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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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105
Drugs Acting on Autonomic Nervous System (ANS)
(b) Semisynthetic Derivatives
Homotropine
Ipratropium bromide
(c) Synthetic Compounds
(i) Mydriatics
Cyclopentolate
Tropicamide
(ii) Antiparkinsonian agents
Procyclidine
Bisperiden
(d) Antisecretory Antispasmodics
(i) Quaternary compounds
Isopropamide
Oxyphenonium
Clidinium
(ii) Tertiary amines
Dicyclomine
Pirenzepine
Atropine
Structure:
O
O
O
H
N
Chemical name:(RS)-(8-Methyl-8-azabicyclo-[3.2.1]-oct-3-yl)-3-hydroxy-2-phenylpropanoate.
Uses: As an antisialogogue agent (Substances that decrease the production of saliva). To
treat the blunt increased vagal tone (decreased pulse and blood pressure) produced by the intra-
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A Textbook of Pharmaceutical
Chemistry
abdominal tract. As an antidote for overdose of cholinergic drugs. As an antidote for the rapid
type of mushroom poisoning due to the presence of the alkaloid muscarine.
Formulations: Ophthalmic, Injectable and Ointment.
Brand names: Atropen and Atrosulph.
Clidinium Bromide
Structure:
N
O
O
O
H
Br
Chemical name: 3-[(2-Hydroxy-2,2-diphenylacetyl)oxy]-1-methyl-1-
azabicyclo[2.2.2]octan-1-ium bromide.
Uses: It is useful in fixed combination with chlordiazepoxide as adjunctive therapy in the
treatment of peptic ulcers. It is very useful in the treatment of acute enterocolitis (Inflammation of
both the small intestine and the colon).
It is used in the treatment of functional GI motility disturbances.
Formulation: Tablet.
Brand names: Normaxin and Cibis.
Ipratropium Bromide
Structure:
N
+
O
OHO
Br
-
Chemical name: [8-methyl-8-(1-methylethyl)-8-azoniabicyclo-[3.2.1]-oct-3-yl]-3-hydroxy-
2-phenyl propanoate.
Uses: It is administered by inhalation in the treatment of Chronic Obstructive Pulmonary
Disease (COPD). It is used to control and prevent symptoms (wheezing and shortness of breath)
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Drugs Acting on Autonomic Nervous System (ANS)
caused by lung disease. It is used to treat rhinorrhea (Rhinorrhoea is a condition where the nasal
cavity is filled with a significant amount of mucus fluid).
Formulations: Tablet, Inhalation and Nasal spray.
Brand names: Atrovent, Apovent, Ipraxa, Rinatec, Ipravent and Ipranase-AQ.
Homatropine
Structure:
O
O
OH
N
Chemical name: N-Methyl-8-azabicyclo-[3.2.1]-oct-3-yl-2-hydroxy-2-phenyl acetate.
Uses: It is used before eye examinations (e.g., refraction), before and after certain eye
surgeries. It is used to treat uveitis (Inflammation of the uvea) and certain inflammatory
conditions of the eye.
Formulations: Ophthalmic and Injectable.
Brand names: Homide, Homatropine Eye, and Equipin.
Tropicamide
Structure:
O
N
N
HO
Chemical name: (RS)-N-Ethyl-3-hydroxy-2-phenyl-N-(pyridine-4-ylmethyl)-propanamide.
Uses: It is useful in the treatment of mydriasis (Dilation of the pupil) and cycloplegia
(Paralysis of the ciliary muscle of the eye).
Formulations: Ophthalmic and Injectable.
Brand names: Optimide, Tromide and Mydriacyl.
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A Textbook of Pharmaceutical
Chemistry
Cyclopentolate
Structure:
O
O
HO
N
Chemical name: (RS)-2-(Dimethylamino)-ethyl-(1-hydroxycyclopentyl)-(phenyl)-acetate.
Uses: It is used before eye examinations (e.g., refraction), before and after certain eye
surgeries. It is useful in the treatment of mydriasis.
Formulations: Ophthalmic and Injectable.
Brand names: Cyclomid Eye and Cyclogyl.
Dicyclomine
Structure:
O
O
N
Chemical name: 2-(Diethylamino)-ethyl-1-cyclohexylcyclohexane-1-carboxylate.
Uses: In the treatment of irritable bowel syndrome. As an antispasmodic.
Formulations: Tablet and Injectable.
Brand names: Cyclopam, Cyclospar-D and Bentyl.
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Drugs Acting on Autonomic Nervous System (ANS)
Procyclidine
Structure:
OH
N
Cl
Chemical name: 1-Cyclohexyl-1-phenyl-3-pyrrolidin-1-yl-propan-1-ol-hydrochloride.
Uses: It is used to treat Parkinsonism and akathisia (Feeling of inner restlessness). To reduce
adverse effects of antipsychotic treatment given for schizophrenia.
Formulations: Tablet and Injectable.
