Depression Pharmacology (Dr. Hamouda) flashcards |

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T/F: Antidepressants are among the most commonly prescribed medications in the USA?

True

The Monamine Hypothesis of Major Depression:

MDD reflects changes in 5-HT/NE and DA levels
Tryptophan depletion; tyrosine hydroxylase inhibition; Reserpine

All available antidepressants _____. (Action).

Increase synaptic monoamines

The Neurotropic Hypothesis of Major Depression

MDD: Disruption of BDNF levels

BDNF is important for...

Neural plasticity and neurogenesis

Antidepressants "Working" Hypotheses:

- Presynaptic monoamines modulate the transcription of postsynaptic proteins (BDNF, GR, Beta adrenoreceptors)
- Chronic enhancement of monoamines results in adaptive increases postsynaptic signaling, and increased neurogenesis

T/F: there is currently a drug that mimics BDNF?

False

Monoamine Oxidase Inhibitors (MAOIs)

Phenelzine
Selegiline
Tranycyclopramine

Tricyclic Antidepressants (TCAs/SERT inhibitors)

Amitriptyline
Nortryptyline
Imipramine
Clomipramine
Despiramine
Doxepin
Amoxapine (more effective, selective)

Selective Serotonin Reuptake Inhibitors (SSRIs)

Fluoxetine
Fluvoxamine
Paroxetine
Sertraline
Citalopram
Escitalopram

Norepinephrine- Serotonin Reuptake Inhibitors (SNRIs/NSRIs)

Venlafaxine
Duloxetine
Levomilnacipram

Drugs with mixed effects:

Nefazodone
Trazodone
Vilazodone
Mirtazapine
Amoxapine
Bupropion
Aripiprazole
Vortioxetine

MAOI site of action

Inhibits monoamine oxidase (in neuron cytosol)

SNRI site(s) of action

Inhibits reuptake via NET and SERT

SSRI site of action

Inhibits reuptake via SERT

TCA site(s) of action

Inhibits reuptake via NET and SERT

MAOI that elevates mood in patients with TB

Iproniazid

Non-selective MAOIs

Phenelzine
Tranycypromine

Selective MAO-B inhibitor (at low doses)

Slegiline

MAOI side effects:

Weight gain
Sexual side effects
Hepatotoxicity
Insomnia/Restlessness (amphetamine-like properties)

MAOI interaction with food

Foods containing tyramine
(Aged cheese, red wine, tap beer, soy, dried sausage, fava beans)

Result of MAOI + tyramine?

Accumulation of tyramine which induces NE and EPI release in the periphery --> increase blood pressure which can lead to stroke or MI

MAO-A degrades....

Norepinephrine
Serotonin
Dopamine

MAO-B degrades...

Dopamine

MAOI interactions with SSRIs/SNRIs/TCAs?

Serotonin syndrome (life-threatening)

Symptoms of overstimulation of 5-HT receptors?

Autonomic effects:
Hypertension
Tachycardia
Hyperthermia
Somatic effects:
Hyperreflexia
tremor
muscle rigidity
Cognitive effects:
Confusion
Irritability
Agication
Delirium
Coma

All TCAs have an ______ structure.

iminodibenzyl (tricyclic)

Generally, TCAs inhibit both _____ and ____.

NET
SERT

TCAs that are more selective for NET inhibition.

Desipramine
Nortriptyline

Clomipramine is much more selective for....

SERT (as opposed to NET)

Imipramine is more selective for ___.

SERT

TCAs are currently used for depression that is _____.

Unresponsive to SSRIs or SNRIs

T/F: All SSRIs on the market contain a halogen on a benzene ring?

True

TCA effect of blocking H1.

Sedative
Used for pruritis

TCA effect of blocking muscarinic receptors

Cognitive dulling
blurred vision
dry mouth
tachycardia
constipation
difficulty urinating
Tolerance may develope

TCA effect of antagonizing alpha-1 receptors

orthostatic hypotension (esp. in elderly)
Sedation

Quinidine-like effects of TCAs

Effects on cardiac conduction (slow heart conduction)

Effects of Amoxapine?

Extrapyramidal side effects (jerking-like movements)

TCA overdose is common in _____.

Suicide attempts

A _____ supply of TCAs can be lethal

week

Treatment of overdose from TCAs

Cardiac monitoring
Airway support
Gastric lavage
Sodium bicarbonate (uncouples TCA from cardiac Na+ channels)

T/F: SSRIs are very popular in clinical use

True

SSRI broad spectrum of uses:

GAD
PTSD
OCD
Panic disorder
PMDD
Bulimia

SSRIs have no affinity for _____, _____ or _____.

