Beta-bloccanti
Meccanismi d’azione dei beta-bloccanti
I beta-bloccanti sono farmaci che bloccano i recettori adrenergici beta:
Beta-1
Sono recettori presenti a livello cardiaco, la cui inibizione ha un effetto inotropo e cronotropo negativo.
Beta-2
Sono recettori presenti soprattutto a livello vascolare e bronchiale la cui inibizione provoca broncocostrizione.
Classificazione (inibizione recettori beta-1)
Beta-bloccanti cardioselettivi.
- es. metoprololo, atenololo, bisoprololo.
Sono utilizzati per trattare l’ipertensione, l’insufficienza cardiaca, l’angina, l’infarto del miocardio.
Beta-bloccanti non cardioselettivi (inibizione recettori beta-1 e beta-2)
- Es. propranololo, sotalolo, pindololo.
Sono utilizzati per trattare l’ipertensione, l’angina, le aritmie.
Beta-bloccanti con effetto vasodilatatore associato.
Antagonisti beta e alfa-1
- Carvedilolo, labetalolo.
Antagonisti beta-1 e agonisti beta-2
- Bisoprololo
Beta-bloccanti con attività simpatico-mimetica intrinseca associata.
- Pindololo, alprenololo, acebutololo, oxprenololo.
Si tratta di farmaci con attività beta agonista debole e quindi inibiscono l’azione di agonisti più potenti. Non diminuiscono molto la frequenza cardiaca a riposo, ma impediscono che aumenti con l’esercizio.
Beta-bloccanti che prolungano l’intervallo QT.
- Sotalolo
Beta-bloccanti con emivita corta.
- Esmololo
Indicazioni
Insufficienza cardiaca dovuta a disfunzione diastolica, come nel caso della cardiomiopatia ipertrofica ostruttiva.
Scompenso cardiaco
I beta-bloccanti inibiscono lo stato iper-catecolaminergico tipico di questa condizione, che è responsabile della destrutturazione delle fibre cardiache e del rimodellamento miocardico. E’ stato dimostrato che aumentano la sopravvivenza nei pazienti con insufficienza cardiaca sistolica, quindi devono sempre essere somministrati in questo contesto se il paziente li tollera. Si consiglia di introdurli nel momento in cui il paziente è stabile emodinamicamente ed euvolemico, e di iniziare con una dose bassa, aumentandola gradualmente. I beta-bloccanti che hanno dimostrato di migliorare la sopravvivenza nei pazienti con insufficienza cardiaca sono: carvedilolo metropolo, bisoprololo e nebivololo.
Cardiopatia ischemica
Sono indicati nel trattamento dell’angina pectoris perché limitano il consumo di ossigeno riducendo la frequenza cardiaca e la contrattilità miocardica. Fanno inoltre parte del trattamento precoce nell’infarto miocardico non complicato, visto che è in tale contesto hanno dimostrato di ridurre la mortalità, l’incidenza di morte improvvisa e in alcuni casi il reinfarto.
Ipertensione arteriosa
I beta-bloccanti non selettivi sono indicati in situazioni internistiche in cui è necessario un effetto “down” sistemico, ossia: ipertiroidismo, tremore essenziale, dissezione aortica, profilassi dell’emicrania, ecc..
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