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Drugs Acting on Central Nervous System 167
5.5.6 Sertraline
Brand Name: Zoloft
Sertraline (Zoloft) is a drug of the class tetralins, a secondary amino compound and a
dichlorobenzene which is substituted at positions 1 and 4 by a methyl amino and a 3,4-
dichlorophenyl group, respectively. It is commonly known as a selective serotonin reuptake
inhibitor (SSRI). It is represented by the following structural formula:
Chemical Name: (1S,4S)-4-(3,4-dichlorophenyl)-N-methyl-1,2,3,4-tetrahydronaphthalen-1-amine
Properties: It occurs as a white crystalline powder that is slightly soluble in water and isopropyl
alcohol, and sparingly soluble in ethanol.
Uses:
➢ Sertraline tablet is used in major depressive disorder (MDD).
➢ It is effective for panic disorder.
➢ It is used for the treatment of social anxiety disorder.
➢ It is used for the treatment of generalized anxiety disorder.
➢ It is used in the treatment of obsessive-compulsive disorder (OCD) in adults and
paediatric patients aged 6-17 years.
➢ It is used for the treatment of Post-traumatic stress disorder (PTSD).
➢ It is used in social anxiety disorder (SAD).
➢ It is used to alleviate the symptoms of premenstrual dysphoric disorder to reduce
bloating, mood swings, irritability, and breast tenderness.
Dosage Forms: Sertraline is available in oral concentrate (20 mg/mL) and oral tablet (100 mg,
25 mg and 50 mg). A dosage of 25 mg or 50 mg per day is the initial therapeutic dosage.
Storage and Stability: Sertraline should store at room temperature between 15°C and 30°C.
Keep it away from light. Keep the bottle closed tightly. Store this medication in moist or damp
areas, such as bathrooms.
Marketed Preparations:
➢ Zoloft-50 mg (Sertraline hydrochloride tablet) – Pfizer
➢ ZUBISERT 100 (Sertraline Hydrochloride 100 mg Tablets) –Green Cross Remedies
➢ Serene 100/50 (Sertraline 100) – Elikem Pharmaceuticals
168 Text Book of Pharmaceutical Chemistry
5.5.7 Citalopram
Brand Name: Celexa
Citalopram is a drug of class selective serotonin reuptake inhibitor (SSRI). Its chemical
structure is unrelated to that of other SSRIs or of tricyclic, tetracyclic, or other available anti-
depressant agents. Citalopram is sold as a racemic mixture, consisting of 50% (R)-(−)-citalopram
and 50% (S)-(+)-citalopram, only the (S)-(+)-enantiomer has the desired anti-depressant effect
with the following structural formula:
Properties: It occurs as a fine, white to off-white powder. Citalopram HBr is sparingly soluble in
water and soluble in ethanol.
Uses:
➢ Citalopram is used for the treatment of depression.
➢ It may be used as part of a combination therapy.
➢ It is used as an anti-depressant.
➢ It is used to treat major depressive disorder.
➢ It is used to treat obsessive compulsive disorder and panic disorder.
➢ It is used to treat social phobia.
Dosage Forms: Celexa is available as tablets or as an oral solution. Tablets come in different
strengths ranging from 10 mg to 40 mg oral tablet (10 mg, 20 mg and 40 mg).
Storage and Stability: Store Citalopram tablets at room temperature. Tablets can be temporarily
stored at temperatures between 15°C and 30°C. Keep the drug away from high temperatures. Do
not store in moist or damp areas. Keep the bottle tightly closed.
Marketed Preparations:
➢ Citalopram tablets, USP 40 mg
➢ CITAPAD-20 (Citalopram Tablets, I.P. 20 mg) – Tripada Healthcare Pvt. Ltd.
➢ Citopram 100 mg Tablet (Citalopram Hydrochloride USP) – Global Pharmaceuticals
➢ Citalo 20 mg (Citalopram HBr) – Platinum Pharmaceutical
Drugs Acting on Central Nervous System 169
5.5.8 Escitalopram
Brand Name: Lexapro
Escitalopram is the drug of class selective serotonin reuptake inhibitor (SSRI). The
S-enantiomer of racemic citalopram. Escitalopram is approximately 150 times more potent
than citalopram’s R-enantiomer role as an anti-depressant. It is represented by the following
structural formula:
Chemical Name: (1S)-1-[3-(dimethylamino)propyl]-1-(4-fluorophenyl)-3H-2-benzofuran-5-carbonitrile
Uses:
➢ Escitalopram is used for the treatment of depression.
