TRANS 070: PSYCHOPHARMACOLOGY Flashcards
subtype of antipsychotic drug that produces a high incidence of extrapyramidal side effects (EPS) at clinically effective doses
Neuroleptic
is the primary indication for antipsychotic drugs
Schizoprenia
INDICATIONS OF ANTIPSYCHOTIC DRUGS
- Schizophrenia is the primary indication for antipsychotic drugs
- Schizoaffective disorders
- Manic phase in bipolar affective disorder
- Monotherapy of acute bipolar depression
- Adjunct in the treatment of unipolar depression
- Agitation (e.g., haloperidol)
- Inability to distinguish between what is real and what is not
- Presence of delusions (false beliefs)
- Various types of hallucinations, usually auditory or visual, tactile, or olfactory
- Grossly disorganized thinking in a clear sensorium
psychosis
- Characterized mainly by a clear sensorium but a marked thinking and perceptual disturbance
- Most common psychotic disorder, present in about 1% of the population
- Considered to be neurodevelopmental disorder
- Studies have established that this is a genetic disorder with high heritability
Schizoprenia
Psychosis is not unique to schizophrenia and is [not present/always present] in all patients with schizophrenia at all times.
not present
identify if this is positive or negative symptom in Schizoprenia?
Hallucinating visually, audibly
Delusional Thinking
Disorganized Thinking
Agitated or Repetitive Movements
Positive
identify if this is positive or negative symptom in Schizoprenia?
Flat Affect
Anhedonia
Extreme Isolation
Resemble Clinical Depression
Negative
is a key factor in the mechanism of action of the main class of second-generation antipsychotic drugs,
5-HT2A-receptor blockade
prototype of 5HT 2A receptor blockade
clozapine is the prototype.
These drugs are inverse agonists of the 5-HT2A receptor; that is, they block the constitute activity of these receptors.
Clozapine. 5HT 2A receptor blockers
These receptors modulate the release of dopamine, norepinephrine, glutamate, GABA, and acetylcholine, among other neurotransmitters in the cortex, limbic region, and striatum.
5HT 2A
[Stimulation/Inhibition] of the serotonergic receptors leads to inhibition of cortical and limbic dopamine release.
Stimulation
Evidence suggest that [excessive/decreased] limbic dopaminergic activity plays a role in psychosis
excessive
[diminished/increased] cortical or hippocampal dopaminergic activity has been suggested to underlie the cognitive impairment and negative symptoms of schizophrenia
Diminished
major excitatory neurotransmitter in the brain
Glutamate
are noncompetitive inhibitors of the NMDA receptor that exacerbate both cognitive impairment and psychosis in patients with schizophrenia. (2)
Phencyclidine and Ketamine
Selective 5-HT2A antagonists, as well as atypical antipsychotic drugs, are much [more potent/less potent] than D2 antagonists in blocking these effects of PCP
more potent
hypofunction of NMDA receptors, located on GABAergic interneurons, leading to [increased/diminished] inhibitory influences on neuronal function, contributed to schizophrenia.
Diminished
Also known as neuroleptics, conventional or typical antipsychotics
First Generation Antipsychotics
Alleviate positive symptoms of schizophrenia
Have significant potential to cause extrapyramidal side effects and tardive dyskinesia
First Gen Antipsychotics
is the primary difference between FGAs and second-generation antipsychotics
propensity to cause movement disorders
- Low activity at histaminic and muscarinic receptors
- Associated with little sedation, weight gain, or anticholinergic activity, but a high risk for extrapyramidal side effects
high potency FGA (first gen antipsychotics)
haloperidol, fluphenazine are examples of?
High Potency FGA
Have high histaminic and muscarinic activity with a corresponding increased prevalence of sedation and anticholinergic effects
• Have lower risk of extrapyramidal side effects
Low Potency FGA
Chlorpromazine is an example of what drug classs?
Low Potency FGA
When you give FGAs you must also treat extrapyramidal side effects. T or F?
