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Flashcards in pharmacology of psychosis Deck (59):
1

neuroleptic

any drug that modifies psychotic behavior and exerts antipsychotic effect

aka antipsychotic

2

psychotropic

any drug used to treat mental illnesses

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group of antipsychotics found to be more useful in treating both positive and negative symptoms of schizophrenia

atypical

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AIMS

involuntary movement scale used to monitor for EPSEs and other effects in schizophrenia patients taking antipsychotics

5

first line treatment for non-psychiatric inpatients experiencing agitation and/or delirium

haloperidol (haldol)

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depot antipsychotics

long-acting, injectable formulations used for long-term maintenance therapy of schizophrenia

subq or IM; releases active compound consistently over long period of time

7

depot preparations available for (3)

- haloperidol decanoate (haldol dec)
-- typical/traditional

- fluphenazine decanoate (prolixin dec)
-- typical/traditional

- risperidone microspheres (risperdal consta) *newer*
-- atypical

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psychosis: definition + s/s

total inability to recognize reality

s/s: delusions, hallucinations, incoherence, catatonia, aggression, violence, inability to process information and come to a conclusion

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psychotic s/s due to imbalance in...

dopamine

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schizophrenia (definition)

chronic psychotic disorder, major category of psychosis
- positive and negative symptoms!

11

neuroleptic malignant syndrome

rare but potentially fatal condition associated with antipsychotic drugs

primary symptoms caused by D2 blockade

12

antipsychotics: adverse effects

- agranulocytosis
- anticholinergic
- arrhythmia
- dermatologic
- gender specific
- hypotension
- metabolic
- neuroleptic malignant syndrome
- sedation, seizures

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side effect: associated anticholinergic effects

anti-SLUD!
dry mouth, nasal congestion, blurred vision, urinary hesitancy/retention, constipation, increased heart rate

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side effect: agranulocytosis (definition)

severely decreased WBC, potentially lethal

possible adverse effect

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side effect: hypotension pathophys

antipsychotics block alpha-1-adrenergic receptors.
tolerance develops in 2-3 months.

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side effect: sedation pathophys

some block histamine, some NE

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female specific side effects

neuroendocrine: galactorrhea, menstrual irregularities
sexual: decreased libido, impaired orgasm

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male specific side effects

neuroendocrine: gynecomastia
sexual: decreased libido, erectile/ejaculatory dysfunction

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side effect: dermatologic

pruritic maculopapular rash
jaundice

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side effect: metabolic

glucose dyscontrol, weight gain

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atropine psychosis: definition

adverse effect; psychotic delirium caused by excess anticholinergic effects

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atropine psychosis: s/s

agitation, confusion, tachycardia, dry flushed skin

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interaction: cns depressants

antipsychotics INCREASE effects

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interaction: anticholinergics

antipsychotics INCREASE effects

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interaction: antihypertensive

antipsychotics INCREASE hypotension

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interaction: levodopa

antipsychotics COUNTERACT effects

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interaction: smoking

smoking INCREASES metabolism of antipsychotics
smoking DECREASES medication-induced parkinsonism

28

interaction: SSRI

SSRI INCREASES antipsychotic levels
SSRY INCREASES EPSE

CAUTION

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interaction: lithium

lithium DECREASES antipsychotic effect
antipsychotic may MASK lithium toxicity

CAUTION

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interaction: tca

INCREASED serum levels of both!!

CAUTION

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typical antipsychotics: aka + how classified

"first generation antipsychotics" (fga)
"traditional"

classified by potency in antagonizing CNS D2 receptors

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typical antipsychotics: moa

- block D2 receptor sites
- in mesolimbic pathway: impact positive symptoms

- partial histamine antagonism
- partial acetylcholine blockage
- antagonism of alpha-1-adrenergic

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typical antipsychotics: structural types (2)

phenothiazine
non-phenothiazine

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typical antipsychotics: routes of administration

oral, IV, IM (depot available)

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typical vs atypical antipsychotics

atypical: effectively treats positive AND negative sx
- EPSE unlikely

typical: not effective in treatment of negative symptoms

36

chlorpromazine (thorazine)

typical antipsychotic
- phenothiazine
- low potency

- target sx: antiemetic, hiccup relief
- more anticholinergic SE
- sedation, hypotension common

