| 词条 | Linagliptin |
| 释义 |
| Verifiedfields = changed | Watchedfields = changed | verifiedrevid = 452028402 | IUPAC_name = 8-[(3R)-3-Aminopiperidin-1-yl]-7-(but-2-yn-1-yl)-3-methyl-1-[(4-methylquinazolin-2-yl)methyl]-3,7-dihydro-1H-purine-2,6-dione | image = Linagliptin.svg | width = 250 | pronounce = {{IPAc-en|ˌ|l|ɪ|n|ə|ˈ|g|l|ɪ|p|t|ɪ|n}} {{respell|LIN|ə|GLIP|tin}} | tradename = Tradjenta, Trajenta, others | Drugs.com = {{drugs.com|monograph|linagliptin}} | MedlinePlus = a611036 | licence_EU = yes | licence_US = Linagliptin | pregnancy_AU = | pregnancy_US = B | pregnancy_category = | legal_AU = S4 | legal_CA = | legal_UK = POM | legal_US = Rx-only | legal_status = Rx-only | routes_of_administration = By mouth (tablets) | synonyms = BI-1356 | bioavailability = ~30% (Tmax = 1.5 hours) | protein_bound = 75–99% (concentration-dependent) | metabolism = Minimal (~10% metabolized) | metabolites = Pharmacologically inactive | elimination_half-life = ~24 hours | excretion = Feces (80%), urine (5%)[1] | IUPHAR_ligand = 6318 | CAS_number_Ref = {{cascite|correct|??}} | CAS_number = 668270-12-0 | ATC_prefix = A10 | ATC_suffix = BH05 | ATC_supplemental = | PubChem = 10096344 | DrugBank_Ref = {{drugbankcite|correct|drugbank}} | DrugBank = | ChEMBL_Ref = {{ebicite|changed|EBI}} | ChEMBL = 237500 | ChEBI_Ref = {{ebicite|changed|EBI}} | ChEBI = 68610 | UNII_Ref = {{fdacite|correct|FDA}} | UNII = 3X29ZEJ4R2 | KEGG_Ref = {{keggcite|correct|kegg}} | KEGG = D09566 | ChemSpiderID_Ref = {{chemspidercite|changed|chemspider}} | ChemSpiderID = 8271879 | chemical_formula = | C=25 | H=28 | N=8 | O=2 | molecular_weight = 472.54 g/mol | smiles = CC#CCN1C2=C(N=C1N3CCC[C@H](C3)N)N(C(=O)N(C2=O)CC4=NC5=CC=CC=C5C(=N4)C)C | StdInChI_Ref = {{stdinchicite|changed|chemspider}} | StdInChI = 1S/C25H28N8O2/c1-4-5-13-32-21-22(29-24(32)31-12-8-9-17(26)14-31)30(3)25(35)33(23(21)34)15-20-27-16(2)18-10-6-7-11-19(18)28-20/h6-7,10-11,17H,8-9,12-15,26H2,1-3H3/t17-/m1/s1 | StdInChIKey_Ref = {{stdinchicite|changed|chemspider}} | StdInChIKey = LTXREWYXXSTFRX-QGZVFWFLSA-N }}Linagliptin, sold under the brand name Tradjenta among others, is a medication used to treat diabetes mellitus type 2.[2] It is generally less preferred than metformin and sulfonylureas.[2][4] It is used together with exercise and diet.[2] It is not recommended in type 1 diabetes.[2] It is taken by mouth.[2] Common side effects include inflammation of the nose and throat.[2] Serious side effects may include angioedema, pancreatitis, joint pain.[4][2] Use in pregnancy and breastfeeding is not recommended.[4] Linagliptin is a dipeptidyl peptidase-4 inhibitor.[2] It works by increasing the production of insulin and decreasing the production of glucagon by the pancreas.[2] Linagliptin was approved for medical use in the United States in 2011.[2] A month supply in the United Kingdom costs the NHS about 33.26 £ as of 2019.[3] In the United States the wholesale cost of this amount is about 391 USD.[4] In 2016 it was the 196th most prescribed medication in the United States with more than 3 million prescriptions.[5] Medical usesResults in 2010 from a Phase III clinical trial of linagliptin showed that the drug can effectively reduce blood sugar.