Psychopharmacology Flashcards
What are the funciton of Acetylcholine?
muscle action
learning
memory
What are the funciton of Dopamine?
movement
learning
attention
emotion
What are the funciton of serotonin?
mood
hunger
sleep
arousal
what are the function of NRE?
alertness
arousal
what is the major inhibitory NT? if undersupply, what happens?
GABA
undersupply:
- seizures
- tremors
- insmonia
what is the major excitatory NT involved in memory? if there’s oversupply, what happens?
glutamate
oversupply:
- overstimulate th brain
- migraines/seizures/avoid MSG, monosodium glutamate in the brain
what are the effects of undersupply for NRE, Serotonin, Dopamine?
Dopamine:
- tremors, DEC mobility in Parkison’s dis
Serotonin:
- depression
NRE:
- depressed mood
what is effect of oversupply of dopamine?
schizophrenia
what includes genetics, rare mutations, lesions, insertion of a diseaes?
Biopsychosocial model
what is the most popular
what happens in the dopamine hypothesis of schizophrenia?
limic dopaminerig c activity & postmortem dopamine receptor density -> psychosis, symptoms of schizophrenia
what are the pos symmptoms of schizophrenia?
- delusions
- hallucinations
what are the neg symptoms of schizophrenia?
anhedonia
affective flattening
avolition
social withdrawal
alogia
what are the 4 dopamine pathways involved in schizophrenia
mesolimbic = causes positive symptoms
Mesocortical = negative, cognitive, & affectiev symptoms
Nigostrial = EPS & TD drug side effects
Tuberohypophyseal = hyperprolactinemia side effects
what are chemical classification of antipsychotics?
Phenothiazine dervicatives
Thioxanthene derivatives
Butyrophenone dervivatives
what is the diff between typical & atypical antipsychotics?
typical = acts on dopaminergic system by blocking D2 receptors
Atypical = minimal extrapyramidal side effects at clinically efefctive antipsychotic doses
what do Atypical antipsychotics treat?
both positive & negative signs & symptoms of schizophrenia
what are the diff 1st gen dopamine reeptor antagonsits (typical)?
Chlorpromazine
Fluphenazine
Flupenthixol
Haloperidol
what type of receptors are found in atypical antipsychotics?
higher degree of occupancy = Serotonergic receptors
lower affinity & occupancy = Dopaminergic receptors
what are the diff 2nd generation or Serotonin dopamine antagonists (atypical)?
Risperidone
Clozapine
Olanzapine
Quetiapine
Paliperidone
Asenapine
Lurasidone
what are the diff 3rd generation partial agonists/antagonist of dopamine & serotonin?
Aripiprazole
Brexiprazole
Cariprazine
What are the AEs of 1st generation antipsychotics?
Acute: Acute dystonia (!), Akathisia, Pseudoparkinonism, Rabbit syndrome, Pisa syndrome
Late: Tardive dyskinesia (!), Hyerprolactinemia
Anticholinergic effects: dry mouth constipation, blurred vision, urinary retention
what is the MOA of 1st generation of antipsychotics?
postsynaptic blockade of brain dopamine D2 receptors
what are the diff high-potency & low-potency first generation antipsychotics? Its Hitaminic & Muscarinic recpetor activity?
high-potency FGA: Fluphenazine, Haloperidol
- LOW receptor activity
Low-potency FGA: Chlorpromazine, Thioridazone
- HIGH receptor activity
what are the diff AEs of High-potency FGAs?
- high risk for extrapyramidal symptoms
- little sedation, weight gain, or anticholinergic activity
what are the diff SEs of low-potency FGAs?
- greater AEs (blurred vision, ocular toxicity, orthostatic HTN, QTc prolongation, urinary retention)
- better tolerated
what are the diff anticholinergic effects of first gen antipsychotics?
Dry mouth or constipation
blurred vision or urinary retention
what are the different SEs of antiosychotics & their receptor types?
D2 = EPS, hyperprolactinemia
M1 = cognitive defects, dry mouth, constipation, INC HR, urinary retenion, & blurred vision
H1 = sedation and weight gain
a1 = hypotension
5-HT2A = anti-EPS
5-HT2C = Satiety blockade
what are the tx for AEs?
