Drug intelligence / Profile preview

levobupivacaine + ketorolac + adrenaline

Development stage
Unknown
Lead developer
CellTech Group
Modality
Small Molecules
Administration
Local Infiltration, Periarticular, Subcutaneous
01

Overview

The drug combination "levobupivacaine + ketorolac + adrenaline" is a multimodal analgesic mixture used primarily for local infiltration analgesia (LIA) in surgical procedures, especially orthopedic surgeries like total knee arthroplasty. This combination leverages the complementary effects of each component to provide effective pain management. ## Composition and Properties This combination consists of three active ingredients: 1. **Levobupivacaine**: A long-acting local anesthetic that is the S(-)-enantiomer of bupivacaine, developed as a safer alternative with lower cardiotoxicity. It works by blocking neuronal voltage-sensitive sodium channels, preventing the transmission of nerve impulses[6]. 2. **Ketorolac**: A non-steroidal anti-inflammatory drug (NSAID) that provides additional analgesic effects through inhibition of prostaglandin synthesis. 3. **Adrenaline** (also known as epinephrine): A vasoconstrictor that prolongs the duration of anesthesia by reducing local blood flow and systemic absorption of the other components. ## Clinical Applications The combination is primarily used for: - Periarticular infiltration during total knee arthroplasty[2][3] - Local infiltration analgesia in various surgical procedures[5][7] - Postoperative pain management[5] In clinical practice, the mixture is typically prepared with specific dosages: - Levobupivacaine: 100-200 mg - Ketorolac: 30 mg - Adrenaline: 0.5 mg These components are usually diluted in normal saline to a final volume of 100 mL and administered at the surgical site[5]. ## Efficacy Studies have shown that this combination effectively reduces: - Postoperative pain scores - Opioid consumption - Length of hospital stay For example, in total knee arthroplasty, the mixture is typically injected at multiple sites including the posterior capsule, medial and lateral collateral ligaments, quadriceps tendon, patellar tendon, and surrounding soft tissues[5]. ## Administration The mixture is typically administered in three stages during surgery: 1. Before prosthesis cementation (posterior capsule) 2. After implantation (surrounding tissues) 3. Subcutaneous tissues before wound closure This staged approach ensures comprehensive coverage of pain-sensitive structures around the surgical site[5].

02

Targets

AR (Adrenergic receptors)PGHS-1 (Prostaglandin G/H Synthase 1)PTGS2 (Prostaglandin-Endoperoxide Synthase 2)NaV (Voltage-gated sodium channels)

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