Med Chem Tutoring for Antidepressants

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Presentation transcript:

Med Chem Tutoring for Antidepressants By Alaina Darby

Which of the following does not inhibit DAT but inhibits both NET and SERT? SNRIs SSRIs NSRIs DNRIs C

Which of the following selectively inhibits NET with no significant affinity to SERT or DAT? SNRIs SSRIs NSRIs DNRIs A

Which of the following inhibits dopamine and norepinephrine reuptake but has little effect on serotonin? SNRIs SSRIs NSRIs DNRIs D

Which of the following has high selectivity and affinity for SERT with low affinity for neuroreceptors or fast sodium channels? SNRIs SSRIs NSRIs DNRIs B

Which of the following are tertiary TCA amines? SNRIs SSRIs NSRIs DNRIs C

Which of the following are secondary TCA amines? SNRIs SSRIs NSRIs DNRIs A

Which of the following is also an atypical antipsychotic? Protriptyline Nortriptyline Amoxapine Desipramine C

Which of the following is not true of tricyclic structures? Can be a 6-7-6 ring system Associated with affinity to particular receptors Restricts motility of the two phenyl rings Can be a 6-6-6 ring system B

Which of the following is the active metabolite of a NSRI? Loxapine Imipramine Amitriptyline Amoxapine D

Which of the following blocks D2 receptors? Loxapine Imipramine Amitriptyline Amoxapine D

Which of the following has the highest affinity and selectivity for NET among the secondary TCAs? Amoxapine Protriptyline Maprotiline Nortriptyline C Also referred to as a tetracyclic antidepressant

Which is not true of the sar for TCAs? Usually substituted benzene rings C-3 ring substituent on the benzene ring generally has little effect on antidepressant activity A Cl substitution at C-3 makes it more selective for serotonin uptake The central ring reduces conformational flexibility of the phenyl rings A

Which is true of the sar for TCAs concerning the side chains? The side chain is never involved in a ring system Branching increases potency for transporter inhibition Usually consists of three carbon atoms separating the nitrogen and tricyclic rings Branching decreases selectivity against serotonin uptake C

Remember Primary: not active Secondary: NET selective Tertiary: NET and SERT C

Which of the following is not a receptor that is blocked by TCAs? Muscarinic Alpha 1 H1 GABA Fast sodium channels All of the above are blocked D

Which of the following is not an advantage of SSRI vs TCA? Lower side chance of cardiotoxicity Fewer side effects Lower chance of suicide Better tolerated C

For which of the following is the S-isomer about 100x more selective than the r-isomer? Paroxetine Fluoxetine Citalopram Sertraline B Citalopram S-isomer is 27x more potent

Which of the following is primarily metabolized by CYP2D6 and acts to inhibit it? Paroxetine Fluoxetine Citalopram Sertraline A Sertraline just inhibits it

Which of the following has two chiral centers? Paroxetine Fluvoxamine Citalopram Sertraline D

Which of the following has lower drug concentrations in smokers? Paroxetine Fluvoxamine Citalopram Sertraline B Metabolized by 1A2

Which of the following is considered to be the most powerful antidepressant made to date? Clomipramine Amitriptyline Trimipramine Doxepin A

Which of the following is the z-isomer more potent for sert? Clomipramine Amitriptyline Trimipramine Doxepin D

Which of the following is a phenylpiperazone derivative that can cause sedation due to h1R blockade? Trazadone Aripiprazole Vilazodone Mirtazapine A

Which of the following is used in conjunction with lithium for bipolar disorder? Trazadone Aripiprazole Vilazodone Mirtazapine B

Which of the following is usually classified as a NaSSA? Trazadone Aripiprazole Vilazodone Mirtazapine D