Antidepressants Flashcards
Which class of antidepressants are used for treatment of neuropathic pain and other pain disorders?
TCAs
What enzyme degrades tyramine and why is this a problem?
MAO - people on MAOIs who eat cheese, soy, or wine can have lethal side effects of excess tyramine - excess catecholamines leading to HTN/stroke
Name the 4 MAOIs
Isocarboxazid
Phenelzine
Tranylcypromine
Selegiline
Rarely prescribed now
What is the method of action of TCAs?
What are common side effects and why?
Block SERT and NET, but also block alpha cholinergic, muscarinic, histamine, and 5-HT
Alpha block: orthostatic hypotension
Anti muscarinic: blurred vision, constipation, dry mouth
H1 block: sedation and weight gain
5-HT block: sexual dysfunction
Increased catecholamines can also cause cardiac overstimulation and can also slow cardiac conduction leading to arrhythmias
Which class of antidepressant drug requires close monitoring of suicidal patients?
TCAs
Which class of antidepressant can lead to conduction block and how do you treat it?
TCAs
With sodium bicarbonate
Which two TCAs are known to have string anti muscarinic effects?
Amitriptyline and imipramine
Which TCA has strong SERT effects but little NET effects?
Clomipramine
Which TCA is strongly associated with sexual dysfunction? Why?
Clomipramine
Strong SERT effects cause sexual dysfunction
Which TCA has strong NET effects?
Nortriptyline
Which TCA is least sedating?
Desipramine
What class of drug is the DoC for depression?
SSRIs
Selective serotonin reuptake inhibitors
What class of antidepressants is the DoC for treatment of anxiety disorders?
SSRIs
Selective serotonin reuptake inhibitors
What disorder can TCAs treat but not SSRIs?
Chronic pain
Which class of antidepressants can treat enuresis? What is it? Why aren’t they commonly prescribed for this indication?
TCAs
Enuresis: involuntary urine voiding
Too many side effects
What are the effects of overdose of SSRIs?
Can cause seizures RARELY fatal
Name the 7 TCAs
Clomipramine Imipramine Nortriptyline Amoxapine Maprotiline Amitriptyline Desipramine
Which SSRI inhibits 3 different CYPs and has a high potential for drug interactions?
Fluvoxamine
Which two antidepressants treat PMS/PMDD? What class?
Fluoxetine and sertraline
SSRIs
Which antidepressant treats bulimia? What class?
Fluoxetine
SSRI
Which SSRI is strongly associated with weight gain?
Paroxetine
What is the only SSRI associated with NE blocking effects?
Paroxetine
Which three SSRIs have low potential for drug interactions?
Citalopram Escitalopram and Sertraline
Blockage of reuptake of what two compounds can be effective in pain management?
NE and 5-HT
What is the difference in effect in stimulating 5HT1A and 5HT2 receptors?
(+) 5HT1A: helps depression
(+) 5HT2: causes agitation, anxiety, and sexual dysfunction
Which SSRIs inhibit CYP2D6 and have high potential for drug interactions?
Fluoxetine and paroxetine
Patient presents with hyperthermia, muscle rigidity, and myoclonus. What is the name of this condition and what causes it?
Serotonin syndrome
Occurs when giving a MAOI + any serotonin reuptake inhibitor like SSRI, SNRI, TCA, or meperidine (opioid analgesic)
Describe the Monoamine hypothesis of depression
Decreases levels of dopamine, serotonin, or NE can cause depression. MAOIs treat it, but the drugs act immediately but the clinical effects are not seen for weeks (something else is going on)
What drugs do you use to treat depression if SSRIs are ineffective? MOA?
SNRIs - serotonin and NE reuptake inhibitors
Block SERT and NET (like TCAs but dont affect the other receptors)
Which drug treats fibromyalgia? Name and class?
Duloxetine - SNRI
Which SNRI blocks both SERT and NET at all doses?
Duloxetine
Which SNRI blocks NET only at high doses?
