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Antidepressant1

Dynamics quiz3

QuestionAnswer
What are TCAs (secondary amines) Desiprimine, Nortriptyline, Protriptyline, Maprotiline, Amoxapine
What are TCAs (tertiary amines) Imipramine, Amitriptyline, Trimiprimine, Doxepin, Clomipramine
Which alpha receptor does TCA mainly binds? alpha 1
TCA are non-selective so which other receptors does it effect? Adrenergic, Histaminergic, and Cholinergic
What are the side effects of TCAs blocking at cholingeric (muscarinic)receptors Anti-SLUDGE * effects can be significant
What are the side effects of TCAs blocking at Histamine Receptors (H1, H2) Sedation and weight gain - tertiary > secondary
What are the side effects of TCAs blocking at adrenergic receptors: Orthostatic hypotension (vasodialation --> decrease BP), reflex tachycardia - tertiary > secondary
TCAs Cardiovascular Side Effects Palpitations, orthostatic hypotension, sinus tachycardia, potential for arrhythmias
TCAs should be given cautiously with what type of patients? TCAs are contraindicated with pts at early recovery from MI. Caution in pts: Advanced cardiovascular disease, CHF, orthostatic hypotension
Why not to give TCAs to patients who are suicidal? Patients may use TCAs to OD. However, if SSRIs do not work, MD may prescribe TCAs for 1 week use.
What should pharmacist counsel TCAs patients? Will develop tolerance to side effects - anticholinergic effects and autonomic effects. * Less tolerance to wt. gain.
What are the side effects that patients of TCAs can develop tolerance? Anticholinergic effects: anti-SLUDGE
Drug Interactions of TCAs (Sedative) Worsen sedation - alcohol, antihistamines, and sedative hypnotics
Drug Interactions of TCAs (Hypotension) Worsen hypotension - alpha- methyldopa, beta-blockers, Clonidine (alpha 2 agonist)
Additive anticholingeric toxicity Antihistamines, antiparkinsonians, and antipsychotics (non-specific)
TCAs acute poisoning treatment No antagonist! Manange CV symptoms in ER or ICU. Use gastic lavage/charcoal to remove? Treat seizures with diazepam.
Selective Serotonin Reuptake Inhibitor More specific so less activity at cholinergic and adrenergic receptors.
Fluoxetine Prozac: SSRI - OCD, Panic disorder
Paroxetine Paxil: SSRI - GAD (Gen. anxiety disorder), OCD, Panic/Social Phobia, PTSD
Sertratline Zolof: SSRI - OCD, Panic/Social Phobia, PTSD
Fluvoxamine Luvox -SSRI- panic disorder/agoraphobia is the only labeled use
Citalopram Celexa - SSRI
Escitalopram Lexapro - SSRI - GAD
Advantages of SSRIs Fewer autonomic side effects than TCAs - so rarely cause cardiac arrhythmias, Increase alertness - usu. take in am. Less sedation than TCAs. Wide therapeutic window.
Significant of SSRIs Structures Many different structure so more flexibility.
SSRI Pharmacokinetics Hepatic CYP P450 metabolism. SSRIs can inhibit the activity of CYP 450. Therefore, inc. drugs serum level that metabolize by P450.
Fluoxetine and cytochrome P450 Inhibits cytochrome P450 isozymes responsible for elimination of TCA’s, neuroleptic drugs, antiarrhythmic, beta-adrenergic antagonists
What are Fluoxetine adverse effects? Adverse effects: Nausea; Diarrhea; Abdominal pain, Anxiety; Akathisia; Agitation, Insomnia, Minimal CV effects, Sexual dysfunction
Created by: MatthewN
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