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Day/night rhythms in the uptake and elimination of the antibiotic Levofloxaci

Conditions
The circadian variation in the relative contribution of intestinal uptake and renal elimination of levofloxacin
Therapeutic area: Body processes [G] - Physiological processes [G07]
Registration Number
EUCTR2013-001976-39-NL
Lead Sponsor
Centre for Human Drug Research
Brief Summary

Not available

Detailed Description

Not available

Recruitment & Eligibility

Status
Authorised-recruitment may be ongoing or finished
Sex
Male
Target Recruitment
Not specified
Inclusion Criteria

1.Healthy male subjects (Caucasians), 18 to 50 years of age, inclusive. Health status is defined by absence of evidence of any active or chronic disease following a detailed medical and surgical history, a complete physical examination including vital signs, 12-lead ECG, haematology, blood chemistry, and urinalysis.
2.Body mass index (BMI) between 18 and 30 kg/m2, inclusive, and with a minimum weight of 50 kg.
3.Regular bedtimes (between 23:00 and 24:00h) and wake-up times (between 07:00 and 08:00) from one week prior to the study.
4.Ability to communicate well with the investigator in the Dutch language.
5.Ability to participate and willing to give written informed consent and to comply with the study restrictions.

Are the trial subjects under 18? no
Number of subjects for this age range:
F.1.2 Adults (18-64 years) yes
F.1.2.1 Number of subjects for this age range 12
F.1.3 Elderly (>=65 years) no
F.1.3.1 Number of subjects for this age range

Exclusion Criteria

1.History of clinically significant haematologic, renal, hepatic, cardiovascular, neurologic, endocrinal, oncologic, pulmonary, immunologic, or psychiatric disorders;
2.Positive for hepatitis B, C or Human Immunodeficiency Virus (HIV);
3.Positive drug screen result (i.e. positive for cocaine, opiates, amphetamine, cannabis and/or benzodiazepines) at screening and before drug administration;
4.Positive alcohol breath test result at screening or before drug administration;
5.Systolic blood pressure (SBP) greater than 140 or less than 90 mm Hg, and diastolic blood pressure (DBP) greater than 90 or less than 50 mm Hg;
6.Any of the following findings in the resting ECG:
a.Screening or baseline ECG with QRS and/or T wave judged to be unfavourable for a consistently accurate QT measurement (e.g., neuromuscular artefact that cannot be readily eliminated, arrhythmias, indistinct QRS onset, low amplitude T wave, merged T- and U-waves, prominent U waves);
b.QTcB> 450 or < 300 msec at screening or baseline visit;
7.Use of prescription medication within 2 weeks prior to drug administration;
8.Use of over-the-counter medication (including homeopathic medicines and vitamins) within 3 days prior to Day 1. An exception is paracetamol (up to 4 g/day). Other exceptions will only be made if the rationale is discussed and clearly documented by the Investigator.
9.History of seizures or any disorder that predispose to seizures;
10.Personal or family history of congenital long QT syndrome or sudden death;
11.History of clinically significant allergies, including relevant drug hypersensitivity or allergy;
12.Presence or history of alcoholism or drug abuse;
13.Use of more than 21 units of alcohol per week;
14.Use of more than 8 units of caffeine per day;
15.Smoking (subjects had to be non-smokers for at least 90 days preceding Screening);
16.Transmeridian flights or shift work within a month prior to the start of the study;
17.Extreme morning and evening types (determined by the Horne-Ostberg Morningness/Eveningness Questionnaire).
18.Participation in another clinical trial within 3 months prior to the start of this study or more than 4 times a year;
19.Loss of blood over 500 mL within 3 months prior to screening;
20.Unsuitable to participate in the study for any reason in the opinion of the PI.

Study & Design

Study Type
Interventional clinical trial of medicinal product
Study Design
Not specified
Primary Outcome Measures
NameTimeMethod
Main Objective: To evaluate diurnal variation of the pharmacokinetics of Levofloxacin;Secondary Objective: To explore the daily variation in the magnitude of QT interval prolongation by Levofloxacin;Primary end point(s): The main PK parameters (Cmax, Tmax, t1/2, Vd, fu, CL and F) will be determined at each of the 6 experimental time points in order to establish their variation during the 24hr period. <br> ;Timepoint(s) of evaluation of this end point: Levofloxacin blood samples are taken on each of the six study days at t=0, 30, 60, 90, 120, 150, 180, 240, 300, 360, 480, 600, 720min after administration
Secondary Outcome Measures
NameTimeMethod
Secondary end point(s): The effect of levofloxacin on QT-interval will be determined at each of the 6 experimental time points in order to establish their variation during the 24hr period.;Timepoint(s) of evaluation of this end point: ECGs are recorded at t=0, 30, 60, 90, 120, 150, 180, 240, 360, 480, 720min
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