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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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65
Drugs Acting on Central Nervous System (CNS)
Alprazolam
Structure:
N
N
Cl
N
N
Chemical name:8-Chloro-1-methyl-6-phenyl-4H-[1,2,4]triazolo[4,3-a][1,4]-benzodiazepine.
Uses: As a sedative and hypnotic.
Formulations: Solid dosage form (Tablet) and Injectables.
Brand names: ALPRAX, ALZOLAM, XANAX, and RESTYL.
Nitrazepam
Structure:
N
H
N
N
O
O
O
Chemical name: 7-Nitro-5-phenyl-1H-benzo[e][1,4]diazepin-2(3H)-one.
Uses: As a sedative and hypnotic. For the treatment of insomnia (lack of sleep).
Formulation: Solid dosage form (Tablet).
Brand names: NITRAVET, SEDAMON, and SOMNITE
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A Textbook of Pharmaceutical
Chemistry
Phenobarbitone
Structure:
HN
NHO
O
O
Chemical name: 5-Ethyl-5-phenyl-1,3-dizinane-2,4,6-trione.
Uses: As a sedative and hypnotic. In the treatment of status epilepticus (type of epilepsy).
Formulations: Solid dosage form (Tablet) and Injectable.
Brand names: Luminal and Gardenal.
Approved New Drugs
Eszopiclone, Zaleplon is the ‘Z-drugs’.
Eszopiclone
Mechanism of action: It binds to the GABA receptor.
Zaleplon
Mechanism of action: It is a nonbenzodiazepine from the pyrazolopyrimidine class, GABA-
A agonist.
Suvorexant and SB334867
Mechanism of action: It is an Orexin receptor antagonist.
7.4 ANTIPSYCHOTICS
Antipsychotics are the agents primarily used to manage psychosis, delusions, and
hallucinations. Psyche means mind, thus these agents are used to treat the abnormal conditions of
mind. These agents either inhibit or alter the behavioral, mood, and emotional responses of a
patient. The antipsychotic agents, now more commonly known as ‘neuroleptics’ are one of the
most important and widely used classes of drugs.
First-generation drugs are known as typical antipsychotics and second-generation are known
as atypical antipsychotics.
67
Drugs Acting on Central Nervous System (CNS)
Various psychiatric illnesses include:
(a) Schizophrenia
It is a neurological as well as a psychological disorder. It is a general disorder of lack of
consciousness, thinking, and perception. The most common symptoms include thought disorders,
delusional perception, hallucinatory voices, speech poverty, and social withdrawal.
(b) Obsessive-Compulsive Disorder
It is characterized by recurrent obsessional thoughts or ideas, images, or impulsiveness that
enters the patients mind again and again.
(c) Mental Retardation
It is composed of incomplete development of the mind, which is characterized by
impairment of skills.
Antipsychotic agents are classified as follows:
(a) Phenothiazines (First-generation Drugs)
Chlorpromazine
Triflupromazine
(b) Butyrophenones
Haloperidol
Trifluperidol
Penfluridol
Droperidol
Sulpiride
(c) Atypical Antipsychotics (Second-generation Drugs)
Clozapine
Risperidone
Olanzapine
Ziprasidone
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A Textbook of Pharmaceutical
Chemistry
Chlorpromazine
Structure:
N
S
N
Cl
Chemical name: 3-(2-Chloro-10H-phenothiazin-10-yl)-N,N-dimethyl-propan-1-amine.
Uses: In the treatment of schizophrenia, bipolar disorder.
Formulation: Solid dosage form (Tablet).
Brand names: Largactil and Thorazine.
Haloperidol
Structure:
OH
N
Cl
O
F
Chemical name: 4-[4-(4-Chlorophenyl)-4-hydroxypiperidin-1-yl]-1-(4-flurophenyl)-butan-
1-one.
Uses: In the treatment of schizophrenia, mania, bipolar disorder, and delirium.
Formulations: Tablet, Injectable, and Drops.
Brand names: Haldol, Halopidol, and Senorm.
69
Drugs Acting on Central Nervous System (CNS)
Risperidone
Structure:
O
N
N
N
N
F
O
Chemical name: 3-[2-[4-(6—Fluoro-1,2-benzoxazol-3-yl)-piperidine-1-yl]ethylmethyl-
6,7,8,9-tetrahydropyrido[1,2-a]pyrimidin-4-one.
Uses: In the treatment of schizophrenia, bipolar disorder, in autism.
Formulation: Tablet.
Brand names: RESPIDON and SIZODON.
Droperidol
Structure:
N
F
O
N
N
O
H
Chemical name: 3-[1-[4-(4-Fluorophenyl)-4-oxobutyl]-3,6-dihydro-2H-pyridin-4-yl]-1H-
benzimidazol-2-one.
Uses: In the treatment of schizophrenia, mania.
Formulations: Tablet and Injectable.
Brand names: Dridol, Innovar, and Xomolix.
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A Textbook of Pharmaceutical
Chemistry
Sulpiride
Structure:
N
N
O
O
S
H
2
N
O
O
H
Chemical name: N-[(1-Ethylpyrrolidin-2-yl)-methyl]-2-methoxy-5-sulfamoylbenzamide.
