GABAergic Modulation in Pain Transmission in Human: Effect of the GABAA Agonist Clobazam on Peripheral and Central Sensitisation

• Status: Completed
• Trial end date: 2011-11-01
• Target enrollment: 0
• Participant gender: Male

Summary

In animal, the GABAergic system modulates central sensitisation, which is a key phenomenon in pain processing. The development of GABAA agonists targeting the subunits of the GABAA receptor implicated in nociception, but not the subunit implicated in sedation is attractive as it opens new perspectives of testing the role of GABAergic modulation of pain processing in human volunteers. The purpose of this subproject is to test the effect of the specific α2 and α3 agonist but sparing α1 effect TPA023 on a human model of peripheral and central sensitisation and to correlate its pharmacodynamic effect with the pharmacokinetic of the compound.

The results would contribute to clarify the potential role of these α2/α3 agonist but sparing α1drugs in clinical pain conditions.

• Phase: Phase 1/Phase 2
• Accepts Healthy Volunteers?: Accepts Healthy Volunteers

Details

• Lead Sponsor: University Hospital, Geneva
• Treatments: Clobazam; Clonazepam; Tolterodine Tartrate

Criteria

Inclusion Criteria:

• Male subject, age between 18 and 60 year old

• Caucasian

• Type 3 skin phototype

• Non smoker or moderate smoker (< 10 cigarettes/day)

• No clinically abnormal findings on history and/or on physical examination

• Presence of an area of secondary hyperalgesia after UVB irradiation

Exclusion Criteria:

• Any concomitant illness

• Current or past history of drug and alcohol abuse or current intake of more than 3 glasses of alcohol a day or more than 21 glasses of alcohol per week

• Psychotropic drug intake during the last month

• Sun allergy or any skin disease

• Current and regular intake of any drugs that might affect nociception Paracetamol, or NSAIDS with a short half lives are permitted but should be stopped at least 48 h before the UVB session