Drug intelligence / Profile preview

tramadol + ropivacaine

Development stage
Unknown
Lead developer
Grünenthal
Modality
Small Molecules
Administration
Epidural, Perineural
01

Overview

A combination of tramadol, a centrally acting analgesic with weak μ-opioid receptor agonist properties and serotonin/norepinephrine reuptake inhibition, and ropivacaine, a long-acting amide local anesthetic. This combination is used in regional anesthesia techniques such as brachial plexus blocks and epidural analgesia to provide enhanced and prolonged pain relief with reduced need for additional opioids. ## Pharmacology Tramadol is a centrally acting analgesic with a dual mechanism of action: it acts as a weak μ-opioid receptor agonist and inhibits the reuptake of serotonin and norepinephrine[1][3]. When combined with ropivacaine, a long-acting amide local anesthetic, the combination provides synergistic analgesic effects. Ropivacaine works by blocking sodium channels in neuronal membranes, preventing the propagation of pain signals[5][6]. It is commonly used for regional anesthesia and acute pain management[6][8]. ## Clinical Applications The tramadol-ropivacaine combination has been studied in various clinical settings: - **Interscalene Brachial Plexus Block**: Adding 100 mg of tramadol to 40 mL of 0.5% ropivacaine improves the onset time and duration of sensory block while reducing morphine consumption during the first 24 hours after shoulder surgery[1][2]. - **Epidural Analgesia**: The combination is used for postoperative pain management in lower abdominal surgeries, with studies comparing different doses of tramadol (50 mg vs 100 mg) combined with ropivacaine[4][5]. ## Advantages The tramadol-ropivacaine combination offers several benefits: 1. **Enhanced Analgesia**: The combination provides more effective pain relief than either agent alone due to their complementary mechanisms[5]. 2. **Reduced Opioid Consumption**: Patients receiving this combination typically require less additional opioid medication postoperatively[1][2]. 3. **Prolonged Duration of Action**: The addition of tramadol extends the duration of sensory block provided by ropivacaine[1][2]. 4. **Improved Hemodynamic Stability**: Higher doses of tramadol (100 mg) with ropivacaine have shown better hemodynamic stability in some studies[4]. ## Side Effects Common side effects include shivering, headache, nausea, and vomiting, though these are generally not significantly different from those seen with ropivacaine alone[4]. The combination may also cause sedation, particularly at higher tramadol doses[4]. It's worth noting that tramadol use carries risks of seizures and serotonin syndrome, especially when used with other serotonergic medications[3]. Additionally, ropivacaine and tramadol can increase the risk of CNS depression when used together[3].

02

Targets

DOR (Opioid Receptor Delta 1)σR (Sigma receptors)MOR (Mu opioid receptor)NaV (Voltage-gated sodium channels)KOR (Kappa opioid receptor)NET (Norepinephrine Transporter)SERT (Sodium-dependent serotonin transporter)

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