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Anti-Psychotics
UMKC SOM Pharmacology
19
Medical
Graduate
11/25/2013

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Cards

Term
Typical First gen High Potency
Definition
Haloperidol, Thiothixene, Perphenazine, Loxapine, Fluphenazine
Term
Typical First gen Low Potency
Definition
Thioridazine, Chlorpromazine
Term
Typical First Gen
MOA
PK
AE
DI
Definition
Block D2 Rs in the mesolimbic pathway
Muscarinic antag leads to EPS symptoms
H1 antag leads to sedation
IV not recommended
CNS: sedation (low), seizures (low)
EPS (high)
CV: QT prolongation
Hyperprolactinemia (typical)
Sexual dysfunction, Weight gain (low)
Neuroleptic Malginant syndrome
Blindness
Agranulocytosis
Term
Atypical Second Gen
MOA
PK
AE
DI
Definition
Clozapine, Risperidone, Olanzapine, Quetapine, Ziprasadone
Both serotonin and DA antag
Block release in the nigrostriatal pathway, mesocortical
*no EPS symptoms
DM higher, Orthostatic Hypotension
Term
MAOIs
MOA
PK
AE
DI
Definition
Non sel: Phenylzine, Isocarboxazid, Trancyclopromine
B only: Selegiline
Increase in effective NE and 5HT
Late onset
Excess adrenergic stim, Orthostatic hypotension and HTN
Sexual dysfunction, weight gain, toxicity
Tyramine containing foods, displaces NE
Levodopa, meperidine, other Ads
Term
Mesocortical tract
Definition
Causes or worsens neg symptoms of schizo
Term
Nigrostriatal
Definition
EPS symptoms
Term
Tuberoinfundibular
Definition
Prolactin increases
Term
TCAs
MOA
PK
AE
DI
Definition
Imipramine, Amitriptyline, Nortriptyline, Desiprimine
Block reuptake of 5HT3, NE and some DA
Muscarinic block, H1 Block, a1 block, Na ch block
Long half life, some monitoring needed
Sedation, orthostatic hypotension
*narrow TI > tachycardia, mydriasis, hypotension,
Term
SSRIs
MOA
PK
AE
DI
Definition
Fluoxetine, Sertraline, Paroxetine, Fluvoxamine, Citalopram
Smoking increases the metabolism of drugs
Binds the non active transporter site
HA, sleep disturbances, tremors, dizziness, nausea
Sexual dysfunction
Serotonin syndrome of HTN crisis (when with tramadol)
Term
NDRI
MOA
PK
AE
DI
Definition
Bupropion
Selective NE and DA reuptake inhibitor
No 5HT3 action, so no sexual dysfunction
Agitation, insomnia, anorexia, irritability, HA, anxiety
Seizures
Term
SNRI
MOA
PK
AE
DI
Definition
Venlafaxine, Duloxetine
5HT3, NE reuptake inhibitor
HTN, Insomnia, agitation, anxiety
Term
NaSSA
MOA
PK
AE
DI
Definition
Mirtazapine
Noradrenergic and 5HT3 blocker
a2 antagonist
Sedation and weight gain
Term
SARI
MOA
PK
AE
DI
Definition
Nefazodone, Trazodone
Serotonin antag reuptake inhibitor
Very sedating, priapism, orhtostatic hypotension, hepatotox
Term
Lithium
MOA
PK
AE
DI
Definition
Sub for Na in APs, by blocking Na exchange across membranes
enhance 5HT3 actions
Blocks adenyl cyclase
PO, therapeutic effect in 3-10 days
Must monitor serum levels
Tremors, slow AV conduction, arrythmias
Nausea, loose stools, tubular necrosis, diabetes insipidus
Wt gain, leukocyosis, teratogenic
Term
Li side effects
Definition
Early, common: fine hand tremor, inc thirst, urination
Persistent, not DR: fine hand tremor, leukocytosis, hypothyroidism
Late SA, DR: Coarse hand tremor, reappearance of GI side effects,
Severe tox: seizures, coma, CV collapse, death
Term
Benzos
MOA
PK
AE
DI
Definition
Diazepam
Anxiolytic effects mediated through interaction with GABAergic neurons
Flumazenil reverses a full agonist BZ acting at the BZ receptor of the GABA complex
IV for SE, hepatically met,
Lorazepam, oxazepam and temazepam do not have active mets
Excess sedation, resp depression, hypotension and bradycardia
Term
Non Benzos
MOA
PK
AE
DI
Definition
Zolpidem, Zaleplon, Eszopidone
GABA A receptors
Rapid onset and short DOA of sedative effects, no amnesia or muslce relax
Schedule 4 drug
Dec latency to sleep
Term
Buspirone
MOA
PK
AE
DI
Definition
Pre and post synaptic serotonin Rs as a partial agonist
For generalized anxiety disorder
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