Antipsychotics Flashcards

1
Q

Schizophrenia positive symptoms

A

Positive Symptoms
Hallucinations
Delusions (bizarre, persecutory)
Disorganized Thought
Perception disturbances
Inappropriate emotions

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2
Q

Schizophrenia Negative Symptoms

A

Blunted emotions (e.g.
flat affect)
Anhedonia
Lack of feeling

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3
Q

Schizophrenia Mood symptoms

A

Loss of motivation
Social withdrawal
Insight
Demoralization
Suicide

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4
Q

Schizophrenia Cognitive symptoms

A

New Learning
Memory
Trouble focusing

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5
Q

Dopamine Hypothesis of Schizophrenia

A

Reduced dopamine activity in mesocortical dopamine pathway may be associated with negative and cognitive symptoms of schizophrenia
An abnormality in DA function has been detected in patients with schizophrenia
A reduction in cortical dopamine transmission (both at the pre- and postsynaptic level)
Hyperactivity of dopamine neurons in the mesolimbic pathway may lead to positive symptoms of schizophrenia

Several drugs (e.g. amphetamines, cocaine, cannabis) have been linked psychosis

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6
Q

Schizophrenia diagnostic criteria

A
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7
Q

Antipsychotic medications overview

A

Target symptoms: Psychosis (alteration in thought process and/or content)
Types
Typical
Atypical
Absorption: variable
Clinical effects seen 30-60 min
IM less variable (avoid 1st pass)
When immobile, less absorption
Metabolism: liver
Excretion: slow
accumulates in fatty tissues
1/2 life of 24 hours or more

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8
Q

Typical Antipsychotics

A

-Also known as conventional or first-generation antipsychotics
-Complex mechanism of action
Used as early treatments of schizophrenia and other psychotic disorders
-Antipsychotics may block D2 receptors in nigrostriatal DA pathway and mesolimbic pathway.
-Movement disorders may appear as a result of this blockage
-Extrapyramidal symptoms mimic Parkinson’s symptoms (e.g. tremors)
-Tardive Dyskinesia may occur with long term use(e.g. tongue protrusion, facial grimacing)
-Mesolimbic pathway hyperactivity is believed to cause positive symptoms (e.g. hallucinations)
-Reduces hyperactivity in MP reducing positive symptoms
-A reduction of D2 receptors in other areas of the brain may block reward mechanisms
-May cause worsening of negative symptoms (e.g. anhedonia)
-Best drug to treat positive symptoms

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9
Q

Common side effects of antipsychotics

A

Cardiovascular - orthostatic hypertension
Weight-gain, dizziness, sedation, dry mouth, constipation
Endocrine and sexual: block dopamine, interfere with prolactin
Blood dyscrasias - agranulocytosis

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10
Q

Sedation in antipsychotics

A

initially considerable; tolerance usually develops after a few weeks of therapy; dysphoria

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11
Q

Postural hypotension in antipsychotic medications

A

results primarily from adrenergic blockade; tolerance can develop

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12
Q

Anticholinergic effects with antipsychotic medications

A

include blurred vision, dry mouth, constipation, urinary retention; results from muscarinic cholinergic blockade

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13
Q

Endocrine effects of antipsychotics

A

increased prolactin secretion can cause galactorrhea; results from anti-dopamine effect

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14
Q

Hypersensitivity reactions to antipsychotics

A

‑ jaundice, photosensitivity, rashes, agranulocytosis can occur

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15
Q

What is an idiosyncratic reaction to antipsychotics

A

Neuroleptic Malignant syndrome

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16
Q

Neuroleptic Malignant syndrome (features, time of max onset, treatment)

A

Neuroleptic malignant syndrome: combination of motor rigidity, hyperthermia, and autonomic dysregulation of blood pressure and heart rate (increased). Features may be catatonia, stupor, fever, myoglobinemia, can be fatal.
Time of maximal risk: weeks, can persist days after stopping neuroleptic.
Treatment: stop neuroleptic immediately, dantrolene or bromocriptine may help.
Antiparkinsonian agents not helpful.

