Metformin: Perbedaan antara revisi
Konten dihapus Konten ditambahkan
kTidak ada ringkasan suntingan |
k Removing from Category:Antidiabetes using Cat-a-lot |
||
| (22 revisi perantara oleh 8 pengguna tidak ditampilkan) | |||
Baris 1:
{{Infobox drug
| image = Metformin.svg
| width =
| alt =
| image2 = Metformin-from-xtal-3D-balls.png
| width2 =
| alt2 =
| caption =
<!-- Clinical data -->
| pronounce = {{IPAc-en|m|ɛ|t|ˈ|f|ɔːr|m|ᵻ|n}}, {{respell|met|FOR|min}}
| tradename = Diabit, Forbetes, Glikos, Glucophage, Gludepatic, dll
| Drugs.com = {{drugs.com|monograph|metformin-hydrochloride}}
| MedlinePlus = a696005
| DailyMedID = Metformin
| pregnancy_AU = C
| pregnancy_AU_comment = <ref name="Drugs.com pregnancy">{{cite web | title=Metformin Use During Pregnancy | website=Drugs.com | date=10 September 2019 | url=https://www.drugs.com/pregnancy/metformin.html | access-date=4 February 2020 | archive-date=16 April 2020 | archive-url=https://web.archive.org/web/20200416182342/https://www.drugs.com/pregnancy/metformin.html | url-status=live }}</ref>
| pregnancy_category =
| routes_of_administration = Oral
| class = [[Antidiabetic agent]]
| ATC_prefix = A10
| ATC_suffix = BA02
| ATC_supplemental = Combinations: {{UBL|
| Metformin and sulfonylureas {{ATC|A10|BD02}}
| Metformin and rosiglitazone {{ATC|A10|BD03}}
| Metformin and pioglitazone {{ATC|A10|BD05}}
| Metformin and sitagliptin {{ATC|A10|BD07}}
| Metformin and vildagliptin {{ATC|A10|BD08}}
| Metformin and saxagliptin {{ATC|A10|BD10}}
| Metformin and linagliptin {{ATC|A10|BD11}}
| Metformin and alogliptin {{ATC|A10|BD13}}
| Metformin and repaglinide {{ATC|A10|BD14}}
| Metformin and dapagliflozin {{ATC|A10|BD15}}
| Metformin and canagliflozin {{ATC|A10|BD16}}
| Metformin and acarbose {{ATC|A10|BD17}}
| Metformin and gemigliptin {{ATC|A10|BD18}}
| Metformin and empagliflozin {{ATC|A10|BD20}}
| Metformin and evogliptin {{ATC|A10|BD22}}
| Metformin and ertugliflozin {{ATC|A10|BD23}}
| Metformin, saxagliptin, and dapagliflozin{{ATC|A10|BD25}}
| Metformin and lobeglitazone {{ATC|A10|BD26}}
| Metformin, linagliptin and empagliflozin {{ATC|A10|BD27}}
| Metformin and teneligliptin {{ATC|A10|BD28}}
}}
<!-- Legal status -->
| legal_AU = S4
| legal_AU_comment = <ref>{{cite web | title=Metformin SANDOZ metformin hydrochloride 850mg tablet bottle (148270) | website=Therapeutic Goods Administration (TGA) | date=27 May 2022 | url=https://www.tga.gov.au/resources/artg/148270 | access-date=29 April 2023}}</ref>
| legal_BR = <!-- OTC, A1, A2, A3, B1, B2, C1, C2, C3, C4, C5, D1, D2, E, F -->
| legal_BR_comment =
| legal_CA = Rx-only
| legal_CA_comment = <ref name="pmid6847752" /><ref>{{Cite web |url=https://health-products.canada.ca/dpd-bdpp/info?lang=eng&code=17104 |title=Metformin Hydrochloride | work = Health Canada |access-date=6 March 2023 |archive-date=6 March 2023 |archive-url=https://web.archive.org/web/20230306055806/https://health-products.canada.ca/dpd-bdpp/info?lang=eng&code=17104 |url-status=live }}</ref>
| legal_DE = <!-- Anlage I, II, III or Unscheduled -->
| legal_DE_comment =
| legal_NZ = <!-- Class A, B, C -->
| legal_NZ_comment =
| legal_UK = POM
| legal_UK_comment = <ref>{{cite web | title=Glucophage 500 mg film coated tablets - Summary of Product Characteristics (SmPC) | website=(emc) | date=25 October 2022 | url=https://www.medicines.org.uk/emc/product/987/smpc | access-date=5 March 2023 | archive-date=20 June 2022 | archive-url=https://web.archive.org/web/20220620110218/https://www.medicines.org.uk/emc/product/987/smpc | url-status=live }}</ref>
| legal_US = Rx-only
| legal_US_comment = <ref name="Glucophage PI" />
| legal_EU = Rx-only
