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MT 6314 2nd Shift > 7.4: Antidepressant Agents > Flashcards

7.4: Antidepressant Agents Flashcards

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1
Q

True or False:

Major depressive disorder is a depressed mood most of the time for at least 2 week or loss of interest or pleasure in most activities.

A

True

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2
Q

True or False:

Other characteristics of major depressive disorder are disturbance in sleep and appetite, deficits in cognition and energy, and thoughts of guilt, worthlessness, and suicide.

A

True

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3
Q

What are the 3 pathophysiology of major depression?

A
  1. Monoamine hypothesis
  2. Neurotrophic hypothesis
  3. Neuroendocrine factors
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4
Q

Determine what kind pathophysiology:

  • Norepineprine (NE) and serotonin (5-HT)
  • Functional decrease in the activity (depression)
  • Functional increase in the activity (mood elevation)
A

Monoamine hypothesis

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4
Q

Determine what kind pathophysiology:

  • Regulation of neural plasticity, resilience, and neurogenesis
  • Exert its influence on neuronal survival and growth effects by activating tyrosine kinase receptor B in both neurons and glia
A

Neurotrophic hypothesis

Brain derived neurotrophic factor (BDNF)

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5
Q

Determine what kind pathophysiology:

It affects
1. Hippocampus
2. Anterior cingulate gyrus
3. Medial frontal cortex

A

Neurotrophic hypothesis

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5
Q

Determine what kind pathophysiology:

Adrenocorticotropic hormone
* Nonsuppression of adrenocorticotropic hormone (ACTH) release in the dexamethasone suppression test
* Dysregulation of the stress hormone axis

A

Neuroendocrine factors

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5
Q

Determine what kind pathophysiology:

  • Thyroid hormone
  • Thyroid dysregulation in depressed patients
  • Blunting of response of thyrotropin to thyrotropin-releasing hormone, and elevations in circulating thyroxine during depressed states
A

Neuroendocrine factors

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6
Q

Determine what kind pathophysiology:

Sex steroids
* Estrogen deficiency states, which occur in the postpartum and postmenopausal periods, are thought to play a role in the etiology of depression in some women
* Severe testosterone deficiency in men is sometimes associated with depressive symptom

A

Neuroendocrine factors

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7
Q

What is the primary action of Selective Serotonin Reuptake Inhibitors (SSRIs)?

A

Inhibition of serotonin transporter (SERT)

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8
Q

What are the 6 major approved SSRIs?

A
  1. Fluoxetine
  2. Sertraline
  3. Citalopram
  4. Paroxetine
  5. Fluvoxamine
  6. Escitalopram

FluSerCiPFE !!! >:(

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9
Q

True or False:

The MOA of SSRIs is Serotonin transporter (SERT) is a glycoprotein with 12 transmembrane regions embedded in the axon terminal and cell body membranes of serotonergic neurons.

A

True

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10
Q

What are the other indications of SSRIs?

A
  1. Generalized Anxiety Disorder (GAD)
  2. Post-traumatic stress disorder (PTSD)
  3. Obsessive Complusive Disorder (OCD)
  4. Panic Disorder
  5. Premenstrual Dysphoric Disorder (PMDD) and Bulimia
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11
Q

What is the half-live of SSRIs?

A

18-24 hours

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12
Q

Identify the drug interactions of SSRIs:

  • Interaction between fluoxetine and a MAOI
  • Life-threatening
  • Reason: Fluoxetine has to be discontinued 4 weeks or longer before an MAOI can be administered
A

Serotonin syndrome

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13
Q

Identify the drug interaction of SSRIs:

  • Severe muscle rigidity
  • Myoclonus
  • Hyperthermia
  • Cardiovascular instability
  • CNS stimulatory effects-seizures
A

Serotonin syndrome

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14
Q

What are the drugs included in Serotonin syndrome?

A
  • MAOIs
  • TCAs
  • Meperidine
  • MDMA (ecstasy)
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15
Q

In serotonin syndrome, what is the antidepressant drug that blocks the 5-HT receptors?

A

Cyproheptadine

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16
Q

What are the 3 antidepressants of SNRIs?

