Antipsychotics (PSYCH DRUGS) Flashcards
Oral First gen/typical antipsychotics
x3
1. Chlorpromazine (100-600mg/day)
2. Haloperidol (5-20mg/day)
3. Trifluoperazine (5-10mg/day)
Oral 2nd gen/atypical antipsychotics AND dose
X7
1. Risperidone (0.5-1mg, max 6mg/day)
2. Paliperidone (6mg, max 12 mg/day
3. Aripiprazole (15 mg ON, max 30mg/day)
4. Olanzapine (5-10 mg, max 20 mg/day)
5. Clozapine (25mg ON, max 900mg)
6. Quetiapine (50mg BD, max 800mg/day)
7. Amisulpride (200mg, max 1200mg/day)
MOA typical/1st gen antipsychotics
D2 receptor blockade (Dopamine receptor antagonist)
Side effects of first gen/typical antipsychotics
X7
1. Extrapyramidal side effects
2. Hyperprolactinemia
3. Sedation
4. Hypotension
5. Weight gain
6. Anticholinergic
7. Sexual side effects
Extrapyramidal side effects =?
x4
1. Acute dystonia
2. Pseudoparkinsonism
3. Akathisia
4. Tardive dyskinesia (chronic use of antipsychotics)
Acute dystonia symptoms
Involuntary movement/contraction of major muscle groups:
1. Oculogyric crisis (fixed upward or lateral gaze)
2. Torsion dystonia
3. Torticollis
4. Spasm of lip, face, throat muscles
5. Grimacing
6. Exaggerated posturing
7. Trismus (jaw muscle)
Mx of acute dystonia
IM benztropine (congentin)
+switch to atypical/2nd gen antipsychotic
Akathisia symptoms
- Restlessness
- Irritability
Mx of Akathisia
Best: propranolol
Acute akathisia: Anticholinergic eg. Benztropine
Chronic akathisia: BZD
Pseudoparkinsonism symptoms
more common
1. Resting Tremors
2. Stiffness of muscle, rigidity
3. Akinesia*, mask like facies, psychomotor retardation (bradykinesia)
4. Postural instability
5. Shuffling gait
Mx of Pseudoparkinsonism
- Gradual dose reduction
- Switch to 2nd gen/atypical antipsychotic
- Anticholinergic (eg. benzhexol)
Tardive dyskinesia Symptoms
- Oro-bucco-lingual and facial dyskinesia eg. Fly catching tongue protrusion
- Athetosis
- Choreiform pill rolling hand movements
- Hip thrusting
Mx of Tardive dyskinesia
- Switch to 2nd gen/atypical antipsychotic
- Maintain pt on lowest effective dose of antipsychotic
- Vitamin E may help alleviate symptoms
Onset of individual EPS symptom
- Acute dystonia: few hrs
- Akathisia: most common after 5 days of initiation
- Pseudoparkinsonism: gradual
- Tardive dyskinesia: at least 6 months, usu after many years
Neuroleptic Malignant Syndrome dx criteria
Associated with use of neuroleptic meds 1. Severe muscle rigidity 2. Elevated temperature 3. 2 or more of the following:
1) diaphoresis
2) dysphagia
3) tremor
4) incontinence
5) changes in level of consciousness ranging from confusion to coma
6) mutism
7) tachycardia
8) elevated or labile BP
9) leukocytosis
10) laboratory evidence of muscle injury (eg. Raised CK)
Mx of Neuroleptic Malignant Syndrome
- Stop antipsychotics
- Supportive measures (for heat): IV hydration, cooling measures, transfer to ICU
- Pharmacological: bromocriptine (to reverse dopamine blockade), dantrolene/lorazepam to reduce rigidity
- After stabilisation, change to a different antipsychotic (less potent eg. Quetiapine)
Hyperprolactinemia manifestations
x4 (reversible)
1. Galactorrhea/gynaecomastia
2. Sexual dysfunction
3. Amenorrhea
4. Hypoestrogenism
Which antipsychotics have hyperprolactinemia as SE?
