Antidepressant Drugs

Question 1

What are the 2 MAOI drugs? Mechanism?

Answer 1

Tranylcypromine, Phenelzine

Irreversibly inhibit both MAOa and MAOb

Question 2

What is the therapeutic use of anti-depressants?

Answer 2

Depression, anxiety, PTSD, chronic pain, enuresis, bulimia, alcoholism

Question 3

What are the side effects of MAOI’s?

Answer 3

Hypertensive crisis (with tyramine-rich foods); serotonin syndrome (MAOI + SSRI); agitation (rare), delerium --> seizures
Anticholinergic, orthostatic hypotension, sexual dysfunction, weight gain, sedation

Question 4

What are the 4 tricyclic Anti-depressants?

Answer 4

Desipramine, Imipramine, Amitriptyline, Nortriptyline

Question 5

What is the mechanism of Amitriptyline, Imipramine and the others in its class?

Answer 5

Block reuptake of NE or 5-HT at varying potencies and selectivity; also variably block muscarinic, a-adrenergic, dopamine, and histamine receptors

Question 6

Which tricyclic antidepressant can also be used for the treatment of tension headaches and migraines?

Answer 6

Amitriptyline (Elavil)

Question 7

What are some side effects of the tricyclic antidepressants?

Answer 7

Sympathomimetic (cardiac arrhythmias and conduction defects, especially at OD)
Antimuscarinic, orthostatic hypotension, sedation (additive with alcohol), seizures
Not very safe; rarely used anymore

Question 8

What is ‘serotonin syndrome’?

Answer 8

caused by combination of SSRI & MAOI
marked increase of serotonin in synapses –> hyperthermia, muscle rigidity, myoclonus, altered mental status, vital signs… potentially lethal

Question 9

What are the 5 SSRI’s?

Answer 9

Fluoxetine (Prozac), Paroxetine (Paxil), Sertraline (Zoloft), Escitalopram (Lexapro), Citalopram (Celexa)

Question 10

What are the 2 SNRI’s?

Answer 10

Duloxetine (Cymbalta), Venlafaxine (Effexor)

Question 11

What are the side effects of SSRI’s? Which 2 are potent potent P450 inhibitors?

Answer 11

Serotonin syndrom (with MAOIs)
Fewer than tricyclics; mostly nausea, decreased sexual function
Fluoxetine and Paroxetine are potent P450 inhibitors

Question 12

What is the mechanism and therapeutic use other than depression of Bupropion? Side effects?

Answer 12

Blocks DA and NE reuptake (only agent with notable selectivity for DA uptake transporter)
maintain nicotine abstinence in quitting smokers
Lowers seizure threshold

Question 13

What is the mechanism of Mirtazapine?

Answer 13

5HT2a antagonists; also inhibit 5HT reuptake

Question 14

What are 3 drugs used to treat Bipolar disease?

Answer 14

Lithium, carbemazepine and valproate

Question 15

What is a possible mechanism of Lithium?

Answer 15

Unknown; lithium depletes secondary messengers IP3 and DAG, important in a-adrenergic and muscarinic-cholinergic transmission

Question 16

What are some side effects of lithium?

Answer 16

Drowsiness, weight gain, tremor, polydipsia, polyuria
Has relatively low margin so elevated levels: neurotoxicity, cardiac toxicity, renal dysfunction (nausea w/vomiting is early warning of OD)