Pharmacology - Test 2 - Antipsychotic Flashcards
Antipsychotic
Drugs
Psychosis
mental disorder of organic and/or emotional origin; derangement of personality/loss of contact with reality
Schizophrenia
psychotic disorder characterized by disturbed thought processes, delusions, or hallucinations, in the absence of a full affective syndrome or organic mental disorder.
Affective Disorder
a disturbance of mood accompanied by related symptoms, and generally involves depression and/or elation.
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.
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
Schizophrenia: 3 symptoms
Positive, Negative, Cognitive
Target receptors of antipsychotics
Dopamine, D2 family
Two dopamine subtype families
D1, D2
D1 subtype
increase cAMP, excitatory
D2 subtype
decrease cAMP, inhibitory
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
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)
subclass causing extrapyramidal motor side effects
typical
subclass NOT causing extrapyramidal motor side effects
atypical
atypical drugs
do not increase prolactin; some can reduce negative and positive symptoms; bind to D2 more briefly
aripiprazol (Abilify) mechanism
D2 PARTIAL AGONIST;
Abilify mechanism
activation of the D2 receptor in states of low dopaminergic tone and inhibition at the receptor in states of high dopaminergic tone.
Abilify tx of:
schizophrenia, bipolar
tricyclic antidepressants mechanism
inhibit MAO transporters: inhibit NE, 5HT uptake; increase 5HT transmission
TCA side effects
-sedation - anticholinergic - orthostatic hypotension - arrhythmias - tachycardia - tremor - transition to hypomanic or manic excitement
therapeutic latency of 2-6 weeks
TCA Prototype
imipramine
Selective Serotonin Uptake Inhibitors (SSRI’s)
mechanism
block SERT, increasing synaptic 5HT levels
SSRI prototype
fluoxetine (prozac)
SSRI side effects
less antimuscarinic than TCA; less anticholinergic (tachycardia)
MAOIs: 2 classes
hydrazine, non-hydrazine
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
Hydrazine prototype
Phenelzine
non-hydrazine prototype
Tranylcypromine
MAOI side effects
orthostatic hypotension; excessive CNS stimulation: tremors and insomnia
MAOI drug interactions
L-DOPA: agitation and hypertension
- tyramine (cheese/ wine/ beer): hypertensive crisis
Mood stabilizers/ Antimanics
haloperidol and aripiprazol, lithium
-treatment of acute mania
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
Lithium mechanism
inhibits GSK-3B (overexpression causes mania in mice), regulates circadian rhythm
Lithium side effects
low margin of therapeutic index tremor, most common, sensitive to propranolol
- mental confusion
- ataxia
- polydipsia and polyurea
- nephrotoxicity
Antimanic drugs
Carbamazepine / valproate (mechanism unknown)
