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Pharm I > Antidepressin > Flashcards

Antidepressin Flashcards

1
Q

Trazodone

Nefazodone

A

5-HT2 antagonists

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2
Q

Trazodone

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

Nefazodone

A

major depressin of disorder

2. received an FDA black box in 2001

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4
Q

Bupropion

A

Unicyclic aminoketone structure

  • CNS activatin properties like amphetamine
  • mid-1990s
  • not related to sexual side effects.
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5
Q

Mirtazapine

A

Tetracyclic

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6
Q

Amoxapine

Maprotiline

A

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

not used as much.

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7
Q

Monoamine oxidase inhibitors MAOIs

A

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

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8
Q

Phenelzine

Tranylcypromine

A

MAOIs

-treatment of depression ureponsive to other antidepressants

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9
Q

Selegiline

A

MAOI

used to treat Parkinson

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10
Q

Hydazine derivative

A

Pheneylzine

Isocarboxazid

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11
Q

Non-hydrazines

A

Tranylcypromine and Selegiline
Moclobemide

Some agents have substantial CNS effects

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12
Q

Vilazodone

Vortioxetine

A

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.

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13
Q

Fluoxetine

A

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.
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14
Q

Fluoxetine

Paroxetine

A

potent inhibitors of the CYP2D6

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15
Q

Fluvoxamine

A

inhibitor of CYP3A4

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16
Q

Citalopram
Escitalopram
Sertraline

A

Only modest CYP interactions

not too much

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17
Q

Vebkafaxine

Desvenlafaxine

A

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.

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18
Q

Duoloxetine

A

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

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19
Q

Milnacipran

Levomilnacipran

A

twice daily

well absorbed

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20
Q

Tricyclic antidepressants

A

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

21
Q

5-HT2 antagonists

A 
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

22
Q

Bupropion

A
  • mean protein binding 85%
  • extensive hepatic metabolic
  • three active metabolites including hydroxybuptopion
  • Biphasic, first phase 1h, second ~14hs
23
Q

Amoxapine

A

dopamine receptor 2 (D2) blocker with antipsychotic effects.

24
Q

Maprotiline

A

well absorbed orally

25
Q

Mirtazapine

A

Half-life 20-40 hours

26
Q

Monoamine oxidase inhibitors

A

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

27
Q

Mechanism of action

A

.

28
Q

SERT

A

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

29
Q

Drugs that block both serotonin and norepinephrine transporters

A 
Newer agents:
venlafaxine
duloexetine
---------
Older group:
tricyclic antidepressants are termed TCAs
30
Q

Venlafaxine

A

weak inhibitor of NET

31
Q

Desvenlafaxine
Duloxetine
Milnacipran

A

more balanced inhibitors of both SERT and NET

32
Q

SNRIs

A

don’t bind to histamines receptors!

-lack potent antihistamine, a-drenergic blocking and anticholinergic effects

33
Q

Milnacipran

Levomilnacipran

A

generally more potent NET than SERT inhibitors

34
Q

TCAs

A

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:

35
Q

5-HT2 antagonists

A

Nefazodone
Trazodone

Mechanism of action:
blockade of the 5-HT2a receptor

36
Q

Nefazodone

A

.MCPP is always at very low concentrations

can cause agonist adverse effects????

37
Q

Trazodone

A

.

38
Q

Tetracyclic & unicyclic antidepressants

A

.

39
Q

Bupropion

A

.

40
Q

Mirtazapine

A

.

41
Q

MAOIs

A 
Mechanism of action:
Forms:
MAOIs classification:
Irreversible, nonselective MAOIs
Reversible and selective inhibitors of MAO-A
Irreversible MAO-B specific agents
42
Q

MAOIs

A 
Mechanism of action:
Forms:
MAOIs classification:
Irreversible, nonselective MAOIs
Reversible and selective inhibitors of MAO-A
Irreversible MAO-B specific agents
43
Q

Irreversible, nonselective MAOIs

A

.

44
Q

Reversible and selective inhibitors of MAO-A

A

.

45
Q

Irreversible MAO-B specific agents

A

.

46
Q

Multimodal serotonergic compounds

A

Vilazodone

Vortioxetine

47
Q

Vilazodone

A

SERT inhibitor and 5-HT1A receptor partial agonist

48
Q

Vortioxetine

A

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

Pharm I (6 decks)

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