➢ It may be used as part of a combination therapy.
➢ It is used for the treatment of major depressive episodes.
➢ It is used for the treatment of social anxiety disorder (social phobia).
➢ It is used for the treatment of obsessive-compulsive disorder.
➢ It is used for the treatment of panic disorder with or without agoraphobia.
➢ It is used for the treatment of generalized anxiety disorder.
Dosage Forms and Strengths: Escitalopram is available as a tablet and oral solution.
➢ Tablet: 5 mg, 10 mg and 20 mg
➢ Capsule: 5 mg, 10 mg and 20 mg
➢ Oral Solution: 5 mg/5 ml
Storage and Stability:
Store it at 25°C (77°F); excursions permitted to 15°C-30°C (59°F-86°F). Keep the
Escitalopram away from high temperatures. Do not store in moist or damp areas. Keep the bottle
tightly closed.
Marketed Preparations:
➢ Escitalopram Tablet (Nexito 20 mg Tab) – Kachhela Medex Pvt. Ltd.
➢ S-Citarest-20 (Escitalopram Tablets I.P.) – Tanishq LifeCare
➢ Lexapro (Escitalopram oxalate) Oral Solution – Amneal Pharmaceuticals, LLS
170 Text Book of Pharmaceutical Chemistry
5.5.9 Fluvoxamine
Brand Names: Luvox, Luvox CR
Fluvoxamine is a selective serotonin reuptake inhibitor (SSRI). Structure of Fluvoxamine is
an oxime O-ether that is benzene substituted by an N-(2-aminoethoxy)-5-methoxypentanimidoyl
group at position 1 and a trifluoromethyl group at position 4. The structural formula is:
Chemical Name: 2-[(E)-[5-methoxy-1-[4-(trifluoromethyl)phenyl]pentylidene]amino]
oxyethanamine
Properties: Fluvoxamine maleate occurs as white to off-white, odorless, crystalline powder
which is sparingly soluble in water; freely soluble in ethanol and chloroform; and practically
insoluble in diethyl ether.
Dosage Forms and Strengths: Fluvoxamine comes in two forms: an oral capsule and an oral
tablet.
➢ Tablets (immediate release): 25 mg, 50 mg and 100 mg
➢ Capsules (extended release): 100 mg and 150 mg
Uses: Fluvoxamine is used for the treatment of:
➢ Obsessive compulsive disorder (OCD) in adults and children aged 8 and older.
➢ Major depressive disorder.
➢ Panic disorder.
➢ Social anxiety disorder.
➢ Post-traumatic stress disorder.
Storage and Stability: Fluvoxamine is stored at room temperature between 15°C to 30°C. Keep
it away from light. Do not store this medication in moist or damp areas.
Marketed Preparations:
➢ Manofluvo-50 (Fluvoxamine Tablet) – CMG Biotech Pvt. Ltd.
➢ Voxa-100 (Fluvoxin 100 mg Tablet) – Elikem Pharmaceuticals Pvt. Ltd.
➢ Fluvoxin 50 mg Tablets (Fluvoxamine) – Demega Formulations
5.5.10 Paroxetine
Brand Names: Brisdelle, Paxil, Paxil CR, Pexeva
Paroxetine structure is a member of piperidines, that consists of piperidine bearing 1,3-
benzodioxol-5-yloxy)methyl and 4-fluorophenyl substituents at positions 3 and 4 respectively. It
is a selective serotonin reuptake inhibitor (SSRI) drug commonly known as Paxil. The structural
formula of paroxetine is:
Drugs Acting on Central Nervous System 171
Chemical Name: (3S, 4R)-3-(1,3-benzodioxol-5-yloxy methyl)-4-(4-fluorophenyl) piperidine
Properties: Paroxetine hydrochloride is an odorless, off-white powder, having a melting point
range of 120°C to 138°C and a solubility of 5.4 mg/mL in water.
Uses: Paroxetine is used for the treatment of:
➢ Depression, including major depressive disorder.
