Eab Brivaracetam Phase lll: results 2013 k。 Mechanism of action Synaptic vesicle protein 2A ligand Inhibits voltage-dependent sodium channels 8.· Efficacy Likely similar to levetiracetam Broad spectrum for generalized and focal seizures KENTUCKY College of Pharmacy
Brivaracetam • Phase III; results 2013 • Mechanism of action – Synaptic vesicle protein 2A ligand – Inhibits voltage-dependent sodium channels • Efficacy – Likely similar to levetiracetam – Broad spectrum for generalized and focal seizures
Brivaracetam i· Pharmacokinetics 00 Linear Low protein-binding; Vd=0.6 L/kg Renally eliminated; t1/2=8 hours o000oc0= Drug-drug interaction Increased concentrations of 10, 11-epoxide of carbamazepine KENTUCKY College of Pharmacy
Brivaracetam • Pharmacokinetics – Linear – Low protein-binding; Vd=0.6 L/kg – Renally eliminated; t1/2=8 hours • Drug-drug interaction – Increased concentrations of 10,11-epoxide of carbamazepine
Multiple sclerosis oE. Disease modifying therapy 00 Fingolimod Teriflunomide Dimethyl fumarate 8家· Symptomatic therapy Dalfampridine Dextromethorphan/quinidine KENTUCKY College of Pharmacy
Multiple Sclerosis • Disease modifying therapy – Fingolimod – Teriflunomide – Dimethyl fumarate • Symptomatic therapy – Dalfampridine – Dextromethorphan/quinidine
Eab Fingolimod Sphingosine-1-phosphate(S1P receptor modulator 00 S1P activates the s1p receptor 1 High levels of S1P1 are seen when lymphocytes are in the lymph nodes and they are low when o000oc0= lymphocytes are in the bloodstream Fingolimod causes the lymphocytes to stay in the lymph nodes and so is immunosuppressive and anti 9 8: inflammatory KENTUCKY College of Pharmacy
Fingolimod • Sphingosine-1-phosphate (S1P) receptor modulator • S1P activates the S1P receptor 1 • High levels of S1P1 are seen when lymphocytes are in the lymph nodes and they are low when lymphocytes are in the bloodstream • Fingolimod causes the lymphocytes to stay in the lymph nodes and so is immunosuppressive and antiinflammatory
Eab Fingolimod Pharmacokinetics oE.- Steady-state concentrations within 1-2 months Metabolized by cyp4F2(major) and CYP2D6, 2E1 3A4, and 4F12(minor) Half-life 6-9 days, effects for 1-2 months a 3. Common adverse effects Headache Liver enzyme elevations Cough Diarrhea KENTUCKY College of Pharmacy
Fingolimod • Pharmacokinetics – Steady-state concentrations within 1-2 months – Metabolized by CYP4F2 (major) and CYP2D6, 2E1, 3A4, and 4F12 (minor) – Half-life 6-9 days, effects for 1-2 months • Common adverse effects – Headache – Liver enzyme elevations – Cough – Diarrhea