Pharm Winter Exam 1 Antidepressants

Front 1

Antidepressant drugs

Back 1

Tricyclic Antidepressants (TCAs)
Monoamine Oxidase Inhibitors(MAOIs)
Selective Serotonin Reuptake Inhibitors (SSRI)

Front 2

Tricyclic antidepressants

Back 2

Tertiary Amines Secondary Amines
--Imipramine --Desipramine
--Amitryptyline --Nortryptyline

Front 3

Monoamine oxidase Inhibitors

Back 3

Phenelzine

Front 4

SSRI

Back 4

Fluoxetine
Paroxetine
Sertraline
Citalopram
Escitalopram

Front 5

Other antidepressants

Back 5

Venlafaxine
Duloxetine
Bupropion
Trazodone

Front 6

TCAs

Mechanism

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1) Inhibit the uptake of NE and 5HT
2) Block Muscarinic, alpha adrenergic, and histamine receptors
3)Not a stimulant
4) No euphoria
5) 2-3 weeks until begins to work

Front 7

TCAs

Pharmako kinetics

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1) Long Half life
2) Metabolized in Liver CYP3A3/4 and CYP2D6
3) Broken down to active metabolites

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TCAs

Nortryptyline

Back 8

Least cardiotoxic
Least sedating

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TCAs

Amitriptyline and Imipramine

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More sedating
More 5HT effect

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TCAs

Nortriptyline and desipramine

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Less sedating
More NE effects

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TCAs

Pharmacological effects CNS

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1) Drowsiness and sedation (histamine blockade) Tolerance develops
2) Impairment in memory and cognition (anticholinergic)
3) Analgesia in spinal chord, reduced substance P

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TCAs

Pharmacological effects peripheral

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1) Cardiac depression
2) Increased irritability (torsades de pointes)
3) alpha 1 blockade: Postural hypotension

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TCAs

Uses

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1) Depression
2) Panic Disorder
3) Pain: Chronic Pain, Headaches
4) Fibromyalgia
5) Enuresis
6) ADHD

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TCAs

Side Effects Autonomic

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1) Caution in Benign Prostatic Hypertrophy
2) Cholinergic blockade
3) Constipation
4) Dry mouth

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TCAs

Side effects Cardiovascular

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1) Orthostatic Hypotension
2) Tachycardia
3) Ventricular arrythmias

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TCAs

CNS Side effects

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1) Sedation
2) Delirium( Toxic dose)
3) Weakness and fatigue

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TCAs

Other Side effects

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1) Weight gain
2) Decrease Seizure Threshold
3) SIADH
4) Sexual Dysfunction
5) Tolerance occurs
6) Can be used in Pregnancy
7) Malaise and muscle aches if suddenly discontinued

Front 18

TCAs

Overdose

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1) Torasades de points
2) Severe hypotension
3) Seizures
4) Respiratory depression
tx: phenytoin

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TCAs

Drug interactions

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1) MAOIs: serotonin syndrome
2) Fluoxetine: TCA toxicity
3) Effect of Clonidine inhibited
4) Sympathomimetic: Hypertension
5) Cocaine: Arrythmias
6) Alcohol: increase sedation
7) Potentiate effect of anticholinergic

Front 20

TCAs

Serotonin Syndrome

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1) Hyperpyrexia
2) Convulsions
3) Coma

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MAOI

Mechanism

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Irreversibly inhibits both MAO-A (5HT) and MAO-B (Dopamine)

Last choice drug

Front 22

MAOI

Pharmacokinetics

Back 22

Absorbed orally
Metabolized in liver
Long Half life: effects persist for 1-3 weeks after discontinuation

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MAOI

Side effects

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1) HYPERTENSIVE CRISIS: Caused by increased tyramine.
Or sympathomimetic drugs
2) Orthostatic hypotension
3) Weight gain
4) Anticholinergic effects

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MAOI

Tyramine containing food

Back 24

Beer
Red Wine
Cheese

Front 25

MAOI

Treatment for Hypertensive crisis

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Phentolamine (alpha blocker)

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MAOIs

Overdose

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Aggitation
Hallucinations
Serotonin Syndrome
Hypo or hypertentsion

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MAOI

Drug interactions

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1) Severe HTN
--Amphetamine
--OTC alpha agonist
--Buspirone
2) Serotonin Syndrome
--Meperidine
--Dextromethorphan
--TCAs
--SSRIs

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SSRI

Mechanism of action

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1) Inhibit reuptake of serotonin
2) As effective as TCAs
3) Take 2-3 weeks to start working
4) Mild side effect profile
5) May alter expression of 5HT receptors long term

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SSRI

Pharmacokinetics

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1) Long Half life
2) Fluoxetine-->norfluoxetine
3) Inhibit CYP2D6

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SSRI

Uses

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1) Depression
2) Panic Disorder
3) OCD (clomipramine and paroxetine)
4) Social anxiety (Paroxetine)
5) Alcoholism
6) Bulimia

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SSRI

Side effects

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1) Gastrointestinal
2) Weight loss initially
3) Weight Gain long term
4) CNS stimulation
5) Sexual Dysfunction
6)Photosensitivity

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SSRI

Drug interactions

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1) MAOI, St. Johns wart, amphetamine: Serotonin syndrome
2) TCA Toxicity
3) Warfarin:Bleeding
4) Phenytoin or carbamazepine toxicity
5)Beta blockers or Calcium channel blockers: Hypotension, heart block
6) Opioids: Less effective

Front 33

SSRI

Fluoxetine (Prozac)

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1) Very long duration of effect
2) Wait 5 weeks after discontinuing before starting new antidepressant
3) Also inhibits Reuptake of NE
4) May cause Insomnia
5) Inhibits CYP2D6

Front 34

SSRI

Sertraline (Zoloft)

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Compared to Fluoxetine:
1) More serotonin selective
2) Less side effects
3) Less drug interactions
4) Shorter duration of action

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SSRI

Paroxetine (Paxil)

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1)Shorter duration of action
2) Used in the Elderly
3) May cause sedation
4) Contraindicated in Pregnancy
5)Anorexia and nausea

Front 36

SSRI

Citalopram and Escitalopram

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1) Faster onset (1-2 weeks)
2) Little effect on CYP2D6

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Inhibitors of NE and 5HT

Venlafaxine and Desvenlafaxine

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1) Inhibit reuptake of both 5HT and NE
2) May be more effective in some pts
3) More side effects that other SSRIs
--increased BP
--SIADH

Front 38

Inhibitors of NE and 5HT

Duloxetine (Cymbalta)

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1) More effective in treating depression
2) Treats physical symptoms also
3) May be hepatotoxic- do not give to any one with liver disease

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Other Antidepressants

Bupropion

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1) Inhibits reuptake of Dopamine
2) Extended release for smoking cessation
3) Reduces cravings

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Other Antidepressants

Bupropion Side effects

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1) Weight loss
2) Anxiety
3) Insomnia
4) Seizures: contraindicated with history of seizures or head trauma
5) Unlikely to cause sexual dysfunction

Front 41

Other Antidepressants

Trazodone

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1) Partial 5HT1A receptor agonist and may block 5HT2A
2) Sleep aid
3) Pain Managment
4) not a good antidepressant

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Other Antidepressants

Trazodone Side effects

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1) sedation
2) Priapism

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Other Antidepressants

St. Johns wort

Back 43

1) Sun sensitivity
2) Interaction with all antidepressants
3) Induces P450 many drug interactions