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Pharmacology Exam 6 > Antipsychotic > Flashcards

Antipsychotic Flashcards

1
Q

PSYCHOTIC DISORDERS - Definition

A

A group of conditions that involve loss of contact with reality

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2
Q

Types of Psychotic Disorders

A

Primary psychosis – no other underlying condition causing psychosis (“psychiatric” cause, e.g., schizophrenia, bipolar)

Secondary psychosis – due to “organic” causes such as drug toxicity, dementia, or a non-psychiatric illness

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3
Q

SCHIZOPHRENIA SYMPTOMS - POSITIVE

A

Positive symptoms - auditory, visual or tactile hallucinations, delusions, disorganized or bizarre behavior

Most dramatic; tend to prompt treatment

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4
Q

SCHIZOPHRENIA SYMPTOMS - NEGATIVE

A

Negative symptoms - inexpressive face or blank looks, few gestures, monotone or monosyllabic speech, inability to feel pleasure, incapacity to initiate volitional behavior

Seem subtle but greatest contributors to long-term impairment and poor QOL

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5
Q

SCHIZOPHRENIA SYMPTOMS - COGNITIVE

A

Cognitive symptoms - poor executive functioning, inability to focus or pay attention, impaired working memory

Seem subtle but greatest contributors to long-term impairment and poor QOL

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6
Q

DOPAMINE RECEPTORS

A

All dopamine receptors are GPCR

D1-like receptors are stimulatory

D2-like receptors are inhibitory (↓ AC, cAMP, PKA)

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7
Q

DOPAMINE PATHWAYS IN BRAIN

A

Antipsychotics block D2 receptors along all 4 pathways

mesocortical pathway

mesolimbic pathway

nigrostriatal pathway

tuberoinfundibular pathway

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8
Q

Mesocortical Pathway

A

DA neurons in the VTA release DA onto the…

frontal cortex (involved in planning, judgment, personality and social behavior)

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9
Q

Mesolimbic Pathway

A

DA neurons in the ventral tegmental area (VTA) release DA onto the…

nucleus accumbens (NAc) and limbic system (involved in reward, motivation & emotion)

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10
Q

Nigrostriatal Pathway

A

DA neurons in the substantia nigra (SN) release DA onto the…

striatum (regulates motor control, posture)

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11
Q

Tuberoinfundibular Pathway

A

DA neurons in the hypothalamus release DA onto the…

pituitary gland, involved in secretion of hormones (e.g., prolactin)

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12
Q

TYPICALS DRUGS– LOW & HIGH POTENCY

A

“First-generation antipsychotics” or “major tranquilizers” or “neuroleptics”

LOW - Chlorpromazine & Thioridazine
HIGH - Perphenazine & Haloperidol

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13
Q

TYPICALS – ADVERSE MOTOR EFFECTS

A

ADVERSE MOTOR EFFECTS extrapyramidal symptoms (EPS) via D2 block:

  • Acute dystonia
  • Parkinsonism
  • Akathisia
  • Tardive dyskinesia

Extrapyramidal tracts - originate in brainstem, carry motor signals to spinal
cord (includes nigrostriatal pathway) - mediates balance, posture, coordination

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14
Q

TYPICALS – ACUTE EXTRAPYRAMIDAL SIDE EFFECTS

A

Acute EPS appear early in treatment, they are dose-related and reversible

Akathisia - uncontrollable restlessness, urge to move

Parkinsonism – rigidity, tremor, bradykinesia (extreme slowness)

Acute dystonia – sustained muscle contractions → painful twisting, abnormal posture

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15
Q

TYPICALS – DELAYED EXTRAPYRAMIDAL SIDE EFFECTS

A

Tardive dyskinesia – repetitive, involuntary movements (grimacing, tongue thrusting, lip smacking, rapid blinking)

Tardive dyskinesias can occur after prolonged use of antipsychotics – higher risk with greater D2 blockade

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16
Q

TYPICALS – OTHER ADVERSE EFFECTS

A

Hyperprolactinemia – due to block of receptors in tuberoinfundibular DA pathway; Causes reproductive organ and endocrine problems in both women and men

