Antipsychotics (Tranquilizers) - PowerPoint Presentation

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Antipsychotics

(Tranquilizers)

Antipsychotic drugs

•

Antipsychotic drugs (also called neuroleptics or tranquilizers) are used

primarily for the treatment of symptoms in mental diseases,

their overall influence being to free the mind from passion or disturbance and thus calm the mind i.e.,

they cause sedation without inducing sleep.

They are also effective in other psychotic states, including manic states with psychotic symptoms such as grandiosity, paranoia, and hallucinations, and delusions.

•

Antipsychotic drugs are not curative and do not eliminate the chronic thought disorder, but they often decrease the intensity of hallucinations and delusions and permit the person with schizophrenia to function in a supportive environment.

•

Tranquilizers are drugs essentially used in the management and treatment of psychoses and neuroses.• They specifically exert their action on the lower brain areas to produce emotional calmness and relaxation without appreciable hypnosis sedation.

Many of these drugs also display clinically beneficial actions like skeletal muscle relaxants, antihypertensive, antiemetic and antiepileptic properties.

Antipsychotics

may be defined as drugs which ameliorate mental aberrations (

deviation from the normal

) that are invariably characteristic features of the psychoses.

History of antipsychotic drugs

• Antipsychotic drugs have been used in Western medicine for more than 50 years.

• Chlorpromazine (1952) and Reserpine were the first drugs found to be useful in schizophrenia.

• Major novel antipsychotics are selective serotonin reuptake inhibitor and it has been introduced in 1980s.

• Little attention was paid to Cade's report in 1949 that Lithium could be used for excitement and mania: its effective use started in the 1960s and now it has a unique place in psychiatry.

Classification of antipsychotic drugs

•

PHARMACOLOGICAL CLASSIFICATION

– FIRST-GENERATION ANTIPSYCHOTIC (low potency)

• Chlorpromazine

•

Prochlorperazine • Thioridazine

– FIRST-GENERATION ANTIPSYCHOTIC (high potency)

• Fluphenazine

• Haloperidol • Pimozide • Thiothixene

– SECONDGENERATION ANTIPSYCHOTIC

•

Aripiprazole

•

Iloperidone

•

Paliperidone

•

Asenapine

•

Lurasidone

•

Quetiapine

•

Clozapine

•

Olanzapine

•

Risperidone

•

Ziprasidone

Classification of antipsychotic drugs

 • CHEMICAL CLASSIFICATION

Antipsychotics

may be classified under the following categories, namely

Reserpine and Related Alkaloids:

Eg.Reserpine

,

Deserpidine

Alkylene Diols:

Eg

. Meprobamate, Tybamate

Diphenylmethane Compounds: Eg. Pipradrol, CaptodiamePhenothiazine Compounds:

Eg

. Chlorpromazine,

Perphenazine

,

Thioridazine

Dibenzazepines:

Eg

.

Loxapine

,

Clozapine

Butyrophenones:

Eg

. Haloperidol,

Droperidol

Azaspirodecanediones:

Eg

.

Buspirone

SYNTHESIS OF SOME ANTIPSYCHOTICS

Pipradrol

:

Uses:

It is used for the treatment of functional fatigue

and

various types

of depressions

Dose:

Usual, 2.5 mg twice daily.

It is synthesized by the reaction of phenyl-2-pyridyl

ketone

with phenyl magnesium

bromide (Grignard reagent) followed by catalytic reduction.

Captodiame

hydrochloride

Synthesis:

Butylphenyl thioether is first prepared by the interaction of

sodium

b

enzenethiolate

and butyl chloride.

The

resulting product on treatment with benzoyl chloride and AlCl

3

yields butyl-p-benzoyl

phenyl

thioether. This

on reaction with zinc and NaOH and carbonyl chloride yields an intermediate which on treatment with

thiourea

, NaOH, 2-dimethyl amine ethyl chloride and

HCl

gives rise to the desired product.

Uses :

It is used for the treatment of anxiety and tension.

It

is an excellent

nonhypnotic

sedative

Dose :

For anxiety and tension;

50 mg three times per day.

Chlorpromazine

Synthesis:

It is prepared by refluxing the toluene solution

of 2-chlorophenothiazine and 3-chloropropyl dimethylamine in the presence of sodamide for several hours, followed by filtration and removal of toluene under reduced pressure.

Uses:

It

is found to be effective in the management of manifestations of psychotic disorders and manic depressive illness, apprehension and anxiety and prior to surgery.

It is also used for the treatment of moderate to severe agitation.

Dose:

Adults-oral, 10 to 50 mg

2

or

3

times daily to a total

dose of 1 g daily.

Children- oral, 0.55 mg/kg every 4 to 6 hrs.