Healthy
Conditions
Brief summary
The objective of this study was to obtain safety and tolerability data and first pharmacokinetic and pharmacodynamic data of escalating doses of ESR 1150 CL.
Interventions
DRUGESR 1150 CL
DRUGPlacebo
Sponsors
Boehringer Ingelheim
Study design
Allocation
RANDOMIZED
Intervention model
CROSSOVER
Primary purpose
TREATMENT
Masking
NONE
Eligibility
Sex/Gender
ALL
Age
18 Years to 50 Years
Healthy volunteers
Yes
Inclusion criteria
* Healthy male and female Caucasian subjects as determined by results of screening * Written informed consent in accordance with Good Clinical Practice and local legislation given * Age ≥ 18 and ≤ 50 years * Broca ≥ - 20 % and ≤ + 20 % * for first part of study: extensive metabolizers of CYP2D6 and/or spartein type; for second part of study: poor metabolizers of CYP2D6 and/or spartein
Exclusion criteria
* Any finding of the medical examination (including blood pressure, pulse rate and electrocardiogram) deviating from normal and of clinical relevance * Gastrointestinal, hepatic, renal, respiratory, cardiovascular, metabolic, immunological or hormonal disorders * Surgery of gastrointestinal tract (except appendectomy) * Diseases of the central nervous system (such as epilepsy) or psychiatric disorders of neurological disorders * History of 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) (≤ 1 month prior to administration or during the trial, except for oral contraceptives) * Use of any drugs which might influence the results of the trial (≤ 10 days prior to administration or during the trial except for oral contraceptives) * Participation in another trial with an investigational drug (≤ 2 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/days) * Drug abuse * Blood donation \> 100 ml (≤ 4 weeks prior to administration or during the trial) * Excessive physical activities (≤ 10 days prior to administration or during the trial) * Any laboratory value outside the reference range of clinical relevance * Females only: * No reliable contraception (examples of reliable contraception: oral contraceptives, 3-month injection, intrauterine device, sterilisation, condoms + spermicide) * pregnancy or breast feeding period
Design outcomes
Primary
| Measure | Time frame | Description |
|---|---|---|
| Number of patients with adverse events | up to 30 days | — |
| Area under the curve (AUC) | up to 24 hours after administration | — |
| Maximum concentration (Cmax) | up to 24 hours after administration | — |
| Time to maximum concentration (tmax) | up to 24 hours after administration | — |
| Apparent total plasma clearance (CLtot/f) | up to 24 hours after administration | — |
| Apparent volume of distribution (Vz/f) | up to 24 hours after administration | — |
| Elimination half-life (t1/2) | up to 24 hours after administration | — |
| Amount excreted in urine (Ae) | up to 24 hours after administration | — |
| Maximum flow rate (Qmax) | up to 8 hours after administration | assessed by free uroflowmetry |
| Average flow rate (Qave) | up to 8 hours after administration | assessed by free uroflowmetry |
| Voided volume (Vcomp) | up to 8 hours after administration | assessed by free uroflowmetry |
| Voiding time (T100) | up to 8 hours after administration | assessed by free uroflowmetry |
| Time to maximum flow (TQmax) | up to 8 hours after administration | assessed by free uroflowmetry |
| Residual urinary volume | up to 8 hours after administration | assessed by means of transabdominal ultrasound evaluation |
| Assessment of micturition pattern | up to 8 hours after administration | evaluated by Independent reviewer |
| Amount of inhibition constants (Ki) at α1A, adrenoreceptor subtype level | up to 8 hours after administration | assessed by ex vivo radioreceptor assay |
Outcome results
None listed