bupivacaine liposome

Action and Spectrum

Actions and Spectrum: 

Actions: 

bupivacaine is a potent local anesthetic that blocks nerve impulses at the administration site. It achieves this by inhibiting the flow of sodium ions into nerve cells, leading to the temporary loss of sensation in the affected area. The liposomal formulation of bupivacaine allows for a slow and controlled drug release over an extended period. This sustained release enables bupivacaine to provide pain relief for up to 72 hours or more, compared to the shorter duration of action seen with conventional bupivacaine. 

Spectrum: 

bupivacaine liposomal is indicated for local analgesia, typically in surgical settings, to manage postoperative pain. It infiltrates the surgical site or specific nerve blocks to relieve pain in the immediate postoperative period. 

bupivacaine liposomal’s spectrum of activity is specific to the area where it is administered, and its effectiveness is primarily limited to local anesthesia at the site of injection or infiltration. It is not used for systemic pain relief or general anesthesia. 

Drug Interaction

Adverse Reaction

Frequency defined 

1-10%  

Hemorrhage (1-3%) 

Severe hemorrhage (3%) 

Anemia (3%) 

Injection site mass (4%) 

Wound secretion (4%) 

Deep thrombophlebitis (2%) 

Allergic reaction (2%) 

Nausea (2%) 

<1% 

Leg edema 

Fever 

Decreased hemoglobin 

Major hemorrhage 

Hypotension 

Hematuria 

Vomiting 

Impaired healing 

Dizziness 

Epistaxis 

Cerebrovascular disorder 

Hematuria 

Leg edema 

Leg pain 

Hematemesis 

Black Box Warning

Black Box Warning: 

None. 

Contraindication / Caution

Contraindication/Caution: 

Contraindications: 

• Hypersensitivity 
• Intravenous regional anesthesia 

Cautions: 

• Cardiovascular effects 
• Neurologic effects 
• Drug interactions 
• Pregnancy  
• Lactation 
• Children 
• Elderly

Pregnancy / Lactation

Pregnancy consideration:  

No data is available. 

Breastfeeding warnings:  

No data is available. 

Pregnancy category: 

• Category A: well-controlled and Satisfactory studies do not show fetal risks in the first or later trimester.        
• Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women. 
• Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.       
• Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.        
• Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.        
• Category N: No data for the drug under this category is available. 

Pharmacology

Pharmacology: 

bupivacaine is an amide-type local anesthetic that blocks nerve impulses in the affected area. It achieves this by inhibiting the influx of sodium ions through voltage-gated sodium channels in nerve cell membranes, thereby preventing the generation and conduction of nerve signals.   

Pharmacodynamics: 

bupivacaine liposomal is indicated explicitly for postoperative pain management. After surgical procedures, local infiltration or nerve blocks with bupivacaine liposomal can provide prolonged pain relief, which can be crucial for patients during their recovery.  

As with other local anesthetics, bupivacaine liposomal may have neurological effects. It is essential to carefully administer the drug to avoid injecting it directly into nerves or neural tissue to minimize the risk of nerve injury, neurotoxicity, or neuropathy. 

Pharmacokinetics: 

Absorption 

bupivacaine liposomal is administered via local infiltration at the surgical site or as peripheral nerve blocks. The liposomal formulation allows for slow and controlled drug release over an extended period, resulting in prolonged local anesthesia. The drug is slowly absorbed from the injection site.

The distribution 

of bupivacaine primarily remains localized at the administration site, as it is intended for local anesthesia. The liposomal formulation helps limit systemic absorption, reducing the risk of systemic toxicity.  

Metabolism 

bupivacaine is metabolized in the liver by the cytochrome P450 enzymes, mainly CYP3A4 and CYP1A2, into inactive metabolites. 

Elimination and Excretion 

The metabolites of bupivacaine and a small amount of unchanged drug are excreted primarily in the urine. 

Adminstartion

Administration: 

bupivacaine liposomal (EXPAREL) is administered through local infiltration or peripheral nerve blocks by healthcare professionals. It intends explicitly for postoperative pain management to provide extended pain relief after surgical procedures.

Patient Information Leaflet

Patient information leaflet 

Generic Name:  bupivacaine liposome 

Pronounced as: bue-PIV-a-kane-LYE-poe-some 

Why do we use bupivacaine liposome? 

bupivacaine liposomal provides extended pain relief compared to conventional bupivacaine. While conventional bupivacaine typically offers local anesthesia for a few hours, bupivacaine liposomal can relieve pain for up to 72 hours or more. This prolonged duration of action is beneficial during the postoperative recovery period, allowing patients to experience reduced pain and discomfort for an extended period.