Drugs acting on the Central

Nervous System (CNS)

Presented By:
Phr. Hemraj Sharma,
HOD, Pharmacy
Rapti Technical School
• Drugs acting on the Central Nervous System
(CNS) are medications that primarily affect the
brain and spinal cord.
 Classification
– Phenothiazines
• Having aliphatic side chain: Chlorpromazine,
Triflupromazine
• Piperidine side chain: Thioridazine
• Piperazine side chain: Trifluperazine, Fluphenazine
– Butyrophenones
• Haloperidol, Trifluperidol, Penfluridol
– Thioxanthenes
• Flupenthixol
– Other heterocyclics
• Pimozide, Loxapine
– Atypical antipsychotics
• Clozapine, Aripiprazole, Risperidone, Ziprasidone,
Olanzapine, Quetiapine
Chlorpromazine
• Chemistry
– It is derivative of phenothiazine
– Dimethylamino propyl group is attached at
position 10.
– Chloro group is present at position 2.
• Physical properties
– It is official as Chlorpromazine hydrochloride.
– It occurs as white to creamy white powder.
– It is very soluble in water, freely soluble in
ethanol.
– It is sensitive to air and light. It decomposes on
exposure being yellow pink or violet.
– MP: 375-378°C.
Stability and Storage
• It is sensitive to air and light, hence should be

stored in tightly closed light resistant

container.
 • Uses
– Psychotic disorders,
– schizophrenia
– Nausea and vomiting
– Intractable hiccups
– Acute intermittent porphyria
Schizophrenia is a serious mental disorder in which people interpret reality abnormally.
Schizophrenia may result in some combination of hallucinations, delusions, and extremely disordered
thinking and behavior that impairs daily functioning, and can be disabling.
Acute intermittent porphyria (AIP) is a rare metabolic disorder that is characterized by partial deficiency
of the enzyme hydroxymethylbilane synthase (also known as porphobilinogen deaminase). This enzyme
deficiency can result in the accumulation of porphyrin precursors in the body.
Trifluoperazine

• Chemistry
– It is derivative of phenothiazine
– It consists of methyl piperazinyl propyl group at
position 10.
– It consists of trifluoromethyl at position 2.
• Physical properties
– It is official as Trifluoperazine Hydrochloride.
– It occurs as white to pale yellow crystalline
powder.
– It is slightly hygroscopic. It is also sensitive to
light.
– It is freely soluble in water, soluble in ethanol.
– MP: 240-243°C.
Stability and storage
• It must be stored in tightly closed light

resistant container.
• Uses
– Psychotic disorders- Schizophrenia
– Non psychotic anxiety.
Haloperidol

• Chemsitry
– It is the derivative of butyrophenone.
– Chlorophenyl and hydroxy group is present at
position 4 of piperidine moiety.
– Fluoro group is attached at position 4 of phenyl
group.
• Physical properties
– It exists as white or faintly yellowish. amorphous
or microcrystalline powder.
– It is practically insoluble in water and sparangly
soluble in alcohol.
– It is odorless and tasteless.
– It is sensitive to light and moisture.
– MP: 151°C
Stability and storage
• It must be stored in well closed light resistant

container.
• Uses
– Psychotic disorders
– Schizophrenia
Anxiolytics: Drugs used to alleviate
symptoms of anxiety and panic disorders,
such as benzodiazepines (e.g., diazepam,
alprazolam)
 Diazepam

