7.2: Antipsychotic & Antidepressants Flashcards

1
Q

A study of the drugs that affect cognition, affect, and behavior of an individual.

A

Psychopharmacology

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2
Q

Inability to distinguish between what is real and what is not real such as:

  • Delusions
  • Hallucinations
  • Disorganized thinking with clear sensorium
A

Psychosis

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3
Q

What is the most common psychotic disorder?

A

Schizophrenia

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4
Q

This disorder has a structural and functional changes in the brain, and dysregulated neurotransmitters.

A

Schizophrenia

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5
Q

3 Neuronal Networks of Psychosis

A
  • Dopamine theory
  • NMDA theory
  • Serotonin theory
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6
Q

Identify this neuronal network of psychosis:

A classic and one of the most enduring ideas in psychopharmacology.

A

Dopamine hypothesis of psychosis

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7
Q

Identify this neuronal network of psychosis:

Increasing evidence implicates both serotonin and glutamate
networks.

A

dopamine hypothesis of psychosis

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8
Q
  • Reduce psychotic symptoms
  • Improve mood and reduce anxiety
  • Neuroleptic
A

Antipsychotic drugs

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9
Q

It is an antipsychotic drug with high incidence of EPS.

A

Neuroleptic

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10
Q

Typical / Classic Drugs of Antipsychotic drugs

A

Phenothiazine
Thioxanthine
Butyrophenone

Mnemonic: PettyBoo (PheThiBu)

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11
Q

Atypical / Newer Agents of Antipsychotic drugs

A

Clozapine
Olanzapine
Risperidone
Quetiapine
Ziprasidone
Aripiprazole

Mnemonic: CROQZA >:( !!

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12
Q

What are the receptors of Typical / Classic Drugs?

A

D2&raquo_space; 5-HT2 receptors

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13
Q

What are the receptors of Atypical / Newer Agents?

A

5-HT2&raquo_space; D2 receptors

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14
Q

Pharmacokinetics:

Well absorbed when administered _____?

A

orally

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15
Q

Pharmacokinetics:

Antipsychotic drugs are extensively bound to ____?

A

plasma proteins

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16
Q

[ Modified T or F ]

Antipsychotic drugs are lipid soluble and short half-lives.

A

First statement is true, Second statement is false.

Should be LONG half-lives

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17
Q

Parenteral forms of Antipsychotic drugs

A
  • Fluphenazine
  • Haloperidol
  • Ziprasidone
  • Olanzapine
  • Aripiprazole

For rapid initiation of tx, uncooperative patients, or depot.

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18
Q

Identify this neuronal network of psychosis:

Schizophrenia is due to excess of functional DA in mesocortical tracts in the brain.

A

Dopamine hypothesis

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19
Q

Dopamine receptors

A
  • GPCR, D1-D5
  • D2
  • Blockade of D2 - EPS
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20
Q

Identify what dopamine receptors:

Located in the caudate, putamen, cortex, hypothalamus – negatively coupled to adenylyl cyclase.

A

D2

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21
Q

[Dopamine receptors]

EPS (tremor, slurred speech, akathisia, dystonia)

A

Blockade of D2

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22
Q

Affinity for other receptors:

A

Atypical antipsychotics

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23
Q

True or False:

Atypical antipsychotics has less EPS than first generation drugs.

A

True

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24
Q

All antipsychotic drugs block H1 receptor to some degree except:

A
  • Haloperidol
  • Iloperidone
  • Lurasidone
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25
Q

What are the effects of first generation drugs?

A

dopamine receptor blockade

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26
Q

Effects of Mesocortical-mesolimbic pathway

A

Antiemetic effect due to blockade of the chemoreceptor trigger zone

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27
Q

Common adverse effects of First generation drugs

A

Extrapyramidal symptoms, hyperprolactinemia (1st Generation)

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28
Q

Treatment of schizophrenia

A
  • Hyperactivity, bizarre thoughts, delusions and hallucinations
  • Effects take several weeks to develop
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29
Q

Clinical use of 1st generation

A

lower cost, EPS

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30
Q

Clinical use of 2nd generation

A
  • Improves negative symptoms
  • emotional blunting, social withdrawal, lack of motivation)
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31
Q

Treatment for mania

A
  • Lithium
  • Second generation drugs, with benzodiazepenes
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32
Q

Prevention of manic phase of bipolar disorder

A
  • Aripiprazole
  • lanzapine
  • Asenapine
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33
Q

What are the drugs used to prevent bipolar depression?

