SSRI

Page 1

Comparison of Commonly Used Antidepressants Generic Name/ Brand Name

Daily Dose

Adverse Effects Anti-cholinergic

Arrhythmias

Interactions Sedation

Additional Information

Weight Gain

Dopamine Reuptake Blocking Agents Bupropion

200 to 450

--

+

--

--

Moderate inhibitor of CYP 2D6

-Contraindicated in patients with or at an increased risk of seizures Lowest sexual dysfunction

Mirtazapine Remeron

30 to 60

+

--

+++

+++

No significant interactions

-Administer dose at bedtime Chronic disease/HIV and cancer

--

--

--

+

Moderate inhibitor of CYP 2D6 at higher doses

-Administer a reduced dose (20 mg daily) to the elderly and those with hepatic impairment Lowest potential drug-drug interactions

Selective Serotonin Reuptake Inhibitors Citalopram/ Celexa Escitalopram/ Lexapro

20 to 60

Fluoxetine/ Prozac Sarafem

Adults 20 to 80

--

--

--

+

Potent inhibitor of CYP 2D6 and 3A4

-Discontinue fluoxetine 7 days prior to starting weekly fluoxetine -Administer a reduced dose to the elderly and those with hepatic impairment

Fluvoxamine/ Luvox

Adults 100 to 300

--

--

--

+

Potent inhibitor of CYP 1A2, 2C19, 3A4

Drug-drug Interactions

Paroxetine/ Paxil Paxil CR

20 to 50 25 to 62.5

+

--

+

++

Potent inhibitor of CYP 2D6

-Administer a reduced dose (20 mg daily) to the elderly and those with hepatic or severe renal impairment

Sertraline/ Zoloft

Adults 100 to 200

--

--

--

+

Moderate inhibitor of CYP

Lowest potential drug-drug interactions

10 to 20

Serotonin Norepinephrine Reuptake Inhibitors Duloxetine/ Cymbalta

40 to 60

--

--

+

--

Inhibits CYP 2D6

-Contraindicated in patients with uncontrolled narrow-angle glaucoma

Venlafaxine/ Effexor Effexor XR

150 to 375 75 to 225

+

+

+

--

No significant interactions

-Blood pressure can increase -Reduce daily dose by 25% to 50% in hemodialysis patients - Potential withdrawal effects

+

--

+

--

Potent inhibitor of CYP 3A4

-Concomitant use with carbamazepine (Tegretol) is contraindindicated -Concomitant use with triazolam (Halcion) is not recommended; decrease triazolam dose by 75% if given with nefazodone -Life-threatening hepatic failure has occurred

Serotonin-2 Receptor Antagonists Nefazodone/ Serzone

300 to 600

Ali Olyaei PharmD, 2005 Important Note: This document is a guideline, and not a policy statement. Always use clinical judgment when making decisions for an individual patient


Duloxetine (Cymbalta) Introduction: Approximately 15% of the general population will experience a major depressive (MDD) event at some point in their lives. A depressive event occurs more often in women than in men. A possible cause of depression is a medical illness, either through psychological stress, the disease itself, or the pharmacological treatment. Neuroendocrine hormonal variations can also contribute to the etiology of MDD, especially when combined with environmental stressors (e.g., death of a relative, assault, or severe relationship issues) An important aim of drug development has been to retain efficacy while reducing side effects and toxicity. It is now clear that selective serotonin reuptake inhibitors (SSRIs) are more effective than noradrenaline reuptake inhibitors (NARIs) in the treatment of obsessional compulsive disorder, and obsessional features in depression predict a responsivity to SSRIs. Furthermore, panic disorder and depression may be more responsive to SSRIs than NARIs. However, there is evidence that inhibition of both sites produces slightly greater efficacy and the addition of an NARI has been reported to potentiate the antidepressant effect of SSRIs Venlafaxine (Effexor速) became the first agent in a category of antidepressants known as the SSNRIs. It lacks the adverse effects of TCAs while implementing the combined antagonism of 5-HT and NE. This mechanism may lead to a more rapid onset of therapeutic effect. Unfortunately, venlafaxine has the potential to increase blood pressure in a dose-dependent manner in approximately 3-13% of patients. Duloxetine is a new addition to the SSNRIs, and it appears to exhibit a greater balance in the relative reuptake inhibition of 5HT and NE. Duloxetine has been shown to be a potent inhibitor of 5-HT and NE reuptake and a weak inhibitor of DA reuptake. Pharmacokinetics: The elimination half-life for duloxetine is approximately 12 hours, with a range of 8-17 hours. Administration with food may delay the maximum concentration (Cmax) by approximately 4 hours (from 6 to 10 hours), and it may also decrease the extent of absorption (AUC) by 10%. Duloxetine is highly protein bound (>90%). It is metabolized by hepatic oxidation through the cytochrome P450 (CYP) 2D6 and 1A2 isoenzymes. The majority (70%) of the metabolites are eliminated in the urine and only 20% are excreted in feces. Unchanged duloxetine represents only 1-3% of the total excreted products. Dosing and Administration: The recommended oral dose for initiation of therapy in MDD is 40 mg/day (administered as 20 mg twice daily) to 60 mg/day (administered either as once daily or as 30 mg twice daily). The recommended dose for diabetic peripheral neuropathic pain is 60 mg daily. Although doses up to 120 mg/day have been utilized, no clinical superiority has been demonstrated when compared to 60 mg/day and an increase of adverse events were noted at higher doses. Withdrawal: Abrupt discontinuation of duloxetine should be avoided if possible. Withdrawal symptoms such as headache, nausea, dizziness, abnormal dreams, sensory


Turn static files into dynamic content formats.

Create a flipbook
Issuu converts static files into: digital portfolios, online yearbooks, online catalogs, digital photo albums and more. Sign up and create your flipbook.