37

haloperidol (haldol)

typical antipsychotic
- nonphenothiazine (butyrophenone)
- high potency

- target sx: agitation, aggression
- unlikely anticholinergic SE
- more EPSE

38

extrapyramidal side effects (EPSE) + onset

acute dystonia (days/hours)
parkinsonism (first month)
akathisia (first 2 months)
tardive dyskinesia (months to years)

39

AD
P
A
TD

mnemonic

always discuss
parkinsonism
at
the diagnosis

acute dystonia
parkinsonism
akathisia
tardive dyskinesia

40

acute dystonia

severe muscle spasm:
face, tongue, neck, back
facial grimacing
abnormal, involuntary upward eye movement
laryngeal spasms


pseudo parkinsonism (epse)

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parkinsonism

major side effect of typical; chronic neurological disorder affecting extrapyramidal motor tract (controls posture, balance, locomotion)

PSEUDO in antipsychotics

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akathisia

trouble sitting still: restless, pacing, constant motion

pseudo parkinsonism (epse)

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tardive dyskinesia

protrusion/rolling of tongue
sucking, smacking of lips
chewing
involuntary movement of body, extremities

pseudo parkinsonism (epse)

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akinesia

absence of movement

CAREFUL - NOT akathisia

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epse: treatment

benztropin (cogentin)
trihexyphenidyl (artane)
-- moa (both): anticholinergic - block central cholinergic receptors
-- dopamine deficiency causes excess cholinergic effects

diphenhydramine (benadryl)
-- moa: suppression of central cholinergic activity
-- prolongs action of dopamine by inhibiting reuptake and storage

46

dopamine deficiency causes

central cholinergic excess effects
(dopamine INVERSE RELATIONSHIP acetylcholine)

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atypical antipsychotics: aka + moa

"second generation antipsychotics"
+ positive AND negative symptoms!
---- superior re: neg
+ weak affinity to D2 receptors
+ stronger affinity to D4
+ block serotonin (5HT-2)

48

atypical antipsychotics: routes of administration

oral + quick dissolve, IM

** NO IV **

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negative symptoms and dopamine pathway theory

1. negative symptoms = result of hypodopaminergic process (frontal lobe)

2. selective subtypes of 5HT inhibit dopamine

3. drugs antagonizing 5HT subtypes = increase frontal lobe dopamine

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atypicals + metabolic syndrome

insulin resistance
hypertension
high serum lipids
obesity
coagulation abnormalities
product label warning for: hyperglycemia, diabetes

51

clozapine (clozaril)

atypical antipsychotic

moa: strong blockade of D1, weaker D2
also blocks 5HT, NE, histamine, ACh

common se: sedation, drowsiness, hypersalivation, tachycardia, dizziness, constipation

adverse: agranulocytosis 1-2%
generalized seizures 3%

52

risperidone (risperdol)

atypical antipsychotic

moa: binds to multiple receptors
- D2 (weak)
- 5HT (strong)
- histamine
- alpha-adrenergic
does NOT block cholinergic receptors

side effects (generally infrequent, mild): fatigue, somnolence, dizziness, agitation

> see especially in non-psych settings <

53

olanzepine (zyprexa)

moa:
- positive effects: dopamine, 5HT
- negative effects: NE, histamine

side effects (mild)
somnolence 26%
hypotension
anticholinergic effects
** longterm use: weight gain **

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aripiprazole (abilify)

moa: dopamine antagonist, serotonin agonist
“dopamine system stabilizer”

nota bene: our book considers this the atypical prototype, other experts think it is TGA (a new category of third generation)

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seroquel (quetiapine fumarate)

atypical antipsychotic - effective in treatment of mood disorders with psychotic symptoms

common SEs: sedation, hypotension, dizziness, weight gain

OTHER

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geodon (ziprasidone)

atypical antipsychotic - effective in treatment of mood disorders with psychotic symptoms

historically associated with cardiac side effects

OTHER

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saphris (asenapine)

atypical antipsychotic - effective in treatment of mood disorders with psychotic symptoms

sublingual

OTHER

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fanapt (iloperidone)

atypical antipsychotic - effective in treatment of mood disorders with psychotic symptoms

approved for schizophrenia only

OTHER

59

latuda (lurasidone)

atypical antipsychotic - effective in treatment of mood disorders with psychotic symptoms

primarily have D2, 5HT2 actions

OTHER

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