BIOAVAILABILITY FILE: LAMOTRIGINE
Tuba İNCEÇAYIR*, İlbeyi AĞABEYOĞLU*^,o
* Gazi University, Faculty of Pharmacy, Department of Pharmaceutical Technology, 06330, Etiler, Ankara, TURKEY
 
^oCorresponding Author

Summary

Lamotrigine (LTG) is a phenyltriazine class anticonvulsant that shows efficacy against partial and generalized epilepsies. It exerts its antiepileptic effects by blocking voltage-sensitive sodium channels and inhibiting the release of excitatory neurotransmitters, particularly glutamate and aspartate. LTG is well absorbed with bioavailability approaching 100%. There is negligible first-pass effect. It is widely distributed to all organs and tissues. The volume of distribution is between 0.87 and 1.2 L/kg in healthy volunteers. Protein binding is about 55%. The half-life of LTG is between 24.1 and 31.2 hours after single oral doses in healthy volunteers, but it may be altered by enzyme-inducing and -inhibiting drugs. Age and disease states play important roles in LTG pharmacokinetics and dosage adjustment. The physicochemical
properties, analytical methods, pharmacokinetics, bioavailability and pharmacology of LTG are discussed in this review.

Key Words :
Lamotrigine, pharmacokinetics, bioavailability, pharmacology