Brand name: Kemadrin.
Tridihexethyl
Structure:
N
+
HO
Chemical name: 3-Cyclohexyl-N,N,N-triethyl-3-hydroxy-3-phenylpropan-1-aminium.
Uses: As an Anticholinergic, antimuscarinic and antispasmodic. To treat nystagmus
(Condition of involuntary eye movement).
Formulations: Tablet and Injectable.
Brand name: Pathilon.
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Chemistry
Isopropamide Iodide
Structure:
N
+
O NH
2
I
Chemical name: 4-Amino-N,N-diisopropyl-N-methyl-4-oxo-3,3-diphenylbutan-1-aminium.
Uses: It is used in the treatment of peptic ulcers and other gastrointestinal disorders
involving hyperacidity.
Formulations: Tablet and Injectable.
Brand names: Gastabid and Stelabid.
Ethopropazine
Structure:
N
S
N
Chemical name: N,N-Diethyl-1-(10H-phenothiazin-10-yl)-2-propanamine.
Uses: It is used in the treatment of Parkinson's disease and also to control severe reactions.
Formulation: Tablet.
Brand names: Dibutil, Parkin, Parsidan and Parsido.
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Drugs Acting on Autonomic Nervous System (ANS)
Fluoxetine
Structure:
H
N O
F
F
F
Chemical name: N-Methyl-3-phenyl-3-[4-(trifluoromethyl)-phenoxy] propan-1-amine.
Uses: As an antidepressive agent, in patients with premature ejaculation.
Formulation: Capsule.
Brand names: Prozac, Sarafem, and Fludac.
General Information
112
Chapter
Drugs Acting on
Cardiovascular System
(CVS)
The cardiovascular system is also called as the circulatory system. It is an organ system that
permits blood to circulate and transport nutrients, oxygen, CO
2
, hormones and blood cells to and
from the cells in the body to provide nourishment and help in fighting diseases, stabilize the body
temperature, pH and maintain hemostasis.
The CVS constitutes blood, heart and blood vessels. The drugs acting on CVS are classified
based on their action and use.
9.1 ANTI-ARRHYTHMIC AGENTS
Anti-arrhythmic agents are used to suppressing abnormal rhythms of the heart such as atrial
fibrillation, atrial flutter, tachycardia, etc. An arrhythmia is an abnormal heart rhythm. It may feel
like fluttering or a brief pause. It may be so brief that it doesn’t change your overall heart rate (the
number of times per minute that your heart beats), or it can cause the heart rate to be too slow or
too fast. Some arrhythmias don’t cause any symptoms. Others can make you feel lightheaded or
dizzy. There are two basic kinds of arrhythmias.
Bradycardia
Bradycardia is the condition, when the heart rate is too slow that is less than 60 beats per
minute.
Tachycardia
Tachycardia is the condition when the heart rate is too fast which may be more than 100
beats per minute.
An arrhythmia may arise because of alteration in
Automaticity
Conduction
The refractory period of the myocardial cells
9
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Drugs Acting on Cardiovascular System (CVS)
Signs and Symptoms of Arrhythmia
Fluttering in the chest or neck.
The heart may not be able to pump enough blood to the body. This can cause tiredness,
lightheadedness, or may make you pass out. It can also cause death.
Bradycardia can cause fatigue, dizziness, lightheadedness, fainting or near-fainting spells,
or in extreme cases, cardiac arrest.
Tachycardia can reduce the heart’s ability to pump, causing shortness of breath, chest
pain, lightheadedness, or loss of consciousness. If severe, it can also cause a heart attack
or death.
Antiarrhythmic agents are classified as follows:
(a) Class-I (Membrane Stabilizing Agents)
(i) Moderately decrease
Quinidine
Procainamide
Disopyramide
(ii) Little decrease
Lidocaine
Mexiletine
(iii) Marked decrease
Propafenone
Flecainide
(b) Class-II (Antiadrenergic Agents)
Propranolol
Sotalol
Esmolol
(c) Class-III (Increase Action Potential)
Amiodarone
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A Textbook of Pharmaceutical
Chemistry
(d) Class-IV (Calcium Channel Blockers)
Verapamil
Diltiazem
Quinidine
It is a stereoisomer of quinine which is an antimalarial drug.
Structure:
OH
N
H
O
N
Chemical name: (S)-(6-Methoxyquinolin-4-yl) [(1S,2R,4S,5R)-5-vinylquinuclidin-2-yl]-
methanol.
Uses: As an anti-arrhythmic agent.
Formulations: Tablet and Injectables.
Brand names: Quininga and Quinidex (Quinidine sulfate).
Procainamide
Structure:
NH
2
N
H
N
O
Chemical name: 4-Amino-N-(2-diethylaminoethyl)-benzamide.
Uses: It is used in the treatment of supraventricular and ventricular arrhythmias.
Formulations: Tablet and Injectables.
Brand names: Procan and Pronestyl.
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