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213 Cards in this Set
- Front
- Back
carbamazepine- brand name
|
tegretol
|
|
carbamazepine- seizure types
|
partial
tonic-clonic |
|
carbamazepine- binding
|
high binding, low albumin can alter free concentration
|
|
carbamazepine- forms
|
tablet, SR, no IV due to low solubility
|
|
carbamazepine- metabolism
|
-liver converts cbz to cbz by 3A4 epoxide to cbz dihydrodiol
-cbz epoxide is active and toxic -autoinduction of 3A4 |
|
carbamazepine- toxicity
|
-concentration related
-headache, anticholinergics, SIADH -leukopenia, hepatitis, rash |
|
carbamazepine- dosing/therapeutic range
|
-start low and titrate up due to autoinduction
-use tid and qid -2-12 ug/ml |
|
carbamazepine- drug interactions
|
-general inducer
|
|
Phenytoin- Brand name
|
Dilantin
|
|
Phenytoin- seizure types
|
partial
tonic-clonic |
|
Phenytoin- binding
|
extensively bound
|
|
Phenytoin- metabolism
|
-t1/2= 24 hours
-saturable metabolism -cyp 2c9, 2c19 -pregnants- increased metabolism and changes in binding -old people- low vmax, low protein -young people- high vmax |
|
Phenytoin- doses
|
-tablets and suspensions are free acid
-capsules and inj are 92% phenytoin -IM- painful, avoid, use fosphenytoin IV- with NS -Fosphenytoin is prodrug, give faster, less phlebitis |
|
Phenytoin- toxicity
|
-CNS effects
-rash -gingival hyperplasia -hirsutism, coarse facial features -osteoporosis due to Vit D metabolsim |
|
Phenytoin- interactions
|
-cyp and ugt inducer
-ca antacids and sulcrafate -enteral feedings decrease absoportion |
|
phenytoin- therapuetic levels
|
10-20 ug/ml total, 1-2 ug/ml free
|
|
valproic acid- brand name
|
dopakote, depakene, depacon
|
|
valproic acid- binding
|
saturable binding
|
|
valproic acid- metabolism
|
-mostly by liver, ugt, b-oxidation
-t1/2- 14 hours in adults, 11 hours in children -toxic metabolite due to cyp oxidation |
|
valproic acid- toxicity
|
-weight gain
-tremors -hyperammonemia -lowered clotting -hair loss |
|
valproic acid- dosing
|
-titrate slowly to avoid slowly
-ER- give once daily but bioavailability is 15% less |
|
valproic acid- forms
|
-depakene capsules, syrup
-depakote capsules- divalproex sodium -depacon- no IM |
|
valproic acid- therapeutic range
|
50-100 ug/ml
|
|
valproic acid- interactions
|
-inhibitor of cyp and udp
-metabolism can be induced |
|
phenobarbital- binding
|
50%
|
|
phenobarbital- metabolism
|
-about half by cyp, some renal excretion
-really long half life |
|
phenobarbital- adverse effects
|
-sedation
-decreased cognitive function -excites kids -megaloblastic anemia (folate deficiency) -osteomalacia -rash |
|
phenobarbital- forms
|
tablets
syrup injection |
|
phenobarbital- drug interactions
|
induces cyp and ugd
|
|
phenobarbital- therapeutic range
|
15-40 ug/ml
|
|
gabapentin- brand name
|
neutontin
|
|
gabapentin- absorption
|
active absorption, saturable at 500 mg
|
|
gabapentin- binding
|
none
|
|
gabapentin- elimination
|
all renal
|
|
gabapentin- drug interactions
|
none
|
|
gabapentin- adverse effects
|
CNS effects
weight gain edema tolerate out |
|
pregabalin- brand name
|
lyrica
|
|
pregabalin- absorption
|
not saturable
|
|
pregabalin- binding
|
none
|
|
pregabalin- elimination
|
renal
|
|
pregabalin- interactions
|
none
|
|
pregabalin- adverse effects
|
dizziness
blurry vision somnolence weight gain euphoria |
|
lamotrigine- brand name
|
lamictal
|
|
lamotrigine- binding
|
55%
|
|
lamotrigine- elimination
|
mostly hepatic glucuronidation
