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Mental Health/Psychiatry > Antipsychotic Medications > Flashcards

Antipsychotic Medications Flashcards

1
Q

Indications for use of antipsychotic agents to treat psychotic symptoms from the following disorders (5)

A
  1. Schizophrenia (most high-profile)
  2. Bipolar disorder (mood stabilizing)
  3. Psychotic depression
  4. Dementia-related psychoses
  5. Drug-induced psychoses
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2
Q

Indications of antipsychotic agents for improvement of mood, reductions of anxiety and sleep disturbances (2)

A
  1. Generally not the drug of choice in non-psychotic patients
  2. Can treat anxiety symptoms in Autism Spectrum Disorder (ASD) - typically risperidone
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3
Q

Antipsychotics are ______ ______, but psychosocial rehabilitation is impossible often without antipsychotic drugs

A

not curative

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4
Q

Indications of antipsychotic agents may also include these conditions (3)

A
  1. Antiemetic effects
  2. Pruritus (nerve-related itching) - Histamine receptor antagonism
  3. Preoperative sedatives
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5
Q

What is the Dopamine Hypothesis of Schizophrenia? (2 parts)

A 
Positive symptoms (hallucinations, delusions) are caused by HYPERACTIVITY of dopamine in the MESOLIMBIC pathway.
- D2 Receptor (D2R) antagonism helps alleviate psychotic symptoms
Negative symptoms (emotional blunting, social withdrawal, lack of motivation) and cognitive impairment are caused by dopamine receptor HYPOFUNCTION in the PREFRONTAL CORTEX.
- Currently cannot be targeted by pharmacotherapies, but negative symptoms can improve with antipsychotic treatment
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6
Q

What is the MOA of Typical Antipsychotics and their general ADRs in major brain pathways? (3 pathways)

A

MOA: Blocks D2R

ADRs:

  1. D2R blockade in mesocortico-mesolimbic pathway alleviates psychotic symptoms, but may induce other behavioral symptoms
  2. D2R blockade in nigrostriatal pathway produces motor disturbances by two opposing mechanisms (EPS and TD)
  3. D2R blockade in tuberoinfundibular pathway increases prolactin secretion, causing hyperprolactinemia and alterations of metabolism
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7
Q

What are some key factors to consider when selecting the right antipsychotic agent for clinical use? (4)

A
  1. Patient response: antipsychotic drugs have similar efficacy; cost and available formularies vary
  2. ADR avoidance: optimize efficacy vs. side effects
  3. Acute psychotic episode vs. chronic maintenance: long-term maintenance required for schizophrenia, longer time spent on it = greater drug success, combination therapy only for refractory patients
  4. Situation and Formulation: Given via IM (emergencies), orally, or LAI?
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8
Q

Classify Typical vs. Atypical Antipsychotic Agents (name, MOA, and scope of clinical use)

A

Typical = first generation

  • MOA: D2R antagonism
  • Less commonly used, but still used in public sector-treated patients

Atypical = second generation

  • MOA: D2R antagonism and inverse agonism of 5-HT2A
  • Improved efficacy against positive symptoms
  • Very few, if any, are effective against negative symptoms
  • Reduced risk of EPS
  • Most drugs cause substantial weight gain; increased risk of DM, especially Olanzapine and Clozapine
  • Associated with metabolic syndromes that can increase risk of CAD, stroke, and HTN
  • More commonly prescribed
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9
Q

Typical Antipsychotics (3 classes; 4 agents)

A
  1. Phenothiazines
    A. Chlorpromazine
    B. Fluphenazine
  2. Thioxanthenes
    A. Thiothixene
  3. Butyrophenones
    A. Haloperidol
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10
Q

General ADRs of Antipsychotics (7)

A
  1. ANS effects: depends of potency of both typical and atypical antipsychotics
  2. Neurological effects: more common in typical agents
  3. Neuroleptic Malignant Syndrome: more common in typical agents
  4. Behavioral effects: more common in typical agents
  5. Metabolic and endocrine effects: metabolic more common in atypical agents; hyperprolactinemia more common in typical agents
  6. Toxic or allergic reactions: Clozapine (fatal agranulocytosis)
  7. Cardiac toxicity: both typical and atypical
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11
Q

Typical antipsychotics also target these receptors and cause associated effects (3)

A
  1. Alpha-adrenergic antagonists: orthostatic hypotension, lightheadedness
  2. Muscarinic antagonists: anticholinergic effects- dry mouth, urinary retention (anti-SLUD)
  3. H1 antagonists: sedation, weight gain
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12
Q

ADRs of antipsychotic agents share a close relationship with D2R affinity. ______ plays an especially strong role in antipsychotic pharmacology; it governs ______ profiles and ______ more than ______.