EPS
- anticholinergic agents
- antihistamine
- beta-blockers
-anxiolytics
Symptomatic/Supportive therapy = other side effects
what is the MOA of 2nd generation antipsychotics?
stimulates serotonin 5HT2A receptor antagonist that accompanies the D2 antagonim
What is the MOA of Risperidone?
typical antipsychotic at doses >6mg
what are the SEs of Risperidone at high dose ?
Common SE: Hyperprolactinemia, weight gain & sedation
High dose: EPS, hypotension
what are SEs of Olanzapine?
common: weight gain, metabolic syndrome (INC TAGs, CHOL, GLucose)
what are SEs of Quetiapine?
Metabolic syndrome (INC TAGs, Chole, CHO)
Orthostatic hypotension
what are SEs of Clozapine?
- Agranulocytosis
- INC risk if seizures, hypertriglyceridemia, hypercholesterolemia, hyperglycemia, non-ketotic hyperosomolar coma & death
what is the effect of Lurasidone?
less hypotension
what is the MOA of Paliperidone?
antagonist at D2-dopaminergic receptors, a1-adrenergic & a2-adrenergic receptors, H1-histaminergic receptors
what is the MOA of Asenapine?
high-affinity antagonist at 5-HT1A-HT2C + HT5-7 serotonergic receptors
what are the common SE of Asenapine?
sedation
dizziness
somnolence
fatigue
dry mouth
weight gain
what is the MOA of Aripiprazole?
partial agonist at D2 & 5HT2A & partial antagonist at 5HT2A
what are SEs of Aripiprazole?
low EPS
no QT prolongation
low sedation
what are the receptors that makes Brexipiprazole antagonists?
5-HT2A, B, 7
Alpha 1A, 1B, 1D, 2C
what are the receptors that make Brexipiprazole partial agonists?
D2, D3 & 5-HT1A receptors
what precaution should be taken for Brexipiprazole?
monitor for clinical worsening & emergence of suicidal thoughts & behaviors for 20yo and below
what are common SE of Brexipiprazole?
weight gain
akathisia
headache
what is the MOA of Glycine transporter 1 receptor?
Glycine is required co-agonist w/ glutamate at NMDA receptors
what is the most popular hypothesis about depression?
imbalance/deficiency of the monoamine NTs (serotonin, NRE, dopamine)
what are the 2 pharmacologic class of antidepressants?
cyclic antidepressants
monoamine oxidase inhibitors
what are the diff cyclic antidepressants?
selective serotonin reuptake inhibitors = Citalopream, Fluoxetine, Paroxetine, Escitalopram, Fluvoxamine, Sertraline
Selective Serotonin-NRE Reuptake inhibtor = Venlafaxine, Desvenlaxafine, Duloxetine, Levomilnacipran
Serotonin-1A Agonist/Serotonin Reuptake Inhibitor = Vilazodone
Noradrenergic/Specific Serotonergic agent = Mirtazapine
Nonselective Cyclic Agents (Mixed reuptake inhibitor/receptor blockers) = Amitriptyline, Desipramine, Imipramine, Maprotiline, Nortriptyline
what are the diff Monoamine oxidase inhibitors
Irreversible MAO Inhibtors = Phenelzine
Irreversible MAO-B inhibitor = Selegiline
what are the things u should consider before prescribing a drug to a px on their first episode?
past history of response to a certain antidepressant
side effect profile
coexisting medical conditions
why is it there is an improvement of symptoms after 3-6 wks of therapy?
increase in brain0derived neutrotophic factors levels -> INC synaptic proteins & receptors to which Serotonin can bind to => INC # of neurons & dendritic sprouts
what are the 1st line of antidepressants due to their efficacy, tolerabiity & general safety profile?
SSRIs
what is the MOA of SSRI?
prevents reuptake & subseqeunt degradation of serotonin
what are important PD of SSRI?
