ليناگلپتن

ليناگلپتن
البيانات السريرية
النُطق	/ˌlɪnəˈɡlɪptɪn/ LIN-ə-GLIP-tin
الأسماء التجارية	Tradjenta, Trajenta, others
أسماء أخرى	BI-1356
AHFS/Drugs.com	Monograph
MedlinePlus	a611036
License data	EU EMA: by INN; US FDA: Linagliptin;
مسارات; الدواء	عن طريق الفم (أقراص)
رمز ATC	A10BH05 (WHO) ;
الحالة القانونية
الحالة القانونية	AU: S4 (Prescription only) ; UK: POM (Prescription only) ; US: ℞-only ; عموماً: ℞ (بوصفة فقط);
بيانات الحركية الدوائية
التوافر الحيوي	~30% (Tmax = 1.5 ساعة)
ارتباط الپروتين	75–99% (حسب التركيز)
الأيض	الحد الأدنى (يستقلب ~10%)
المستقلبات	Pharmacologically inactive
Elimination half-life	~24 ساعة
الإخراج	البراز (80%)، البول (5%)
المعرفات
	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;
رقم CAS	668270-12-0 ;
PubChem CID	10096344;
IUPHAR/BPS	6318;
ChemSpider	8271879 ;
UNII	3X29ZEJ4R2;
KEGG	D09566 ;
ChEBI	CHEBI:68610 ;
ChEMBL	CHEMBL237500 ;
Chemical and physical data
التركيب	C25H28N8O2
الكتلة المولية	472.54 g/mol
3D model (JSmol)	Interactive image;
	SMILES CC#CCN1C2=C(N=C1N3CCC[C@H](C3)N)N(C(=O)N(C2=O)CC4=NC5=CC=CC=C5C(=N4)C)C;
	InChI InChI=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 ; Key:LTXREWYXXSTFRX-QGZVFWFLSA-N ;
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ليناگلپتن Linagliptin، يُباع تحت الاسم التجاري ترادجـِنتا وغيرها، هو دواء يستخدم لعلاج سكري النمط الثاني.^[2] It is generally less preferred than metformin and sulfonylureas.^[2]^[3] ويستخدم الدواء مع ممارسة التمرينات الرياضية واتباع حمية غذائية.^[2] لا يوصى باستخدامه لمرضى السكري النمط الثاني.^[2] يؤخذ عن طريق الفم.^[2]

Common side effects include inflammation of the nose and throat.^[2] Serious side effects may include angioedema, pancreatitis, joint pain.^[3]^[2] Use in pregnancy and breastfeeding is not recommended.^[3] 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]

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الاستخدامات الطبية

Results in 2010 from a Phase III clinical trial of linagliptin showed that the drug can effectively reduce blood sugar.^[6]

الآثار الجانبية

Linagliptin 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]^{[مرجع دائرة مفرغة]}.

آلية العمل

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

المصطلح

Linagliptin is the INN.^[10]

انظر أيضاً

إمپاگليفلوزين/ليناگلپتن

المصادر

^ ^أ ^ب "Tradjenta (linagliptin) Tablets. Full Prescribing Information" (PDF). Boehringer Ingelheim Pharmaceuticals, Inc. Ridgefield, CT 06877 USA. Retrieved 10 November 2016.
^ ^أ ^ب ^ت ^ث ^ج ^ح ^خ ^د ^ذ ^ر "Linagliptin Monograph for Professionals". Drugs.com (in الإنجليزية). American Society of Health-System Pharmacists. Retrieved 6 April 2019.
^ ^أ ^ب ^ت ^ث British national formulary : BNF 76 (76 ed.). Pharmaceutical Press. 2018. p. 680. ISBN 9780857113382.
^ "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.

وصلات خارجية

"Linagliptin". Drug Information Portal. U.S. National Library of Medicine.
Trajenta (Australia)
"Trajenta EPAR". European Medicines Agency (EMA).

[PI-1] أ ^ب "Tradjenta (linagliptin) Tablets. Full Prescribing Information" (PDF). Boehringer Ingelheim Pharmaceuticals, Inc. Ridgefield, CT 06877 USA. Retrieved 10 November 2016.

[AHFS2019-2] أ ^ب ^ت ^ث ^ج ^ح ^خ ^د ^ذ ^ر "Linagliptin Monograph for Professionals". Drugs.com (in الإنجليزية). American Society of Health-System Pharmacists. Retrieved 6 April 2019.

[BNF76-3] أ ^ب ^ت ^ث British national formulary : BNF 76 (76 ed.). Pharmaceutical Press. 2018. p. 680. ISBN 9780857113382.

[NADAC2019-4] "NADAC as of 2019-02-27". Centers for Medicare and Medicaid Services (in الإنجليزية). Retrieved 3 March 2019.

[5] "The Top 300 of 2019". clincalc.com. Retrieved 22 December 2018.

[6] "Four Phase III Trials Confirm Benefits of BI's Oral, Once-Daily Type 2 Diabetes Therapy". Genetic Engineering & Biotechnology News. 28 June 2010.

[7] "DPP-4 Inhibitors for Type 2 Diabetes: Drug Safety Communication - May Cause Severe Joint Pain". FDA. 2015-08-28. Retrieved 1 September 2015.

[8] ttps://docs.boehringer-ingelheim.com/Prescribing%20Information/PIs/Tradjenta/Tradjenta.pdf?DMW_FORMAT=pdf)

[9] Bronchial hyperresponsiveness

[INN-10] "International Nonproprietary Names for Pharmaceutical Substances (INN). Recommended International Nonproprietary names: List 61" (PDF). World Health Organization. p. 66. Retrieved 10 November 2016.

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وبينار	مصادر	صور	الأخبار	فيديو

البيانات السريرية

النُطق	/ˌlɪnəˈɡlɪptɪn/ LIN-ə-GLIP-tin
الأسماء التجارية	Tradjenta, Trajenta, others
أسماء أخرى	BI-1356
AHFS/Drugs.com	Monograph
MedlinePlus	a611036
License data	EU EMA: by INN US FDA: Linagliptin
مسارات الدواء	عن طريق الفم (أقراص)
رمز ATC	A10BH05 (WHO)
الحالة القانونية
الحالة القانونية	AU: S4 (Prescription only) UK: POM (Prescription only) US: ℞-only عموماً: ℞ (بوصفة فقط)
بيانات الحركية الدوائية
التوافر الحيوي	~30% (T_max = 1.5 ساعة)
ارتباط الپروتين	75–99% (حسب التركيز)
الأيض	الحد الأدنى (يستقلب ~10%)
المستقلبات	Pharmacologically inactive
Elimination half-life	~24 ساعة
الإخراج	البراز (80%)، البول (5%)^[1]
المعرفات
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
رقم CAS	668270-12-0^Y
PubChem CID	10096344
IUPHAR/BPS	6318
ChemSpider	8271879^N
UNII	3X29ZEJ4R2
KEGG	D09566^Y
ChEBI	CHEBI:68610^N
ChEMBL	CHEMBL237500^N
Chemical and physical data
التركيب	C₂₅H₂₈N₈O₂
الكتلة المولية	472.54 g/mol
3D model (JSmol)	Interactive image
SMILES CC#CCN1C2=C(N=C1N3CCC[C@H](C3)N)N(C(=O)N(C2=O)CC4=NC5=CC=CC=C5C(=N4)C)C
InChI InChI=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^N Key:LTXREWYXXSTFRX-QGZVFWFLSA-N^N
^NY (what is this?) (verify)