A
  • Quetiapine
  • Lurasidone
  • Olanzapine
  • Carizapine
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34
Q

Treatment for Tourette syndrome

A

Molindone

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35
Q

Treatment for Psychotic symptoms in Alzheimers and Parkinsonism

A

Molindone

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36
Q

Reversible neurologic effects

A

Toxicity

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37
Q

Parkinson-like symptoms

A

Dose-dependent EPS

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38
Q

Dose-dependent EPS, which can resemble Parkinson-like symptoms, are common with __________. However, they are less frequent with _____________

A

• high-potency first-generation antipsychotics like Haloperidol, Fluphenazine, and Trifluoperazine

• second-generation drugs like Clozapine.

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39
Q

True or False:

Dose-dependent EPS management typically involves increasing the dose and using antimuscarinic agents to alleviate symptoms.

A

False

Should be reducing the dose.

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40
Q

Dose-dependent EPS movement problems such as akathisia (restlessness) and dystonias (involuntary muscle contractions) are also observed and can be managed with _______?

A

antimuscarinic agents or diphenhydramine

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41
Q

Endocrine effects of antipsychotic medications can include primarily __________. These effects are particularly prominent with medications like __________.

A

• hyperprolactinemia, gynecomastia, and infertility ( due to the blockade of dopamine D2 receptors in the pituitary gland )

• Risperidone

42
Q

Toxicity of Neuroleptic malignant syndrome

A

hyperthermia

43
Q

Neuroleptic malignant syndrome treatment typically involves medications such as

A

dantrolene, diazepam, and dopamine agonists.

44
Q

marked with chlorpromazine

A

Sedation

45
Q

Among the antipsychotics, ______ & _______ are among the least sedating options, while aripiprazole and lurasidone are also known for causing less sedation.

A

fluphenazine and haloperidol

46
Q

Visual toxicity

A

retinal deposits with thioridazine

47
Q

Cardiac rhythm abnormalities toxicity

A
  • Thioridazine
  • Quetiapine
  • Ziprasidone
48
Q

Agranulocytosis toxicity

A

Clozapine

49
Q

Commonly used for manic phase of bipolar disorder

A

Lithium

50
Q

MOA of lithium

A

inhibits enzymes for recycling neuronal membrane phosphoinositides → depletion of PIP2 , IP3, DAG →
prevents amine neurotransmission

51
Q

[ T or F ]

It is important to monitor plasma level to establish effective and safe dosage for lithium

A

True

52
Q

Used in bipolar disorder to decrease manic behavior and reduces frequency and magnitude of mood swings.

A

Lithium

53
Q

Lithium toxicity

A
  • Tremor, ataxia, sedation, aphasia [ TASA ]
  • Thyroid enlargement
  • Cardiac abnormalities in the fetus
54
Q

Other drugs for Bipolar Disorder

A

Antiseizure drugs:
• Valproic acid
• Carbamazepine and lamotrigine

55
Q

Prolongs inactivation of voltage gated Na channels, GABAA agonist

A

Valproic acid

56
Q

antimanic effects when failed to respond to lithium

A

Valproic acid

57
Q

Prolongs inactivation of voltage gated Na channels

A

Carbamazepine and lamotrigine

58
Q

for mania and prophylaxis of depressive phase

A

Carbamazepine and lamotrigine

59
Q

Feelings of sadness and or loss of interest in normally pleasurable activities, leading to emotional and physical problems, with resulting impairment in social, occupational and other areas of functioning for 2 weeks.

A

Depression

60
Q

Depression symptoms

A
  • Depressed mood
  • Changes in appetite
  • Sleeping problems
  • Fatigue
  • Feeling of guilt and worthlessness
  • Concentration problems
  • Suicidal thoughts
61
Q

Monoamine hypothesis

A

• noradrenaline
• dopamine
• serotonin

62
Q

Hyperactive dopamine in the mesolimbic pathway

A

Dopamine theory

63
Q

Identify what neuronal network of psychosis:

NMDA receptor hypofunction

A

NMDA theory

64
Q

5-HT2A receptor hyperfunction in the cortex

A

Serotonin theory

65
Q

Depression is associated with loss of neurotrophic support

A

Neurotrophic hypothesis

66
Q

Identify what pathopsyiology:

For neural plasticity, resilience, and neurogenesis.