A
  • Venlafaxine and Duloxetine
  • Tricyclic Antidepressants
  • 5HT2A Antagonists
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17
Q

Identify this antidepressant of SNRIs:

  • Metabolized in the liver to Desvenlafaxine
  • Lowest protein binding amongst all anti-depressant (27-30%)
  • Similar half lives of 11 hours (once daily dosing)
  • 45% are excreted unchanged in the urine
A

Venlafaxine

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18
Q

Identify this antidepressant of SNRIs:

  • Well-absorbed
  • Half-life: 12 hours
  • Tightly bound to protein
A

Duloxetine

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19
Q

Identify this antidepressant of SNRIs:

  • NET is structurally very similar to the 5-HT transporter
  • 12-transmembrane domain complex that allosterically binds norepinephrine
  • NET also has a moderate affinity for dopamine
A

Venlafaxine

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20
Q

True or False:

Venlafaxine is a strong inhibitor of NET.

A

False

Weak dapat.

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21
Q

True or False:

Desvenlafaxine, duloxetine, and milnacipran are more balanced inhibitors of both SERT and NET.

A

True

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22
# True or False: Nonetheless, the affinity of most SNRIs tends to be **much greater for SERT** than for NET.
True
23
# True or False: The SNRIs differ from the TCAs in that they **lack the potent antihistamine**, **-adrenergic blocking**, and **anticholinergic effects of the TCAs.**
True
24
# True or False: SNRIs tend to be favored over the TCAs in the treatment of **MDD and pain syndromes** because of their better tolerability.
True
25
# Identify this antidepressant: * **Imipramine, amitriptyline** * Structurally related to the phenothiazine antipsychotics * Well absorbed **orally** * May undergo **first-pass metabolism** * **High volume of distribution** * Not readily dialyzable
Tricyclic antidepressants (TCAs)
26
# Identify this antidepressant: * **Extensive hepatic metabolism is required** before elimination * Plasma half-lives of **8-36 hours** * **Once-daily dosing** * **Wide therapeutic window** * Serum are reliable in predicting response and toxicity * **Nortriptyline, desipramine**
Tricyclic antidepressants (TCAs)
27
# Identify this antidepressant (Mode of transmission): * **Inhibit the reuptake mechanisms** (transporters) responsible for the termination of the synaptic actions of **both NE and 5-HT** * **Potentiation of NTA actions** at postsynaptic receptors
Tricyclic antidepressants (TCAs)
28
# Identify this antidepressants of SNRIs on its pharmacologic effects: * Inhibits the reuptake of **NE** at nerve endings in the ANS * Peripheral autonomic **sympathomimetic effects** * **Sedation is common** * **Antagonism** of **muscarinic receptors** * Marked with **amitriptyline**
Tricyclic antidepressants (TCAs)
29
# Identify this antidepressants based on pharmacologic effects: * Cardiovascular effects * Hypotension from alpha-adrenoceptorblockade * Arrhythmias * Convulsions * Overdosage
Tricyclic antidepressants (TCAs)
30
# Identify this antidepressants based on its clinical uses: * Major depressive disorders * Alternative agent * Psychomotor retardation * Sleep disturbances * Poor appetite * Weight loss
Tricyclic antidepressants (TCAs)
31
# Identify this antidepressant based on its toxicities: 1. Pharmacodynamic actions 2. Sympathomimetic effects 3. Atropine-like effects 4. Orthostatic hypotension, ECG abnormalities, and cardiomyopathies 5. Tremor and paresthesias 6. Weight gain
Tricyclic antidepressants (TCAs)
32
# Identify this antidepressants: * **Trazodone** and **Nefazodone** * **Rapidly absorbed** and undergoes **extensive hepatic metabolism** * **Short half** loves thus requires split dosing * Trazodone prescribed as singe dose at night as a hypnotic in lower doses than are when used for depression * **Active metabolites** * Nefazodone are potent inhibtor of CYP3A4
5-HT2 antagonists
33
What are the other drugs that do not fit into the other categories of Tetracyclic and Unicyclic Antidepressants?
* Bupropion * Mirtazapine * Amoxapine * Maprotiline
34
# Identify this antidepressant of Tetracyclic and Unicyclic: * **unicyclic aminoketone structure** * resembles **amphetamine** in chemical structure AND has central nervous system (CNS) activating properties * rapidly absorbed and has a **mean protein binding of 85%** * has three active metabolites one of which is being developed as an anti depressant.
Bupropion
