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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
PK of MAOIs: Absorption, Metabolism, DI
- 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
26
TCAs: secondary amines- notriptyline (Pamelor) and Desipramine (Norpramine) have more effects on which NT?
NE over 5HT | Also have less/no H1, M1, a1 effects
27
TCAs: tertiary amines: Amitriptyline (Elavil), Imipramine (Tofranil), Doxepin (Sinequan), and Clomipramine (Anafranil) have more effects on which NT?
5HT over NE | ***Have unwanted SE at H1, M1, a1
28
1. Notriptyline is the active metabolite of what drug? | 2. Desipramine is the active metabolite of what drug?
1. Amitriptyline | 2. Imipramine
29
MOA of TCAs:
Antagonize 5HT and NE reuptake transporters increasing levels in the synaptic cleft.
30
TCAs have no effect on which NT?
Dopamine
31
Aside from depression TCA's can also be used to treat what?
Neuropathic pain (and sleep disturbances) at low doses
32
AE of TCAs:
First degree AV block, bundle branch block
33
PK of TCAs:
Substrates of CYP450, especially 2D6 | ex. rotanavir increases levels
34
TCAs have a ______ dosing range.
wide
35
SSRI's are more _______ and have ____ AE than TCA's.
selective | less
36
SSRI's are usually the ____ ____ in antidepressant therapy.
first line
37
MOA of SSRI's:
Selective inhibitor of 5HT transporters increasing synaptic 5HT levels. At high doses selectivity is lost and they will bind NE transporters as well.
38
SSRI's include:
``` Fluoxetine (Prozac) Citalopram (Celexa) Fluvoxamine (Luvox) Paroxetine (Paxil) Sertraline (Zoloft) Escitalopram (Lexapro) ```
39
AE of SSRIs:
*Sexual dysfunction (5HT2rc) | Serotonin syndrome
40
What are the s/s of serotonin syndrome?
Hyperthermia, muscle rigidity, myoclonus, rapid fluctuations in mental status and VS
41
PK of SSRI's:
Fluoxetine (Prozac), Paroxatine (Paxil), and Sertraline (Zoloft) are substrates and inhibitors of CYP 2D6
42
What do SNRI's do?
Blocks reuptake transporter of 5HT and NE
43
Venlafaxine (Effexor): Type or reuptake inhibitor, MOA, Metabolism, AE:
SNRI Blockage of 5HT and NE reuptake transporter is concentration dependent Metabolized to active metabolite (desvenlafaxine-Pristig) by CYP 2D6 AE: Increased BP
44
Duloxetine (Cymbalta): Type of reuptake inhibitor, MOA, uses, Metbolism, AE:
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
Atypical antidepressants include:
Buproprion (Wellbutrin) Mirtazapine (Remeron) Nefazodone (Serzone) Trazadone
46
Buproprion (Wellbutrin): MOA, PK, CI, AE
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
Mirtazapine (Remeron): MOA, PK, AE
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
Nefazodone (Serzone): MOA, PK, AE
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
Trazadone: MOA, PK, dosing, AE
``` Atypical antidpressant Inhibits 5HT transporter PK: metabolized by CYP3A4 Antidepressant at high doses and sleep agent at lower doses AE: priapism ```
50
Serotonin receptor agonists include: (1)
Buspirone (Buspar)
51
MOA of Buspar:
Agonizes 5HT1A rc
52
Primary use of Buspar and advantages:
Anxiety Non-sedating, non-addictive (non-benzo anxiolytic)
53
Buspar AE:
Nausea, dizziness
54
Modafinil (Provigil) and Armodafinil (Nuvigil) are more commonly used for what rather than depression?
Narcolepsy
55
What is the MOA of amphetimine, methamphetamine, methyphenidate (Ritalin, Concerta), modafinil (Provigil), and armodafinil (Nuvigil)?
Unknown May interfere with ability of synaptic vesicles to store monoamines May displace 5HT, DA, NE from storage vesicles and prevent reuptake
56
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)?
Methylphenidate is more commonly used for depression | AE: psychosis, alertness
57
What is lithium's MOA:
Interference with formation of cAMP and IP3 | Numerous other effects on NT systems
58
Lithium is used for control of:
Mania and depression
59
Half-life of lithium:
12-27hrs
60
Lithium has a ______ TI which is ___-____ mEq/L
Narrow | 0.7-1.2
61
PK and DI of Lithium:
Lithium is secrete and reabsorbed in the renal tubules. | Renal insufficiency, diuretics, and probenecid can increase lithium levels
62
AE of Lithium include:
``` Nausea Thirst Polyuria Hypothyroidism Tremor Weakness Mental confusion Teratogenesis ```
63
Anticonvulsants that are used as mood stabilizers in Bipolar d/o include:
Carbamazepine | Valproic Acid

Pharmacology (48 decks)

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