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Progestinici. Definizione

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Progestinici. Definizione Progestinici. Definizione • I progestinici sono prodotti di sintesi che, come il progesterone, "trasformano" l'endometrio preparato dagli estrogeni, inducendovi quelle modificazioni di tipo "secretorio" che, alla sospensione del trattamento, ne permettono lo sfaldamento con un regolare flusso mestruale. Title • time and place of presentation • Page # 1 PROGESTINICI DI SINTESI • POICHE’ IL PROGESTERONE NATURALE E’ POCO ATTIVO SE SOMMINISTRATO PER VIA ORALE, A CAUSA DI UNA IMPORTANTE INATTIVAZIOZIONE EPATICA, LA RICERCA FARMACOLOGICA SI E’ DA SEMPRE INDIRIZZATA SULLO SVILUPPO DI PROGESTINICI DI SINTESI CON ADEGUATA POTENZA PROGESTINICA E ADEGUATA BIODISPONIBILITA’ ORALE. Title • time and place of presentation • Page # 2 PROGESTINICI DI SINTESI • Progestinici = • Progesterone naturale + • prodotti di sintesi Title • time and place of presentation • Page # 3 Progestinici di sintesi • Prodotti dotati di elevata attività dovuta • - ad alta affinità con i recettori per il PROGESTERONE • - e/o a lenta metabolizzazione • - e/o a produzione di metaboliti attivi così da poter essere impiegati, contrariamente al PROGESTERONE, a basso dosaggio anche per via orale. Title • time and place of presentation • Page # 4 Progestinici Sintetici PRODOTTI CON ELEVATA ATTIVITA’ PER: • Alta affinità per i recettori • Rallentata metabolizzazione e lunga emivita • Produzione di metaboliti attivi • (es. desogestrel >> 3 -keto - DSG) • Combinazione dei punti precedenti • Possibilità di somministrazione a bassi dosaggi per via orale, a differenza del progesterone naturale Title • time and place of presentation • Page # 5 Progestinici di sintesi impiegati nella terapia sostitutiva • Derivati del progesterone - didrogesterone (retroprogesterone) • Derivati del 19-nortestosterone - noretisterone acetato - levonorgestrel • Derivati del 17-idrossiprogesterone - medrossiprogesterone acetato (MAP) - medrogestone - ciproterone acetato • Derivati del 19-norprogesterone - nomegestrolo acetato Title • time and place of presentation • Page # 6 Formula di struttura del colesterolo e di alcuni progestinici OH …. C CH HO Colesterolo O Noretisterone CH3 CH3 OH CH2 OH ….C CH CH 2 ….C CH O Levonorgestrel O Gestodene (⊗15 levonorgestrel) Title • time and place of presentation • Page # 7 CLASSIFICAZIONE DEI PROGESTINICI (I) • a) derivati del P naturale • - P micronizzato • - didrogesterone • b) derivati del 17OH - progesterone • - MAP • - CPA Title • time and place of presentation • Page # 8 CLASSIFICAZIONE DEI PROGESTINICI (II) • Pregnani: Metile in C18 sostituito da gruppo etile C21 derivati dal progesterone • Estrani: C18 derivati dal testosterone (C19). • Gruppo metile in C19 • Gonani: C18 derivati dal testosterone (C19). Title • time and place of presentation • Page # 9 Progesterone like derivatives C – H3 • Micronized progesterone C - O • Dehydroprogesterone • Medrogestone • Nomegestrol acetate O 17 progesterone derivatives • medroxyprogesterone acetate OH C-CH • cyproterone acetate • clormadinone acetate megestrol acetate • O 19 nortestosterone derivatives C – H3 C - • noretisterone C – H2 • noretisterone acetate O • desogestrel • gestodene • norgestimate O Title • time and place of presentation • Page # 10 Progestinici molecola nome commerciale . medrossiprogesterone ac. Provera G, Farlutal . Didrogesterone Dufaston . medrogestone Colprone . Levonorgestrel Microlut . nomegestrolo acetato Lutenyl . noretisterone acetato Primolut-Nor . progesterone micronizzato Esolut, Crinone, Prometrium Title • time and place of presentation • Page # 11 Classificazione dei Progestinici di Sintesi Spirolactone Pregnan Estran Gonan i i i Norpregnani Noretisterone Levonorgestrel Nomegestrolo Etinodiol Linestrenolo o Nestoron Dienoges Norgestimate e t MAP Clormadinone Desogestre l Drospirenone Ciproterone Didrogesterone Gestoden e Trimegestrone Title • time and place of presentation • Page # 12 L’albero dei Progestinici Puro Agonista attività attività Antiestrogena Progesterone CPA Antiandrogena CMA LNG DNG DRSP attività Estrogena NETA LNG DSG attività MPA GSD Androgena MGA attività Glucocorticoide DRSP attività Antimineralo- corticoide Title • time and place of presentation • Page # 13 PROGESTINICI vie di somministrazione • Via Orale (Progestinici di sintesi, P Micronizzato) • Via Percutanea (Progesterone) • Via Transdermica (NETA, Levonorgestrel) • Via Vaginale (Progesterone) • Via Intramuscolare (Progesterone; 17OH-progesterone caproato) • Via Intrauterina (IUD) (Levonorgestrel) Title • time and place of presentation • Page # 14 PROGESTINICI Farmacocinetica e Biodisponibilità • Variabilità tra i diversi progestinici nel legame con le binding proteins plasmatiche (Albumina,CBG, SHBG) • Peculiarità delle varie vie di