buprenorphine transdermal

Action and Spectrum

Actions and Spectrum:  

The action of buprenorphine is to bind to opioid receptors in the brain and spinal cord, which results in a reduction of pain perception. It is a partial agonist, meaning that it does not fully activate the receptors like other opioids such as morphine or fentanyl. This can make it a safer option for pain management as it has a lower risk of respiratory depression and other adverse effects. 

The spectrum of buprenorphine transdermal refers to the range of conditions that it can be used to treat. buprenorphine is typically used for the management of chronic pain, such as that caused by arthritis, cancer, or nerve damage. It may also be used in the treatment of opioid addiction, as it can help to reduce withdrawal symptoms and cravings. However, when used for addiction treatment, buprenorphine is usually administered in a different form, such as a tablet or film placed under the tongue. 

Drug Interaction

Adverse Reaction

Frequency defined 

Adults 

>10% 

Vomiting (11%) 

Pruritus at application site (15%) 

Nausea (23%) 

Constipation (14%) 

Somnolence (14%) 

Headache (16%) 

Dizziness (16%)  

1-10% 

Rash at application site (6%) 

Fatigue (5%) 

Hyperhidrosis (4%) 

Pruritus (4%) 

Falls (4%) 

Diarrhea (3%) 

Pain in extremity (3%) 

Insomnia (3%) 

Dyspnea (3%) 

Dyspepsia (3%) 

Urinary tract infection (3%) 

Back pain (3%) 

Joint swelling (3%) 

Hypoesthesia (2%) 

Black Box Warning

Black Box Warning:  

buprenorphine Transdermal is a prescription medication used to manage chronic pain in patients who require around-the-clock opioid treatment. However, it carries a black box warning due to its potential for abuse, addiction, and misuse. 

Overdose and death can result from the misuse, addiction, and abuse of buprenorphine transdermal. Patients who have a history of substance abuse, including alcohol abuse or addiction, are at a heightened risk of misusing and abusing this medication.

Taking higher doses than prescribed, obtaining the drug from illicit sources, or administering it via alternate routes (such as snorting or injecting) are other factors that can increase the risk of misuse or abuse. 

To prevent such risks, patients must be closely monitored for signs of misuse or abuse. These signs may include changes in mental status, respiratory depression, or circulatory collapse. If any of these symptoms appear, immediate medical attention should be sought. 

Contraindication / Caution

Contraindication/Caution:  

Hypersensitivity: Individuals who have a known hypersensitivity or allergy to buprenorphine or any of its components should not use this medication. 

Respiratory depression: buprenorphine transdermal can cause respiratory depression, particularly in individuals who have pre-existing respiratory conditions or who are taking other medications that depress the respiratory system. Therefore, it is contraindicated in individuals with severe respiratory insufficiency, severe asthma, or respiratory depression. 

Acute or severe bronchial asthma: buprenorphine transdermal should not be used in individuals with acute or severe bronchial asthma or hypercapnia.  

Paralytic ileus: buprenorphine transdermal is contraindicated in individuals with paralytic ileus, which causes the intestines to stop functioning properly.  

Liver failure: buprenorphine is metabolized in the liver, and individuals with severe hepatic impairment or liver failure should not use buprenorphine transdermal.  

Children: buprenorphine transdermal is not recommended for use in children under 18 years of age. 

Pregnancy / Lactation

Pregnancy warnings:     

Pregnancy category: N/A 

Lactation: Excreted into human milk is unknown 

Pregnancy Categories:         

Category A: Studies that were well-controlled and met expectations revealed no risk to the fetus in 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: buprenorphine is a potent analgesic drug that is commonly used in the treatment of moderate to severe pain, as well as for the management of opioid dependence. Buprenorphine can be administered through several routes, including transdermal patches. 

Pharmacodynamics: 

The pharmacodynamics mechanism of buprenorphine transdermal involves its ability to bind to and activate opioid receptors and its sustained release profile. These actions contribute to its analgesic effects and safety profile in treating chronic pain. 

MOA:  

The mechanism of action of buprenorphine involves binding to the mu-opioid receptors in the central nervous system, which results in a decrease in pain sensation. Buprenorphine also has partial agonist activity at the kappa-opioid receptors, which contributes to its analgesic effects. 

Pharmacokinetics:  

Absorption:  

buprenorphine Transdermal patches are designed to release the drug through the skin into the bloodstream. The absorption of buprenorphine through the skin is slow and steady, which leads to a constant concentration of the drug in the blood over time. The absorption rate is affected by the integrity of the skin, the patch formulation, and the site of application. 

Distribution:  

After absorption, buprenorphine is distributed throughout the body, primarily in the liver and brain. Buprenorphine has a high protein binding capacity, which means that it binds strongly to plasma proteins and has a low volume of distribution.  

Metabolism:  

buprenorphine is metabolized in the liver by the cytochrome P450 enzyme system, primarily CYP3A4 and CYP2C8. The metabolites of buprenorphine are primarily excreted in the urine, and the main metabolite is norbuprenorphine. 

Excretion and elimination:  

buprenorphine and its metabolites are excreted primarily in the urine, with a small amount excreted in the feces. The elimination half-life of buprenorphine is approximately 20-73 hours, depending on the individual and the dose. 

Adminstartion

Administration:  

Before administering buprenorphine transdermal, the patient’s medical history should be evaluated to ensure that it is an appropriate treatment option for them. It is important to consider any previous reactions to opioids or other medications, as well as any underlying medical conditions. 

buprenorphine transdermal patches come in different strengths. The healthcare provider should determine the appropriate strength based on the patient’s current opioid use and pain level. 

To use the patch, choose a clean, dry, and hair-free spot on your upper arm, chest, back, or side. 

 To prevent skin irritation or damage, alternate the site of application each time you apply a new patch. 

Each patch should remain on the skin for 7 days. If a patch falls off before the 7 days are up, replace it with a new one right away.  

The patient should not cut or alter the patch in any way. 

The patient should avoid exposing the patch to excessive heat or direct sunlight, as this may affect the medication’s effectiveness. 

If the patient experiences any side effects, such as dizziness, nausea, or respiratory depression, they should seek medical attention immediately.  

When discontinuing buprenorphine transdermal, the patch should be removed gradually to avoid withdrawal symptoms. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: buprenorphine transdermal 

Why do we use buprenorphine transdermal?   

buprenorphine transdermal patches are used to manage pain in people who require continuous, around-the-clock pain relief. Buprenorphine is an opioid medication that works by binding to certain receptors in the brain and nervous system to reduce pain. 

The transdermal delivery system provides a constant and controlled release of the medication over a 7-day period. This eliminates the need for frequent dosing, which can be a significant benefit for people with chronic pain. Additionally, transdermal delivery avoids the first-pass metabolism that occurs with oral medications, which can lead to unpredictable and variable effects. 

buprenorphine transdermal patches are also used in the treatment of opioid addiction. In this case, the medication is used to help reduce cravings and withdrawal symptoms in people who are trying to stop using opioids. The transdermal delivery system provides a consistent and reliable dose of buprenorphine, which can help people manage their addiction and prevent relapse.