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Eslicarbazepine acetate (ESL) is a new, once daily, orally administered, third generation antiepileptic drug which is indicated in the treatment of partial-onset seizures. ESL is known to exert it's anticonvulsant effect by blocking the voltage-gated sodium channels. Several clinical trials and pharmacological studies have revealed that seizure control was better with ESL monotherapy (1 200 or 1 600 mg once daily) following a switch from other antiepileptic drugs in comparison with pseudo-placebo patients. The studies have indicated the ESL to be well tolerated and produced only mild to moderate emergent adverse events with the therapy. Being a dibenzazepine family member, structure and chemistry of ESL resembles more or less to carbamazepine and oxcarbazepine. ESL differs structurally from carbamazepine and oxcarbazepine at the 10, 11 position of dibenazepine nucleus. This molecular variation results in differences in metabolism and thus helps to prevent the formation of toxic epoxide metabolites. ESL following oral administration is rapidly metabolised to active metabolite namely S-licarbazepine which is responsible for its pharmacological activity. ESL exhibits acceptable pharmacokinetic profile and shows insignificant drug-drug interactions. In phase III clinical program, ESL was found to be efficacious and well tolerated in adult patients with partial onset seizures previously not controlled with treatment with one or two other antiepileptic drugs. [ABSTRACT FROM AUTHOR]

The pentacyclic triterpenic acids isolated from the oleo gum resin of various Boswellia species are collectively called as Boswellic acids (BA). The oleo gum resin obtained from Indian variety i.e. Boswellia serrata (Family – Burseraceae) is commonly known as Salai guggal. The resin fraction of Salai guggal is rich in Boswellic acids and its essential oil is composed of a mixture of mono, di and sesquiterpenes while gum fraction chiefly contains pentose and hexose sugars. This oleo-gum resin is quite popular among traditional practitioners of traditional Chinese and Indian Systems of medicine owing to their wide range of useful biological properties such as anti-inflammatory, anti-arthritic, anti-rheumatic, anti-diarrheal, anti-hyperlipidemic, anti-asthmatic, anti-cancer, anti-microbial anti-fungal, anti-complementary and analgesic activity, etc. It has been used as a herbal medicine since the prehistoric time to cure acute and chronic ailments including inflammatory diseases. Phytochemical investigation of this herbal medicine lead to identification of Boswellic acids which are found to be novel, potent, specific anti-inflammatory agents due to non-redox inhibition of 5-lipoxygenase (5-LO) enzyme. However, the other important targets of Boswellic acids also include topoisomerases, angiogenesis, and cytochrome p450 enzymes. This review is a sincere attempt to discuss and present the current status of therapeutic potential, phytochemical as well as pharmacological profile of Boswellic acids primarily obtained from B. serrata . [ABSTRACT FROM AUTHOR]

Dronedarone, a benzofuran containing chemical compound, is a derivative of amiodarone which is classified as a Class III antiarrhythmic agent. It is prescribed to the cardiovascular patients who have paroxysmal or persistent atrial fibrillation to lower the chances of hospitalization. Amiodarone, sotalol, procainamide dofetilide, quinidine, ibutilide, flecainide, and propafenone are the other useful medicinal products used to treat atrial fibrillation or cardiac arrhythmia. Dronedarone was approved for clinical use in atrial fibrillation by the Food and Drug Administration in 2009. The generic name for dronedarone is Multaq (Sanofi Aventis). This article briefly highlights the important pharmacological, pharmacodynamic and pharmacokinetic properties of dronedarone. [ABSTRACT FROM AUTHOR]

In the last few decades, metabolite identification and detection have become an integral component of drug discovery process. The detection and depiction of an identified metabolite is significant for the development of safe and effective therapeutic agents as these metabolites may be pharmacologically active or toxic in nature. A (UPLC-MS/MS) method was developed for the quantification of eslicarbazepine acetate metabolite (M3), cis -10,11-dihydro-5 H -dibenz[b,f]azepine-10,11-diol, in rat plasma. Eslicarbazepine acetate was extracted from rat plasma by precipitation technique using acetonitrile as a precipitating solvent. Chromatographic separation was accomplished using acetonitrile-0.01 M potassium dihydrogen phosphate (60:40, v/v) as mobile phase at a flow rate of 0.2 ml/min on Waters Acquity BEH 150 × 2.1 mm, 1.7 µm, C18 column at 30˚ C. The linearity of the calibration curve was 5–100 ng/ml for metabolite M3. The overall intra- and inter-day precision did not exceed 3%. In silico , in vitro and in vivo approaches have been used to facilitate the detection and depiction of eslicarbazepine acetate metabolites. MetabolExpert was used to predict the probable metabolites of the compounds. Metabolite of eslicarbazepine acetate was identified using human liver microsomes. [ABSTRACT FROM AUTHOR]