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Pharmacology > Antidepressants, Anxiolytics, Mood Stabilizers > Flashcards

Antidepressants, Anxiolytics, Mood Stabilizers Flashcards

1
Q

Which NTs modulate mood, sleep-wake cycle, motivation, and pain perception?

A

NE

5HT

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2
Q

Basic A.A. of 5HT:

A

Tryptophan

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3
Q

Once 5HT is released into the synapse it does 1 of what 3 things?

A
  1. Bind to autoreceptor (5HT1D rc) present on the neuron that released the 5HT= negative feedback
  2. Reuptaken into the neuron to be repackaged into the vesicle or broken down by MAO
  3. Bind to post-synaptic rc
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4
Q

Basic A.A. building block for NE is:

A

Tyrosine, via dopamine

Tyrosine –> L-dopa –>Dopa–>synaptic vessicle–>NE

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5
Q

Once NE is released into the synapse it does 1 of what 3 things?

A
  1. Bind to autoreceptor (adrenergic, a2rc)
  2. Reuptaken and repackaged or broken down by MAO
  3. Binds to post-synaptic rc
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6
Q

Depression in a result of a decrease in what two NTs?

A

Serotonin and/or NE

simplified, immediate increase of NTs does not always alleviate depression

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7
Q

Generally how long is needed for an anti-depressant to have full effect and what could this be d/t?

A

About 1 month

At first autoreceptors may result in balance

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8
Q

Increased 5HT results in:

A

Increased appetite, improved sleep, improved mood (typical symptoms)

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9
Q

Which receptor of serotonin is thought to be specifically linked to mood?

A

5HT1a

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10
Q

On target SE of increased 5HT include:

A

5HT2 rc=increased anxiety, jitteriness, sexual dysfunction, sleep disturbances (initially)
5HT3 rc= nausea, diarrhea

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11
Q

Off target SE of increased 5HT include:

A

H1 rc: sedation, weight gain
M1 : anticholinergic, dry mouth, blurred vision, constipation
alpha1 rc: vasodilation, hypotension, orthostasis

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12
Q

Increased NE results in:

A

Increased interest, energy, concentration(cognition), and mood

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13
Q

SE of NE include:

A

(On target)

Increased BP, HR, anxiety

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14
Q

What drug typically prescribed for HTN inhibits packaging of NTs and can cause depression?

A

Reserpine

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15
Q

MAOI’s MOA:

A

Inhibition of MAO causes increased availability of NE and 5HT

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16
Q

What is an important AE of MAOI’s?

A

Tyramine toxicity, via inhibition of GI and hepatic MAO which is responsible for tyramine metabolism. Tyramine can displace catecholamines and lead to a hypertensive crisis.

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17
Q

How can the major AE of MAOI’s be avoided?

A

Tyramine restricted diet. Decreased processed meats, cheese, red wine

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18
Q

Non-selective, irreversible MAOI’s include:

A

Phenelzine(Nardil)

Isocarboxazid (Marplan)

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19
Q

Non-selective reversible MAOI’s include:

A

Tranylcypromine (Parnate)

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20
Q

Selective MAO-A inhibitors (RIMA):

A

Meclobemide
Befloxatone
Brofaromine

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21
Q

Selective, irreversible MAO-B inhibitors:

A

Selegiline

Rasagiline

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22
Q

Which NTs do MAO-A and MAO-B inhibitors, inhibit breakdown of?

A

MAO-A: epi, NE, 5HT

MAO-B: dopamine

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23
Q

Which MAOI is available in a transdermal patch and used more often for Parkinson’s?

A

Selegiline

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24
Q

Which MAOI has a decreased risk of tyramine toxicity d/t to its avoiding the GI tract and how?

A

Selegiline

Transdermal patch avoids GI tract and first pass metabolism

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25
Q

PK of MAOIs: Absorption, Metabolism, DI

A
  • Well absorbed
  • Lipophilic easily crosses BBB
  • Hepatically metabolized to active metabolites that are inactivated in the liver and excreted by the kidneys
  • CYP450 reactions that usually increase levels of MAOI
  • DI with TCAs, SSRI, pseudoephedrine, dextromethorphan
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26
Q

TCAs: secondary amines- notriptyline (Pamelor) and Desipramine (Norpramine) have more effects on which NT?

A

NE over 5HT

Also have less/no H1, M1, a1 effects

27
Q

TCAs: tertiary amines: Amitriptyline (Elavil), Imipramine (Tofranil), Doxepin (Sinequan), and Clomipramine (Anafranil) have more effects on which NT?

A

5HT over NE

***Have unwanted SE at H1, M1, a1

28
Q
  1. Notriptyline is the active metabolite of what drug?

2. Desipramine is the active metabolite of what drug?

A
  1. Amitriptyline

2. Imipramine

29
Q

MOA of TCAs:

A

Antagonize 5HT and NE reuptake transporters increasing levels in the synaptic cleft.

30
Q

TCAs have no effect on which NT?

A

Dopamine

31
Q

Aside from depression TCA’s can also be used to treat what?

A

Neuropathic pain (and sleep disturbances) at low doses

32
Q

AE of TCAs:

A

First degree AV block, bundle branch block

33
Q

PK of TCAs:

A

Substrates of CYP450, especially 2D6

ex. rotanavir increases levels

34
Q

TCAs have a ______ dosing range.

