Metformien

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Metformien

Bal-en-stokkiemodel van die metformienmolekuul
Chemie
IUPAC naam N,N-Dimethylimido=
dicarbonimidic diamide
Chemiese formule C4H11N5
Molêre massa 129.167 g/mol
CAS-nommer 657-24-9
Farmakokinetika
Biobeskikbaarheid 50–60%[1][2]
Proteïengebonde Minimaal[1]
Metabolisme Nie deur die lewer
Uitskeiding Uriene (90%)
Halfleeftyd 4–8.7 uur

Metformien, wat onder andere onder die handelsnaam Glucophage verkoop word, is die belangrikste eersteliniemedikasie vir die behandeling van tipe 2-diabetes,[3][4][5][6] veral by mense wat oorgewig is.[7] Dit word ook gebruik in die behandeling van polisistiese ovariumsindroom.[8] Dit word soms as 'n byvoegsel gebruik om die risiko van metaboliese sindroom te verminder by mense wat antipsigotika gebruik.[9] Metformien word nie met gewigstoename geassosieer nie[10] en word per mond geneem.[8]

Metformien word oor die algemeen goed verdra. Algemene newe-effekte sluit in diarree, naarheid en maagpyn.[8] Dit het 'n klein risiko om lae bloedsuiker te veroorsaak. Hoë bloedmelksuurvlakke is 'n bekommernis as die medikasie in te hoë dosisse gebruik word of voorgeskryf word aan mense met ernstige nierprobleme.[11][12]

Metformien is 'n biguanied anti-hiperglukemiese middel. Dit werk deur glukoseproduksie in die lewer te verminder, die insuliensensitiwiteit van liggaamsweefsel te verhoog,[8] en GDF15-afskeiding te verhoog, wat eetlus en kalorie-inname verminder.[13][14][15][16]

Mediese gebruike[wysig | wysig bron]

Metformien word gebruik om bloedglukose te verlaag in diegene met tipe 2 diabetes.[8] Dit word ook gebruik as 'n tweedelyn middel vir onvrugbaarheid by vroue met polisistiese ovariumsindroom.[17]

Tipe 2-diabetes[wysig | wysig bron]

Die American Diabetes Association en die American College of Physicians beveel albei metformien aan as 'n eerstelynmiddel om tipe 2 diabetes te behandel.[18][19][20] Dit is net so effektief as repaglinied en meer effektief as al die ander orale middels vir tipe 2 diabetes.[21]

Die gebruik van metformien verminder liggaamsmassa by mense met tipe 2-diabetes[22][23] in teenstelling met sulfonielureumderivate, wat met gewigstoename geassosieer word.[24] Sommige bewyse toon dat metformien geassosieer word met gewigsverlies in vetsug in die afwesigheid van diabetes.[25][26] Metformien het 'n laer risiko van hipoglukemie as die sulfonielureums,[27][28] alhoewel hipoglukemie selde voorgekom het tydens intense oefening, kalorie-tekort, of wanneer dit saam met ander middels gebruik word om bloedglukose te verlaag.[29][30] Metformien verminder lae-digtheid lipoproteïen en trigliseriede vlakke effens. [31][32]

Gewigsverandering[wysig | wysig bron]

Die gebruik van metformien word tipies geassosieer met gewigsverlies.[33] Dit blyk veilig en doeltreffend te wees om die gewigstoename wat deur die antipsigotiese medisyne olansapien en klosapien veroorsaak word, teen te werk.[34][35] Alhoewel 'n beskeie ommekeer van klosapien-geassosieerde gewigstoename gevind word met metformien, is primêre voorkoming van gewigstoename meer waardevol.[36]

Gebruik saam met insulien[wysig | wysig bron]

Metformien kan die insulienbehoefte verminder by tipe 1-diabetes, alhoewel met 'n verhoogde risiko van hipoglukemie.[37]

Lewensverlenging[wysig | wysig bron]

Daar is bewyse dat metformien nuttig kan wees om lewensduur te verleng, selfs in andersins gesonde mense. Dit het aansienlike belangstelling ontvang as 'n middel wat veroudering vertraag, moontlik deur soortgelyke meganismes as die behandeling van diabetes (insulien- en koolhidraatregulering). [38][39]

Alzheimersiekte[wysig | wysig bron]

