Raloxifene

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Raloxifene


Nome IUPAC
[6-hydroxy-2-(4-hydroxyphenyl)-benzothiophen-3-yl]-[4-[2-(1-piperidyl)ethoxy]phenyl]-methanone
Caratteristiche generali
Formula bruta o molecolare	C₂₈H₂₇NO₄S
Massa molecolare (u)	473.584 g/mol
Numero CAS	84449-90-1
Numero EINECS	686-786-1
Codice ATC	G03XC01
PubChem	5035
DrugBank	DBDB00481
SMILES	`C1CCN(CC1)CCOC2=CC=C(C=C2)C(=O)C3=C(SC4=C3C=CC(=C4)O)C5=CC=C(C=C5)O`
Dati farmacologici
Modalità di somministrazione	Orale
Indicazioni di sicurezza
Frasi H	---
Consigli P	---^[1]
Modifica dati su Wikidata · Manuale

Il raloxifene è un farmaco della categoria dei modulatori selettivi del recettore degli estrogeni, utilizzato nella pratica clinica per contrastare, nella donna in postmenopausa, gli effetti negativi della carenza di estrogeni sul metabolismo osseo. Trova applicazione nella prevenzione di fratture osteoporotiche^[2]. Sono in corso (2018) studi per la sua approvazione come trattamento per la prevenzione del tumore alla mammella^[3].

Indicazioni

Prevenzione e Trattamento dell'Osteoporosi post-menopausale per ridurre il rischio di frattura vertebrale

Il Raloxifene ha dimostrato negli studi clinici di ridurre le fratture vertebrali di circa il 35 % ma non ha mostrato effetti di riduzione delle fratture extra-vertebrali o fratture di femore. Dagli studi eseguiti è emerso che il Raloxifene è in grado di ridurre l'incidenza di cancro al seno estrogeno positivo (ER+) similmente al Tamoxifene.

Negli USA il farmaco è stato oggetto di una controversia, riguardante la Eli Lilly and Company, riferita alla promozione commerciale fatta sulla presunta riduzione del rischio di cancro alla mammella e del rischio cardiovascolare.

In Italia il Raloxifene è stato autorizzato dall'AIFA per uno Studio clinico di fase 3 per valutare l’efficacia e la sicurezza in pazienti adulti paucisintomatici affetti da COVID-19.^[4]

Dosaggi

Osteoporosi, 60 mg 1 volta al giorno.

Controindicazioni

Sconsigliato in soggetti con insufficienza renale ed epatica, da evitare in caso di gravidanza, allattamento materno e presenza di carcinoma endometriale. Prima di somministrare occorre effettuare un'accurata anamnesi al riguardo delle trombosi venose.

Effetti indesiderati

Fra gli effetti indesiderati si riscontrano trombosi venosa, vampate, ipertensione, insonnia, cefalea, nausea, rash cutaneo, edema, crampi che si dislocano alle gambe.

Note

^ Sigma Aldrich; rev. del 28.08.2012, riferita al cloridrato
^ http://www.agenziafarmaco.gov.it/sites/default/files/Determinazione_446-2017_agg_nota79.pdf
^ https://www.ncbi.nlm.nih.gov/pubmed/18462184
^ Sperimentazioni cliniche - COVID-19 | Agenzia Italiana del Farmaco, su aifa.gov.it. URL consultato il 26 aprile 2021.

Bibliografia

British national formulary, Guida all’uso dei farmaci 4 edizione, Lavis, agenzia italiana del farmaco, 2007.

Altri progetti

Wikimedia Commons contiene immagini o altri file su raloxifene

Collegamenti esterni

(EN) raloxifene, su Enciclopedia Britannica, Encyclopædia Britannica, Inc.

Portale Chimica

Portale Medicina

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