| legal_EU_comment = <ref>{{cite web | title=Metformin and metformin-containing medicines | website=[[European Medicines Agency]] (EMA) | date=13 October 2016 | url=https://www.ema.europa.eu/en/medicines/human/referrals/metformin-metformin-containing-medicines | access-date=10 June 2024 | archive-date=18 November 2023 | archive-url=https://web.archive.org/web/20231118173723/https://www.ema.europa.eu/en/medicines/human/referrals/metformin-metformin-containing-medicines | url-status=live }}</ref>
| legal_UN = <!-- N I, II, III, IV / P I, II, III, IV -->
| legal_UN_comment =
| legal_status = <!-- For countries not listed above -->
<!-- Pharmacokinetic data -->
| bioavailability = 50–60%<ref name = D95>{{cite journal | vauthors = Dunn CJ, Peters DH | title = Metformin. A review of its pharmacological properties and therapeutic use in non-insulin-dependent diabetes mellitus | journal = Drugs | volume = 49 | issue = 5 | pages = 721–49 | date = May 1995 | pmid = 7601013 | doi = 10.2165/00003495-199549050-00007 }}</ref><ref name=D03>{{cite journal | vauthors = Hundal RS, Inzucchi SE | title = Metformin: new understandings, new uses | journal = Drugs | volume = 63 | issue = 18 | pages = 1879–94 | year = 2003 | pmid = 12930161 | doi = 10.2165/00003495-200363180-00001 }}</ref>
| protein_bound = Minimal<ref name = D95 />
| metabolism = Bukan dengan hati<ref name = D95 />
| metabolites =
| onset =
| elimination_half-life = 4–8,7 jam<ref name = D95 />
| duration_of_action =
| excretion = Urin (90%)<ref name = D95 />
<!-- Identifiers -->
| index2_label = as HCl
| CAS_number = 657-24-9
| CAS_number2 = 1115-70-4
| PubChem = 4091
| PubChem2 = 14219
| IUPHAR_ligand = 4779
| DrugBank = DB00331
| DrugBank2 = DBSALT000114
| ChemSpiderID = 3949
| ChemSpiderID2 = 13583
| UNII = 9100L32L2N
| UNII2 = 786Z46389E
| KEGG = D04966
| KEGG2 = D00944
| ChEBI = 6801
| ChEBI2 = 6802
| ChEMBL = 1431
| ChEMBL2 = 1703
| NIAID_ChemDB =
| PDB_ligand =
| synonyms = ''N'',''N''-dimetilbiguanida<ref>{{cite journal | vauthors = Sirtori CR, Franceschini G, Galli-Kienle M, Cighetti G, Galli G, Bondioli A, Conti F | title = Disposition of metformin (N,N-dimethylbiguanide) in man | journal = Clinical Pharmacology and Therapeutics | volume = 24 | issue = 6 | pages = 683–93 | date = December 1978 | pmid = 710026 | doi = 10.1002/cpt1978246683 | s2cid = 24531910 }}</ref>
<!-- Chemical and physical data -->
| IUPAC_name = ''N'',''N''-Dimetilimidodikarbonimidat diamida
| C = 4 | H = 11 | N = 5
| SMILES = CN(C)C(=N)N=C(N)N
| SMILES2 = Cl.CN(C)C(=N)NC(N)=N
| StdInChI = 1S/C4H11N5/c1-9(2)4(7)8-3(5)6/h1-2H3,(H5,5,6,7,8)
| StdInChI2 = 1S/C4H11N5.ClH/c1-9(2)4(7)8-3(5)6;/h1-2H3,(H5,5,6,7,8);1H
| StdInChI_comment =
| StdInChIKey = XZWYZXLIPXDOLR-UHFFFAOYSA-N
| StdInChIKey2 = OETHQSJEHLVLGH-UHFFFAOYSA-N
| density = 1.3±0.1<ref name="chemsrc">{{Cite web|url=https://www.chemsrc.com/en/cas/657-24-9_889579.html|title=Metformin|website=www.chemsrc.com|access-date=10 May 2018|archive-date=12 June 2017|archive-url=https://web.archive.org/web/20170612212251/http://www.chemsrc.com/en/cas/657-24-9_889579.html|url-status=live}}</ref>
| density_notes =
| melting_point =
| melting_high =
| melting_notes =
| boiling_point =
| boiling_notes =
| solubility =
| sol_units =
| specific_rotation =
}}
[[Berkas:Metformin 500mg Tablets.jpg|al=Metformin Obat Diabetes|jmpl|Metformin Obat Diabetes]]
