Pharmacology of Antipsychotic Drugs Flashcards
What disease do antipsychotic drugs treat
Schizophrenia
How do ALL antipsychotic drugs control symptoms
Inhibit dopamine transmission
What are the receptors in the D1 family
D1 receptors, D5 receptors
Which type of antipsychotics block the D1 receptors
Phenothiazines
What receptors are located in the limibc system, amygdala
D3 and D5, D4
What are the receptors in the D2 family
D2 receptors, D3 receptors, D4 receptors
What receptors in the D2 family are blocked by all antipsychotics
D2 receptors
T/F: The dopamine receptors that are encountered for schizophrenia are all post synaptic
True
Which dopamine receptor does clozapine have the highest affinity for
D4
Are dopamine autoreceptors post-synpatic or pre-synaptic, what happens when encountered with an agonist, antagonists
Pre-synaptic, inhibits release of dopamine, increases dopamine release
What is the pathophysiology of schizophrenia
Hyperactivity of dopamine in the mesolimbic pathway (positive symptoms) and hypoactivity of dopamine in the mesocortical pathway
What are the 4 most used phenothiazines
Chlorpromazine, thioridazine, trifluoperazine, fluphenazine
What is the thioxanthene used in schizophrenia
Thiothixene
What is the butyophenones, what receptors does it interact with
Haloperidol, alpha-1 and D2
What are the antipsychotics considered others
Molindone, loxapine, reserpine
What are the mixed antagonists antipsychotics
Clozapine, Olanzapine, quetiapine
What are the seotonin dopamine antagonists, which has alpha-1 activity
Risperidone, plaiperidone, ziprasidone, iloperidone, asenapine, lurasidone/ risperidone
What are the dopamine partial agonist and 5-HT2A antagonists
Aripiprazole, Brepiprazole, Cariprazine
T/F: Antipsychotics cure scizophrenia
False: Antipsychotics supress psychotic behavior but DO NOT CURE IT
How long does it take for antipyschotics to have full onset of action, which takes up to 12 weeks
2-6 weeks, clozapine
How does serotonin affect dopamine
The more serotonin available the less dopamine available
What is the MOA of atypical APs, How is this special
5HT2 antagonism increases dopamine release in prefrontal cortex (mesocortical pathway), NO 5HT2 antagonism/link in mesolimbic pathway therefore only D2 antagonism in the Mesolimbic pathway
Why are the extrapyramidal side effects (shaking and slow movement) using APs
Blockade of D2 receptors in nigrostriatal pathway leading to excess acetylcholine
What drugs can be given to counter EPS side effects
Antimuscarinics: cover the ACH receptors on the GABA system causing less side effects
5HT2 antagonists: increases release of dopamine to outcompete the D2 antagonism keeping ACH and dopamine in balance
What is the mechanism of tardive dyskinesia, which antipsychotics cause this
Prolonged blockade of D2 receptors leads to hypersensitivity of D2 receptors, typical
What are the antimuscarnic side effects of antipsychotics
Urinary retention, constipation, blurred vision, dry mouth drowsiness
What are the antiadrenergic effects of antispychtics
Decreased blood pressure, dizziness, drowsiness
What are the antihistamine effects of antipsychotics
Weight gain and sedation
What AP causes agranulocytosis
Clozapine
T/F: All antipsychotics lower the seizure threshold with clozapine needing the most caution
True
What does blocking dopamine in the tuberoinfundibular pathway cause
elevate prolactin
What are the effects of pure D2 antagonism in the mesolimbic pathway, mesocortical pathway, nigrostriatal pathway, tuberoinfundibular pathway
Reduced positive symptoms of schizophrenia and lack of pleasure and reward, increased negative symptoms of schizophrenia, parkinsonism (EPS), elevated prolactin
What are the benefits of of using serotonin anatagonists in schizophrenia patients and dopamine partial agonist
NO parkinsonism, No elevated prolactin, reduces positive symptoms and reduced negative symptoms