A

Potency; ADR; severity; efficacy

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13
Q

Higher antipsychotic affinity = higher ______ for D2 receptors

A

specificity

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14
Q

In clinical use, higher potency = ______ ______ and lower potency = ______ ______

A

Lower dose; higher dose

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15
Q

Extrapyramidal symptoms (EPS) occur due to a ______ of D2R, which alters ______/______ balance.

A

blockade; dopamine/acetylcholine

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16
Q

Relative excess of ______ influence results in EPS.

A

cholinergic

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17
Q

Symptoms of EPS include (3)

A
  1. Dystonia (sustained contraction of muscles leading to twisting, distorted postures)
  2. Parkinson-like symptoms
  3. Akathesia (motor restlessness)
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18
Q

EPS symptoms are generally ______- and ______-dependent.

A

time; dose

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19
Q

Drugs that have stronger ______ activity have a lower risk of developing EPS.

A

anticholinergic

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20
Q

Treatment of EPS (3)

A
  1. Amantadine: prodopaminergic drug that increases effective dopamine signaling
  2. Benztropine: an anticholinergic drug that counters the effects of excess cholinergic effects, but may cause anti-muscarinic effects (anti-SLUD)
  3. Diphenhydramine: antihistamine also good for acute EPS
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21
Q

Treatment of akathesias (2)

A
  1. Clonazepam (benzodiazepine)

2. Propranolol (beta-blocker)

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22
Q

Tardive dyskinesia (TD) occurs with ______-______ treatment with antipsychotic agents, due to ______ of dopaminergic receptors. Neuronal response to dopaminergic input ______ response to cholinergic input (______ of EPS), resulting in ______ and ______ movements, including bilateral and facial jaw movements, “fly-catching”, or “worm-like” tongue movement.

A

long-term; sensitization; overpowers; opposite; excess; involuntary.

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23
Q

TD symptoms may improve after ______ of drug, but in many cases is ______ and ______.

A

cessation; irreversible; persistent

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24
Q

Treatment of TD (1 class; 2 agents)

A
  1. VMAT inhibitors: decreases dopamine packaged and released from vesicles
    A. Valbenazine
    B. Deutetrabenazine
25
Q

TD is most commonly observed when high potent agents like ______.

A

Haloperidol

26
Q

Neuroleptic malignant syndrome (NMS) resembles severe ______ with ______ ______. Symptoms include muscle rigidity (“lead-pipe rigidity”), fever, altered mental status and stupor, unstable BP, myoglobinemia, and elevated serum creatine kinase. The condition is ______, but ______ in 10-20% of cases if untreated.

A

Parkinsonism; autonomic instability; rare; fatal

27
Q

Treatment of neuroleptic malignant syndrome (2)

A
  1. Dantrolene

2. Bromocriptine

28
Q

Neuroleptic malignant syndrome may ______ for more than ______ ______ after the offending agent in discontinued. Symptom ______ is associated with ______.

A

persist; one week; persistence; mortality

29
Q

NMS most frequently occurs with ______ doses of ______ agents.

A

high; potent

30
Q

Time of neurological ADRs onset is crucial for the correct diagnosis. List ADRs in shortest time of onset to longest.

A

Acute dystonia < akathesia < Parkinsonism < NMS < Perioral tremor (“rabbit syndrome”) < TD

31
Q

Psychiatric side effects of antipsychotics include 1. ______ and 2. ______, caused by ______ and ______ antagonism.

A
  1. Akinesia: diminished spontaneity, apathy, withdrawal, appearance of depression; mimics negative symptoms
  2. Dysphoria: altered, unstable mood
    D1R; D2R
32
Q

______ and ______ are also psychiatric side effects that can be induced by large doses of typical antipsychotics, especially in ______ patients. These side effects resemble ______.

A

Delirium; psychosis; elderly; pseudodementia

33
Q

Hyperprolactinemia due to ______ blockade in the ______ pathway causes ______ of prolactin by the ______ ______.

A

D2R; tuberoinfundibular; hypersecretion; pituitary gland

34
Q

______ of the D2R antagonists by ______ antipsychotics correlates with with prolactin ______.

A

Potency; typical; elevation

35
Q

Hyperprolactinemia can induce ______, sexual dysfunction, or ______ in women and men.

A

galactorrhea; infertility

36
Q

For hyperprolactinemia, if switching or stopping the antipsychotic agent is not feasible, ______ can be used

A

Bromocriptine

37
Q

Low-potency ______ frequently cause cardiovascular effects, such as ______ ______ and ______.

A

phenothiazines; orthostatic hypotension; tachycardia

38
Q

Typical Antipsychotic: Chlorpromazine and Thioridazine (General, Receptor Targets, and ADRs)

A

General: Phenothiazine agents produce more sedation and weight gain (H1) than other typical antipsychotics. Chlorpromazine is the least potent of this class.

