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Pharmacology Test 1 > Antidepressants > Flashcards

Antidepressants Flashcards

1
Q

SSRI

A

Antidepressant

First Line

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2
Q

SNRIs

A

Antidepressant

First Line

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3
Q

Bupropion

A

Antidepressant

First Line

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4
Q

Mirtazapine

A

Antidepressant

First Line

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5
Q

TCAs

A

Antidepressant

Second Line/Alternative Agent

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6
Q

MAOIs

A

Antidepressant

Second Line/Alternative Agent

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7
Q

Major Depressive Disorder

A

5+ for atleast 2 weeks

  • DEPRESSED MOOD
  • DIMINISHED INTEREST/PLEASURE (anhedonia)
  • significant weight loss/gain
  • insomnia or hypersomnia
  • psychomotor agitation/retardation
  • fatigue or loss of energy
  • feelings of worthlessness or excessive guilt
  • diminished ability to think or concentrate; indecisivenss
  • recurrent thoughts of death; suicidal ideation or attempt
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8
Q

The Monoamine Hypothesis

A
  • depressed mood results from decreased monoamine neurotransmission
  • major classes of clinically useful drugs INCREASE monoamine neurotransmission by LIMITING THE REUPTAKE OF MONOAMINE NEUROTRANSMITTERS or by preventing their breakdown
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9
Q

Process of release/effect of NT

A

Neurotransmitters:

  • synthesized from amino acid precursors in specific neurons
  • packaged into vesicles
  • released in response to stimulus
  • bind postsynaptic receptors
  • subject to reuptake by presynaptic transporters
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10
Q

Catecholamines from Tyrosine

A

Monoamine Neurotransmitters

  • epinephrine
  • dopamine
  • norepinephrine
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11
Q

Tryptamines from Tryptophan

A

Monoamine Neurotransmitter

- serotonin

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12
Q

Reserpine

A

inhibits VMAT

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13
Q

SSRI Site of Action

A
  • block reuptake of serotonin

- serotonin left in extracellular space left to interact with receptors for longer period of time

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14
Q

SNRI Site of Action

A
  • block reuptake of serotonin and norepinephrine
  • same as TCAs
  • serotonin and norepi left in extracellular space left to interact with receptors for a longer period of time
  • ** MORE SELECTIVE THAT TCAs***
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15
Q

TCAs Site of Action

A
  • block reuptake of serotonin and norepinephrine
  • same as SNRIs
  • serotonin and norepi left in extracellular space left to interact with receptors for a longer period of time
  • ** INTERACT WITH A WHOLE BUNCH OF OTHER RECEPTORS AS WELL ***
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16
Q

MAOIs Site of Action

A
  • prevent breakdown of monoamines in presynaptic cell
  • inhibit MAO; prevents breakdown of NT, increasing amount in extracellular space
  • ACT INTRACELLULARLY
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17
Q

Bupropion Site of Action

A
  • blocks reuptake of DOPAMINE and norepinephrine

- acts on dopaminergic neuron

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18
Q

Mirtazapine Site of Action

A
  • blocks presynaptic a2 receptors and some 5-HT2/3 receptors
  • antagonist of presynaptic a2 autoreceptor, which ENHANCES RELEASE OF NE and 5-HT
  • block binding of NT to presynaptic recpetor
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19
Q

Limitations to Monoamine Hypothesis

A
  • clinically useful antidepressants act rapidly at pharmacologic sites of action, yet clinical effects require 3+ weeks of therapy
  • while reserpine rapidly depletes neurotransmitter, several weeks of treatment are required to induce depression
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20
Q

Major Antidepressant Site of Action Targets

A

Neurotransmitter reuptake transporters

* activity limited by reuptake rate*

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21
Q

Autoreceptors

A
  • found on presynaptic cell
  • respond to level of neurotransmitter
  • when reuptake is blocked, elevated NT in synapse leads to down-regulation of synthesis and release of additional NT
  • upon chronic use, autoreceptors may be down regulated, thereby relieving inhibition of NT synthesis and release, and enhancement of neurotransmission
  • receptors constantly bound to ligand, receptor downregulated and removed from cell surface
  • MAY ACCOUNT FOR LIMITATIONS OF HYPOTHESIS
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22
Q

