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PHARMACOKINETICS
TDM
ACUTE MANAGEMENT
MIXED BAG
ENDS WITH mg
100
The half-life of all of the SSRIs except fluoxetine (Prozac).
What is 15-30 hrs. Fluoxetine's half-life is 2-4 days & the metabolite norfluoxetine's half-life is 7-15 days. [pg 217]
100
The three groupings of patients related to their ability to clear TCAs.
What are normal or extensive metabolizers (90% of pts), poor metabolizers (5-10% of pts, genetically deficient in 2D6), and ultrarapid metabolizers (0.5% of pts). [pg 222]
100
The definitions of response rate and remission rate.
What is 50% or greater reduction in baseline sxs (response) and a decrease in symptoms below a pre-determined cutoff score (remission). [pg 226]
100
This class of medications may improve both depression and panic disorder when the depression is secondary to the panic disorder, but can cause depression in some people.
What are benzodiazepines. [pg 243]
100
Celexa is titrated from this starting dose to this usual effective dose.
What is 20mg/day to 40mg/day. [pg 250]
200
These P450 enzymes metabolize citalopram/escitalopram (Celexa/Lexapro), fluvoxamine (Luvox), fluoxetine (Prozac), paroxitine (Paxil), and sertraline (Zoloft).
What are 2C19 & 3A4, 1A2, 2D6, 2D6 (low concentrations) & 3A4 (high concentrations), 3A4 & 2C19 & 2C9 & 2D6 & 2B6. [pg 217]
200
A non-TCA antidepressant that may benefit from TDM.
What is Bupropion. This medication has a dose-dependent increased risk of seizures, the seizures tend to occur within days of a dosage change and within hours of the last dose, and are more likely in people with low BMI. [pg 223]
200
The definition of a flat dose-response curve.
There is no advantage in increasing the dose above the usually effective minimum dose. Usual effective doses for SSRIs are Celexa 40mg/day, Lexapro 20mg/day, Prozac 20mg/day, Paxil 20mg/day, Zoloft 50mg/day. [pg 228]
200
This neutraceutical is an effective reuptake pump inhibitor for serotonin, dopamine, and norepinephrine, but causes significant induction of CYP 3A4.
What is St. John's Wort (hypericum). [pg 246-247]
200
You can start at this therapeutic dose of Effexor.
What is 75mg/day. Effexor has an ascending dose-response curve, so increasing the dose above the usually effective dose (75mg) dose produce increased antidepressant effects. [pg 251]
300
The half-life of venlafaxine (Effexor), desvenlafaxine (Pristiq), and duloxetine (Cymbalta).
5 hours for Effexor, 11 hours for Pristiq, and 8-17 hrs for Cymbalta. [pg 218]
300
The recommended way to get an accurate TCA plasma level.
1 week after initiating a standard TCA dose most pts are at a steady state. A trough blood sample is then drawn 10-12 hrs after the last dose.
300
Targeting this combination of receptors has shown a more rapid onset of antidepressant action than either alone.
What are combined NE and 5HT reuptake inhibitors (eg, Effexor & Cymbalta). [pg 231]
300
A naturally occurring substance that shows efficacy comparable with TCAs for treatment of depression.
What is SAMe. This has been shown to be effective (dose range 200-1600 mg/day) for MDD but has precipitated mania in bipolar pts. [pg 248]
300
The starting dose of Selegiline patch, phenelzine, tranylcypromine, and moclobemide.
What is 20mg/day, 15mg BID, 10mg BID, 100-200mg TID. [pg 252]
400
This drug ismetabolized by oxidation as well as P450 2B6, and has a half-life of 8-10 hrs.
What is Bupropion (Wellbutrin). It is metabolized into 3 active metabolites, all of which have half-lives of 24 hrs or more. [pg 220]
400
The blood level above which there is significantly increased risk of both CNS and cardiac toxicity.
What is 450 ng/ml. [pg 224]
400
This class of antidepressants may be "cleaner" in terms of more specific serotonin receptor targeting.
What is triazolopyridines (nefadozone & trazodone). These medications agonize 5HT-1A receptors while antagonizing (blocking) 5HT-2A, thus decreasing the adverse SE while promoting the antidepressant effects. [pg 235]
400
This 5HT-1A partial agonist was studied for efficacy as an antidepressant but was not found to be superior to placebo.
What is Buspirone (Buspar). [pg 245]
400
The usual doses & titration schedule for imipramine.
25mg TID, increasing by 25mg/day every 2-3 days as tolerated, with a goal of achieving a total daily dose of 150mg by the end of the first week. [pg 252]
500
The principle pathway for TCA elimination (after undergoing first-past metabolism).
What is aromatic hydroxylation via CYP 2D6. TCAs are metabolized by three oxidative pathways: N-demethylation (1A2, 2C19, 3A4), N-oxidation (2D6), and aromatic hydroxylation (2D6). The first-pass metabolism is mediated via 3A4.
500
The symptoms of TCA CNS toxicity.
First, an increase in affective symptoms (low mood, poor concentration, social withdrawal, lethargy). Next ataxia and tremor develop, then psychotic sxs. The final stage is delirium +/- seizures. [pg 224]
500
This class of medications may be preferable in atypical depressions, or when other agents have failed.
What are MAOIs. [pg 240]
500
This medication may improve symptoms in apathetic, senile geriatric pts.
What is methylphenidate. [pg 242]
500
Be cautious not to exceed these amounts per dosage in order to decrease the risks of adverse effects.
For Bupropion: do not exceed 150mg IR or 200mg SR for any individual dose and doses should be at least 4 hours apart to decrease the risks of seizures. [pg 251] For TCAs: 150-200mg per dose, and divided doses are recommended for elderly, very young, or medically ill pts. [pg 252]