bupivacaine implant

Action and Spectrum

Actions and Spectrum: 

Action: 

Local Anesthetic Action: Bupivacaine works by blocking nerve signals in the area where it’s applied. It inhibits the influx of sodium ions through specific sodium channels in nerve membranes, thereby preventing the generation and conduction of nerve impulses. This action results in temporary numbness and loss of sensation in the targeted area. 

Extended Pain Relief: Bupivacaine implants are formulated to release the medication slowly and steadily over a prolonged duration, providing sustained pain relief. This sustained release helps in managing pain over an extended period, potentially reducing the need for frequent re-administration of the drug. 

Spectrum: 

Pain Management: The range of bupivacaine’s effects encompasses its ability to effectively alleviate different forms of pain, such as postoperative pain, chronic pain conditions, and specific nerve-related pain syndromes. By delivering a controlled dose of the anesthetic directly to the site of action, these implants aim to minimize discomfort and improve the patient’s quality of life. 

Drug Interaction

Adverse Reaction

Frequency defined  

>10% 

Incision site swelling (14.6%) 

1-10% 

Oral hypoesthesia (2.2%) 

Pyrexia (2.4%) 

Scrotal swelling (2.9%) 

Seroma (2.9%) 

Blurred vision (3.6%) 

Tremor (3.6%) 

Headache (4.1%) 

Postprocedural discharge (4.9%) 

Dysgeusia (7.5%) 

Black Box Warning

Black Box Warning:  

None

Contraindication / Caution

Contraindication/Caution:  

Allergy or hypersensitivity: People with a known allergy or hypersensitivity to bupivacaine or any components of the implant should avoid using it. 

Local infection: Implantation of bupivacaine devices should be avoided in the presence of active local infections at the implantation site due to the risk of exacerbation or spread of the infection. 

Bleeding disorders: Patients with bleeding disorders or those taking anticoagulant medications may have an increased risk of bleeding or hematoma formation at the implantation site. 

Neurological disorders: Pre-existing neurological disorders or conditions may pose risks when using bupivacaine implants. For instance, patients with pre-existing neurological deficits or spinal cord injuries might have increased susceptibility to neurotoxicity. 

Septicemia: Patients with systemic infections, particularly those with septicemia, should avoid implantation of bupivacaine devices due to the potential for worsening the systemic infection. 

Pregnancy and lactation: The use of bupivacaine implants during pregnancy or lactation should be carefully considered due to possible hazards to the developing child or nursing newborn. The safety of bupivacaine in pregnancy is not well-established. 

Pregnancy / Lactation

Pregnancy warnings:     

Pregnancy category: N/A 

Lactation: Excreted into human milk is known 

Pregnancy Categories:         

Category A: Studies that were well-controlled and met expectations revealed no risk to the fetus in either the first or second trimester. 

Category B: There were a lack of studies on pregnant women and no evidence of risk to the fetus in animal experiments.   

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: There is no data available for the drug under this category

Pharmacology

Pharmacology: Bupivacaine belongs to a class of local anesthesia. 

Pharmacodynamics:  

Bupivacaine blocks sodium channels in nerve membranes, inhibiting the generation and conduction of nerve impulses. This blockade prevents the initiation and transmission of nerve impulses, leading to local anesthesia. 

Pharmacokinetics: 

Absorption 

The peak plasma time is achieved within three hours; the range of peak plasma concentration is 663 ng/ml. 

Distribution 

The rate of bound protein is 95 percent ,the drug crosses the placenta through the process of passive diffusion. 

Metabolism 

The drug’s metabolism mainly occurs in the liver through conjugation with glucuronic acid. The metabolite formed is pipecoloxylidine. 

Excretion & Elimination 

The half-life duration is 19 hours, and the excretion is mainly through kidneys through unchanged 6%. 

Adminstartion

Administration:  

Patient Evaluation: Before the procedure, the patient’s medical history, current medications, allergies, and any previous adverse reactions to anesthetics are assessed. This evaluation helps determine the patient’s suitability for bupivacaine implantation. 

Preparation: The area where the implant will be placed is sterilized to minimize the risk of infection. The patient may be given local anesthesia or sedation to ensure comfort during the procedure. 

Implantation Procedure: The bupivacaine implant, which typically comes in the form of a biodegradable matrix or device containing the medication, is surgically placed under the skin or in a specific tissue location where pain management is required. Surgeons or trained healthcare professionals perform this procedure using specialized tools and techniques. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: bupivacaine implant 

Why do we use bupivacaine implant?  

Bupivacaine implants are often used after surgical procedures to manage postoperative pain. The implant slowly releases bupivacaine, providing continuous pain relief at the site of surgery for several days. 

In orthopedic surgeries such as joint replacement or spinal procedures, bupivacaine implants can be placed directly into the surgical site to manage pain during the critical initial recovery period. 

For certain chronic pain conditions, such as severe back pain or neuropathic pain, bupivacaine implants may be used to provide longer-lasting relief compared to traditional local anesthetic injections.