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104 Cards in this Set

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prevalence of depression
estimated to be around 16%
risk factors for reoccurence of depression (4)
-1st degree relative w/ depression
-1st episode occurring before 20
->2 prior episodes of depression
-h/o recurrence w/in 1yr after medication d/c'd
45-60% of pts w/ major depression have a neuroendocrine abnormality. Types of neuroendocrine abnormalities (3)
-hypersecretion of cortisol
-lack of cortisol suppression after dexamethasone administration
-abnormal or decreased TSH after receiving TRH
endocrine disorders associated w/ depression (1)
hypothyroidism
deficiency states associated w/ depression (3)
-pernicious anemia
-wernicke's encephalopathy
-severe anemia
infections associated w/ depression (3)
-influenza
-TB
-AIDS
metabolic disorders associated w/ depression (2)
-hypokalemia
-hyponatremia
cardiovascular disorders associated w/ depression (3)
-post MI
-post CVA
-CHF
neurologic disorders associated w/ depression (4)
-alzheimer's dz
-parkinson's dz
-post CVA
-MS
psychiatric disorders associated w/ depression (4)
-anxiety disorders
-eating disorders
-schizophrenia
-substance dependence
time for antidepressant effects to be seen after initial dose
2-4wks
FDA warning w/ antidepressants
increased risk of suicidal thinking and behavior in children and adolescents
alpha1 adrenergic blockade adverse effect
orthostatic hypotension
cholinergic blockade
constipation, blurred vision, urinary retention, dry mouth
histaminergic blockade
weight gain, sedation
dopamine reuptake inhibition
psychotic features, activation
serotonin reuptake inhibition
NVD, anxiety, sexual dysfunction, insomnia
norepinephrine reuptake inhibtion
sexual dysfunction, insomnia, tachycardia, tremor
symptoms of serotonin syndrome
confusion, seizures, tachycardia, agitation, hyperthermia, tremor, coma, HTN, ataxia
tricyclic classification
mixed 5-HT/NE reuptake inhibitor (block reuptake of DA)

-block the cholinergic, histaminergic, and alpha1 adrenergic receptors
TCAs have been found effect in the management of what conditions besides depression? (4)
-enuresis
-trigeminal/post-herpetic neuralgias
-diabetic neuropathy
-enuresis
-migraine prophylaxis
secondary vs tertiary amines
secondary preferred since they have less anticholinergic effects
TCA adverse effects
-anticholinergic, antihistaminergic, alpha1 adrenergic blockade
-cardiac conduction delays
-drowsiness, wkness, fatigue
-excessive perspiration
-sexual dysfunction, szrs
-weight gain
TCA w/ FDA indication for OCD
clomipramine (Anafranil)
TCA with FDA indication for anxiety associated w/ alcoholism
doxepin (Sinequan)
TCA w/ FDA indication for enuresis in children
imipramine (Tofranil)
TCA pharmokinetics
-food
-t1/2
-food does not delay or affect absorption
-t1/2 of all TCAs is 24hrs, so once daily dosing normally used
TCA drug interactions
-INCREASES RISK OF SZRS
-cardiac arrhythmias
-bupropion, alcohol
-quinolones
dosing for TCA's, starting dose vs therapeutic dose
starting dose does not equal therapeutic dose
secondary amines TCAs
desipramine, nortriptyline, protripyline
Venlafaxine classification
serotonin noradrenergic reuptake inhibitors (SNRIs) (potent inhibitor of 5-HT and NE reuptake, weak inhibitor of DA reuptake)
FDA indications of venlafaxine (4)
-depression
-GAD
-SAD
-panic d/o
non-FDA indications for venlafaxine (2)
-OCD
-post-traumatic stress d/o
Venlafaxine adverse effects
-agitation
-constipation
-dizziness, dry mouth
-headache
-insomnia
-nausea
-SEXUAL DYSFUNCTION, sweating
Venlafaxine may cause a _____ with higher doses
dose related increase in BP
Venlafaxine PK's
-food
-t1/2
-food has no significant effect on absorption
-3-7hrs and 11-13hrs for active metabolite = BID dosing normally used (IR) and daily dosing for ER
Venlafaxine drug interactions
-serotonin syndrome
-MAO-inhibitors
-TCAs
-other serotonergic meds
duloxetine (Cymbalta) MOA
inhibitor of 5-HT and NE reuptake, weak inhibitor of DA reuptake
duloxetine FDA indications
-depression
-diabetic neuropathic pain
(anxiety???)
duloxetine adverse effects
-constipation
-diarrhea, dizziness, dry mouth
-fatigue
-insomnia, INCREASE LFTs
-NAUSEA
duloxetine PK's
-food
-t1/2
-food may delay the rate & extent of absorption
-t1/2=12hrs
normalization of sleep and appetite
week 1
improvement in energy
week 2
improvement in mood
week 4
SSRI FDA indicacted for OCD
fluvoxamine (Luvox)
SSRIs adverse effects
-anxiety
-headache
-nausea
-sexual dysfunction, sleep disturbances
-tremor
fluoxetine has been associated w/ the most...
agitation
paroxetine has been associated w/ the most...
sedation and weight gain
sertraline has been associated with the most...
