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145 Cards in this Set
- Front
- Back
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tyramine effect
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taken into cell and causes NE to be released
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MAOIs side effects
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orthostatic hypotension
insomnia sexual dysfunction |
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use of MAOIs
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atypical and refractory depression
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synaptic effects of TCAs
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block 5HT reuptake
block NE reuptake block anticholinergic M1 receptors block α1 receptors block histamine H1 and H2 receptors |
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use of TCAs
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depressive syxs that also include:
considerable anxiety (OCD) insomnia somatic syxs (pain) |
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TCA for OCD
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clomipramine
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TCA for pain
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amitriptyline
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TCA anticholinergic side effects
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dry mouth
blurred vision tachycardia urinary retention constipation confusion |
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TCA adrenergic side effects
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dizziness
decreased blood pressure drowsiness |
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TCA histaminergic side effects
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sedation
weight gain decreased stomach acid production |
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other side effects of TCAs
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slowed cardiac electical conduction
lowered seizure threshold decreased levels of valproate |
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most epileptogenic TCA
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maprotiline
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amoxapine and unique characteristic
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TCA
significant DA blocking activity - similar side effect profile to typical antipsychotic |
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TCAs
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amitriptyline (elavil)
clomipramine (anafranil) doxepin (sinequan) imipramine (tofranil) trimipramine (surmontil) desipramine (norpramin) nortriptyline (pamelor or aventyl) protriptyline (vivactil) amoxapine (asendin) maprotiline (ludiomil) |
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SSRIs
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citalopram (celexa)
escitalopram (lexapro) fluoxetine (prozac) fluvoxamine (luvox) paroxetine (paxil) sertraline (zoloft) |
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uses of SSRIs
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major depression
anxiety disorders bulimia migraines |
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SSRIs used for what anxiety disorders?
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panic disorder
OCD PTSD social phobia |
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side effects of SSRIs
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agitation
akasthesia insomnia nocturnal myoclonus sexual dysfunction appetite suppression nausea gi distress diarrhea headache |
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fluoxetine benefit
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longest half life
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common side effect with sertraline
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gi upset
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mechanism for SSRIs effect on depression
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disinhibition of 5HT pathway from midbrain raphe to prefrontal cortex;
maintenance dose = starting dose; onset of response = 3.6 weeks; expect complete remission |
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mechanism for SSRIs effect on OCD
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disinhibition of 5HT pathway from midbrain raphe to basal ganglia;
maintenance dose > starting dose; onset of response = 12-26 weeks; usual response is <50% improvement |
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mechanism for SSRIs effect on panic disorder
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disinhibition of 5HT pathway from midbrain raphe to limbic cortex and hippocampus;
usual starting dose is lower than for other conditions; maintenance dose may be > starting dose; target symptoms may worsen at first; usual response >50% improvement |
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which condition do SSRIs initially worsen symptoms in?
