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Nefazodone
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| Systematic (IUPAC) name | |
| 2-[[3-[4-(3-chlorophenyl)-1-piperazinyl]]propyl]-5-ethyl-2,4-dihydro-4-(2-phenoxyethyl)-3H-1,2,4-triazol-3-one | |
| Identifiers | |
| CAS number | |
| ATC code | N06 |
| PubChem | |
| DrugBank | |
| Chemical data | |
| Formula | C25H32ClN5O2 |
| Mol. mass | 470.01 g/mol |
| Pharmacokinetic data | |
| Bioavailability | 20% (variable) |
| Protein binding | >99% |
| Metabolism | Hepatic (active metabolites, including mCPP)1 |
| Half life | 2–4 hours |
| Excretion | In urine (55%) and feces (20–30%) |
| Therapeutic considerations | |
| Pregnancy cat. |
C(US) |
| Legal status |
℞ Prescription only |
| Routes | Oral |
Nefazodone hydrochloride (trade name Serzone, Nefadar) is an antidepressant drug marketed by Bristol-Myers Squibb. Its sale was discontinued in 2003 in some countries, due to the small possibility of hepatic (liver) injury, which could lead to the need for a liver transplant, or even death. The incidence of severe liver damage is approximately one in 250,000 to 300,000 patient-years.2 On May 20, 2004, Bristol-Myers Squibb discontinued the sale of Serzone in the United States and Canada. Several generic formulations of nefazodone are still available.34
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Structure and mode of action
Nefazodone is most closely related to trazodone (trade name Desyrel). Nefazodone is not considered to be an SSRI, MAOI or tricyclic antidepressant. It is not chemically related to either bupropion/amfebutamone, or venlafaxine.
It operates by blocking post-synaptic serotonin type-2A receptors and, to a lesser extent, by inhibiting pre-synaptic serotonin and norepinephrine (noradrenaline) reuptake. Nefazodone is also a relatively potent alpha-1 adrenoceptor antagonist.5
Dosing
Nefazodone doses for adults typically start at 50 mg twice daily uptitrated by 100 mg/day per week to a maximum of 600 mg (300 mg twice daily), according to Food and Drug Administration (FDA) regulations. Some patients with severe depression were treated with more than 600 mg/day. Most patients were treated with 300 mg–600 mg daily.
Side effects
Unlike most SNRIs and SSRIs, Nefazodone has no negative effects on libido or sexual functioning, and is actually sometimes used as an antidote to SSRI induced impotence and anorgasmia in men.6
Interactions
Nefazodone is a potent inhibitor of CYP3A4, an isozyme of the cytochrome P450 system, and may therefore interact adversely with many commonly-used medications that are metabolized by CYP3A4.17
Advantages
Nefazodone's claimed advantages over other antidepressants include reduced possibility of disturbed sleep or sexual dysfunction, and ability to treat some patients who did not respond to other antidepressant drugs.
Notes
- ^ a b Lexi-Comp (September 2008). "Nefazodone". The Merck Manual Professional. Retrieved on November 29, 2008.
- ^ Rxlist.com: "Nefazodone Prescribing Information", accessed 8 January 2007.]
- ^ FDA Orange Book, accessed 15 January 2006.
- ^ About.com: "Serzone Pulled from U.S. Market", accessed 15 January 2006.
- ^ Sanchez, C; J. Hyttel (1999). "Comparison of the Effects of Antidepressants and Their Metabolites on Reuptake of Biogenic Amines and on Receptor Binding". Celular and Molecular Neurobiology 19 (4): 467–89. doi:.
- ^ http://sulcus.berkeley.edu/mcb/165_001/papers/manuscripts/_684.html
- ^ Spina E, Santoro V, D'Arrigo C (July 2008). "Clinically relevant pharmacokinetic drug interactions with second-generation antidepressants: an update". Clin Ther 30 (7): 1206–27. PMID 18691982, http://linkinghub.elsevier.com/retrieve/pii/S0149-2918(08)80047-1.
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Wikipedia content modification information:
- This page was last modified on 29 November 2008, at 16:00.
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