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Pharm blk4- SSRI
| Question | Answer |
|---|---|
| what is the prototype SSRI | sertraline (zoloft) |
| what is the first group of depressive symptoms to subside, and how long does this take | neurovegetative symptoms - about two weeks |
| what symptoms were mentioned to be in this group (4) | 1) sleep disturbances; 2) altered appetite; 3) decreased energy; 4) increased anxiety |
| what group of symptoms subsides next, and how long after treatment begins | cognitive symptoms - 4-6 weeks |
| what symptoms were mentioned to be in this group (3) | 1) sadness; 2) hopelessness; 3) poor concentration |
| how do SSRI side effects compare to TCAs and MAOIs | milder |
| what are the main categories of adverse effects that occur with SSRIs (4) | 1) GI; 2) CNS; 3) sexual; 4) weight change |
| what are the most common GI side effects with SSRI | 1) nausea; 2) diarrhea |
| why does nausea occur | 5-HT-3 receptor is in the CTZ |
| what SSRI may have fewer GI side effects | paroxetine |
| what group of side effects does paroxetine have more of than other SSRIs | mild anticholinergic effects |
| what three were mentioned | 1) constipation; 2) urinary retention; 3) dry mouth |
| who should paroxetine be avoided in | patients taking other anticholinergic medication |
| what SSRI is the most activating in the CNS | fluoxetine |
| what are four common CNS side effects of SSRIs | 1) anxiety; 2) tremors; 3) insomnia; 4) extrapyramidal |
| what AE are activating SSRIs especially likely to cause | insomnia |
| what coincides with lessening of sleep disturbances/insomnia | sleep improves when depression subsides |
| in what patients are activating SSRIs desirable (1) and undesirable (2) | desirable in patients without energy, undesirable in patients complaining of: 1) too much anxiety; 2) lack of sleep |
| what SSRI has the highest propensity for extrapyramidal side effects | paroxetine |
| what is the incidence of sexual dysfunction with SSRIs, and in what sex is this most common | 30-50%, most common in men |
| what sexual side effects happen in males (2) | 1) delayed ejaculation; 2) lack of orgasm |
| what sexual side effects happen in females (3) | 1) decreased libido; 2) orgasm trouble; 3) lack of lubricaiton |
| what SSRI causes the most sexual dysfunction | paroxetine |
| what other sexual adverse effect can happen in both sexes | emotional blunting of feelings of romance |
| what may be the mechanism for this | excess 5-HT nonselectively taken up into DA terminals - 5-HT hijacking DA signaling in the brain |
| what other feelings are affected by emotional blunting (3) | 1) less ability to become angry; 2) less ability to care about others feelings; 3) less ability to feel pleasure |
| what generally happens to weight with SSRIs, and how does this compare to TCAs and MAOIs | weight is gained, but less than with TCA or MAOI |
| what SSRI causes the most weight gain | paroxetine |
| so, what side effects does paroxetine cause more than other SSRIs (4) | 1) GI; 2) extrapyramidal; 3) sexual dysfunction; 4) weight gain |
| what is the leading cause of noncompliance with SSRIs | sexual dysfunction |
| what are the underlying mechanisms that cause sexual dysfunction (2) | 1) postsynaptic stimulation of 5-HT2 receptors; 2) decreased sympathetic stimulation |
| is sexual dysfunction generally transient or does it persist | typically transient, but can persist |
| what SSRI has the least sexual side effects | escitalopram (lexapro) |
| what other drugs have low sexual side effects, and what MOA is each | 1) bupropion (SDRI); 2) mirtazapine (blocks presynaptic alpha-2 receptors); 3) nefazadone (blocks postsynaptic 5-HT2A receptors |
| what are the three stages in antidepressant therapy | 1) acute; 2) continuation; 3) maintenance |
| how long is the acute phase, and what is the goal | about 12 weeks, goal to induce remission |
| what is the goal of step two (continuation), and how long does it last (range) | keep in remission - lasts 4-9 months |
| what is the minimum duration for stages 1 + 2 | 7 months |
| how long must stage 3 last | stage 3 is not for all patients |
| what happens to the risk for depression in pregnancy, and what % of women have depression during pregnancy | risk increases, 10% of women have depression during pregnancy |
| what % of women who stop therapy early in pregnancy suffer relapse by the third trimester | 50%; 68% total relapse rate given in next slide for women who discontinue treatment |
| what is the relapse rate during pregnancy for women who maintain meds | 26% |
| does SSRI cross into the fetus, or into breast milk | yes |
| what is SSRI concentration in fetal brain compared to mother | 85% |
| what is SSRI use in pregnancy associated with | 1) lower birth weight (0.5 lb); 2) persistent pulmonary hypertension of the newborn (associated with late/3rd trimester use) |
| what are the long term developmental consequences | unknown |
| so, which groups of ADs were mentioned to be safe and effective in pregnancy (2), but with what caveat | 1) TCAs; 2) SSRIs - although increased short-term neonatal adverse effects after exposure to ADs in 3rd trimester can occur |
| which class (SSRIs or TCAs) has a more favorable side-effect profile | SSRIs |
| what should be done during discontinuation of antidepressants (what reduction per time, and how long between reductions) | slow taper - reduce dose by 25% per week |
| what exception is there, and why | unnecessary for fluoxetine - long half life |
| when is there tolerance or drug-seeking behavior | there is not |
| what symptoms were listed under "discontinuation syndrome" (list) | dizziness, vertigo, ataxia, parasthesia, numbness, electric-shock-like sensations, lethargy, headache, tremor, sweating, anorexia, insomnia, nightmares, excessive dreaming, nausea, vomiting, diarrhea, irritability, anxiety/axitation, low mood |
| what type of drug interactions do SSRIs have | P-450 |
| what P450 enzymes were mentioned (3) | 1) 3A4; 2) 2D6; 3) 2C9 |
| what SSRI was mentioned to have the greatest effect on P450s | fluoxetine |
| what SSRI has the least effect on P450s | sertraline (zoloft) |
| what drugs were SSRIs specifically said to be able to result in elevated levels of (2 classes, 1 example from each) | 1) benzodiazepenes (diazepam/valium); 2) anti-seizure (phenytoin) |
| what should SSRIs never be used with, and why | MAOIs - can precipitate 5-HT syndrome |
| what four symptoms were mentioned in this lecture for 5-HT (serotonin) syndrome | 1) agitation; 2) hypertension; 3) confusion; 4) fever |
| what are the two options for switching medications (and trying to avoid serotonin syndrome) | 1) immediate substitution; 2) cross-taper (introduction of new drug while tapering dosage of the first) |
| when switching medications, for what kinds of medications is it typically ok to use immediate substitution | one SSRI for another |
| what exception is there, and why | should stop fluoxetine for a few days to a week before introducing another SSRI, because of its long half life |
Created by:
mcafej02
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