• Chemistry
– It is the derivative of 1,4 benzodiazepine.
– Ketone group is present at position 2.
– Phenyl group is present at position 5.
– Chloro group is present at position 7.
– Methyl group is present at position 1.
• Physical properties
– Occurs as white or almost white crystalline
powder.
– Very slightly soluble in water, soluble in ethanol.
– Sensitive to light and moisture.
– Odorless or almost odorless.
– Slightly bitter taste.
– MP 125-126°C.
• Stability and Storage
– Store protected from light and moisture.
• Uses
– Anxiety disorder
– Siezure disorder
– Preoperative sedation
– Sedation in ICU patients
– Muscle spasms
– Alcohol withdrawal
Lorazepam
• Chemistry
– It is the derivative of 1,4 benzodiazepine.
– Hydroxy group is present at position 3.
– o-chlorophenyl group is present at position 5.
– Chloro group is present at position 7.
– Keto group is present at position 2.
• Physical properties
– Occurs as white to almost white crystalline
powder.
– Practically insoluble in water, sparingly soluble in
ethanol.
– Sensitive to light and moisture.
– Odorless.
– MP: 166-168°C
• Stability and Storage
– Store protected from light and moisture.
• Uses
– Anxiety disorders
– Short term treatment of insomnia
– Preoperative sedation
– Chemotherapy induced nausea and vomiting
– Anxiolytic/sedation in ICU patients
Nitrazepam
• Chemistry
– Derivative of 1,4 benzodiazepine
– Phenyl group is present at position 5
– Nitro group is present at position 7.
– Ketone group is present at position 2.
• Physical properties
– Occurs as yellow crystalline powder.
– Practically insoluble in water, slightly soluble in
alcohol.
– Sensitive to light and moisture.
– Odorless or almost odorless.
– MP 224-226°C.
Stability and Storage
• Store protect from light and moisture.
• Uses
– Anxiety
– Short term use in insomnia
– Induce Amnesia
– Can also be used in muscle relaxant
Alprazolam
• Chemistry
– Methyl triazole group is fused along with
benzodiazepine ring along position 1 and 2.
– Chloro group is present 7 of benzodiazepine ring.
– Phenyl group is present at position 5 of
benzodiazepine ring.
• Physical properties
– Occurs as white to off white crystalline powder.
– Practically insoluble in water, soluble in alcohol.
– Sensitive to light, moisture and high temperature.
– Odorless.
– MP: 228-229°C
• Stability and Storage
– Store protected from light and moisture at
controlled room temperature (20-25°C)
• Uses
– Anxiety disorders
– Panic disorders
– Anxiety caused by depression
 Sedatives & Hypnotics
• Sedatives are CNS depressants that reduce restlessness
and emotional tension without producing sleep.
• Hypnotics are CNS depressants that reduce restlessness
and emotional tension by producing sleep.
• Usually sedative and hypnotic action is dose dependent.
For example Phenobarbitone administered 25 mg acts
as sedative while 100 mg produces hypnotic action.
• Hypnotics used in large dose may cause poisoning ,
anesthesia, and even death. The effect of progress is as
follows:
Sedation→Hypnosis →Anesthesia →Coma →Death
 Barbiturates
• Barbiturates are a class of depressant
drugs that are chemically derived
from barbituric acid. They are effective when
used medically as anxiolytics, hypnotics,
and anticonvulsants,

Barbituric acid, the parent structure of all

barbiturates
Phenobarbitone

• Chemistry
– It is the derivative of barbituric acid (pyrimidine
2,4,6 trione)
– Phenyl group and ethyl group are attached at
position 5.
• Physical properties
– White to colorless crystalline powder
– Very slightly soluble in water, soluble in ethanol.
Phenobarbitone sodium is soluble in water.
– Sensitive to light and moisture.
– Odorless
– MP 174-178°C.
• Stability and Storage
– Store protected from light and moisture
• Uses
– Sedation
– Hypnosis
– Seizure
– Insomnia
– Status epilepticus
Antidepressants
• These are the drugs that can elevate mood in
depressive illness.
• Depression is a condition characterized by sad
mood, lack of interest and pleasure, less
energy, agitation, change in appetite and sleep,
suicidal thoughts.
Imipramine
• Chemistry
– It is the derivative of 10, 11
dihydrodibenzoazepine.
– Dimethyl amino propyl group is attached at
position 5.
• Physical properties
– Official as Imipramine HCl
– Occurs as white or slightly yellow crystalline
powder.
– Freely soluble in water and ethanol.
– Sensitive to light, moisture and excess heat.
– MP: 168-170°C.
• Stability and Storage
– Store protected from light, moisture and high
temperature.
• Uses
– Depression and related illness
Amitriptyline
• Chemistry
– It is the derivative of dibenzocycloheptane.
– Dimethyl amino propyl group is attached to
position 5 by double bond.
• Physical properties
– Official as Amitriptyline HCl
– Exists as white to almost white crystalline powder.
– Freely soluble in water and ethanol
– Hygroscopic and degrades when exposed to air.
– Almost odorless.
– MP 196-197°C.
• Stability and Storage
– Hygroscopic and degrades when exposed to air.
– Store in a well closed container.
• Uses
– Depression
– Prophylaxis of migraine
– Postherpetic neuralgia (nerve pain)
Antiepileptics
• Antiepileptics: Antiepileptics, also known as
antiseizure medications or anticonvulsants, are a
class of drugs used to prevent or reduce the
occurrence of seizures in individuals with epilepsy.
• Epilepsy is a neurological disorder characterized by
recurring seizures, which are caused by abnormal
electrical activity in the brain. Antiepileptic drugs
work by suppressing or controlling this abnormal
activity to prevent seizures.
• Anticonvulsants: Anticonvulsants, as
mentioned earlier, are synonymous with
antiepileptics. They refer to a group of
medications used to manage seizures and
prevent their recurrence in individuals with
epilepsy.
• The primary goal of anticonvulsant therapy is
to control seizures and improve the quality of
life for people living with epilepsy.
Anticonvulsants may also be used to treat
other conditions, such as bipolar disorder,
neuropathic pain, and mood disorders.
Carbamazepine
• Chemistry
– Derivate of iminostilbene (dibenzoazepine)
– Amide group at position 5
• Physical properties
– Occurs as white or yellowish white crystalline
powder.
– Practically insoluble in water, sparingly soluble in
ethanol.
– Sensitive to moisture
– Exhibits polymorphism.
– MP: 190-193°C.
• Stability and Storage
– Store in tightly closed container.
• Uses
– Epilepsy
– Trigeminal neuralgia (nerve pain)
– Post herpetic neuralgia
– Schizophrenia
– Bipolar mania
Phenytoin 1

