Fluvoxamine.

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Presentation transcript:

Fluvoxamine

Overview Effects on s1 receptor FDA-approved for OCD but not for depression Potential DDI through inhibition of CYP 450 isoenzymes Dosage range of 100-300 mg/day

Pharmacology and MOA

Pharmacodynamics SERT inhibition Sigma 1 agonism Hindmarch, I., & Hashimoto, K. (2010). Cognition and depression: the effects of fluvoxamine, a sigma‐1 receptor agonist, reconsidered. Human Psychopharmacology: Clinical and Experimental, 25(3), 193-200. Schatzberg, Alan F., and Charles B. Nemeroff, eds. The American psychiatric publishing textbook of psychopharmacology. American Psychiatric Pub, 2009.

Clinical Uses

FDA-Approved Indications Fluvoxamine Fluvoxamine CR OCD X Social Anxiety Disorder x Depression: approved in Europe, Australia, Latin America and other countries.

Other clinical uses Anxiety disorders Panic disorder Generalized anxiety disorder Posttraumatic stress disorder Schatzberg, Alan F., and Charles B. Nemeroff, eds. The American psychiatric publishing textbook of psychopharmacology. American Psychiatric Pub, 2009.

Pharmacokinetics

Fluvoxamine pharmacokinetics Half-life 9-28 hours CYP 450 Inhibits a number of CYP 450 isoenzymes

Fluvoxamine inhibits CYP1A2 and CYP3A4 Also: CYP 2C9 and CYP 2C19 Luvox CR (Fluvoxamine CR) [Prescribing Information]. Palo Alto, CA: Jazz Pharmaceuticals, Inc. Accessed May 2014 Schatzberg, Alan F., and Charles B. Nemeroff, eds. The American psychiatric publishing textbook of psychopharmacology. American Psychiatric Pub, 2009.

CYP450 3A4 Potential Interactions Can reduce the clearance of: Antipsychotics: Pimozide Thioridazine Benzodiazepines: Alprazolam Diazepam Carbamazepine Luvox CR (Fluvoxamine CR) [Prescribing Information]. Palo Alto, CA: Jazz Pharmaceuticals, Inc. Accessed May 2014 Schatzberg, Alan F., and Charles B. Nemeroff, eds. The American psychiatric publishing textbook of psychopharmacology. American Psychiatric Pub, 2009.

CYP450 1A2 Potential Interactions Can increase levels of: Clozapine Theophyline Tizanidine Luvox CR (Fluvoxamine CR) [Prescribing Information]. Palo Alto, CA: Jazz Pharmaceuticals, Inc. Accessed May 2014 Schatzberg, Alan F., and Charles B. Nemeroff, eds. The American psychiatric publishing textbook of psychopharmacology. American Psychiatric Pub, 2009.

Adverse Effects

Adverse effects Postmarketing clinical studies: Pregnancy category C Nausea Somnolence Asthenia Weight gain: “no transient or negligible effect” Pregnancy category C Serretti, A., & Mandelli, L. (2010). Antidepressants and body weight: a comprehensive review and meta-analysis. The Journal of clinical psychiatry,71(10), 1259-1272. Sadock, B J., V A. Sadock, and P Ruiz. Kaplan and Sadock's Comprehensive Textbook of Psychiatry. 9th ed. Philadelphia: Lippincott Williams & Wilkins, 2009.

Prescribing information

Dosage range Dose OCD 100-300 mg/day Social anxiety disorder Depression Starting dose: 50 mg at bedtime, increase by 50 mg every 4 to 7 days. Sadock, B J., V A. Sadock, and P Ruiz. Kaplan and Sadock's Comprehensive Textbook of Psychiatry. 9th ed. Philadelphia: Lippincott Williams & Wilkins, 2009. Luvox CR (Fluvoxamine CR) [Prescribing Information]. Palo Alto, CA: Jazz Pharmaceuticals, Inc. Accessed May 2014

Dosage forms Strength Tablets 25 mg, 50 mg scored, 100 mg scored Twice daily (if higher than 100 mg/day) Capsules (Controlled Release) 100 mg, 150 mg Once daily Sadock, B J., V A. Sadock, and P Ruiz. Kaplan and Sadock's Comprehensive Textbook of Psychiatry. 9th ed. Philadelphia: Lippincott Williams & Wilkins, 2009. Luvox CR (Fluvoxamine CR) [Prescribing Information]. Palo Alto, CA: Jazz Pharmaceuticals, Inc. Accessed May 2014