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måndag 5 december 2016

Meglitinidit


Meglitinidi

Rakenne ei ole sulfonyyliurean:
Nateglinidi ( Starlix) on rakenteeltaan
(-/-N( 8trans-4-isopropyl cyclohexane) carbonyl)-D-Phenylalanine
Tästä oli Suomessakin mainosta
En kuitenkaan löydä FASS- tekstistä varsinaisesti.
  • Meglitinidit muiden antidiabetikaryhmien kanssa tutkittavana: https://www.ncbi.nlm.nih.gov/pubmed/26063450
  • Tutkittaessa uusia glifloziineja jotka kuuluvat SGLT2-estäjiin) selviteltiin (helmikuu 2016) interaktioita muihin antidiabetikavalmisteisiin ja joukossa mainitaan myös meglitinidivalmiste. nateglinidi. https://www.ncbi.nlm.nih.gov/pubmed/26158794Sitaatti: AbstractOBJECTIVE: Tofogliflozin is an oral hypoglycemic agent with a novel mechanism of action that reduces blood glucose levels by promoting glucose excretion in urine, achieved by selectively inhibiting sodium-glucose co-transporter 2 (SGLT2). We evaluated the effects of several selected anti-type 2 diabetes mellitus (T2DM) drugs- glimepiride, metformin, sitagliptin, pioglitazone, miglitol, nateglinide, and voglibose-on the pharmacokinetics and pharmacodynamics of tofogliflozin, and the effects of tofogliflozin on the pharmacokinetics of these anti-T2DM drugs in healthy male volunteers.CONCLUSIONS: Neither the pharmacokinetics nor the pharmacodynamics of tofogliflozin was affected by any of the anti-T2DM drugs evaluated in this study, nor was the pharmacokinetics of any of the anti-T2DM drugs affected by tofogliflozin in healthy male volunteers.
  • Nateglinidi-metformiini-kombinaation mahdollasta terapeuttista vaikutusta pohditaan (kesä 2016): https://www.ncbi.nlm.nih.gov/pubmed/26314243
  • Teknetiumisotooppi-Nateglinidillä* on tutkittu betasolufunktiota.
    Am J Transl Res. 2016 Apr 15;8(4):1857-63. eCollection 2016. Distribution of pancreatic B cell imaging agent (99m)Tc-DTPA-NGN2 in the body and animal experimental research on pancreatic B cell functional imaging.Liu ZH1, Xie Y1, Tang J2, Liu CF3. PURPOSE: To explore the feasibility of the application of (99m)Tc-DTPA-Nateglinide as a nuclear medicine imaging agent for evaluating pancreatic B cell function. (1) Distribution of the experiment: Forty-two mice were selected and divided into seven groups. Each mice was injected with 3.7 MBq (100 μCi) of (99m)Tc-DTPA-NGN2 from the vena caudalis and was sacrificed by bloodletting at five minutes, 15 minutes, 30 minutes, one hour, two hours, four hours and six hours, respectively. Then, their tissues and organs such as the heart, liver, spleen, brain, kidneys, bones, small bowels, stomach and pancreas,and blood were collected, weighted, and their radioactivity was tested. Subsequently, the percentage injection dose rate (%ID/g) per gram of tissue was calculated. (2) Imaging experiment: Thirty-five mice were selected and divided into seven groups. Each was injected with 18.5 MBq (100 μCi) of (99m)Tc-DTPA-NGN2 from the vena caudalis and imaging were conducted at the same time as above. (3) Forty-eight Wistar rats were attained and randomly divided into four groups. The first group served as the healthy control group, while the second, third and fourth groups were diabetic model groups induced by intraperitoneally injecting STZ at different doses. Each group was injected with (99m)Tc-DTPA-Nateglinide from the vena caudalis, and radiological evaluations were conducted at 30 minutes, one hour, 1.5 hours and two hours, respectively. The data obtained were estimated using a correlation comparison with the levels of insulin and immunohistochemical count of beta cells.RESULTS: The (99m)Tc-DTPA-Nateglinide demonstrated good imaging in the pancreases of mice and rats, and was positively correlated to the level of insulin and the number of pancreatic beta cells. CONCLUSION: Pancreatic beta cell imaging using (99m)Tc-DTPA-Nateglinide may be a method to evaluate pancreatic beta cell function.





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