Die moontlikheid dat metformien die aanvang of vordering van Alzheimersiekte kan vertraag, of selfs kan voorkom, word ondersoek. Daar is 'n verskeidenheid van navorsing gepubliseer in hierdie veld in 'n poging om 'n korrelasie tussen tipe 2-diabetes en Alzheimer se siekte vas te stel.[40] Navorsing sluit studies in met deelnemers wat nie met diabetes gediagnoseer is nie.[41]

Kontraindikasies[wysig | wysig bron]

Metformien is teenaangedui by mense met:

  • Ernstige nierversaking (geskatte glomerulêre filtrasietempo (eGFR) onder 30 ml/min/1,73 m2 )[42]
  • Bekende hipersensitiwiteit vir metformien[42]
  • Akute of chroniese metaboliese asidose, insluitend diabetiese ketoasidose (van onbeheerde diabetes),[42] met of sonder koma [43]

Nadelige gevolge[wysig | wysig bron]

Die mees algemene nadelige effek van metformien is gastroïntestinale irritasie, insluitend diarree, krampe, naarheid, braking en verhoogde winderigheid; Metformien word meer algemeen geassosieer met gastroïntestinale nadelige effekte as die meeste ander antidiabetiese medisyne.[44] Die ernstigste potensiële nadelige effek van metformien is melksuur-asidose; hierdie komplikasie is skaars, en blyk verband te hou met verswakte lewer- of nierfunksie.[45] Metformien is nie goedgekeur vir gebruik in diegene met ernstige niersiekte nie, maar kan steeds gebruik word teen laer dosisse in diegene met nierprobleme.[46]

Chemie[wysig | wysig bron]

Metformienhidrochloried (1,1-dimetielbiguaniedhidrochloried) is vrylik oplosbaar in water, effens oplosbaar in etanol, maar byna onoplosbaar in asetoon, eter of chloroform. Die pKa van metformien is 12,4.[47] Die gewone sintese van metformien, wat oorspronklik in 1922 beskryf is, behels die eenpotreaksie van dimetielamienhidrochloried en 2-sianoguanidien oor hitte.[48][49]

Verwysings[wysig | wysig bron]

