Healthy
Conditions
Brief summary
To assess the steady state pharmacokinetics of Desipramine with/without concomitant administration of Crobenetine.
Interventions
DRUGDesipramine tablet
DRUGCrobenetine infusion
DRUGPlacebo infusion
Sponsors
Boehringer Ingelheim
Study design
Allocation
RANDOMIZED
Intervention model
CROSSOVER
Primary purpose
TREATMENT
Masking
SINGLE
Eligibility
Sex/Gender
MALE
Age
21 Years to 50 Years
Healthy volunteers
Yes
Inclusion criteria
All participants in the study should be healthy males, range from 21 to 50 years of age and their bodymass index (BMI) be within 18.5 to 29.9 kg/m2. In accordance with Good Clinical Practice and local legislation all volunteers will have given their written informed consent prior to admission to the study.
Exclusion criteria
* Any finding of the medical examination (including blood pressure, pulse rate and ECG) deviating from normal and of clinical relevance * Gastrointestinal, hepatic, renal, respiratory, cardiovascular, metabolic, immunological or hormonal disorders * Diseases of the central nervous system (such as epilepsy) or psychiatric disorders or neurological disorders * History of relevant orthostatic hypotension, fainting spells or blackouts * Chronic or relevant acute infections * History of allergy/hypersensitivity (including drug allergy) which is deemed relevant to the trial as judged by the investigator * Intake of drugs with a long half-life (\> 24 hours) within at least one month or less than ten half-lives of the respective drug before enrolment in the study * Use of any drugs which might influence the results of the trial (within one week prior to administration or during the trial) * Participation in another trial with an investigational drug (within two months prior to administration or during the trial) * Smoker (\> 10 cigarettes or \> 3 cigars or \> 3 pipes/day) * Inability to refrain from smoking on trial days * Alcohol abuse (\> 60 g/day) * Drug abuse * Blood donation (\>= 100 mL within four weeks prior to administration or during the trial) * Excessive physical activities (within the last week before the study) * Any laboratory value outside the reference range of clinical relevance * Cytochrome P450 2D6 poor metaboliser (to be determined by phenotyping or genotyping)
Design outcomes
Primary
| Measure | Time frame |
|---|---|
| Area under the concentration time curve for desipramine at steady state (AUC,ss) | up to 168 hours after start of drug administration |
| Maximum plasma concentration of desipramine at steady state (Cmax,ss) | up to 168 hours after start of drug administration |
Secondary
| Measure | Time frame | Description |
|---|---|---|
| Area under the concentration time curve from zero time extrapolated to infinity(AUC0-infinity) | up to 168 hours after start of drug administration | — |
| Time to reach maximum concentration of desipramine at steady state (tmax,ss) | up to 168 hours after start of drug administration | — |
| Apparent terminal rate constant (λz) | up to 168 hours after start of drug administration | — |
| Apparent terminal half-live in plasma (t1/2) | up to 168 hours after start of drug administration | — |
| Mean residence time (MRT) | up to 168 hours after start of drug administration | — |
| Total clearance (CL) | up to 168 hours after start of drug administration | — |
| Individual time courses of plasma concentrations | up to 168 hours after start of drug administration | — |
| Observed concentration of crobenetine (C,h) | 1 and 6 hours after start of infusion | — |
| Number of subjects with adverse events | up to 8 days after last drug administration | — |
| Number of subjects with clinically significant findings in vital signs | up to 8 days after last drug administration | blood pressure, pulse rate |
| Number of subjects with clinically significant findings in 12-lead ECG | up to 8 days after last drug administration | — |
| Number of subjects with clinically significant findings in laboratory tests | up to 8 days after last drug administration | — |
| Apparent volume of distribution (V) | up to 168 hours after start of drug administration | — |
| Area under the concentration time curve from zero time to time of last quantifiable drug concentration (AUC0-tz) | up to 168 hours after start of drug administration | — |
Outcome results
None listed