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panic disorder
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mechanism for SSRIs effect on bulimia
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disinhibition of 5HT pathway from midbrain raphe to hypothalamus;
starting dose higher than for other conditions; maintenance dose may be > starting dose; onset of response quicker than other conditions |
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condition with quickest response to SSRIs
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bulimia
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condition requiring lower starting doses of SSRIs
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panic disorder
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condition requiring higher starting doses of SSRIs
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bulimia
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only SSRI with significant DA reuptake inhibition
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sertraline
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unique characteristic to sertraline and benefit/disadvantage
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significant DA reuptake inhibition - may be superior in treating melancholic depression and depression with delusions but may cause more anxiety, panic, and insomnia
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fluoxetine effects metabolism of which drugs
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inhibits 2D6
TCAs tegretol codeine its own metabolism |
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most activating SSRI and why
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paroxetine
NE reuptake inhibition at higher doses |
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paroxetine half life and effects on metabolism
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short half life so may experience discontinuation syndrome;
potent 2D6, weak 3A3/4 inhibitor - strongly inhibits its own metabolism |
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SSRI discontinuation syndrome and likely culprit
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paroxetine;
agitation, akathesia, dystonia, restlessness, dizziness, gi syxs |
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most likely to cause weight gain of SSRIs
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paroxetine
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fluvoxamine interactions
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strongly inhibits 2CI9 and IA2
affects theophylline dosing raise clozaril and zyprexa levels floxin antibiotics some 3A3/4 inhibition |
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most selective SSRI
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citalopram/escitalopram
may be best tolerated |
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lexapro
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active isomer of celexa with 10 mg dose probably equaling the efficacy of 20-40 mg of celexa
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venlafaxine (effexor)
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combination SSRI and NERI
used for pts not responding to SSRI |
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side effects of venlafaxine at low to medium doses
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nausea
agitation sexual dysfunction insomnia |
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side effects of venlafaxine at high doses
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hypertension
severe insomnia agitation nausea headache |
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duloxetine (cymbalta)
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combination SSRI and NERI
FDA approved for MDD, GAD, fibromyalgia, diabetic peripheral neuropathy, urinary incontinence |
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useful for pts with depression and neuropathic pain
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duloxetine
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nefazodone (serzone)
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5HT2 blocker, some SSRI capacity, mildly NERI
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side effects of nefazodone
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fulminant pancreatitis
liver failure (black box warning) |
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trazodone (desyrel)
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5HT2 blocker
some SSRI capacity H1 blocker α1 blocking very short half life |
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side effects of trazodone
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sedation
orthostatic hypotension priapism |
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mirtazapine (remeron)
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α2 antagonist - disinhibit NE and 5HT neurons;
5HT2/3 receptor blockade; potent H1 blockade |
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side effects of mirtazapine
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sedation
weight gain agranulocytosis (rare) |
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theoretical use of mirtazapine
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depression associated with anxiety, agitation, and insomnia;
should reverse SSRI induced sexual dysfunction, nausea, and gi upset |
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bupropion (wellbutrin or zyban)
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NERI and DARI;
stimulating agent |
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uses/advantages of bupropion
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smoking cessation
GAD SAD ADHD little or no sexual dysfunction |
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which antidepressant has little or no sexual dysfunction
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bupropion
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bupropion side effects
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lower seizure threshold
stimulating (avoid in pts already agitated and severely insomniac) |
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contraindications for bupropion
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seizure disorder
head injury predisposing to seizure young females with anorexia/bulimia |
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relative contraindications to ECT
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space-occupying intracerebral lesions
recent mi recent cerebrovascular accident large, unstable aneurysm |
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pathway associated with positive syxs of schizophrenia
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hyperactivity of mesolimbic pathway
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positive syxs
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delusions
hallucinations disorganized speech disorganized behavior agitation |
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pathway associated with negative and cognitive syxs of schizophrenia
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deficits in mesocortical pathway
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negative syxs
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passivity
apathetic social withdrawal sterotyped thinking anhedonia attentional impairment emotional withdrawal |
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cognitive syxs of schizophrenia
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impaired verbal fluency
problems with focus/attention problems with serial learning |
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nigrostriatal pathway
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blockade causes parkinsonian syxs and hyperkinetic movement such as tardive dyskinesia
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typical versus atypical psychotics
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atypicals have more selectivity for mesolimbic DA pathway and relatively less activity in nigrostriatal pathway
