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43 Cards in this Set
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Antidepressant drugs
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Tricyclic Antidepressants (TCAs)
Monoamine Oxidase Inhibitors(MAOIs) Selective Serotonin Reuptake Inhibitors (SSRI) |
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Tricyclic antidepressants
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Tertiary Amines Secondary Amines
--Imipramine --Desipramine --Amitryptyline --Nortryptyline |
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Monoamine oxidase Inhibitors
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Phenelzine
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SSRI
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Fluoxetine
Paroxetine Sertraline Citalopram Escitalopram |
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Other antidepressants
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Venlafaxine
Duloxetine Bupropion Trazodone |
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TCAs
Mechanism |
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 |
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TCAs
Pharmako kinetics |
1) Long Half life
2) Metabolized in Liver CYP3A3/4 and CYP2D6 3) Broken down to active metabolites |
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TCAs
Nortryptyline |
Least cardiotoxic
Least sedating |
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TCAs
Amitriptyline and Imipramine |
More sedating
More 5HT effect |
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TCAs
Nortriptyline and desipramine |
Less sedating
More NE effects |
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TCAs
Pharmacological effects CNS |
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 |
1) Cardiac depression
2) Increased irritability (torsades de pointes) 3) alpha 1 blockade: Postural hypotension |
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TCAs
Uses |
1) Depression
2) Panic Disorder 3) Pain: Chronic Pain, Headaches 4) Fibromyalgia 5) Enuresis 6) ADHD |
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TCAs
Side Effects Autonomic |
1) Caution in Benign Prostatic Hypertrophy
2) Cholinergic blockade 3) Constipation 4) Dry mouth |
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TCAs
Side effects Cardiovascular |
1) Orthostatic Hypotension
2) Tachycardia 3) Ventricular arrythmias |
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TCAs
CNS Side effects |
1) Sedation
2) Delirium( Toxic dose) 3) Weakness and fatigue |
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TCAs
Other Side effects |
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 |
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TCAs
Overdose |
1) Torasades de points
2) Severe hypotension 3) Seizures 4) Respiratory depression tx: phenytoin |
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TCAs
Drug interactions |
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 |
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TCAs
Serotonin Syndrome |
1) Hyperpyrexia
2) Convulsions 3) Coma |
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MAOI
Mechanism |
Irreversibly inhibits both MAO-A (5HT) and MAO-B (Dopamine)
Last choice drug |
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MAOI
Pharmacokinetics |
Absorbed orally
Metabolized in liver Long Half life: effects persist for 1-3 weeks after discontinuation |
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MAOI
Side effects |
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 |
Beer
Red Wine Cheese |
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MAOI
Treatment for Hypertensive crisis |
Phentolamine (alpha blocker)
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MAOIs
Overdose |
Aggitation
Hallucinations Serotonin Syndrome Hypo or hypertentsion |
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MAOI
Drug interactions |
1) Severe HTN
--Amphetamine --OTC alpha agonist --Buspirone 2) Serotonin Syndrome --Meperidine --Dextromethorphan --TCAs --SSRIs |
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SSRI
Mechanism of action |
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 |
1) Long Half life
2) Fluoxetine-->norfluoxetine 3) Inhibit CYP2D6 |
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SSRI
Uses |
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 |
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 |
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 |
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SSRI
Fluoxetine (Prozac) |
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 |
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SSRI
Sertraline (Zoloft) |
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) |
1)Shorter duration of action
2) Used in the Elderly 3) May cause sedation 4) Contraindicated in Pregnancy 5)Anorexia and nausea |
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SSRI
Citalopram and Escitalopram |
1) Faster onset (1-2 weeks)
2) Little effect on CYP2D6 |
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Inhibitors of NE and 5HT
Venlafaxine and Desvenlafaxine |
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 |
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Inhibitors of NE and 5HT
Duloxetine (Cymbalta) |
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 |
1) Inhibits reuptake of Dopamine
2) Extended release for smoking cessation 3) Reduces cravings |
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Other Antidepressants
Bupropion Side effects |
1) Weight loss
2) Anxiety 3) Insomnia 4) Seizures: contraindicated with history of seizures or head trauma 5) Unlikely to cause sexual dysfunction |
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Other Antidepressants
Trazodone |
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 |
1) sedation
2) Priapism |
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Other Antidepressants
St. Johns wort |
1) Sun sensitivity
2) Interaction with all antidepressants 3) Induces P450 many drug interactions |