Neuroleptic malignant syndrome (NMS) - rare, but life-threatening, idiosyncratic
reaction to dopamine-blocking drugs, characterized by…
- fever
- muscular rigidity
- altered mental status
- autonomic dysfunction

low-potency typicals most potently block these three off-target receptors (histamine, muscarinic and adrenergic)

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17
Q

ATYPICAL ANTIPSYCHOTICS

A

Atypicals are “atypical” due to lack of neuroleptic effects (once thought essential)

MOA: Block 5-HT more strongly than D2; Lower risk of dopamine-related adverse
effects (EPS, NMS, hyperprolactinemia)

Atypical antipsychotics are now more commonly prescribed than typicals

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18
Q

CLOZAPINE

A

THE FIRST ATYPICAL (produces negligible EPS)

USE: treatment-resistant patients only; schizophrenia (more effective)

BLACK BOX WARNINGS…

  1. Agranulocytosis → REMS program
  2. Orthostatic hypotension / bradycardia
  3. Seizures
  4. Myocarditis / cardiomyopathy
  5. Dementia-related psychosis
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19
Q

ATYPICAL ANTIPSYCHOTICS – RECEPTOR BLOCKING

A

Like high potency typicals, atypicals have fewer off-target side effects

MOA: Atypicals block serotonin receptors more strongly than dopamine receptors;
serotonin blockade may contribute to therapeutic and adverse effects

20
Q

ATYPICAL ANTIPSYCHOTICS – ADVERSE EFFECTS

A

clozapine & olanzapine cause metabolic problems, including weight gain (drug discontinuation), dyslipidemia, and type 2 diabetes, requiring monitoring

Samidorphan, an opioid receptor antagonist is given with olanzapine to reduce weight gain

Prolonged QTc interval - caused by inhibition of the delayed potassium rectifier current IKr (rapid) by specific drugs

Retinal deposits:

  • Thioridazine only**
  • Associated with browning of vision
21
Q

Treatments

A

Drugs reduce symptoms

Atypicals are slightly better for treating negative symptoms

High rates of discontinuation for all antipsychotics

22
Q

What factors make treatment adherence difficult in schizophrenia?

A
  • Severe, unpleasant, disabling drug side effects / incomplete efficacy
  • Lack of insight about being ill
  • Increased rates of unemployment, homelessness, substance use
23
Q

What approaches can increase compliance?

A
  • Counseling and support
  • Behavioral strategies
  • Long-acting injections (depot)
24
Q

Which pathways likely mediate the therapeutic effects of antipsychotic agents?

A

MC & ML

25
Q

Which pathways likely contribute to the adverse effects of antipsychotic agents?

A

NS and TI

26
Q

(a) Name 4 antipsychotic adverse effects (extrapyramidal effects) that result from D2R blockage along the nigrostriatal pathway
(b) Which 3 occur immediately after starting an antipsychotic, or increasing the dose, and are dose-related and reversible?
(c) Which 1 occurs only after prolonged antipsychotic drug use, and can be irreversible after a certain point?

A

Acute EPS appear early in treatment; they are dose-related and reversible

  1. Akathisia: uncontrollable restlessness, urge to move
  2. Parkinsonism: rigidity, tremor, bradykinesia (extreme slowness)
  3. Acute Dystonia: sustained muscle → painful twisting, abnormal posture
  4. Tardive Dyskinesia: repetitive, involuntary movements (grimacing, tongue thrusting, lip smacking, rapid blinking)

(b)
- Akathisia: uncontrollable restlessness, urge to move

  • Parkinsonism: rigidity, tremor, bradykinesia (extreme slowness)
  • Acute Dystonia: sustained muscle → painful twisting, abnormal posture

(c)

  • Tardive Dyskinesia: repetitive, involuntary movements (grimacing, tongue thrusting, lip smacking, rapid blinking
  • Can occur after prolonged use of antipsychotics - higher risk with greater D2 blockade
  • Irreversible if not caught early
  • Patient pay not notice symptoms
27
Q

Name 1 antipsychotic adverse effect that results from D2R blockage along the tuberoinfundibular pathway – what general kinds of problems does this cause?

