请输入您要查询的百科知识：

　

词条 Desvenlafaxine
释义

  1. Medical uses

  2. Adverse effects

  3. Pharmacology

  4. Approval status

     United States  Canada  European Union  Australia 

  5. See also

  6. References

  7. External links

{{Drugbox
| Verifiedfields = changed
| Watchedfields = changed
| verifiedrevid = 443583795
| IUPAC_name = 4-[2-dimethylamino-1-(1-hydroxycyclohexyl)
ethyl]phenol
| image = Desvenlafaxine.svg
| width = 180
| alt = Skeletal formula
| image2 = Desvenlafaxine molecule ball.png
| alt2 = Ball-and-stick model of desvenlafaxine
| tradename = Pristiq, Desfax, Ellefore, others
| Drugs.com = {{drugs.com|monograph|desvenlafaxine-succinate}}
| MedlinePlus = a608022
| licence_US = Desvenlafaxine
| pregnancy_AU = B2
| pregnancy_US = C
| legal_AU = S4
| legal_CA = Rx-only
| legal_US = Rx-only
| routes_of_administration = By mouth
| synonyms = O-desmethylvenlafaxine
| bioavailability = 80%
| protein_bound = Low (30%)
| metabolism = CYP3A4, (CYP2D6 is not involved)
| elimination_half-life = 11 h
| excretion = 45% excreted unchanged in urine
| IUPHAR_ligand = 7158
| CAS_number_Ref = {{cascite|correct|??}}
| CAS_number = 93413-62-8
| ATC_prefix = N06
| ATC_suffix = AX23
| PubChem = 125017
| DrugBank_Ref = {{drugbankcite|correct|drugbank}}
| DrugBank = DB06700
| ChemSpiderID_Ref = {{chemspidercite|correct|chemspider}}
| ChemSpiderID = 111300
| UNII_Ref = {{fdacite|correct|FDA}}
| UNII = NG99554ANW
| KEGG_Ref = {{keggcite|correct|kegg}}
| KEGG = D07793
| ChEBI_Ref = {{ebicite|changed|EBI}}
| ChEBI = 83527
| ChEMBL_Ref = {{ebicite|correct|EBI}}
| ChEMBL = 1118
| C=16 | H=25 | N=1 | O=2
| molecular_weight = 263.38 g/mol
| smiles = OC2(C(c1ccc(O)cc1)CN(C)C)CCCCC2
| StdInChI_Ref = {{stdinchicite|correct|chemspider}}
| StdInChI = 1S/C16H25NO2/c1-17(2)12-15(13-6-8-14(18)9-7-13)16(19)10-4-3-5-11-16/h6-9,15,18-19H,3-5,10-12H2,1-2H3
| StdInChIKey_Ref = {{stdinchicite|correct|chemspider}}
| StdInChIKey = KYYIDSXMWOZKMP-UHFFFAOYSA-N
}}Desvenlafaxine, sold under the brand name Pristiq among others, is a medication used to treat major depressive disorder.[1] Evidence supports a benefit up to eight weeks.[1] It appears less effective than its parent compound venlafaxine.[1] It is taken by mouth.[2]

Common side effects include dizziness, trouble sleeping, increased sweating, constipation, sleepiness, anxiety, and sexual problems.[2] Serious side effects may include suicide in those under the age of 25, serotonin syndrome, bleeding, mania, and high blood pressure.[2] A withdrawal syndrome may occur if the dose is rapidly decreased.[2] It is unclear if use during pregnancy or breastfeeding is safe.[3] It is an antidepressant of the serotonin-norepinephrine reuptake inhibitor (SNRI) class.[2]

Desvenlafaxine was approved for medical use in the United States in 2008.[2] Use in Europe was declined in 2009.[1] In the United States the wholesale cost is about 25.20 USD per month.[4] In 2016, it was the 272nd most prescribed medication in the United States, with more than a million prescriptions.[5]

Medical uses

Desvenlafaxine is primarily used as a treatment for major depressive disorder.[6] Use has only been studied up to 8 weeks.[2] It, however, appears less effective than venlafaxine.[1]

