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pr3153 > IC8 - Pharmacology of Antidepressants & Antipsychotics > Flashcards

IC8 - Pharmacology of Antidepressants & Antipsychotics Flashcards

1
Q

What does MAO inhibitors do?

A

Increase biological availability of monoamines

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2
Q

Phenelzine is ______ for MAO.

A

non selective

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3
Q

Is phenelzine an irreversible or reversible MAO inhibitor?

A

Irreversible

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4
Q

List 3 adverse effects of MAOIs.

A
  1. Postural hypotension
  2. Restlessness
  3. Insomnia
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5
Q

What is one DDI of MAOIs?

A

Drugs increasing serotoninergic function

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6
Q

What are the major food limitations of MAOIs?

A

Cheese and concentrated yeast products

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7
Q

What are the side effect that may arise due to drug food interaction with MAOIs?

A
  1. Acute hypertension
  2. Severe throbbing headache
  3. Intracranial haemorrhage
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8
Q

Explain how consumption of cheese with MAOI can lead to undesirable effects.

A
  1. Amines (e.g. tyramine) in foods (e.g. cheese) are broken down by MAO in the intestines and liver.
  2. MAOIs can lead to accumulation of tyramine and sympathomimetic effects.
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9
Q

Drug food interaction is less likely in ______, MAO-A selective inhibitor.

A

reversible

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10
Q

List one reversible, MAO-A selective inhibitor.

A

Moclobemide

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11
Q

Name one Tricyclic antidepressants that is selective for norepinephrine transporter.

A

Despiramine

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12
Q

Despiramine is selective for _____ transporter.

A

norepinephrine

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13
Q

Name three tricyclic antidepressants that is non-selective for norepinephrine or serotonin transporter.

A
  1. Imipramine
  2. Amitriptyline
  3. Nortriptyline
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14
Q

Imipramine, amitriptyline, nortriptyline are TCAs that are non-selective for ________ and ______ transporter.

A

norepinephrine, serotonin

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15
Q

What are the adverse effects of TCAs?

A
  1. Sedation (H1 Histamine antagonism)
  2. Postural hypotension (α-adrenoceptor sympathetic block)
  3. Dry mouth, blurred vision, constipation (muscarinic receptor antagonism)
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16
Q

List two SSRIs.

A
  1. Fluoxetine
  2. Citalopram
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17
Q

What are the advantages of SSRIs?

A
  1. Low affinity for αadrenoceptors (Lack of cardiovascular effects, safer in overdose)
  2. Lack of effect at histamine receptors (Reduced sedation)
  3. Low affinity for muscarinic cholinergic receptors (Minimal anticholinergic side
    effects (e.g. dry mouth and constipation)
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18
Q

What are the adverse effects of SSRIs?

A

Nausea, insomnia, sexual dysfunction

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19
Q

What are the two adverse effects that may be arise due to discontinuation/ rebound symptoms of withdrawal when plasma levels of drug drop between doses?

A

Nausea, insomnia

20
Q

What is one of the SSRIs that has sedative effects?

A

Citalopram

21
Q

What are severe reactions of SSRIs that can results from DDI with MAOIs?

A

Serotonin syndrome such as tremor, hyperthermia, cardiovascular collapse

22
Q

List three examples of serotonin and noradrenaline reuptake inhibitors (SNRIs).

A

Venlafaxine, desvenlafaxine, duloxetine

23
Q

What are the advantages of venlafaxine?

A
  1. Fewer adverse effects than TCAs.
  2. Work slightly faster than other antidepressants.
  3. Work better in treatment-resistant patients
24
Q

What are the adverse effects of SNRIs?

A
  1. Serotoninergic adverse effects (Nausea, Insomnia, Sexual dysfunction)
  2. Serotonin syndrome such as tremor, hyperthermia, cardiovascular collapse when combined with serotoninergic drugs and MAOIs.
25
Q

Withdrawal effects of SNRIs are ______ than for SSRI s and TCAs.

A

stronger

26
Q

All antipsychotic drugs are _____ antagonists.

A

D2 (dopamine)

27
Q

List 2 D2 receptor antagonists that are used as typical/ atypical antipsychotic.

A
  1. Haloperidol
  2. Clozapine
28
Q

What are the three dopamine pathways of the brain?

A
  1. Mesocortical/ Mesolimbic pathway
  2. Nigrostriatal pathway
  3. Tuberoinfundibular
29
Q

Atypical antipsychotics usually have _____ antagnosim effects.

A

5HT2 (serotonin)

30
Q

List two typical antipsychotics drugs.

A

Chlorpromazine
Haloperidol

31
Q

List 4 atypical antipsychotics drugs.

A
  1. Amisulpride
  2. Clozapine
  3. Olanzapine
  4. Risperidone
32
Q

Which antipsychotic drugs class has less extrapyramidal side effects?

A

Atypical

33
Q

What are the side effects of antipsychotic drugs?

A
  1. Sedation (H1 Histamine antagonism)
  2. Postural hypotension (α-adrenoceptor sympathetic block)
  3. Dry mouth, blurred vision, constipation (muscarinic receptor antagonism)
34
Q

Haloperidol has _____ sider effects than chlorpromazine.

A

lesser

35
Q

Halperidol is selective for the _____ receptor.

A

α1-adrenoceptor

36
Q

Most atypical antipsychotics have greater affinity at ______ and _____.

A

5HT2, D4

Note: These do not define atypicality

37
Q

What is the core of action for most atypical antipsychotic drug?

A

Serotonin-dopamine antagonism

38
Q

What is a major side effect of clozapine?

A

Agranulocytosis

39
Q

Dry mouth, constipation and blurred vision are evident in atypical antipsychotics particularly _______.

A

Clozapine, olanzapine

40
Q

List two atypical antipsychotics drugs where sedation as side effect is mainly evident.

A

Clozapine, Olanzapine

41
Q

Postural hypotension and reflex tachycardia is especially evident in _____, an atypical antipsychotic.

A

Risperidone

42
Q

Which atypical antipsychotic drug is a selective D2/3 antagonist?

A

Almisulpride

43
Q

List three adverse effects of amisulpride.

A
  1. Increased prolactin
  2. Breast swelling, pain, lactation
  3. Gynecomastia (males)
44
Q

List three atypical antipsychotics that can induce diabetes and weight gain

A

Clozapine
Olanzapine
Risperidone

45
Q

List 4 reasons for lack of EPS in atypical antipsychotics drugs.

A
  1. Potent 5-HT2A receptor antagonism vs. weak D2 antagonism (clozapine, olanzapine)
  2. High D3 to D2 antagonism ratio (amisulpride)
  3. High D4 to D2 antagonism ratio (clozapine)
  4. High D2 to D1 antagonism ratio (amisulpride, risperidone)

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