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high potency typical antipsychotics
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fluphenazine (prolixin)
haloperidol (haldol) pimozide (orap) thiothiene (navane) trifluoperazine (stelazine) |
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mid potency typical antipsychotics
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loxapine (loxitane)
molindone (moban) perphenazine (trilafon) |
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low potency typical antipsychotics
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chlorpromazine (thorazine)
thioridazine (mellaril) mesoridazine (serentil) |
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which antipsychotics are available as injections
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fluphenazine
haloperidol |
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side effects of high potency typical antipsychotics
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EPS
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side effects of low potency typical antipsychotics
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orthostasis
sedation anticholinergic effects |
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atypical antipsychotics
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clozapine (clozaril)
risperidone (risperdal) olanzapine (zyprexa) quetiapine (seroquel) ziprasidone (geodon) aripiprazole (abilify) paliperidone (invega) |
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clozapine side effects
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hypotension
seizures agranulocytosis weight gain constipation sialorrhea cardiomyopathy tachycarida sedation |
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use of clozapine
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treatment-refractory cases
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characteristics of agranulocytosis with clozapine
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1-2% of patients;
greatest risk in first 6 months, decreases thereafter; risk is not dosage related; augmentation with GM-CSF |
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risperidone side effects
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hyperprolactinemia
hypotension |
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consta
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long acting injection risperidone - every 2 weeks, continue oral for 3-4 weeks after first injection
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paliperidone
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major active metabolite of risperidone;
little benefit as risperidone is available in generic form |
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olanzapine side effects
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weight gain/metabolic syn
increased LFTs sedation hypotension constipation |
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quetiapine side effects
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initial sedation
asymptomatic LFT elevation hypotension hypnotic uses short half life = bid dosing |
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ziprasidone
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less likely to cause sedation and weight gain;
short half life - bid dosing |
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ziprasidone side effects
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prolong QTc interval
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aripiprazole differences from other atypicals
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partial D2 agonist activity
very long half life |
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aripiprazole precautions
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2D6 and 3A4 metabolize it - higher levels when administered with prozac, ketoconazole, etc.
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antipsychotic with highest likelihood of initiating arrhythmias
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ziprasidone - prolong QTc interval
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associated with malignant arrhythmias
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thioridazine
mesoridazine (metabolite) |
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pts should avoid ziprasidone if
(may be more of a theoretical concern) |
taking antiarrhythmics
taking arrhythmogenic agents have sinus bradycardia have high grade AV block hypokalemic or hypomagnesemic |
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orthostatic hypotension is most common in
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low potency antipsychotic
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may cause nasal congestion
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risperidone
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particularly associated with decreased libido and also retrograde ejaculation
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thioridazine
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most dramatic weight gain seen with
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olanzapine
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allergic dermatitis and photosensitivity associated with
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chlorpromazine
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irreversible pigmentation of retina
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thioridazine
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acute dystonia treatment
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benztropine
benadryl lorazepam |
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akathesia treatment
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beta blockers
benzodiazepines clonidine anticholinergics amantadine |
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treatment for parkinsonian side effects
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amantadine (symmetrel)
anticholinergics: benztropine (cogentin) biperiden (akineton) ethopropazine (parsidol) orphenadrine (norflex) procyclidine (kemadrin) trihexyphenidyl (artane) |
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amantadine mechanism
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enhance DAergic transmission in the CNS
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NMS
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muscular rigidity
dystonia akinesia mutism obtundation agitation hyperpyrexia sweating increased HR and BP leukocytosis increased CPK, LFTs myoglobinuria |
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NMS treatment
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dantrolene
bromocriptine |
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dantrolene mechanism
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skeletal muscle relaxant
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bromocriptine mechanism
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DA agonist
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drugs that alter lithium excretion
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increase Li levels:
thiazides NSAIDS ACEIs ARBs decrease Li levels: xanthine osmotic diuretics |
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recommended baseline testing before starting Li
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UA
TSH T2 pregnancy test serum creatinine |
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early warnings of Li toxicity
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dysarthria
new/worse tremor and ataxia diarrhea anorexia n/v |
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Li side effects
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benign postural tremor
weight gain polydipsia nephrogenic diabetes insipidus hypothyroid memory impairment slow reaction time lack of spontaneity lost creativity |
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baseline labs for valproate