diarrhea
SSRIs most likely to cause drug interactions (2)
fluoxetine and paroxetine (potent inhibitors of CYP2D6)
fluoxetine metabolism
-elimination t1/2 of 2-3d
-norfluoxetine (active metabolite) has elimination t1/2 of 7-9d, so once daily or once weekly dosing normally used
all other SSRIs t1/2
24h so once daily dosing normally used
SSRIs starting dose vs. therapeutic dose
sometimes starting dose = therapeutic dose
paxil CR
releases lower in GI tract to prevent nausea (not controlled release)
SSRIs pregnancy category
all C, except paxil (D)
SSRIs drug interactions:
most likely to occur with...
least likely to occur with...
warfarin
SSRIs drug interactions that increases risk for serotonin syndrome (5)
MAOIs, sibutramine, lithium, triptans, st.johns wort
Agents with mixed serotonin effects
trazodone, nefazodone,
trazodone and nefazodone MOA
5-HT reuptake inhibitor; 5-HT2 antagonist; low affinity for alpha1 receptors
effects of 5-HT2 antagonist properties of trazodone and nefazodone
reduced anxiety, sexual dysfunction, insomnia
most popular use of trazodone
sedative-hypnotic
trazodone and nefazodone adverse effects
-constipation
-dry mouth
-headache
-nausea
-ORTHOSTATIC HYPOTENSION
-PRIAPISM
-SEDATION, somnolence
nefazodone black box warning
hepatotoxicity-check LFTs
trazodone/nefazodone PK's
-food
-t1/2
-food decreases the extent of absorption and bioavailablity of nefazodone
-2-4h for nefazodone = BID dosing
-3-6h for trazodone
nefazodone is potent inhibitor of...
CYP3A4
identify antidepressants associated w/ the following characteristics
-Activating
-SNRIs
-SSRIs (except paxil and luvox)
sedating
-TCA
-nefazodone
-trazodone
associated w/ sexual dysfunction
-TCA
-SNRIs
-SSRIs
associated w/ weight gain
-TCA
-Paxil
potentially hepatotoxic
-nefazodone
-luvox
Bupropion MOA
mixed DA/NE reuptake inhibitor (DA reuptake inhibitor w/ possible noradrenergic activity)
bupropion FDA indications (3)
-depression
-seasonal affective d/o
-smoking cessation
(NOT helpful w/ anxiety)
off label indication for bupropion
sexual dysfunction
bupropion adverse effects
-agitation, anxiety
-constipation
-dizziness, dry mouth
-headache
-insomnia
-N/V
-tremor
bupropion is contraindicated in what patients
in patients having seizures
bupropion drug interactions:
use w/ caution with these agents due to lowering of seizure threshold
-antipsychotics
-ANTIDEPRESSANTS (ESP TCAs)
-ALCOHOL
bupropion max dose
450mg/day; need at least 300mg/day to treat indications
mirtazapine (Remeron) MOA
-mixed serotonin/NE effects
-enhances central noradrenergic and serotonin activity the antagonism of central presynaptic alpha2 adrenergic autoreceptors and heteroreceptors
mirtazapine effects on blockade of serotonin type 2 receptors
reduced insomnia, anxiety, sexual dysfunction
mirtazapine effects on blockade of serotonin type 3 receptors
reduced nausea
additional effects of mirtazapine
anticholinergic, antihistaminergic (at lower doses -> sedation and wt gain
mirtazapine adverse effects
-constipation
-dry mouth
-increased appetite
-SEDATION
-WEIGHT GAIN
(increase in cholesterol, increase in LFTs, agranulocytosis, neutropenia--rare)
mirtazapine PK's
-food
-t1/2
-food does not affect rate or extent of absorption
-t1/2=20-40hrs, once daily dosing normally used
higher doses may cause what with mirtazapine?
activation rahter than sedation
FDA indication of mirtazapine
-depression
-PTSD (offlabel???)
phenelzine (Nardil) and tranylcypromine (Parnate) MOA
MAO inhibitors-increase concentration of NE, DA, 5-HT within the neuronal synapse
MAO inhibitors adverse effects
may cause serotonin syndrome and hypertensive crisis
MAO inhibitors absoluate dietary restrictions
-aged chesses
-aged & cured meats
-improperly stored/spoiled meats
-sauerkraut
-soy sauce, soybean condiments
-tap beer
MAO inhibitors moderate dietary restrictions
-red or white wine
-bottled or canned beer
selegiline MOA
MAO-I type B selective
FDA indication for selegiline
depression
selegiline administration
available in transdermal system
St. Johns Wort MOA
believed to inhibit reuptake of serotonin
drug interactions w/ st. johns wort
-OCs
-serotonergic meds (serotonin syndrome)
-warfarin
st. johns wort adverse effects
insomnia, vivid dreams, restlessness, anxiety, irritability, GI upset, dry mouth, dizziness, HA, photo dermatitis
treatment phase guidelines in major depressive d/o
ACUTE
-length of treatment
-indications
-6-12wks
-all pts w/ acute major depressive episode
CONTINUATION
-6-12months
-all pts responsive to acute treatment of major depressive episode
MAINTENANCE
-variable (2-5yrs to indefinitely)
-pts w/ >=3 prior depressive episodes or high-risk factors for recurrences
activating
-bupropion
-high dose mirtazapine
sedating
-low dose mirtazapine
associated w/ weight gain
-mirtazapine
may cause seizures
-bupropion
-TCAs
treating dry mouth
-chew on sugarless candy
-drink fluids
constipation
increase dietary fiber