A

Hyperprolactinemia: due to block of receptors in tuberoinfundibular DA pathway: causes reproductive organ and endocrine problems in both women and men

28
Q

Name 1 rare but life-threatening idiosyncratic reaction to dopamine-blocking drug

A

Neuroleptic malignant syndrome (NMS) - rare, but life-threatening, idiosyncratic reaction to dopamine-blocking drugs, characterized by fever, muscular rigidity, altered mental status, and autonomic dysfunction

29
Q

Rank the classes of antipsychotic agents from most to least likely to produce dopamine-blockage related adverse effects.

A
  • Low-potency typicals most potently block off target receptors
  • Atypicals have weaker dopamine blockage affinity, but stronger serotonin receptor affinity
30
Q

What type of receptors are D2 dopamine receptors?

A

D2-like receptors are inhibitory; decrease AC, cAMP, PKA

31
Q

Are antipsychotics agonist or antagonist at D2 receptors?

A

antagonists

32
Q

rank the classes of antipsychotic agents from strongest to weakest binding at D2 receptors

A
  • Atypicals- weakest binding at D2 receptor

- Typical antipsychotics side chains affect “tightness” of binding to D2 and other receptors

33
Q

Are binding affinity and potency related – how? And is this the same as efficacy?

A

Yes, binding affinity and potency are similar in that they decide dose and side effects

Efficacy is equivalent to intrinsic affinity

34
Q

Which class of antipsychotics binds serotonin receptors with the highest affinity, and more strongly than they block D2 receptors?

A

Atypicals

35
Q

What types of side effects arise from antipsychotics’ antagonist effects at dopamine (see objective A), serotonin, histamine, and adrenergic receptors?

A

Dopamine: extrapyramidal symptoms, weight gain, endocrine effects

Seortonin: weight gain, diabetes, increased appetite

Histamine: weight gain, diabetes, sedation

Adrenergic: postrural hypotension, dizziness, syncope

36
Q

Which antipsychotic class most potently blocks off-target receptors?

A

Low potency typicals (histamine, muscarinic and adrenergic)

37
Q

Blockage of which two types of neurotransmitter receptors contributes to the therapeutic effects of antipsychotics?

A

Blockage of serotonin and dopamine receptors

38
Q

Which class is most likely to produce weight gain, dyslipidemia and type 2 diabetes?

A

Atypicals; requires monitoring

Weight gain is major cause of drug discontinuation

39
Q

Do antipsychotic drugs cure or prevent schizophrenia?

A

No, antipsychotic drugs just treat the symptoms of schizoprenia

40
Q

How long does it take for antipsychotics to produce clinical improvements, and why?

A

Clinical improvements are delayed; usually become maximal over weeks to months

41
Q

Are the 3 classes similarly effective for positive symptoms? What about negative symptoms?

A

All antipsychotics have similar efficacy against positive symptoms
Atypicals are more effective at treating negative symptoms

42
Q

What was the first atypical antipsychotic, and what is its major use today?

A

Clozapine: The First Atypical antipsychotic - produce negligible EPS
- Despite safety concerns, is approved for use (with monitoring) for treatment-resistant patients only

43
Q

What are the 5 black box warnings for clozapine?

A

Clozapine/s 5 FDA Black Box Warnings:

  1. Agranulocytosis → REMS program
  2. Orthostatic hypotension / bradycardia
  3. Seizures
  4. Myocarditis / cardiomyopathy
  5. Dementia-related psychosis
44
Q

Are antipsychotics generally well-tolerated?

A

Antipsychotics show a high rate of discontinuation, with percentage of patients with first-episode schizophrenia discontinuing treatment within one year

45
Q

What is the major cause of discontinuation of atypical antipsychotics?

A

Severe, unpleasant, disabling drug side effects / incomplete efficacy
Lack of insight about being ill
Increased rates of unemployment, homelessness, substance use

Pharmacology Exam 6 (5 decks)

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