Pharmacology - Antidepressants
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- Name some of the tricyclic antidepressants. Which ones are tertiary amines and which are secondary?
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Tertiary = Clomipramine, Amitriptyline, Trimipramine, doxepin
Secondary = Nortriptyline, Protriptyline, desipramine
*CAT NaP - tertiary amines cause sedation, secondary barely do - Name some of the heterocyclic antidepressants. Which are second generation and which are third?
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Second gen: Bupropion, Amoxapine, Trazodone
Third gen: Mirtazapine, Nefazodone, Venlafaxine
*BAT MaN Van - TMN block 5-HT2 receptors - How do tricyclic and heterocyclic antidepressants work?
- they inhibit the reuptake of NE or 5HT
- What receptors do they block that cause side effects?
- muscarinic, histamine, alpha-1, amine reuptake transporters
- What side effects may result?
- anticholinergic, sedation, postural hypotension, tremor/insomnia
- What are the effects of overdosing on a tri/heterocyclic antidepressant?
- convulsions, severe arrhythmias, respiratory depression
- Amoxapine can cause side effects similar to what class of drugs? Why?
- antipsychotics; it is a dopamine receptor antagonist
- What are the uses of tricyclic and heterocyclic antidepressants?
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unipolar and bipolar depression, enuresis, pain syndromes, prophylaxis of migraine, bulimia, diabetic neuropathy, phobias
*i've seen trazodone used for sedation only (tx insomnia) -
Name some SSRIs.
*h for common names -
FLUoxetine, FLUvoxamine, PAroxetine, Sertraline, Citalopram
*ok this is dumb but... Flu! Flu! PASs the vitamin C! - What are the uses of SSRIs?
- depression, panic disorders, OCD, PTSD, bulimia
- What are the side effects of SSRIs?
- behavioral changes, sexual dysfunction, nervousness, nausea, dyspepsia, insomnia, headache
- What is serotonin syndrome and how is it caused?
- hyperthermia, muscle rigidity, myoclonus, rapid changes in vitals and mental status; SSRIs + MAOIs
- How do MAOIs work?
- They increase NE and 5HT by inhibiting their metabolism, resulting in down-regulation of their receptors.
- What do MAOIs have to do with tyramine??
- MAO breaks down dietary tyramine and circulating epinephrine. If someone on MAOIs eats tyramine, it won't be metabolized and could cause severe hypertension and stroke.
- Name three MAOIs.
- phenelzine, tranylcypromine, L-deprenyl (aka seligiline.. MAO-B only)
- What inactivates phenelzine?
- acetylation
- When are MAOIs used?
- depression when tricyclics don't work; phobias, narcolepsy, panic attacks
- What are the side effects of MAOIs?
- restlessness, insomnia, dizziness; orthostatic hypotension at start of tx, constipation, urinary retention, etc
- Our teacher says MAOIs (phenelzine, tranylcypromine, seligiline) are irreversible; which two are reversible?
- moclobemide, clorgyline
- What should you NOT take if you're on an MAOI?
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anything that increases NE (tyramine, tcas, l-dopa, alpha agonists)
anything that increases 5HT (ssri)
opiates
*all of these can be FATAL!! - How does lithium work?
- prevents recycling of phosphoinositides, so no PIP2, so no IP3 or DAG; this diminishes the effects of excess catecholamines or serotonin
- Loss of what ion increases lithium in the body?
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sodium (Na+)
*this means diuretics will increase lithium - When is lithium used?
- acute mania, prevention of manic and depressive episodes in bipolar patients, and alternative to antidepressant therapy
- What are the toxicities of lithium?
- acute intoxication leads to nausea, vomiting, and tremors; late toxicity includes convulsions, coma, and death
- When is lithium contraindicated?
- in pregnancy and breastfeeding
- How is lithium excreted?
- by the kidneys
- What side effects may lithium cause?
- thyroid enlargement, polydipsia, polyuria, and fatigue