Vortioxetina

A vortioxetina é um medicamento antidepressivo multimodal utilizado para o tratamento do transtorno depressivo maior em adultos, geralmente quando outros medicamentos antidepressivos não tenham eficácia satisfatória. Seu metabolismo é realizado pelas enzimas do citocromo P450 e pela Glucuronosiltransferase. A vortioxetina tem um perfil farmacocinético favorável com exposição proporcional à dose e linear, biodisponibilidade oral moderada, ampla distribuição tecidual e meia-vida de eliminação longa. Esse medicamento possui o nome comercial de Brintellix.[1][2]

Mecanismo de ação

O mecanismo de ação da vortioxetina está relacionado à modulação direta da atividade de receptores serotoninérgicos e à inibição do transportador de serotonina (5-HT). A vortioxetina atua como um agonista do receptor 5-HT1A, 5-HT3, 5-HT7 e antagonista do receptor 5-HT1D, agonista parcial do receptor 5-HT1B,e inibidor do transportador 5-HT. Alguns estudos pré-clínicos sugerem que a vortioxetina pode exercer sua atividade antidepressiva através da modulação da neurotransmissão em múltiplos sistemas, incluindo serotonina, norepinefrina, sistemas de dopamina, acetilcolina, histamina e glutamato.[3][4][5] O uso de agonista do receptor 5-HT1A está associado à atividade antidepressiva. O antagonismo contra o receptor 5-HT7 pode promover o efeito antidepressivo da droga que ocorre inibindo a recaptação da serotonina. O receptor 5-HT1B aumenta a concentração de serotonina no córtex pré-frontal, enquanto os agonistas do receptor 5-HT1B aumentam a taxa de disparo dos neurônios serotoninérgicos nos núcleos da rafe.[6][7][8][9][10]

Farmacocinética

A vortioxetina apresenta baixos níveis de toxicidade e, devido ao seu metabolismo intensivo no fígado e forte ligação às proteínas plasmáticas, a vortioxetina apresenta baixo potencial para causar interações farmacocinéticas e medicamentosas.[11] A vortioxetina é lentamente e bem absorvida após a administração oral e o pico da concentração plasmática é alcançado dentro de 7 a 11 horas. Após múltiplas doses de 5, 10, ou 20 mg/dia, valores médios de concentração máxima de 9 a 33 mg/mL. A biodisponibilidade absoluta é de 75%. Nenhum efeito dos alimentos sobre a farmacocinética é relatado.[12]

A vortioxetina é metabolizada através da oxidação das enzimas do citocromo P450 (CYP) e pela Glucuronosiltransferase. As enzimas do citocromo P450 que degradam o composto original incluem CYP2D6, CYP3A4 / 5, CYP2A6, CYP2C9 e CYP2C19, com CYP2D6 sendo a enzima primária.[13] A vortioxetina é quase totalmente eliminada pelo fígado, e com baixos níveis de eliminação pela urina e nas fezes.O principal metabólito da vortioxetina é farmacologicamente inativo.

Efeitos adversos

Os efeitos adversos mais comuns da vortioxetina são:[14]

