Tranquilizers

• A tranquilizer is a drug which is designed for the treatment of anxiety, fear, tension, agitation, and disturbances of the mind, specifically to reduce states of anxiety and tension.

• Psychoses mean mental condition raised by disturbance in mental function.

• Mental disease has always been puzzling and frightening things.

• They are quite different from other disease of mankind.

Psychoses may be:

1. Organic psychoses where there is memory distrurnace clouding of consciousness due to endocrinal abnormalities of head injury.

2. Functional psychoses may be:

a) Manic: disturbance of mood.

b) Schizophrenia in which there is disordered of thoughts emotions

c) Hallucinations

d) Anxiety where feeling of fear.

Classifications of Tranquilizers:

1. Phenothiazine derivatives and related tricyclic compound:

a) Phenothiazine derivatives: e.g. chlorpromazine, Prochlorperazine trifluoroperazine.

b) Thioxanthenes derivatives: e.g. chlorprothixene ,flupenthixol

2. Butyrophenones: e.g. haloperidol, trifluoperidol (Triperidol)

3. Dibenzodiazepines: e.g. clozapine

4. Benzamides and salicylamides e.g. Sulpiride

5. Diphenyl butyl piperidine derivatives: e.g. pimozide

6. Miscellaneous: e.g. Reserpine.

Chlorpromazine

Structure of Chlorpromazine:

Chemical name: 2-chloro, 10 (dimethyl amino propyl) phenothiazine.

Physical properties of Chlorpromazine:

• It is hydrochloride salt is white or cream coloured powder.

• It has slight odour.

• It is very soluble in water

• It is freely soluble in alcohol

• It is decomposed on exposure to light, becoming yellow to pink and finally violet.

Chemical properties of Chlorpromazine:

• When it is oxidised with conc. sulphuric acid it gives red colour.

• When it is treated with conc. Nitric acid, it oxides to give red coloured substance which on standing to becomes yellowish.

• It is also oxidised by ceric ammonium sulphtae solution.

Stability and storage of Chlorpromazine:

• It is discolored when exposed to light and hence it is stored in well closed light resistant containers.

Uses of Chlorpromazine:

It is used to treat:

• Schizophrenia

• Mania and hypomania

• Used to control nausea and vomiting.

• Used to produce pre and post-operative sedation, which enhance the effect of barbiturates and analgesics.

• It acts as vasodilators.

• It reduces the salivary and gastric secretion.

• It has local anesthetics property.

Pharmaceutical formulations: Chlorpromazine elixir, injection, tablets, suppositories

Brand names: Largactil, Chorozine, Copamide

Prochlorperazine

Physical properties of Prochlorperazine:

• It is official as maleate salt which is white to yellow crystalline powder.

• It is odourless

• It has slightly bitter taste.

• It is very soluble in water and alcohol.

Stability and storage of Prochlorperazine:

• It is affected by light hence it is stored in well closed light resistant containers.

Uses of Prochlorperazine:

• As under chlorpromazine

• It is less sedative and more effective as antiemetic

Pharmaceutical formulations: Prochlorperazine tablets, capsules

Brand names: Mentil, Stemetil

Trifluoperazine

Physical properties of Trifluoperazine:   

• It is official as a hydrochloride salt which is white or pale yellow crystalline powder.

• It is odorless.

• It has bitter taste.

• It is hygroscopic.

• It is freely soluble in water.

Stability and storage of Trifluoperazine:

• It is hygroscopic .it is oxidised by oxygen in presence of moisture and sunlight. Hence it is stored in well closed light resistant containers.

Uses of Trifluoperazine:

• As under chlorpromazine.

Pharmaceutical formulations: Trifluoperazine tablets, capsules, injections

Brand names: Stelabid, Eskazine, Siquil

Haloperiodol

Structure of Haloperiodol:

Chemical names: 4-[4-(p- chlorophenyl), 4 –hydroxy piperidine] 4’ –florobutyroohenone.

Physical properties of Haloperiodol:

• It is white to faint yellowish, amorphous or microcrystalline powder.

