II. Mechanism
III. Indications
IV. Background
V. Safety
- Pregnancy
- Most commonly used SSRI in pregnancy, and preferred agent
- Low first trimester pregnancy risk
- But has been associated with increased risk of atrial and ventricular defects and Craniosynostosis
- Bérard (2015) Am J Obstet Gynecol 212(6):795.e1-795.e12 +PMID: 25637841 [PubMed]
-
Lactation
- Consider safe in Lactation (poorly secreted into Breast Milk)
VI. Preparations
- Tablets (Scored): 25, 50, 100 mg
- Oral concentrate: 20 mg/ml (60 ml bottle)
VII. Dosing
- Start
- Children (ages 6-12 years of age): 25 mg orally each morning
- Adults (and children over age 12): 50 mg orally each morning
- Elderly: 25 mg orally each morning
- Titrate
- Adults: Increase by 50 mg every 2 weeks
- Maximum: 200 mg per day
VIII. Drug Interactions
- Significantly raises Pimozide levels
- Concurrent use with Pimozide is contraindicated
- Metabolized by Cytochrome P450 2C9, 2C19, 2D6 and 3A4
- Moderate Cytochrome P450-2D6 Inhibitor
- Also inhibits Cytochrome P450-2C and P450-3A4
- Clinically Significant interactions are uncommon
- Highly Protein bound
- Interacts with other Protein bound medications (but does not appear to significantly affect their drug levels)
- Absorption affected by food intake
- Raises Tricyclic Antidepressant levels
- Allow two week wash-out prior to starting MAO Inhibitor
IX. Pharmacokinetics
- Half Life: 1 to 4 days
- Therapeutic Blood level 9.5 to 56 ng/ml
X. Adverse Effects
- See Antidepressant Adverse Effects
- Increased risk of Gastrointestinal Bleeding
- Neutral on the sedation to excitation continuum
- Anxiety, Insomnia or other sleep disturbance
-
Diarrhea or gastrointestinal upset
- Diarrhea more common than with Fluoxetine
- Usually resolves within 2 weeks
-
Sexual Dysfunction may be more common
- Includes decreased libido
- See Antidepressant Induced Sexual Dysfunction
-
Antidepressant Withdrawal symptoms on stopping
- Taper 50 mg per every 5-7 days
- Taper to 25-50 mg daily before stopping
XI. Resources
XII. References
- (2023) Med Lett Drugs Ther 62(1592): 25-32
- Olson (2020) Clinical Pharmacology, Medmaster Miami, p. 38-9
- Hamilton (2020) Tarascon Pocket Pharmacopoeia
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