SSRI uses

A
  • MAJOR DEPRESSION
  • anxiety disorder
  • OCD
  • PTSD
  • PMDD
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23
Q

SNRI uses

A
  • major depression
  • anxiety disorder
  • chronic pain
  • fibromyalgia
24
Q

Bupropion uses

A
  • major depression*
  • *first-line alternative to SSRI or SNRI when anxiety is not a prominent symptom
  • smoking cessation
25
Q

Mirtazapine uses

A
  • major depression*

- * particularly useful in patients with insomnia or marked weight loss

26
Q

TCAs uses

A
  • alternative agent

- major depression (when unresponsive to other drugs)

27
Q

MAOIs

A
  • alternative agent

- major depression (when unresponsive to other drugs)

28
Q

Anti-depressant Boxed Warning

A

SUICIDE RISK

29
Q

Antidepressant Adverse Events (All)

A
  • suicide risk

- mania (most often in patients with undiagnosed bipolar disorder)

30
Q

SSRIs Adverse Events

A
  • inhibit 5-HT reuptake SELECTIVELY compared to NE reuptake; side effects limited to effects on 5-HT mediated responses

Adverse Events:

  • nausea
  • headache
  • anxiety
  • agitation
  • insomnia
  • sexual dysfunction
  • seizures with gross overdose
31
Q

SNRIs Adverse Events

A
  • inhibit reuptake of both 5-HT and NE; side effects due to excess of both serotonin and norepi
Adverse Events:
\_\_\_\_\_\_\_\_\_\_\_\_\_\_\_\_\_\_\_\_\_\_\_\_\_\_
- nausea
- headache
- anxiety
- agitation     ...........................  same as SSRIs
- insomnia
- sexual dysfunction
seizures with gross overdose
\_\_\_\_\_\_\_\_\_\_\_\_\_\_\_\_\_\_\_\_\_\_\_\_\_\_
- anticholinergic
- sedation
- hypertension (veniafaxine)
32
Q

Bupropion Adverse Events

A
  • inhibits reuptake transporters for NE and dopamine
  • resembles amphetamine
  • ** especially helpful in patients with impaired concentration ***
  • ** alternative for patients with antidepressant-induced sexual dysfunction ***

Adverse Events:

  • nausea
  • headache
  • anxiety
  • irritability
  • insomnia
  • mild hypertension and tachycardia
  • tremor
  • appetite suppression
  • dose related seizures (minimized with EXT release formulation)
33
Q

Why Sexual Dysfunction with SSRIs and SNRIs but not Bupropion?

A
  • sexual dysfunction associated with SSRIs and SNRIs due to stimulation of 5-HT receptor subtypes in the brain and spinal cord
34
Q

Mirtazapine Adverse Events

A
  • antagonist of a2 autoreceptor; enhances release of NE and 5-HT
  • antagonist at 5-HT 2/3 receptors
  • ** particularly useful in patients with INSOMNIA or marked WEIGHT LOSS***
  • ** helpful in patients who experience nausea with SSRIs, SNRIs, or bupropion ***

Adverse Events:

  • sedation
  • weight gain
  • dizziness
  • dry mouth
  • constipation
35
Q

When beneficial for Bupropion Use?

A
  • patients with impaired concentration

- alternative for patients with antidepressant-induced sexual dysfunction

36
Q

When beneficial for Mirtazapine Use?

