Antidepressants and Mood Stabilizers Flashcards by Daniel Wakefield

What are the TCAs?

Amitriptyline
Imipramine
Nortriptyline

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What are the MOA of the TCAs?

SNRIs: Decrease Serotonin and NE retake into presynaptic terminals, increasing neurotransmitter action and changing receptor profiles. Also blocks muscarinic Ach, serotonin, and histamine receptors, which leads to ADE.

+Serotonin, NE
-Ach, serotonin, and histamine

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What are the AEs of the TCAs? how?

Orthostatic hypotension: a blocker
Anti-SLUDGEBBB: mAch blocker
Glaucoma: mAch blocker
Sedation: a and histamine blocker
Weight gain
Sexual disturbance

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What are the acute and chronic effect of TCAs?

Acute: drowsy, decreased cognition
Chronic: normal cognition, not drowsy

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What is CI with TCAs?

Drugs: clonidine, alcohol
Disease: glaucoma

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What are the atypical antidepressants?

Not TCAs: 
Amoxamine
Maprotiline
Trazodone
Nefazadone
Mirtizapine
Buproprion
Venlafaxine
Duloxetine

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What is the MOA/AE of amoxamine?

MOA: inhibts NE>5HT/DAT
AE: Blocks DOPA–>Extrapyrimidal: dopa antagonism

Use: depression in psychotic patients

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What is the MOA/AE of maprotiline?

MOA: Serotonin/NE reuptake inhibitor (SNRI)
AE: seizure risk

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What is the MOA/AE of Trazodone and nefazodone?

Use: Anxiety + insomnia

MOA: mild SSRI, SARI: but mainly a 5HT1a agonist/5HT2a blocker (weird…)
AE: CYP’s
Neftazone: hepatotoxic

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What is the MOA/AE of mirtazepine?

MOA: presynaptic a2 antagonist leads to increased Serotonin/NE release
antagonizes 5HT2 receptors
AE: blocks sertonin, sedation (blocks histamine), WEIGHT GAIN (less GI and sex disturbance than SSRIs)

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What is the MOA/AE of Buproprion?

Use: smoking cessation, slow release
MOA: weak dopa/serotonin/NE blocker
*METABOLITES–>SNRI
AE: restlessness, anxiety, SEIZURES

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What is the MOA /AE of venlafaxine?

MOA: SSRI with NO antihistamine/Ach
AE: LOW ADs! small hypertension

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What is the MOA/AE of duloxetine?

SNRI

AD: Cyps

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What is the MOA of the SSRIs?

MOA: increase JUST serotonin effects
AE: sexual dysfunction, GI, teratogen, serotonin syndrome
*Low OD rate due to high TI

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What is the MOA/AE of the MAOis?

MOA: IRREVERSIBLY inhibiti MAO-a and b via OXIDATIVE metabolism
AE: Tyramine reaction, less sleep, orthostatic hypotension, weight gain, sexual dysfunction

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What are the targets of MAO A and B?

A: NE, serotonin, TYRAMINE

B: Dopamine

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What patient profile leads to short effectiveness of MAOis?

Fast Acetylators

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What is the acute and chronic patient effects in MAOis?

Acute: arousal and EUPOHORIA

Chronic: just arousal, no euphoria (2-6 weeks)

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What are the SSRIs?

Citalopram
Fluoxetine
Paroxetine
Sertraline
FLuvoxamine

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What are the MOAis?

Trancypromine

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What are the mood stabilizers?

Lithium
Valproate
Carbamazapine
Lamotrigine

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What is the MOA/AE of Lithium?

MOA: IP3 signal inhibitor

AE: Diuretics/NSAIEDs-->renal toxic
Hits all high flow organs:
Brain: tremor, ataxia, sedation
Glands: edema, THYROID decrease
Kidney: nephrogenic diabetes insipidus
Teratogen: Ebstein anomaly
Skin: acne and psoriasis
Heart: swinging between tachycardia and bradycardia

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What is the MOA/AE of Valproate?

MOA: Na/Ca blocker, Increase GABA and K conductance

AE: Inhibits UGT–>increases its own concentration
CI: Phenytoin displacement from proteins
Heartburn
Liver toxicity

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What is the MOA/AE of Carbamazapine?

