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Pharm Exam 3 > Antipsychotics > Flashcards

Antipsychotics Flashcards

1
Q

Antipsychotics

A

Schizophrenia

Bipolar

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2
Q

Psychosis

A
  • Break from reality (distorted or non-existent sense of reality)
  • Hallucinations: seeing, hearing feeling things that aren’t there
  • Delusions: firm, fixed beliefs that are untrue and seem irrational to others
  • Sx of mental illness
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3
Q

Psychotic disorder

A

Mood disorders with psychotic features

  • Bipolar
  • Major depression

Substance-induced psychosis
Dementia/delirium with psychotic features
Schizophrenia
Schizoaffective disorder

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4
Q

Antipsychotics

A

Dopamine hypothesis: overstimulation of DA receptors
- Chlorpromazine: induced state of mental indifference in pts; sedation w/o narcosis

Motivational salience

  • Antipsychotics block dopaminergic effects
  • Drugs don’t erase delusions by blocking dopamine
  • Delusions/hallucinations are dormant
  • Normal thoughts also blocked
  • Patients report dysphoria
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5
Q

Indications

A
  • Schizophrenia
  • Bipolar disorder
  • Acute psychosis (mania)
  • Major depression with psychotic features
  • Severe behavioral problems
  • Tourette syndrome (haloperidol)
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6
Q

First Generation Antipsychotics

A 
Haloperidol (Haldol)
Fluphenazine (Prolixin)
Perphenazine (Trilafon)
Thioridazine (Mellaril)
Chlorpromazine (Thorazine)
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7
Q

First Generation Antipsychotics MOA

- Don’t get used much due to the blocking of dopamine receptors, causing movement problems

A

D2 receptor antagonist
- Antipsychotic effects: relief of positive sx (delusions hallucinations, thought disorders, movement disorders)
ADR:
- Induction of EPS: abnormal, involuntary movements (akathisia, dystonia, dyskinesia, pseudoparkinsonism)
- Increased prolactin levels (lacrimation/ breast development)

5HT2c receptor antagnoist
- ADR: contributes to wt gain

Alpha 1 antagonist
- ADR: sedation

H1 antagonist
- ADR: sedation, wt gain

M1 antagonist
- ADR: anticholinergic effects (urinary retention, constipation, dry mouth, blurred vision, confusion)

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8
Q

First generation ADRs

A
  • Movement disorder (dystonia, bradykinesia, tremor, akathisia, choreoathertosis)
  • Anhedonia
  • Sedation
  • Wt gain
  • Temperature dysregulation
  • Hyperprolactinemia (galactorrhea/ amenorrhea)
  • Postural hypotension
  • Sunburn
  • Prolonged QT
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9
Q

Second generation (Atypical) antipsychotics

A 
Aripiprazole (Abilify)
Brexpiprazole (Rexulti)
Asenapine Maleate (Saphris)
Clozapine (Clozaril) 
Iloperidone (Fanapt)
Lurasidone (Latuda)
Olanzapine (Zyprexa)
Paliperidone (Invega)
Quetiapine (Seroquel)
Risperidone (Risperdal)
Ziprasidone (Geodon)
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10
Q

Second Generation Antipsychotics MOA

A
  • Antipsychotic effects w/o the extrapyramidal sx
  • Helps with negative sx: apathy, social withdrawal, decreased motivation, cognitive impairment

D2 receptor antagonist
5HT1 receptor agonist: antidepressant/anxiolytic
5HT2A antagonist: negative sx improvement
5HT2c receptor antagonist
Alpha 1 antagonist
H1 antagonist
M1 antagonist

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11
Q

Second generation ADR

A
  • DM
  • Hypercholesterolemia
  • Sedation
  • Moderate movement disorder
  • Hypotension

Risperidone
- Hyperprolactinemia

Olanzapine
- Wt gain

Clozapine

  • Seizures
  • Nocturnal salivation
  • Agranulocytosis
  • Myocarditis
  • Lens opacities
  • Wt gain
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12
Q

Avoiding second generation ADR best choices

A

Sedation

  • W/O: Aripiprazole, Iloperidone, Lurasidone
  • W/: Clozapine

Wt Gain

  • W/O: Aripiprazole, Lurasidone, Ziprasidone
  • W/: Clozapine

EPS

  • W/O: Clozapine, Iloperidone, Quetiapine
  • w/ Paliperidone
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13
Q

Antipsychotic black box

A
  • Increased mortality in eldery pts with dementia related psychosis
  • Causes varied: CV (heart failure, sudden death); Infection (pneumonia)
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14
Q

Aripiprazole

A
  • Schizophrenia
  • Bipolar disorder (monotherapy or adjunctive to Li or valproate)
  • Adjunct treatment of major depressive disorder
  • Irritability associated with autistic disorder
  • Acute treatment of agitation
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15
Q

Brexpiprazole (Rexulti)

