Anti Psychotic Drug...Report

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    ANTIPSYCHOTIC

    DRUGS

    REPORTED BY REX MENDOZA

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    Psychosis

    Losing contact with reality

    Characterized by more than onesymptom, but these may include

    difficulty in processing information and

    coming to a conclusion, delusions ,hallucinations, incoherence, catatonia

    and aggressive or violent behavior.

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    Modes of Action

    All anti-psychotic drugs have inhibitoryeffects on the D2 receptor

    Some have actions against the D4receptor

    All have other effects - to varyingdegrees

    Serotonin blockade (may improvenegative symptoms)

    Histamine H1 blockade (drowsiness)

    Alpha adrenoceptor blockade (postural

    hypotension)

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    Clinical Effects

    Control the positive features of the disease,but little effect on the negative features(clozapine may be superior in this regard)

    The main side-effects are on theextrapyramidal motor system - leading torigidity, tremor, and loss of mobility anddyskinesia

    Tardive dyskinesia is a late onset disordercharacterised by repetitive abnormalmovements of face and upper limbs. Thismay be due to proliferation of D2 receptors in

    the striatum

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    Clinical Effects

    Newer atypical anti-psychotic drugs

    are less inclined to produce these

    effects - possible due to their greateraffinity for the mesolimbic over the

    striatal areas of the brain

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    Other Effects

    some are effective anti-emetics

    anti-muscarinic effects lead to dry mouth, blurredvision, difficulty with micturition

    Eantagonist effects lead to hypotension antihistamine effects (H1 receptor) lead to

    drowsiness

    prolactin stimulation may lead to breastdevelopment

    agranulocytosis is fairly common with an atypicaldrug - clozapine

    Neuroleptic malignant syndrome is a rare butserious effect leading to autonomic instability andhyperthermia

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    Classification of anti-

    psychotic drugs classical/ typical

    chlopromazine (gen)

    haloperidol (gen)

    fluphenazine (gen)thioridazine (auth)

    note: classification isbased on fewer EPS

    side-effects,fewer long-term ADRs, efficacy in

    treatment-resistantgroups, negative

    symptoms

    atypical

    clozapine (sec100)

    risperidone (auth)olanzapine (auth)

    quetiapine (auth)

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    Phenothiazines

    Pharmacologic effects:

    (2) autonomic nervous system: block -

    adrenergic and M-Cholinergic receptors andresult in hypotension, dry mouth,

    constipation and blurred vision.

    (3) Endocrine system: increase the release

    of prolactin and decrease corticotropin

    release and secretion of pituitary growth

    hormone.

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    Therapeutic uses

    (1) treatment of psychotic disorders:schizophrenia, mania, paranoid states,alcoholic hallucinosis.

    (2) treatment of nausea and vomitingof certain causes.

    (3) anesthesia in hypothermia and

    artificial hibernation (used withpethidine and promethazine).

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    Adverse Effects

    Extrapyramidal motor disturbances: (1)

    Parkinson-like symptoms; (2) akathisia;

    (3) acute dystonias.

    Treatment: anticholinergic

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    Adverse Effects

    Tardive dyskinesia comprises mainly

    involuntary movements of face and

    tongue, but also of trunk and limbs,appearing after months or years of

    antipsychotic treatment. It may be

    associated with proliferation of

    dopamine receptors (possiblypresynaptic) in corpus striatum.

    Treatment is generally unsuccessful.

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    Adverse Effects

    Pseudodepression and Schizophrenia-

    like syndrome.

    Seizures. Cardiac toxicity and endocrine effects.

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    Adverse Effects

    Other side-effects (dry mouth,constipation, blurred vision,hypotension, etc.) are due to block ofother receptors, particularly adrenoceptors and muscarinic AChreceptors.

    Contact dermatitis, blood dyscrasias,obstructive jaundice sometimes occurswith phenothiazines.

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    Thioxanthenes

    Chlorprothixene: mild antipsychotic

    action, and antianxiety and

    antidepressant action.

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    Butyrophenones

    Haloperidol: control psychomotor

    excitement.

    Adverse effects: severe extrapyramidalsymptoms.

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    Others

    Clozapine:

    (1) be effective in treating some

    patients with psychosis unresponsiveto standard neuroleptic drug.

    (2) blocks D4 receptor and have lowaffinity for D1 and D2 dopamine

    receptors. (3) lacks extrapyramidal side effects.

    (4) must monitor the granulocyte

    counts weekly.

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    Others

    Risperidone: be used first episode in

    and chronic schizophrenia.