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mania
Psychoses
False
perceptions (Hallucinations)
False
beliefs (Delusions)
Affective Disorders
Emotional
disturbances:
Mood is very low (Depression)
Mood is very high (Mania)
Schizophrenia
Most
Types of Schizophrenia
Paranoid
Disorganised
Catatonic
forms
Symptoms
Positive
Antipsychotic Drugs
Mechanisms
of action
-competitive blockade of dopamine receptors
and serotonin receptors
-adverse effect result from blockade of different
receptors
Antagonism
of D2 receptors in mesolimbic
pathways suppress the positive symptoms of SCh
Blockade of D2 receptors in the basal ganglia is
responsible for parkinsonian and other
extrapyramidal side effects of anti psychotic drugs
Some
Continued
Dopamine reduction causes dopamine upregulation and super sensitivity to dopamine
agonists and then delayed extrapyramidal side
effect called tardive dyskinesia.
In mesocortical and nigrostriatal pathways, 5HT2 receptors mediate presynaptic inhibition of
dopamine release.
Blockade of 5-HT2 receptors by atypical drugs
increase dopamine release in these pathways.
Continued
In mesocortical pathway, this action alleviate
negative symptoms of Sch.
In nigrostriatal pathway, increased dopamine
release counteracts the extrapyramidal side
effects caused by D2 receptor blockade.
Drug Classification
Typical
antipsychotic drugs
-Phenothiazines
-Thioxanthenes
-Butyrophenones
- some Azepines (eg loxapine)
Atypical antipsychotic drugs
-other Azepines (clozapine, olanzapine)
-Benzisoxasole (risperidone)
Phenothiazines
Chlorpromazine,
Fluphenazine, Thioridazine,
Trifluoperazine
Similar therapeutic effects
Different potency and side effect
Chlo. And Thio. lower potency, more autonomic
side effects and fewer extrapyramidal side
effects than high potency
Flu. Higher potency
of D2 receptors
weeks
Less agitated, fewer auditory hallucinations,
disappear of paranoid delusions
Behavioural improvement
Adverse effects
1- Extrapyramidal side effects
-Acute: 1- Akathisia
2- Pseudoparkinsonism
3- Dystonias
-Chronic: Tardive dyskinesia
continued
2- neuroleptic malignant syndrome
3-increase serum prolactin levels
4-impair thermoregulation cause poikilothermy
Continued
Neuroleptic malignant syndrome
Supportive care
Discontinuing of drug
Administration of bromocryptine
Change to atypical
Indication of Phenothiazines
Schizophrenia
Drug-induced
psychosis
Psychosis associated with the manic phase of
bipolar disorder.
Dementia
Severe mental retardation
Some of them for management of nausea and
vomiting
activity
And so fewer extrapyramidal side effect
High doses of thioridazine cause pigmentary
retinopathy and cardiac arrythmia
Thioxanthenes
Thiothixene
Butyrophenones
Haloperidol
Azepines
Loxapine
(atypical)
Loxapine properties are similar to phenothiazines
Clozapine has fewer extrapyramidal side effect
and greater activity against negative symptoms
and its use is with 1.3% first year incidence of
potentially fatal agranulocytosis.
Other atypical drugs are amisulpride, quetiapine,
risperidone and zotepine.
continued
Olanzapine
is:
As effective as haloperidol in alleviating of
positive symptoms.
Superior to haloperidol in alleviating of
negative symptoms.
Fewer extrapyramidal side effects
At high doses may cause akathisia,
pseudoparkinsonism, and dystonias.
Risperidone
Its
Antidepressant drugs
1.
2.
3.
4.
Tricyclic antidepressants
Selective serotonin reuptake inhibitors (SSRI)
Monamine oxidase inhibitors (MAOI)
Others
Tricyclic antidepressants
Amitriptyline, nortriptyline, imipramine,
clomipramine, desipramine
They block neuronal reuptake of NE and serotonin,
but at different degrees
Side effects:
Autonomic side effects by blocking muscarinic
and a-adrenergic receptors, sedation, induce
seizure, orthostatic hypotension
Overdose cause life-threatening cardiac arrythmia.
Indications
Depression
Phobic,
They
Adverse effects
Fewer
Indications
Depression
Eating
Others (Atypical)
1.
2.
3.
4.
Continued
1.
2.
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