ليناگلپتن


ليناگلپتن Linagliptin
الاسم النظامي (أيوپاك)
الاسم النظامي (أيوپاك)
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
المعينات Identifiers
رقم CAS	668270-12-0
كود ATC	A10BH05
PubChem	10096344
بيانات كيميائية
الصيغة	₂₅₂₈₈₂
كتلة جزيئية	472.54 g/mol
SMILES	search in eMolecules, PubChem
مرادفات	BI-1356
بيانات الحركية الدوائية Pharmacokinetic
التوافر الحيوي	~30% ( = 1.5 ساعة)
رابط بروتيني	75–99% (حسب الهجريز)
الأيض	الحد الأدنى (يستقلب ~10%)
عمر النصف	~24 ساعة
اخراج	البراز (80%)، البول (5%)
اعتبارات علاجية
بيانات الترخيص	EU US
فئة السلامة أثناء الحمل	B(الولايات المتحدة)
الوضع القانوني	Prescription Only (S4)(استراليا) POM(المملكة المتحدة) (الولايات المتحدة) ℞ Prescription only
المسارات	عن طريق الفم (أقراص)

ليناگلپتن Linagliptin، يُباع تحت الاسم التجاري ترادجـِنتا وغيرها، هودواء يستخدم لعلاج سكري النمط الثاني. It is generally less preferred than metformin and sulfonylureas. ويستخدم الدواء مع ممارسة التمرينات الرياضية واتباع حمية غذائية. لا يوصى باستخدامه لسقمى السكري النمط الثاني. يؤخذ عن طريق الفم.

Common side effects include inflammation of the nose and throat. Serious side effects may include angioedema, pancreatitis, joint pain. Use in pregnancy and breastfeeding is not recommended. Linagliptin is a dipeptidyl peptidase-4 inhibitor. It works by increasing the production of insulin and decreasing the production of glucagon by the pancreas.

Linagliptin was approved for medical use in the United States in 2011. A month supply in the United Kingdom costs the NHS about £33.26 as of 2019. In the United States the wholesale cost of this amount is about 391 USD. In 2016 it was the 196th most prescribed medication in the United States with more than ثلاثة million prescriptions.

الاستخدامات الطبية

Results in 2010 from a Phase III clinical trial of linagliptin showed that the drug can effectively reduce blood sugar.

الآثار الجانبية

Linagliptin may cause severe joint pain.

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 states the drug is contraindicated for people with bronchial hyperreactivity. Asthma is a form of bronchial hyperreactivity^[].

آلية العمل

Linagliptin belongs to a class of drugs called DPP-4 inhibitors.

المصطلح

Linagliptin is the INN.

انظر أيضاً

إمپاگليفلوزين/ليناگلپتن

المصادر

^ "Tradjenta (linagliptin) Tablets. Full Prescribing Information" (PDF). Boehringer Ingelheim Pharmaceuticals, Inc. Ridgefield, CT 06877 USA. Retrieved 10 November 2016.
^ "Linagliptin Monograph for Professionals". Drugs.com (in الإنجليزية). American Society of Health-System Pharmacists. Retrieved 6 April 2019.
^ British national formulary : BNF 76 (76 ed.). Pharmaceutical Press. 2018. p. 680. ISBN .
^ "NADAC as of 2019-02-27". Centers for Medicare and Medicaid Services (in الإنجليزية). Retrieved 3 March 2019.
^ "The Top 300 of 2019". clincalc.com. Retrieved 22 December 2018.
^ "Four Phase III Trials Confirm Benefits of BI's Oral, Once-Daily Type 2 Diabetes Therapy". Genetic Engineering & Biotechnology News. 28 June 2010.
^ "DPP-4 Inhibitors for Type 2 Diabetes: Drug Safety Communication - May Cause Severe Joint Pain". FDA. 2015-08-28. Retrieved 1 September 2015.
^ https://docs.boehringer-ingelheim.com/Prescribing%20Information/PIs/Tradjenta/Tradjenta.pdf?DMW_FORMAT=pdf)
^ Bronchial hyperresponsiveness
^ "International Nonproprietary Names for Pharmaceutical Substances (INN). Recommended International Nonproprietary names: List 61" (PDF). World Health Organization. p. 66. Retrieved 10 November 2016.