- Schizophrenia, adjunct for MDD

A
  • WARNING: increased mortality and CVA in elderly dementia pts with psychosis, tardive dyskinesia, NMS
  • Hyperglycemia, hyperlipidemia, wt gain, blood dyscrasias, akathisia, somnolence, anxiety, restlessness
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16
Q

Asenapine (Saphris)

  • Acute treatment of manic or mixed episodes associated with bipolar I disorder in adults (monotherapy or adjunctive therapy with either Li or valproate)
  • Acute and maintenance treatment of schizophrenia in adults
A
  • MOA: DA, 5HT, NE, H1 receptor antagonist

- ADR: Insomnia, somnolence, N/V, anxiety, agitation, HA, constipation, psychosis; same warning as iloperidone

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17
Q

Clozapine (Clozaril, Versacloz)

  • Treatment resistant schizophrenia
  • Reduce the risk of suicidal behavior in younger pts with schizophrenia
A

WARNING

  • Increased risk of angranulocytosis
  • Myocarditis, orthostasis, bradycardia
  • Lower seizure threshold

DRUG INTERACTION

  • Decreases cigarette smoking (may change drug metabolism): Clozapine 1A2 substrate vs Tobacco 1A2 inducer
  • Lower dose with P450 1A2 inhibitors (Ciprofloxacin)
  • Avoid use of strong P450 3A4 inducers
18
Q

Olanzapine

A
  • Schizophrenia
  • Bipolar disorder
  • Treatment resistant depression
  • Agitation associated with schizophrenia and bipolar I mania
19
Q

Quetiapine

A
  • Schizophrenia
  • Bipolar disorder
  • Adjunctive therapy for major depressive disorder
20
Q

Iloperidone (Fanapt)

- Treatment of schizophrenia in adults

A
  • MOA: unknown, likely DA and 5 HT2 antagonist, alpha adrenergic antagonism
  • ADR: dizziness, somnolence, tachycardia, N, dry mouth; Impaired thinking, judgement, motor skills; Long QT; NMS, tardive dyskinesia; Orthostasis; hyperprolactinemia; priapism
  • DRUG INTERACTION: 2D6 and 3A4 substrate
21
Q

Paliperidone (Invega)

- Schizophrenia, schizoaffective disorder

A
  • MOA: active metabolite of risperidone; DA, 5HT2a, H1, alpha receptor antagonist
  • ADR: HA, tachycardia, somnolence, anxiety, akathisia, EPS; same warning as iloperidone
22
Q

Risperidone

A
  • Schizophrenia
  • Bipolar disorder
  • Irritability associated with autism
23
Q

Ziprasidone

A
  • Schizophrenia

- Bipolar disorder

24
Q

Monitoring SGAs

A
  • Medication and FH, CVD
  • Weight
  • Waist circumference
  • Blood pressure
  • Fasting plasma glucose level
  • Fasting lipid profile
25
Q

Antipsychotics treatment goals

A

Initial response

  • Positive subjective response immediately following therapy: predicts potential benefit with medication
  • Is there onset of dysphoria or anxiety: leads to negative attitude towards therapy
  • No initial dose is too low, high doses are less effective– start low and go slow

7 day goals

  • Decrease in agitation, hostility, aggression, and anxiety
  • Normalization of sleeping and eating patterns
  • Titrate medication close to or to effective dose

2-3 week goals

  • Increase socialization, self care habits, and mood
  • Reach target dose and maintain
26
Q

Schizophrenia Treatment

A

Consider

  • Major suicide risk
  • Metabolic issues (especially with Olanzapine) and treatment induced side effects
  • Severe agitation or violence
  • Non-compliance
  • Depression or mood sx
  • Substance abuse
  • Prodromal or first episode
  • Catatonia or NMS

Monotherapy of atypical

  • Aripiprazole
  • Olanzapine
  • Quetiapine
  • Risperidone
  • Ziprasidone
  • If not available, a trial of Haloperidol, Chlorpromazine

If psychosis persists, trial of second atypical

27
Q

Acute Psychosis Treatment

A

If no past successful treatment

Less Urgent (regular oral)

  • Olanzapine
  • Risperidone
  • Quetiapine

In the middle (rapid dissolving oral)

  • Olanzapine
  • Risperidone
  • Aripiprazole

More urgent (IM)

  • Olanzapine
  • Ziprasidone
  • Haloperidol IM (or IV) alone w/ Lorazepam
28
Q

Good response

A
  • Prior response to a drug
  • Absence of EtOH or drug abuse
  • Acute onset/short duration of illness
  • Acute stressors or other precipitating factors
  • Later age of onset
  • Affective sx (depression and anxiety)
  • Family history of affective illness
  • Medication compliance
  • Negative sx don’t response as well
29
Q

Treatment of Extrapyramidal Sx

A

Acute Dystonia

  • Benzotropine mesylate (Cogentin)
  • Diphenhydramine (Benadryl)
  • Trihexyphenidyl (Artane)