t1/2- 15 hours with inducer, 60 hours with inhibitor, 24 hours alone |
|
lamotrigine- drug interaction
|
-metabolism is induced by inducers (cbz, pht, pb, oxc) and bcp
-metabolism is inhibited by vpa -does not cause interactions |
|
lamotrigine- adverse effects
|
-modest sedation
-minimal cognitive impairment -headache -insomnia -rash: due to rapid titration, concomitant VPA, kids, rash with other AEDs |
|
lamotrigine- therapeutic monitoring
|
4-20 ug/ml
|
|
Topiramate- brand name
|
topamax
|
|
Topiramate- mechanism
|
-blocks voltage-gated sodium and calcium channels
-enhance gaba activity -blockade of excitatory glutamate |
|
Topiramate- elimination
|
renal
|
|
Topiramate- binding
|
low
|
|
Topiramate- interactions
|
inhibits 2c19
induces 3a4 |
|
Topiramate- adverse effects
|
-with high doses
-CNS -kidney stones -weight loss |
|
zonisamide- brand name
|
zonegran
|
|
zonisamide- binding
|
40%
|
|
zonisamide- t1/2
|
long
|
|
zonisamide- drug interactions
|
-does not inhibit or induce
|
|
zonisamide- metabolism
|
by cyp 3a4
|
|
zonisamide- adverse effects
|
-CNS
-depression -kidney stones -rash -increse in serum creatinine |
|
levatiracetem- brand name
|
keppra
|
|
levatiracetem- binding
|
low
|
|
levatiracetem- metabolism
|
mostly renal and metabolized outside of liver
|
|
levatiracetem- therapeutic monitoring
|
10-50 ug/ml
|
|
levatiracetem- adverse effects
|
-sedation
-behavioral effects -weight neutral -titrate slowly |
|
oxcarbazepine- brand name
|
trileptal
|
|
oxcarbazepine- interactions
|
-induces 3a4 and ugt
-inhibits 2c19 -increases pht levels -pb, cbz, pht decreases levels |
|
oxcarbazepine- adverse effects
|
-CNS effects
-abdominal pain -tremors -hyponatremia |
|
mental status exam
|
joimat
judgement, orientation, intellectual function, memory/mood, apprearance/affect, thought |
|
types of schizophrenia
|
-paranoid
-disorganized -catatonic -undifferentiated -residual -schizophreniform -schizoaffective disorder -psychotic disorder due to general medical condition or sunstance induced |
|
criteria for schizophrenia
|
-2 or more of the following: dilusions, hallucinations, disorganized speech, disorganized or catonic behavior, negative symptoms
-social or occupational dysfunction -continuous signs of the disorder for more than 6 months -exclude mood disorders -not due to medical disorder or substance -PPD must have delusions or hallucinations for a month |
|
epidemiology of schizophrenia- age
|
15-25
|
|
epidemiology of schizophrenia- males to female
|
equal
|
|
clinical couse of schizophrenia- onset
|
abrupt or insidious, most have prodromal phase with negative symptoms
|
|
clinical couse of schizophrenia- intitial diagnosis
|
with positive symptoms
|
|
clinical couse of schizophrenia- disease course
|
fluctuates but ends up deteriorating
|
|
clinical couse of schizophrenia- remission
|
unlikely
|
|
schizophrenia- positive symptoms
|
hallucinations
delusions disorganzed speech bizarre behavior psychomotor aggitation |
|
schizophrenia- negative symptoms
|
alogia
flattened affect avolition anhedonia poverty of speech psychomotor retardation |
|
schizophrenia- other symptoms
|
cognitive symptoms
mood symptoms social and occupational symptoms |
|
etiology of schizophrenia-
|
general 1%
sibling 10% offspring 13% dizygotic twin 10-15% monozygotic twin 50% |
|
pathophysiology of schizophrenia
|
-diseases or drugs that cause DA enhancement cause positive symptoms
--amphetamine and cocaine -DA high in limbic -DA low in prefrontal -low glutamate -NMDA receptor dysfunction |