Doses of 50-400 mg/day appear effective for major depressive disorder, although no additional benefit was demonstrated at doses greater than 50 mg/day, and adverse events and discontinuations were more frequent at higher doses.[7]

Desvenlafaxine improves the HAM-D17 score[8] and measures of well being such as the Sheehan Disability Scale (SDS) and 5-item World Health Organization Well-Being Index (WHO-5).[9]

Adverse effects

Frequency of adverse effects:[6][10][11]

Very common adverse effects include:{{colbegin|colwidth=15em}}
  • Nausea
  • Headache
  • Dizziness
  • Dry mouth
  • Hyperhidrosis
  • Diarrhea
  • Insomnia
  • Constipation
  • Fatigue
{{colend}}Common adverse effects include:{{colbegin|colwidth=15em}}
  • Tremor
  • Blurred vision
  • Mydriasis
  • Decreased appetite
  • Sexual dysfunction
  • Insomnia
  • Anxiety
  • Elevated cholesterol and triglycerides
  • Proteinuria
  • Vertigo
  • Feeling jittery
  • Asthenia
  • Nervousness
  • Hot flush
  • Irritability
  • Abnormal dreams
  • Urinary hesitation
  • Yawning
  • Rash
{{colend}}Uncommon adverse effects include:{{colbegin|colwidth=15em}}
  • Hypersensitivity
  • Syncope
  • Depersonalization
  • Hypomania
  • Withdrawal syndrome
  • Urinary retention
  • Epistaxis (nose bleed)
  • Alopecia (hair loss)
  • Orthostatic hypotension
  • Peripheral coldness
{{colend}}Rare adverse effects include:{{colbegin|colwidth=15em}}
  • Hyponatraemia (low blood sodium)
  • Seizures
  • Extrapyramidal side effects
  • Hallucinations
  • Angioedema
  • Photosensitivity reaction
  • Stevens-Johnson syndrome
{{colend}}Common however unknown intensity of adverse effects include:{{colbegin|colwidth=15em}}
  • Abnormal bleeding (gastrointestinal bleeds)
  • Narrow-angle glaucoma
  • Mania
  • Interstitial lung disease
  • Eosinophilic pneumonia
  • Hypertension
  • Suicidal behavior and thoughts
  • Serotonin syndrome
{{colend}}

Pharmacology

Desvenlafaxine is a synthetic form of the isolated major active metabolite of venlafaxine, and is categorized as a serotonin-norepinephrine reuptake inhibitor (SNRI). When most normal metabolizers take venlafaxine, approximately 70% of the dose is metabolized into desvenlafaxine, so the effects of the two drugs are expected to be very similar.[12] It works by blocking the "reuptake" transporters for key neurotransmitters affecting mood, thereby leaving more active neurotransmitters in the synapse. The neurotransmitters affected are serotonin (5-hydroxytryptamine) and norepinephrine (noradrenaline). It is approximately 10 times more potent at inhibiting serotonin uptake than norepinephrine uptake.[13]

Transporter Ki[nM][13][14]
SERT 40.2
NET 558.4

Approval status

United States

Wyeth announced on 23 January 2007 that it received an approvable letter from the Food and Drug Administration for desvenlafaxine. Final approval to sell the drug was contingent on a number of things, including:

  • A satisfactory FDA inspection of Wyeth's Guayama, Puerto Rico facility, where the drug is to be manufactured;
  • Several postmarketing surveillance commitments, and follow-up studies on low-dose use, relapse, and use in children;
  • Clarity by Wyeth around the company's product education plan for physicians and patients;
  • Approval of desvenlafaxine's proprietary name, Pristiq.[15]

The FDA approved the drug for antidepressant use in February 2008, and was to be available in US pharmacies in May 2008.[16]

In March 2017, the generic form of the drug was made available in the US.

Canada

On February 4, 2009, Health Canada approved use of desvenlafaxine for treatment of depression.[17][18]

European Union

In 2009, an application to market desvenlafaxine for major depressive disorder in the European Union was declined.[1] In 2012, Pfizer received authorization in Spain to market desvenlafaxine for the disorder but it is not being sold.[19][20]

Australia

Desvenlafaxine is classified as a schedule 4 (prescription only) drug in Australia. It was listed on the PBS (Pharmaceutical Benefits Scheme) in 2008 for the treatment of major depressive disorders.

