Anti-psychotics Flashcards
Found to improve psychosis and block dopamine receptors
Chlorpromazine
The first generation antipsychotics are
Haloperidol and the -azine’s
For the first generation or typical antipsychotics, the primary antipsychotic effect is from
D2 receptor blockade
Found on post synaptic CNS neurons
-G-protein coupled
D2 receptors
Activates adenylyl Cyclades which increases cAMP
D1 receptors
Inhibits adenylyl Cyclades which decreases cAMP
D2 receptors
What is the effect of a D2 blockade?
Increase in cAMP
Depresses nervous system activity
Neuroepileptics
Motor dysfunction associated with decreased CNS dopamine
-Tremors and rigidity
Parkinson’s disease
Has the pharmacological characteristics of: a1 = 5-HT which is greater than D2 effects
Chlorpromazine
Has the pharmacological characteristics of effect of: D2 effects are greater than a1, which are greater than 5HT, which are greater than H1
Haloperidol
Which Typical antipsychotics are used as anti-emetics?
Prochlorperazine/chlorpromazine
Some typical antipsychotics cause an ACh muscarinic receptor blockade, which results in
Dry mouth and constipation
The alpha-1 blockade seen in typical antipsychotics results in
Hypotension
Response to dopamine receptor blockade
-Movement side effects
Extrapyramidal Symptoms
Acute side effect of dopamine receptor blockade
-Involuntary contraction of muscles
Dystonia
Anticholinergic that blocks M1 receptors and improves dystonia
Benztropine
Occurs within days following dopamine receptor blockade
-Most common EPS adverse effect
Akathisia
Restlessness, urge to move that is sometimes misdiagnosed as worsening agitation
Akathisia
Drug-induced Parkinsonism that begins weeks after starting an anti-psychotic
Bradykinesia
What can we use to treat the anti-psychotic induced Bradykinesia?
Benztropine
Can occur months to years after starting an anti-psychotic
-Common symptom is choreoathetosis
Tardive Dyskinesia
Irregular migrating contractions and twisting/writhing of the mouth, tongue, face, and limbs
Choreoathetosis
Is often irreversible, meaning that stopping the drug doesn’t help
Choreoathetosis
What are the three high potency typical antipsychotics
-Little effects on histamine and muscarinic receptors
Haloperidol, trifluoperazine, and fluphenazine
The high potency typical antipsychotics haloperidol, trifluoperazine, and fluphenazine are all at high risk for
Extrapyramidal Side Effects (EPS)
The two low potency typical antipsychotics with less EPS are?
Thioridazine and chlorpromazine
Have more non-neurological side effects like sedation and dry mouth
Thioridazine and chlorpromazine
Rare, dangerous reaction to neuroleptic
-Usually starts 7-10 days after treatment has started
Neuroleptic Malignant Syndrome (NMS)
Characterized by fever and rigid muscles with mental status changes (encephalopathy)
NMS
A sign of muscle damage in NMS is elevated
Creating kinase
To treat NMS, give
Dantrolene (muscle relaxant) and Bromocriptine (dopamine agonist)
Similar in presentation to malignant hyperthermia
NMS
May block cardiac potassium channels, which prolongs the QT interval
Typical Antipsychotics
May cause corneal deposits and may accelerate aging of the lens
Chlorpromazine
Causes retinal deposits and may cause “browning” of vision
Thioridazine
What are the 2nd generation antipsychotics?
-apines and -idones
The defining feature of atypical antipsychotics is less
EPS adverse effects
What are the pharmacological characteristics of clozapine as far as it’s receptor affinity:
Bigger affects on a1 than 5-HT which are bigger than D2
Have fewer EPS and anti-cholinergic effects but may prolong QT interval
Antipsychotics
May occur with any antipsychotic, but is especially common with clozapine and olanzapine
Metabolic Syndrome
Toxic to bone marrow and has the defining side effect o agranulocytosis
Clozapine
We must monitor WBCs during therapy with
Clozapine
Antipsychotics are the most common drug-induced cause of
Hyperprolactinemia
Dopamine blockade causes increases in prolactin. This leads to:
- ) In Men?
- ) In Women?
- ) Gynecomastia
2. ) Amenorrhea
The highest rates of Hyperprolactinemia are seen with which drugs
- ) Typicals?
- ) Atypicals?
- ) Haloperidol and Fluphenazine
2. ) Risperidone and Paliperidone
A partial D2 agonist that has less dopamine blockade adverse effects
Aripiprazole
The most common side effect of aripiprazole is
Akathisia