ダパグリフロジン
ダパグリフロジン (Dapagliflozin) is a pharmaceutical product classified in SGLT-2 inhibitor among type 2 diabetes therapeutic drugs. The product name is フォシーガ. (Ono Pharmaceutical sale, Bristol Myers production, アストラゼネカコ promotion) produced it in Japan on March 24, 2014 and was approved [1].
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| Material name by the IUPAC glossology | |
|---|---|
| (2S,3R,4R,5S,6R) -2-[4-chloro-3-(4-ethoxybenzyl) phenyl] -6-(hydroxymethyl)tetrahydro-2H-pyran-3,4,5-triol | |
| Clinical data | |
| Sale name | フォシーガ |
| Legal regulation |
|
| Dosage method | Oral |
| Pharmacokinetics data | |
| Bioavailability | 78% |
| Plasma protein combination | 91-92% |
| Metabolism | The liver and kidney metabolism |
| Half-life | 8.1-12.1 hours |
| Excretion | Urine (75%), feces (21%) |
| Identification | |
| CAS number (MeSH) | 461,432-26-8  |
| ATC cord | A10BX09 (WHO) |
| PubChem | CID: 9887712 |
| ChemSpider | 8063384  |
| UNII | 1ULL0QJ8UC |
| KEGG | D08897 |
| ChEMBL | CHEMBL429910 |
| Another name | BMS-512148 |
| Chemical data | |
| Chemical formula | C21H25ClO6 |
| Molecular weight | 408.873 g/mol |
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Table of contents
Adaptation
- Type 2 diabetes
Action mechanism
SGLT (British: Sodium-Glucose Co-Transporter： Sodium-dependent glucose transportation carrier) controls the cotransport in the cell of sodium and glucose with the membrane protein which there is in the cell surface. There is a lot SGLT-2 to kidney proximal tubule in one of the subtypes of SGLT and takes an important role in reuptake from all over the urine of glucose (there is a lot SGLT-1 on a small intestine mucous membrane and takes absorption of glucose from a diet). ダパグリフロジン controls reuptake from all over the original urine of sodium and glucose by inhibiting this SGLT-2 selectively and reduces blood sugar level by promoting urinary excretion of glucose. Because they show blood sugar descent action in insulin independency and do not present with hyperinsulinemia, it is hoped that a side effect of direct action of insulin (hypoglycemia, weight gain) is hard to develop.
Clinical trial
A blood pressure drop, a serum uric acid level drop, improvement, the weight loss of the cholesterol profile were significantly accepted other than hypoglycemia at the clinical trial stage, too.
Side effect
The side effect was seen in 17.0% at the time of the clinical trial, and the breakdown was micturition (3.6%), 口渇 (1.8%), sexual organs infection (1.7%), urinary tract infection (1.7%).
The serious side effect listed in an attached document is hypoglycemia, pyelonephritis, sepsis, dehydration, ketoacidosis [2]. Fatty acid metabolism aggravates even an example having good blood sugar control, and ketoacidosis is possible.
- Dehydration ... For sodium diuresis, osmolar diuresis, volume of urine rises approximately 400mL/day.
- Urinary tract infection ... Bacterial infections increase by urine sugar.
Three death example was reported by the interim report of the investigation just after marketing [3]. Or the details such as the causes of death are conducting all an unidentified investigation from a remedy start - approximately two months later for 46 days.
Source
- Public information document of ^ AstraZeneca
- ^ "フォシーガ lock 5mg/ フォシーガ lock 10 mg attachment document" (September, 2015). June 27, 2016 reading.
- The ^ "marketing an investigation 5 human deaths example of the SGLT2 inhibitor" (October 17, 2014). October 26, 2014 reading.
Allied item
Outside link
This article is taken from the Japanese Wikipedia ダパグリフロジン
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