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Psychiatry > Antipsychotics MOA > Flashcards

Antipsychotics MOA Flashcards

1
Q

D2 antagaonization adverse effects

A

Mesolimbic: Reduction of positive sx
Mesocortical: worsen/cause negative sx
Tuberofundibular: hyperprolactinemia
Nigrastriatal: worsening of movement disorders (EPS early, TD late effect)

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2
Q

Clinical effects of D2 antagonism

A

Reduce positive sx of schizophrenia

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3
Q

Histamine (H1) antagonism

A

Sedation, apprtite stimulation, weight gain

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4
Q

Muscarinic (M1) antagonism

A

Anticholinergic effects

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5
Q

Noradrenergic (alpha-1)

A

Orthostatic hypotension

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6
Q

Serotonin (5-HT2A)

A

May increase DA activity in mesocortical pathway (improving -ve sx) and nigrostriatal (decreasing EPS)

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7
Q

Lab tests for Antipsychotics general

A 
ECG at baseline 
EEG if seizures of myoclonus occur
Fasting blood glucose at baseline and routinely (6mo,12mo then annually) 
A1c if impaired fbg ot diabetes present
Lipid at baseline and routinely as indicated 
CBC baseline and as indicated 
LFT baseline then 1mo then as indicated
Prolactin level as indicated
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8
Q

What are 2nd gen AP?

A 
Olanzapine 
Quetiapine 
Risperidone 
Paliperidone
Ziprasidone
Lurasidone
Asenapine
Clozapine
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9
Q

What are 3rd gen AP

A

Brexpiprazole

Aripiprazole

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10
Q

What are 1st gen AP

A

Low: Chlorpromazine, methotrimeprazine
Inter: loxapine, perphenazine, zuclopenthixol
High: flupentixol, fluphenazine, haloperidol, pimozide, trifluoperazine

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11
Q

What determines potency?

A

D2 receptor binding affinity

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12
Q

Low vs high potency AE

A

Low potency cause more alpha-1, H1, and M1 AE (postural hypotension, sedation, anticholinergic)
High potency cause more D2 related AE (EPS, hyperprolactinemia)
Moderate potency fall in between

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13
Q

FGA general Adverse Effects

A

CNS: confusion, disturbed concentration, disorientation (high dose/elderly), EPS, TD, NMS, sedation, seizures (lower threshold)
Anticholinergic: blurry vision, dry eyes, constipation, delirium, dry mouth, urinary retention
CV: arrhythmias, QTc, tachycardia, ortho hypotension, syncope, VTE,
Endocrine: dyslipidemia, antidiuertic hormone dysfunction (polydipsia, hyponatremia), glucose intolerance, hyperprolactinemia, metabolic syndrome, weight gain
GI: sialorrhea, dyspepsia
Sexual: decreased libido, anorgasmia, ejaculatory/erectile dysfunction,
Heme: blood dyscrasias (aplastic anemia, eosinophilia, leukopenia, thrombocytopenia)
Temperature dysregulation

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14
Q

FGA discontinuation syndrome

A

Exacerbation of psychosis, movement disorders, rebound type reaction when prolonged antagonist is removed, other typical D/C symptoms (N/V, diaphoresis, insomnia, anxiety, confusion, muscle pain etc.)

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15
Q

DI with alpha-1 blockers (prazosin, doxazosin etc.) effect

A

Additive hypotension, esp with low potency

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16
Q

DI with adsorbants (cholestyramine, charcoal, attapulgite) effects

A

Oral absorption decreased when used simultaneously; give 1h before or 2h after AP

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17
Q

DI with antiarrhythmics

A

Amiodarone and quinidine inhibit CYP2D6 and may increase some FGA levels

Dont combine with chlorpromazine, fluphenazine, pimozide or thioridazine, phenothiazines or zuclopenthixol; caution due to QTc prolongation and arrhythmias

18
Q

DI with Macrolides (clarith, eryth, telithromycin)

A

Possible additive QT prolongationand arrhythmias

Clarithromycin inhibit CYP3A4

19
Q

DI with quinolones (cipro, levo, moxifloxacin)

A

Possible additive QTc prolongation/arrhythmias

Cipro inhibits CYP1A2

20
Q

DI with anticholinergics

A

Increased side effect risk

21
Q

DI with warfarin

A

Chlorpromazine/halodol decrease INR

22
Q

DI with anticonvulsants

A

FGA may reduce seizure threshold

Carbamazepine: induction of CYP3A4/1A2/2D6 and UGT1A4

Phenytoin: induces CYP2C9/3A4
Phenobarbital induces CYP2C9/3A4/1A2

23
Q

DI with Antidepressants

A

Additive QTc prolongation

Fluvoxamine inhibit CYP1A2/3A4
Paroxetine/fluoxetine/duloxetine inhibit 2D6

24
Q

DI with antifungals

A

Additive QTc prolongation

Ex: ketoconazole inhibits CYP3A4

25
Q

DI with antihypertensives

A

Additive hypotension effect
Additive QTc prolongation
B-blocker ex: propranolol inhibits CYP2D6

26
Q

DI with antiretrovirals

A

Varying degrees of inhibition of CYP2D6/3A4

27
Q

DI with antitubercular (rifampin, isoniazid etc)

A

Induce CYP3A4 and/or P-gp

28
Q

DI with diuretics (lasix, HCTZ)

A

Addititive QTc prolongation, electrolyte disturbances

29
Q

DI with H2 antagonists (cimetidine)

A

Reduced absorption fue to reduced gastric pH, inhibition of CYP2D6

30
Q

DI with OC (estrogen)

A

Potentiates hyperprolactinemia

31
Q

DI with prokinetic/antiemetic (metoclopramide)

A

Metoclopramide is a potent central dopamine receptor antagonist that can cause EPS, hyperprolactinemia, and rarely NMS - may increase AE with AP

32
Q

DI with smoking

A

Hydrocarbons of smoking induce CY1A2

33
Q

DI with stimulants

A

AP may impair stimulatory effects of amphetamines

34
Q

DI with sympathomimetics (cocaine, epinephrine, dopamine)

A

Increased EPS risk with cocaine
Epi/Dopa avoid use for treatment of FGA-induced hypotension due to block of periphera alpha1 preventing alpha vasoconstricting effects and leaving beta receptors unopposed

35
Q

DI with zileuton

A

Inhibits CYP3A4

36
Q

What is metabolic syndrome?

A

A cluster of CVD risk factors that include: abdominal obesity, hypertension, impaired glucose tolerance,

37
Q

Clozapine plasma levels?

A

350-550 ng/mL or 1050-1650 nmol/L

38
Q

Clozapine lab monitoring on initiation and dose changes, CBC (neutrophils, WBC)

A

Hypotension, sedation, and seizures

39
Q

Which drug may result in a methadone false positive drug screen?

A

Quetiapine

40
Q

Which electrolytes to check for ziprasidone

A

Serum K and Mg, especislly is starting or starting a diuretic

41
Q

What SGAs need to be taken with food?

A

Lurasidone (>350 cal)
Ziptasidone (>500 cal)
Arsenapine AVOID food/drink 10min post dose
Quetiapine take with or without but stay consistant as high fat meal (800-1000 cal) increase exposure which maybe relevant for some patients
Risperidone avoid cola or tea
Grapefruit juice: avoid clozapine, iloperidone, quetiapine, ziprasidone

Psychiatry (2 decks)

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