• It has odourless

• It has tasteless.

• It is practically insoluble in water

• It is sparingly soluble in alcohol.

Storage: stored in well closed containers.

Uses of Haloperiodol:

• Acute schizophrenia

• Mania and hypomania

• Behavioral disturbance

• Severe anxiety

• Childhood development disordered

• It is used as an antiemetic

• It potentiates the cation of CNS depressant like analgesic barbiturates, anesthetics

Pharmaceutical formulations: Haloperiodol tablets, injections, capsules, elixir

Brand names: Halidol, Tarncodol

Triperiodol

Physical properties of Triperiodol:

• It is white or yellowish crystalline powder

• It is odorless

• It is tastless

• It is practically insoluble in water.

Stability, storage, and uses as under haloperidol

Pharmaceutical formulations: Triperiodol tablets

Brand names: Triperidol

Chlordizepoxide

Physical properties of Chlordizepoxide:

• It is official as hydrochloride salt

• It is white crystalline powder.

• It has slightly odor

• It has very bitter taste.

• It is soluble in water.

Chemical properties of Chlordizepoxide:

• When it is hydrolysed it is converted to demoxepam with the removal of methyl amino group. 

• On further degradation it is converted to 2-amino, 5-chloro benzoquinone in which 4, 5 azeomethine linkage is ruptured.

Stability and storage of Chlordizepoxide:

• It is affected by air, moisture and sunlight hence it is stored in well closed light resistant containers.

Uses of Chlordizepoxide:

It is used to treat:

• Symptoms of anxiety

• Psychosomatic disordered

• Insomnia associated with anxiety

• Muscle spasm

• It is also used in premedication in anesthesia

Pharmaceutical formulations: Chlordizepoxide tablets, injections

Brand names: Tropium, Librium

Diazepam

Structure of Diazepam:

Chemical name: 7 Chloro, 2, 3 dihydro, 1 methyl 5 phenyl 1H-1 4 benzodizepine -2-one.

Physical properties of Diazepam:

• It is white pale yellow crystalline powder

• It is odorless

• It is tasteless first followed by bitter taste

• It is sparingly soluble in water

• It is soluble in alcohol,

Stability and storage of Diazepam:

• It is degraded by moisture and light.

• Hence it is stored in tightly closed light resistant containers

Uses of Diazepam:

• For management of anxiety and tension state.

• For management of acute alcoholic withdrawal.

• To relief from skeletal muscle spasm.

• To treat epilepsy

• To produce sedations

• To treat excitation state.

• As premedication for surgical dressing

Pharmaceutical formulations: Diazepam tablets, capsules, injections, elixir.

Brand names: Calmpose, sedanite

Lorazepam

Physical properties of Lorazepam:

• It is white to off white powder

• It is odorless

• It is practically insoluble in water

• It is slightly soluble in alcohol

Storage of Lorazepam:

• It is degraded by moisture and light. Hence it is stored in tightly closed light resistant containers

Treatment  of Lorazepam:

It is used to treat:

• For management of anxiety and tension state.

• Insomnia associated with anxiety

• Epileptic seizures (IV)

• As premedication for surgical dressing

Pharmaceutical formulations: Lorazepam tablets, injection

Brand names: Ativen, Lorapam, Alzapam

Meprobamate

Physical properties of Meprobamate:

• It is white crystalline powder or granular crystalline aggregates.

• It is odorless

• It has bitter characteristic state.

• It is slightly soluble in water

• Freely soluble in alcohol

Chemical properties of Meprobamate:

• When it is treated with dimethyl amino benzaldehyde solution in sulphuric acid a yellow colour is produced with changes to orange on standing.

Stability and storage: it is stored in well closed containers.

Uses of Meprobamate:

• For management of anxiety and tension state.

• Muscle skeletal relaxant

• Petit mal type of epilepsy

Pharmaceutical formulations: Meprobamte tablets, capsules, injection, oral suspensions

Brand names: Equanil, Cadiporm, PMT