Antipsychotic Agents
→ Treatment: mainly Schizophrenia
Drug Name Category / Conventional or Characteristics etc. Treated symptoms (mostly Side effects Side effects that are not First line.
Pharmacological Profile Atypical? besides antipsychotic effects) caused by this drug Second line,
(e.g. opposed to other drugs)
etc.
Clozapine • Serotonin 5HT2A- • “Prototypical” • Antipsychotics are generally dosed so that • Aggression and violence • Of all others, has greatest • few if any Most likely
(pine) Dopamine D2 atypical about 60% of D2 receptors are occupied • (Rare) “awakening” in from risk to develop extrapyramidal effects used when
Antagonist antipsychotic but that’s lower for clozapine of return to nearly normal level agranulocytosis (life • No dyskinesia other
• Serotonin-dopamine • Very complex pharmacological profile of cognitive, interpersonal and threatening, sometimes fatal) antipsychotics
• No elevated prolactin
antagonist (SDA) • Can show greater efficacy than other vocational functioning 0.5-2% of patients have failed.
atypical antipsychotics with 5HT2A • Reduces suicide risk - monitor blood count!
antagonism • May reduce tardive • Increased risk of seizures It’s the “gold
• Only antipsychotic to reduce suicide risk • Very sedating standard” for
dyskinesia severity (esp. long treating
treatment intervals • Excessive salivation
schizophrenia,
• Increased myocarditis risk
however,
• Weight gain because of its
(likely due to blockage of side effects, it’s
H1-histamine & 5HT2C not first line
receptors) treatment
Olanzapine • Serotonin 5HT2A- • Atypical • Chemical structure related to clozapine • Also used in bipolar disorder • Weight gain • lacks EPS (also at high When other
(pine) Dopamine D2 • More potent than clozapine and treatment resistant (likely due to blockage of doses) agents with
Antagonist • Tends to be used in higher doses (>15mg a depression H1-histamine & 5HT2C • lacks sedating lower weight
day) (esp. when combined with receptors) properties (only gain or lower
• Sometimes exceeds 40mg off label fluoxetine) • High cardiometabolic risks somewhat sedating in cardio
• Requires monitoring for efficacy and risks • Increases triglyceride levels some) metabolic risks
• Available as an oral disintegrating tablet, as • Increases insulin resistance • doesn’t often raise fail, this drug
an acute intramuscular injection and long- prolactin levels tends to be
acting 4-week intramuscular depot used
Quetiapine • Antagonist at Serotonin • Atypical • Chemical structure related to clozapine • Robust antidepressant • Very sedating at its peak
(pine) 5HT2A and Dopamine • But: several differentiating effects (due to antihistamine
D2 receptors pharmacologic properties (especially at • Papa Bear (800 mg) best as properties)
different doses and oral formulations) antipsychotic also for • Weight gain
• Pharmacological effects are due to parkinson patients who are • Increase fasting triglycerin
quetiapine itself and its active metabolite treated for psychosis levels
norquetiapine • Mama Bear (300mg) best for • can increase insulin
• Overall very complex set of binding resistance (especially
antidepressant and bipolar
properties moderate to high doses)
as well as unipolar depressed
• Acts like several different drugs depending
patients
on dose / formulation
• Baby bear (50mg) best as
• IR formulation
hypnotic
• rapid onset, short duration, only once a
day (usually at night) • Insomnia (in combo with
• XR formulation other antidepressants)
• anxiety (in combo with other
• Slower to reach peak, still rapid
occupation of 60%, lasts several hours antidepressants)
linger than IR
• It’s ideal as a antipsychotic but not as a
hypnotic (peak too delayed, hangover
effect)
→ Treatment: mainly Schizophrenia
Drug Name Category / Conventional or Characteristics etc. Treated symptoms (mostly Side effects Side effects that are not First line.
Pharmacological Profile Atypical? besides antipsychotic effects) caused by this drug Second line,
(e.g. opposed to other drugs)
etc.
Clozapine • Serotonin 5HT2A- • “Prototypical” • Antipsychotics are generally dosed so that • Aggression and violence • Of all others, has greatest • few if any Most likely
(pine) Dopamine D2 atypical about 60% of D2 receptors are occupied • (Rare) “awakening” in from risk to develop extrapyramidal effects used when
Antagonist antipsychotic but that’s lower for clozapine of return to nearly normal level agranulocytosis (life • No dyskinesia other
• Serotonin-dopamine • Very complex pharmacological profile of cognitive, interpersonal and threatening, sometimes fatal) antipsychotics
• No elevated prolactin
antagonist (SDA) • Can show greater efficacy than other vocational functioning 0.5-2% of patients have failed.
atypical antipsychotics with 5HT2A • Reduces suicide risk - monitor blood count!
antagonism • May reduce tardive • Increased risk of seizures It’s the “gold
• Only antipsychotic to reduce suicide risk • Very sedating standard” for
dyskinesia severity (esp. long treating
treatment intervals • Excessive salivation
schizophrenia,
• Increased myocarditis risk
however,
• Weight gain because of its
(likely due to blockage of side effects, it’s
H1-histamine & 5HT2C not first line
receptors) treatment
Olanzapine • Serotonin 5HT2A- • Atypical • Chemical structure related to clozapine • Also used in bipolar disorder • Weight gain • lacks EPS (also at high When other
(pine) Dopamine D2 • More potent than clozapine and treatment resistant (likely due to blockage of doses) agents with
Antagonist • Tends to be used in higher doses (>15mg a depression H1-histamine & 5HT2C • lacks sedating lower weight
day) (esp. when combined with receptors) properties (only gain or lower
• Sometimes exceeds 40mg off label fluoxetine) • High cardiometabolic risks somewhat sedating in cardio
• Requires monitoring for efficacy and risks • Increases triglyceride levels some) metabolic risks
• Available as an oral disintegrating tablet, as • Increases insulin resistance • doesn’t often raise fail, this drug
an acute intramuscular injection and long- prolactin levels tends to be
acting 4-week intramuscular depot used
Quetiapine • Antagonist at Serotonin • Atypical • Chemical structure related to clozapine • Robust antidepressant • Very sedating at its peak
(pine) 5HT2A and Dopamine • But: several differentiating effects (due to antihistamine
D2 receptors pharmacologic properties (especially at • Papa Bear (800 mg) best as properties)
different doses and oral formulations) antipsychotic also for • Weight gain
• Pharmacological effects are due to parkinson patients who are • Increase fasting triglycerin
quetiapine itself and its active metabolite treated for psychosis levels
norquetiapine • Mama Bear (300mg) best for • can increase insulin
• Overall very complex set of binding resistance (especially
antidepressant and bipolar
properties moderate to high doses)
as well as unipolar depressed
• Acts like several different drugs depending
patients
on dose / formulation
• Baby bear (50mg) best as
• IR formulation
hypnotic
• rapid onset, short duration, only once a
day (usually at night) • Insomnia (in combo with
• XR formulation other antidepressants)
• anxiety (in combo with other
• Slower to reach peak, still rapid
occupation of 60%, lasts several hours antidepressants)
linger than IR
• It’s ideal as a antipsychotic but not as a
hypnotic (peak too delayed, hangover
effect)
