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Pharmacology Antidepressants Test| 81 Questions with Answers Verified 100% Correct
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Pharmacology Antidepressants Test| 81 Questions with Answers Verified 100% Correct
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Pharmacology Antidepressants Test| 81Questions with Answers Verified 100% Correct
Name the tricyclic antidepressants. - ✔✔• Amitriptyline
• Nortriptyline
• Imipramine
• Desipramine
• Clomipramine
What is the mechanism of action for TCAs? - ✔✔They *block the uptake of norepinephrine
and serotonin* by nerve terminals by competition for the binding site of the carrier protein;
this causes increased monoamine concentration in the cleft. In addition to their effects on
amine uptake, most TCAs also block α-adrenergic, muscarinic, histamine and 5-HT receptors.
Which TCAs tend to block SERT with higher affinity? Which prefer NET? - ✔✔Clomipramine
has very little affinity for NET but potently binds and blocks SERT. On the other hand,
desipramine and nortriptyline are more selective for NET.
How are TCAs given? Do they penetrate the CNS? - ✔✔TCAs are well absorbed upon oral
administration; they are lipophilic and therefore penetrate into the CNS; their lipophilicity also
causes these drugs to have variable half-lives.
Why is the bioavailability of TCAs low? - ✔✔As a result of variable first pass metabolism in
the liver, TCAs have low and inconsistent bioavailability. Therefore, the patient's response is
used to adjust dosage.
How are TCAs metabolized? - ✔✔TCAs are metabolized by the hepatic microsomal system
and conjugated with glucuronic acid; ultimately, TCAs are excreted as inactive metabolites via
the kidney.
, What are the adverse effects of TCAs? - ✔✔• Anti-muscarinic symptoms
• Cardiac overstimulation.
• TCAs slow cardiac conduction (Class I antiarrhythmics)
• Orthostatic hypotension and reflex tachycardia (α1)
• Sedation and weight gain (H1 blockade)
• Sexual effects are common (clomipramine)
What is the cause of TCA-induced arrhythmia? - ✔✔*TCAs inhibit cardiac fast sodium
channels*, resulting in arrhythmia and possibly death (very common with TCA intoxication).
Inhibition of sodium channels *prolongs phase-zero myocardial depolarization*, resulting in
decreased conduction with a *prolonged QRS complex and negative inotropic effects*.
How do TCAs interact with other drugs? - ✔✔• Elevations of TCA levels occur with CYP2D6
inhibitors
• Caucasians have a CYP2D6 polymorphism (slow met.)
• Worsening orthostatic hypotension with antihypertensives
What precautions should be taken with TCAs? - ✔✔• Narrow therapeutic index
• Depressed patients who are suicidal should be given only limited quantities of these drugs
and be monitored closely.
What are the signs of TCA overdose? - ✔✔The most common method used in suicide
attempts, overdose on TCAs can induce lethal arrhythmias (ventricular tachycardia and
fibrillation). Additionally, blood pressure changes and anticholinergic effects including altered
mental status and seizures are sometimes seen in TCA overdoses.
How is TCA overdose treated? - ✔✔Treatment includes cardiac monitoring, airway support
and gastric lavage. Sodium bicarbonate has been useful in reversing conduction block.
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