➢ Panic disorder, obsessive compulsive disorder (OCD) and anxiety.
➢ Post-traumatic stress disorder (PTSD) and premenstrual dysphoric disorder (PMDD).
➢ Hot flashes related to menopause.
➢ Social anxiety disorder and panic disorder.
➢ Agoraphobia and generalized anxiety disorder occasionally.
Storage and Stability: It should be kept at room temperature, between 15°C -30°C. Keep away
from light and moisture. The suspension and controlled release tablets should be stored at or
below 77°F (25°C).
Dosage Forms: Paxil tablets are available as:
➢ Tablets: 10 mg, 20 mg, 30 mg and 40 mg
➢ Paxil CR Tablets: 12.5 mg, 25 mg and 37.5 mg
➢ Suspension: 10 mg/5ml
Marketed Preparations:
➢ Pexep 40 (Paroxetine Tablet 40 mg) – Medexim India
➢ Setoxline CR 12.5 (Paroxetine CR Tablets 12.5 mg) – Lifecare Neuro Products Limited
➢ Paxil Cr (Paroxetina/ Paroxetina) 25 mg – Guru Baba Pharmax Pvt. Ltd.
➢ Pexep CR (Paroxetine) 25 mg – Intas Pharmaceuticals Limited
5.6 EXERCISE
A. Long Answer Type Questions
1. What are general anesthetics? Write the classification of general anesthetics and explain
the uses and properties of Thiopental sodium.
2. What are sedative hypnotics? Classify them and write the ideal characteristics of
hypnotics.
172 Text Book of Pharmaceutical Chemistry
3. What are antipsychotics? Give the structure and medicinal uses of any two antipsychotic
agents.
4. What are anti-depressants? Write the properties, chemical name and uses of
Amitriptyline hydrochloride.
5. Give the marketed preparations of Thiopental sodium and Carbamazepine.
6. Define anticonvulsants. Give the structure properties and medicinal uses of Phenytoin.
B. Short Answer Type Questions
1. Define local anesthetics.
2. Write the uses of:
(a) Thiopental Sodium
(b) Ketamine Hydrochloride
(c) Propofol
3. Define sedative hypnotics.
4. Give the structure and uses of any two anticonvulsant drugs.
5. Write the properties and uses of Sertraline.
6. Write the doses and medicinal uses of Citalopram.
7. What are general anesthetics? Write the various stages of general anesthesia.
8. What are convulsions? Explain in brief the type of generalized tonic-clonic convulsion.
C. Fill in the Blanks
1. Ketalar is the brand name of _______________.
2. DUXILA- 30 is the marketed preparation of _______________.
3. Brand name of Citalopram is _______________.
4. Brisdelle is the brand name of _______________.
5. Olanzapine belongs to the class _______________.
6. Alprazolam is used to treat _______________.
7. Phenobarbital is the drug used as a _______________.
8. Structure of clonazepam _______________.
9. Brand name of Lamotrigine _______________.
10. Write the chemical names of Nitrazepam _______________.
Answers
1. Ketamine hydrochloride
2. Duloxetine
3. Celexa
Drugs Acting on Central Nervous System 173
4. Paroxetine
5. Thienobenzodiazepine
6. Anxiety disorders
7. Sedative hypnotics
8.
9. Lamictal
10. 7-nitro-5-phenyl-1,3-dihydro-1,4-benzodiazepin-2-one
Chapter
6
DRUGS ACTING ON AUTONOMIC
NERVOUS SYSTEM
STRUCTURE
6.1 Sympathomimetic Agents
6.2 Adrenergic Antagonists
6.3 Cholinergic Drugs and Related Agents
6.4 Cholinergic Blocking Agents
6.5 Synthetic Cholinergic Blocking Agents
6.6 Exercise
6.1 SYMPATHOMIMETIC AGENTS
Sympathomimetics are the group of drugs that produces an effect similar to that produced by
stimulation of the sympathetic nervous system. These drugs are also known as adrenergic drugs.
Direct acting agonists are the drugs that directly stimulate adrenergic receptors while
indirect acting agonists enhance the actions of endogenous adrenergic transmitters.
Classification of Sympathomimetic Drugs
Sympathomimetic drugs are classified according to the receptors they target.
