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75 Cards in this Set
- Front
- Back
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depression results from imbalance of 3 neurotransmitters and 1 receptor
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NE
5HT DA Beta receptors |
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antidep. are ______% bound
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90-95%
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with any heavily bound drug you think about
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drug interactions
ex. warfarin adderall |
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antidepressants metabolized by ______ and the metabolites are excreted by the _______
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liver
kidney (urine) |
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antidepressants usually have ______ half lives
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long
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antidepressants have ________ therapeutic index
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small
-caution with seizures! (antidep. can lower the seizure threshold) |
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classes of antidepressants
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-tricyclics
-SSRIs -SNRIs -MAOIs -atypicals |
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pts can take antidepressants to treat:
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depression, anhedonia (no pleasure), decreased energy, insomnia, hypersomnia, loss of appetite, increased appetite, suicidal thoughts
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many depressed ppl are histrionic, meaning:
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depression takes over thoughts and conversations
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antidepressants are prescribed for affective disorders that are characterized by:
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extreme depression
extreme elation (or both) |
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depression tx usually takes
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2-4 wks, and leads to 85% remission
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tricyclics general action
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inactivate the amine pump on teh presynaptic nerve terminal
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effect of inactivating the amine pump
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limited reuptake of NE and 5HT (therefore increased levels of each)
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tricyclics also have effects on what receptors (which create the SE)
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-muscarinic
-histamine type 1 -alpha 1 |
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two types of tricyclics
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tertiary
secondary |
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tertiary tricyclics are
_______acting and are better at blocking reuptake of ______ |
longer acting
better at serotonin reuptake block (preference to increase serotonin) |
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name 5 tertiary tricyclics
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1. amitryptyline
2. clomipramine 3. doxepin 4. imipramine 5. trimipramine |
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amitryptyline alternate route
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IM
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clomipramine usually given to treat
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OCD
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clomipramine can cause what adverse SE
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seizures (not very selective)
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doxepin side effect
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sedation
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doxepin does NOT have what SE
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cardiovascular
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imipramine alternate route and preparation
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IM
pamoate formulation |
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trimipramine SE
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-very sedating
-anticholinergic |
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secondary tricyclics are
_________acting and are better at blocking ________ |
shorter acting
better at blocking uptake of NE |
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secondary amines tend to be _________ of tertiary amines
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metabolites (the secondary amines are already broken down)
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name five secondary amines
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1. amoxapine
2. desipramine 3. maprotiline 4. nortryptyline 5. protryptyline |
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amoxapine is a metabolite of
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the antipsychotic loxapine
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due to amoxapine being a metabolite of loxapine, it has _______SE
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dopaminergic and adrenergic SE
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desipramine is the metabolite of
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imipramine
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maprotiline risky SE
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seizures
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nortryptyline is a metabolite of
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amitrypryline
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nortryptyline is indicated for what type of patients
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elderly
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protryptyline indicated for what type of pts
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"sleepy" depressives, because it is non sedating
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gen. characteristics of 5HT
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has modulary effects (enhances other neurotransmitters, not alot of primary action by itself)
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serotonin is involved in what activities?
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(MESS):
Mood (increased) Eating (decreased) Sex (decreased) Sleeping (increased) |
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big compliance issues w/ serotonin due to
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decreased libido (happens w/ any age pt)
pt sleepy all day and up all night |
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What SE do you expect to occur with increased NE?
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-increased HR
-increased BP -increased activity -increased alertness -decreased GI motility -pupil dilation (become tolerant to this) |
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tricyclics called "dirty" and "promiscuous" because they
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sit on lots of diff. receptors (muscarinic, histamine, alpha 1)
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muscarinic effects include
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parasympathetic (SLUDE)
Salivation Lacrimation Urination Defecation Emesis |
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so, by blocking muscarinic receptors (like tricyclics do), you will have what SE
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-dry mouth
-dry eyes -urine retention -constipation -antiemetic |
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by blocking alpha effects (like tricyclics do) you will cause what SE
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vasodilation and
ORTHOSTATIC HYPOTEN. (fainting) |
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by blocking histamine effects (like tricyclics do) you will cause what SE
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sedation (think Benadryl, an antihistamine that is also used as a sleep aid)
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can a person w/ depression expect immediate effects?