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17
Q
A
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18
Q

Dantrolene in neuroleptic malignant syndrome

A
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19
Q

Bromocriptine in neuroleptic malignant syndrome:

A
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20
Q

Which medications are in the typical antipsychotic class?

A

Phenothiazines and haloperidol

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21
Q

Which medications are in the atypical antipsychotic class?

A

Clozapine (Clozaril)
Risperidone (Risperdal)
Paliperidone (Invega)
Olanzapine (Zyprexa)
Quetiapine (Seroquel)
Ziprasidone (Geodon)

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22
Q

Haloperidol

A

Dosages: 1-40 mg/day for po forms
Immediate Release Injection: 2-5 mg
Decanoate Injection: 50-100 mg/ML

Weight gain – weight gain may occur
Sexual dysfunction result from NE and SE blockade (erectile dysfunction, retrograde ejaculation, loss of libido and anorgasmia in men and women)
Seizures-generalized grand mal
Photosensitivity, jaundice, agranulocytosis
Muscle spasm, restlessness, loss of balance, uncontrolled movement, EPS, akathisia.

Neuroleptic malignant syndrome: combination of motor rigidity, hyperthermia, and autonomic dysregulation of blood pressure and heart rate (increased)

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23
Q

Which medications are in the phenothiazine class

A

Chlorpromazine(thorazine), thioridazine(mellaril), Trifluoperazine(stelazine).

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24
Q

Common side effects of phenothiazines

A

Weight gain - weight gain is common
Sedation : More common
Sexual dysfunction result from NE and SE blockade (erectile dysfunction, priapism (Thorazine), loss of libido and anorgasmia in men and women)
Seizures - <1% for generalized grand mal
QTc prolongation in Thioridazine
Photosensitivity, jaundice, agranulocytosis
Akathisia
Neuroleptic malignant syndrome: combination of motor rigidity, hyperthermia, and autonomic dysregulation of blood pressure and heart rate (increased)

25
Q

Common side effects of typical antipsychotics:

A

Prolactin elevation
Galactorrhea and amenorrhea may occur
Anticholinergic effects (e.g. dry mouth, constipation, etc)
Weight gain, orthostatic hypotension, and drowsiness

26
Q

Common doses of phenothiazines

A

Thorazine dose 200-800 mg/day,
Mellaril 200-800 mg/day
Stelazine: 15-20 mg/day

27
Q

Beers criteria warning for antipsychotics

A

BEERS criteria: avoid in elderly unless is necessary due to danger to self or others.

28
Q

Black Box Warning for antipsychotics

A

Black box warning: Avoid in elderly patients with dementia related psychosis due to increased risk of CVA and death.

29
Q

What are extrapyramidal symptoms

A
30
Q

Tardive dyskinesia Etiology, features, time of maximal risk

A

Etiology: Chronic blockade of D2 receptors in nigrostriatal pathway
Features: Oral-facial dyskinesia, widespread choreoathetosis or dystonia
Time of maximal risk: After months or years of treatment.
Treatment: antiparkinsonian agents often help

31
Q

Tardive Dyskinesia Treatment

A

FDA Approved Treatment for tardive dyskinesia:
-Valbenazine (Ingrezza) starting dose, 40mg, after 7 days, 80 mg daily
-Deutetrabenazine (Austedo) starting dose 12mg, increase by 6mg daily, 48mg daily maximum

32
Q

Valbenazine (Ingrezza)

A

need to look up

33
Q

Deutetrabenazine (Austedo)

A

need to look up

34
Q

How common are acute movement disorders associated with antipsychotics:

A

Can occur in 90% of all patients

35
Q

Acute movement disorders (etiology)

A

D2 receptors blockade in nigrostriatal pathway

36
Q

Acute Movement disorders (treatment)

A

Anticholinergic medication for dystonia, parkinsonism (Artane and Cogentin)
Akathisia does not usually respond to anticholinergic medication. Beta blockers have best success.

