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53 Cards in this Set
- Front
- Back
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What receptor actions do TCAs have (4)?
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5-HT and NE uptake inhibition
Muscarinic antagonism Histaminergic antagonism Alpha-adrenergic antagonism |
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Where are TCAs metabolized?
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In the liver
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Uses of TCAs include (6)?
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UNIPOLAR depression
Schizoaffective disorder Panic disorder Agoraphobia Sleep disorders requiring REM suppression Adjunctive treatment in chronic pain |
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@ THERAPEUTIC doses, main side effects of TCAs include (8)?
(Think about response to each receptor activity) |
Sedation
Insomnia Restlessness Fine tremor Sexual side effects Orthostatic hypotension Cholinergic blockade Weight gain |
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This is a huge risk w/ TCAs, and is why they're only given out in small amounts
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OD
Lethal dose is only 10-20 times a daily dose |
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What type of TCA is Amitriptyline?
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Tertiary
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What type of TCA is Imipramine?
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Tertiary
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Which is the only TCA used to treat OCD?
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Clomipramine
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What is significant about the receptor action of clomipramine?
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Very powerful, SELECTIVE 5-HT uptake inhibition
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Which TCA can control cataplexy in narcoleptics?
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Clomipramine
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Names of the SSRIs we need to know (4)
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Fluoxetine
Sertraline Fluvoxamine Paroxetine |
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Where are SSRIs metabolized?
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In the liver
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What is significant about the urinary excretion of SSRIs?
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There is none
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Rare side effect of SSRIs?
(Study done on this in kids) |
Suicidal ideation
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What type of drugs should SSRIs NOT be combined with?
Why? |
MAO-Is
Risk of Serotonin Syndrome |
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What is Serotonin Syndrome?
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A toxic accumulation of serotonin
Causes headaches, dizziness, even coma or death |
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Beyond general uses of SSRIs, what can fluoxetine also be used for?
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Cataplexy in narcoleptics
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What advantages do SSRIs have when compared to TCAs (2)?
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Much larger therapeutic index (less risk of OD)
Much less side effects |
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What prominent side effect of SSRIs is similar to one seen w/ TCAs?
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Sexual side effects
(due to excess 5-HT) |
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What disadvantages do SRRIs have when compared to TCAs?
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LESS effective in severe depression
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What receptor action does Reboxetine have?
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Blockade of NE uptake
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What is the name of the only SNRI we need to know?
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Venlafaxine (Effexor)
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What receptor action does Buproprion have?
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Blocks NE and DA uptake
Has "stimulant-like" effects due to DA |
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What type of depression is Buproprion most effective in?
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That associated w/ psychomotor retardation
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What is the major risk when using Buproprion?
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It is highly prone to cause seizures
Lowers the seizure threshold significantly |
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Where is MAO located?
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In mitochondria
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What is the preferred substrate for MAO-A?
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5-HT
Reason for durg interaction w/ SSRIs |
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Which MAO isoenzyme needs to be inhibited for an anti-depressant effect?
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MAO-A
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Which isoenzymes of MAO do phenelzine and tranylcypromine inhibit?
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BOTH, A and B
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Which is more reversible?
Tranylcypromine or Phenelzine |
Tranylcypromine
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Side effetcs of MAO-Is include (7)?
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Euphoria
Weakness Dry mouth Blurred vision Inhibition of ejaculation Orthostatic hypotension Dizziness |
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Phenelzine & traylcypromine are particularly useful treating what?
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Atypical depression
NOTE: can also treat narcolepsy |
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Which isoenzyme of MAO does selegline inhibit?
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MAO-B
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Through what mechanism does selegline affect Parkinson's disease?
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MAO-B deaminates DA
Inhibition of MAO-B --> increased DA |
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What drugs do MAO-Is have major interactions w/ (4)?
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Sympathomimetic amines ("Wine & Cheese Syndrome") [tyramine/ephedrine]
SSRIs (Serotonin Syndrome) L-Dopa Meperidine |
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How long after discontinuation of MAO-Is can Meperidine be used?
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Should NOT be used within 2 weeks of discontinuation of MAO-Is
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MAO-Is can have a potentially fatal interaction w/ this opiate
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Meperidine (Demerol)
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What two drugs can be used to manage "Wine & Cheese Syndrome"?
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I.V. phenotlamine & I.M. chlorpromazine
(alpha-antagonist properties counter severe hypertension) |
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How long does Li take to produce an anti-manic effect?
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5 - 6 days
Blood levels have to be built up slowly |
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How does Li interact w/ TCAs (2)?
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Can boost the anti-depressant effects of TCAs
In severe polyuria, TCAs can cause urine retention |
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What drugs can be used during the Lithium "lag period"?
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Anti-psychotics or BDZs
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How is Li administered?
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ONLY orally
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What is the CSF concentration of Li relative to the plasma conc.?
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Twice the plasma concentration
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How is Li eliminated (2)?
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By the kidney
Through sweating (5%) |
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What two approaches can be taken against Li OD?
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Osmotic diuretic plus NaHCO3 -- increase excretion
Plasma dialysis (for severe cases) |
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What cardiac effects does Li have (2)?
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QRS widening
T-wave flattening |
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How does Li affect thyroid hormones?
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Decreases both T3 and T4
Can cause goiter (4%) |
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What are some of the early side effects of Li (5)
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TREMOR
GI distress Weakness Polyuria Edema |
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What drug interactions can Li show (2)?
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Thiazide diuretics decrase Li excretion
(Li excretion lowered in conditions of Na reabsorption) In severe polyuria, TCAs can cause urine retention |
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What is the Berridge hypothesis?
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Explanation of Li's effects
Li inhibits IP1 and IP2 recycling Ultimately, Li inhibits PIP2 stores The effects of hormones that act via PLC are diminished |
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How long does carbamazepine require for symptom relief?
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1 - 2 weeks
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Which anti-epileptics can be used as mood stabilizers in BPD (2)?
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Carbamazepine
Valproic Acid |
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How long does it take to restore MAO activity after inhibition?
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~2 - 3 weeks
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