A

Brain-derived neurotrophic factor (BDNF)

67
Q

Tricyclic antidepressants examples

A
  • Amitryiptyline
  • Clomipramine
  • Imipramine
68
Q

Related to phenothiazine antipsychotics

A

Tricyclic antidepressants

69
Q

Identify this antidepressant:

Well absorbed orally, but undergo first-pass effect

A

Tricyclic antidepressants (TCA)

70
Q

• Excessive hepatic metabolism required
• Forms active metabolites

A

Tricyclic antidepressants

71
Q

Long half life (OD dosing)

A

Tricyclic antidepressants

72
Q

Selective serotonin reuptake inhibitors example

A
  • Paroxetine
  • Escitalopram
  • Fluoxetine
  • Fluvoxamine
  • Sertraline

PEFFS

73
Q

Require hepatic metabolism

A

Selective serotonin reuptake inhibitors

74
Q

half life of several days – once a week dosing

A

Fluoxetine

75
Q

Heterocyclics examples

A
  • Bupropion
  • Amoxapine
  • Mirtazapine

HETERO BAM!

76
Q

Pharmacokinetics similar to TCA

A

Heterocyclics

77
Q

Identify this antidepressant based on its pharmacokinetics:

Short half lives
(BID to TID dosing)

A

Nefazodone and trazodone

5-HT2 antagonist

78
Q

5-HT-NE reuptake inhibitors

A
  • Duloxetine
  • Venlafaxine
79
Q

5-HT antagonists

A
  • Nefazodone
  • Trazodone
80
Q

Monoamine Oxidase Inhibitors examples

A
  • Phenelzine
  • Selegiline
  • Tranylcypromine

PST MOA !

81
Q

Related to amphetamines and orally active

A

Monoamine Oxidase Inhibitors

82
Q

metabolizes NE, Epinephrine, Serotonin

A

MAO-A

83
Q

metabolizes Dopamine, Tyramine

A

MAO B

84
Q

fastest in onset, short duration of action and Inhibitors of hepatic drug metabolizing enzymes

A

Tranylcypromine

85
Q

Other drugs with antidepressant action

A

Ketamine
Brexanolone

86
Q

NMDA antagonist

A

Ketamine

87
Q

modulator of GABA A receptors

A

Brexanolone

88
Q

What drug is used for postpartum depression?

A

Brexanolone

89
Q

Anesthetic agent that has antidepressant action as long as 1 week

A

Ketamine

90
Q

• Inhibit the reuptake transporters that terminate the actions of NE and 5-HT

• Blocks H receptors and α-adrenoceptors

A

Tricyclic antidepressants

91
Q

Identify this antidepressant:

  • Highly selective on Serotonin Transporter (SERT) - allosterically inhibit the transporter
  • Minimal inhibitory effects on NE
A

SSRI

92
Q

Bind to transporters for both serotonin and NE

A

SNRI

93
Q

• Nefazodone and trazodone – blocks 5HT2A receptor in
the neocortex
• Anti-anxiety and anti-depressant

A

5-HT2 Receptor Antagonist

94
Q

• Increase brain amine levels, interfering with metabolism
→ increase in vesicular stores of NE and 5-HT

A

MAO Inhibitor

95
Q

increase amine release by antagonism
of α-2 receptors

A

Mirtazapine

96
Q

no effect on 5-HT or NE amine ransporters

A

Bupropion

97
Q

Clinical Uses of Major depressive disorders

A
  • Primary indication of antidepressants
  • Newer drugs more tolerable side effects (SSRI, SNRI, 5-HT
    antagonists, certain heterocyclics)
98
Q

Identify this pharmacologic effects:

  • Sympathomimetic effects - Increase NE
  • Chronic use - low BP
A

Amine uptake blockage

99
Q

Identify this pharmacologic effects:

Common in TCA and heterocyclic (mirtazapine) and 5-HT2 blockers (nefazodone and trazodone)

A

Sedation

100
Q

Identify this pharmacologic effects:

  • Occurs with all TCA except amitryptaline and doxepine
  • Atroine like effects - minimal with SSRI and buproprion
A

Muscarinic blockade

101
Q

Identify this pharmacologic effects:

  • Common with TCA: hypotension, arrhythmias
  • Cardiotoxicity: venlafaxine
A

Cardiovascular effects

102
Q

Identify this pharmacologic effects:

  • TCA and MAOIs lower consulsive threshold
  • Overdoses of maprotiline and SSRI’s
A

Seizures