- All first gen/typical antipsychotics
- Risperidone (the only 2nd gen/atypical antipsychotic)
Special features of Chlorpromazine
More sedating among first gen antipsychotics
Special features of haloperidol
High potency but more EPS among first gen antipsychotics
Depot First gen/typical antipsychotics + Dose
- Flupenthixol (Fluanxol) - 20-60 mg every month
- Zuclopenthixol - 200-600mg every month
Depot 2nd gen/typical antipsychotics
- Risperidone (Consta) - 2-weekly IM, unpopular
- Paliperidone (Sutenna) - monthly
Side effect of 2nd gen/atypical antipsychotics
- X7 of first gen antipsychotics (less of EPSE)
- Weight gain
- Prolonged QTc
- Neuroleptic malignant syndrome
<Aripiprazole least/minimal SE>
Indication for 2nd gen/atypical antipsychotics
- Schizophrenia (positive and negative symptoms)
- Bipolar disease (with or without psychotic features)
- Major depression with psychotic features
- Agitation
- Delirium
MOA of 2nd gen/atypical antipsychotics
- Blocks D2
- Blocks 5HT2A *reduced EPSE and also targets negative symptoms in schozophrenia
- Blocks alpha adrenergic
Drug for treatment resistant schizophrenia
Clozapine (2nd gen/atypical antipsychotic)
Potential life threatening SE of clozapine
Fatal Agranulocytosis / blood dyscrasia
+ fatal myocarditis or cardiomyopathy
+ fatal pulmonary embolism
+ seizures
Before starting and during prescription of clozapine, what must be done?
Frequent RBC monitoring (weekly for first 18 weeks then fortnightly or monthly thereafter until a year)
MOA of clozapine (and thus good for treatment resistant schizophrenia)
- Dopamine (D1, D3, D4)
- Alpha adrenergic (alpha 1&2)
- Histaminergic (H1)
- Muscarinic anticholinergic (M1)
- Serotonergic (5HT1A, 2C, 6&7)
2nd gen/atypical antipsychotics good for negative symptoms of schizophrenia
COCA
1. Clozapine
2. Olanzapine
3. Cariprazine
4. Amisulpride
Side effect concern: QTc prolongation
1. Antipsychotic to avoid
2. Antipsychotic to use
- Avoid: first gen/typical antipsychotic (haloperidol, chlorpromazine)
- Use: aripiprazole (or lurasidone, brexpiprazole)
Side effect concern: EPSE
1. Antipsychotic to avoid
2. Antipsychotic to use
- Avoid: Haloperidol
- Use: 2nd gen (Aripiprazole, Olanzapine, Risperidone, Quetiapine, Clozapine)
Side effect concern: Weight gain
1. Antipsychotic to avoid
2. Antipsychotic to use
- Avoid: olanzapine, clozapine
- Use: Aripiprazole, Haloperidol, Trifluoperazine
Side effect concern: Sedation
1. Antipsychotic to avoid
2. Antipsychotic to use
- Avoid: Quetiapine, Olanzapine, Clozapine
- Use: Aripiprazole
Side effect concern: Seizure
1. Antipsychotic to avoid
2. Antipsychotic to use
- Avoid: Chlopromazine, clozapine
- Use: Haloperidol, Sulpride, Risperidone, Aripiprazole
Highest risk of metabolic syndrome among 2nd gen/atypical antipsychotics
Clozapine
Antipsychotic in ACUTE mx
- Oral or depot antipsychotics for rapid tranquilisation
- oral rapidly dissolvable tablets: PO olanzapine 10 mg STAT or PO risperidone quicklet 2 mg STAT or
- IM haloperidol 5 mg STAT - Alternatives:
1) IM lorazepam 2mg STAT
2) Antihistamine
Ix before and after starting antipsychotics
- PE - weight (metabolic syn), BP, EPSE
- ECG - QTc (when initiating rx)
- labs - fasting blood glucose, fasting lipid (triglycerides, cholesterol) *baseline and at least every 12 months