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platelet counts
LFTs |
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valproate dose-related adverse events
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gi effects
tremor sedation LFT elevations |
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sustained release formulation of valproate is indicated for
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migraine
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black box warning for valproate
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hepatotoxicity
pancreatitis teratogenicity |
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carbamazepine side effects
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agranulocytosis;
vasopressin-like effect --> hyponatremia or water intoxication; decreased AV conduction; aplastic anemia; hepatitis; benign rash; gi effects; dizziness, ataxia, sedation |
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carbamazepine OD treatment
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lavage and charcoal
romazicon to reverse sedation |
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may produce false positive pregnancy tests
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carbamazepine
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carbamazepine interactions
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induces its own metabolism
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oxcarbazepine
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structural analogue of carbamazepine
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gabapentin side effects
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sedation
dizziness ataxia fatigue |
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lamotrigine and valproate interaction
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lamotrigine half life is doubled by valproate (reduced by most anticonvulsants)
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lamotrigine side effects
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stevens-johnson syn (within 1st 8 wks)
dizziness diplopia ataxia n/v |
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topiramate side effects
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anorexia/weight loss
dose related psychomotor slowing somnolence concentration ataxia |
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pregabalin approved for treatment of
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neuropathy
postherpetic neuralgia adjunct for partial seizures fibromyalgia |
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mood stabilizers
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lithium
valproate (depakote) carbamazepine (tegretol) oxcarbazepine (trileptal) gabapentin (neurontin) lamotrigine (lamictal) topiramate (topamax) tiagabine (gabitril) pregabalin (lyrica) |
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indications for anxiolytics and sedatives-hypnotics
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anxiety disorders
insomnia alcohol/sedative withdrawal |
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effective in treating alcohol withdrawal and delirium tremens
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lorazepam (ativan)
outpatient: chlordiazepoxide (librium) diazepam (valium) |
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benzos adverse effects
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sedation
ataxia confusion weakness dizziness anterograde amnesia |
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avoid chlordiazepoxide and diazepam in
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pts with liver diseas due to risk of toxicity from impaired metabolism
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advantages of non-benzo hypnotics
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less cognitive, memory, motor side effects
shorter half life no dependence, tolerance, withdrawal syxs |
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zaleplon and zolpidem mechanism
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binds GABA receptor at different receptor sidtes, rapid onset of action
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eszopiclone
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non-benzo hypnotic
not limited to short-term use |
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ramelteon (rozerem) mechanism
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melatonin receptor agonsit for insomnia
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ramelteon side effects
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increase prolactin levels
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long half life benzos
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diazepam (valium)
clonazepam (klonopin) chlordiazepoxide (librium) |
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intermediate half life benzos
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lorazepam (ativan)
temazepam (restoril) |
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short half life benzos
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alprazolam (xanax)
oxazepam (serax) triazolam (halcion) |
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buspirone (buspar)
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unrelated to benzos
5HT1A agonist effective in GAD |
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beta blockers for which anxiety disorders
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situational or performance anxiety
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hydroxyzine (vistaril, atarax) and diphenhydramine (benadryl)
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antihistamines used as hypnotics
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sedative antidepressants
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TCAs
trazodone mirtazapine nefazodone |
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adverse effects of stimulants
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exacerbate tics
increased BP tachycardia euphoria/activation/insomnia decreased appetite weight loss |
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atomoxetine (strattera)
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selective NE reuptake inhibitor
tx of adult and child ADHD inability to be an abuse substance |
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effective for adult ADHD
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bupropion (wellbutrin)
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α agonists in behavior disorders
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benefit in ADHD, esp hyperactive/impulsive syxs;
aggression/impulsivity; clonidine guanfacine |
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reversible cholinesterase inhibitors
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donepezil (aricept)
rivastigmine (exelon) galantamine (reminyl) tacrine (cognex) |
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use of reversible cholinesterase inhibitors
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treatment of cognitive dysfunction associated with dementia
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galantamine side effects
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gi side effects pronounced and significant
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rivastigmine side effects
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n/v
anorexia dairrhea (worse than donepezil) |
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memantine (namenda)
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NMDA receptor antagonist;
treat cognitive dysfunction associated with dementia |
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treatment of mild cases of serotonin syndrome
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lorazepam
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treatment of severe cases of serotonin syndrome
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cyproheptadine
propranolol (block actions of serotonin) |
