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8/6/2019 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.