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Akarboza

Akarboza
Haworthova projekcija akarboze
Model kroglic in paličic akarboze molecule
Klinični podatki
Blagovne znamkeGlucobay, Precose, Prandase
Sinonimi(2R,3R,4R,5S,6R)-5-{[(2R,3R,4R,5S,6R)-5- {[(2R,3R,4S,5S,6R)-3,4-dihidroksi-6-metil- 5-{[(1S,4R,5S,6S)-4,5,6-trihidroksi-3- (hidroksimetil)cikloheks-2-en-1-il]amino} tetrahidro-2H-piran-2-il]oksi}-3,4-dihidroksi- 6-(hidroksimetil)tetrahidro-2H-piran-2-il]oksi}- 6-(hidroksimetil)tetrahidro-2H-piran-2,3,4-triol
AHFS/Drugs.commonograph
MedlinePlusa696015
Licenčni podatki
Nosečnostna
kategorija
  • AU: B3
  • ZDA: B (raziskave na živalih niso dokazale škodljivosti)
Način uporabeskozi usta (v obliki tablet)
Oznaka ATC
Pravni status
Pravni status
  • UK: Rp (Le na recept)
  • ZDA: le na recept
Farmakokinetični podatki
Biološka razpoložljivostskrajno nizka
Presnovav prebavilih (z glukozidazo, maltogenično α-amilazo in ciklomaltodekstrinazo iz črevesnega mikrobioma)
Razpolovni čas2 h
Izločanjeskozi ledvice (manj kot 2 %)
Identifikatorji
  • O-4,6-dideoksi-4-[[(1S,4R,5S,6S)-4,5,6-trihidroksi-3-(hidroksimetil)-2-cikloheksen-1-il]amino]-α-D-glukopiranozil-(1→4)-O-α-D-glukopiranozil-(1→4)-D-glukopiranoza
Številka CAS
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEMBL
CompTox Dashboard (EPA)
ECHA InfoCard100.054.555 Uredite to na Wikipodatkih
Kemični in fizikalni podatki
FormulaC25H43NO18
Mol. masa645,61 g·mol−1
3D model (JSmol)
  • O([C@H]1[C@H](O)[C@@H](O)[C@H](O)O[C@@H]1CO)[C@H]4O[C@@H]([C@@H](O[C@H]3O[C@H](C)[C@@H](N[C@H]2/C=C(/CO)[C@@H](O)[C@H](O)[C@H]2O)[C@H](O)[C@H]3O)[C@H](O)[C@H]4O)CO
  • InChI=1S/C25H43NO18/c1-6-11(26-8-2-7(3-27)12(30)15(33)13(8)31)14(32)19(37)24(40-6)43-22-10(5-29)42-25(20(38)17(22)35)44-21-9(4-28)41-23(39)18(36)16(21)34/h2,6,8-39H,3-5H2,1H3/t6-,8+,9-,10-,11-,12-,13+,14+,15+,16-,17-,18-,19-,20-,21-,22-,23-,24-,25-/m1/s1
  • Key:XUFXOAAUWZOOIT-SXARVLRPSA-N

Akarbóza (INN)[1][2] je učinkovina z antidiabetičnim delovanjem,[3] ki se uporablja za zdravljenje sladkorne bolezni tipa 2, v nekaterih državah pa tudi pri moteni toleranci za glukozo (prediabetesu). Farmacevtsko podjetje Bayer ga v Evropi in na Kitajskem trži pod imenom Glucobay, v Severni Ameriki pod imenom Precose in v Kanadi kot Prandase. Njegovo klinično uporabo omejujeta delna učinkovitost in pojavljanje neželenih učinkov, zlasti napenjanja in driske.[4]

Akarboza zavira encim glukozidazo alfa v črevesju in s tem preprečuje razgradnjo večjih ogljikovih hidratov (disaharidov, oligosaharidov in polisaharidov) na monosaharide, vključno z glukozo, ki se lahko nato vsrka skozi prebavila v krvni obtok.[5][6]

Sklici

[uredi | uredi kodo]
  1. Elks J, Ganellin CR (1990). Elks J, Ganellin CR (ur.). The Dictionary of Drugs: Chemical Data: Chemical Data, Structures and Bibliographies. Springer. str. 1–. doi:10.1007/978-1-4757-2085-3. ISBN 978-1-4757-2085-3.
  2. »International Nonproprietary Names for Pharmaceutical Substances. Recommended International Nonproprietary Names (Rec. INN): List 19« (PDF). Svetovna zdtavstvena organizacija. 1979. Pridobljeno 9. novembra 2016.
  3. https://www.termania.net/slovarji/slovenski-medicinski-slovar/5504748/akarboza?query=Akarboza&SearchIn=All, Slovenski medicinski e-slovar, vpogled: 7. 4. 2023.
  4. Kresge N (21. november 2011). »China's Thirst for New Diabetes Drugs Threatens Bayer's Lead«. Bloomberg Business Week. Arhivirano iz prvotnega spletišča dne 21. novembra 2011. Pridobljeno 1. aprila 2016.
  5. Jang MU, Kang HJ, Jeong CK, Kang Y, Park JE, Kim TJ (Februar 2018). »Functional expression and enzymatic characterization of Lactobacillus plantarum cyclomaltodextrinase catalyzing novel acarbose hydrolysis«. Journal of Microbiology. 56 (2): 113–118. doi:10.1007/s12275-018-7551-3. PMID 29392561. S2CID 2660911.
  6. http://www.cbz.si/cbz/bazazdr2.nsf/o/9A3C085CFC2B1D21C12579C2003F5527/$File/s-020415.pdf, Povzetek glavnih značilnosti zdravila Glucobay, Centralna baza zdravil, vpogled: 7. 4. 2023.
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Akarboza
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