37
Q

akathisia

A

Akathisia: Inability to sit still, restlessness, It is motor restlessness rather than anxiety.
Time of maximal risk: 5-60 days
Treatment: reduce dose or change drug: antiparkinsonian agents, benzodiazepene or propranolol may help

38
Q

Parkinsonism:

A

Parkinsonism: rigidity, akinesia (slow movement), and tremor, masklike face, loss of spontaneous movements, bradykinesia, shuffling gait.
Time of maximal risk: 5-30 days
Treatment: antiparkinson agents may help.

39
Q

Acute Dystonia

A

Acute Dystonia: involuntary muscle spasms, abnormal postures, oculogyric crisis, torticollis,
-involuntary spasms of muscles of tongue, face,neck, back. May mimic seizures. Not hysteria.
Time of maximal risk: 1-5 days
Treatment: antiparkinsonian agents are diagnostic and curative.

40
Q

Treatment for acute muscular symptoms related to antipsychotics:

A

Diphenhydramine hydrochloride, 25 or 50 mg intramuscularly or po
Benztropine, 1 or 2 mg intramuscularly or slowly intravenously, followed by oral medication.
Propranolol, 20-80 mg per day
Bromocriptine, 10-40 mg per day
Selective beta1-adrenergic receptor antagonists, less effective.

41
Q

Perioral tremor(“Rabbit syndrome”)

A

Features: Perioral tremor(may be late variant of parkinsonism).
Time of maximal risk: After months or years of treatment
Treatment: Antiparkinsonian agents can help.

42
Q

Clozaril

A

-Atypical, 2nd Generation Antipsychotic
-(Gold Standard) Used when other antipsychotics have failed
-Dose: Initiate at 12.5 mg once a day or BID, then titrate up based on clozapine plasma level ranging from 250 to 350 ng/ml.
-Reduces the risk of suicide in patients with schizophrenia
-Neutropenia (WBC <3,000/mcL and Agranulocytosis <500/mcL) may occur
-Major side effects include seizures in high doses, increased weight gain, increased cardiovascular risks
-Strict ANC monitoring must be adhered to

43
Q

Asenapin(saphris)

A

FDA Approved: Schizophrenia (Acute and maintenance)
Antagonist to D2 and 5-HT2A receptors
Given sublingually as an oral disintegrating tab to enhance absorption
Usual dose 5mg to 10mg bid
May be used as a rapid PRN agent
Major side effects include sedation, lower risk of EPS, weight gain, dyslipidemia, mouth numbing and foul taste
Do not eat or drink for 10 minutes after administration

44
Q

Lurasidone(Latuda)

A

Antagonist to D2 and 5-HT2A receptors
Starting dose 40mg, maintenance dose 40mg-160mg daily
Antidepressant properties, useful in bipolar depression
Less risk for sedation, lesser risk of weight gain and dyslipidemia
Moderate EPS, recommended to be given at night
Must be taken with a 350 calorie meal for optimal absorption

45
Q

Olanzapine (zyprexa)

A

5HT2A and D2 receptor antagonist
Available in tablets, disintegrating tablets, and long acting injection
Schizophrenia dosing: 5mg-10mg daily up to 20mg daily maintenance dose
Widely prescribed and used in combination with other agents (e.g. antidepressants)
Major side effects include significant weight gain, increased cardiometabolic risks, increased triglycerides, and insulin resistance may occur

46
Q

Risperidone(Risperdal)

A

Antagonist to D2 and 5-HT2A receptors
Usual dose 2mg-8mg daily
Also used in adolescents and children with psychosis
Used to treat irritability in children and adolescents with autism disorder
Available in tablets, dissolvable tablets, liquid, and depot injectable formulations
Major side effects include sedation, lower risk of EPS, weight gain, dyslipidemia

47
Q

Paliperidone(Invega)