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no, will usu. take several weeks to get to therapeutic levels, as well as untherapeutic levels
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SSRIs have a safer SE profile than tricyclics. Why?
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they are selective only for serotonin, so none of the BP/fainting effects.
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The SE that the SSRIs do cause include:
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MESS
Mood (increased) Eating (decreased) Sex (decreased) Sleeping (increased) |
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what are the first line drugs for depression?
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SSRIs. Also the second, third, fourth, etc. line. If one doesn't work, try another SSRI.
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name 6 SSRIs
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1. Citaloporam
2. Escitalopram 3. Fluoxetine 4. Paroxetine 5. Sertraline |
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Paroxetine (paxil) noted for what SE
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anticholinergic
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paxil is also approved for what condition
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social phobia
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SNRI (selective norepi reuptake inhibitors) have what general SE profile?
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fewer antimuscarinic effects than the tricyclics and have a more potent adrenergic effects compared to the 5HT effects
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name 3 SNRIs
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1. duloxetine
2. milnacipran 3. venlafaxine |
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which SNRI has produced withdrawals and rebound effects?
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venlafaxine (effexor)
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MAOI general M of A
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inactivate the MAO enzyme which metabolizes NE and 5HT
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MAOIs are usually last resort agents b/c
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they are a crude way to increase levels of both neurotransmitters.
-lowers sz. threshold -dietary restrictions -lots of drug interactions |
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MAOI dietary restrictions:
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any TYRAMINE containing foods
-"party foods" wine cheese peanuts raisins shellfish |
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what happens if you eat tyramine containing food with MAOI?
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hypertensive crisis (body normally contains tyramine but an MAOI causes too much neurotransmitter release)
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MAOI causes increased levels of what neurotransmitters
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NE, 5HT, DA
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name 3 MAOIs
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1. isocarboxazid
2. phenelzine 3. tranylcypromine |
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atypical M of A
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not known, except for bupropion (wellbutrin)
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favorable SE profile w/ atypicals b/c:
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no sexual SE, because no action on 5HT
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name 5 atypical antidepressants
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1. bupropion
2. nefazodone 3. mirtazapine 4. reboxetine 5. trazadone |
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bupropion M of A
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blocks reuptake of
-DA (dopamine) -NE (like cocaine!) |
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bupropion SE
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3x incidence of seizure
stimulant effect |
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potential drug interaction bupropion
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stimulants like adderall or cocaine
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nefazodone primary M of A
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serotonergic mechanisms
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mirtazapine acts at what receptors
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-histamine
-5HT2A -alpha 1 (centrally) -alpha 2 (centrally) |
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mirtazapine most prominant SE
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sedation (histamine)
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trazadone has primarily what receptor action?
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serotonergic
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trazadone has no ________SE due to serotonin receptor action
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no CV or anticholinergic SE
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trazadone adverse SE
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priapism
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which atypical isn't given anymore due to hepatotoxicity?
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nefazodone
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primary adverse effect of all antidepressants?
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sedation
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3 main dangerous adverse effects of antidepressants in general to consider:
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1. CV (orthostatic hypot., antimuscarinic effects at SA node, can unmask sympathetic influences)
2. seizures (lowers sz thresh) 3. blood abnormalities (agranulocytosis, bone marrow depression, thrombocytopenia, eosinophilia) |
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potential drug interactions with antidep. in general
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1. CNS depressants
2. antimuscarinic agents 3. MAOIs 4. sympathomimetics (amphetamine, tyramine, pseudoephedrine, phenylpropanolamine) |
