PharmacokineticsPhase 4NCT01214941
Effect of Itraconazole and Ticlopidine on the Pharmacokinetics and Pharmacodynamics of Oral Tramadol
A Phase 4 study testing Ticlopidine and Ticlopidine and itraconazole in people with Pharmacokinetics and Pharmacodynamics, run by Turku University Hospital at 1 site in Finland.
Trial summary
Tramadol is an opioid analgesic, which is widely used in the treatment of acute and neuropathic pain. After oral administration, tramadol is rapidly and almost completely absorbed. Tramadol is extensively metabolised by O- and N-demethylation, which are catalysed by the liver CYP-450 enzymes. Read more about this study
- Who is it for?
- Ages 18 to 40 yearsHealthy volunteers can take part
- Conditions the study is for
- Pharmacokinetics, Pharmacodynamics
- What is being tested?
- Ticlopidine and Ticlopidine and itraconazole
- Type of treatment
- Pill or oral medicine
- Could I receive a placebo?
- Yes, some participants may receive a placebo
- How many people
- 12 participants
- Where
- 1 siteFinland
- Study dates
- Sep 2010to Dec 2010
- Phase
- Phase 4
- Are there results?
- None posted in the registry
Key requirements
Who can take part, as listed by the sponsor. Only the study team can confirm whether you are eligible, so take this list to your doctor.
- Ages 18 to 40 years
- All sexes
- Healthy volunteers accepted
- Adult
Who may be able to join
- Healthy volunteers
- Age 18-40
- Body weight within ±15% of the ideal weight for height
Who cannot join
- A previous history of intolerance to the study drugs or to related compounds and additives
- Concomitant drug therapy of any kind for at least 14 days prior to the study
- Existing or recent significant disease
- History of hematological, endocrine, metabolic or gastrointestinal disease, including gut motility disorders
- History of asthma or any kind of drug allergy
- Previous or present alcoholism, drug abuse, psychological or other emotional problems that are likely to invalidate informed consent, or limit the ability of the subject to comply with the protocol requirements
Show all 14Show fewer
- A positive test result for urine toxicology
- A "yes" answer to any one of the Abuse Questions
- Pregnancy or nursing
- Donation of blood for 4 weeks prior and during the study
- Special diet or life style conditions which would compromise the conditions of the study or interpretation of the results
- Participation in any other studies involving investigational or marketed drug products concomitantly or within one month prior to the entry into this study
- Smoking for one month before the start of the study and during the whole study period
- Any history of coagulation abnormality, also in first degree relatives
Trial locations and contacts
1 site in 1 country.
Finland1 site
Department of Anaesthesiology, Intensive Care, Emergency Care and Pain Medicine, Turku University and Turku University Hospital
Turku, 20521
About this study
Tramadol is an opioid analgesic, which is widely used in the treatment of acute and neuropathic pain. After oral administration, tramadol is rapidly and almost completely absorbed. Tramadol is extensively metabolised by O- and N-demethylation, which are catalysed by the liver CYP-450 enzymes. O-desmethyltramadol is an active metabolite and its formation is catalysed by CYP2D6. The formation of inactive metabolites is catalysed by CYP3A4 and 2B6. This study is aimed to investigate the possible interaction of oral tramadol with itraconazole and ticlopidine, which are inhibitors of CYP3A4 and 2B6. Twelve healthy male or female adult non-smoking volunteers aged 18-40 years with body weights within ±15% of the ideal weight for height are taken into the study. Primary endpoints of the study are plasma concentrations of tramadol and its metabolites.
- Conditions
- Pharmacokinetics, Pharmacodynamics
- Being tested
- Placebo, Ticlopidine, Ticlopidine and itraconazole
What participants receive
What participants receive. In a randomised study each person is assigned to one group by chance.
PlaceboDrug
The subjects will be given orally placebo twice a day for 5 days prior to the study.
TiclopidineDrug
The subjects will be given orally ticlopidine 250mg twice a day for 5 days prior to the study.
Ticlopidine and itraconazoleDrug
The subjects will be given orally ticlopidine 250mg twice a day and itraconazole 200mg as a single daily dose for 5 days prior to the study.
| Study group | Role | What they receive |
|---|---|---|
| Placebo | Placebo comparator | Not described Receives: Drug: Placebo |
| Ticlopidine | Active comparator | Not described Receives: Drug: Ticlopidine |
| Ticlopidine and itraconazole | Active comparator | Not described Receives: Drug: Ticlopidine and itraconazole |
What is being measured
The primary outcome is the main question the study is designed to answer.