|
goals of schizophrenia
|
-acute stabalization: reduce threat, improve function, interventions
-stabalization: minimize relapse, compliance, optimize dose -maintenance: improve QOL, maintain function, monitor for relapse, minimize ADR, maintain compliance and dose |
|
conventional antipsychotics
-mesolimbic -mesocortical -nigrotriatal -tuberoinfundibular |
-stops positive symptoms
-increases negative symptoms -causes EPS -prolactin rises |
|
high potency convential antipsychotics
|
haloperidol, fluphenazine
|
|
mid potency convential antipsychotics
|
loxapine, molindone, thiothixene, perphenazine
|
|
low potency convential antipsychotics
|
thioidazine, mesoridazine chloropromazine
|
|
EPS- acute dystonia
|
-acute muscle spasms
-within 5 days of initiation -due to high potency, IM/IV, large dose -treat with diphenhydramine, benztropine, anticholinergics, switch meds |
|
EPS- pseudoparkinsonism
|
-20-40%
-starts within several months -DA block cuases relative imbalance of DA and ACh -decrease movement, muscle rigidity, resting hand tremor, drooling, mask-like face, shuffling gait -treat by lowering dose, changing AP, give amantidine (antiparkinson agent)but will make worse |
|
EPS- akathisia
|
-20% to all conventionals, 50% in high potency
-days to weeks, often months -more presynaptic DA blockade vs postsynaptic DA blockade -DA blockade in mesocortical tract increases locomotor activity -can't distinguish from anxiety or psychosis -inner restlessness, can't sit still -treat- either up or lower dose, change AP or add b-blocker or add nezodiazepine |
|
Tardive dyskinesia
|
-pathology: postsyn DA block leads to hypersensitivity
-Incidence: 20% on conventionals -Risks: conventional AP, elderly, women -Presentation: involuntary movements, lip smacking, blinking, face, neck, trunk, extremities -Treatment: none -management: minimize exposure, minimize dose, Vit E, change to clozapine |
|
neuroleptic mailignant syndrome
|
-inidence is .2%
-mortatlity is 5-20% -mean age- 40 -higher risk: mood disorders, lithium, catatonia - all classes of typical AP -1/3 will represent if rechallenged |
|
nms diagnosis criteria
|
-on AP for 7 days
-hyperthermia >38 -muscle rigidity -5 of the following: change in mental status, tachycardia, labile bp, tachypnea or hypoxia, diaphoresis or sialorrhea, tremor, incontinence, CPK elevation or myoglobinuria, leukocytosis, metabolic acidosis -no other drug or medical reason |
|
NMS treatment
|
-reduce risk factors
-early recognition and dc of AP -supportive care --fluids --temperature --cardiac, respiratory, kidneys -DA agonists- bromocriptine, amantadine |
|
Depot Ap
|
-haloperidol- 10-15 times daily dose, once a month
-fluphenazine- 1.25 times daily amount, every 2 weeks -z track method -stabalize on oral first |
|
olanzapine- brand name
|
zyprexa
|
|
olanzapine- EPS
|
none
|
|
olanzapine- TD
|
low
|
|
olanzapine- adverse effects
|
-sedation
-weight gain -orthostatic hypotension -anticholinergics |
|
olanzapine- forms
|
-rapid dissolve- zyprexa zydis
-Im is short acting |
|
olanzapine- dose
|
5-20 mg/day
|
|
Riperidone- brand name
|
Risperdal
|
|
Riperidone- EPS
|
dose related > 6 mg
|
|
Riperidone- Td
|
low
|
|
Riperidone- adverse effects
|
-prolactin elevation
-othrostasis -sexual dysfunction |
|
Riperidone- forms
|
M tab
LA inj: risperdal consta (2 wk) |
|
Riperidone- dose
|
4-16 mg
|
|
quetiapine- brand name
|
seroquel
|
|
quetiapine- EPS
|
none
|
|
quetiapine- TD
|
low
|
|
quetiapine- adverse effects
|
sedation