T
Aliphatic phenothiazine antipsychotic which blocks postsynaptic mesolimbic dopaminergic receptors in the brain
Chlorpromazine
exhibits a strong alpha-adrenergic blocking effect and depresses the release of hypothalamic and hypophyseal hormones
Chlorpromazine
Prototypical 1st gen antipsychotic and the FIRST ANTIPSYCHOTIC MEDICATION. First synthesized in France in 1952
Chlorpromazine
T or F? No antipsychotic has been shown to be significantly more effective than chlorpromazine in treating schizophrenia with the notable exception of clozapine
T
• Usual dose for schizophrenia of Chlorpromazine?
• Usual dose for schizophrenia: 200 – 800mg daily, in 2-4 divided doses
popular brand name of chlorpromazine?
Thorazine
adverse effects of chlorpromazine?
ADVERSE EFFECTS:
- EPS, sedation, weight gain, dry mouth, blurred vision, urinary retention, constipation, orthostatic hypotension
Butyrophenone antipsychotic that non-selectively blocks postsynaptic dopaminergic D2 receptors in the brain
• Available in oral and parenteral (IM, IV preparations)
Haloperidol (haldol)
what preparation is used as a rapid tranquilizer to control acute episodes of agitation and violence in patients with schizophrenia. (Dose: 2.5mg – 10mg
IM
Piperazine phenothiazine antipsychotic which blocks non-selectively postsynaptic mesolimbic dopaminergic D2 receptors in the brain
FLUPHENAZINE DECANOATE
Commonly used as a depot injection in cases of noncompliance to daily oral antipsychotic therapy
FLUPHENAZINE DECANOATE
Dose of FLUPHENAZINE DECANOATE
Dose: 6.25 to 25 mg every 2 weeks; the effects of a single injection may last 4 to 6 weeks
Adverse effects? FLUPHENAZINE DECANOATE
ADVERSE EFFECTS:
- EPS, increased risk for tardive dyskinesia
involuntary choreoathetoid movements of the mouth, tongue, face, extremities, or trunk, including lip-smacking, tongue writhing, or thrusting jaw movements, facia grimacing, and trunk or extremity writhing
Tardive dyskinesia
fever, muscle rigidity, mental status changes, and autonomic instability, generally accompanied by rhabdomyolysis and creatine kinase elevation
Neuroleptic malignant syndrome
menstrual irregularities, infertility, galactorrhea, loss of libido, and erectile and ejaculatory dysfunction
Prolactin Elevation
Constitute the bulk of antipsychotics nowadays
Generally, have lower risk of extrapyramidal side effects and tardive dyskinesia compared with first generation antipsychotics
SECOND GENERATION ANTIPSYCHOTICS (SGA1)
Alleviate both positive and negative symptoms of schizophrenia
SECOND GENERATION ANTIPSYCHOTICS (SGA1)
useful for treatment-resistant schizophrenia
Clozapine
is the most powerful antipsychotics under second generatio
Clozapine
Second generation antipsychotics as a group usually has [more/less] extrapyramidal symptoms; the side effects are usually metabolic
less
MOA of SGA
Post synaptic blockade of brain dopamine (D2) receptors,
Aripirazole and Brexipiprazole: MOA?
Aripirazole and Brexipiprazole: D2 receptor partial agonist
MOA Cariprazin
Cariprazin: D3/D2 receptor partial agonist
MOA Pimavenserin
Serotonin HT2A inverse agonist and antagonist
Prototype SGA
CLOZAPINE (CLOZARIL)
strongest affinity for muscarinic receptors (kaya madaming anticholinergic symptoms) among the SGAs and patient reports of side effects are most frequent
CLOZAPINE (CLOZARIL)
May cause agranulocytosis in up to 2% of patients
Dose-related lowering of seizure threshold
- Associated with potentially fatal cases of myocarditis and cardiomyopathy
- Changes in blood pressure, heart rate
- Anticholinergic side effects: Dry mouth, sialorrhea (excessive salivation), constipation
CLOZAPINE (CLOZARIL)
Pagnaka CLOZAPINE. Madalas may CBC monitoring to check