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104 Cards in this Set
- Front
- Back
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prevalence of depression
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estimated to be around 16%
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risk factors for reoccurence of depression (4)
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-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 |
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45-60% of pts w/ major depression have a neuroendocrine abnormality. Types of neuroendocrine abnormalities (3)
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-hypersecretion of cortisol
-lack of cortisol suppression after dexamethasone administration -abnormal or decreased TSH after receiving TRH |
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endocrine disorders associated w/ depression (1)
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hypothyroidism
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deficiency states associated w/ depression (3)
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-pernicious anemia
-wernicke's encephalopathy -severe anemia |
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infections associated w/ depression (3)
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-influenza
-TB -AIDS |
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metabolic disorders associated w/ depression (2)
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-hypokalemia
-hyponatremia |
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cardiovascular disorders associated w/ depression (3)
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-post MI
-post CVA -CHF |
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neurologic disorders associated w/ depression (4)
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-alzheimer's dz
-parkinson's dz -post CVA -MS |
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psychiatric disorders associated w/ depression (4)
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-anxiety disorders
-eating disorders -schizophrenia -substance dependence |
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time for antidepressant effects to be seen after initial dose
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2-4wks
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FDA warning w/ antidepressants
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increased risk of suicidal thinking and behavior in children and adolescents
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alpha1 adrenergic blockade adverse effect
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orthostatic hypotension
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cholinergic blockade
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constipation, blurred vision, urinary retention, dry mouth
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histaminergic blockade
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weight gain, sedation
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dopamine reuptake inhibition
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psychotic features, activation
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serotonin reuptake inhibition
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NVD, anxiety, sexual dysfunction, insomnia
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norepinephrine reuptake inhibtion
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sexual dysfunction, insomnia, tachycardia, tremor
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symptoms of serotonin syndrome
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confusion, seizures, tachycardia, agitation, hyperthermia, tremor, coma, HTN, ataxia
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tricyclic classification
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mixed 5-HT/NE reuptake inhibitor (block reuptake of DA)
-block the cholinergic, histaminergic, and alpha1 adrenergic receptors |
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TCAs have been found effect in the management of what conditions besides depression? (4)
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-enuresis
-trigeminal/post-herpetic neuralgias -diabetic neuropathy -enuresis -migraine prophylaxis |
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secondary vs tertiary amines
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secondary preferred since they have less anticholinergic effects
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TCA adverse effects
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-anticholinergic, antihistaminergic, alpha1 adrenergic blockade
-cardiac conduction delays -drowsiness, wkness, fatigue -excessive perspiration -sexual dysfunction, szrs -weight gain |
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TCA w/ FDA indication for OCD
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clomipramine (Anafranil)
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TCA with FDA indication for anxiety associated w/ alcoholism
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doxepin (Sinequan)
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TCA w/ FDA indication for enuresis in children
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imipramine (Tofranil)
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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 |
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TCA drug interactions
-INCREASES RISK OF SZRS -cardiac arrhythmias |
-bupropion, alcohol
-quinolones |
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dosing for TCA's, starting dose vs therapeutic dose
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starting dose does not equal therapeutic dose
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secondary amines TCAs
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desipramine, nortriptyline, protripyline
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Venlafaxine classification
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serotonin noradrenergic reuptake inhibitors (SNRIs) (potent inhibitor of 5-HT and NE reuptake, weak inhibitor of DA reuptake)
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FDA indications of venlafaxine (4)
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-depression
-GAD -SAD -panic d/o |
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non-FDA indications for venlafaxine (2)
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-OCD
-post-traumatic stress d/o |
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Venlafaxine adverse effects
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-agitation
-constipation -dizziness, dry mouth -headache -insomnia -nausea -SEXUAL DYSFUNCTION, sweating |
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Venlafaxine may cause a _____ with higher doses
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dose related increase in BP
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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 |
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Venlafaxine drug interactions
-serotonin syndrome |
-MAO-inhibitors
-TCAs -other serotonergic meds |
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duloxetine (Cymbalta) MOA
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inhibitor of 5-HT and NE reuptake, weak inhibitor of DA reuptake
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duloxetine FDA indications
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-depression
-diabetic neuropathic pain (anxiety???) |
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duloxetine adverse effects
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-constipation
-diarrhea, dizziness, dry mouth -fatigue -insomnia, INCREASE LFTs -NAUSEA |
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duloxetine PK's
-food -t1/2 |
-food may delay the rate & extent of absorption
-t1/2=12hrs |
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normalization of sleep and appetite
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week 1
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improvement in energy
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week 2
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improvement in mood
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week 4
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SSRI FDA indicacted for OCD
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fluvoxamine (Luvox)
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SSRIs adverse effects
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-anxiety
-headache -nausea -sexual dysfunction, sleep disturbances -tremor |
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fluoxetine has been associated w/ the most...
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agitation
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paroxetine has been associated w/ the most...
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sedation and weight gain
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sertraline has been associated with the most...
