Leitura clínica
Comentário
Imunossupressor por inibição da calcineurina utilizado na prevenção da rejeição de órgãos transplantados (rim, fígado, coração...) e no tratamento de formas graves de doenças autoimunes: eczema atópico, psoríase, artrite reumatoide, colite ulcerativa, síndrome nefrótica, anemia aplásica, asma, síndrome de Behçet, hepatite crônica ativa, esclerose múltipla, miastenia gravis, sarcoidose, esclerite ou uveíte e esclerodermia, entre outras. Administração sistêmica oral em uma ou duas doses diárias, injetável parenteral, na forma de colírio e inalatória. Seu elevado peso molecular e alta fixação a proteínas explicam a escassa excreção (<0,36 mg/L) obtida em colostro e leite materno. (Li 2022, Kociszewska 2020, Mazzuoccolo 2014, Osadchy 2011, Moretti 2003, Muñoz-Flores 2001, Nyberg 1998, Thiru 1997, Behrens 1989, Ziegenhagen 1988, Flechner 1985, Lewis 1983) Não foram observados problemas de desenvolvimento nem imunológicos, a curto ou longo prazo, em lactentes cujas mães a tomavam. (Coscia 2025, LI 2022, Mazzuoccolo 2014, Lahiff 2011, Morton 2011, Moretti 2003, Muñoz-Flores 2001, Nyberg 1998, Thiru 1997) Os níveis plasmáticos na maioria desses lactentes foram indetectáveis ou muito baixos (Osadchy 2011, Lahiff 2011, Morton 2011, Moretti 2003, Munoz-Flores 2001, Nyberg 1998, Ziegenhagen 1988, Flechner 1985 ), com exceção de um que apresentou níveis terapêuticos. (Moretti 2003) Sua baixa biodisponibilidade oral, ainda mais diminuída no caso de coincidir com a ingestão de alimento, em especial se este for gorduroso, diminuiria a passagem para o plasma do lactente a partir do leite materno ingerido. Embora percentualmente alta, a quantidade total de álcool contida em cada dose do medicamento é insuficiente para contraindicar seu uso durante a amamentação. Há observações isoladas de que a ciclosporina pode diminuir a produção de prolactina. (Nagar 1992, Ramirez 1991) Os lactentes que foram expostos a inibidores da calcineurina durante a gravidez podem ter deficiência imunitária no primeiro ano de vida (Grimer 2007), daí a importância de não serem privados da amamentação sem um motivo demonstrado. Diversas sociedades médicas e consensos de especialistas consideram seguro o uso deste medicamento durante a amamentação. ( Russell 2023, Sammaritano 2020, Yeung 2020, Mahadevan 2019, Götestam-Skorpen 2016, Flint 2016, Constantinescu 2014, Thiagarajan 2013, van der Houde 2010) Pode consultar abaixo a informação destes produtos relacionados: Artrite Reumatoide (AR) Materna (Bastante seguro. Efeitos adversos leves ou pouco prováveis. Compatível em determinadas circunstâncias. Acompanhamento recomendado. Leia o Comentário.) Doença inflamatória intestinal (DII) materna (Bastante seguro. Efeitos adversos leves ou pouco prováveis. Compatível em determinadas circunstâncias. Acompanhamento recomendado. Leia o Comentário.) Esclerose múltipla materna (Bastante seguro. Efeitos adversos leves ou pouco prováveis. Compatível em determinadas circunstâncias. Acompanhamento recomendado. Leia o Comentário.) Miastenia gravis materna (Produto seguro e/ou a amamentação é a melhor opção.) Transplante materno (Bastante seguro. Efeitos adversos leves ou pouco prováveis. Compatível em determinadas circunstâncias. Acompanhamento recomendado. Leia o Comentário.)
Encontrabilidade
Outros nomes e marcas
Sinônimos e grafias 7
- Κυκλοσπορίνη
- سيكلوسبورين
- Циклоспорин
- 环孢素
- シクロスポリン
- OL-27-400
- L04AD01; S01XA18
Marcas comerciais na fonte 29
- Capimune
- Capsorin
- Cequa
- Cipos
- Ciqorin
- Closporil
- Deximune
- Emicrox
- Equoral
- Genfar
- Gengraf
- Gengraf (金格福)
- Ikervis
- Ilast
- Imunofar
- Inmunosporin
- Lacrinmune
- Modusik-A
- Neoral
- Restasis
- Restasis (Рестасис)
- Sandimmun
- Sandimmun (Сандиммун)
- Sandimmun (山地明)
- Sandimmune
- Sigmasporin
- Sporilen
- Supremunn
- Verkazia
Dados da fonte
Farmacocinética
| Variável | Valor | Unidade |
|---|---|---|
| Biodisp. oral | 30 | % |
| Peso Molecular | 1203 | daltons |
| Unión proteínas | 93 | % |
| Vd | 3 - 5 | l/Kg |
| pKa | 11,83 | - |
| Tmax | 1 - 2 | horas |
| T½ | 6,3 | horas |
| Índice L/P | 0,17 - 0,4 | - |
| Dosis Teórica | 0,015 - 0,15 | mg/Kg/d |
| Dosis Relativa | 0,2 - 3 | % |
| Dosis Rel. Ped. | 0,25 - 5 | % |
Rastreabilidade
Bibliografia
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