  1. ↑ 1,0 1,1 Dunn CJ, Peters DH (Mei 1995). "Metformin. A review of its pharmacological properties and therapeutic use in non-insulin-dependent diabetes mellitus". Drugs. 49 (5): 721–49. doi:10.2165/00003495-199549050-00007. PMID 7601013.
  2. ↑ Hundal RS, Inzucchi SE (2003). "Metformin: new understandings, new uses". Drugs. 63 (18): 1879–94. doi:10.2165/00003495-200363180-00001. PMID 12930161.
  3. ↑ Draznin B, Aroda VR, Bakris G, Benson G, Brown FM, Freeman R, et al. (Januarie 2022). "9. Pharmacologic Approaches to Glycemic Treatment: Standards of Medical Care in Diabetes-2022". Diabetes Care. 45 (Suppl 1): S125–S143.
  4. ↑ Cosentino F, Grant PJ, Aboyans V, Bailey CJ, Ceriello A, Delgado V, et al. (Januarie 2020). "2019 ESC Guidelines on diabetes, pre-diabetes, and cardiovascular diseases developed in collaboration with the EASD". European Heart Journal. 41 (2): 255–323.
  5. ↑ "Metformin Hydrochloride". The American Society of Health-System Pharmacists. Geargiveer vanaf die oorspronklike op 24 Desember 2016. Besoek op 2 Januarie 2017.
  6. ↑ Maruthur NM, Tseng E, Hutfless S, Wilson LM, Suarez-Cuervo C, Berger Z, et al. (Junie 2016). "Diabetes Medications as Monotherapy or Metformin-Based Combination Therapy for Type 2 Diabetes: A Systematic Review and Meta-analysis". Annals of Internal Medicine. 164 (11): 740–751. doi:10.7326/M15-2650. PMID 27088241. S2CID 32016657.
  7. ↑ Cosentino F, Grant PJ, Aboyans V, Bailey CJ, Ceriello A, Delgado V, et al. (Januarie 2020). "2019 ESC Guidelines on diabetes, pre-diabetes, and cardiovascular diseases developed in collaboration with the EASD". European Heart Journal. 41 (2): 255–323. doi:10.1093/eurheartj/ehz486. PMID 31497854.
  8. ↑ 8,0 8,1 8,2 8,3 8,4 "Metformin Hydrochloride". The American Society of Health-System Pharmacists. Geargiveer vanaf die oorspronklike op 24 Desember 2016. Besoek op 2 Januarie 2017.
  9. ↑ de Silva VA, Suraweera C, Ratnatunga SS, Dayabandara M, Wanniarachchi N, Hanwella R (Oktober 2016). "Metformin in prevention and treatment of antipsychotic-induced weight gain: a systematic review and meta-analysis". BMC Psychiatry. 16 (1): 341. doi:10.1186/s12888-016-1049-5. PMC 5048618. PMID 27716110.
  10. ↑ "Type 2 diabetes and metformin. First choice for monotherapy: weak evidence of efficacy but well-known and acceptable adverse effects". Prescrire International. 23 (154): 269–272. November 2014. PMID 25954799.
  11. ↑ Blumenberg A, Benabbas R, Sinert R, Jeng A, Wiener SW (April 2020). "Do Patients Die with or from Metformin-Associated Lactic Acidosis (MALA)? Systematic Review and Meta-analysis of pH and Lactate as Predictors of Mortality in MALA". Journal of Medical Toxicology. 16 (2): 222–229. doi:10.1007/s13181-019-00755-6. PMC 7099117. PMID 31907741.
  12. ↑ Lipska KJ, Bailey CJ, Inzucchi SE (Junie 2011). "Use of metformin in the setting of mild-to-moderate renal insufficiency". Diabetes Care. 34 (6): 1431–7. doi:10.2337/dc10-2361. PMC 3114336. PMID 21617112.
  13. ↑ Coll AP, Chen M, Taskar P, Rimmington D, Patel S, Tadross JA, et al. (Februarie 2020). "GDF15 mediates the effects of metformin on body weight and energy balance". Nature. 578 (7795): 444–448. doi:10.1038/s41586-019-1911-y. PMC 7234839. PMID 31875646.
  14. ↑ Day EA, Ford RJ, Smith BK, Mohammadi-Shemirani P, Morrow MR, Gutgesell RM, et al. (Desember 2019). "Metformin-induced increases in GDF15 are important for suppressing appetite and promoting weight loss". Nature Metabolism. 1 (12): 1202–1208. doi:10.1038/s42255-019-0146-4. PMID 32694673. S2CID 213199603.
  15. ↑ Pappachan JM, Viswanath AK (Januarie 2017). "Medical Management of Diabesity: Do We Have Realistic Targets?". Current Diabetes Reports. 17 (1): 4. doi:10.1007/s11892-017-0828-9. PMID 28101792. S2CID 10289148.
  16. ↑ LaMoia TE, Butrico GM, Kalpage HA, Goedeke L, Hubbard BT, Vatner DF, et al. (10 Maart 2022). "Metformin, phenformin, and galegine inhibit complex IV activity and reduce glycerol-derived gluconeogenesis". Proceedings of the National Academy of Sciences of the United States of America. 119 (10): e2122287119.