Concentration of tramadol and its metabolites in plasma
Measured: 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12, 24, 48 hours after administration of tramadol
Secondary outcomes (4)
Metabolites of tramadol in urine
Urine will be collected for 24 hours and M1 and M2 metabolites of tramadol are quantified from 0-12h and 12-24h fractions
Measured: 0-12 and 12-24 hour fractions after administration of tramadol
Serotonin concentrations
Serotonin concentrations will be analyzed with chromatographical methods from the blood samples drawn 0, 4 and 8 hours after tramadol administration
Measured: 0, 4 and 8 hours after tramadol administration
Pharmacodynamic effects
The psychomotor effects of tramadol will be assessed with the measurement of pupil size with Cogan's pupillometer, Maddox wing test and digit symbol substitution test
Measured: 1, 2, 3, 4, 5, 6, 8, 10, 12 hours after administration of tramadol
Analgesia
The analgesic effect of tramadol will be evaluated using the cold pressor test. Briefly, the subject's hand is immersed into ice-cold water of + 4° C up to the wrist. The subject is told to keep his or her hand in the water and to report when the cold sensation becomes painful. Cold pain threshold is defined as the latency from the immersion of the hand to the subject's first report of pain. Cold pain intensity is assessed at 30 s intervals following immersion of the hand in cold water for up to 60s . A verbal numerical rating scale of 0-100 will be used.
Measured: 1, 2, 3, 4, 5, 6, 8, 10, 12 hours after the administration of tramadol
Timeline
From the start of the study to its completion; the mark is today. Estimated dates are the sponsor’s plan.
- First posted5 Oct 2010 (estimated)
- Study startSep 2010
- Primary completionDec 2010
- Study completionDec 2010
Resources
- Official record on ClinicalTrials.govThe registry entry this page is built from, with its full change history.
- Publications (1)Papers the sponsor has linked to this study.
- Other trials for PharmacokineticsStudies of the same condition, open and under way.
- More trials run by Turku University HospitalThe sponsor's other registered studies.
- What the trial phases meanHow a treatment moves from first tests in people to approval.
More details
For doctors and researchers: how the study is designed, who runs it, and its registry IDs.
Study design
- Study type
- Interventional
- Phase
- Phase 4
- Primary purpose
- Basic science
- Allocation
- Randomised
- Intervention model
- Crossover
- Masking
- Single blind
- Who is masked
- Participant
- Enrolment
- 12 participants (actual)
Sponsor and investigators
- Lead sponsor
- Turku University Hospital
- Sponsor type
- Other government
- Investigators
- Klaus T Olkkola, MD, PhD, Prof, Principal investigator, Turku University Hospital and Turku University
IDs, dates and publications
- ClinicalTrials.gov ID
- NCT01214941
- Sponsor's protocol ID
- 54/180/2010
- Other IDs
- 2010-020617-82
- Status last verified
- Oct 2010
- First submitted
- 4 Oct 2010
- Last updated
- 13 Apr 2011
- Results posted
- No
- Data monitoring committee
- No
Publications
Hagelberg NM, Saarikoski T, Saari TI, Neuvonen M, Neuvonen PJ, Turpeinen M, Scheinin M, Laine K, Olkkola KT. Ticlopidine inhibits both O-demethylation and renal clearance of tramadol, increasing the exposure to it, but itraconazole has no marked effect on the ticlopidine-tramadol interaction. Eur J Clin Pharmacol. 2013 Apr;69(4):867-75. doi: 10.1007/s00228-012-1433-0. Epub 2012 Oct 26.
PubMed 23099620
Study at a glance
From the registry record, last updated by the sponsor on 13 Apr 2011. Recruitment status is as the sponsor reported it: confirm with the study team.
- Official title
- Effect of Itraconazole and Ticlopidine on the Pharmacokinetics and Pharmacodynamics of Oral Tramadol
- ClinicalTrials.gov ID
- NCT01214941
- Acronym / sponsor ID
- 54/180/2010
- Conditions
- Pharmacokinetics, Pharmacodynamics
- Phase
- Phase 4
- Study type
- Interventional
- Recruitment status
- Completed
- Enrolment
- 12 participants (actual)
- Lead sponsor
- Turku University HospitalOther government
- Study start
- Sep 2010
- Primary completion
- Dec 2010 (actual)
- Study completion
- Dec 2010 (actual)
- First posted
- 5 Oct 2010 (estimated)
- Results
- Not posted in the source record
Clinical summary
The research question as the sponsor registered it. This describes what the study plans to test, not what it found.
Tramadol is an opioid analgesic, which is widely used in the treatment of acute and neuropathic pain. After oral administration, tramadol is rapidly and almost completely absorbed. Tramadol is extensively metabolised by O- and N-demethylation, which are catalysed by the liver CYP-450 enzymes. O-desmethyltramadol is an active metabolite and its formation is catalysed by CYP2D6. The formation of inactive metabolites is catalysed by CYP3A4 and 2B6. This study is aimed to investigate the possible interaction of oral tramadol with itraconazole and ticlopidine, which are inhibitors of CYP3A4 and 2B6. Twelve healthy male or female adult non-smoking volunteers aged 18-40 years with body weights within ±15% of the ideal weight for height are taken into the study. Primary endpoints of the study are plasma concentrations of tramadol and its metabolites.
