Different classes of drugs have been by far used for the treatment of hypertension; the most common are diuretics, β-blocker, calcium channel blockers, ACE inhibitors and angiotensin receptor blockers (ARBS). Over the last few years, it has been developed a new class of drug with an innovative mechanism of action; the direct renin inhibitors (DIRS) act on the renin-angiotensin- aldosterone system (RAA), and block the action of renin enzyme, which is the physiological activator of the system. Aliskiren is considered the progenitor of this new class of drugs and is the first orally renin inhibitor to have passed the third phase of clinical trials. It is an antihypertensive drug that effectively controls blood pressure, with effects comparable or even higher than other classes of hypertensive agents. Aliskiren is able to reduce plasmatic renin activity (PRA), contrary to ACE inhibitors and ARBS; moreover, a lasting reduction of blood pressure, in addition to prolonged PRA suppression, have been observed even after the treatment interruption. Its biological half-life is about 40 hours, which allows best control of blood pressure within 24 hours. Aliskiren does not affect critically the activity of the enzymes of the cytochrome P450 system, that is way it has been associated with few pharmacological interactions. In conclusion, according to several results from the specific studies, aliskiren can be considered a valid alternative for the pharmacological treatment of hypertension, is suitable for the general population, can be used alone or combined with other antihypertensive agents, is effective from moderate to severe hypertension levels, is also suitable for special population such as overweight, aged or diabetic people, with good tollerance and very few side effects compared to placebos.
Diverse classi di farmaci sono usate da tempo per il trattamento dell’ipertensione, tra quelle di prima linea troviamo: diuretici, β-bloccanti, Ca-antagonisti, ACE-I e sartani. Negli ultimi anni è stata sviluppata una nuova classe di farmaci con un meccanismo d’azione innovativo, gli inibitori diretti della renina o DRIS, i quali agiscono a livello del sistema renina-angiotensina-aldosterone (RAA) bloccando l’azione dell’enzima renina, ovvero l’attivatore fisiologico del sistema. Aliskiren rappresenta il capostipite di questa nuova classe di farmaci, è il primo inibitore diretto della renina per via orale ad avere raggiunto e superato la fase tre di sperimentazione clinica. È un farmaco antiipertensivo che esercita un’efficace controllo della pressione, con un effetto paragonabile o addirittura superiore rispetto ad altre classi di agenti antiipertensivi. Aliskiren è in grado di ridurre l’attività plasmatica della renina (PRA) a differenza di ACE-I e sartani, inoltre è stata osservata una persistente riduzione della pressione arteriosa e una soppressione prolungata della PRA anche dopo la sospensione del trattamento. Ha un’emivita di eliminazione media di 40 ore che permette un controllo ottimale della pressione nelle 24 ore. Non influenza significativamente l’attività degli enzimi del sistema citocromo P450, per questo è stato associato a poche interazioni farmacologiche. Dai numerevoli risultati ottenuti dagli studi eseguiti si può concludere che aliskiren rappresenta un’interessante opzione di trattamento farmacologico dell’ipertensione, utilizzabile nella popolazione generale, da solo o in combinazione con altri agenti antiipertensivi, con una buona efficacia per diversi gradi di ipertensione da lieve-moderata a grave ed anche in popolazioni speciali quali obesi, anziani e diabetici, con buona tollerabilità e ridotti effetti collaterali comparabile a placebo.
Aliskiren: nuovo approccio terapeutico per il trattamento dell’ipertensione arteriosa
PEDRI, MONICA
2014/2015
Abstract
Different classes of drugs have been by far used for the treatment of hypertension; the most common are diuretics, β-blocker, calcium channel blockers, ACE inhibitors and angiotensin receptor blockers (ARBS). Over the last few years, it has been developed a new class of drug with an innovative mechanism of action; the direct renin inhibitors (DIRS) act on the renin-angiotensin- aldosterone system (RAA), and block the action of renin enzyme, which is the physiological activator of the system. Aliskiren is considered the progenitor of this new class of drugs and is the first orally renin inhibitor to have passed the third phase of clinical trials. It is an antihypertensive drug that effectively controls blood pressure, with effects comparable or even higher than other classes of hypertensive agents. Aliskiren is able to reduce plasmatic renin activity (PRA), contrary to ACE inhibitors and ARBS; moreover, a lasting reduction of blood pressure, in addition to prolonged PRA suppression, have been observed even after the treatment interruption. Its biological half-life is about 40 hours, which allows best control of blood pressure within 24 hours. Aliskiren does not affect critically the activity of the enzymes of the cytochrome P450 system, that is way it has been associated with few pharmacological interactions. In conclusion, according to several results from the specific studies, aliskiren can be considered a valid alternative for the pharmacological treatment of hypertension, is suitable for the general population, can be used alone or combined with other antihypertensive agents, is effective from moderate to severe hypertension levels, is also suitable for special population such as overweight, aged or diabetic people, with good tollerance and very few side effects compared to placebos.È consentito all'utente scaricare e condividere i documenti disponibili a testo pieno in UNITESI UNIPV nel rispetto della licenza Creative Commons del tipo CC BY NC ND.
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https://hdl.handle.net/20.500.14239/17925