ADRs: Low-potency agents are associated with increased serum triglycerides and hyperglycemia. Moderate to high potential for EPS. Non-ANS cardiovascular toxicity. Thioridazine associated with torsades de pointes and was removed from the market (sometimes used as a second-line agent)

39
Q

Typical Antipsychotic: Fluphenazine (General and ADRs)

A

General: Commonly used LAI for noncompliant patients. Administered every 2-3 weeks.

ADRs: Oral formulation has high EPS potential. Low potential for weight gain, sedation, and orthostasis. Low to moderate potential for anti-muscarinic effects.

40
Q

Typical Antipsychotic: Haloperidol (General and ADRs)

A

General: most widely used typical antipsychotic. Can be used to manage acute psychotic states. Commonly used as LAI for noncompliant patients. Administered every 4 weeks.

ADRs: Greater incidence of EPS. Low potential for orthostasis, weight gain, sedation.

41
Q

Serotonin and Glutamatergic Hypotheses of Schizophrenia

A

Agonism of 5-HT2A and 5-HT2C receptors are the basis of hallucinatory activity of illicit drugs, like LSD. Agonism of 5-HT2A leads to depolarization of glutamatergic neurons, which stabilizes NMDA receptor. Increased glutamatergic activity may increase psychotic symptoms. However, NMDAR antagonists (PCP and ketamine) exacerbate cognitive impairment and psychosis in some patients with schizophrenia. Agonism of 5-HT2C inhibits cortical and limbic dopaminergic release (can reduce psychotic symptoms).

42
Q

What is inverse agonism? Inverse agonism vs. Antagonism.

A

Prevents an agonist from binding and stabilizes the inactive form of a receptor. This REDUCES basal activity of the receptor.

An antagonist prevents an agonist from binding, but does not affect the basal activity of the receptor.

43
Q

Atypical antipsychotics have ______ effect on D2Rs, ______ more effect on ______ receptors than typical antipsychotic agents. Atypical antipsychotic agents, like ______, are ______ ______ of 5-HT2A receptors.

A

less; but; 5-HT2A; clozapine; inverse agonists

44
Q

Inverse agonism of 5-HT2A receptors ______ activity of glutamatergic neurons and ______ psychotic symptoms. Inverse agonism of 5-HT2C receptors may therefore lead to ______ dopamine in the mesocortical structures. However, this is balanced by D2R ______.

A

reduces; lessens; increased; antagonism

45
Q

ADRs of antipsychotic agents share a close relationship with D2R affinity. Atypical antipsychotics have ______ D2R potency. This causes ______ on-target ADRs and ______ off-target ADRs.

A

lower; fewer; more

46
Q

Receptor affinity of antipsychotic agents: Chlorpromazine, Haloperidol, Clozapine, Olanzapine, Aripiprazole, and Quetiapine

A

Chlorpromazine: alpha-adrenergic 1 = 5-HT2A > D2 > D1
Haloperidol: D2 > alpha-adrenergic 1 > D4 > 5-HT2A > D1 > H1
Clozapine: D4 = alpha-adrenergic 1 > 5-HT2A > D2 = D1
Olanzapine: 5-HT2A > H1 > D4 > D2 > alpha-adrenergic 1 > D1
Aripiprazole: D2 = 5-HT2A > D4 > alpha-adrenergic 1 = H1&raquo_space; D1
Quetiapine: H1 > alpha-adrenergic 1 > muscarinic 1,3 > D2 > 5-HT2A

47
Q

Patients taking atypical antipsychotics need to be monitored using the following metrics: (7)

A
  1. Personal and family hx of obesity, DM, HLD, HTN, and CVD
  2. Weight and height for BMI
  3. Waist circumference
  4. BP
  5. Fasting glucose
  6. Fasting lipids
  7. If patient has DM, HgA1c and sometimes insulin
48
Q

For patients taking Clozapine, monitoring intervals include: (4)

A
  1. All monitoring labs at baseline
  2. Weight every 4 weeks, and then quarterly after 12 weeks
  3. Weight, BP, fasting glucose, and fasting lipids at 12 weeks
  4. All monitoring labs annually
49
Q

Indications for use of atypical antipsychotics (8)

A
  1. Schizophrenia
  2. Acute mania
  3. Adjunctive therapy in treatment-resistant depression
  4. Adjunctive therapy in major depressive disorder
  5. PTSD
  6. Anxiety disorders
  7. Behavioral disturbances associated with dementia: BLACK BOX WARNING- elderly patients with dementia-related psychoses are at increased risk of death by stroke
  8. Psychotic depression and psychosis secondary to head trauma, dementia, or other treatment drugs
50
Q

Atypical Antipsychotic: Clozapine (General, MOA, ADRs, and Contraindications)

A

General: Reserved for individuals refractory to all other antipsychotics. Not a first-line treatment. For treatment of patients with a low threshold for EPS.

