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53 Cards in this Set

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What receptor actions do TCAs have (4)?
5-HT and NE uptake inhibition

Muscarinic antagonism
Histaminergic antagonism
Alpha-adrenergic antagonism
Where are TCAs metabolized?
In the liver
Uses of TCAs include (6)?
UNIPOLAR depression

Schizoaffective disorder
Panic disorder
Agoraphobia

Sleep disorders requiring REM suppression
Adjunctive treatment in chronic pain
@ 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
This is a huge risk w/ TCAs, and is why they're only given out in small amounts
OD

Lethal dose is only 10-20 times a daily dose
What type of TCA is Amitriptyline?
Tertiary
What type of TCA is Imipramine?
Tertiary
Which is the only TCA used to treat OCD?
Clomipramine
What is significant about the receptor action of clomipramine?
Very powerful, SELECTIVE 5-HT uptake inhibition
Which TCA can control cataplexy in narcoleptics?
Clomipramine
Names of the SSRIs we need to know (4)
Fluoxetine
Sertraline
Fluvoxamine
Paroxetine
Where are SSRIs metabolized?
In the liver
What is significant about the urinary excretion of SSRIs?
There is none
Rare side effect of SSRIs?
(Study done on this in kids)
Suicidal ideation
What type of drugs should SSRIs NOT be combined with?

Why?
MAO-Is

Risk of Serotonin Syndrome
What is Serotonin Syndrome?
A toxic accumulation of serotonin

Causes headaches, dizziness, even coma or death
Beyond general uses of SSRIs, what can fluoxetine also be used for?
Cataplexy in narcoleptics
What advantages do SSRIs have when compared to TCAs (2)?
Much larger therapeutic index (less risk of OD)

Much less side effects
What prominent side effect of SSRIs is similar to one seen w/ TCAs?
Sexual side effects
(due to excess 5-HT)
What disadvantages do SRRIs have when compared to TCAs?
LESS effective in severe depression
What receptor action does Reboxetine have?
Blockade of NE uptake
What is the name of the only SNRI we need to know?
Venlafaxine (Effexor)
What receptor action does Buproprion have?
Blocks NE and DA uptake

Has "stimulant-like" effects due to DA
What type of depression is Buproprion most effective in?
That associated w/ psychomotor retardation
What is the major risk when using Buproprion?
It is highly prone to cause seizures
Lowers the seizure threshold significantly
Where is MAO located?
In mitochondria
What is the preferred substrate for MAO-A?
5-HT

Reason for durg interaction w/ SSRIs
Which MAO isoenzyme needs to be inhibited for an anti-depressant effect?
MAO-A
Which isoenzymes of MAO do phenelzine and tranylcypromine inhibit?
BOTH, A and B
Which is more reversible?

Tranylcypromine or Phenelzine
Tranylcypromine
Side effetcs of MAO-Is include (7)?
Euphoria
Weakness
Dry mouth
Blurred vision
Inhibition of ejaculation
Orthostatic hypotension
Dizziness
Phenelzine & traylcypromine are particularly useful treating what?
Atypical depression

NOTE: can also treat narcolepsy
Which isoenzyme of MAO does selegline inhibit?
MAO-B
Through what mechanism does selegline affect Parkinson's disease?
MAO-B deaminates DA
Inhibition of MAO-B --> increased DA
What drugs do MAO-Is have major interactions w/ (4)?
Sympathomimetic amines ("Wine & Cheese Syndrome") [tyramine/ephedrine]
SSRIs (Serotonin Syndrome)
L-Dopa
Meperidine
How long after discontinuation of MAO-Is can Meperidine be used?
Should NOT be used within 2 weeks of discontinuation of MAO-Is
MAO-Is can have a potentially fatal interaction w/ this opiate
Meperidine (Demerol)
What two drugs can be used to manage "Wine & Cheese Syndrome"?
I.V. phenotlamine & I.M. chlorpromazine
(alpha-antagonist properties counter severe hypertension)
How long does Li take to produce an anti-manic effect?
5 - 6 days

Blood levels have to be built up slowly
How does Li interact w/ TCAs (2)?
Can boost the anti-depressant effects of TCAs

In severe polyuria, TCAs can cause urine retention
What drugs can be used during the Lithium "lag period"?
Anti-psychotics or BDZs
How is Li administered?
ONLY orally
What is the CSF concentration of Li relative to the plasma conc.?
Twice the plasma concentration
How is Li eliminated (2)?
By the kidney
Through sweating (5%)
What two approaches can be taken against Li OD?
Osmotic diuretic plus NaHCO3 -- increase excretion

Plasma dialysis (for severe cases)
What cardiac effects does Li have (2)?
QRS widening
T-wave flattening
How does Li affect thyroid hormones?
Decreases both T3 and T4
Can cause goiter (4%)
What are some of the early side effects of Li (5)
TREMOR
GI distress
Weakness
Polyuria
Edema
What drug interactions can Li show (2)?
Thiazide diuretics decrase Li excretion
(Li excretion lowered in conditions of Na reabsorption)

In severe polyuria, TCAs can cause urine retention
What is the Berridge hypothesis?
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
How long does carbamazepine require for symptom relief?
1 - 2 weeks
Which anti-epileptics can be used as mood stabilizers in BPD (2)?
Carbamazepine
Valproic Acid
How long does it take to restore MAO activity after inhibition?
~2 - 3 weeks