'''Metformin''' adalah [[anti-diabetes oral]] yang termasuk pada kelas [[biguanid]].<ref name="web1">{{cite web|url=http://www.news-medical.net/health/Metformin-What-is-Metformin-(Indonesian).aspx|title=Metformin|accessdate=May 15 2014}}</ref> Metformin merupakan [[obat]] pilihan pertama untuk penderita diabetes tipe 2, khususnya untuk orang-orang dengan kelebihan berat badan dan gemuk serta orang-orang dengan fungsi [[ginjal]] yang normal.<ref name="web1"/> Metformin digunakan untuk penderita diabetes yang baru terdiagnosis stelah dewasa.<ref name="web2">{{cite web|url=http://www.dechacare.com/METFORMIN-P590.html|title=Metformin|accessdate=may 15 2014|archive-date=2014-05-14|archive-url=https://web.archive.org/web/20140514081323/http://www.dechacare.com/METFORMIN-P590.html|dead-url=yes}}</ref> Obat ini dapat digunakan sebagai kombinasi terapi pada penderita yang tidak responsif atau tidak mempan setelah penggunaan terapi tunggal [[sulfonilurea]].<ref name="web2"/> Selain itu, kadang digunakan pula untuk mengurangi dosis insulin apabila dibutuhkan.<ref name="web2"/>
== Sejarah ==
Pada tahun 1929, [[Slotta]] dan [[Tschesche]] meneliti aksi penurunan gula darah pada kelinci, dan tidak ada yang lebih baik dari penurunan dari analog biguanid seperti [[sintalin]].<ref name="web3">{{en}} {{cite web|url=http://www.news-medical.net/health/Metformin-History.aspx|title=Metformin History|accessdate=May 15 2014}}</ref> Namun, metformin ini baru terkenal pada akhir tahun 1940-an.<ref name="web3"/> Kemudian pada 1950, ditemukan bahwa metformin tidak meurunkan tekanan darah dan denyut jantung pada hewan, tidak seperti obat-oabt lainnya.<ref name="web3"/> Pada tahun yang sama, seorang dokter terkemuka [[Filipina]], [[Eusebio Y. Garcia]], menggunakan metformin untuk melawan [[influenza]].<ref name="web3"/> Ia juga meyakini bahwa metformin memiliki aktivitas [[bakteriostatik]], [[antiviral]], [[antimalarial]], [[antipiretik]], dan [[analgesik]].<ref name="web3"/>
== Mekanisme aksi ==
Efek utama metformin yaitu untuk mengurangi produksi glukosa hepatik.<ref name="web4">{{en}} {{cite web|url=http://www.uptodate.com/contents/metformin-in-the-treatment-of-adults-with-type-2-diabetes-mellitus|title=Metformin in The Treatment of Adults with Type 2 Diabetes Mellitus|accessdate=May 15 2014}}</ref> Selain itu, metformin meningkatkan penggunaan glukosa [[insulin]] yang diperantarai oleh [[jaringan perifer]] (seperti [[otot]] dan [[hati]]), terutama setelah makan, dan memiliki efek [[antilipolitik]] yang menurunkan konsentrasi serum [[asam lemak]] bebas, sehingga mengurangi ketersediaan substrat untuk [[glukoneogenesis]].<ref name="web4"/>
Metformin juga meningkatkan penggunaan glukosa usus melalui metabolisme tanpa penggunaan oksigen.<ref name="web4"/> [[Laktat]] yang dihasilkan oleh proses ini sebagian besar dimetabolisme di hati sebagai substrat untuk glukoneogenesis.<ref name="web4"/> Efek yang terakhir bisa melindungi terhadap [[hipoglikemia]].<ref name="web4"/>
Mekanisme molekuler dari metformin tidak sepenuhnya diketahui.<ref name="web4"/> Aktivasi enzim [[AMP]] yang diaktivasi oleh [[protein kinase]] (AMPK) tampaknya menjadi mekanisme yang menurunkan serum lipid dan konsentrasi glukosa darah.<ref name="web4"/> Hal tersebut kemudian menekan [[lipogenesis]] dan menurunkan lemak seluler sintesis asam di hati dan otot, yang pada gilirannya meningkatkan sensitivitas insulin dan mengurangi kadar glukosa darah.<ref name="web4"/>
Baris 35 ⟶ 157:
== Referensi==
{{reflist}}{{Farmasi-stub}}
[[Kategori:Obat Esensial Nasional Indonesia]]
[[Kategori:Biguanid]]
[[Kategori:guanidina]]
[[Kategori:Antipenuaan]]
[[Kategori:Obat dengan cara kerja yang belum diketahui]]
[[Kategori:Obat piatu]]
[[Kategori:Obat yang dikembangkan oleh Boehringer Ingelheim]]
[[Kategori:Obat yang dikembangkan oleh Merck KGaA]]
[[Kategori:Obat Esensial Organisasi Kesehatan Dunia]]
| |||