MOA: Inhibit voltage gated Na channels
AE: induces Cyps--> DECREASES its own concentration, generates 10,11 epoxide metabolite
Decreases OCP efficacy=RED FLAG
Diplopia
Ataxia
Stevens Johnson syndrome
APLASTIC ANEMIA

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What are the Benzodiazapines?

``` Alprazolam CHlordiazepoxide Clonazepam Clorazepate Diazepam Lorazepam Oxazepam Prazepam ```

What is the MOA/AE of BZDs?

MOA: Allosteric GABA ^potency *binds at unique site from flumazenil AE: Sedation, Teratogen, Depenence, Tolerance

Anxiety Rx?

Alprazolam, lorazepam, clonazepam

Panic attack Rx?

Alprazolam

BZD with TCA activity?

Alprazolam

ONLY BZD with muscle relaxation?

Diazepam: "muscles Die with diazepam"

Alcohol withdrawal Rx?

Chlordiazepoxide Diazepam Lorazepam with hepatic disease

What is the MOA/AE of Buspirone?

MOA: Decrease Serotonin Increase NE/Dopa *slow onset AE: same as BZDs???

What is the MOA/AE of Propranolol?

MOA: Beta blocker for stage fright | *does not act in area of brain involving emotion, just autonomics

What is the biogenic amine theory of depression?

Depression is due to DECREASES in NE and Serotonin

What are the evidences for the biogenic amine theory of depression?

1. our drugs work | 2. Reserpine blocks monoamine storage and causes depression

Locus ceruleus=

Raphe nucleus=

serotonin

Why is response to antidepressants delayed?

1. It takes a few weeks to reset cellular machinery: receptors and signals have to be synthesized 2. stress hormones (cortisol) takes time to be regulated

What is the recent evidence about cytokines?

They have a antidepressant effect (CI for NSAIDs?)

What classes are included in atypical antidepressants?

SNRIs NRIs etc...

What is the BLACK BOX warning for ALL antidepressants?

SUICIDAL THOUGHTS!!!!

What are antidepressants substrates for in the BBB?

P-glycoprotein/ABCB1 transporter: MDR-1 testing shows that mutation in MDR-1 will decrease effectiveness of drugs because the receptor pumps them out of the brain

What drugs are MDR-1/P-gp substrates?

Citalopram Venlafaxine Paroxetine Amitriptyline

What drugs are NOT MDR-1/P-gp substrates?

Mirtizapine | FLuoxetine

Bed wetting Rx?

Imipramine

TCA effects?

+: 5HT, NE | -: mAch, 5HT, Histamine

Do TCAs have euphoria?

NO euphoria, MAOis have euphoria

How are 3* amines metabolized to 2* amines?

Demethylation

Imipramine-->

Desipramine

Amitriptyline-->

Nortriptyline

What is the tricyclic ring of TCAs metabolized by?

CYPs-->conjugation

What other drugs are CI with TCAs?

Alcohol: potentiate ANY other enruo drug, really Clonidine

What antidepressant probably has the least side effects?

Venlafaxine

What is first line depression therapy?

SSRIs: citalopram/fluozetine/paroxetine/sertraline/fluvoxamine

When is MAOi therapy indicated?

In patients unresponsive to other treatments and not suitable for electroconvulsive therapy.

What else are MAOis used in?

Panic disorder Agoraphobia (ironic, because these drugs have scary side effects)

Cold remedies, diet aids, stimulants with MAOis-->

Hypertensive reaction

Meperidine, dextromethorphan with MAOis-->

FEVER, delerium , seizures, death

Tyramine and SSRIs with MAOis-->

Serotonin syndrome

What are the advantages to anticonvulsants for mania over lithium?

You can increase the dose faster, get a quicker response, and better TI. BUT, there is less experience and we are not sure that they work well in severe disease.

What types of bipolar indicate lithium/anticonvulsant use?

Mild: anticonvulsant Severe: Lithium

What drug indicates liver monitoring?

Valproate

Antidepressants and Mood Stabilizers Flashcards

(62 cards)