Referências

  1. ↑ Chellappan, Dinesh Kumar; Candasamy, Mayuren (2016). «Cellulitis – Current Management Approach Through Complementary and Alternative Medicine». Advances in Pharmacoepidemiology & Drug Safety. 05 (05). ISSN 2167-1052. doi:10.4172/2167-1052.1000211 
  2. ↑ Baldwin, David S.; Florea, Ioana; Jacobsen, Paula L.; Zhong, Wei; Nomikos, George G. (dezembro de 2016). «A meta-analysis of the efficacy of vortioxetine in patients with major depressive disorder (MDD) and high levels of anxiety symptoms». Journal of Affective Disorders. 206: 140–150. ISSN 0165-0327. doi:10.1016/j.jad.2016.07.015 
  3. ↑ Pehrson, Alan L.; Sanchez, Connie (1 de agosto de 2013). «Serotonergic modulation of glutamate neurotransmission as a strategy for treating depression and cognitive dysfunction». CNS Spectrums. 19 (2): 121–133. ISSN 1092-8529. doi:10.1017/s1092852913000540 
  4. ↑ Mørk, Arne; Montezinho, Liliana P.; Miller, Silke; Trippodi-Murphy, Crista; Plath, Niels; Li, Yan; Gulinello, Maria; Sanchez, Connie (abril de 2013). «Vortioxetine (Lu AA21004), a novel multimodal antidepressant, enhances memory in rats». Pharmacology Biochemistry and Behavior. 105: 41–50. ISSN 0091-3057. doi:10.1016/j.pbb.2013.01.019 
  5. ↑ Stahl, Stephen M. (30 de junho de 2015). «Modes and nodes explain the mechanism of action of vortioxetine, a multimodal agent (MMA): blocking 5HT3 receptors enhances release of serotonin, norepinephrine, and acetylcholine». CNS Spectrums. 20 (5): 455–459. ISSN 1092-8529. doi:10.1017/s1092852915000346 
  6. ↑ Celada, Pau; Bortolozzi, Analía; Artigas, Francesc (12 de junho de 2013). «Serotonin 5-HT1A Receptors as Targets for Agents to Treat Psychiatric Disorders: Rationale and Current Status of Research». CNS Drugs. 27 (9): 703–716. ISSN 1172-7047. doi:10.1007/s40263-013-0071-0 
  7. ↑ Bonaventure, P.; Kelly, L.; Aluisio, L.; Shelton, J.; Lord, B.; Galici, R.; Miller, K.; Atack, J.; Lovenberg, T. W. (31 de janeiro de 2007). «Selective Blockade of 5-Hydroxytryptamine (5-HT)7 Receptors Enhances 5-HT Transmission, Antidepressant-Like Behavior, and Rapid Eye Movement Sleep Suppression Induced by Citalopram in Rodents». Journal of Pharmacology and Experimental Therapeutics. 321 (2): 690–698. ISSN 0022-3565. doi:10.1124/jpet.107.119404 
  8. ↑ Costall, Brenda; Naylor, Robert (1 de fevereiro de 2004). «5-HT3 Receptors». Current Drug Target -CNS & Neurological Disorders. 3 (1): 27–37. ISSN 1568-007X. doi:10.2174/1568007043482624 
  9. ↑ Chen, Grace; Højer, Astrid-Maria; Areberg, Johan; Nomikos, George (junho de 2018). «Vortioxetine: Clinical Pharmacokinetics and Drug Interactions». Clinical Pharmacokinetics (em inglês). 57 (6): 673–686. ISSN 0312-5963. doi:10.1007/s40262-017-0612-7 
  10. ↑ Sowa-Kućma, Magdalena; Pańczyszyn-Trzewik, Patrycja; Misztak, Paulina; Jaeschke, Rafał R.; Sendek, Katherine; Styczeń, Krzysztof; Datka, Wojciech; Koperny, Magdalena (agosto de 2017). «Vortioxetine: A review of the pharmacology and clinical profile of the novel antidepressant». Pharmacological Reports. 69 (4): 595–601. ISSN 1734-1140. doi:10.1016/j.pharep.2017.01.030 
  11. ↑ Baldwin, David S; Chrones, Lambros; Florea, Ioana; Nielsen, Rebecca; Nomikos, George G; Palo, William; Reines, Elin (9 de fevereiro de 2016). «The safety and tolerability of vortioxetine: Analysis of data from randomized placebo-controlled trials and open-label extension studies». Journal of Psychopharmacology. 30 (3): 242–252. ISSN 0269-8811. doi:10.1177/0269881116628440 
  12. ↑ «ANVISA :: Bulário Eletrônico :: 2013». www.anvisa.gov.br. Consultado em 29 de junho de 2019 
  13. ↑ Hvenegaard, M. G.; Bang-Andersen, B.; Pedersen, H.; Jorgensen, M.; Puschl, A.; Dalgaard, L. (11 de abril de 2012). «Identification of the Cytochrome P450 and Other Enzymes Involved in the In Vitro Oxidative Metabolism of a Novel Antidepressant, Lu AA21004». Drug Metabolism and Disposition. 40 (7): 1357–1365. ISSN 1521-009X. doi:10.1124/dmd.112.044610 
  14. ↑ www.dynamed.com https://www.dynamed.com/topics/dmp~AN~T907305. Consultado em 29 de junho de 2019  Em falta ou vazio |título= (ajuda)
  15. ↑ Dziwota, Ewelina; Olajossy, Marcin (novembro de 2016). «VORTIOXETINE - THE NEW ANTIDEPRESSANT AGENT WITH PROCOGNITIVE PROPERTIES». Acta Poloniae Pharmaceutica. 73 (6): 1433–1437. ISSN 0001-6837. PMID 29634095 