35
What is the biphasic elimination of bupropion in 1st phase and 2nd phase?
1 hour; 14 hours
36
# Identify this antidepressant of Tetracyclic and Unicyclic: * not commonly associated with sexual side effects. * **tetracyclic chemical structure** * belongs to the **piperazino-azepine** group * demethylated followed by hydroxylation and glucuronide conjugation * half-life: **20–40 hours**, dosed once in evening
Mirtazapine
37
# Identify this antidepressant of Heterocyclic Antagonists: * MOA: **complex pharmacology** * An antagonist of the presynaptic 2 autoreceptor and **enhances the release** of both **Norepinephrine and 5-HT** * **Antagonist** of **5-HT2** and **5-HT3**receptors * **Potent H1 antagonist** (drug's sedative effects)
Mirtazapine
38
# Identify this antidepressant of Tetracyclic and Unicyclic: * **N-methylated metabolite** of loxapine * Share structural similarities with Maprotiline * Rapidly absorbed with protein binding of about **85%.** * Half-life: **variable**, **divided doses** * **7- hydroxyamoxapine**: potent D2 blocker, associated with antipsychotic effects
Amoxapine
39
# Identify this antidepressant of Tetracyclic and Unicyclic: * MOA: **potent NET inhibitors** and **less potent SERT inhibitors.** * Both possess **anticholinergic properties** * A **moderate inhibitor** of the **postsynaptic D2 receptor**
Amoxapine and Maprotiline
40
# Identify this antidepressant of MAOIs: * C-N-N moiety * **Phenelzine, isocarboxazid** * **No longer marketed** * Combine **irreversibly** with MAO
Hydrazides
41
# Identify this antidepressant of MAOIs: * Lack the C-N-N moiety * **Tranylcypromine** * Combine **reversibly** with MAO
Nonhydrazides
42
This is structurally **related to amphetamines**, **orally active**, and has a **nonselective inhibitors.**
Monoamine oxidase inhibitors (MAOIs)
43
What are the **two selective inhibitors** of MAOIs?
1. MAO-A 2. MAO-B
44
# Identify if MAO-A or MAO-B: Metabolizes **NE**, **5-HT** and **tyramine**
MAO-A
45
# Identify if MAO-A or MAO-B: Metabolizes **dopamine.**
MAO-B
46
It is the **selective inhibitor** of MAOIs and is used in parkinson's disease, selectively inhibits MAO-b at low dose, and is less selective at higher doses.
Selegiline
47
# Identify this **drug** of **MAOIs**: * **Fastest onset** of effect * **Shorter duration of action** (about 1 week)
Tranylcypromine
48
# True or False: MAOIs are given daily, and persists even after these drugs are no longer detectable in plasma.
True
49
# True or False: The MOA of MAOIs increases in **brain amine levels** by interfering with their **metabolism** in the nerve endings, and **increase vesicular stores of NE and 5-HT.**
True
50
# True or False: When the neuronal activity of MAOIs discharges the vesicles, it increases the amount of amines released.
True
51
# True or False: MAOIs enhances the action of NTAs.
True
52
# Identify the antidepressant based on its pharmacologic effects: * **Increase NE in sympathetic nerve terminals** * **Peripheral sympathomimetic effects** * Long-term use can **decrease BP** * **CNS stimulating effects** * **Seizures** may occur with overdosage
Monoamine oxidase inhibitors (MAOIs)
53
What are the clinical uses of MAOIs?
* Major depressive disorders * Anxiety * Phobic features * Hypochondriasis
54
What are the toxicities of MAOIs?
* Hyperthermia * CNS stimulation, agitation and convulsions * Shock
55
# Identify this antidepressants based on drug interaction: * Inhibitors of **hepatic drug-metabolizing enzymes** * **Hypertensive crisis** * Occur in patients who **consume food with high concentration** of **indirect sympathomimetic tyramine** * Administration with SSRIs have resulted to **serotonin syndrome**
Monoamine oxidase inhibitors (MAOIs)
56
Enumerate the MAO inhibitors:
* Phenelzine * Selegiline * Tranylcypromine | PST MAO! >:(
57
Enumerate the TCAs
* Amitriptyline * Clomipramine * Imipramine | TCA ACI
58
Enumerate the heterocyclic antidepressants:
* Bupropion * Amoxapine * Mirtazepine
59
Enumerate the SNRI inhibitors:
* Duloxetine * Venlafaxine
60
Enumerate the 5-HT antagonists:
* Nefazodone * Trazodone
61
Enumerate the SSRIs:
* Escitalopram * Fluoxetine * Fluvoxamine * Paroxatine * Sertraline

MT 6314 2nd Shift (8 decks)

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