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    Antipsychotics: Presented by

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    Kiran
    Antipsychotics are used to treat psychoses like schizophrenia by depressing the central nervous system and reducing dopamine levels. This helps reduce hallucinations, delusions, and abnormal behavior while facilitating social adjustment. Major classes of antipsychotics include phenothiazines, thioxanthenes, dibenzazepines, butyrophenones, and others. The mechanisms and structures that increase their antipsychotic effects involve electron-withdrawing groups on phenothiazine rings, piperazine side chains, and tertiary nitrogen groups on side chains.

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    Antipsychotics: Presented by

    Uploaded by

    Kiran
    159 views21 pages
    Antipsychotics are used to treat psychoses like schizophrenia by depressing the central nervous system and reducing dopamine levels. This helps reduce hallucinations, delusions, and abnormal behavior while facilitating social adjustment. Major classes of antipsychotics include phenothiazines, thioxanthenes, dibenzazepines, butyrophenones, and others. The mechanisms and structures that increase their antipsychotic effects involve electron-withdrawing groups on phenothiazine rings, piperazine side chains, and tertiary nitrogen groups on side chains.

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    Antipsychotics

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    Antipsychotics are used to treat psychoses like schizophrenia by depressing the central nervous system and reducing dopamine levels. This helps reduce hallucinations, delusions, and abnormal behavior while facilitating social adjustment. Major classes of antipsychotics include phenothiazines, thioxanthenes, dibenzazepines, butyrophenones, and others. The mechanisms and structures that increase their antipsychotic effects involve electron-withdrawing groups on phenothiazine rings, piperazine side chains, and tertiary nitrogen groups on side chains.

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    159 views21 pages

    Antipsychotics: Presented by

    Uploaded by

    Kiran
    Antipsychotics are used to treat psychoses like schizophrenia by depressing the central nervous system and reducing dopamine levels. This helps reduce hallucinations, delusions, and abnormal behavior while facilitating social adjustment. Major classes of antipsychotics include phenothiazines, thioxanthenes, dibenzazepines, butyrophenones, and others. The mechanisms and structures that increase their antipsychotic effects involve electron-withdrawing groups on phenothiazine rings, piperazine side chains, and tertiary nitrogen groups on side chains.

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    © All Rights Reserved
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    of 21

    Antipsychotics

    Presented By:
    Mr. Kiran D. Baviskar,
    Assist. Professor
    Dept. of Pharmaceutics,

    Smt. Sharadchandrika Suresh Patil College of Pharmacy, Chopda.


    Antipsychotics used to treat psychoses like schizophrenia,
    mania, sensile dementia and behavior disorders. These drugs
    act by depressing CNS (decreasing dopamine level) by
    producing sedation without producing sleep.

    Clinically, these agents counteract or minimize hallucinations


    and delusions, alleviate psychomotor excitement, and facilitate
    social readjustment.

    Antipsychotics are also known as neuroleptics (formerly


    ataractics and major tranquillizers) .
    Psychosisis a severe mental illness leading to impairment of
    thoughts. A psychotic disorder is usually characterized by
    withdrawal from reality and its symptoms are divided into two
    types:
     Positive and
     Negative.
    Positive psychosis symptoms include
    (i) auditory-, visual-, tactile, gustatory-hallucinations,
    (ii) delusions,
    (iii) disorganized thought and speech, and
    (iv) disorganized behavior.
    Negative psychotic symptoms include
    (i) decrease or complete loss of the ability to emotionally
    respond to people,
    (ii) decrease in speaking, and
    (iii) difficulty sticking with activities and tasks (abolition), for
    instance getting dressed in the morning.

    Positive psychosis symptoms are exceedingly first associated


    with schizophrenia (abnormal social behavior and failure to
    respond to reality) and then with post-traumatic stress
    disorder.
    Antipsychotic drugs (also called neuroleptics) are primarily
    used in the therapy of psychoses, including schizophrenia,
    organic psychoses, the manic phase of manic-depressive
    illness and other acute or chronic idicpathic' psychotic
    illnesses.
    Antipsychotics are not CNS depressants.
    Nuclear neuroimaging findings suggested that psychiatric
    patients correspond to increased dopamine level in brain.
    Therefore, drugs inhibiting dopaminergic
    neurotransmission have been clinically used in the
    management of several neurological and psychiatric
    disorders.
    Antipsychotics are mainly classified as follows:

    Phenothiazine derivatives- Chlorpromazine, Fluphenazine

    Thioxanthene derivatives- Chlorprothixene

    Dibenzazepines- Loxapine, Clozapine

    Butyrophenons- Haloperidol, Droperidol


    Dihydroindolones- Molindone, Oxypertine

    Diphenylbutylpiperdines- Pimozide, Penfluridol

    Benzamide -Sulpiride, Clebopride

    Miscellaneous.
    SAR of Antipsychotics:
    Phenothiazines are the derivatives of phenothiazine tricyclic
    heterocyclic moiety. The central ring possesses nitrogen and
    sulphur heteroatoms.

    1.Substitution at the second position of phenothiazine nucleus


    by electron withdrawing substituent increases antipsychotic
    activity. Ex: Chlorpromazine (chlorine).

    2. Substitution at the 3-position of phenothiazine nucleus


    increases antipsychotic activity than unsubstituted derivatives
    but not by substitution at 2-position.

    3. Substitution at 1 and 4 positions of phenothiazine nucleus


    reduces the antipsychotic activity.
    4. Phenothiazines must have a nitrogen-containing side-chain
    substituent on the ring nitrogen for antipsychotic activity. The
    ring and side-chain nitrogen must be separated by a three
    carbon chain.

    5. The side chains are either aliphatic, piperazine, or piperidine


    derivatives. Piperazine side chains confer the greatest potency
    and the highest pharmacological selectivity.

    6. Fluphenazine and long chain alcohols form stable, highly


    lipophilic esters, which possess markedly prolonged activity.
    7. Substitution on the side chain with a'large or polar group
    such as phenyl, dimethylamino or hydroxyl results in loss of
    tranquilizing activity.

    8. Side chain containing N-atom should be tertiary for


    optimum activity. The two methyl group gives maximum
    activity but if anyone of them derivatised cause decrease in
    activity.

    9. Side chain containing 3 carbon atoms gives neuroleptic


    activity whereas 2 carbon atom chain shows antihistaminic
    and anticholinergic activity.

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