Sympathomimetic Agents
Direct Acting
Indirect Acting Agents
Mixed Acting
Hydroxy Amphetamine
Pseudoephedrine
Norepinephrine
Epinephrine
Phenylephrine
Dopamine
Terbutaline
Salbutamol
Naphazoline
Tetrahydrozoline
Ephedrine
Metaraminol
Drugs Acting on Autonomic Nervous System 175
DIRECT ACTING AGENTS
6.1.1 Norepinephrine
Brand Names: Levarterenol, Levophed Bitartrate
Norepinephrine, also called noradrenaline, is a naturally occurring catecholamine that is
released predominantly from the ends of sympathetic nerve fibers that functions as a
neurotransmitter in the sympathetic nervous system.
Chemical Name: 4-[(1R)-2-amino-1-hydroxyethyl] benzene-1,2-diol
Properties: Epinephrine appears as white to off-white microcrystalline powder or granules,
odorless. Its melting point is 211°C -212°C. Aqueous solutions are slightly alkaline, slightly bitter
and numbing taste. It is sparingly soluble in water, dilute hydrochloric acid; very slightly soluble
in alcohol and ether; and readily soluble in acids.
Uses: Norepinephrine is used to treat a variety of conditions.
➢ It is used to treat life-threatening low blood pressure (hypotensive state).
➢ It is used in the treatment of peripheral vasomotor collapse.
➢ It is used in the treatment of myocardial infarction.
➢ It is used in septicemia, blood transfusion, and drug reactions.
➢ It is used in the treatment of poliomyelitis and spinal anesthesia.
Stability and Storage: Norepinephrine contains catechol nucleus which can be oxidized readily
on exposure to air and light. Therefore, it is stored in airtight closed container or preferably in a
sealed tube under vacuum or under inert gas. It is stored at –20°C under desiccating conditions.
Dosage Forms:
➢ Norepinephrine available in injectable solution
➢ Noradrenaline (Norepinephrine) 0.08 mg/mL, solution for infusion
Marketed Preparations:
➢ ACTIZA (Norepinephrine Injection) – Actiza Pharmaceutical Pvt. Ltd.
➢ Norepinalth (Norepinalth Norepinephrine Bitartrate Injection) – Livealth Biopharma Pvt.
Ltd.
➢ Nor-Adrenecure (Norepinephrine Injection) – Pharma Cure
176 Text Book of Pharmaceutical Chemistry
Officials:
➢ Noradrenaline, I.P.
➢ Noradrenaline Bitartrate, I.P.
➢ Noradrenaline Bitartrate Injection, I.P.
6.1.2 Epinephrine
Brand Names: Adrenalin, Allerject, Anapen, Articadent, Astracaine
Epinephrine is a hormone and neurotransmitter produced by the adrenal glands that can also
be used as a drug due to its various important functions. It is also known as adrenaline.
Epinephrine is closely related in structure to norepinephrine, differing only in the presence of
a methyl group on the nitrogen side chain. Natural epinephrine is the R-(−)-L-epinephrine
stereoisomer. The chemical structure of epinephrine is:
Chemical Name: 4-[(1R)-1-hydroxy-2-(methylamino) ethyl] benzene-1, 2-diol
Properties: Epinephrine appears as white to nearly-white microcrystalline powder or granules,
odorless. Its melting point is 211°C-212°C. Aqueous solutions are slightly alkaline and have
slightly bitter, numbing taste.
Uses:
➢ Epinephrine is used to treat the symptoms of cardiac arrest.
➢ It is the drug of choice for treating anaphylaxis.
➢ It is also used as a bronchodilator for asthma and superficial bleeding.
➢ It is beneficial in the treatment of bronchiolitis.
➢ Racemic epinephrine has historically been used for the treatment of croup (type
of respiratory infection).
Dosage Forms: Adrenalin available in clear, colorless solution supplied as 1 mg/mL in a single
dose clear glass vial and as 30 mg/mL (1 mg/mL) in a multiple dose amber glass vial.
Stability and Storage: Epinephrine solution deteriorates readily on exposure to air or light,
turning pink from oxidation. Thus, it should be stored in airtight containers in cool dark place at
room temperature, between 15°C to 25°C, but not refrigerated, as temperatures below 15°C may
damage the injector mechanism. The shelf life of adrenaline injector devices is usually 12 to 18
months.