8013 week 1 pharm review Flashcards
3 monoamine neurotransmitters
Dopamine
Norepinephrine
Serotonin
Dopamine NT receptors
D1-5
Dopamine is responsible for
movement control, emotional response, pleasure and pain
Dopamine
Too little:
Too much:
Parkinsons
Psychosis and mood disorders
Norepinephrine receptors
Adrenergic NT binds to alpha & beta adrenergic receptors
NE increase in adrenergic activity causes…
causes increased HR, BP, alertness, anxiety and hyperactivity
NE reuptake inhibitors do what…
NE Agonists do what…
increase NE and improve symptoms of depression
decrease NE and help with symptoms of anxiety
Serotonin receptors…
5HT 1-7
Serotonin regulates…
sleep
mood
pain
peristalsis
Appetite
vasoconstriction
5HT 1A is associated with
depression
5HT 2A is associated with
psychosis
Gaba vs Glutamate (how they work)
inhibitory (hyperpolarizing a receptor preventing it from firing and results in anti-anxiety, anti-epileptic, and sedative effect)
excitatory (master switch that works on any receptor and contributes to learning and memory. Excess can lead to neurodegeneration like Parkinsons/Alzheimers/Schizophrenia)
All antipsychotics block the ___ system in the brain
DA
Low potency FGAs require…
higher dosing and vice versa
potency of rx determines dose needed to elicit response
high potency FGA cause AE due to..
not hitting ACH
Low potency FGA example
Chlorpromazine/Thorazine
2 moderate potency FGAs
Loxapine/Loxitane
Perphenazine/Trilafon
2 high potency FGAs
Haloperidol/Haldol
Fluphenazine/Prolixin
How do FGAs work
Antagonism of D2 receptors with an optimal effect at a 60-70% D2 receptor blockade
low potency FGAs have a high potency for which receptors
cholinergic and andrenergic
high potency FGAs block ___ but not ___
DA
ACH
low potency FGAs AE
Anticholinergic: Dry mouth, constipation, blurred vision, orthostatic hypotension
high potency FGAs AE
Extrapyramidal : Akathesia, akinesia, dyskinesia, dystonia, tardive dyskinesia
FGAs target all DA which may result in ___
increased neg AE, EPS, hyperprolactinemia
NMS risk from FGA is high with ____ but increased with ___
high dose FGA
dehydration, exercise, exhaustion
10 SGAs
Clozapine/Clozaril
Aripiprazole/abilify
Asenapine/saphris
Cariprazine/vraylar
Iloperidone/fanapt
Lurasidone/Latuda
Olanzapine/Zyprexa
Quetiapine/Seroquel
Risperidone/Risperdal
Ziprasidone/geodon
How do SGAs work?
Both DA and 5ht antagonist counterbalancing DA depletion in areas of the brain that cause EPS, hyperprolactinemia, and negative sx reducing occurrence
shorter duration of DA block than FGAs
SGA AEs
cardiometabolic syndrome: Wt gain, HTN, inc lipids, inc glucose
Also sedation, EPSE, anticholinergic possible
SGAs with least likely cardiometabolic syndrome AE
Abilify and Geodon
How do SSRIs work?
inhibit uptake of 5ht, some DA, NE
Most common AE for SSRI
GI
Neuropsych
Sex dysfunction
Also consider: SI, SS, W/D, Apathy
4 SNRIs
Desvenlafaxine/Pristiq
Duloxetine/Cymbalta
levomilnacipran./Fetzima
Venlafaxine/Effexor xr
How do SNRIs work?
inhibit 5ht and NE
Most common SNRI AE
Drowsy
Dry mouth
Dizzy
Constipation
Nervous
Sweat
Anorexia
NDRI example
Bupropion
How does Bupropion (NDRI) work
inhibit NE and DA (not 5ht)
impacts adrenergic system
Bupropion CI and most common AE
CI: Sz hx
AE: Insomnia and agitation (no dec libido)
If anxiety is worse than depression choose
SSRI over NDRI
NASSA example
norandrenergic and specific serotonergic antidepressants
Mirtazapine/Remeron
How does Mirtazapine (NASSA) work?
