In vivo biopharmaceutical characterisation of a new formulation containing the antiepileptic drug lamotrigine in comparison to plain and dispersible/chewable lamotrigine tablets.

Aim: Two studies in healthy male volunteers were carried out to evaluate the pharmacokinetic profile of a new divisible formulation of lamotrigine (CAS 84057-84-1, Plexxo, Lamotrigin Desitin) in plasma in comparison to plain or dispersible lamotrigine tablets.

Methods: The plasma pharmacokinetics of lamotrigine were analysed after administration of single doses of 100 mg lamotrigine given as one tablet of the new formulation and either the plain or the dispersible reference formulation in two separate studies. In each study the data of 24 subjects were analysed according to the study protocol.

Single dose pharmacokinetics of alpha-dihydroergocryptine in patients with moderate to severe renal insufficiency.

Aim: This study was carried out to evaluate the pharmacokinetic profile of alpha-dihydroergocryptine (CAS 14271-05-7, DHEC, Almirid) in plasma and urine in patients with moderately to severely impaired renal function (creatinine clearance < 30 ml.min-1.1.

Erythromycin increases plasma concentrations of alpha-dihydroergocryptine in humans.

Objective: Our objective was to investigate the potential for relevant pharmacotherapeutic interaction between cytochrome P4503A4 (CYP3A4)-inhibiting agents such as erythromycin and the dopamine agonist alpha-dihydroergocryptine (DHEC).

Methods: The study was carried out as a single-center, controlled, nonblinded, 2-way crossover clinical trial with randomly allocated period-balanced sequences, investigating two treatments of a single oral dose of 10 mg DHEC (on the morning of day 1), once administered alone (reference), once along with a 4-day treatment (days -2 to 1) of 500 mg erythromycin 3 times daily. Periods were separated by a washout of at least 14 days.

Influence of the dopamine agonist alpha-dihydroergocryptine on the pharmacokinetics of levodopa in patients with Parkinson's disease.

This study investigated whether chronic coadministration of alpha-dihydroergocryptine (DHEC) altered the plasma pharmacokinetics of individualized treatments with levodopa in 12 patients with Parkinson's disease. Steady-state pharmacokinetics of plasma levodopa (L-Dopa) under combined treatment were compared with those under treatment with L-Dopa alone. There was no evidence of increased exposure to L-Dopa caused by concomitant treatment with DHEC.

Plasma and urine pharmacokinetics of the dopamine agonist alpha-dihydroergocryptine in patients with hepatic dysfunction.

Objective: The aim of this study was to evaluate the pharmacokinetic behavior of unchanged alpha-dihydroergocryptine (DHEC, Almirid, Desitin Arzneimittel GmbH, Hamburg, Germany, under licence of Polichem S.A., Luxembourg) and total DHEC (unchanged DHEC and pooled metabolites) in plasma and urine in patients with impaired hepatic function, following administration of single oral doses.