buprenorphine subdermal implant

Action and Spectrum

Actions and Spectrum: 

The mu-opioid receptors in the brain and central nervous system are basically what the buprenorphine subdermal implant does when it works. Compared to complete opioid agonists like morphine, partial agonists like buprenorphine have reduced intrinsic activity, which results in less euphoria and respiratory depression. Instead, it creates a ceiling effect that restricts its impact on breathing and lowers the risk of overdose. 

The range of diseases that the buprenorphine subdermal implant can be used to address is referred to as its therapeutic spectrum. buprenorphine is used to treat chronic pain, opioid dependency, and the withdrawal symptoms connected to opioid addiction. 

Drug Interaction

Adverse Reaction

Frequency defined  

1-10% 

Fatigue (3%) 

Pyrexia (3%) 

Pain (4%) 

Dyspnea (1%) 

Skin lesion (1%) 

Laceration (3%) 

Asthenia (2%) 

Chills (2%) 

Dizziness (4%) 

Implant-site hemorrhage (7%) 

Vomiting (6%) 

Depression (6%) 

Sedation (1%) 

Paraesthesia (1%) 

Nausea (6%) 

Flatulence (1%) 

Toothache (5%) 

Implant-site erythema (10%) 

Cough (3%) 

Migraine (2%) 

Excoriation (2%) 

Oropharyngeal pain (5%) 

Rash (2%) 

Scratch (1%) 

Somnolence (3%) 

Upper abdominal pain (3%) 

Implant-site edema (5%) 

Chest pain (1%) 

Local swelling (1%) 

Constipation (6%) 

Implant-site hematoma (7%) 

>10% 

Implant-site pain (13%) 

Implant-site pruritus (12%) 

Headache (13%) 

Black Box Warning

Black Box Warning 

According to the buprenorphine subdermal implant’s black box warning, the drug has the potential to induce fatal overdose and other significant side effects, especially in people who are not already tolerant to opioids. 

Contraindication / Caution

Contraindication/Caution: 

Contraindication: 

• Intolerance to buprenorphine or any of the implant’s components 
• hypercarbia or acute or severe bronchial asthma 
• using drugs that depress the central nervous system, such as monoamine oxidase inhibitors 

Caution: 

• respiratory depression, especially in patients not yet accustomed to opioids 
• Particularly in people with compromised heart function, hypotension 
• buprenorphine is metabolised in the liver, causing hepatic impairment. 
• buprenorphine may accumulate in people with severe renal impairment due to renal impairment. 
• buprenorphine can cross the placenta and is secreted in breast milk during pregnancy and breastfeeding. 

Pregnancy / Lactation

Pregnancy warnings:     

Pregnancy category: N/A 

Lactation: Excretion into human milk is known (at low levels) 

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 lack of studies on pregnant women and no evidence of risk to the foetus 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 available 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 

Over the course of several months, the subdermal implant offers a steady release of buprenorphine. Diffusion, in which the drug molecules move through the implant matrix and into the surrounding tissue, is how the medication is released from the implant. 

Pharmacodynamics 

The interaction of buprenorphine subdermal implant with the mu-opioid receptor and other receptor systems in the central nervous system constitutes its pharmacodynamics. 

buprenorphine has a ceiling effect on respiratory depression and analgesia because it is a partial agonist at the mu-opioid receptor. This means that at greater doses, it only slightly intensifies its effects. This makes it a less dangerous option than full agonists like morphine or oxycodone for the treatment of opioid dependency and chronic pain. 

Pharmacokinetics 

Absorption  

A sustained-release formulation called buprenorphine subdermal implant is placed beneath the skin. Over the course of several months, the implant distributes buprenorphine, maintaining a constant medicine level in the blood. Diffusion is the process by which medication molecules are absorbed; they do this by moving through the implant matrix and into the surrounding tissue. 

Distribution 

Due to its high lipophilicity, buprenorphine has a strong affinity for fat tissue. Additionally, it is found in the brain and central nervous system as well as other parts of the body. buprenorphine’s subdermal implant formulation makes it possible for stable blood levels of the medicine, which reduces swings in drug levels. 

Metabolism 

buprenorphine is metabolised in the liver largely by the CYP3A4 enzyme, with CYP2C8 and CYP2C19 playing a smaller role. The metabolites are subsequently eliminated by urine. 

Elimination and excretion 

buprenorphine and its metabolites are eliminated in the urine, with a negligible quantity also passing via the feces. buprenorphine has an elimination half-life of between 24 and 42 hours, depending on the method of administration and the patient’s metabolic rate. 

Adminstartion

Administration:  

The implant is placed under the skin through a small incision made in the upper arm during the implantation surgery. The surgery is carried out in a hospital setting and lasts between 15 to 30 minutes. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: buprenorphine subdermal implant 

Why do we use buprenorphine subdermal implant? 

A drug called buprenorphine subdermal implant is used to treat chronic pain and opioid dependence.  

Adults who started therapy with a transmucosal buprenorphine-containing medication can treat their opioid dependence with a buprenorphine subdermal implant.  

The use of buprenorphine subdermal implants for the management of chronic pain is also recommended for patients who need constant, round-the-clock opioid therapy and for whom other forms of treatment are insufficient.