Antidepressin

Question 1

Trazodone

Nefazodone

Answer 1

5-HT2 antagonists

Question 2

Trazodone

Answer 2

1. Hypnotic
2. structure has a trizolo moiety
   3.

Question 3

Nefazodone

Answer 3

major depressin of disorder

2. received an FDA black box in 2001

Question 4

Bupropion

Answer 4

Unicyclic aminoketone structure

• CNS activatin properties like amphetamine
• mid-1990s
• not related to sexual side effects.

Question 5

Mirtazapine

Answer 5

Tetracyclic

Question 6

Amoxapine

Maprotiline

Answer 6

tetracyclic
amoxapine is the N-methylated metabolic of loxapine
share structural similarities and side effects comparable to the TCAs.

not used as much.

Question 7

Monoamine oxidase inhibitors MAOIs

Answer 7

get therapeutic effects
introduced in 1990s.
not used as much.
toxicity and lethal effect and drug interactions

Question 8

Phenelzine

Tranylcypromine

Answer 8

MAOIs

-treatment of depression ureponsive to other antidepressants

Question 9

Selegiline

Answer 9

MAOI

used to treat Parkinson

Question 10

Hydazine derivative

Answer 10

Pheneylzine

Isocarboxazid

Question 11

Non-hydrazines

Answer 11

Tranylcypromine and Selegiline
Moclobemide

Some agents have substantial CNS effects

Question 12

Vilazodone

Vortioxetine

Answer 12

Multimodal serotonergic compounds

• SERT inhibitors
• BOTH HAVE RAPID ONSET
• both have partial agonist effects on 5-HT1A

vortioxetine has partial agonist at 5-HT1A, 5-HT1B and antagonist at 5-HT3, 5-HT7

Both are approved for MDD
possibly fewer side effects.

Question 13

Fluoxetine

Answer 13

very different from other SSRI drugs.

• metabolized to an active product Norfluoxetine:
  
  • have a methyl group within it.
• have the LONGEST HALF-LIFE. need to be very careful in terms of MAOI
• has to be discontinued 4 weeks or longer.
• minimizes the risk of serotonin syndrome.

Question 14

Fluoxetine

Paroxetine

Answer 14

potent inhibitors of the CYP2D6

Question 15

Fluvoxamine

Answer 15

inhibitor of CYP3A4

Question 16

Citalopram
Escitalopram
Sertraline

Answer 16

Only modest CYP interactions

not too much

Question 17

Vebkafaxine

Desvenlafaxine

Answer 17

HL~1 hr. once a day dosing
both have the lowest protein binding
-Desvenlafaxine is extreted 45% unchanged in the urine (conjugated), venlafaxine is 4-8% unchanged in the urine.

Question 18

Duoloxetine

Answer 18

extensive oxidative metabolism
CYP2D6 and CYP1A2
hepatic impairment significantly alters duoloxetine levels unlike desvenlafaxine

Question 19

Milnacipran

Levomilnacipran

Answer 19

twice daily

well absorbed

Question 20

Tricyclic antidepressants

Answer 20

well absorbed
long half-lives
does only daily at NIGHT because of their sedating effects
extensive metabolism:
TCA levels can affect fluoxetine.
substrate of the CYP2D6 system. genetic polymorphism for CYP2D6

*Desipramine and Nortriptyline

Question 21

5-HT2 antagonists

Answer 21

Trazodone
Nefazodone
-rapidly absorbed
-hepatic metabolism
-limited bioavailability because of extensive metabolism
-often a single night dose, low dose

Nefazodone is a potent inhibitor of CYP3A4

Question 22

Bupropion

Answer 22

• mean protein binding 85%
• extensive hepatic metabolic
• three active metabolites including hydroxybuptopion
• Biphasic, first phase 1h, second ~14hs

Question 23

Amoxapine

Answer 23

dopamine receptor 2 (D2) blocker with antipsychotic effects.

Question 24

Maprotiline

Answer 24

well absorbed orally

Question 25

Tetracyclic and unicyclic agents -------------- Mirtazapine

Answer 25

Half-life 20-40 hours

Question 26

Monoamine oxidase inhibitors

Answer 26

different MAOIs are metabolized via different pathways -tend to have extentsive first-pass effects -may substantially decrease bioavailability -------------------- alternative routes of administration are being developed selegiline is available in both transdermal and sublingual form

Question 27

Mechanism of action

Answer 27

.

Question 28

SERT

Answer 28

transmembrane in axon terminals 12 transmemb region?? -transport Na+, Cl- and serotonin into the cell and bind to intracellular K+ results in return of the transporter to its original conformation -serotonin released inside cell -binding to the serotonin transporter causes tonic inhibition of the dopamine system

Question 29

Drugs that block both serotonin and norepinephrine transporters

Answer 29

``` Newer agents: venlafaxine duloexetine --------- Older group: tricyclic antidepressants are termed TCAs ```

Question 30

Venlafaxine

Answer 30

weak inhibitor of NET

Question 31

Desvenlafaxine Duloxetine Milnacipran

Answer 31

more balanced inhibitors of both SERT and NET

Question 32

SNRIs

Answer 32

don't bind to histamines receptors! | -lack potent antihistamine, a-drenergic blocking and anticholinergic effects

Question 33

Milnacipran | Levomilnacipran

Answer 33

generally more potent NET than SERT inhibitors

Question 34

TCAs

Answer 34

bind to a lot of different receptors potent to SERT ---------------- Imipramine has more serotonin effects initially -Can have later balanced effects with more NET inhibition ----------- common adverse effects:

Question 35

5-HT2 antagonists

Answer 35

Nefazodone Trazodone Mechanism of action: blockade of the 5-HT2a receptor

Question 36

Nefazodone

Answer 36

.MCPP is always at very low concentrations | can cause agonist adverse effects????

Question 37

Trazodone

Answer 37

.

Question 38

Tetracyclic & unicyclic antidepressants

Answer 38

.

Question 39

Bupropion

Answer 39

.

Question 40

Mirtazapine

Answer 40

.

Question 41

MAOIs

Answer 41

``` Mechanism of action: Forms: MAOIs classification: Irreversible, nonselective MAOIs Reversible and selective inhibitors of MAO-A Irreversible MAO-B specific agents ```

Question 42

MAOIs

Answer 42

``` Mechanism of action: Forms: MAOIs classification: Irreversible, nonselective MAOIs Reversible and selective inhibitors of MAO-A Irreversible MAO-B specific agents ```

Question 43

Irreversible, nonselective MAOIs

Answer 43

.

Question 44

Reversible and selective inhibitors of MAO-A

Answer 44

.

Question 45

Irreversible MAO-B specific agents

Answer 45

.

Question 46

Multimodal serotonergic compounds

Answer 46

Vilazodone | Vortioxetine

Question 47

Vilazodone

Answer 47

SERT inhibitor and 5-HT1A receptor partial agonist

Question 48

Vortioxetine

Answer 48

SERT inhibitor, partial agonist (5-HT1a and 5-HT1b) and antagonist (5-HT3, 5-HT7)