(b) Competitive Antagonists
Non-selective
Ergot alkaloids class
Ergotamine
Ergotoxine
Imidazoline class
Phentolamine
Tolazoline
(c) Alpha-1 (-1) Selective Antagonists
Prazosin
Terazosin
Doxazosin
Tamsulosin
(d) Alpha-2 (-2) Selective Antagonists
Yohimbine
(e) Nonselective Antagonists
Beta (β) blockers class
Propanolol
Sotalol
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A Textbook of Pharmaceutical
Chemistry
Timolol
(α) and (β) blockers class
Labetalol
Carvedilol
(f) Beta (β) Selective Antagonists
Metoprolol
Atenolol
Esmolol
Betaxolol
Acebutolol
Practalol
Phenoxybenzamine
Structure:
O
N
Cl
Chemical name: (RS)-N-benzyl-N-(2-chloroethyl)-1-phenoxypropan-2-amine.
Uses: It is useful in the treatment of hypertension, sweating caused by certain kinds of
tumor-like pheochromocytoma. (Pheochromocytoma: It is a rare tumor of adrenal gland tissue. It
results in the release of too much epinephrine and norepinephrine hormones that control heart rate,
metabolism, and blood pressure, results in increasing the blood pressure than normal level).
Formulations: Capsule and Injectable.
Brand names: Dibenzyline and Fenoxine.
91
Drugs Acting on Autonomic Nervous System (ANS)
Phentolamine
Structure:
HO
N
N
N
H
Chemical name: 3-[(4,5-Dihydro-1H-imidazol-2-ylmethyl)(4-methylphenyl)amino]-phenol.
Uses: In the prevention of dermal necrosis. For the diagnosis of pheochromocytoma by the
phentolamine blocking test.
Formulations: Solution and Injectable.
Brand names: Regitine and Fentanor.
Tolazoline
Structure:
N
HN
Chemical name: 2-Benzyl-4,5-dihydro-1H-imidazole.
Uses: It is a vasodilator used to treat spasms of peripheral blood vessels (Acrocyanosis).
It is useful in the treatment of:
Arteriosclerosis Obliterans
Causalgia (severe burning pain in a limb)
Peripheral Vascular Diseases
Persistent Fetal Circulation Syndrome
Raynaud’s Disease (Medical condition in which spasm of arteries cause episodes of
reduced blood flow).
Scleroderma
Spasm
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A Textbook of Pharmaceutical
Chemistry
Thromboangiitis Obliterans
Thrombophlebitis (inflammation of the wall of a vein).
As a veterinary medicine.
Formulation: Injectable.
Brand name: Priscoline hydrochloride.
Prazosin
Structure:
N
N
O CH
3
O
CH
3
NH
2
NN
O
O
Chemical names: [4-(4-Amino-6,7-dimethoxy-2-quinazolinyl)-1-piperazinyl](2-furyl)-
methanone.
Uses: In the treatment of hypertension or benign prostatic hyperplasia. Also useful to prevent
strokes and heart attacks.
Formulation: Tablet.
Brand names: Minipress, Vasoflex, and Lentopres.
Doxazocin
Structure:
N
NO
O
N
N
O
O
O
NH
2
93
Drugs Acting on Autonomic Nervous System (ANS)
Chemical name: (RS)-2-[4-(2,3-Dihydro-1,4-benzodioxine-2-carbonyl)-piperazin-1-yl]-6,7-
dimethoxyquinazolin-4-amine.
Uses: It is used to treat hypertension (high blood pressure) or to improve urination in men
with benign prostatic hyperplasia (enlarged prostate).
Formulation: Tablet.
Brand names: Cardura, Duracard, Carduran, and Doxapress.
Propranolol
Structure:
HO
N
H
O
Chemical name: (RS)-1-(1-Methylethylamino)-3-(1-naphthyloxy)-propan-2-ol.
Uses: It is used to treat tremors, angina (chest pain), and hypertension. It is also used to treat
or prevent heart attack and to reduce the severity and frequency of migraine attacks.
Formulations: Tablet, Injectable, and Liquid.
Brand names: Ciplar, Betabloc, Inderal, and Hemangeol.
Contraindications: It should not be used if the patient is suffering from asthma, very slow
heartbeats or a serious heart condition such as “sick sinus syndrome” or “AV block”.
Babies who are having weight less than 4.5 pounds should not be given Hemangeol oral
liquid (Propranolol 4.28 mg/ml).
Metoprolol
Structure:
O
O
O
H
NH
Chemical name: (RS)-1-(Isopropylamino)-3-[4-(2-methoxyethyl)phenoxy]-propan-2-ol.
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A Textbook of Pharmaceutical
Chemistry
Uses: It is useful in the treatment of
Heart failure.
Vasovagal syncope.
Adjunct in treatment of hyperthyroidism.
Metoprolol is used to treat angina (chest pain) and hypertension (high blood pressure).
Formulations: Tablet and Injectable.
Brand names: Lopressor and Metolar XR.
Atenolol
Structure:
O
NH
2
O
OH
NH
Chemical name: (RS)-2-{4-[2-Hydroxy-3-(propan-2-ylamino)-propoxy]-phenyl}-acetamide.
Uses: It is used to treat angina (chest pain), and hypertension.
Formulations: Tablet and Injectable.
Brand names: Tenormin, Aten, and Betacard.
Acebutolol
Structure:
HN
O
O
O
OH
NH
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