Fluoxetine - longest 1/2 life
Sertraline = less sedating
Paroxetine = greatest sedating properties
what are common SEs of SSRIs?
headache, GI symptoms
Decreased libido
Discontinuation syndrome = if px suddenly stops taking of drug (dizziness, lethargy, nausea, vomiting, diarrhea, headache)
what is the C/I of px taking SSRi?
intake of MAOi due to Serotonin syndrome
What are the triad of symptoms that present in Serotonin syndrome
mental status changes
autonomic hyperactivity
neuromuscular abnormalities
wha tis the MOA of SNRI (serotonin NRE reuptake inhibitor)
inhibitor of 5HT, NE transporters
What are common AEs of SNRI?
nausea, headache
agitation
sedation
what is the indication of Noradrenergic specific serotnergic antidepressant?
MDD w/ insomnia
what is the indicaition of SNRI?
MDD, GAD
pain due to DM nephropahty, fibromyalgia
what is the D/I of Serotonin simulator/modulator?
serotonin syndrome -> dont take with other SSRIs?
what are indications for tricyclic antidpressants?
unresponseive to SSRI or SNRI
insomnia
neuropathic pain
nocturnal enuresis
MDD
what are the 2 classes of Drugs for ADHD?
psychostimulants
non-sychostimulants
what are the psychostimulants & non- for ADHD?
Methylphenidate
Dextroapmhetamine
non-psychostimulants: Atomoxetine
what are the MOA of each psychostimulants for ADHD?
Methylphenidate = INC synaptic dopamine & NRE
Dextroamphetamine = competitive i & pseudosubstrate for presynaptic transporters for DA, NE, 5-HT
what is the MOA of atomoxetine?
no stimulant or euphoriant activity
INC NRE & DA in frontal cortex
in what cases do u use psychostimualnts
> 6yo
ADHD, narcolepsy
what are indications of sex drive antidepressants?
reduction of sexual arousal, libido
disruptive sexual behavior
sex offenders
what re the 3 classes of sex-drive depressants and ex?
Anti-androgen/Progestogen -> Cyproterone
Progestogen -> Medroxyprogesterone
Anti-androgen, 5a reductase i -> Finasteride
what are the diff mood stabilizers?
Lithium
Anticonvulsants: Valproic acid, Carbamazepine, Lamotrigine
Antipsychotics
Antipsychotic/Antidepressant combination
what is the gold std/1st line for mania?
lithiu,
what is the MOA of lithium?
inhibits inisoitol monophosphate –> inhibits glycogen synthase kinase-3 enzyme that appears to limit neurotrophic & neuroprotective processes
what are the different enzymes affected by lithium? (!)
- inositol monophosphate
- inositol polyphosphate 1-phosphate
- glycogen synthase kinase-3
what are AEs of lithium?
cardiac arrhythmia
bradycardia
sinoatrial dysfunction
abnormal T-waves on ECG
ST segment depression
what anticonvulsant is effective as lithium in mania prophylaxis but not in depression prophylaxis?
valproic acid
what are AEs of valproic acid?
hepatic toxicity, pancreatitis
what is the indication of Carbamazepine & Lamotrigine?
Lamotrigine = bipolar depression
Carbamazepine = acute mania & mania prophylaxis
what are the 3 types of insomnia?
transient insomnia = <4 wks duration
short-term insomnia = 4wk - 6 mons
chronic insomnia - >6 mons
what are the FDA approved drugs for insomnia?
Nonbenzodiazepines
Ramelteon: Melatonin agonist
Benzodiazepines
what is the indication of Nonbenzodiazepines?
short term tx duration of insomnia
what is the insomnia indicator of Ramelteon?
initial insomnia (sleep onset)
unlikely ti improve sleep maintenance
what re indication sof Benzodiazepines (anxiolytics)?
GAD
panic disorder
insomnia
seizure disorder
what is the MOA of Benzodiazepines?
positive allosteric modulators fo GAVA at limbic system, brainsem reticular formation, and cortex
what are AEs of BEnzodiazepines?
mood disturbance/rebound anxiety
Dependence (within 3-4 wks)
what are D/I of Benzodiazepines?
Cimetidine = INC benzodiazepin levels, CYP inhibition
Ethanol = INC sedation/respiratory depression, CNS depression, synergism
Opioids = INC sedation/respiratory depression, CNS additive