A

Antagonist to D2 and 5-HT2A receptors
Active metabolite of risperidone. Not hepatically metabolized, excreted in urine.
Available in sustained release tablets (ER) and long-acting injections, usually 4 weeks
Usual dose 6mg daily, up to 12 mg daily
Less risk for sedation, orthostasis, fewer EPS, increase hyperprolactinemia,
Increase risk for hyperprolactinemia, prolonged QTc interval
Used more frequently to enhance patient drug compliance
Monitor for tolerability to risperidone or po paliperidone prior to giving long acting injection

48
Q

Quetiapine (seroquel)

A

Higher potency on D2 receptor but has affinity towards 5-HT2A, H1, alpha 1 and 5-HT1A
Available in various formulation forms (IR, XR and tabs)
Maintenance dose 150mg-750mg divided bid or tid
It has antipsychotic, antidepressants, and hypnotic effects depending on the dose (lower dose=hypnotic effects)
Major side effects include weight gain, increased cardiometabolic risks, increased triglycerides, and insulin resistance may occur

49
Q

Ziprasidone (Geodon)

A

Antagonist to D2 and 5-HT2A receptors
Starting dose, 20mg po bid, Maximum 160mg daily
Available in tablets and intramuscular forms (not long acting)
May have antidepressant actions
Taken with at least 500 calories of food for optimal absorption
Less risk of weight gain, less risk of triglyceride elevation, insulin resistance, dyslipidemia
Known to significantly prolong QTc interval

50
Q

Aripiprazole (abilify)

A

Partial D2 and 5-HT1A agonist, 5-HT2A antagonist
Starting and target dose, 10mg to 15mg, max dose 30mg
Used to treat schizophrenia. Also used in children and adolescents to treat schizophrenia
Used with SSRIs/SNRIs to manage treatment-resistant major depressive disorder and bipolar depression
Less risk for weight gain, dyslipidemia, QTc prolongation
Can reduce drug induced hyperprolactinemia

51
Q

Prescribing recommendations for antipsychotics

A

Recommendations for PMHNPs prescribing Antipsychotics
Prescribing antipsychotics may be challenging with certain patients
Patients co-morbidities should be considered
Studies may or may not match the actual patients’ conditions
Different atypical antipsychotics have distinctive effects
Consider risks/benefits for choosing the right antipsychotic for a patient

52
Q

EPS etiology:

A

Etiology
D2 receptors blockade in nigrostriatal pathway
Increases in antipsychotics

53
Q

EPS Treatment

A

Treatment
Prevention by using lowest possible dosage,
Minimize use of PRN,
Closely monitor individuals in high-risk groups
Monitoring tools (AIMS Scale)

54
Q

What is tardive dyskinesia

A

-Irregular, repetitive involuntary movements of mouth, face, and tongue, including chewing, tongue protrusion, lip smacking, puckering of the lips, and rapid eye blinking. Abnormal finger movements are common.
-Begin after 6 months, but also as antipsychotics are withdrawn
Irreversible – controversy

55
Q

Atypical antipsychotic overview:

A

-Also known as second-generation antipsychotics
-Antipsychotic actions to manage positive symptoms similar to typical antipsychotics
-Lower risk of EPS and hyperprolactinemia
-Serotonin-Dopamine Antagonists
-Best drugs to treat negative symptoms

56
Q

Actions of atypical antipsychotics:

A

-Primarily Block D2 and 5HT2A receptors
-Hypothetically regulate downstream dopamine release
-Act as brakes to dopamine release
-Low risk of EPS due to blockage of D2 and 5HT2A receptors
-Hyperprolactinemia is impaired by blocking 5HT2A receptors
-Antidepressant actions in bipolar and unipolar depression
-Antimanic actions
-Anxiolytic actions
-Sedative-hypnotic actions

57
Q

Major side effects of atypical antipsychotics

A

Metabolic actions
Weight gain
Risk for obesity
Risk for dyslipidemia
Risk for diabetes
Cardiovascular disease

58
Q
A