• Corpus ID: 28324103

THE INFLUENCE OF SERTRALINE ON THE PHARMACOKINETICS OF CARVEDILOL . A PRECLINICAL STUDY ON RATS

@inproceedings{Abrudan2017THEIO,
  title={THE INFLUENCE OF SERTRALINE ON THE PHARMACOKINETICS OF CARVEDILOL . A PRECLINICAL STUDY ON RATS},
  author={Maria B. Abrudan and Dana Maria Muntean and Maria Adriana Neag and Laurian Vlase and Ana-Maria Gheldiu},
  year={2017}
}
The objective of this study was to investigate the effect of multiple-dose sertraline on the pharmacokinetic profile of carvedilol in rats. Carvedilol was orally administrated in rats (3.57 mg/kg body mass (b.m.)) on the absence of sertraline or after a pre-treatment with multiple oral doses of sertraline (7.14 mg/kg b.m.). The plasma concentrations of carvedilol were estimated by HPLC-MS. After carvedilol co-administration with sertraline, an approximately 7.7-fold increase in the exposure of… 

Figures and Tables from this paper

INFLUENCE OF FLUVOXAMINE ON CARVEDILOL’S PHARMACOKINETICS IN RATS

The pharmacokinetic drug-drug interaction between carvedilol and fluvoxamine in vivo was demonstrated in vivo and the PK parameters were calculated by non-compartmental analysis.

Pharmacokinetic interactions study between carvedilol and some antidepressants in rat liver microsomes – a comparative study

The co-administration of tested antidepressants led to a significant alteration of carvedilol’s metabolism in vitro, and CYP2D6 inhibition is the main pharmacokinetic mechanism that can explain these drug-drug interactions, with possible clinical implications.

Influence of concomitant medication on plasma concentration of amiodarone in patients with atrial fibrillation - a pilot study

Furosemide may influence the pharmacokinetics of P-gp-interfering drugs and an underuse of amiodarone is reported, although the relevance of these findings needs to be confirmed and further research is needed.

References

SHOWING 1-10 OF 32 REFERENCES

The Pharmacokinetic Interaction Study between Carvedilol and Bupropion in Rats

Carvedilol was shown to have higher plasma concentrations, delay in maximum concentration, and a prolonged half-life, after being pretreated with bupropion, and the administration of multiple-dose bupropions influences the pharmacokinetics of carvedilol (single oral dose) in rats.

Evaluation of effects of polymorphism for metabolic enzymes on pharmacokinetics of carvedilol by population pharmacokinetic analysis.

The results suggested that the factors of interindividual variation for carvedilol clearance were creatinine clearance and polymorphisms of UGT2B7 and CYP2D6 in the Japanese population with heart disease.

Population pharmacokinetic analysis of drug–drug interactions among risperidone, bupropion, and sertraline in CF1 mice

It is suggested that pharmacokinetic interactions exist among these three psychoactive drugs involving inhibition of drug metabolizing enzymes and/or P-gp and other drug transporters present in the BBB.

The Impact of Paroxetine Coadministration on Stereospecific Carvedilol Pharmacokinetics

This study demonstrated a PK drug—drug interaction between paroxetine and carveilol, with considerable interparticipant variability in carvedilol PK parameters and magnitude of drug interaction.

Assessment of a Potential Pharmacokinetic Interaction between Nebivolol and Bupropion in Healthy Volunteers

The study concluded that bupropion influenced the PKs of nebivolol in healthy volunteers, but a clinical relevance was not established, however, this latter aspect requires further investigation.

THE IMPACT OF COMBINED ADMINISTRATION OF SEROTONIN-SPECIFIC REUPTAKE INHIBITORS WITH ATORVASTATIN ON THE LIVER AND KIDNEYS . IN VITRO AND IN VIVO STUDIES

The results of in vitro and in vivo experiments indicate this combination superior safety profile in comparison to atorvastatin coupled with paroxetine, and the adverse effect observed may point out the possibility of minor liver and kidney disorders during the longterm treatment with parxetine and atorVastatin.

Clinical Pharmacokinetics and Pharmacodynamics of Carvedilol

Carvedilol lowers blood pressure as a result of its β-blocking and vasodilatory activity and reduces left ventricular hypertrophy and has no significant adverse metabolic effects.

The extent and determinants of changes in CYP2D6 and CYP1A2 activities with therapeutic doses of sertraline.

In conclusion, sertraline treatment at a mean daily dosage of 94.0 mg did not significantly change CYP1A2 activity and resulted in a modest inhibition of CYP2D6 activity.

Carvedilol pharmacokinetics and pharmacodynamics in relation to CYP2D6 and ADRB pharmacogenetics.

Carvedilol is a drug where CYP2D6-related pharmacokinetic variation is apparently not carried forward into pharmacodynamic variation, and current knowledge does not allow utilizing ADRB1 and ADRB2 genotypes for clinical treatment decisions, which should stimulate further research on the impact of these genotypes in health and disease.