hypotension HA weight gain lenticular formation |
|
quetiapine- dose
|
250-750 mg
|
|
ziprasidone- brand name
|
geoedon
|
|
ziprasidone- eps
|
none
|
|
ziprasidone- td
|
low
|
|
ziprasidone- adverse effects
|
mild sedation
minimal weight gain QTc prolongation |
|
ziprasidone- forms
|
IM available
|
|
ziprasidone- dose
|
40-160 mg/day
|
|
clozapine- brand name
|
clozaril
|
|
clozapine- eps
|
minimal
|
|
clozapine- td
|
low
|
|
clozapine- adverse effects
|
agranulocytosis
seizures sedation hypotension salivatoin weight gain |
|
clozapine- who
|
refractory patients
|
|
clozapine-monitoring
|
-weekly 6 months, bi weekly 6-12 months, monthly post 12 months
-WBC and ANC -don't do if WBC<3500 and ANC<2000 |
|
clozapine- dose
|
200-900 mg
|
|
aripiprazole- brand name
|
abilify
|
|
aripiprazole- moa
|
partial agonist of D2 receports
antagonist of 5HT2A partial agonist of 5HT1A |
|
aripiprazole- EPS
|
none
|
|
aripiprazole- TD
|
none
|
|
aripiprazole- adverse effects
|
anxiety
HA Nausea constipatin |
|
aripiprazole- dose
|
5-30 mg/day
|
|
metabolic syndrome
|
-need 3 of the following: abdominal obesity, hypertension, impaired fasting glucose, decreased HDl, elevated triglycerides
-atypical AP have been associated with weight gain, diabetes, lipid abnormalaties |
|
Good reponse to treatment
|
-have precipitating factors
-abrupt onset -positive symptoms -less frequent family history -good premorbid adjustment |
|
bad response to treatment
|
-no precipitating factors
-insidious onset -negative symptoms -frequent in family history -poor premorbid adjustment |
|
Criteria for depressions
|
->5 of the following: DSIGECAPS
-social/occupational dysfunction -not due to medical condition or drug use -not due to bereavement -not due to another mental health illness |
|
types of depressions
|
-major (atypical, typical, psychotic)
-dysthimia -organic caused -substance induced -medication induced |
|
epidemiology of depression
|
-17%
-late 20s -episode lasts 16 weeks |
|
risks of depressions
|
family history
female previous episode chronic illness substance abuse |
|
pathophysiology of depression
|
-chemical imbalance
-decreased levels of neurotransmitter (5HT, DA, NE) -dysregulation of receptors |
|
Lab assessment for depression
|
-cbc for anemia
-thyroid- hypothyroid -urine drug screen for substance abuse |
|
amitriptyline-brand name
|
elavil
|
|
amitriptyline- antidepressant class
|
TCA
|
|
nortiptyline- brand name
|
pamelor
|
|
nortriptyline- antidepressant class
|
TCA
|
|
impiramine- brand name
|
tofranil
|
|
impiramine- antidepressant class
|
TCA
|
|
desipramine- brand name
|
norpramin
|
|
desipramine- antidepressant calss
|
TCA
|
|
clomipramine- brand name
|
anafranil
|
|
clmipramine- antidepressant class
|
TCA
|
|
TCA mechanism of action
|
-5HT and NE reuptake inhibitor
-amount of 5HT and HE effects depends on structure: --three amines: 5HT --two amines: NE |
|
TCA side effects
|
-cardiovascular
-anticholinergic -sedation -weight gain -sexual dysfunction |
|
Phenelizine- brand name
|
nardil
|
|
phenelizine- antidepressant class
|
MAOI
|
|
tranylcypromine- brand name
|
parnate
|
|
tranylcypromine- antidepressant class
|
MAOI
|
|
MAOI mechanism of action
|
irreversible inhibition of MAOA and MAOB which increases 5HT, DA, NE
|
|
MAOI side effects
|
-hypotension
-dizziness -weight gain -insomnia -cardiac effect -constipation -sexual dysfunction |
|
MAOI risks
|
-hypertensive crisis
-food-drug interaction with tyramine |
|
MAOI drug interactions
|
-stimulants
