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Antipsychotics
Module 3.6
26
Pharmacology
Graduate
11/19/2011

Additional Pharmacology Flashcards

 


 

Cards

Term
Positive symptoms
Definition

Things that are there that should not be there. Hyperactivity of mesolimbic dopa pathway

 

 Delusions, hallucinations, disorganized speech, catatonic behavior

Term
Negative symptoms
Definition

Symptoms that should be there and aren't

hypoactivity of mesocorticaldopa path

 

flat affect, lack of speech (alogia), avolition

Term
Nigrostriatal pathway
Definition
insufficient dopa causes EPS, motor symptoms
Term
Tuberinfundibular pathway
Definition
insufficient dopamine increases prolactin level (sexual dys, gynecomastia, milk secretions, menstrual cycle dist.)
Term
Mesolimbic Pathway
Definition
excess dopamine contributes to positive sx
Term
mesocortical pathway
Definition
insuff dopa contributes to neg sx
Term
insufficiency in frontal cortex also results in ADHD. Stimulants used to prevent reutake and increase release
Definition
Norepinephrine
Term

 

 

Antagonize d2 receptors in all CNS Dopaminergic Pathways

Definition

Typical antipsychotics

 

aka: 1st gen

Term

 D2 receptor antagonism

causing...

 

EPS

Tardive dyskinesia-

Neuro malig syndrome

Increased prolactin

Definition

Typical Antipsychotic On target A/E 

 

Higher potency cause this more often

Term

antagonism at muscarinic and alpha receptor

causing...

 

Anticholinergic effects

Hypotension

Failure to ejaculate

Sedation

 

Definition

Typical antipsychotic Off target A/E

 

Lower potency drugs cause this more

Term
Atypical antipsychotics
Definition

Effective in treating negative sx (except risperidone)

 

Antagonism of 5HT2, D2 , and poss D4 antagonism

 

Dissociate quickly from D2 dont help positive sx but cause LESS EPS

 

A/E: agent specific

Term
Typical antipsych examples
Definition
[image]
Term
Percentages of D2 saturation that will cause effects
Definition

40% akathisia

60% improves positive sx

80% dystonia

Term
Acute EPS
Definition

Dystonia (muscle stiffness)-tx with antichol 

 

Akathisia (restlessness)-tx with b-blocker: propanolol is lipophilic crosses BBB

 

pseudoparkinsonism (rigidity bradykinesia tremor)-anticholinergic, amantadine 

 

 

Term
Chronic EPS
Definition

Pseudoparkinsonism, tardive dyskinesia

 

 

Term
Neuroleptic malignant syndrome (NMS)
Definition

analogous to serotonin syndrome

fever

muscle rigidity

increased CPK

Delirium

 

Remove med, treat sx

Term

Antagonize effects at 5HT2a and Dopamine 

 

cause less EPS prolactin effects, helps negative sx equally

 

QT prolongations possible

 

Definition
[image]
Term
Clozapine
Definition

last line due to...

1-2% in 1st 6 months develop agranulocytosis

monitoring cbc important

 

A/E: orthostatic hypotension, weight gain, hyperglycemia, sedation, constipation

 

Metabolized: CYP2d6, 3a4, 1a2 (smoking increases metabolism)

Term
Paliperidone (invega)
Definition

Primary active metabolite of risperidone

 

Dosing: osmotic delivery do not crush/ chew

 

Metabolism: RENAL 60%

*can be used with low hepatic function

 

no IDENTIFIED interactions

Term
Iloperidone (fanapt)
Definition

MAE: same

 

A/E: orthostatic hypotension, qt prolongation

Metabolized: CYP2D6

 

Term
CYPD26
Definition
enzyme that metabolizes many CNS drugs 
Term
Abilify
Definition

partial agonist at D2 receptors (elicits reduced response compared to natural NT)

 

Partial agonist at %HT1a

Antagonist at %HT2a, H1, alpha1

 

Partial agonism leads to unpredictable levels of receptor activity-NOT COMBINED with OTHER DRUGS

 

Term
Zyprexa
Definition

Metabolized CYP1A2 (smoking increases metabolization)

 

coated: if cut use immediately due to rapid oxidation

Term
Seroquel
Definition

Wide dosing range

 

Drug interactions less clinically significant

 

Can be used at low doses to sedate

 

high doses for antipsychotic use

Term
Formulations of Antipsychotic
Definition

All PO

Some Liquid

Some ODT: NOT absorbed across mucosa, same as PO efficacy used for noncompliant PO

 

IM: agitated pts

 

Depot: long acting 2-4 weeks

 

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