CMN 548 Module 5 Psychopharmacology
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What are the two basic mechanisms for studying receptors?
Ans: - Measure the binding of a ligand (radioactively traced)
- Measure the physiologic consequences of agonist binding (and
effects of the antagonist)
How do didactic depictions of neurotransmitter signaling differ from
real life?
Ans: - There are hundreds to thousands of axons connecting to
one dendrite
- A single transmitter can evoke multiple pathways
Pharmacokinetic drug interactions are...
Ans: the effects of drugs on the PLASMA concentrations of
each other
Pharmacokinetic concepts describe and predict...
Ans: - the time course of drug concentration in different parts
of the body
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- onset, duration, absorption, distribution, metabolism,
excretion
Remission
Ans: - Preferred outcome of treatment
- Absolute score of 7 or less on the HAMD (Hamilton
depression) scale
- <10 on the MADRS (Montgomery-Asberg Depression Rating
Scale)
Responders are patients who...
Ans: improve but do not experience full resolution of
symptoms
- 50% of greater decrease from baseline on HAMD and MADRS
depression ratings
What is the probability of remission from OCD with SSRI treatment
over 3 years of treatment?
Ans: - 38% full remission
- 65% partial remission
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Withdrawal symptoms are worse with drugs that have this
pharmacokinetic property.
Ans: Short elimination half life
Which medications are most often associated with mentally and
physically distressing discontinuation reactions?
Ans: - Sedative hypnotics and opiates
- Barbiturate (part of the sedative hypnotic class) withdrawal
can be fatal
Which benzodiazepine produces more intense withdrawal symptoms
that it's counterparts?
Ans: Alprazolam (Xanax)
Which SSRI produces more intense withdrawal symptoms that it's
counterparts?
Ans: Paroxetine (Paxil)
Medications with this pharmacokinetic property have delayed
discontinuation symptoms.
Ans: Long elimination half life
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- Fluoxetine (Prozac, SSRI) has a long elimination half life of its
active metabolite
What is autoinhibition?
Ans: Dose dependent inhibition of a medication's own
metabolism
- Paroxetine (Paxil, SSRI) inhibits P450 CYP 2D6 which is what
metabolizes the medication
Bupropion (Wellbutrin, atypical antidepressant) inhibits this enzyme
system and paroxetine (Paxil, SSRI) is metabolized by it.
Ans: CYP 2D6
- Discontinuing bupropion would result in a rapid increase in
metabolism of Paroxetine and drop in plasma concentrations
- Paroxetine would need to be increased
What effect have sustained release alprazolam, paroxetine, and
venlafaxine had on withdrawal reactions?
Ans: None.
- They do not reduce severity of withdrawal because the long
half life is due to delayed absorption not prolonged elimination
- Only benefit is the in reduced dosing frequency
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