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PR3153 > Antipsychotics Pharmacology > Flashcards

Antipsychotics Pharmacology Flashcards

1
Q

List 2 1st Gen antipsychotics

A

Chlorpromazine, Haloperidol,
Mesoridazine, Trifluoperazine, Perphenazine, Loxapine, Mloindone, Fluphenazine, Flupenthixol, Zuclopenthixol, Pipothiazine, Sulpiride

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2
Q

List 3 2nd Gen antipsychotics

A

Clozapine, Olanzapine, Quetiapine, Risperidone, Amisulpride, Aripiprazole,
Paliperidone, Ziprasidone, Brexpiprazole, Asenapine, Iloperidone, Lurasidone, Cariprazine, Lumateperone

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3
Q

What drugs causes EPS? What’s the mechanism?

A

1st and 2nd gen antipsychotics
D2 antagonism in nigrostriatal pathway

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4
Q

Atypical antipsychtics produce less severe EPS due to:

A
  • Greater 5-HT2 and D4 affinity
  • Mixed antagonism at α-adrenergic, H1, muscarinic acetylcholine, and 5-HT2 receptors

D4 are less abundantly found in striatum, striatum contains mostly D1 and D2

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5
Q

List the presentation, risks and management of Dystonia

A
  • Presentation: muscle spasms
  • Risks: FGAs (haloperidol), neuroleptic-naive pts, young maes
  • Management: IM anticholinergics

EPS: dystonia, pseudo-parkinsonism, akathisia, tardive dyskinesia
Anticholinergics: benztropine, diphenhydramine

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6
Q

List the presentation, risks and management of Akathisia

A
  • Presentation: restlessness
  • Risks: FGAs > risperidone > olanzapine > quetiapine, clozapine
  • Management: ↓antipsychotic dose/ switch to SGA, clonazepam PRN, propranolol 20mg TDS (max 160mg/d)

EPS: dystonia, pseudo-parkinsonism, akathisia, tardive dyskinesia

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7
Q

List the presentation, risks and management of Pseudo-Parkinsonisn

Is pseudo-parkinsonism reversible?

A
  • Presentation: tremors, cogwheel rigidity, bradykinesia
  • Risks: Elderly female, neurologic damage (trauma, stroke)
  • Management: ↓antipsychotic dose/ switch to SGA, anticholinergics PRN

Occurs within 1st few weeks of tx, reversible once drug is stopped

EPS: dystonia, pseudo-parkinsonism, akathisia, tardive dyskinesia
Anticholinergics: benztropine, diphenhydramine

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8
Q

List the presentation, risks and management of Tardive Dyskinesia

Is tardive dyskinesia reversible?

A
  • Presentation: orofacial movements, choreiform hand movements, pelvic thrusting
  • Risks: FGAs > SGAs, pts who develop acute EPS when initiated on FGAs, worsen w anticholinergics
  • Management: discontinue anticholinergics, ↓antipsychotic dose/ switch to SGA, clonazepam PRN, valbenazine 40-80mg/d

is Irreverisble!

EPS: dystonia, pseudo-parkinsonism, akathisia, tardive dyskinesia
Valbenazine: reversible inhibitors of vesicular monoamine transporter 2 (VMAT2)

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9
Q

List the presentation, risks and management of hyperprolactinemia

A
  • Presentation: breast swelling, lactation, gynaecomastia
  • Risks: FGAs, paliperidone ≥ risperidone > other SGAs
  • Management: ↓FGAs dose, switch to aripiprazole, dopamine agonists (amantadine, bromocriptine)

Hyperprolactinemia occurs due to increased prolactin secretion, due to dopamine blockade in anterior pituitary gland/ tuberoinfundibular pathway

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10
Q

List the presentation, risks and management of α-adrenergic antagonism

A
  • Presentation: postural hypotension
  • Risks: chlorpromazine, clozapine > risperidone, quetiapine, paliperidone > olanzapine, aripiprazole, ziprasidone, lurasidone
  • Management: switch to lower risk agents, NIL SEs for amisulpride
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11
Q

List the presentation, risks and management of muscarinic antagonism

A
  • Presentation: dry mouth, constipation, blurred vision, orthostatic hypotension, weight gain, arrhythmias, seizure
  • Risks: FGAs, clozapine, olanzapine > other SGAs
  • Management: switch to lower risk agents, NIL SEs for amisulpride/ haloperidol
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12
Q

List the presentation, risks and management of H1 antagonism

A
  • Presentation: sedation
  • Risks: chlorpromazine > clozapine > quetiapine > olanzapine > risperidone, aripiprazole, paliperidone
  • Management: switch to lower risk agents, NIL SEs for amulsipride/ haloperidol
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13
Q

List the presentation, risks and management of IKr antagonism

A
  • Presentation: QTc prolongation
    Risks:
  • High doses, IV haloperidol, ↓K+, IHD, female
  • Chlorpromazine > ziprasidone > haloperidol > iloperidone > quetiapine > risperidone > olanzapine
  • Management: switch to lower risk agent if QTc >440ms (males) or 470ms (female), refer to cardio if >500ms
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14
Q

1st gen antipsychotics antagonises ________ only, whereas 2nd gen antagonises both ________ and ________.

________ antagonism improves ________ symptoms. ________ antagonism improves ________ symptoms.

A

dopamine, dopamine and serotonin

Dopamine antagonism: improves positive symptoms (delusions, paranoia, hallucinations, etc.)
Serotonin antagonism: improves negative symptoms (social withdrawal)

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15
Q

List the presentation, risks and management of 5-HT antagonism

A
  • Presentation: (metabolic) weight gain, DM, increase in lipids
    Risks:
  • High doses, IV haloperidol, ↓K+, IHD, female
  • Chlorpromazine > ziprasidone
  • Management: switch to lower risk agents, NIL SEs for amulsipride/ haloperidol
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16
Q

List the presentation, risks and management of neuroleptic malignant syndrome

A
  • Presentation: muscle rigidity, fever, autonomic dysfunction, altered consciousness, increased creatinine kinase
  • Risks: all antipsychotics
  • Management: IV dantrolene 50mg TDS, oral dopamine agonist (amantadine, bromocriptine), switch to SGAs
17
Q

List the risks and management of agranulocytosis

A
  • Risks: clozapine
  • Management: discontinue if severe -> WBC < 3 x 109/L or ANC < 1.5 x 109/L
18
Q

What antipsychotics are safe to use in pregnancy? What to monitor?

A

Olanzapine, clozapine
Monitor for gestational DM

19
Q

What antipsychotics are safe/ not safe to use in breastfeeding?

A

Safe: Olanzapine, quetiapine
Not safe: clozapine (continue on drug and not breastfeed)

20
Q

What antipsychotics are safe/ not safe to use in renal impairment?

A

Safe: aripiprazole
Not safe: amisulpride, sulpiride

21
Q

What antipsychotics are safe/ not safe to use in hepatic impairment?

A

Safe: amisulpride, sulpiride
Not safe: aripiprazole

22
Q

What conditions should the use of antipsychotics be cautioned in?

11

A
  • QTC prolongation (C/I!)
  • Parkinson’s disease
  • Epilepsy and conditions predisposing to seizures
  • Depression
  • Myasthenia gravis
  • Prostatic hypertrophy
  • Angle-closure glaucoma
  • Severe respiratory disease
  • Hx of jaundice
  • Blood dyscrasias, esp for clozapine
  • Elderly with dementia

PR3153 (10 decks)

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