Pharmacokinetic interaction between linagliptin and tadalafil in healthy Egyptian males using a novel LC-MS method
Aim: Assessment of pharmacokinetic interaction between linagliptin (LNG) and tadalafil (TDL) in healthy males. Methods: First, a novel LC-MS method was developed; second, a Phase IV, open-label, cross-over study was performed. Volunteers took single 20-mg TDL dose on day 1 followed by wash out period of 2 weeks then multiple oral dosing of 5-mg/day LNG for 13 days. On day 13, volunteers were co-administered 20-mg TDL. Results: LNG and TDL single doses did not affect QTc interval. Smoking did not alter pharmacokinetics/pharmacodynamics of LNG and TDL. Co-administration of LNG with TDL resulted in TDL longer time to reach maximum plasma concentration (Tmax), decreased oral clearance (Cl/F) and oral volume of distribution (Vd/F), increased its maximum plasma concentration (Cmax), area under concentration-time curve (AUC), muscle pain and QTc prolongation. Conclusion: LNG and TDL co-administration warrants monitoring and/or TDL dose adjustment.
| Medienart: |
E-Artikel |
|---|
| Erscheinungsjahr: |
2019 |
|---|---|
| Erschienen: |
2019 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:11 |
|---|---|
| Enthalten in: |
Bioanalysis - 11(2019), 14 vom: 19. Juli, Seite 1321-1336 |
| Sprache: |
Englisch |
|---|
| Beteiligte Personen: |
Mourad, Sara S [VerfasserIn] |
|---|
| Links: |
|---|
| Themen: |
3X29ZEJ4R2 |
|---|
| Anmerkungen: |
Date Completed 17.01.2020 Date Revised 17.01.2020 published: Print-Electronic Citation Status MEDLINE |
|---|
| doi: |
10.4155/bio-2018-0097 |
|---|
| funding: |
|
|---|---|
| Förderinstitution / Projekttitel: |
|
| PPN (Katalog-ID): |
NLM299802124 |
|---|
| LEADER | 01000naa a22002652 4500 | ||
|---|---|---|---|
| 001 | NLM299802124 | ||
| 003 | DE-627 | ||
| 005 | 20231225101133.0 | ||
| 007 | cr uuu---uuuuu | ||
| 008 | 231225s2019 xx |||||o 00| ||eng c | ||
| 024 | 7 | |a 10.4155/bio-2018-0097 |2 doi | |
| 028 | 5 | 2 | |a pubmed24n0999.xml |
| 035 | |a (DE-627)NLM299802124 | ||
| 035 | |a (NLM)31368774 | ||
| 040 | |a DE-627 |b ger |c DE-627 |e rakwb | ||
| 041 | |a eng | ||
| 100 | 1 | |a Mourad, Sara S |e verfasserin |4 aut | |
| 245 | 1 | 0 | |a Pharmacokinetic interaction between linagliptin and tadalafil in healthy Egyptian males using a novel LC-MS method |
| 264 | 1 | |c 2019 | |
| 336 | |a Text |b txt |2 rdacontent | ||
| 337 | |a ƒaComputermedien |b c |2 rdamedia | ||
| 338 | |a ƒa Online-Ressource |b cr |2 rdacarrier | ||
| 500 | |a Date Completed 17.01.2020 | ||
| 500 | |a Date Revised 17.01.2020 | ||
| 500 | |a published: Print-Electronic | ||
| 500 | |a Citation Status MEDLINE | ||
| 520 | |a Aim: Assessment of pharmacokinetic interaction between linagliptin (LNG) and tadalafil (TDL) in healthy males. Methods: First, a novel LC-MS method was developed; second, a Phase IV, open-label, cross-over study was performed. Volunteers took single 20-mg TDL dose on day 1 followed by wash out period of 2 weeks then multiple oral dosing of 5-mg/day LNG for 13 days. On day 13, volunteers were co-administered 20-mg TDL. Results: LNG and TDL single doses did not affect QTc interval. Smoking did not alter pharmacokinetics/pharmacodynamics of LNG and TDL. Co-administration of LNG with TDL resulted in TDL longer time to reach maximum plasma concentration (Tmax), decreased oral clearance (Cl/F) and oral volume of distribution (Vd/F), increased its maximum plasma concentration (Cmax), area under concentration-time curve (AUC), muscle pain and QTc prolongation. Conclusion: LNG and TDL co-administration warrants monitoring and/or TDL dose adjustment | ||
| 650 | 4 | |a Clinical Trial, Phase IV | |
| 650 | 4 | |a Journal Article | |
| 650 | 4 | |a LC–MS | |
| 650 | 4 | |a QTc interval | |
| 650 | 4 | |a diabetes | |
| 650 | 4 | |a erectile dysfunction | |
| 650 | 4 | |a gliptins | |
| 650 | 4 | |a pharmacokinetics | |
| 650 | 7 | |a Linagliptin |2 NLM | |
| 650 | 7 | |a 3X29ZEJ4R2 |2 NLM | |
| 650 | 7 | |a Tadalafil |2 NLM | |
| 650 | 7 | |a 742SXX0ICT |2 NLM | |
| 700 | 1 | |a El-Kimary, Eman I |e verfasserin |4 aut | |
| 700 | 1 | |a Barary, Magda A |e verfasserin |4 aut | |
| 700 | 1 | |a Hamdy, Dalia A |e verfasserin |4 aut | |
| 773 | 0 | 8 | |i Enthalten in |t Bioanalysis |d 2009 |g 11(2019), 14 vom: 19. Juli, Seite 1321-1336 |w (DE-627)NLM196969840 |x 1757-6199 |7 nnns |
| 773 | 1 | 8 | |g volume:11 |g year:2019 |g number:14 |g day:19 |g month:07 |g pages:1321-1336 |
| 856 | 4 | 0 | |u http://dx.doi.org/10.4155/bio-2018-0097 |3 Volltext |
| 912 | |a GBV_USEFLAG_A | ||
| 912 | |a GBV_NLM | ||
| 951 | |a AR | ||
| 952 | |d 11 |j 2019 |e 14 |b 19 |c 07 |h 1321-1336 | ||