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Psychopharmacology Weekly Question Series- Sertraline

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Solved Psychopharmacology Weekly Question Series- Sertraline

Post  Admin on Sat Feb 18, 2012 5:07 pm




Q.1: Which of the following statement is false regarding Sertraline:

(a) Sertraline is more potent at blocking Dopamine receptor uptake, than are other SSRIs or TCAs.
(b) Alpha-1 receptor antagonism of Sertraline is at least 10 fold more than that of other SSRIs.
(c) Among SSRIs, Sertraline is the most potent of all in blocking serotonin re-uptake.
(d) Peak plasma levels of Sertraline are somewhat lower in young males, compared to females and older males.
(e) Renal impairment does not appreciably influence the metabolism of Sertraline


Q.2: Which of the following statement is false regarding the Indication for Sertraline use:

(a) Sertraline is approved for use in children for the treatment of OCD.
(b) Sertraline is not more efficacious than placebo in patients with predominantly combat-related PTSD.
(c) Sertraline is not approved for use in children for the treatment of Social Anxiety Disorder.
(d) Sertraline can be used for the alleviation of hot flashes associated with menopause.
(e) Sertraline is not safe for the treatment of depression in patients with cardiovascular disease.



Q.3: Which of the following is most common side effect of Sertraline use:

(a) Insomnia, somnolence
(b) Diarrhea, Nausea
(c) Headache
(d) Ejaculation failure
(e) Dry mouth



Q.4: Which of the following drug combination with Sertraline is considered as "Risk X" drug interaction:

(a) Alcohol
(b) Lithium
(c) Aspirin
(d) Methylene Blue
(e) Warfarin

---------------------------------------------------------------------------------------------------------------------------

Answers Will be Posted Later this Week. Everyone is encouraged to participate in discussion. Share this weekly Question series with your friends and colleagues. Sharing your Knowledge is the Best way of Learning.



Last edited by Admin on Wed Mar 07, 2012 8:48 pm; edited 9 times in total

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Solved Re: Psychopharmacology Weekly Question Series- Sertraline

Post  P450 on Sat Feb 18, 2012 6:53 pm

(c) Among SSRIs, Sertraline is the most potent of all in blocking serotonin re-uptake.

False: I believe citalopram (maybe escitalopram) is the most potent inhibitor of the serotonin transporter.

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Solved Re: Psychopharmacology Weekly Question Series- Sertraline

Post  Admin on Sun Feb 19, 2012 3:26 pm

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Solved Re: Psychopharmacology Weekly Question Series- Sertraline

Post  P450 on Sun Feb 19, 2012 8:30 pm

Q.2: Which of the following statement is false regarding the Indication for Sertraline use:

(e) Sertraline is not safe for the treatment of depression in patients with cardiovascular disease.

False: According to data from SADHART, sertraline IS safe in depressed pt's with CV disease.

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Solved Re: Psychopharmacology Weekly Question Series- Sertraline

Post  Admin on Mon Feb 20, 2012 9:23 pm

Admin wrote:
Q.1: Which of the following statement is false regarding Sertraline:

(a) Sertraline is more potent at blocking Dopamine receptor uptake, than are other SSRIs or TCAs.
(b) Alpha-1 receptor antagonism of Sertraline is at least 10 fold more than that of other SSRIs.
(c) Among SSRIs, Sertraline is the most potent of all in blocking serotonin re-uptake.
(d) Peak plasma levels of Sertraline are somewhat lower in young males, compared to females and older males.
(e) Renal impairment does not appreciably influence the metabolism of Sertraline

Answer: (c)
Among the various SSRIs, Sertraline is second only to paroxetine in potency for 5-HT reuptake blockade.
Source:
- Hiemke C, Härtter S. Pharmacokinetics of selective serotonin reuptake inhibitors. Pharmacol Ther. 2000 Jan;85(1):11-28. Review. PubMed PMID: 10674711.
- Owens MJ, Knight DL, Nemeroff CB: Second-generation SSRIs: human monoamine transporter binding profile of escitalopram and R-fluoxetine. Soc Biol Psychiatry 50:345–350, 2001. PubMed PMID: 11543737.





Admin wrote: Q.2: Which of the following statement is false regarding the Indication for Sertraline use:

(a) Sertraline is approved for use in children for the treatment of OCD.
(b) Sertraline is not more efficacious than placebo in patients with predominantly combat-related PTSD.
(c) Sertraline is not approved for use in children for the treatment of Social Anxiety Disorder.
(d) Sertraline can be used for the alleviation of hot flashes associated with menopause.
(e) Sertraline is not safe for the treatment of depression in patients with cardiovascular disease.