Histamine receptors
ACh receptors
Alpha adrenoreceptors

First part of SERT inhibition by SSRIs

Activation of 5-HT1A and 5-HT7
Activation of 5-HT1D autoreceptors
This decreases 5-HT release

Second part of SERT inhibition by SSRIs

Desensitization/down regulation of autoreceptors
Increased 5-HT in the synapse
Activation of post-synaptic 5-HT receptors

Long term "adaptive" effects of inhibiting SERT

Increase adrenergic or serotonergic receptor density/sensitivity
Increased receptor-G protein coupling
Phosphorylation of nuclear transcription factors
Induction of neurotrophic factors
Increased neurogenesis from progenitor cells in hippocampus
Reduced expression of SERT

Adverse effects of SSRIs

HA, insomnia, anxiety, irritability, decreased libido, ED, GI upset (improves with time), weight gain

Paroxetine specifically is associated with ______.

Increased risk of congenital cardiac malformation in the first trimester of pregnancy

FDA Warning: All antidepressants have the risk of _______ in patients under the age of 25.

Increased suicidality

T/F: All of the SSRIs are orally active?

True

Fluoxetine is metabolized to ____? This allows for a ______ dosing schedule.

Norfluoxetine

Weekly

_____ and _____ have little effect on CYP enzymes. (SSRIs).

Citalopram
Sertaline

_______ interactions are most common with SSRIs.

Pharmacokinetic

Most commonly inhibited CYP enzymes by SSRIs.

CYP2D6
CYP3A4

______ interaction are the most serious interaction with SSRIs.

Pharmacodynamic

NSRIs are __________ to each other.

Chemically unrelated

Generally NSRIs have a higher affinity for _____ than for ____.

SERT
NET

T/F: NSRIs have little affinity for other receptors.

True

Serotonergic side effects of NSRIs

Similar to SSRIs:
Nausea, constipation, insomnia, HA, sexual dysfunction

Noradrenergic side effects of NSRIs

Increased blood pressure and heart rate
CNS activation, insomnia, anxiety, agitation

_______ has more cardiac toxicity than the other NSRIs or SSRIs.

Venlafaxine

______ has rare hepatic toxicity.

Duloxetine

NSRIs are contraindicated in combination with _____.

MAOIs

_______ is used for smoking cessation.

Bupropion

Off label uses for Bupropion include:

Neuropathic pain
Weight loss

Bupropion inhibits:

NET
DAT (NDRI)
Blocks VMAT

Bupropion is metabolized by _____ to _____.

CYP2B6
Hydroxybupropion

Bupropion is associated with an increased risk of _____.

Seizures

5-HT2A Agonism

Hallucinogenic and anxiogenic
(LSD and mescaline)

5-HT2A Antagonism

Antianxiety, antipsychotic, antidepressant
(Nefazodone and Trazodone)

Trazodone site and mode of action

Inhibits postsynaptic 5-HT2A receptors

Weak, but selective inhibitor of SERT

Weak blocker of presynaptic alpha-adrenergic rc.

Antagonist of H1 rc.

Trazodone is metabolized by ____ to ____.

CYP3A4
m-chlorphenylpiperazine

Trazadone side effects

Less sexual SE than SSRIs
GI upset
Orthostatic hypotension
Sedation

Currently trazodone is used as _____.

An unlabeled hypnotic

Nefazodone site and mode of action

Inhibitor of postsynaptic 5-HT2A Rc

Weak inhibitor of SERT and NET

Blocks H1 and alpha adrenergic rc

Nefazodone is to _____ and _____.

hydroxynefazodone
m-cpp

Nefazodone is an inhibitor of the _____ enzyme.

CYP3A4

Nefazodone side effects

GI upset
Orthostatic hypotension
Hepatotoxicity

Nefazodone has a black box warning for ______.

Hepatotoxicity

Mirtazapine is used in patients with _____ and ____.

Depression
Insomnia

Mirtazapine site and mode of action

Antagonist of presynaptic a2 autoreceptors

Antagonist of 5-HT2 and 5-HT3 Rc.

Potent H1 antagonist

Side effect of mirtazapine

Somnolence
Increased appetite
Weight gain
Rare: Agranulocytosis

T/F: Mirtazapine has sexual side effects.

False

Amoxapine is only used for ______.

Unresponsive depression

Amoxapine undergoes _____ metabolism to _____.

Hepatic
7-hydroxyamoxapine

7-hydroxyamoxapine is a potent _____ blocker, leading to _____ effects and ________.

D2
Antipsychotic
Parkinsonian syndrome
(Strong extrapyramidal side effects).

Sudden withdrawal of an antidepressant can precipitate a ______.

Discontinuation Syndrome

Symptoms of Discontinuation Syndrome

Dizziness
HA
Nervousness
Nausea
Insomnia

Discontinuation Syndrome is most intense with ____ and _____.

Paroxetine
Venlafaxine

Discontinuation Syndrome is less common with ____.

Fluoxetine

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