Study design
- Primary purpose
- Basic science
- Allocation
- Randomised
- Intervention model
- Crossover
- Masking
- Single blind (participant)
- Number of arms
- 3
| Arm | Type | Receives |
|---|---|---|
| Placebo | Placebo comparator | Drug: Placebo |
| Ticlopidine | Active comparator | Drug: Ticlopidine |
| Ticlopidine and itraconazole | Active comparator | Drug: Ticlopidine and itraconazole |
Who may qualify
- Ages
- 18 to 40 years
- Sex
- All
- Healthy volunteers
- Accepted
- Age groups
- Adult
Key inclusion criteria (3 listed)
- Healthy volunteers
- Age 18-40
- Body weight within ±15% of the ideal weight for height
Key exclusion criteria (14 listed)
- A previous history of intolerance to the study drugs or to related compounds and additives
- Concomitant drug therapy of any kind for at least 14 days prior to the study
- Existing or recent significant disease
- History of hematological, endocrine, metabolic or gastrointestinal disease, including gut motility disorders
- History of asthma or any kind of drug allergy
Eligibility is decided by the study team after screening; this overview does not establish that a patient qualifies. Full inclusion and exclusion criteria.
Interventions
| Intervention | Type | Arms |
|---|---|---|
| PlaceboThe subjects will be given orally placebo twice a day for 5 days prior to the study. | Drug | Placebo |
| TiclopidineThe subjects will be given orally ticlopidine 250mg twice a day for 5 days prior to the study. | Drug | Ticlopidine |
| Ticlopidine and itraconazoleThe subjects will be given orally ticlopidine 250mg twice a day and itraconazole 200mg as a single daily dose for 5 days prior to the study. | Drug | Ticlopidine and itraconazole |
Primary outcome
Concentration of tramadol and its metabolites in plasma
Time frame: 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12, 24, 48 hours after administration of tramadol
4 secondary outcomes
Metabolites of tramadol in urine
Time frame: 0-12 and 12-24 hour fractions after administration of tramadol
Serotonin concentrations
Time frame: 0, 4 and 8 hours after tramadol administration
Pharmacodynamic effects
Time frame: 1, 2, 3, 4, 5, 6, 8, 10, 12 hours after administration of tramadol
Analgesia
Time frame: 1, 2, 3, 4, 5, 6, 8, 10, 12 hours after the administration of tramadol
Results and safety
The study is completed, but results are not available in the source record. That does not mean the treatment did or did not work.
Research links
- Official record on ClinicalTrials.govLast updated by the sponsor 13 Apr 2011.
- Derived from this study: PubMed 23099620Hagelberg NM, Saarikoski T, Saari TI, Neuvonen M, Neuvonen PJ, Turpeinen M, Scheinin M, Laine K, Olkkola KT. Ticlopidine inhibits both O-demethylation and renal clearance of tramadol, increasing the exposure to it, but itraconazole has no marked effect on the ticlopidine-tramadol interaction. Eur J Clin Pharmacol. 2013 Apr;69(4):867-75. doi: 10.1007/s00228-012-1433-0. Epub 2012 Oct 26.
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Referral and contact
AzTrials does not enrol participants or take referrals. Contact the study team or a site listed below; they decide who can take part. This study is not recruiting at the moment.
Klaus T Olkkola, MD, PhD, Prof principal investigator
Turku University Hospital and Turku University
1 site in 1 country: see every site and its status.
Questions about this trial
What is this clinical trial studying?
A Phase 4 study testing Ticlopidine and Ticlopidine and itraconazole in people with Pharmacokinetics and Pharmacodynamics, run by Turku University Hospital at 1 site in Finland.
The full registered description is in the About this study section and the official record.
Who may be eligible to take part?
The sponsor lists 3 inclusion and 14 exclusion criteria. Eligibility is decided by the study team after screening, so read the full criteria and contact a listed site.
Is this clinical trial currently recruiting?
The record says: finished, as of the sponsor's last update on 13 Apr 2011. Status can change between updates, so confirm with the study contact before making plans.
Where is the study taking place?
The record lists 1 site in Finland. Whether a site is taking part right now should be confirmed with that site. See every site.
What are the possible benefits and risks?
They depend on the study and the treatment, and no study can promise a benefit. Some participants in this study may receive a placebo. The study team explains the known risks during informed consent, before anyone joins; the record itself does not list them.
What does this phase mean?
Phase 4 studies take place after a treatment is approved, to learn more about its long-term benefits and risks in everyday use.
Not every study follows the same path, and some studies (observational studies, device studies) have no phase.
Are results available for this study?
The study is completed, but results are not available in the source record. That does not mean the treatment did or did not work.
How can a doctor refer a patient or contact the research team?
The record lists no contact. The official record names the sponsor, who can be asked directly. AzTrials does not enrol participants or take referrals.
What does the primary outcome measure?
Concentration of tramadol and its metabolites in plasma (time frame: 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12, 24, 48 hours after administration of tramadol). It is what the study was designed to measure, not a finding.
Where can I read the original study information?
On the ClinicalTrials.gov record for NCT01214941, which also lists 1 linked publication.
Does a listing mean the treatment is approved or proven to work?
No. A listing means the study is registered. It does not show that the treatment is safe, works, or is approved by a regulator.
How often is this information updated?
AzTrials copies changed records from ClinicalTrials.gov every night and reloads the whole registry every week. The sponsor last updated this record on 13 Apr 2011.