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Farmaci della coagulazione
Coagulanti:
- Nonafact è usato per il trattamento e la prevenzione delle emorragie in pazienti con emofilia B (patologia emorragica ereditaria causata dalla carenza di fattore IX
- Ac. tranexamico: (Tranex fl, Ugurol fl): ctg B1 della FDA e quindi da utilizzare solo in caso di effettiva necessità.
- Trombina ad azione locale: (spongostan emostatico spugnette) utilizzato in forma di spugna di gel riassorbibile; converte il fibrinogeno in fibrina
- Etamsilato (Dicynone): l’azione terapeutica del Dicynone si esplica attraverso un aumento dell’adesività piastrinica, senza peraltro interferire con il fenomeno dell’aggregazione.
Anticoagulanti:
- le cumarine possono attraversare la placenta e arrivare al feto, che è molto sensibile alla loro azione. La sindrome fetale da warfarin si può verificare fino nel 25% dei feti esposti alla warfarina durante il 1° trimestre; le anomalie includono l’ipoplasia del naso, la granulia miliariforme delle ossa (evidenziabile alle radiografie), l’atrofia ottica bilaterale e i vari gradi di ritardo mentale. L’esposizione alla warfarin durante il 2-3° trimestre è stata correlata all’atrofia ottica, alla cataratta, al ritardo mentale, alla microcefalia e alla microftalmia. Si possono inoltre verificare delle emorragie fetali e materne.
- Eparina, una grande molecola a elevata carica con un passaggio transplacentare minimo, è l’anticoagulante di prima scelta durante la gravidanza. Tuttavia, il prolungato (>6 mesi) uso in gravidanza può causare, nella madre, osteoporosi e trombocitopenia.
- Eparine a basso peso molecolare: rispetto all’eparina presentano un minimo passaggio transplacentare; un minor rischio di trombocitopenia e osteoporosi e non sono assorbite dal tubo digerente fetale.
- Abciximab (Reopro): è il frammento Fab di un anticorpo monoclonale chimerico IgG1 prodotto da una linea cellulare
ricombinante in coltura a perfusione continua. Il ReoPro deve essere usato solo in ambiente ospedaliero e in associazione con acido acetilsalicilico ed eparina. È diretto contro il recettore glicoproteico (GP) IIb/IIIa (aIIbß3) situato sulla superficie delle piastrine umane. ReoPro inibisce l’aggregazione piastrinica prevenendo il legame del fibrinogeno, del fattore di von Willebrand e di altre molecole adesive con i siti recettoriali GPIIb/IIIa presenti sulle piastrine attivate. Inoltre ReoPro si lega al recettore della vitronectina (aVß3) presente sulle piastrine e sulle cellule endoteliali. Ctg C; non vi sono dati sulla somministrazione in gravidanza o durante l’allattamento. - Streptotochinasi: è un enzima prodotto da alcuni batteri (fra tutti streptococcus piogene) capace di attivare il plasminogeno in plasmina che a sua volta è capace di solubilizzare la fibrina. Utilizzato nell’infarto del miocardio, embolia polmonare e trombosi venosa profonda. Una piccolo percentuale attraversa la barriera placentare mentre non si hanno dati sull’ecrezione nel latte materno.
- Urochinasi: enzima estratto dall’urina umana che determina l’attivazione enzimatica del sistema fibrinolitico endogeno, convertendo il plasminogeno ematico inattivo in plasmina.
- Reteplase è il nome di un inibitore della protease; in Italia non si trova in commercio. Copia dell’enzima naturale, t-PA, ma modificato in modo che abbia un effetto più rapido e più duraturo. Viene prodotto con il metodo del “DNA ricombinante”: viene cioè ottenuto da un batterio in cui è stato immesso un gene (DNA) che lo rende in grado di produrlo. Reteplase induce la conversione del plasminogeno in plasmina,
- Alteplase: versione ricombinante del tissue Plasminogen Activator ( t-PA ).
- Tenecteplase: noto anche come TNK t-PA è una variante dell’Alteplase. Le lettere T, N, K del TNK t-PA rappresentano le 3 regioni modificate, mediante sostituzione di aminoacidi, a partire dalla proteina naturale t-PA.
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Tab. 18 – Farmaci della coagulazione |
management |
||
|
Coagulanti, antiemorragici |
Trombina ad azione locale |
Spongostan |
Ctg A1 FDA |
|
Ac tranexamico (34) |
Tranex, Ugurol |
Ctg B1; solo in caso |
|
|
Ac. Ascorbico + |
Idro P2 ascorbico cf |
Ctg C; solo in caso |
|
|
Fattore IX della coagulazione |
Nonafact fl ev |
Ctg C della FDA |
|
|
Etamsilato |
Dicynone cpr, fl im/ev |
Ctg B3; non ci sono sufficienti dati sulla |
|
|
anticoagulanti, antiaggreganti |
Cumarine |
Sintrom cpr, Coumadin |
Ctg D della FDA Embriopatia da Warfarin: ipoplasia emorragie neonatali |
|
eparina |
Calciparina fl sc Clarisco fl ev/sc |
Ctg C della FDA Passaggio transplacentare minimo, Non Escrezione nel latte materno minima Osteoporosi e Trombocitopenia nella gravida |
|
|
Eparine a basso peso molecolare |
Fragmin Clexane fl Fraxiparina fl Seleparina Trombenox |
Ctg B3 della FDA Passaggio transplacentare minimo Non assorbite dal tubo digerente fetale minor rischio di trombocitopenia e osteoporosi |
|
|
Abciximab |
Reopro |
Ctg D |
|
|
Streptokinasi (32) |
Streptase, Kabikinase |
Ctg C Modesto passaggio transplacentare; non si |
|
|
Urokinase |
Urokinasi |
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|
Reteplase |
Rapilysin fl |
versione Ctg C Non si |
|
|
Alteplase |
Actilyse , Actplas |
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|
Tenecteplase |
Metalyse |
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