Read other articles:

Hartenholm

Hartenholm Lambang kebesaranLetak Hartenholm di Segeberg NegaraJermanNegara bagianSchleswig-HolsteinKreisSegeberg Municipal assoc.Kaltenkirchen-LandPemerintahan • MayorJohannes Herman Richter (FDP)Luas • Total15,37 km2 (593 sq mi)Ketinggian33 m (108 ft)Populasi (2013-12-31)[1] • Total1.755 • Kepadatan1,1/km2 (3,0/sq mi)Zona waktuWET/WMPET (UTC+1/+2)Kode pos24628Kode area telepon04195Pelat kendaraanSESit...

 

Dewan Perwakilan Rakyat Daerah Kabupaten Pesawaran

Dewan Perwakilan Rakyat Daerah Kabupaten PesawaranDewan Perwakilan RakyatKabupaten Pesawaran2019-2024JenisJenisUnikameral Jangka waktu5 tahunSejarahSesi baru dimulai20 Agustus 2019PimpinanKetuaSuprapto (PDI-P) sejak 3 Februari 2021 Wakil Ketua IPaisaludin (PAN) sejak 7 Oktober 2019 Wakil Ketua IIMusannif Yasser Syamsurya, S.E., M.M. (Demokrat) sejak 7 Oktober 2019 Wakil Ketua IIIZulkarnain (PKB) sejak 7 Oktober 2019 KomposisiAnggota45Partai & kursi  PDI-P (9) ...

 

Arborea

Arborea ArborèaKomuneComune di ArboreaLokasi Arborea di Provinsi OristanoNegara ItaliaWilayah SardiniaProvinsiOristano (OR)Pemerintahan • Wali kotaManuela PintusLuas • Total94,96 km2 (36,66 sq mi)Ketinggian7 m (23 ft)Populasi (2016) • Total3,910[1]Zona waktuUTC+1 (CET) • Musim panas (DST)UTC+2 (CEST)Kode pos09092Kode area telepon0783Situs webhttp://www.comune.arborea.or.it Arborea (bahasa Sardinia: Arb...

Daftar Bupati Rejang Lebong

Bupati Rejang LebongLambang Kabupaten Rejang LebongPetahanaDrs. Syamsul Effendi, M.M.sejak 26 Februari 2021KediamanPendapa Kabupaten Rejang LebongMasa jabatan5 tahunDibentuk1959Pejabat pertamaBurhan DahriSitus webwww.rejanglebongkab.go.id Berikut ini adalah Daftar Bupati Rejang Lebong dari masa ke masa. No Bupati Mulai Jabatan Akhir Jabatan Prd. Ket. Wakil Bupati 1 Burhan Dahri 1959 1964 1 2 Letkol. Inf.Sjarifuddin Abdullah 1964 1966 2 [1] 3 Letkol. M. Daud Mustafa 1968 1973 3 &#...

 

Appingedam

AppingedamBekas munisipalitas / kota BenderaLambang kebesaranNegaraBelandaProvinsiGroningenMunisipalitasEemsdeltaLuas(2006) • Total24,62 km2 (951 sq mi) • Luas daratan23,84 km2 (920 sq mi) • Luas perairan0,78 km2 (30 sq mi)Populasi (1 Januari 2007) • Total12.190 • Kepadatan511/km2 (1,320/sq mi) Sumber: CBS, Statline.Zona waktuUTC+1 (CET) • Musim panas (DST)UTC+2 ...

 

Players' Union

Former trade union of the United Kingdom The Association Football Players' and Trainers' Union (AFPTU), commonly known as the Players' Union, in the United Kingdom was the original association that became the Professional Footballers' Association. Their stated aims were freedom of movement of players and obtaining the same employment rights as other workers.[1] The Players' Union was formed at a meeting on 2 December 1907 when Charlie Roberts and Billy Meredith (who had been involved ...

