Evaluation of drug interactions of saxagliptin with sildenafil in healthy volunteers.
Purpose: The purpose of this study is to investigate the effect of sildenafil a CYP3A4 substrate and inhibitor on the pharmacokinetics and safety of saxagliptin. Methods: Eighteen healthy volunteers were recruited in sequential; single-center study to determine pharmacokinetic parameters of saxaglip...
| Publicado en: | European Journal of Clinical Pharmacology Vol. 78; no. 12; pp. 1935 - 1945 |
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| Autores principales: | , , , |
| Formato: | research tables/charts Journal Article |
| Publicado: |
Springer Nature
Dec2022
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| Acceso en línea: | Ver este registro en EBSCOhost |
| fields | @attributes: recordID: 1 pdfLink: plink: https://search.ebscohost.com/login.aspx?direct=true&db=ccm&AN=160141327&site=ehost-live header: @attributes: shortDbName: ccm uiTerm: 160141327 longDbName: CINAHL Complete uiTag: AN controlInfo: bkinfo: dissinfo: jinfo: jid: 00316970 NP9 jtl: European Journal of Clinical Pharmacology issn: 00316970 maglogo: N pubinfo: dt: Dec2022 vid: 78 iid: 12 pid: 237 pub: Springer Nature place: New York, New York artinfo: ui: 160141327 160141327 160141327 10.1007/s00228-022-03397-w 160141327 ppf: 1935 ppct: 10 formats: fmt: – @attributes: type: T – @attributes: type: P tig: atl: Evaluation of drug interactions of saxagliptin with sildenafil in healthy volunteers. aug: au: Mansour, Rania Y. ElBorolossy, Radwa Shaheen, Sara M. Sabri, Nagwa A. affil: MScs. Of Clinical Pharmacy, Faculty of Pharmacy, Ain Shams University, Cairo, Egypt sug: subj: Drug Interactions Evaluation Hypoglycemic Agents Pharmacokinetics Sildenafil Pharmacodynamics Safety Human Sildenafil Administration and Dosage Confidence Intervals Mass Spectrometry ab: Purpose: The purpose of this study is to investigate the effect of sildenafil a CYP3A4 substrate and inhibitor on the pharmacokinetics and safety of saxagliptin. Methods: Eighteen healthy volunteers were recruited in sequential; single-center study to determine pharmacokinetic parameters of saxagliptin and sildenafil, and (AUC0-∞), (AUC0-t); Cmax; tmax; t½, ke; ka were measured using validated LC–MS/MS method. Therapeutic doses were given as follows: Sildenafil 50 mg single dose on day one, then washout period from day two till day eight. Saxagliptin 5 mg once/day was given from day 9 till day 12; then on day 13, the two drugs were co-administered. Blood samples for pharmacokinetic analysis were collected on days 1 and 13 for sildenafil and on days 12 and 13 for saxagliptin. Results: Saxagliptin ratios of T/R and 90% CI were 132.1% (122.7–142.3) for AUC0–t, and 167.6% (154.6–181.8) for Cmax. On the other hand, sildenafil pharmacokinetics were not affected. Gmax changed from 93.7 mg/dl to 95.6 mg/dl (P > 0.001) and AUCg0-t from 512.8 ng.h/ml to 532.75 ng.h/ml (P > 0.001) after co-administration of both drugs. Conclusion: Sildenafil significantly affected the pharmacokinetic parameters of saxagliptin when co-administered. Registration: This trial was registered at clinicaltrials.gov under identifier number: [NCT04170790] in November 2019. pubtype: Academic Journal doctype: research tables/charts Journal Article ougenre: Article language: English refInfo: holdings: @attributes: islocal: N |
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