A

wide

35
Q

SSRI’s are more _______ and have ____ AE than TCA’s.

A

selective

less

36
Q

SSRI’s are usually the ____ ____ in antidepressant therapy.

A

first line

37
Q

MOA of SSRI’s:

A

Selective inhibitor of 5HT transporters increasing synaptic 5HT levels.
At high doses selectivity is lost and they will bind NE transporters as well.

38
Q

SSRI’s include:

A 
Fluoxetine (Prozac)
Citalopram (Celexa)
Fluvoxamine (Luvox)
Paroxetine (Paxil)
Sertraline (Zoloft)
Escitalopram (Lexapro)
39
Q

AE of SSRIs:

A

*Sexual dysfunction (5HT2rc)

Serotonin syndrome

40
Q

What are the s/s of serotonin syndrome?

A

Hyperthermia, muscle rigidity, myoclonus, rapid fluctuations in mental status and VS

41
Q

PK of SSRI’s:

A

Fluoxetine (Prozac), Paroxatine (Paxil), and Sertraline (Zoloft) are substrates and inhibitors of CYP 2D6

42
Q

What do SNRI’s do?

A

Blocks reuptake transporter of 5HT and NE

43
Q

Venlafaxine (Effexor): Type or reuptake inhibitor, MOA, Metabolism, AE:

A

SNRI
Blockage of 5HT and NE reuptake transporter is concentration dependent
Metabolized to active metabolite (desvenlafaxine-Pristig) by CYP 2D6
AE: Increased BP

44
Q

Duloxetine (Cymbalta): Type of reuptake inhibitor, MOA, uses, Metbolism, AE:

A

SNRI
Blockage of 5HT and NE reuptake transporter
Can be used for neuropathic pain
Metabolized by CYP2D6 and 1A2
AE: Increased transaminases, slight chance of increased BP

45
Q

Atypical antidepressants include:

A

Buproprion (Wellbutrin)
Mirtazapine (Remeron)
Nefazodone (Serzone)
Trazadone

46
Q

Buproprion (Wellbutrin): MOA, PK, CI, AE

A

Atypical antidepressant
Inhibits dopamine and NE reuptake
PK: hepatically metabolized by CYP2B6
CI: sz disorder, eating disorder (may cause sz)
AE: **Least sexual side effects ( no effect on 5HT)

47
Q

Mirtazapine (Remeron): MOA, PK, AE

A

Atypical antidepressant
Antagonizes 5HT 2/3 and alpha2 adrenergric rc (may affect 5HT1, but antidepressant activity is not well described)
PK: Substrate of CYP3A4
AE: less sexual side effects (usu. d/t 5HT2 agonism), acts on H1 rc= sedation, increased appetite (increasing dose can decrease these AE)

48
Q

Nefazodone (Serzone): MOA, PK, AE

A

Atypical antidepressant
Inhibits 5HT transporter
Antagonizes 5HT2 (less sexual dysfunction and anti-anxiety properties
PK: Substrate and inhibitor of CYP3A4
AE: antagonizes histamine and a1 adrenergic rc =sedation and orthostasis
*hepatotoxicity and fuliminant liver failure (2nd or 3rd line drug)

49
Q

Trazadone: MOA, PK, dosing, AE

A 
Atypical antidpressant
Inhibits 5HT transporter 
PK: metabolized by CYP3A4
Antidepressant at high doses and sleep agent at lower doses 
AE: priapism
50
Q

Serotonin receptor agonists include: (1)

A

Buspirone (Buspar)

51
Q

MOA of Buspar:

A

Agonizes 5HT1A rc

52
Q

Primary use of Buspar and advantages:

A

Anxiety
Non-sedating, non-addictive
(non-benzo anxiolytic)

53
Q

Buspar AE:

A

Nausea, dizziness

54
Q

Modafinil (Provigil) and Armodafinil (Nuvigil) are more commonly used for what rather than depression?

A

Narcolepsy

55
Q

What is the MOA of amphetimine, methamphetamine, methyphenidate (Ritalin, Concerta), modafinil (Provigil), and armodafinil (Nuvigil)?

A

Unknown
May interfere with ability of synaptic vesicles to store monoamines
May displace 5HT, DA, NE from storage vesicles and prevent reuptake

56
Q

Which one of these is most commonly used for depression and what are all their AE: amphetimine, methamphetamine, methylphenidate (Ritalin, Concerta), modafinil (Provigil), and armodafinil (Nuvigil)?

A

Methylphenidate is more commonly used for depression

AE: psychosis, alertness

57
Q

What is lithium’s MOA:

A

Interference with formation of cAMP and IP3

Numerous other effects on NT systems

58
Q

Lithium is used for control of:

A

Mania and depression

59
Q

Half-life of lithium:

A

12-27hrs

60
Q

Lithium has a ______ TI which is ___-____ mEq/L

A

Narrow

0.7-1.2

61
Q

PK and DI of Lithium:

A

Lithium is secrete and reabsorbed in the renal tubules.

Renal insufficiency, diuretics, and probenecid can increase lithium levels

62
Q

AE of Lithium include:

A 
Nausea
Thirst
Polyuria
Hypothyroidism
Tremor 
Weakness 
Mental confusion 
Teratogenesis
63
Q

Anticonvulsants that are used as mood stabilizers in Bipolar d/o include:

A

Carbamazepine

Valproic Acid

Pharmacology (48 decks)

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