Cambridge Theatre

Cambridge Theatre Cambridge Theatre pada 2011 Alamat Earlham Street, Seven Dials Kota London, WC2 Negara Britania Raya Penetapan Kelas II Arsitek Wimperis, Simpson & Guthrie Dimiliki LW Theatres Kapasitas 1,231 di 3 lantai Jenis Teater West End Dibuka 4 September 1930; 93 tahun lalu (1930-09-04) Produksi 'Matilda the Musical' [http://Cambridge Theatre (Situs Web Resmi) Cambridge Theatre (Situs Web Resmi)] Cambridge Theatre adalah sebuah teater West End, di tempat persimpangan di Ear...

 

RimWorld

Artikel ini sedang dalam perubahan besar untuk sementara waktu.Untuk menghindari konflik penyuntingan, dimohon jangan melakukan penyuntingan selama pesan ini ditampilkan.Halaman ini terakhir disunting oleh AABot (Kontrib • Log) 78 hari 1427 menit lalu. Pesan ini dapat dihapus jika halaman ini sudah tidak disunting dalam beberapa jam. Jika Anda adalah penyunting yang menambahkan templat ini, harap diingat untuk menghapusnya setelah selesai atau menggantikannya dengan {{Under constr...

 

Erik Demaine

Erik D. DemaineLahir28 Februari 1981 (umur 43)Halifax, Nova Scotia, KanadaTempat tinggalCambridge, MassachusettsKebangsaanKanadaAmerika SerikatAlmamaterUniversitas DalhousieUniversitas WaterlooPenghargaanMacArthur Fellow (2003), Penghargaan Nerode (2015)Karier ilmiahInstitusiInstitut Teknologi MassachusettsDisertasiFolding and Unfolding (2001)Pembimbing doktoral Anna Lubiw Ian Munro Mahasiswa doktoral Mohammad Hajiaghayi Mihai Pătrașcu Erik D. Demaine (lahir 28 Februari 1981) ada...

Romulus dan Remus

Untuk kisah Romulus secara khusus, lihat Romulus. Romulus dan Remus beserta serigala yang mengasuh mereka Romulus dan Remus adalah pendiri kota Roma dalam mitologi Romawi. Dahulu, menurut legenda mereka dipelihara oleh seekor serigala betina hingga mereka menjadi remaja. Remus dan Romulus adalah anak dari seorang Perawan Vesta Rhea Silvia (anak dari Numitor, raja Alba Longa) dengan dewa Mars. Ketika menginjak usia dewasa, mereka mengetahui asal usul kelahirannya, dan membunuh Amulius, adik Nu...

 

1997 National League Division Series

1997 National League Division SeriesTeamsTeam (Wins) Manager SeasonFlorida Marlins (3) Jim Leyland 92–70, .568, GB: 9San Francisco Giants (0) Dusty Baker 90–72, .556, GA: 2DatesSeptember 30 – October 3TelevisionESPN (in Florida)NBC (in San Francisco)TV announcersChris Berman and Ray Knight (in Florida)Bob Costas, Joe Morgan, and Bob Uecker (in San Francisco)RadioCBSRadio announcersJerry Coleman and Hank GreenwaldTeamsTeam (Wins) Manager SeasonAtlanta Braves (3) Bobby Cox 101–61, .623...

 

COVID-19 pandemic in Illinois

This article needs to be updated. Please help update this article to reflect recent events or newly available information. (October 2023)Ongoing COVID-19 viral pandemic in Illinois, United States COVID-19 pandemic in IllinoisDiseaseCOVID-19Virus strainSARS-CoV-2LocationIllinois, United StatesFirst outbreakWuhan, Hubei, ChinaIndex caseChicagoArrival dateJanuary 24, 2020(4 years, 3 months, 2 weeks and 2 days)Confirmed cases4,139,537 [1]Recovered98% (recovery rate)Dea...

