{"id":90957,"date":"2018-02-10T20:00:00","date_gmt":"2018-02-10T20:00:00","guid":{"rendered":""},"modified":"2023-01-06T20:44:59","modified_gmt":"2023-01-06T20:44:59","slug":"biguanide_10","status":"publish","type":"post","link":"https:\/\/cvnextjob.com\/index.php\/2018\/02\/10\/biguanide_10\/","title":{"rendered":"Biguanide"},"content":{"rendered":"
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Baze farmacodinamice Nu stimuleaz\u0103 pancreasul fiind active \u015fi \u00een absen\u0163a acestuia \u015fi \u00een diabetul aloxanic precum \u015fi dup\u0103 hipofizectomie \u015fi suprarenalectomie. Inhib\u0103 absorb\u0163ia glucozei din intestin. Inhib\u0103 neoglucogeneza \u015fi glicogenoliza hepatic\u0103 \u015fi stimuleaz\u0103 glicoliza anaerob\u0103. (Shen, Bressler, 1977). La animale normale ac\u0163iunea apare numai dup\u0103 doze mari. La om efectul hipoglicemiant apare \u00een doze terapeutice numai la diabetici cu hiperglicemie. Ac\u0163iunea este cu at\u00e2t mai slab\u0103 cu c\u00e2t diabetul este mai echilibrat. Biguanidele favorizeaz\u0103 consumul intracelular de glucoz\u0103, reactiveaz\u0103, la nivelul mu\u015fchilor, insulina inactivat\u0103 prin legarea de proteine.la om ac\u0163iunea \u00eencepe dup\u0103 2-3 zile \u015fi este maxim\u0103 dup\u0103 15-30 zile. Au efect cetogen precum \u015fi anorexigen, antilipidogen, fibrinolitic, hipotiroidian. Baze farmacotoxicologice Hiporexie, gre\u0163uri, gust metalic, usc\u0103ciunea gurii, constipa\u0163ie sau diaree. Anestezie, cefalee. Un efect advers particular, cunoscut de mult timp, este acidoza lactic\u0103, fenomen cu inciden\u0163\u0103 rar\u0103 dar grav, uneori letal. Concentra\u0163ia lactatului este propor\u0163ional\u0103 cu doza administrat\u0103. Efectul este consecin\u0163a cre\u015fterii glicolizei anaerobe. Acest efect advers este mai frecvent la finformin (Phenforminum\u2014D.C.I., Dibotin R , D.B.I.R , InsoralR). Datorit\u0103 acestui efect, produsele care con\u0163in fenformin, au fost supuse restric\u0163iilor sau retrase din terapeutic\u0103 \u00een unele \u0163\u0103ri (ex. R.F.G., Canada, Norvegia, S.U.A.). \u00cen alte \u0163\u0103ri s-a considerat c\u0103 se poate men\u0163ine \u00een uz substan\u0163a respectiv\u0103, dar se insist\u0103 pt. respectarea anumitor indica\u0163ii, valabile pt. toate biguanidele care reduc la minimum riscul de acidoz\u0103 lactic\u0103. Baze farmacoterapice \u015fi farmacoepidemiologice Pt. a ob\u0163ine efecte terapeutice optime \u015fi a evita reac\u0163iile adverse, \u00eendeosebi acidoza lactic\u0103 trebuie s\u0103 se aib\u0103 \u00een vedere mai multe aspecte. Prescrierea biguanidelor se va face numai la diabetici adul\u0163i, neinsulinodependen\u0163i, f\u0103r\u0103 tendin\u0163\u0103 la cetoz\u0103, fie \u00een asociere cu o sulfoniluree, fie c\u00e2nd tratamentul dietetic sau sc\u0103derea ponderal\u0103 sunt insuficiente sau c\u00e2nd sulfonilureele nu pot fi folosite. Pe c\u00e2t posibil, se vor evita, pentru formin, doze mai mari de 100 