somministrazione Title • time and place of presentation • Page # 15 PROGESTINICI FARMACOCINETICA E BIODISPONIBILITA’ legame di differenti progestinici alle proteine di trasporto Title • time and place of presentation • Page # 16 Processi principali che influenzano la farmacocinetica di un ormone steroideo dopo somministrazione orale tessuti Tratto GI Legame Rilascio dalla fegato plasma a proteine forma assunta e recettori Metabolismo Legame a enzimatico proteine tessuti Clivaggio degli Steroidi coniugati Prodotti finali del metabolismo Title • time and place of presentation • Page # 17 Farmacocinetica del progesterone • Il progesterone micronizzato, somministrato per via orale, viene rapidamente assorbito e metabolizzato a livello intestinale ed epatico. • Livelli plasmatici massimi di progesterone vengono raggiunti assieme ai suoi prinicipali metaboliti dopo ca 4 ore. • La somministrazione orale di 200mg di progesterone garantiscono livelli plasmatici simili alla fase luteale per non oltre 6-7 ore. • Anche dosi maggiori per os non sembrano garantire una adeguata trasformazione endometriale in menopausa. Title • time and place of presentation • Page # 18 Parametri farmacocinetici di vari progestinici Parametro NET NETA LNG GSD DSG DRSP Biodisponibilità (% della 65 ~50* 100 100 75** ~ 76 dose orale) Emivita (ore) 8 8* 16 12 12** 30 Volume di distribuzione 240 240* 120 32 110** 4 L/kg (litri) *dati relativi al NET che è il metabolita attivo del NETA Fotherby, 1994 **dati relativi al metabolita principale, 3-keto-DSG Kuhnz, 1990 ***dati non disponibili Kuhnz, 1992 Title • time and place of presentation • Page # 19 Livelli sierici di P dopo somministrazione per differenti vie ng/ml Crema vaginale (100 mg) os (100 mg) i.m. (50 mg) ovuli (100 mg) ore Sitruk-Ware R. Contraception 1987;36:373 Title • time and place of presentation • Page # 20 Livelli sierici di P dopo somministrazione di 50mg di progesterone per via vaginale prima e dopo estrogenizzazione ng/ml dopo trattamento con ECE prima ore Sitruk-Ware R. Contraception 1987;36:373 Title • time and place of presentation • Page # 21 Azioni dei progestinici. I. • Oltre all'azione sull'endometrio, il PROGESTERONE e i PROGESTINICI presentano una serie di altri effetti, parte dei quali può avere rilievo clinico. • Alcuni di tali effetti differiscono molto a seconda del dosaggio e della via di somministrazione del farmaco ed anche a seconda dell'entità dell'azione determinata dal contemporaneo trattamento estrogenico. • Alcuni effetti sono praticamente nulli con il progesterone e con certi progestinici, mentre sono presenti o particolarmente spiccati con altri progestinici. Ciò è dovuto al fatto che questi ultimi, per analogie d'ordine biochimico, presentano anche azioni proprie di altri ormoni steroidei. Title • time and place of presentation • Page # 22 Azioni dei progestinici. II. • In particolare i vecchi derivati del 19-nortesto-sterone, quali il noretisterone acetato e il norgestrel, presentano una residua AZIONE ANDROGENICA; • azione androgenica, se pur decisamente meno spiccata e per certi aspetti irrilevante, possiede anche il MAP; • praticamente privi di azioni androgenica sono altri derivati del 17 idrossiprogesterone (ciproterone acetato, medrogestone), i derivati del progesterone (didrogesterone) e quelli del 19-norprogesterone (nomegestrolo acetato). Title • time and place of presentation • Page # 23 Azione dei progestinici. III. • La residua AZIONE ANDROGENICA di un progestinico si manifesta soprattutto quando questo sia somministrato per os (a causa del “primo passaggio epatico"), con effetti che contrastano quelli determinati dagli estrogeni. Title • time and place of presentation • Page # 24 Attività farmacodinamiche dei diversi progestinici attività attività attività anti- attività attività androgena progestinica glucocorticoide androgena antimineralcort PROGESTERONE + - - + + LEVONORGESTREL + - + - - DESOGESTREL + - + - - GESTODENE + - + +* - NORGESTIMATE + - + - - CIPROTERONE A. + +* - + - DIENOGEST + - - + - DROSPIRENONE + - - + + *) attività trascurabile alle dosi d’uso Title • time and place of presentation • Page # 25 Schindler A E et Al. Maturitas, 2003; 46S1:S7-S16 Title • time and place of presentation • Page # 26 Effetti metabolici dei progestinici di sintesi } LDL metabolismo lipidico HDL } trigliceridi metabolismo glucidico resistenza periferica insulina iperinsulinemia } SHBG metabolismo proteico fibrinolisi IGF-1 IGFBP-1 Title • time and place of presentation • Page # 27 Attività Antiandrogena Dienogest Clormadinone TM CPA NOM G ac Riduzion e 100 40 20 15 prostata ratto (%) Drospirenon Progestero e ne Sitruk-Ware, Climacteric 2005 Title • time and place of presentation • Page # 28 attività Antiandrogena Efficacia Relativa 100 Hershberger test 50 100 40 30 20 0 10 CPACPA DNGDNG DRSPDRSP CMACMA
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