Tramadol

Generic Name
Tramadol
Brand Names
Conzip, Durela, Qdolo, Ralivia, Ryzolt, Seglentis, Tridural, Ultracet, Ultram, Zytram
Drug Type
Small Molecule
Chemical Formula
C16H25NO2
CAS Number
27203-92-5
Unique Ingredient Identifier
39J1LGJ30J
Background

Tramadol is a centrally acting synthetic opioid analgesic and SNRI (serotonin/norepinephrine reuptake-inhibitor) that is structurally related to codeine and morphine. Due to its good tolerability profile and multimodal mechanism of action, tramadol is generally considered a lower-risk opioid option for the treatment of moderate to severe pain. It is considered a Step 2 option on the World Health Organization's pain ladder and has about 1/10th of the potency of morphine.

Tramadol differs from other traditional opioid medications in that it doesn't just act as a μ-opioid agonist, but also affects monoamines by modulating the effects of neurotransmitters involved in the modulation of pain such as serotonin and norepinpehrine which activate descending pain inhibitory pathways. Tramadol's effects on serotonin and norepinephrine mimic the effects of other SNRI antidepressants such as duloxetine and venlafaxine.

Tramadol exists as a racemic mixture consisting of two pharmacologically active enantiomers that both contribute to its analgesic property through different mechanisms and are also themselves metabolized into active metabolites: (+)-tramadol and its primary metabolite (+)-O-desmethyl-tramadol (M1) are agonists of the μ opioid receptor while (+)-tramadol inhibits serotonin reuptake and (-)-tramadol inhibits norepinephrine reuptake. These pathways are complementary and synergistic, improving tramadol's ability to modulate the perception of and response to pain.

Tramadol has also been shown to affect a number of other pain modulators within the central nervous system as well as non-neuronal inflammatory markers and immune mediators. Due to the broad spectrum of targets involved in pain and inflammation, it's not surprising that the evidence has shown that tramadol is effective for a number of pain types including neuropathic pain, post-operative pain, lower back pain, as well as pain associated with labour, osteoarthritis, fibromyalgia, and cancer. Due to its SNRI activity, tramadol also has anxiolytic, antidepressant, and anti-shivering effects which are all frequently found as comorbidities with pain.

Similar to other opioid medications, tramadol poses a risk for development of tolerance, dependence and abuse. If used in higher doses, or with other opioids, there is a dose-related risk of overdose, respiratory depression, and death. However, unlike other opioid medications, tramadol use also carries a risk of seizure and serotonin syndrome, particularly if used with other serotonergic medications.

Indication

Tramadol is approved for the management of moderate to severe pain in adults.

Tramadol is also used off-label in the treatment of premature ejaculation.

Associated Conditions
Acute Pain, Premature Ejaculation, Severe Pain, Acute, moderate, severe Pain, Moderate Pain
Associated Therapies
-

Method of Pre-treatment for Application of QUTENZA Capsaicin 8% Patch

First Posted Date
2011-08-12
Last Posted Date
2018-04-23
Lead Sponsor
Astellas Pharma Inc
Target Recruit Count
122
Registration Number
NCT01416116
Locations
🇧🇪

Site 102, Antwerpen, Belgium

🇧🇪

Site 103, Genk, Belgium

🇧🇪

Site 101, Roeselare, Belgium

and more 17 locations

Analgesic Effect of Different Combinations of Dexketoprofen Trometamol With Tramadol Hydrochloride in a Model of Moderate to Severe Pain

First Posted Date
2011-03-02
Last Posted Date
2013-08-12
Lead Sponsor
Menarini Group
Target Recruit Count
745
Registration Number
NCT01307020
Locations
🇩🇪

Klinik für Mund-, Kiefer- und Gesichtschirurgie, Universitätsklinikum Schleswig Holstein, Campus Kiel, Kiel, Schleswig-Holstein, Germany

🇮🇹

Centro di Ricerche Cliniche di Verona Srl. Policlinico G.B.Rossi, Verona, Italy

🇬🇧

University Dental School Manchester, Manchester, England, United Kingdom

and more 13 locations

The Effects of Three Oral Medications on Post-operative Pain Following Endodontic Treatment

Phase 1
Completed
Conditions
First Posted Date
2010-08-10
Last Posted Date
2010-08-10
Lead Sponsor
Azad University of Medical Sciences
Registration Number
NCT01178203

Efficacy, Safety, Tolerability and Pharmacokinetics of Concomitant Administration of Tramadol With Duloxetine or Pregabalin

First Posted Date
2010-05-05
Last Posted Date
2013-05-31
Lead Sponsor
Turku University Hospital
Registration Number
NCT01116531
Locations
🇫🇮

Department of Anaesthesiology, Intensive Care, Emergency Care and Pain Medicine, Turku University and Turku University Hospital, Turku, Finland

Study to Evaluate Efficacy and Safety in Male Subjects With Premature Ejaculation

First Posted Date
2009-09-24
Last Posted Date
2012-08-27
Lead Sponsor
Bausch Health Americas, Inc.
Target Recruit Count
1050
Registration Number
NCT00983736
Locations
🇧🇬

MHAT Plovdiv, Plovdiv, Bulgaria

🇷🇴

Spitalul Clinic de Urgenta Militar Central "Dr. Carol Davila", Bucuresti, Romania

🇨🇿

Psychiatricke Oddeienf and Sexuologicka Ambulance, Pardubice, Czech Republic

and more 44 locations

Development of Cocktail for Measuring the Activity of Important Cytochrome P450 Enzymes

First Posted Date
2009-09-22
Last Posted Date
2010-06-28
Lead Sponsor
University of Southern Denmark
Target Recruit Count
412
Registration Number
NCT00981929
Locations
🇩🇰

University of Southern Denmark, Clinical Pharmacology, Odense, Fyn, Denmark

Efficacy of Extended Release Tramadol for Treating Prescription Opioid Withdrawal

Phase 2
Completed
Conditions
Interventions
First Posted Date
2009-09-18
Last Posted Date
2017-04-05
Lead Sponsor
Michelle Lofwall
Target Recruit Count
53
Registration Number
NCT00980044
Locations
🇺🇸

University of Kentucky, Lexington, Kentucky, United States

Comparative Bioavailability Between Two Tramadol Formulations: Study of the Better Controlled Release of a New 200 mg Once A Day (OAD) Formulation Versus Zytram® 200 mg

Phase 1
Completed
Conditions
Interventions
First Posted Date
2009-06-02
Last Posted Date
2012-04-27
Lead Sponsor
Labopharm Inc.
Target Recruit Count
26
Registration Number
NCT00911742

A Study to Compare the Relative Bioavailability of Two 200 Mg Tramadol Hydrochloride Tablet Products Under Fasting Conditions

Phase 1
Completed
Conditions
Interventions
First Posted Date
2009-02-03
Last Posted Date
2012-04-30
Lead Sponsor
Labopharm Inc.
Target Recruit Count
26
Registration Number
NCT00834366
© Copyright 2024. All Rights Reserved by MedPath