mg\/zi:; preparatele retard, care evit\u0103 atingerea de concentra\u0163ii mari, ar fi preferabile. Se va da aten\u0163ie deosebit\u0103 cazurilor de contraindica\u0163ii, reprezentate de situa\u0163ii patologice care favorizeaz\u0103 acidoza lactic\u0103, de ex. Insuficien\u0163a renal\u0103 ( cu creatinemie peste 1,2 mg%, SI=110 \uf06dmol\/l), insuficien\u0163\u0103 hepatic\u0103, alcoolici, insuficien\u0163\u0103 cardiac\u0103, infarct miocardic, st\u0103ri care favorizeaz\u0103 hipoxia (\u015foc cardiogen sau toxiinfec\u0163ios, hemoragii, embolie pulmonar\u0103, gangren\u0103, tulbur\u0103ri ale circula\u0163iei arteriale periferice), diete hipocalorice severe \u015fi \u00eendeosebi st\u0103rile de inani\u0163ie, administrarea de diuretice \u015fi antihipertensive care pot afecta func\u0163ia renal\u0103, urografie. Bolnavii la care se administreaz\u0103 buguanide vor fi examina\u0163i periodic, pt. a decela factorii \u015fi condi\u0163iile care pot favoriza acidoza lactic\u0103; va avea \u00een vedere c\u0103 persoanele care au dep\u0103\u015fit v\u00e2rsta de 60 de ani sunt mai susceptibile la acest efect advers. Bolnavii trata\u0163i \u015fi cei care \u00eei \u00eengrijesc vor fi instrui\u0163i asupra semnelor de acidoz\u0103 lactic\u0103 (anorexie, gre\u0163uri, vome, cre\u015fterea amplitudinii \u015fi frecven\u0163ei mi\u015fc\u0103rilor respiratorii, dureri abdominale, diaree, pierderea cuno\u015ftin\u0163ei). Exemple de biguanide Diabetin (buforminum) Produc\u0103tor: Sicomed Compozi\u0163ie: Comprimate retard con\u0163in\u00e2nd 100 mg buformin\u0103 clorhidric\u0103. Ac\u0163iune terapeutic\u0103: Antidiabetic oral de sintez\u0103, activ numai \u00een prezen\u0163a insulinei endogene sau exogene. Indica\u0163ii: Diabetul zaharat de tip II c\u00e2nd regimul dietetic nu poate restabili echilibrul metabolic. Contraindica\u0163ii: Coma \u015fi precoma diabetic\u0103, acidoz\u0103, insuficien\u0163a renal\u0103 \u015fi hepatic\u0103 sau cardiovascular\u0103 grav\u0103, sarcin\u0103, diabetul zaharat de tip I netratat corect cu insulin\u0103. Reac\u0163ii adverse: Dup\u0103 1-2 luni de tratament pot ap\u0103rea: astenie, sc\u0103derea \u00een greutate. Mod administrare: Tratamentul va fi strict individualizat, taton\u00e2ndu-se doza eficient\u0103. \u00cen general sunt necesare 2-3 comprimate la pacien\u0163ii cu glicemia de 200 mg %. Doza zilnic\u0103 este de dou\u0103 prize (diminea\u0163a \u015fi seara), dup\u0103 mese. Doza de \u00eentre\u0163inere este de 1-2 comprimate pe zi, asociate la nevoie cu alte antidiabetice orale. Diabetin \u2013 Retard (buformine, buformin-retard, silubin-retard) Prezentare: Comprimate de 170 mg de buformin\u0103 tosilat sub form\u0103 retard. Ac\u0163iune terapeutic\u0103: Biguanid\u0103 antidiabetic\u0103 cu efect prelungit. Indica\u0163iile \u015fi contraindica\u0163iile sunt acelea\u015fi cu ale medicamentului Meguan. Administrare: Dou\u0103 prize, diminea\u0163a \u015fi seara. Poate fi suficient un singur comprimat, diminea\u0163a. Reac\u0163ii