See also

  • Ansofaxine

References

1. ^1 2 3 {{cite web |title=Withdrawal Assessment Report for Dessvenlafaxime |url=https://www.ema.europa.eu/en/documents/withdrawal-report/withdrawal-assessment-report-ellefore_en.pdf |website=EMA |accessdate=22 March 2019 |page=3}}
2. ^1 2 3 4 5 6 7 8 {{cite web |title=Desvenlafaxine Succinate Monograph for Professionals |url=https://www.drugs.com/monograph/desvenlafaxine-succinate.html |website=Drugs.com |publisher=American Society of Health-System Pharmacists |accessdate=18 March 2019 |language=en}}
3. ^{{cite web |title=Desvenlafaxine Pregnancy and Breastfeeding Warnings |url=https://www.drugs.com/pregnancy/desvenlafaxine.html |website=Drugs.com |accessdate=19 March 2019}}
4. ^{{cite web |title=NADAC as of 2019-02-27 |url=https://data.medicaid.gov/Drug-Pricing-and-Payment/NADAC-as-of-2019-02-27/s7c9-pfa6 |website=Centers for Medicare and Medicaid Services |accessdate=3 March 2019 |language=en}}
5. ^{{cite web |title=The Top 300 of 2019 |url=https://clincalc.com/DrugStats/Top300Drugs.aspx |website=clincalc.com |accessdate=22 December 2018}}
6. ^1 {{cite web|title=PRODUCT INFORMATION PRISTIQ® desvenlafaxine (as succinate)|website=TGA eBusiness Services|publisher=Pfizer Australia Pty Ltd|date=10 December 2012|accessdate=8 November 2013|url=https://www.ebs.tga.gov.au/ebs/picmi/picmirepository.nsf/pdf?OpenAgent&id=CP-2010-PI-06360-3|format=PDF}}
7. ^{{Cite journal|last=Perry|first=Richard|last2=Cassagnol|first2=Manouchkathe|date=2009|title=Desvenlafaxine: a new serotonin-norepinephrine reuptake inhibitor for the treatment of adults with major depressive disorder|journal=Clinical Therapeutics|volume=31 Pt 1|pages=1374–1404|doi=10.1016/j.clinthera.2009.07.012|issn=1879-114X|pmid=19698900}}
8. ^{{cite journal |vauthors=Thase ME, Kornstein SG, Germain JM, Jiang Q, Guico-Pabia C, Ninan PT |title=An integrated analysis of the efficacy of desvenlafaxine compared with placebo in patients with major depressive disorder |journal=CNS Spectr |volume=14 |issue=3 |pages=144–54 |date=March 2009 |pmid=19407711 |doi= |url=}}
9. ^{{cite journal |vauthors=Soares CN, Kornstein SG, Thase ME, Jiang Q, Guico-Pabia CJ |title=Assessing the efficacy of desvenlafaxine for improving functioning and well-being outcome measures in patients with major depressive disorder: a pooled analysis of 9 double-blind, placebo-controlled, 8-week clinical trials |journal=J Clin Psychiatry |volume=70 |issue=10 |pages=1365–71 |date=October 2009 |pmid=19906341 |doi=10.4088/JCP.09m05133blu |url=}}
10. ^{{cite web|title=DESVENLAFAXINE tablet, extended release [Ranbaxy Pharmaceuticals Inc.]|website=DailyMed|publisher=Ranbaxy Pharmaceuticals Inc.|date=March 2013|accessdate=9 November 2013|url=http://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=91cf39c9-4d26-480a-a3a3-a3d8d4c4d222}}
11. ^{{cite web|title=desvenlafaxine (Rx) - Pristiq, Khedezla|website=Medscape Reference|publisher=WebMD|accessdate=9 November 2013|url=http://reference.medscape.com/drug/pristiq-khedezla-desvenlafaxine-342964}}