MOA: Antagonist of 5-HT2A, D1, D3, D4, and alpha-adrenergic receptors. Low affinity for D2R.

Most prominent ADRs: weight gain, constipation, small bowel obstruction (can be FATAL), myocarditis, cardiomyopathy, leukopenia, granulocytopenia, and agranuclocytosis (can be FATAL)

Contraindications: WBC below 3500 cells/mm3, previous bone marrow disorder, hx of agranulocytosis during clozapine treatment

51
Q

Atypical Antipsychotics: Aripiprazole [Abilify] (General, MOA, and ADRs)

A

General: Can be used to treat schizophrenia, bipolar disorder, Autism Spectrum Disorder, adjunctive treatment in MDD

MOA: Partial agonist of D2 and 5-HT1A. Antagonist of 5-HT2A. Available PO and LAI.

ADRs: Low occurrence of EPS. Low potential for weight gain, sedation, and anti-muscarinic effects.

52
Q

Atypical Antipsychotic: Olanzapine (General, MOA, and ADRs)

A

General: Used for schizophrenia, acute treatment of manic or mixed episode with Bipolar I, maintenance treatment of Bipolar I, and treatment-resistant depression with fluoxetine.

MOA: Antagonist of 5-HT2A, D1, D2, alpha-adrenergic 1, 5-HT1A, muscarinic 1-5, and H1. Available PO and extended-release injectable suspension (Relprevv). Long-acting atypical IM (gluteal) injection indicated for schizophrenia.

ADRs: Weight gain, somnolence, dry mouth, dizziness, constipation, dyspepsia, increased appetite. Dose-related risk of EPS (akathesia, tremors). Transaminase elevation. BLACK BOX WARNING- cardiorespiratory arrest and sudden death; patients should be monitored for at least 3 hours after initial dose.

53
Q

Atypical Antipsychotic: Quetiapine (General, MOA, and ADRs)

A

General: Used for schizophrenia, acute treatment of manic episodes with Bipolar I, Bipolar depression, and off-label uses for sleep, anxiety, and delirium at low doses.

MOA: Relatively weak antagonist of D2, 5-HT2, 5-HT6, D1, H1, alpha-adrenergic 1 and 2. At low doses below 200 mg, no D2R blockade is appreciated. Available PO and extended release.

Most prominent ADRs: Least likely to cause EPS. DDIs with drugs that increase the QTc interval.

54
Q

Atypical Antipsychotic: Risperidone (General, MOA, and ADRs)

A

General: Used for acute and maintenance treatment of schizophrenia in adults and adolescents ages 13-17, acute manic episodes in Bipolar I (ages 10+), irritability associated with ASD in ages 5-16 years.

MOA: Antagonist of 5-HT2A, D2, alpha-adrenergic, and H1. Low affinity for muscarinic receptors. Available PO.

ADRs: Much lower likelihood of EPS, elevates prolactin, weight gain, anxiety, N/V, rhinitis, ED, increased pigmentation, dizziness, hyperkinesia, somnolence.

55
Q

Rate of relapse may be lower with ______ antipsychotic agents compared to ______ antipsychotics, particularly ______ vs. ______. ______ or more psychotic episodes secondary to schizophrenia usually require 5 years of treatment.

A

atypical; typical; risperidone; haloperidol; two

56
Q

Pharmacokinetics of the typical and atypical antipsychotics (2)

A
  1. First-pass metabolism

2. Most are completely metabolized by cytochrome P450 enzymes; CYP2D6, CYP1A2, CYP3A4

57
Q

Dosage and patient adherence of antipsychotic agents

A

The low-end of the dosage range should be tried for at least several weeks. Once-daily doses should usually be given at night for chronic maintenance treatment.

58
Q

Pharmacodynamic DDIs are more significant that pharmacokinetic DDIs. Additive effects of antipsychotics may occur when combined with: (4)

A
  1. Sedatives
  2. Alpha-adrenergic receptor blockers
  3. Anticholinergic drugs
  4. Quinidine-like action

*Antidepressants or benzodiazepines are sometimes used to manage depression and anxiety in psychotic patients.

59
Q

Antipsychotics and Overdose (6)

A
  1. Overdose is rarely fatal, with the exception of thioridazine, which causes TdP
  2. Drowsiness proceeds to coma, with an intervening period of agitation
  3. Neuromuscular excitability may be increased and proceed to convulsions
  4. Pupils are miotic, and DTRs are decreased
  5. Hypotension and hypothermia
  6. Patients should be given the usual “ABCD” treatment for poisonings and treated supportively

Mental Health/Psychiatry (6 decks)

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