Valproic acid fails to displace phenobarbitone and carbamazepine from plasma protein binding sites in epileptic patients.

Pisani, F; Oteri, G.; Perri, R. Di

doi:10.1111/j.1365-2125.1981.tb01859.x

Brit J Clinical Pharma

1981

DOI: 10.1111/j.1365-2125.1981.tb01859.x

|View full text |Cite

Valproic acid fails to displace phenobarbitone and carbamazepine from plasma protein binding sites in epileptic patients.

F Pisani¹,

G. Oteri²,

R. Di Perri³

Help me understand this report

Search citation statements

Order By: Relevance

Paper Sections

Select...

Citation Types

Supporting

Mentioning

Contrasting

Year Published

1986

1996

Publication Types

Select...

Article5

Relationship

Self Cite0

Independent5

Authors

Journals

Cited by 5 publications

References 14 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

Comparison of Equations for Predicting Bound Serum Concentrations of Carbamazepine and Carbamazepine‐10, 11‐epoxide After Polytherapy in Patients with Epilepsy

Kodama¹,

Kuranari²,

Kodama³

et al. 1995

The Journal of Clinical Pharma

View full text Add to dashboard Cite

In a previous study, an equation with in vivo population binding parameters of carbamazepine and carbamazepine-10, 11-epoxide (CBZ-E) to serum proteins for the relation between unbound and bound serum concentrations was defined. A review by Pynnönen indicates that the average bound/unbound plasma fraction ratio is 3.0 for carbamazepine and 1.0 for CBZ-E. In this study, the ability of equations with in vivo population binding parameters of the previous study (method 1) or with the average bound/unbound plasma fraction ratio of 3.0 of Pynnönen (method 2) to predict the bound serum carbamazepine concentration was retrospectively evaluated using 85 serum samples from 46 patients with epilepsy taking carbamazepine polytherapy. In 21 serum samples from 16 patients, the ability of these equations to predict bound serum CBZ-E concentration was also determined with in vivo population binding parameters from the previous study (method A) or with the average bound/unbound plasma fraction ratio of 1.0 of Pynnönen (method B). Mean prediction error, mean absolute prediction error (MAE), and root mean squared error (RMSE) were calculated for each method, and these values served as a measure of prediction bias and precision. Method 1 showed a bias to overpredict bound serum carbamazepine. The MAE and RMSE were significantly smaller with method 2 (MAE = 2.4 mumol/L; RMSE = 3.2 mumol/L) than with method 1 (MAE = 4.1 mumol/L; RMSE = 4.8 mumol/L). Method 2 was superior to method 1 in terms of accuracy and precision. For bound CBZ-E prediction, method B had a bias to underprediction. The MAE and RMSE were smaller with method A (MAE = 0.581 mumol/L; RMSE = 0.796 mumol/L) than with method B (MAE = 0.724 mumol/L; RMSE = 0.905 mumol/L). Method A was superior to method B in terms of accuracy and precision.

show abstract

Comparison of Equations for Predicting Bound Serum Concentrations of Carbamazepine and Carbamazepine‐10, 11‐epoxide After Polytherapy in Patients with Epilepsy

Kodama¹,

Kuranari²,

Kodama³

et al. 1995

The Journal of Clinical Pharma

View full text Add to dashboard Cite

show abstract

Evaluation of Equations for Unbound Serum Concentration Prediction of Carbamazepine and Carbamazepine-10,11-epoxide in Polytherapy Pediatric Patients with Epilepsy

Kodama

Kuranari

Kodama

et al. 1995

Journal of Pharmaceutical Sciences

View full text Add to dashboard Cite

Sodium Valproate and Valpromide: Differential Interactions with Carbamazepine in Epileptic Patients

et al. 1986

View full text Add to dashboard Cite

To evaluate the comparative effects of valproic acid (VPA) and valpromide (VPM) on plasma levels and protein binding of carbamazepine (CBZ) and CBZ-10,11-epoxide (CBZ-E), 12 adult epileptic patients stabilized on CBZ monotherapy were divided into two groups. One group (n = 6) received sodium valproate (1,100 mg/day) for 2 weeks, while the other group (n = 6) was given, for the same period, a dosage of VPM (1,200 mg/day) expected to produce VPA levels equivalent to those achieved with valproate. Plasma CBZ levels were not affected by either treatment. In the valproate-treated group, plasma CBZ-E levels increased by 101% (range, 29-238%) within 1 week of combined therapy (p less than 0.02) and returned to baseline values after VPA treatment was stopped. In the VPM-treated patients, the elevation of plasma CBZ-E levels was much greater. In this group, plasma CBZ-E increased by 330% (range, 110-864%), and this was associated in two patients with the appearance of adverse effects which subsided after reducing the VPM dosage. The plasma protein binding of CBZ and CBZ-E was not affected significantly by VPM or valproate therapy. Plasma VPA levels were similar in the two groups. It is concluded that VPM is not simply a prodrug of VPA. Although both VPA and VPM increase CBZ-E levels--probably by inhibiting the enzyme epoxide hydrolase--the interaction caused by VPM is of much greater magnitude and potential clinical significance.

show abstract

scite is a Brooklyn-based organization that helps researchers better discover and understand research articles through Smart Citations–citations that display the context of the citation and describe whether the article provides supporting or contrasting evidence. scite is used by students and researchers from around the world and is funded in part by the National Science Foundation and the National Institute on Drug Abuse of the National Institutes of Health.

Contact Info

customersupport@researchsolutions.com

10624 S. Eastern Ave., Ste. A-614

Henderson, NV 89052, USA

This site is protected by reCAPTCHA and the Google Privacy Policy and Terms of Service apply.

Blog Terms and Conditions API Terms Privacy Policy Contact Cookie Preferences Do Not Sell or Share My Personal Information

Made with 💙 for researchers

Part of the Research Solutions Family.

Valproic acid fails to displace phenobarbitone and carbamazepine from plasma protein binding sites in epileptic patients.

Cited by 5 publications

References 14 publications

Comparison of Equations for Predicting Bound Serum Concentrations of Carbamazepine and Carbamazepine‐10, 11‐epoxide After Polytherapy in Patients with Epilepsy

Comparison of Equations for Predicting Bound Serum Concentrations of Carbamazepine and Carbamazepine‐10, 11‐epoxide After Polytherapy in Patients with Epilepsy

Evaluation of Equations for Unbound Serum Concentration Prediction of Carbamazepine and Carbamazepine-10,11-epoxide in Polytherapy Pediatric Patients with Epilepsy

Sodium Valproate and Valpromide: Differential Interactions with Carbamazepine in Epileptic Patients

Contact Info

Product

Resources

About