  17. ↑ Lord JM, Flight IH, Norman RJ (Oktober 2003). "Metformin in polycystic ovary syndrome: systematic review and meta-analysis". BMJ. 327 (7421): 951–3. doi:10.1136/bmj.327.7421.951. PMC 259161. PMID 14576245.
  18. ↑ Bennett WL, Maruthur NM, Singh S, Segal JB, Wilson LM, Chatterjee R, et al. (Mei 2011). "Comparative effectiveness and safety of medications for type 2 diabetes: an update including new drugs and 2-drug combinations". Annals of Internal Medicine. 154 (9): 602–13. doi:10.7326/0003-4819-154-9-201105030-00336. PMC 3733115. PMID 21403054.
  19. ↑ Inzucchi SE, Bergenstal RM, Buse JB, Diamant M, Ferrannini E, Nauck M, et al. (Junie 2012). "Management of hyperglycemia in type 2 diabetes: a patient-centered approach: position statement of the American Diabetes Association (ADA) and the European Association for the Study of Diabetes (EASD)". Diabetes Care. 35 (6): 1364–79. doi:10.2337/dc12-0413. PMC 3357214. PMID 22517736.
  20. ↑ Qaseem A, Humphrey LL, Sweet DE, Starkey M, Shekelle P (Februarie 2012). "Oral pharmacologic treatment of type 2 diabetes mellitus: a clinical practice guideline from the American College of Physicians". Annals of Internal Medicine. 156 (3): 218–31. doi:10.7326/0003-4819-156-3-201202070-00011. PMID 22312141.
  21. ↑ Jia Y, Lao Y, Zhu H, Li N, Leung SW (Januarie 2019). "Is metformin still the most efficacious first-line oral hypoglycaemic drug in treating type 2 diabetes? A network meta-analysis of randomized controlled trials". Obesity Reviews. 20 (1): 1–12. doi:10.1111/obr.12753. PMID 30230172.
  22. ↑ Coll AP, Chen M, Taskar P, Rimmington D, Patel S, Tadross JA, et al. (Februarie 2020). "GDF15 mediates the effects of metformin on body weight and energy balance". Nature. 578 (7795): 444–448. doi:10.1038/s41586-019-1911-y. PMC 7234839. PMID 31875646.
  23. ↑ Johansen K (Januarie 1999). "Efficacy of metformin in the treatment of NIDDM. Meta-analysis". Diabetes Care. 22 (1): 33–7. doi:10.2337/diacare.22.1.33. PMID 10333900.
  24. ↑ Johansen K (Januarie 1999). "Efficacy of metformin in the treatment of NIDDM. Meta-analysis". Diabetes Care. 22 (1): 33–7. doi:10.2337/diacare.22.1.33. PMID 10333900.
  25. ↑ Golay A (Januarie 2008). "Metformin and body weight". International Journal of Obesity. 32 (1): 61–72. doi:10.1038/sj.ijo.0803695. PMID 17653063.
  26. ↑ Mead E, Atkinson G, Richter B, Metzendorf MI, Baur L, Finer N, et al. (November 2016). "Drug interventions for the treatment of obesity in children and adolescents". The Cochrane Database of Systematic Reviews. 11 (11): CD012436. doi:10.1002/14651858.CD012436. hdl:10149/620651. PMC 6472619. PMID 27899001.
  27. ↑ Maharani U (2009). "Chapter 27: Diabetes Mellitus & Hypoglycemia". In Papadakis MA, McPhee SJ (reds.). Current Medical Diagnosis and Treatment 2010 (49th uitg.). McGraw-Hill Medical. pp. 1092–93. ISBN 978-0-07-162444-2.
  28. ↑ Bolen S, Feldman L, Vassy J, Wilson L, Yeh HC, Marinopoulos S, et al. (September 2007). "Systematic review: comparative effectiveness and safety of oral medications for type 2 diabetes mellitus". Annals of Internal Medicine. 147 (6): 386–99. doi:10.7326/0003-4819-147-6-200709180-00178. PMID 17638715.
  29. ↑ DiPiro JT, Talbert RL, Yee GC, Matzke GR, Wells BG, Posey LM (2005). Pharmacotherapy: a pathophysiologic approach. New York: McGraw-Hill. ISBN 978-0-07-141613-9.
  30. ↑ "Glucophage package insert". Princeton, NJ: Bristol-Myers Squibb Company. 2009. Geargiveer vanaf die oorspronklike op 29 Augustus 2021 – via DailyMed.
  31. ↑ Maharani U (2009). "Chapter 27: Diabetes Mellitus & Hypoglycemia". In Papadakis MA, McPhee SJ (reds.). Current Medical Diagnosis and Treatment 2010 (49th uitg.). McGraw-Hill Medical. pp. 1092–93. ISBN 978-0-07-162444-2.
  32. ↑ Bolen S, Feldman L, Vassy J, Wilson L, Yeh HC, Marinopoulos S, et al. (September 2007). "Systematic review: comparative effectiveness and safety of oral medications for type 2 diabetes mellitus". Annals of Internal Medicine. 147 (6): 386–99. doi:10.7326/0003-4819-147-6-200709180-00178. PMID 17638715.