Akathisia

  • Clonazepam
  • Lorazepam
  • Pramipexole
  • Propranolol
  • Ropinirole

Neuroleptic Malignant Syndrome

  • Dantrolene
  • Anticholinergics (Benztropine, Trihexyphenidyl)
  • Dopamine agonists (Amantadine, Bromocriptine, Ropinirole, Pramipexole)

Parkinsonism

  • Amantadine
  • Anticholindergics (Benztropine, Trihexyphenidyl)
  • Pramipexole
  • Ropinirole

Neuroleptic-induced catatonia

  • Anticholinergics (Benztropine, Trihexyphenidyl)
  • Bromocriptine
  • Dopamine agonist (Amantadine, Bromocriptine, Ropinirole, Pramipexole)
30
Q

d

A

d

31
Q

Lithium

- First line for manic episodes/maintenance treatment of bipolar disorder

A
  • CONTRAINDICATION: renal or cardiovascular dz; severe debilitation, dehydration, or sodium depletion; pts receiving diuretics; risk of Li toxicity is very high in these pts
  • WARNING: pregnancy; Renal toxicity
  • NTI drug
32
Q

Lithium toxicity

A
  • Early sx: D/V, drowsiness, muscle weakness, lack of coordination
  • Higher levels: giddiness, ataxia, blurred vision, tinnitus and a large output of dilute urine
33
Q

Lithium ADR

A

Neuro
- tremor, muscle hyperirritability, ataxia, hyperactive DTR, blackout, seizures, slurred speech)

CV

  • Cardiac arrhythmia, hypotension, peripheral circulatory collapse, sinus node dysfunction with severe bradycardia
  • BRUGADA SYNDROME: ST elevation (can lead to afib, fever, nightmares, syncope, risk of sudden death)

GI
- Anorexia, N/V/D

GU
- Albuminuria, oliguria, polyuria, glycosuria

Derm
- Drying and thinning of hair, alopecia, chronic folliculitis, xerosis cutis, and exacerbation of psoriasis

Autonomic Nervous System
- Blurred vision, dry mouth

Thyroid abnormalities
- Euthyroid goiter, hypothyroidism

EEG changes
- Diffuse slowing, widening of frequency spectrum, potentiation and disorganization of background rhythm

EKG changes
- Reversible flattening, isoelectricity or inversion of T waves

Miscellaneous
- Fatigue, lethargy, dehydration, wt loss, tendency to sleep

34
Q

Bipolar Mania

A

Over joyful or excited state

35
Q

Treatment

A

Lithium

Anticonvulsant

  • divalproex
  • lamotrigine
  • carbamazepine
  • topiramate
  • oxcarbazemine (only of CBZ intolerance)

Atypical antipsychotic

  • olanzapine
  • risperidone
  • quetiapine
  • ziprasidone

Electroconvulsive

36
Q

Euphoric Mania/ hypomania

A

Monotherapy
- Lithium OR Divalproex OR Olanzapine

Two drug combination

  • (Lithium OR Anticonvulsant) + Anticonvulsant
  • (Lithium OR Anticonvulsant) + Atypical antipsychotic

Triple combination
- Lithium + Anticonvulsant (Divalproex, Carbamazepine) + Atypical antipsychotic (Olanzapine, Risperidone, Quetiapine, Ziprasidone)

Electroconvulsive OR add clozapine

37
Q

Dysphoric Mania/ hypomania

A

Monotherapy
- Divalproex OR Olanzapine

Two drug combination

  • (Lithium OR Anticonvulsant) + Anticonvulsant
  • (Lithium OR Anticonvulsant) + Atypical antipsychotic

Triple combination
- Lithium + Anticonvulsant (Divalproex, Carbamazepine) + Atypical antipsychotic (Olanzapine, Risperidone, Quetiapine, Ziprasidone)

Electroconvulsive OR add clozapine

38
Q

Psychotic Mania

A

Monotherapy
- Lithium OR Divalproex OR Olanzapine

Two drug combination
- (Lithium + Anticonvulsant– Divalproex, Carbamazepine) + Atypical antipsychotic– Olanzapine, Risperidone, Quentiapine, Ziprasidone

39
Q

Bipolar Treatment

A

Mania treatment

Mixed Episode treatment

40
Q

Mania

A
  • Lithium
  • Valproate
  • Carbamazepine
  • Aripiprazole
  • Olanzapine
  • Quetiapine
  • Risperidone
  • Ziprasidone

Combination
- (Lithium OR Valproate) + (Aripiprazole OR Olanzapine OR Quetiapine OR Risperidone)

Maybe helpful

  • Clozapine
  • Oxcarbazepine
41
Q

Mixed Episode

A
  • Valproate
  • Carbamazepine
  • Aripiprazole
  • Olanzapine
  • Risperidone
  • Ziprasidone

May be helpful

  • Clozapine
  • Lithium
  • Oxcarbazepine
  • Quetiapine

Pharm Exam 3 (5 decks)

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