[6] Side effectsLinagliptin may cause severe joint pain.[1][7] The U.S. Food and Drug Administration (FDA) is warning that the type 2 diabetes medicines like sitagliptin, saxagliptin, linagliptin, and alogliptin may cause joint pain that can be severe and disabling. FDA has added a new Warning and Precaution about this risk to the labels of all medicines in this drug class, called dipeptidyl peptidase-4 (DPP-4) inhibitors. Trajenta's Prescribing Information[8] states the drug is contraindicated for people with bronchial hyperreactivity. Asthma is a form of bronchial hyperreactivity[9]. Mechanism of actionLinagliptin belongs to a class of drugs called DPP-4 inhibitors. TerminologyLinagliptin is the INN.[10] See also
References1. ^1 {{cite web|title=Tradjenta (linagliptin) Tablets. Full Prescribing Information|url=http://docs.boehringer-ingelheim.com/Prescribing%20Information/PIs/Tradjenta/Tradjenta.pdf?DMW_FORMAT=pdf|publisher=Boehringer Ingelheim Pharmaceuticals, Inc. Ridgefield, CT 06877 USA|accessdate=10 November 2016}} {{Oral hypoglycemics}}2. ^1 2 3 4 5 6 7 8 9 {{cite web |title=Linagliptin Monograph for Professionals |url=https://www.drugs.com/monograph/linagliptin.html |website=Drugs.com |publisher=American Society of Health-System Pharmacists |accessdate=6 April 2019 |language=en}} 3. ^1 2 3 {{cite book|title=British national formulary : BNF 76|date=2018|publisher=Pharmaceutical Press|isbn=9780857113382|pages=680|edition=76}} 4. ^{{cite web |title=NADAC as of 2019-02-27 |url=https://data.medicaid.gov/Drug-Pricing-and-Payment/NADAC-as-of-2019-02-27/s7c9-pfa6 |website=Centers for Medicare and Medicaid Services |accessdate=3 March 2019 |language=en}} 5. ^{{cite web |title=The Top 300 of 2019 |url=https://clincalc.com/DrugStats/Top300Drugs.aspx |website=clincalc.com |accessdate=22 December 2018}} 6. ^{{cite news|url=http://www.genengnews.com/gen-news-highlights/four-phase-iii-trials-confirm-benefits-of-bi-s-oral-once-daily-type-2-diabetes-therapy/81243585/|title=Four Phase III Trials Confirm Benefits of BI’s Oral, Once-Daily Type 2 Diabetes Therapy|publisher=Genetic Engineering & Biotechnology News|date=28 June 2010}} 7. ^{{cite web|title=DPP-4 Inhibitors for Type 2 Diabetes: Drug Safety Communication - May Cause Severe Joint Pain|url=http://www.fda.gov/Safety/MedWatch/SafetyInformation/SafetyAlertsforHumanMedicalProducts/ucm460238.htm|website=FDA|accessdate=1 September 2015|date=2015-08-28}} 8. ^https://docs.boehringer-ingelheim.com/Prescribing%20Information/PIs/Tradjenta/Tradjenta.pdf?DMW_FORMAT=pdf) 9. ^https://en.wikipedia.org/wiki/Bronchial_hyperresponsiveness 10. ^{{cite web|title=International Nonproprietary Names for Pharmaceutical Substances (INN). Recommended International Nonproprietary names: List 61|url=http://www.who.int/medicines/publications/druginformation/innlists/RL61.pdf|publisher=World Health Organization|accessdate=10 November 2016|page=66}} External links{{Commons category}}
7 : Alkynes|Dipeptidyl peptidase-4 inhibitors|Piperidines|Quinazolines|Xanthines|Eli Lilly and Company|Boehringer Ingelheim |
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