-CNS antihypertensives -antidepressents -start SSRI after 14 days -5 half-life wash out of previous antidepressant |
|
Tyramine contraindications
|
-absolute: aged cheese, aged and cured meats, banana peel, sauerkraut, soy sauce, tap beer, marmite
-moderate: red/white wine, bottled/canned beer |
|
MAOI and merperidine/demerol
|
agitation, seizures, coma
|
|
MAOI and SSRI
|
hypertensive crisis
|
|
MAOI and TCA
|
hypertensive crisis
|
|
MAOI and stimulants
|
hypertensive crisis
|
|
MAOI and levadopa
|
hypertensive crisis
|
|
selegiline patch- brand name
|
emsam
|
|
selegiline patch- indication
|
major depression
|
|
selegiline patch- Mechanism of action
|
-MAOA inhibitor, MAO B at dose dependent
-food restrictions at 9 mg -start low |
|
citalopram- brand name, andtidepressant class
|
celexa
SSRI |
|
escitalopram- brand name, antidepressant class
|
lexapro
SSRI |
|
Fluoxetine- brand name, antidepressant class
|
prozac, prozac weekly, sarafem
SSRI |
|
Fluvoxamine- brand name, antidepressant class
|
luvox
SSRI |
|
Paroxetine- brand name, antidepressant class
|
paxil, paxil CR
SSRI |
|
sertraline- brand name, antidepressant class
|
zoloft
SSRI |
|
fluoxetine- half life
|
long (72 hours)
|
|
fluoxetine- metabolism
|
2d6, 3a4, 2c inhibition
|
|
sertraline- metabolite
|
active
|
|
fluoxetine- metabolite
|
active
|
|
fluvoxamine- metabolism
|
1a2, 3a4, 2c inhibition
|
|
paroxetine- side effects
|
anticholinergic
|
|
paroxetine- half life
|
shortest
|
|
paroxetine- metabolite
|
not active
|
|
paroxetine- inhibition
|
2d6
|
|
citalopram- activity
|
only 5HT activity
|
|
escitalopram- what is it
|
s-enantiomer of citalopram
|
|
SSRI side effects
|
-2 weeks: nausea, diarrhea, sedation, insomnia, anxiety
-chronic: headache, sexual dysfunction, night sweats, nightmares |
|
SSRI toxicity
|
serotonin syndrome: hyperthermia, excitement, rigidity, hypotensinon, diaphoresis, tachycardia
|
|
Venlafaxine- brand name
|
effexor, effexor ER
|
|
Venlafaxine- MOA
|
SNRI but only at higher doses
|
|
Venlafaxine- metabolite
|
active
|
|
Venlafaxine- side effects
|
-N/D
-headache -hypertension -sexual dysfunction -nervousness -anxiety -XR reduces side effects |
|
Duloxetine- brand name
|
cymbalta
|
|
Duloxetine- MOA
|
SNRI
|
|
Duloxetine- side effects
|
nausea
insomnia headache |
|
Duloxetine- substrate fo
|
2d6, 1a2
|
|
Buproprion- brand name
|
wellbutrin, wellbutrin SR, wellbutin XL
|
|
Buproprion- MOA
|
NDRI
|
|
Buproprion- contraindications
|
seizure disorder
eating disorder zyban |
|
Buproprion- side effects
|
GI upset
headache restlessness seizures insomnia no sexual dysfuntion |
|
Nefazodone- brand name
|
serzone
|
|
Nefazodone- MOA
|
SRI and S2 antagonist
|
|
Nefazodone- drug interactions
|
3a4 inhibitor
|
|
Nefazodone- forms available
|
only generic due to liver damage
|
|
Nefazodone- side effects
|
dry mouth
nausea dizziness constipation sedation liver failure: monitor LFT no sexual dysfunction |
|
Mirtazapine- brand name
|
remeron, remeron sol tabs
|
|
Mirtazapine- MOA
|
-alpha 2 antagonist, 5HT3, 2A, 2C antagonist
-increased NE, 5HT |
|
Mirtazapine- side effects
|
Sedation
weight gain dry mouth constipation no sexual dysfunction |
|
Trazodone- class
|
heterocyclic antidepressant
|
|
Trazadone- MOA
|
increase 5HT, block H1
|
|
Trazadone- uses
|
insomnia now, not depressino
|
|
SJW-interaction
|
bcp
|
|
refractory depression
|
-adequate trial of initial agent
-assess for unrecognized drug and medical causes -combo antidepressants -augmentation: lithium, antipsychotics, stimulants, thyroid -ECT |