Venlafaxine
Name the 6 SSRIs
Citalopram Escitalopram Fluoxetine Fluvoxamine Paroxetine Sertraline
Which SNRI has no sedative effects?
Venlafaxine
Name the 2 SNRIs
Venlafaxine
Duloxetine
What is the advantage of using SNRIs over SSRIs?
SNRIs have fewer CYP interactions
Name the 1 NDRI
Bupropion
Which antidepressant treats diabetic neoropathy? Name and class
Duloxetine - SNRI
Which antidepressant can be used to stop smoking? Name and class. MOA?
Bupropion
NDRI - NE and dopamine reuptake inhibitors
Block reuptake of NE and dopamine and also increase their release
Which class of antidepressant is LEAST effective in treating anxiety?
NDRI
Which hormone affected by antidepressants leads to sexual dysfunction? Which class of antidepressants doesn’t have this side effect?
Serotonin
NDRIs
Which class of antidepressant blocks serotonin reuptake but also prevents agitation, anxiety, and sexual dysfunction? How?
SARIs - 5HT2 antagonist/reuptake inhibitors
5HT blockage treats depression
Blockage of 5HT2 prevents the side effects
Which SARI is associated with hepatotoxicity and is no longer commonly prescribed?
Nefazodone
Overdose of bupropion causes what symptoms?
Seizures
Which antidepressant is used to treat insomnia? Drug and class
Trazodone - SARI
Used as a hypnotic
Name the two SARIs
Nefazodone
Trazodone
Wich antidepressant has priapism as an AE? Drug and class?
Trazodone - SARI
Which class of antidepressants is NOT a reuptake inhibitor? MOA?
NASSAs - noradrenergic and specific serotonergic antidepressants
Antagonist at presynaptic alpha2 receptors (this leads to inc release of NE and 5HT) but also antagonist at 5HT2 and 5HT3 and H1 (sedation and wt gain) receptors
Antagonism at H1 receptors is associated with what to side effects?
Sedation and wt gain
Name the 1 NASSA - what is special about this drug amongst antidepressants?
Mirtazapine - NOT a reuptake inhibitor
DoC for bipolar disorder? MOA?
Lithium
Inositol depletion theory: Gq activates PLC which cleaves PIP2 to DAG and IP3. IP3 inactivated to IP2 which is degraded to IP1 to inositol to PI and back to PIP2.
Lithium blocks IP2 -> IP1 AND IP1 -> inositol which stops signaling cascade in brain
Noncompetitive inhibitor though so only works at active receptors
Which drug used to treat bipolar disorder has a narrow therapeutic index and must be titrated?
Lithium - double the dose can cause death
Pt with bipolar disorder has tremor. What drug is he on?
Lithium
How is lithium delivered and what needs to be monitored?
Rapidly absorbed orally and plasma levels of drug need to be monitored.
What two drugs are common substitutes for lithium in treatment of bipolar disorder? What class of drugs are they?
Valproate and carbamazepine
Antiepileptics
What bipolar medication requires monitoring of liver function tests?
Valproate - antiepileptic
Which bipolar drug requires monitoring of CBC?
Carbamazepine - antiepileptic
Which bipolar drug can lead to neural tube defects?
Valproate - antiepileptic
What two atypical antipsychotics can be used to treat bipolar pts?
Olanzapine and atripiprazole
What three atypical antipsychotics can be used to treat acute mania or mixed episodes?
Quetiapine
Risperidone
Ziprasidone
What antiepileptic can be used in maintainence treatment for bipolar pts?
Lamotigine
Pt with bipolar disorder develops diabetes insipidus and acneiform skin lesions. What drug is he on?
Lithium
Common side effects of lithium?
Confusion, motor impairment, tremor (most people develop this), sedation, ataxia, aphasia
Which drug used to treat bipolar patients leads to severe cardiac problems in the child if used during pregnancy?
Lithium
- ipramine and - triptyline are common endings of what class of drug?
TCAs