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diarrhea
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SSRIs most likely to cause drug interactions (2)
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fluoxetine and paroxetine (potent inhibitors of CYP2D6)
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fluoxetine metabolism
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-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 |
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all other SSRIs t1/2
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24h so once daily dosing normally used
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SSRIs starting dose vs. therapeutic dose
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sometimes starting dose = therapeutic dose
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paxil CR
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releases lower in GI tract to prevent nausea (not controlled release)
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SSRIs pregnancy category
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all C, except paxil (D)
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SSRIs drug interactions:
most likely to occur with... least likely to occur with... |
warfarin
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SSRIs drug interactions that increases risk for serotonin syndrome (5)
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MAOIs, sibutramine, lithium, triptans, st.johns wort
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Agents with mixed serotonin effects
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trazodone, nefazodone,
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trazodone and nefazodone MOA
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5-HT reuptake inhibitor; 5-HT2 antagonist; low affinity for alpha1 receptors
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effects of 5-HT2 antagonist properties of trazodone and nefazodone
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reduced anxiety, sexual dysfunction, insomnia
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most popular use of trazodone
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sedative-hypnotic
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trazodone and nefazodone adverse effects
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-constipation
-dry mouth -headache -nausea -ORTHOSTATIC HYPOTENSION -PRIAPISM -SEDATION, somnolence |
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nefazodone black box warning
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hepatotoxicity-check LFTs
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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 |
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nefazodone is potent inhibitor of...
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CYP3A4
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identify antidepressants associated w/ the following characteristics
-Activating |
-SNRIs
-SSRIs (except paxil and luvox) |
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sedating
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-TCA
-nefazodone -trazodone |
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associated w/ sexual dysfunction
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-TCA
-SNRIs -SSRIs |
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associated w/ weight gain
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-TCA
-Paxil |
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potentially hepatotoxic
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-nefazodone
-luvox |
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Bupropion MOA
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mixed DA/NE reuptake inhibitor (DA reuptake inhibitor w/ possible noradrenergic activity)
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bupropion FDA indications (3)
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-depression
-seasonal affective d/o -smoking cessation (NOT helpful w/ anxiety) |
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off label indication for bupropion
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sexual dysfunction
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bupropion adverse effects
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-agitation, anxiety
-constipation -dizziness, dry mouth -headache -insomnia -N/V -tremor |
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bupropion is contraindicated in what patients
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in patients having seizures
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bupropion drug interactions:
use w/ caution with these agents due to lowering of seizure threshold |
-antipsychotics
-ANTIDEPRESSANTS (ESP TCAs) -ALCOHOL |
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bupropion max dose
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450mg/day; need at least 300mg/day to treat indications
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mirtazapine (Remeron) MOA
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-mixed serotonin/NE effects
-enhances central noradrenergic and serotonin activity the antagonism of central presynaptic alpha2 adrenergic autoreceptors and heteroreceptors |
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mirtazapine effects on blockade of serotonin type 2 receptors
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reduced insomnia, anxiety, sexual dysfunction
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mirtazapine effects on blockade of serotonin type 3 receptors
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reduced nausea
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additional effects of mirtazapine
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anticholinergic, antihistaminergic (at lower doses -> sedation and wt gain
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mirtazapine adverse effects
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-constipation
-dry mouth -increased appetite -SEDATION -WEIGHT GAIN (increase in cholesterol, increase in LFTs, agranulocytosis, neutropenia--rare) |
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mirtazapine PK's
-food -t1/2 |
-food does not affect rate or extent of absorption
-t1/2=20-40hrs, once daily dosing normally used |
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higher doses may cause what with mirtazapine?
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activation rahter than sedation
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FDA indication of mirtazapine
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-depression
-PTSD (offlabel???) |
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phenelzine (Nardil) and tranylcypromine (Parnate) MOA
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MAO inhibitors-increase concentration of NE, DA, 5-HT within the neuronal synapse
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MAO inhibitors adverse effects
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may cause serotonin syndrome and hypertensive crisis
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MAO inhibitors absoluate dietary restrictions
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-aged chesses
-aged & cured meats -improperly stored/spoiled meats -sauerkraut -soy sauce, soybean condiments -tap beer |
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MAO inhibitors moderate dietary restrictions
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-red or white wine
-bottled or canned beer |
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selegiline MOA
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MAO-I type B selective
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FDA indication for selegiline
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depression
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selegiline administration
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available in transdermal system
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St. Johns Wort MOA
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believed to inhibit reuptake of serotonin
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drug interactions w/ st. johns wort
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-OCs
-serotonergic meds (serotonin syndrome) -warfarin |
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st. johns wort adverse effects
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insomnia, vivid dreams, restlessness, anxiety, irritability, GI upset, dry mouth, dizziness, HA, photo dermatitis
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treatment phase guidelines in major depressive d/o
ACUTE -length of treatment -indications |
-6-12wks
-all pts w/ acute major depressive episode |
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CONTINUATION
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-6-12months
-all pts responsive to acute treatment of major depressive episode |
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MAINTENANCE
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-variable (2-5yrs to indefinitely)
-pts w/ >=3 prior depressive episodes or high-risk factors for recurrences |
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activating
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-bupropion
-high dose mirtazapine |
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sedating
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-low dose mirtazapine
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associated w/ weight gain
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-mirtazapine
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may cause seizures
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-bupropion
-TCAs |
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treating dry mouth
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-chew on sugarless candy
-drink fluids |
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constipation
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increase dietary fiber
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