• Chemistry
– Derivative of imidazolidine 2,4 dione (hydantoin)
– 2 phenyl group at position 5
– Two carbony group are also present
– It consists of two nitrogen at position 1 and 3.
• Physical properties
– Official as phenytoin sodium
– Occurs as white powder
– Soluble in water and alcohol.
– Hygroscopic in nature, light sensitive
– Odorless
– MP: 286-296°C
• Stability and Storage
– Hygroscopic in nature and also affected by light.
So, store in tightly closed container protected
from light.
• Uses
– Seizure
– Status epilepticus
– Anticonvulsant
Valproic acid

• Chemistry
– Chemically it is 2-propyl pentanoic acid.
– Sodium valproate is sodium salt of valproic acid.
• Physical properties
– Official as sodium valproate
– Occurs as white or almost white crystalline
powder.
– Very soluble in water and ethanol.
– Hygroscopic in nature
– MP 300°C (sodium valproate)
• Stability and storage
– Store in a tightly closed container.
• Uses
– Complex partial seizure
– Absence seizure
– Migraine
– Bipolar mania
 Antiparkinsons drugs
• Antiparkinsonian drugs are medications used
to manage the symptoms of Parkinson's
disease, a neurological disorder characterized
by tremors, stiffness, slow movement, and
impaired balance.
• These drugs aim to increase dopamine levels
in the brain or mimic the action of dopamine to
alleviate symptoms
• Eg: Levodopa, carbidopa
 Levodopa

• Levodopa (L-Dopa): Levodopa is the most effective

medication for relieving the motor symptoms of
Parkinson's disease. It is converted into dopamine in
the brain, supplementing the deficiency caused by
the disease.
• Chemistry
– It is cathecholamine derivative.
– It consists of a chiral center and consists of four different
groups.
• Hydrogen
• Methyl group
• Carboxylic acid
• Amino group
 Catecholamines
• These are monoamines that have catechol and
a amine side chain.

catechol
67
• Physical properties
– Occurs as white or almost white crystalline powder.
– Levodopa is sparingly soluble in water but more
soluble in polar organic solvents like ethanol and
methanol.
– MP: 295-297°C

Storage: Store in a tightly closed container.

• Uses:
• It is used to treat symptoms of Parkinson's disease
(stiffness, tremors, spasms, poor muscle control).
• Levodopa is often combined with another
medication called carbidopa to enhance its
effectiveness and reduce side effects.

•
 Carbidopa

• Chemistry
– It is cathecholamine derivative.
– Also contains hydrazine molecule.
• Physical properties
– Occurs as white or almost white crystalline powder.
– Levodopa is sparingly soluble in water but more
soluble in polar organic solvents like ethanol and
methanol.
– MP: 276-282°C
Storage: Store in a tightly closed container.
• Uses:
• It is used to treat symptoms of Parkinson's disease (stiffness,
tremors, spasms, poor muscle control).
• Carbidopa is often combined with another medication called
Levodopa to enhance its effectiveness and reduce side effects.

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