pharmacokinetic-pharmacodynamic interaction between four different single doses of bia 3-202 and a single dose of levodopa/benserazide (100/25 mg)

Conditions: Parkinson's Disease

Summary: the purpose of this study is to investigate the tolerability, pharmacokinetic profile of bia 3-202 and its metabolites, and the pharmacokinetic and pharmacodynamic interaction between 4 different single doses of bia 3-202 (50 mg, 100 mg, 200 mg and 400 mg) and a single dose of standard levodopa 100 mg/benserazide 25 mg (madopar® 125) in adult male and female healthy volunteers.

this was a single centre, double-blind, randomised, placebo-controlled, single-graded-dose, crossover study with five single-dose treatment periods. the washout period between doses was 15±2 days. for each of the five treatment periods, volunteers were to be admitted at the ufh on the day before the treatment day. on each treatment period, the pre-dose assessment were to be completed, bia 3-202/placebo was to be administered concomitantly with the dose of madopar® 125 and post-dose assessments were to be completed. subjects were discharged 30 h post-dose. subjects should attend five treatment periods and were to receive a different dose of bia 3-202 or placebo during each of these treatment periods.

Eligibility criteria:
inclusion criteria: * male and female subjects aged between 18 and 45 years, inclusive. * subjects of body mass index (bmi) between 19 and 28 kg/m2, inclusive. * subjects who were healthy as determined by pre study medical history, physical examination, and 12- lead ecg. * subjects who had clinical laboratory tests acceptable to the investigator. * subjects who were negative for hbsag, anti-hcv ab and hiv-1 and hiv-2 ab tests at screening. * subjects who were negative for drugs of abuse at screening and admission. * subjects who were non-smokers or who smoked less than 10 cigarettes or equivalent per day. * subjects who were able and willing to give written informed consent. * (if a woman) she was not of childbearing potential by reason of surgery or, if of childbearing potential, she used one of the following methods of contraception: double barrier, intrauterine device or abstinence. exclusion criteria: subjects who did not conform to the above inclusion criteria, or * subjects who had a clinically relevant history or presence of respiratory, gastrointestinal, renal, hepatic, haematological, lymphatic, neurological, cardiovascular, psychiatric, musculoskeletal, genitourinary, immunological, dermatological, connective tissue diseases or disorders. * subjects who had a clinically relevant surgical history. * subjects who had a clinically relevant family history. * subjects who had a history of relevant atopy. * subjects who had a history of relevant drug hypersensitivity. * subjects who had a history of alcoholism or drug abuse. * subjects who consumed more than 28 units of alcohol a week. * subjects who had a significant infection or known inflammatory process on screening and/or admission. * subjects who had acute gastrointestinal symptoms at the time of screening and/or admission (e.g., nausea, vomiting, diarrhoea, heartburn). * subjects who had an acute infection such as influenza at the time of screening and/or admission. * subjects who had used prescription drugs within 4 weeks of first dosing. * subjects who had used oral contraceptives or over the counter medication excluding oral routine vitamins but including mega dose vitamin therapy within one week of first dosing. * subjects who had used any investigational drug and/or participated in any clinical trial within 3 months of their first admission to the study. * subjects who had previously received bia 3-202. * subjects who had donated and/or received any blood or blood products within the previous 3 months prior to screening. * subjects who were vegetarians, vegans and/or had medical dietary restrictions. * subjects who could not communicate reliably with the investigator. * subjects who were unlikely to co-operate with the requirements of the study. * (if woman) she was pregnant or breast-feeding. * (if woman) she was at childbearing potential and she did not use an approved effective contraceptive method or she used oral contraceptives. * subjects who were unwilling or unable to give written informed consent.

Keywords: parkinson's disease nebicapone