adverse: Anorexie, gust metalic sau amar, grea\u0163\u0103, vom\u0103, diaree, foarte rar acidoz\u0103 lactic\u0103 (risc letal, se opre\u015fte medica\u0163ia imediat \u015fi se instituie tratamentul adecvat). Mai bine suportat dec\u00e2t meguanul. Meguan (metforminum) Produc\u0103tor: Sicomed Compozi\u0163ie: Comprimate con\u0163in\u00e2nd 0,500 g clorhidrat de metformin\u0103. Ac\u0163iune farmacoterapeutic\u0103: Agent hipoglicemiant din grupa biguamidelor, ce favorizeaz\u0103 consumul intracelular de glucoz\u0103 \u015fi reactiveaz\u0103 la nivel muscular insulina inactivat\u0103 prin legarea de proteine. Timpul de \u00eenjum\u0103t\u0103\u0163ire este aproximativ 3 ore; nu se leag\u0103 de proteinele plasmatice; se excret\u0103 prin urin\u0103 sub form\u0103 nemodificat\u0103. Indica\u0163ii: \u00cen asociere cu regimul alimentar \u00een tratamentul diabetului non-insulinodependent de tip II, diabet la obezi, diabet pletoric, diabetul adultului supraponderal, diabetul adultului normoponderal. \u00cen completarea tratamentului cu insulin\u0103 \u00een diabetul zaharat de tip I, diabet instabil, diabet insulinodependent. Contraindica\u0163ii: Insuficien\u0163\u0103 renal\u0103 organic\u0103 sau func\u0163ional\u0103; infec\u0163ie urinar\u0103, deshidratare, vom\u0103, febr\u0103, st\u0103ri infec\u0163ioase, insuficien\u0163\u0103 hepatocelular\u0103, intoxica\u0163ie alcoolic\u0103 acut\u0103, decompensare acidocetozic\u0103, precom\u0103 diabetic\u0103, sarcin\u0103. Reac\u0163ii adverse: Tulbur\u0103ri gastrointestinale la \u00eenceputul tratamentului ce se redreseaz\u0103 spontan. Mod de administrare: \u00cen diabetul noninsulinodependent: 2-3 comprimate pe zi \u00een timpul meselor sau dup\u0103 (posologie adoptat\u0103 \u00een func\u0163ie de testele biologice); \u00een diabetul insulinodependent, \u00een completarea tratamentului cu insulin\u0103, 2-3 tb.\/zi. Condi\u0163ii de p\u0103strare: La ad\u0103post de lumin\u0103, umiditate \u015fi c\u0103ldur\u0103. Metformin BMS \u2013 antidiabetic oral (metforminum) Prezentare: Con\u0163ine clorhidrat de metformin BP ca substan\u0163\u0103 activ\u0103; con\u0163ine 500 mg metformin: comprimate filmate albe, rotunde, convexe. Propriet\u0103\u0163i: Reducerea glucozei \u00een s\u00e2nge \u00een prezen\u0163a insulinei endogene sau exogene. Nu cauzeaz\u0103 crize hipoglicemice. Efect de sc\u0103dere ponderal\u0103 la diabetici. Absorb\u0163ia este relativ lent\u0103, comparativ cu eliminarea rapid\u0103 sub form\u0103 nemodificat\u0103. Indica\u0163ii: Diabet zaharat stabil la maturitate, necomplicat cu cetoze, \u00een special la supraponderali. Este necesar\u0103 combinarea cu sulfoniluree \u00een cazurile dificile. Metformin poate fi utilizat \u00een diabete labile ca supliment al tratamentului cu insulin\u0103 pentru a evita criza hipoglicemic\u0103. Dozaj \u015fi administrare: Individualizat, ini\u0163ial 500 mg de dou\u0103 ori pe zi, la mas\u0103, ce se poate cre\u015fte gradat la maxim 1 g de trei ori pe