Leitura clínica
Comentário
O metotrexato (MTX) é um antimetabólito antineoplásico análogo e antagonista do ácido fólico, com propriedades antineoplásicas e imunossupressoras por interferir com a síntese e replicação celular do ADN. Indicado no tratamento de certas neoplasias, problemas reumáticos: artrite, psoríase grave, síndrome de Reiter, doença inflamatória intestinal (Pfizer 2019 y 2008, AEMPS 2018, EMA 2017) e, fora de indicação, na esclerose múltipla e em alguns processos obstétricos: aborto, gravidez ectópica, placenta acreta. (Prac Com Am Soc Rep Med 2013, Kulier 2011) USOS OBSTÉTRICO E IMUNOSSUPRESSOR: Administração em Obstetrícia com fins expulsivos: dose intramuscular única ou por 3 dias de 50 mg/m 2 de superfície corporal. Administração em processos reumáticos e autoimunes: oral (também subcutânea ou intramuscular) 7,5 a 20 mg (10-15 mg/m 2 de superfície corporal) uma vez por semana. A excreção no leite materno é muito escassa (Brown 2017, Østensen 2006, Johns 1972) , talvez por um elevado volume de distribuição e um pKa muito baixo que o torna muito insolúvel em líquidos em pH fisiológico. (Götestam 2016) Após doses isoladas de 50 mg/m2 SC com fins obstétricos, inclusive após doses de 92 mg diários durante 4 dias, foram encontrados níveis no leite materno indetectáveis ou ínfimos (Baker 2018, Tanaka 2009) . Também foi constatada passagem nula ou ínfima para o leite quando utilizado em baixas doses semanais (25 mg) durante o tratamento de manutenção da artrite reumatoide e outras doenças autoimunes. (Delaney 2017, Thorne 2014) Não foram publicados nem observados problemas em bebês que mamavam cujas mães o tomavam . (Thorne 2014) As recomendações de especialistas e a atitude prática entre os clínicos sobre manter o tratamento durante a amamentação estão divididas. (Huang 2016, Götestam 2016, Martínez 2009, Weber 2008, Østensen 2007) Vários autores consideram seguro o uso isolado ou semanal em baixa dose durante a amamentação . Anderson 2018, Delaney 2017, Noviani 2016, Thorne 2014, Koren 2013, Østensen 2009, Tanaka 2009, Weber 2008, Moretti 2000, Goldsmith 1989, Johns 1972) Alguns recomendam controles clínicos ou hematológicos ou níveis de MTX no bebê que mama (Rademaker 2017, Almas 2016, Østensen 2009) e administrar ácido fólico ao bebê que mama. (Almas 2016) Pode-se reduzir a exposição a quase a metade interrompendo a amamentação 24 horas após a dose do fármaco, extraindo e descartando o leite nesse intervalo (CRAT 2020, Delaney 2017, Hale 2017 p628, Noviani 2016) , o que na prática significa não amamentar no dia da dose do MTX e sim no restante da semana. Outros autores e consensos de especialistas desaconselham seu uso durante a amamentação (Bermas 2017, Flint 2016, Nguyen 2016, Götestam 2016, Kavanaugh 2015, van der Woude 2015, Mahadevan 2015, Grunewald 2015, Samaritano 2014, Mervic 2014, Huang 2014, Sammaritano 2014, Mottet 2007, Temprano 2005, WHO 2002, AAP 2001, Janssen 2001) Você pode consultar abaixo as informações deste produto relacionado: Metotrexato (uso oncológico) (Pouco seguro. Efeitos adversos moderados/graves. Compatível em alguma circunstância. Acompanhamento recomendado. Usar alternativa mais segura ou interromper a amamentação por 5 a 7 meias-vidas (T½). Leia o comentário.)
Encontrabilidade
Outros nomes e marcas
Sinônimos e grafias 8
- Ametopterina. Ácido 4-Amino-10-metilfólico
- MTX. Metotrexato disódico. Metotrexato sódico
- μεθοτρεξάτη ή αμεθοπτερίνη
- ميثوتريكسات
- Метотрексат
- 甲氨蝶呤
- メトトレキサート
- L01BA01; L04AX03
Marcas comerciais na fonte 49
- Abitrexate
- Artrait
- Atrexel
- Bertanel
- Ebetrex
- Ebetrexac
- Ebetrexat
- Emthexate
- Ervemin
- Fauldexato
- Ifamet
- Imeth
- Lantarel
- Ledertrexate
- Ledertrexato
- MTX
- Matrex
- Maxtrex
- Medsatrexate
- Metex
- Methacor
- Methobion
- Methoblastin
- Metoart
- Metodik
- Metoject
- Metoject (Методжект)
- Metolate
- Metotab
- Metrex
- Neometho
- Novatrex
- Onkomet
- Otaxem
- Otrexup
- Pterin
- Reumaflex
- Rheumatrex
- Sactiva
- Securact
- Texate
- Tratoben
- Trexall
- Trexan
- Trixate
- Trixilem
- Xantromid
- Zexat (Зексат)
- Zexate
Dados da fonte
Farmacocinética
| Variável | Valor | Unidade |
|---|---|---|
| Biodisp. oral | 60 (20 - 95) | % |
| Peso Molecular | 454 | daltons |
| Unión proteínas | 50 | % |
| Vd | 0,4 - 0,8 | l/Kg |
| pKa | 3,41 | - |
| Tmax | oral: 1 - 2; IM: 0,5 -1 | horas |
| T½ | 3 - 10 (dos. < 30 mg/m2) | horas |
| Índice L/P | 0,08 - 0,1 | - |
| Dosis Teórica | 0,0013 - 0,0034 | mg/Kg/d |
| Dosis Relativa | 0,08 - 0,81 | % |
| Dosis Rel. Ped. | 0,04 - 0,1 | % |
Rastreabilidade
Bibliografia
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