Anxiety and Depression Comparison of the Serotonergic Antidepressants Douglas L. Geenens, D.O. Faculty in Psychopharmacology, Menninger Associate Clinical Professor, University of Health Sciences, College of Osteopathic Medicine Assistant Clinical Professor, University of Missouri at Kansas City School of Medicine Adjunct Clinical Professor, University of Kansas School of Medicine
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Anxiety and Depression Comparison of the Serotonergic Antidepressants Douglas L. Geenens, D.O. Faculty in Psychopharmacology, Menninger Associate Clinical.
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Anxiety and DepressionComparison of the Serotonergic Antidepressants
Douglas L. Geenens, D.O.Faculty in Psychopharmacology, Menninger
Associate Clinical Professor, University of Health Sciences, College of Osteopathic Medicine
Assistant Clinical Professor, University of Missouri at Kansas City School of Medicine
Adjunct Clinical Professor, University of Kansas School of Medicine
Variables to Compare
• Research and Development
• Indications
• Efficacy
• Structure
• Pharmacodynamics*
• Pharmacokinetics*
• Side-effects*
• Dosing Preparations
• Cost Considerations
Currently Available in U.S.A.• fluoxetine (Prozac) 1988• sertraline (Zoloft) 1992• paroxetine (Paxil) 1993
• Paroxetine appears to cause higher rates of sexual dysfunction in most head to head studies. (potency and anti-ACH effects)
• Paroxetine may be the d.o.c. for premature ejaculation. (prolongs orgasmic latency 8 fold)
Rates of Sexual DysfunctionMontejo et al, 2001
• N = 1022– Celexa (28.7)
– Paxil (23.4)
– Effexor (159.5)
– Zoloft (90.4)
– Luvox (115.7)
– Prozac (24.5)
– Remeron (37.7)
– Serzone (324.6)
– 72.7%
– 70.7%
– 67.3%
– 62.9%
– 62.3%
– 57.7%
– 24.4%
– 8.0%
Dosing Preparations
• Similarities
• All available in tablets (fluoxetine 10 mg only).
• Differences
• Liquid preparations:– fluoxetine (mint)
– paroxetine (orange)
– sertraline (mint)
– citalopram (mint)
• Capsule preparation: fluoxetine
• Sustained release: paroxetine
Cost Considerations• fluoxetine:
– 10 mg scored tab, 10 and 20 mg pulvules are the same cost – 40 mg dose offers no cost savings.– 90 mg weekly is competitive – Generic preparation available
• sertraline: 25, 50, and 100 mg tablets are the same cost. All are scored.
• paroxetine: 10, 20, 30, 40 mg tablets are the same cost. 10 and 20 mg tablet are scored. 12.5, 25, 37.5 CR are the same cost.
• fluvoxamine: 25, 50, and 100 mg tabs. 50 and 100 mg tablets are scored.
• citalopram: 20 and 40 mg tablets are the same cost. Both doses are scored.
• S-citalopram: 10 and 20 mg tabs. Both doses are scored.
fluoxetine (Prozac)• Most US research across the diagnostic spectrum.
• Indicated for Bulimia, Geriatric Depression, and PMDD, plus two others.
• Longest half-life.
• Relatively fewer side effects.
• Potential for drug-drug interactions, especially psychiatric (2D6) is a concern.
• At doses below 10 mg, inexpensive.
• At higher doses, cost is incrementally higher. Some cost savings with weekly dose and generic prep.
• Available in a liquid dosing form (mint).
sertraline (Zoloft)
• Six indications, including PTSD, PMDD, and OCD in children.
• Most dopamine transporter blocking potency.
• Intermediate half-life with no active metabolites.
• Linear pharmacokinetics.
• Lower potential for drug-drug interactions.
• Relatively fewer side-effects (watch for GI).
• At lower doses, may be the most cost effective.
• Available in liquid dosing form (mint).
paroxetine (Paxil)• Indicated for Social Phobia, plus five others.
• Significantly more anti-ACH affinity, thus more anti-ACH side effects.
• Intermediate half-life, no active metabolites.
• Potential for drug-drug interactions, especially psychiatric (2D6) is of concern.
• Worst side effect profile and highest rates of sexual dysfunction. May be d.o.c. for premature ejaculation.
• Liquid preparation available (orange).
• At higher doses, may be the most cost effective.
• Available in sustained release form.
fluvoxamine (Luvox)
• Two indications, includes OCD in children.• Intermediate half-life, no active metabolites.
• Side-effect profile is relatively worse.• Dosing often requires titration.
• Highest potential for drug-drug interactions.• May be inexpensive at lower doses, and expensive
at higher doses.
citalopram (Celexa)• One indication, depression.
• Low potency at 5-HT reuptake blockade (60% at 40mg).
• Linear dose-response curve.
• Intermediate half-life. No active metabolites.
• Linear pharmacokinetics.
• Fewer side effects at low doses.
• Lower potential for drug-drug interactions.
• Cost effective throughout dosage range (40mg).
• Liquid preparation available (mint).
S-citalopram (Lexapro)
• Most selective of the SSRIs• Flat-dose response curve
• Potency of blocking 5-HT is comparable to sertraline
Beyond the SSRIs
• Effexor
• Serzone
• Remeron
• 5-HT, NE, and DA reuptake block.
• 5-HT2 block; weaker 5-HT and NE reuptake block.
• 5-HT and NE increase (via alpha 2 antagonism); 5-HT2 and 5-HT3 block.
Anxiety and DepressionComparison of the Serotonergic Antidepressants
Douglas L. Geenens, D.O.Faculty in Psychopharmacology, Menninger