Langquaid

Langquaid Lambang kebesaranLetak Langquaid di Kelheim NegaraJermanNegara bagianBayernWilayahNiederbayernKreisKelheimMunicipal assoc.Langquaid Subdivisions8 OrtsteilePemerintahan • MayorHerbert Blascheck (CSU)Luas • Total56,63 km2 (2,186 sq mi)Ketinggian389 m (1,276 ft)Populasi (2013-12-31)[1] • Total5.303 • Kepadatan0,94/km2 (2,4/sq mi)Zona waktuWET/WMPET (UTC+1/+2)Kode pos84083–84085Kode area telepon...

 

List of association football stadiums by capacity

List of football stadiums redirects here. For American football stadiums, see List of American football stadiums by capacity. For Canadian football stadiums, see List of Canadian football stadiums by capacity. For Australian football stadiums, see Australian rules football playing field. For stadiums of any use, see List of stadiums by capacity. This article needs additional citations for verification. Please help improve this article by adding citations to reliable sources. Unsourced materi...

 

Benifairó de les Valls

Questa voce o sezione sull'argomento centri abitati della Spagna non cita le fonti necessarie o quelle presenti sono insufficienti. Puoi migliorare questa voce aggiungendo citazioni da fonti attendibili secondo le linee guida sull'uso delle fonti. Segui i suggerimenti del progetto di riferimento. Benifairó de les Vallscomune(ES) Benifairó de les Valls/Benifairó de los Valles Benifairó de les Valls – Veduta LocalizzazioneStato Spagna Comunità autonoma Valencia ProvinciaVa...

1943 in the United States

USA-related events during the year of 1943 ← 1942 1941 1940 1943 in the United States → 1944 1945 1946 Decades: 1920s 1930s 1940s 1950s 1960s See also: History of the United States (1918–1945) Timeline of United States history (1930–1949) List of years in the United States 1943 in the United States1943 in U.S. states and territories States Alabama Arizona Arkansas California Colorado Connecticut Delaware Florida Georgia Idaho Illinois Indiana Iowa Kansas Kentucky Louisiana Mai...

 

أندريه هال (لاعب كرة قدم أمريكية مواليد 1982)

  لمعانٍ أخرى، طالع أندريه هال (توضيح). أندريه هال معلومات شخصية الميلاد 20 أغسطس 1982 (42 سنة)  سانت بيترسبرغ  مواطنة الولايات المتحدة  الطول 70 بوصة  الوزن 212 رطل  الحياة العملية المدرسة الأم جامعة جنوب فلوريدا  المهنة لاعب كرة قدم أمريكية  الرياضة كرة القد...

 

Chi Lăng

Đối với các định nghĩa khác, xem Chi Lăng (định hướng). Dãy núi Cai Kinh phía tây và cánh đồng Chi Lăng Chi Lăng (支棱) là một cửa ải nổi tiếng trong lịch sử Việt Nam. Nơi đây vốn là một thung lũng có sông Thương chảy qua, trải dài gần 20 km từ sông Hóa đến xã Mai Sao, thuộc huyện Chi Lăng, tỉnh Lạng Sơn. Phía đông thung lũng là dãy núi đất Thái Họa – Bảo Đài, còn phía tây là dãy núi...

Daniel Gélin

French actor (1921–2002) This article needs additional citations for verification. Please help improve this article by adding citations to reliable sources. Unsourced material may be challenged and removed.Find sources: Daniel Gélin – news · newspapers · books · scholar · JSTOR (February 2011) (Learn how and when to remove this message) Daniel GélinGélin in 1963BornDaniel Yves Alfred Gélin(1921-05-19)19 May 1921Angers, Maine-et-Loire, FranceDied...

 

Jesús Navas

Jesús NavasNavas in allenamento con il Siviglia nel 2017Nazionalità Spagna Altezza170 cm Peso60 kg Calcio RuoloDifensore Squadra Siviglia CarrieraGiovanili 2000-2001 Siviglia Squadre di club1 2002-2003 Siviglia Atlético33 (3)[1]2003-2013 Siviglia285 (23)2013-2017 Manchester City123 (4)2017- Siviglia223 (3) Nazionale 2004-2005 Spagna U-215 (0)2009-2024 Spagna56 (5) Palmarès  Mondiali di calcio OroSudafrica 2010  Europei di calcio OroPolo...