12. ^{{cite book|title=Foye's Principles of Medicinal Chemistry|year=2012|publisher=Lippincott Williams & Wilkins |isbn=978-1-60913-345-0 |page=609|first1=Thomas L.|last1=Lemke |first2=David A. |last2=Williams}}
13. ^1 {{cite journal|title=Desvenlafaxine succinate: A new serotonin and norepinephrine reuptake inhibitor|journal=The Journal of Pharmacology and Experimental Therapeutics|date=August 2006|volume=318|issue=2|pages=657–665|author1=Deecher, DC |author2=Beyer, CE |author3=Johnston, G |author4=Bray, J |author5=Shah, S |author6=Abou-Gharbia, M |author7=Andree, TH |doi=10.1124/jpet.106.103382|pmid=16675639|url=http://jpet.aspetjournals.org/content/318/2/657.full.pdf|format=PDF}}
14. ^{{cite web|title=PDSP Ki Database |website=Psychoactive Drug Screening Program (PDSP) |author1=Roth, BL |author2=Driscol, J |url=https://pdsp.unc.edu/databases/pdsp.php?recDDRadio=recDDRadio&receptorDD=&receptor=&speciesDDRadio=speciesDDRadio&speciesDD=&species=&sourceDDRadio=sourceDDRadio&sourcesDD=&source=&hotDDRadio=hotDDRadio&hotLigandDD=&hotLigand=&testDDRadio=testDDRadio&testLigandDD=8475&testLigand=&refDDRadio=refDDRadio&referenceDD=&reference=&KiGreater=&KiLess=&kiAllRadio=all&doQuery=Submit+Query |publisher=University of North Carolina at Chapel Hill and the United States National Institute of Mental Health |accessdate=7 July 2018 |date=Dec 2012 |deadurl=no |df= }}
15. ^{{cite press release |url = http://www.biospace.com/news_story.aspx?StoryID=43424&full=1 |title = Wyeth Receives Approvable Letter From FDA For Pristiq (Desvenlafaxine Succinate) For The Treatment Of Major Depressive Disorder |date = 2007-01-23 |accessdate = 2007-04-04}}
16. ^{{cite press release |url = http://www.wyeth.com/news?nav=display&navTo=/wyeth_html/home/news/pressreleases/2008/1204331198948.html |title = FDA Approves Pristiq |date=2008-02-29 |publisher = Wyeth |accessdate = 2008-02-29}}
17. ^Health Canada Notice of Compliance - Pristiq. February 4, 2009, retrieved on March 9, 2009.
18. ^{{cite web|url=http://www.hc-sc.gc.ca/dhp-mps/prodpharma/sbd-smd/drug-med/sbd_smd_2009_pristiq_115439-eng.php|title=Summary Basis of Decision (SBD) PrPristiq™|date=2009-05-29|publisher=Health Canada|accessdate=2016-12-30}}
19. ^{{cite web|url=http://www.aemps.gob.es/cima/especialidad.do?metodo=verPresentaciones&codigo=75561 |title=Pristiq 100 mg Comprimidos de Liberacion Prolongada |publisher=AEMPS Medicines Online Information Center - CIMA |accessdate=2016-12-30}}
20. ^{{cite web|url=http://www.aemps.gob.es/cima/especialidad.do?metodo=verPresentaciones&codigo=75560 |title=Pristiq 50 mg Comprimidos de Liberacion Prolongada |publisher= AEMPS Medicines Online Information Center - CIMA |accessdate=2016-12-30}}

External links

  • [https://druginfo.nlm.nih.gov/drugportal/name/desvenlafaxine Drug information from the NIH]
{{Antidepressants}}{{Monoamine reuptake inhibitors}}{{Phenethylamines}}

8 : Cyclohexanols|Phenethylamines|Phenols|Serotonin-norepinephrine reuptake inhibitors|Tertiary alcohols|Human drug metabolites|RTT|Antidepressants
随便看

　

开放百科全书收录14589846条英语、德语、日语等多语种百科知识，基本涵盖了大多数领域的百科知识，是一部内容自由、开放的电子版国际百科全书。

　

Copyright © 2023 OENC.NET All Rights Reserved
京ICP备2021023879号 更新时间：2024/11/10 23:28:28