Antagonnist of adrenergic and specific serotonin receptors
antagonist of histamine
tx Major depression
Mirtazapine (NASSA) AE
Wt gain
somnolence (dec with higher dosing)
ortho hypo
dizzy
less libido issues than SSRI
Poss to cause agranulosis
Serotonin modulator and stimulator example
Vilazodone/viibryd
How does Viibryd work
inhibit and partial agonist of 5ht
does not bind to NE or DA
take with food
metab CYP3A4
comes with starter kit but expensive
Viibryd AE
GI
HA
SRI example
Serotonin reuptake inhibitor
Vortioxetine/brintellix
How does Brintellix work?
inhibit 5ht
very long half life and high protein bound
Brintellix caution
Do not use with Bupropion due to inc blood level
SSRI/Antipsychotic combo rx
Symbyax/fluoxetine-olanzapine
How does Symbyax/fluoxetine-olanzapine work?
Agonist of 5ht/DA/NE
Used to tx BP1 acute depression and tx resistant depression
Symbyax/fluoxetine-olanzapine AE
Dry mouth
somnolence
inc apetitie
peripheral edema
drowsiness
blurred vision
TCA examples
Amitriptyline/Elavil
Clomipramine/Anafranil
Imipramine/Tofranil
Desipramine/norpramin
Nortriptyline/Pamelor
Protriptyline/vivactil
How does a TCA work
Block 5ht and NE
Used to tx severe depression
TCA AE and caution
drowsy, wt gain, hypotension, dizzy
lethal in overdose with poss arrhythmia and Sz
1st line tx for anxiety
SSRI/SNRI
THEN
Anxyolitics
3 anxyolitics
BZO
Buspirone
Clonidine
1 short BZD and length and what better for
Triazolam/Halcion=short
<12 hrs
sleep/insomnia
3 long BZD and length
Chlordiazepoxide/Librium=long
Clonazepam/klonopin=long
Diazepam/valium=long
> 24 hours
4 intermediate BZD and length
Alprazolam/Xanax=intermediate
Lorazepam/Ativan=intermediate
Oxazepam/serax=intermediate
Temazepam/Restoril=intermediate
12-24 hours
How does a BZD work?
Increase the inhibitory effect of GABA as an agonist
How does Buspirone work?
partial 5ht agonist
Gold standard and only true mood stabilizer
Lithium
Lithium manages…
Depressive and Manic phases of BP for acute and prophylaxis
Other rx considered mood stabilizers
Anticonvulsants: carbamazepine, Lamictal and valproic acid and some atypical antipsychotics
Sx of manic phase of BP
grandiosity, elevated mood, hyperactivity, irritability, pressured speech, reduced need for sleep, flight of ideas, impulsivity and agitation
Sx of depressive phase of BP
sadness, anhedonia, hypersomnia, weight gain, fatigue, indecisiveness, and suicidality
Lithium reduces the risk of suicidality in BP to
80%
Lithium onset
slow (6-10 days)
may need to be paired with antipsychotic for faster effect
Lithium therapeutic index
0.6-1.2
> 1.5 is toxic
How often check serum lithium
q2wks during mania
q2mo for maintenance
Lithium AE early
Diarrhea
commit
drowsy
muscular weakness
lack of coordination
Lithium AE intermediate
Ataxia
Tinnitus
Blur vision
polyuria
Lithium AE severe
Multiple organ involvement
Lithium CI
Renal and cardiac dz
severe dehydration
sodium depletion
Anticonvulsant rx
Valproic acid/Depakene
Divalproex/Depakote
Carbamazepine/Tegretol
Lamotrigine/Lamictal
Oxcarbazepine/Trileptal
Gabapentin/Neurontin
Topiramate/topamax
Anticonvulsant black box warning
hepatotoxicity and pancreatitis
Anticonvulsant AEs
Inc SI, depression
Lamictal associated with SJS
Lithium/Carbamazepine/Valproate may cause hypothyroid
6 atypical antipsychotics FDA approved for BP
Aripiprazole/abilify
Clozapine/Clozaril
Olanzapine/Zyprexa
Quetiapine/Seroquel
Risperidone/Risperdal
Ziprasidone/Geodon
but none have significant evidence for prophylaxis of BP and dont prevent new mania or depression episodes