A
  • patients with insomnia or marked weight loss

- helpful in patients who experience nausea with SSRIs, SNRIs, or bupropion

37
Q

Tricyclic Antidepressants Site of Action

A
  • inhibit reuptake transporters for BOTH NE and 5-HT (like SNRIs)
  • * tend to interact with a variety of OTHER receptors, therefore have a broader range of side effects than SNRIs*
38
Q

Tricyclic Antidepressant Adverse Events

A

Those for SNRIs

  • nausea
  • headache
  • anxiety
  • agitation
  • insomnia
  • sexual dysfunction
  • extrapyramidal effects (early in treatment)
  • seizures with gross overdose
  • serotonin syndrome with MAOI
  • anticholinergic
  • sedation

PLUS
- orthostatic hypotention
- weight gain
- arrhythmias
**********

39
Q

Reuptake Blockers SNRI & TCAs
venlafaxine (SNRI)
imipramine (TCA)
amitriptyline (TCA)

A

SNRI & TCAs 5-HT ++ NE +

SAME mechanism of action; same effect on 5-HT and NE differ in spectrum of side effects

IMIPRAMINE AND AMITRIPTYLINE ACTIVATE MANY OTHER RECEPTORS which are why they are problematic to take

40
Q

Reuptake Blockers SSRIs
fluoxetine
paroxetine
sertraline

A

ALL: 5-HT +++

fluoxetine: NE 0
paroxetine: NE +
sertraline: NE 0

41
Q

MAOIs site of action
phenelzine
tranylcypromine

A
  • inhibit Monoamine Oxidase (MAO)
  • phenelzine combines IRREVERSIBLY with MAO to provide long-lasting inhibition
  • tranylcypromine does not bind irreversibly, but still has prolonged effect
42
Q

MAOIs Adverse Events

A
  • hypertensive reactions in response to INDIRECTLY ACTING SYMPATHOMIMETICS (otherwise typically lower blood pressure)
  • hypertensive crisis with tyramine containing foods
  • hyperthermia
  • CNS stimulation leading to agitation and convulsions
  • seizures with overdose
  • serotonin syndrome with SSRIs/SNRIs
43
Q

Pharmacokinetics of Antidepressant Agents

A 
In general most:
- have rapid oral absorption
- reach peak plasma concentration in 2-3 hours
- have t1/2 of .5-1 day
are tightly bound to plasma proteins
- metabolized by liver
- eliminated by kidney
44
Q

Pharmacokinetics of specific drugs may influence choice of agent: SSRIs; escitalopram and citalopram

A
  • several SSRIs are moderate to strong inhibitors of CYP2D6

- escitalopram and citalopram exhibit age-dependent decrease in CYP2C19 metabolism (use with care in elderly)

45
Q

Fluoxetine half life

A

7-10 days much longer than most

avg .5-1 day

46
Q

Drug Interactions

SNRIs, TCAs, Mirtazapine, Trazodone

A
  • additive with other sedatives, particularly alcohol and benzodiazepines
47
Q

SSRIs Drug Interactions

A
  • additive effects on QT interval and torsade de pointes with other QT-interval prolonging drugs
48
Q

SSRIs and SNRIs Drug Interactions

A
  • increased risk of bleeding with antiplatelet or anticoagulant drug (SSRIs and SNRIs)
  • risk of serotonin syndrome with MAOIs
49
Q

Serotonin Syndrome

A
  • can be caused by all serotonergic drugs; rare but potentially life-threatening triad of abnormalities consisting of cognitive, autonomic and somatic effects due to excess serotonin
  • can progress toward coma and death

Management: sedation (benzodiazepines), paralysis, intubation and ventilation

50
Q

Overdoses TCAs

A
  • extremely dangerous; prescribed on “no refill basis”, small quantities
51
Q

Overdoses MAOIs

A
  • intoxication rare, requires supportive treatment
52
Q

Overdoses SSRIs

A
  • OD fatalities rare

- intoxication requires supportive treatment

53
Q

Overdoses Bupropion

A
  • seizures
54
Q

Overdoses Mirtazapine

A
  • disorientation, tachycardia
55
Q

Overdoses of Antidepressants Newer Agents

A
  • often involves other drugs, including alcohol

Pharmacology Test 1 (8 decks)

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