Pharmacology - Test 2 - Antipsychotic Flashcards Preview

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Flashcards in Pharmacology - Test 2 - Antipsychotic Deck (36):
1

Antipsychotic

Drugs

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Psychosis

mental disorder of organic and/or emotional origin; derangement of personality/loss of contact with reality

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Schizophrenia

psychotic disorder characterized by disturbed thought processes, delusions, or hallucinations, in the absence of a full affective syndrome or organic mental disorder.

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Affective Disorder

a disturbance of mood accompanied by related symptoms, and generally involves depression and/or elation.

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Manic disorder

predominant mood is elevated, expansive or irritable, and is associated with other symptoms, such as hyperactivity, flight of ideas, inflated self-esteem, accelerated speech, and distractibility.

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Major Depressive disorder

emotional state of dejection, usually associated with loss of interest in pleasure, sleep disturbances, and feelings of worthlessness or guilt, which is not a reaction to a particular environmental event

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Schizophrenia: 3 symptoms

Positive, Negative, Cognitive

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Target receptors of antipsychotics

Dopamine, D2 family

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Two dopamine subtype families

D1, D2

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D1 subtype

increase cAMP, excitatory

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D2 subtype

decrease cAMP, inhibitory

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Side effects of antipsychotics, due to binding of other receptors

alpha 1: orthostatic HoTN; H1 histamine: sedation; mucarinic: sedation, dry mouth; 5HT2 serotonin: aid in antipsychotic effects

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BLockade of D2 causes extrapyramidal motor effects

-Parkinsonian symptoms (MOST COMMON), -Akathesia (discomfort in legs that results in walking about),
-Tardive dyskinesia (stereotyped involuntary movements)

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subclass causing extrapyramidal motor side effects

typical

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subclass NOT causing extrapyramidal motor side effects

atypical

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atypical drugs

do not increase prolactin; some can reduce negative and positive symptoms; bind to D2 more briefly

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aripiprazol (Abilify) mechanism

D2 PARTIAL AGONIST;

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Abilify mechanism

activation of the D2 receptor in states of low dopaminergic tone and inhibition at the receptor in states of high dopaminergic tone.

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Abilify tx of:

schizophrenia, bipolar

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tricyclic antidepressants mechanism

inhibit MAO transporters: inhibit NE, 5HT uptake; increase 5HT transmission

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TCA side effects

-sedation
 -        anticholinergic
 -        orthostatic hypotension
 -        arrhythmias
 -        tachycardia
 -        tremor
 -        transition to hypomanic or manic excitement

therapeutic latency of 2-6 weeks

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TCA Prototype

imipramine

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Selective Serotonin Uptake Inhibitors (SSRI’s)
mechanism

block SERT, increasing synaptic 5HT levels

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SSRI prototype

fluoxetine (prozac)

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SSRI side effects

less antimuscarinic than TCA; less anticholinergic (tachycardia)

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MAOIs: 2 classes

hydrazine, non-hydrazine

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MAOI mechanism

 irreversible inhibition of MAO, leading to increased levels of NE, 5HT, and DA; maximal inhibition of MAO seen within a few a days, but the antidepressant effect takes longer to develop

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Hydrazine prototype

Phenelzine

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non-hydrazine prototype

Tranylcypromine

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MAOI side effects

orthostatic hypotension; excessive CNS stimulation: tremors and insomnia

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MAOI drug interactions

L-DOPA: agitation and hypertension
-  tyramine (cheese/ wine/ beer): hypertensive crisis

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Mood stabilizers/ Antimanics

haloperidol and aripiprazol, lithium
- treatment of acute mania

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Lithium

calming effect in acute mania; effect slow to develop; recommended use with haloperidol for treatment of severe manic reaction
-prophylaxis in bipolar affective disorder

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Lithium mechanism

inhibits GSK-3B (overexpression causes mania in mice), regulates circadian rhythm

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Lithium side effects

low margin of therapeutic index tremor, most common, sensitive to propranolol
- mental confusion
- ataxia
- polydipsia and polyurea
- nephrotoxicity

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Antimanic drugs

Carbamazepine / valproate (mechanism unknown)