Mental Health Book

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Nefazodone

Aka: Nefazodone, Serzone
  1. Mechanism
    1. Serotonin Antagonist and Reuptake Inhibitor
      1. Binds postsynaptic Serotonin-2 Receptor (5-HT-2)
      2. More Serotonin binds Serotonin-1 Receptor (5-HT-1)
        1. Anti-depressant effect
      3. Blocks 5-HT-2 Activity
        1. Blocks 5-HT-2 inhibition of 5-HT-1
        2. Blocks Sexual Dysfunction
        3. Blocks Insomnia and anxiety effects
    2. Phenylpiperazine related to Trazodone (Desyrel)
      1. Less Sedation than Trazodone
      2. Less Orthostasis than Trazodone
      3. No Priapism
  2. Background
    1. Costs: $50 per month
  3. Indications
    1. Major Depression
      1. Consider for severe Refractory Depression Management
    2. Anxiety Disorder
    3. Post-Traumatic Stress Disorder (PTSD)
  4. Contraindications
    1. Liver disease
    2. Concurrent medication use
      1. Cisapride
      2. MAO inhibitor
      3. Triazolam
      4. Terfenadine
      5. Astemizole
  5. Efficacy
    1. Shown to be as effective as Imipramine
    2. No comparison trials with SSRIs
  6. Pharmacokinetics
    1. Half life: 18 hours
    2. Steady state in 4-5 days
    3. Inhibits cytochrome P450 3A4
    4. Clearance decreased
      1. Elderly
      2. Hepatic dysfunction
  7. Dosing: General
    1. Start: 100 mg PO qhs for 3 days
    2. Twice daily dosing (FDA approved dosing, or anxiety)
      1. Next: 100 mg PO bid for 7 days
      2. Next: Increase at 1 week intervals to 300 mg PO bid
    3. Once daily dosing (typical dosing by psychiatrists)
      1. Next: 200 mg PO qhs for 7 days
      2. Next: Increase at 1 week intervals upto 600 mg PO qhs
    4. Maximum: 600 mg per day
  8. Dosing: Elderly over age 65 years
    1. Start: 50 mg PO bid
    2. Next: 50-200 mg PO bid
  9. Advantages
    1. Less Sexual Dysfunction than SSRIs
    2. Minimal agitation compared with SSRIs
    3. Rapid onset
    4. May increase REM Sleep
    5. No cardiotoxicity
  10. Precautions
    1. Risk of liver failure (one per 250,000)
    2. Contraindicated in comorbid liver disease
    3. Patient and physician watch closely for hepatotoxicity
    4. Consider Liver Function Testing
  11. Adverse effects (May be intolerable)
    1. Sedation (limiting adverse effect)
      1. Some psychiatrists dose only in evening
    2. Anticholinergic Symptoms increased over SSRIs
      1. Confusion
      2. Dry Mouth
      3. Constipation
      4. Nausea
      5. Dizziness
      6. Blurred vision
    3. Other Adverse Effects
      1. Postural Hypotension
      2. Headaches
    4. Anxiety may occur due to metabolite (mCPP)
      1. See Drug Interactions below
  12. Drug Interactions
    1. Stop MAO inhibitor 14 days prior to starting Serzone
    2. Inhibits Cytochrome P450 system (CYP3A4, CYP2D6)
      1. Metabolite mCPP cleared by Cytochrome P450-2D6
        1. Paxil and Prozac inhibit Cytochrome P450-2D6
        2. Excess mCPP (decreased clearance) causes agitation
      2. Decreased clearance of
        1. Antihistamines
        2. Alprazolam
        3. Triazolam
  13. References
    1. (1995) Med Lett Drugs Ther 37(946): 33-34 [PubMed]
    2. Sundberg (1995) Depression Primary Care, PGM, p. 45-57
Medication Costs
nefazodone (on 12/21/2016 at Medicaid.Gov Pharmacy Drug pricing)
NEFAZODONE HCL 100 MG TABLET Generic $1.29 each
NEFAZODONE HCL 150 MG TABLET Generic $1.29 each
NEFAZODONE HCL 200 MG TABLET Generic $1.31 each
NEFAZODONE HCL 250 MG TABLET Generic $1.46 each
FPNotebook does not benefit financially from showing this medication data or their pharmacy links. This information is provided only to help medical providers and their patients see relative costs. Insurance plans negotiate lower medication prices with suppliers. Prices shown here are out of pocket, non-negotiated rates. See Needy Meds for financial assistance information.

nefazodone (C0068485)

Definition (NCI_NCI-GLOSS) A drug used to treat depression. It belongs to the family of drugs called antidepressant agents.
Concepts Pharmacologic Substance (T121) , Organic Chemical (T109)
MSH C051752
SnomedCT 108435006, 372491002
LNC LP18140-1, MTHU003461
English nefazodone, nefazodone [Chemical/Ingredient], NEFAZODONE, Nefazodone, Nefazodone (product), Nefazodone (substance)
Spanish nefazodona (producto), nefazodona (sustancia), nefazodona
Sources
Derived from the NIH UMLS (Unified Medical Language System)


Serzone (C0591424)

Concepts Pharmacologic Substance (T121) , Organic Chemical (T109)
MSH C051752
English serzone, dutonin, Dutonin, Bristol-Myers Squibb brand of nefazodone hydrochloride, Bristol-Myers brand of nefazodone hydrochloride, Serzone
Sources
Derived from the NIH UMLS (Unified Medical Language System)


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