Uses: In the treatment of schizophrenia, mania.
Formulations: Tablet, Capsule, and Solution.
Brand names: Dogmatil, Espiride, and Prometar.
Note: In India, Levosulpiride is used.
Approved New Drugs
The atypical antipsychotics include:
Quetiapine (Seroquel, AstraZeneca)
Mechanism of action: It acts as an antagonist of D2 receptors in the mesolimbic pathway,
and has more efficacy than other drugs.
Aripiprazole (Abilify, Bristol-Myers Squibb/Otsuka)
Mechanism of action: It acts as a partial agonist of the dopamine D2 and the serotonin 5-
HT-1A receptors, and as an antagonist of serotonin 5-HT-2A receptor.
Aripiprazolelauroxil (Aristada)
Cariprazine (Vraylar)
Mechanism of action: It acts as a partial agonist of the dopamine D2 and D3 receptors with
high affinity than other drugs available in the market.
7.5 ANTICONVULSANTS (ANTIEPILEPTICS)
These drugs are used in the treatment of seizures, convulsions, or epileptic attacks. They are
also called antiepileptic drugs.
The term epilepsy is derived from the Greek word epilambenein which means ‘to seize or
convulsions’. A convulsion is a violent involuntary spasmodic contraction of the skeletal
musculature.
71
Drugs Acting on Central Nervous System (CNS)
Epilepsy is a collective term called for a group of chronic CNS disorders having in common
the occurrence of self-limited and sudden attacks of seizure. All forms of epilepsy have their
origin in the brain.
John Jackson proposed that these seizures are caused by occasional, sudden, excessive, and
local discharges of grey matter. This abnormal focus may originate as a result of local
biochemical changes in the system.
Types of Epilepsy
(a) Generalized Epilepsy
It spreads very quickly into the entire part of the brain.
(a) Tonic-clonic seizures or grandmal epilepsy: Here mass stimulation of cortical neurons
occurs. Initially, generalized tonic activity followed by a clonic phase. It results due to a
potent cerebral excitation and is also known as major seizures. Total attacks last for
several minutes.
(b) Absence or minor seizures or petitmal epilepsy: It is reported to occur mainly in young
children between the ages of 6 to 14 years. A seizure rapidly disappears after adolescence.
(c) Myoclonic epilepsy: The attack is characterized by the jerky muscular movements of the
head, limbs, or body. The duration of attack remains near about one second and it
reappears at about 5 seconds intervals for a period of a minute.
(d) Infantile epilepsy: Functional pyridoxine deficiency is one of the recognized causes
responsible for it.
E.g., throbbing of the head in an infant.
(B) Partial Epilepsy
In this type, the initial neuronal discharge originates from a specific cortical area.
(a) Motor epilepsy: Only one entire side of the body is affected but consciousness is usually
not lost.
(b) Sensory epilepsy: This is similar to motor epilepsy except that it arises in the sensory
cortex.
(c) Akinetic epilepsy: In which no convulsions are seen. The patient may fall on the ground
without loss of consciousness.
(d) Status epilepticus: It is a state in which one attack follows another without the patient
regaining consciousness. The attack may be grand mal, petit mal, or partial in nature. It
may be fatal in nature.
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A Textbook of Pharmaceutical
Chemistry
They are classified as follows:
(a) Barbiturates
Phenobarbitone
(b) Iminostilbane
Carbamazepine
(c) Hydantoin
Phenytoin
(d) Succinimide
Ethosuximide
(e) Phenyltriazine
Lamotrigene
(f) Aliphatic carboxylic acid derivative
Sodium valproate
(g) Cyclic GABA analogues
Gabapentin
(h) Deoxy barbiturate
Primidone
(i) Benzodiazepines
Diazepam
Lorazepam
(j) Miscellaneous
Topiramate
Vigabatrin
Tiagabine
Zonisamide
73
Drugs Acting on Central Nervous System (CNS)
Phenytoin
Structure:
NH
H
N
O
O
Chemical name: 5,5-Diphenylimidazolidine-2,4-dione.
Uses: In the treatment of tonic-clonic seizures, partial seizures.
Formulations: Tablet, Capsule, and Suspension.
Brand names: Dilantin and Eptoin.
Ethosuximide
Structure:
N
H
O
O
H
3
C
CH
3
Chemical name: 3-Ethyl-3-methyl-pyrrolidine-2,5-dione.
Uses: A choice of drug in the treatment of absence seizure or petitmal epilepsy.
Formulations: Syrup and Capsule.
Brand name: Zarontin.
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A Textbook of Pharmaceutical
Chemistry
Carbamazepine
Structure:
N
O
NH
2
Chemical name: 5H-dibenzo [b,f]azepine-5-carboxamide.
Uses: As an anticonvulsant agent.
Formulations: Tablet and Syrup.
Brand names: Tegretol, Mazetol, and Carbatol.
Clonazepam
Structure:
N
H
N
O
O
2
N
Cl
Chemical name: 5-(2—Chlorophenyl)-7-nitro-1,3-dihydro-1,4-benzodiazepin-2-one.
Uses: In the treatment of seizures, panic disorder.
Formulations: Tablet and Injectables.
Brand names: Lonazep and Rivitril.
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