zi. Dozajul de men\u0163inere este 1,7 g zilnic \u00een doz\u0103 unic\u0103 diminea\u0163a sau divizat\u0103 \u00een dou\u0103 doze. Contraindica\u0163ii: Metformin este contraindicat \u00een cetoacidoz\u0103 sau com\u0103 diabetic\u0103, insuficien\u0163a sever\u0103 renal\u0103 sau hepatic\u0103, cardiac\u0103 sau infarct miocardic recent. Nu este recomandat\u0103 administrarea \u00een sarcin\u0103. Al\u0103ptare: nu exist\u0103 informa\u0163ii suficiente. Efecte adverse: Este bine tolerat, dar se pot produce tulbur\u0103ri gastrointestinale care dispar cu reducerea dozajului. Se va \u00eencepe cu doze mici care cresc treptat. Rar, reac\u0163ii alergice u\u015foare. Precau\u0163ii: Nu se produce hipoglicemie prin monoterapie cu Metformin. Totu\u015fi, ea se poate produce c\u00e2nd se administreaz\u0103 Metformin \u00eempreun\u0103 cu sulfoniluree, insulin\u0103 sau alcool. La doze excesive, se poate declan\u015fa acidoza. Semne \u015fi simptome sugestive sunt: grea\u0163\u0103, diaree, durere abdominal\u0103, dispnee. Tratament: Este recomandat\u0103 terapia intens\u0103 de sus\u0163inere care trebuie condus\u0103 spre corectare pierderii de lichid \u015fi a tullbur\u0103rilor metabolice.<\/div>\n","protected":false},"excerpt":{"rendered":"

Baze farmacodinamice Nu stimuleaz\u0103 pancreasul fiind active \u015fi \u00een absen\u0163a acestuia \u015fi \u00een diabetul aloxanic precum \u015fi dup\u0103 hipofizectomie \u015fi suprarenalectomie. Inhib\u0103 absorb\u0163ia glucozei din intestin. Inhib\u0103 neoglucogeneza \u015fi glicogenoliza hepatic\u0103 \u015fi stimuleaz\u0103 glicoliza anaerob\u0103. (Shen, Bressler, 1977). La animale normale ac\u0163iunea apare numai dup\u0103 doze mari. La om efectul hipoglicemiant apare \u00een doze terapeutice […]<\/p>\n","protected":false},"author":2,"featured_media":0,"comment_status":"closed","ping_status":"closed","sticky":false,"template":"","format":"standard","meta":[],"categories":[1],"tags":[],"aioseo_notices":[],"_links":{"self":[{"href":"https:\/\/cvnextjob.com\/index.php\/wp-json\/wp\/v2\/posts\/90957"}],"collection":[{"href":"https:\/\/cvnextjob.com\/index.php\/wp-json\/wp\/v2\/posts"}],"about":[{"href":"https:\/\/cvnextjob.com\/index.php\/wp-json\/wp\/v2\/types\/post"}],"author":[{"embeddable":true,"href":"https:\/\/cvnextjob.com\/index.php\/wp-json\/wp\/v2\/users\/2"}],"replies":[{"embeddable":true,"href":"https:\/\/cvnextjob.com\/index.php\/wp-json\/wp\/v2\/comments?post=90957"}],"version-history":[{"count":0,"href":"https:\/\/cvnextjob.com\/index.php\/wp-json\/wp\/v2\/posts\/90957\/revisions"}],"wp:attachment":[{"href":"https:\/\/cvnextjob.com\/index.php\/wp-json\/wp\/v2\/media?parent=90957"}],"wp:term":[{"taxonomy":"category","embeddable":true,"href":"https:\/\/cvnextjob.com\/index.php\/wp-json\/wp\/v2\/categories?post=90957"},{"taxonomy":"post_tag","embeddable":true,"href":"https:\/\/cvnextjob.com\/index.php\/wp-json\/wp\/v2\/tags?post=90957"}],"curies":[{"name":"wp","href":"https:\/\/api.w.org\/{rel}","templated":true}]}}