alexa Pharmacokinetics and Safety of Sublingual Flumazenil (CRLS035) in Healthy Adults (Potential Therapy for Hepatic Encephalopathy)
ISSN: 2153-0645

Journal of Pharmacogenomics & Pharmacoproteomics
Open Access

Like us on:
OMICS International organises 3000+ Global Conferenceseries Events every year across USA, Europe & Asia with support from 1000 more scientific Societies and Publishes 700+ Open Access Journals which contains over 50000 eminent personalities, reputed scientists as editorial board members.

Open Access Journals gaining more Readers and Citations

700 Journals and 15,000,000 Readers Each Journal is getting 25,000+ Readers

This Readership is 10 times more when compared to other Subscription Journals (Source: Google Analytics)

Research Letter

Pharmacokinetics and Safety of Sublingual Flumazenil (CRLS035) in Healthy Adults (Potential Therapy for Hepatic Encephalopathy)

Saadi T1, Kramskay R1, Zilberman Peled B2, Katz N3, Peled N2 and Baruch Y1,4*

1Liver Unit, Rambam Health Care Campus, Haifa, Israel

2Coeruleus Ltd, Israel

3Sleep Laboratory, Assuta Medical Center, Tel Aviv, Israel

4Bruce Rappaport Faculty of Medicine, Technion-Israel Institute of Technology, Haifa, Israel

*Corresponding Author:
Dr. Yaacov Baruch, MD
Liver Unit, Rambam Health Care Campus
POB 9602, Haifa 31096, Israel
Tel: +972-4-854-3049
Fax: +972-4-854-2477
E-mail: [email protected]

Received date: August 08, 2014; Accepted date: September 11, 2014; Published date: September 20, 2014

Citation: Saadi T, Kramskay R, Peled BZ, Katz K, Peled N, et al. (2014) Pharmacokinetics and Safety of Sublingual Flumazenil (CRLS035) in Healthy Adults (Potential Therapy for Hepatic Encephalopathy). J Pharmacogenomics Pharmacoproteomics 5:140. doi: 10.4172/2153-0645.1000140

Copyright: © 2014 Saadi T, et al. This is an open-access article distributed under the terms of the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are credited.

 

Abstract

Flumazenil, a GABAA receptor antagonist, has a significant clinical benefit especially in overt hepatic encephalopathy patients, although it requires intravenous access. A novel highly concentrated sublingual spray formulation of flumazenil (CRLS035) was developed by Coeruleus Ltd. The aim of this study was to determine the single dose safety and pharmacokinetics of sublingual CRLS035 versus flumazenil intravenously (IV) in healthy volunteers.
Ten healthy adult volunteers participated in the study. CRLS035 was administered sublingually in two doses (1.1 mg and 2.2 mg) vs. IV flumazenil (0.2 mg). Subjects were evaluated after a high-fat diet and water consumption. Blood samples were collected pre- and post-dose at eight time points. Flumazenil levels were analyzed for Cmax, Tmax, Cmin, Tmin, AUC0-∞, AUC0-t and T1/2. Safety variables included local oral area and assessment of systemic adverse events.
The estimated bioavailability of the two sublingual doses was 14% and 11%, respectively. The bioequivalence of the 1.1 mg sublingual dose was similar to the 0.2 mg IV dose. Water consumption and the high-fat diet did not change the pharmacokinetic parameters significantly. No associated adverse events were reported across the study.
The pharmacokinetics of sublingual flumazenil is comparable to intravenous administration and the drug is safe. The sublingual approach allows convenient and better treatment availability for patients with hepatic encephalopathy.

Keywords

Share This Page

Additional Info

Loading
Loading Please wait..
 
Peer Reviewed Journals
 
Make the best use of Scientific Research and information from our 700 + peer reviewed, Open Access Journals
International Conferences 2017-18
 
Meet Inspiring Speakers and Experts at our 3000+ Global Annual Meetings

Contact Us

Agri, Food, Aqua and Veterinary Science Journals

Dr. Krish

[email protected]

1-702-714-7001 Extn: 9040

Clinical and Biochemistry Journals

Datta A

[email protected]

1-702-714-7001Extn: 9037

Business & Management Journals

Ronald

[email protected]

1-702-714-7001Extn: 9042

Chemical Engineering and Chemistry Journals

Gabriel Shaw

[email protected]

1-702-714-7001 Extn: 9040

Earth & Environmental Sciences

Katie Wilson

[email protected]

1-702-714-7001Extn: 9042

Engineering Journals

James Franklin

[email protected]

1-702-714-7001Extn: 9042

General Science and Health care Journals

Andrea Jason

[email protected]

1-702-714-7001Extn: 9043

Genetics and Molecular Biology Journals

Anna Melissa

[email protected]

1-702-714-7001 Extn: 9006

Immunology & Microbiology Journals

David Gorantl

[email protected]

1-702-714-7001Extn: 9014

Informatics Journals

Stephanie Skinner

[email protected]

1-702-714-7001Extn: 9039

Material Sciences Journals

Rachle Green

[email protected]

1-702-714-7001Extn: 9039

Mathematics and Physics Journals

Jim Willison

[email protected]

1-702-714-7001 Extn: 9042

Medical Journals

Nimmi Anna

[email protected]

1-702-714-7001 Extn: 9038

Neuroscience & Psychology Journals

Nathan T

[email protected]

1-702-714-7001Extn: 9041

Pharmaceutical Sciences Journals

John Behannon

[email protected]

1-702-714-7001Extn: 9007

Social & Political Science Journals

Steve Harry

[email protected]

1-702-714-7001 Extn: 9042

 
© 2008-2017 OMICS International - Open Access Publisher. Best viewed in Mozilla Firefox | Google Chrome | Above IE 7.0 version
adwords