Answer: (e)
Sertraline is one of the few antidepressants that has been shown to be safe and effective for the treatment of depression in patients with cardiovascular disease. While the mechanism of cardiovascular benefit is not entirely clear, sertraline may decrease platelet adherence, thus decreasing the likelihood of recurrent myocardial events.
Source:
- McFarlane A, Kamath M, Fallen E, et al: Effect of sertraline on the recovery rate of cardiac autonomic function in depressed patients after acute myocardial infarction. Am Heart J 142:617–623, 2001
- Shapiro P, Lesperance F, Frasure-Smith N, et al: An open-label preliminary trial of sertraline for treatment of major depression after acute myocardial infarction (the SADHAT Trial). Am Heart J 137:1100–1106, 1999.

Sertraline has also been shown to improve quality-of-life measurements in depressed patients with acute coronary syndrome and stroke.
Source:
- Swenson JR, O'Connor CM, Barton D, et al: Influence of depression and effect of treatment with sertraline on quality of life after hospitalization for acute coronary syndrome. Am J Cardiol 92:1271–1276, 2003
- Murray V, von Arbin M, Bartfai A, et al: Double-blind comparison of sertraline and placebo in stroke patients with minor depression and less severe major depression. J Clin Psychiatry 66:708–716, 2005

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Everyone is encouraged to try Question 3 & 4.
Answers will be posted later this week.



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Solved Re: Psychopharmacology Weekly Question Series- Sertraline

Post  P450 on Mon Feb 20, 2012 9:45 pm

Right on about q1. I was thinking about SERT inhibition selectivity with Citalopram and Escitalopram. Although in the SSRIs chapter of the latest K and S on table 31.27-2, escitalopram is second to paroxetine in terms of potency, then sertraline. Maybe some newer data!

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Solved Re: Psychopharmacology Weekly Question Series- Sertraline

Post  Admin on Mon Feb 20, 2012 10:01 pm

P450 wrote:Right on about q1. I was thinking about SERT inhibition selectivity with Citalopram and Escitalopram. Although in the SSRIs chapter of the latest K and S on table 31.27-2, escitalopram is second to paroxetine in terms of potency, then sertraline. Maybe some newer data!

Good point.
Here is the detailed explanation of article published by Owen et al.



Owens and colleagues have assayed the relative potency of escitalopram and other SSRIs in the inhibition of the neuronal uptake of the monoamine neurotransmitters serotonin (5-HT), norepinephrine (NE) and dopamine (DA).
A lower inhibitory constant (Ki) indicates that the compound produces inhibition at a lower concentration (represented in nanomoles per liter), i.e., it is more potent.
Escitalopram and the other SSRIs are potent and selective serotonin reuptake inhibitors, but the serotonin selectivity ratio (comparing the extent of serotonin reuptake inhibition to the extent of inhibition of norepinephrine reuptake) indicates that escitalopram is the most selective inhibitor of serotonin reuptake studied to date.

Both serotonergic and noradrenergic systems are thought to play a role in depression and in its treatment, and the selectivity of a compound to inhibit one transporter over another has not been associated with greater clinical efficacy. However, some of the CNS-related adverse effects associated with antidepressant therapy such as agitation, anxiety, nervousness, insomnia, and even tremor may be due to an increase in noradrenergic tone. Thus, treatment with an agent that has minimal effect on the noradrenergic system may result in a lower incidence of these side effects.

Reference
1. Owens MJ, Knight DL, Nemeroff CB. Second-generation SSRIs: human monoamine transporter binding profile of escitalopram and R-fluoxetine. Biol Psychiatry. 2001;50(5):345-350.

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Solved Re: Psychopharmacology Weekly Question Series- Sertraline

Post  Admin on Fri Feb 24, 2012 2:08 pm

Admin wrote:
Q.3: Which of the following is most common side effect of Sertraline use:

(a) Insomnia, somnolence
(b) Diarrhea, Nausea
(c) Headache
(d) Ejaculation failure
(e) Dry mouth

Answer- (b) Diarrhea, Nausea

Common Side Effects includes:
- Gastrointestinal disturbance (nausea, 27%; diarrhea/loose stools, 21%)
- Sleep disturbance (insomnia, 22%; somnolence, 14%)
- Headache (26%)
- Dry mouth (15%), and
- Sexual dysfunction (ejaculation failure, 14%; decreased libido, 6%).


Admin wrote:] Q.4: Which of the following drug combination with Sertraline is considered as "Risk X" drug interaction:

(a) Alcohol
(b) Lithium
(c) Aspirin
(d) Methylene Blue
(e) Warfarin

Answer- (d) Methylene Blue

Alcohol: "Risk D" (consider therapy modification)
Aspirin: "Risk C" (Monitor Therapy)
Lithium: "Risk C" (Monitor Therapy)
Warfarin: "Risk C" (Monitor Therapy)

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