  33. ↑ Yerevanian A, Soukas AA (Junie 2019). "Metformin: Mechanisms in Human Obesity and Weight Loss". Current Obesity Reports. 8 (2): 156–164. doi:10.1007/s13679-019-00335-3. PMC 6520185. PMID 30874963.
  34. ↑ Choi YJ (2015). "Efficacy of adjunctive treatments added to olanzapine or clozapine for weight control in patients with schizophrenia: a systematic review and meta-analysis". TheScientificWorldJournal. 2015: 970730. doi:10.1155/2015/970730. PMC 4310265. PMID 25664341.
  35. ↑ Praharaj SK, Jana AK, Goyal N, Sinha VK (Maart 2011). "Metformin for olanzapine-induced weight gain: a systematic review and meta-analysis". British Journal of Clinical Pharmacology. 71 (3): 377–82. doi:10.1111/j.1365-2125.2010.03783.x. PMC 3045546. PMID 21284696.
  36. ↑ Siskind DJ, Leung J, Russell AW, Wysoczanski D, Kisely S (2016). "Metformin for Clozapine Associated Obesity: A Systematic Review and Meta-Analysis". PLOS ONE. 11 (6): e0156208. Bibcode:2016PLoSO..1156208S. doi:10.1371/journal.pone.0156208. PMC 4909277. PMID 27304831.
  37. ↑ Vella S, Buetow L, Royle P, Livingstone S, Colhoun HM, Petrie JR (Mei 2010). "The use of metformin in type 1 diabetes: a systematic review of efficacy". Diabetologia. 53 (5): 809–20. doi:10.1007/s00125-009-1636-9. PMID 20057994.
  38. ↑ Novelle MG, Ali A, Diéguez C, Bernier M, de Cabo R (Maart 2016). "Metformin: A Hopeful Promise in Aging Research". Cold Spring Harbor Perspectives in Medicine. 6 (3): a025932. doi:10.1101/cshperspect.a025932. PMC 4772077. PMID 26931809.
  39. ↑ Kulkarni AS, Gubbi S, Barzilai N (Julie 2020). "Benefits of Metformin in Attenuating the Hallmarks of Aging". Cell Metabolism. 32 (1): 15–30. doi:10.1016/j.cmet.2020.04.001. PMC 7347426. PMID 32333835.
  40. ↑ Campbell JM, Stephenson MD, de Courten B, Chapman I, Bellman SM, Aromataris E (2018). "Metformin Use Associated with Reduced Risk of Dementia in Patients with Diabetes: A Systematic Review and Meta-Analysis". Journal of Alzheimer's Disease. 65 (4): 1225–1236. doi:10.3233/jad-180263. PMC 6218120. PMID 30149446.
  41. ↑ Campbell JM, Stephenson MD, de Courten B, Chapman I, Bellman SM, Aromataris E (Augustus 2017). "Metformin and Alzheimer's disease, dementia and cognitive impairment: a systematic review protocol". JBI Database of Systematic Reviews and Implementation Reports. 15 (8): 2055–2059. doi:10.11124/JBISRIR-2017-003380. PMID 28800055.
  42. ↑ 42,0 42,1 42,2 "Metformin: medicine to treat type 2 diabetes". National Health Service. 25 Februarie 2019. Geargiveer vanaf die oorspronklike op 11 Maart 2021. Besoek op 15 Oktober 2020.
  43. ↑ "METFORMIN HYDROCHLORIDE". NICE. Geargiveer vanaf die oorspronklike op 10 Junie 2021. Besoek op 15 Oktober 2020.
  44. ↑ Bolen S, Feldman L, Vassy J, Wilson L, Yeh HC, Marinopoulos S, et al. (September 2007). "Systematic review: comparative effectiveness and safety of oral medications for type 2 diabetes mellitus". Annals of Internal Medicine. 147 (6): 386–99. doi:10.7326/0003-4819-147-6-200709180-00178. PMID 17638715.
  45. ↑ Khurana R, Malik IS (Januarie 2010). "Metformin: safety in cardiac patients". Heart. 96 (2): 99–102. doi:10.1136/hrt.2009.173773. PMID 19564648. S2CID 9746741.
  46. ↑ Heaf J (Junie 2014). "Metformin in chronic kidney disease: time for a rethink". Peritoneal Dialysis International. 34 (4): 353–7. doi:10.3747/pdi.2013.00344. PMC 4079480. PMID 24711640.
  47. ↑ Tilley J, Grimsby J, Erickson S, Berthel S (2010). "Diabetes Drugs: Present and Emerging". Burger's Medicinal Chemistry and Drug Discovery. pp. 1–38. doi:10.1002/0471266949.bmc198. ISBN 978-0471266945.
  48. ↑ Werner E, Bell J (1922). "The preparation of methylguanidine, and of ββ-dimethylguanidine by the interaction of dicyandiamide, and methylammonium and dimethylammonium chlorides respectively". J. Chem. Soc., Trans. 121: 1790–95. doi:10.1039/CT9222101790. Geargiveer vanaf die oorspronklike op 8 Junie 2021. Besoek op 4 September 2020.
  49. ↑ Shapiro SL, Parrino VA, Freedman L (1959). "Hypoglycemic Agents. I Chemical Properties of β-Phenethylbiguanide. A New Hypoglycemic Agent". J Am Chem Soc. 81 (9): 2220–25. doi:10.1021/ja01518a052.
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