buprenorphine

medtigo

buprenorphine

Brand Name :

Buprenex

Synonyms :

buprenorphine

Class :

Opioid Analgesics; Analgesics, Opioid Partial Agonist

Action and Spectrum

Actions and Spectrum:

Actions:

Pain Management: buprenorphine is used to manage moderate to severe pain. It works by binding to specific receptors in the brain and spinal cord (mu-opioid receptors), which reduces the perception of pain.

Opioid Dependence Treatment: buprenorphine is also used in the treatment of opioid dependence, as it can help to reduce withdrawal symptoms and cravings in individuals who are addicted to opioids. buprenorphine works by binding to the mu-opioid receptors, which reduces the effects of other opioids and can help to prevent withdrawal symptoms.

Spectrum:

Opioid Receptor Affinity: buprenorphine has a high affinity for the mu-opioid receptors, which allows it to bind strongly to these receptors and produce its effects.

Partial Agonist Properties: buprenorphine is a partial agonist, meaning that it activates the mu-opioid receptors to a lesser extent than full agonist opioids, such as morphine. This reduced activation helps to reduce the risk of respiratory depression (shallow breathing) and overdose, which are major concerns with full agonist opioids.

Ceiling Effect: buprenorphine also has a ceiling effect, meaning that its effects will reach a maximum point and then stop increasing, even with higher doses. This helps to reduce the risk of overdose, as the effects of the drug will not increase beyond a certain point, even with higher doses.

Dosing & Uses

Drug Interaction

Adverse Reaction

Frequency Defined

10%:

Headache (29.1-30%)

Withdrawal syndrome (18.4-22%)

Pain (18.4-24%)

Insomnia (21.4%)

Back pain (7.8-14%)

Nausea (10-13.6%)

Sweating (12-12.6%)

Infection (11.7%)

Constipation (7.8-11%)

Asthenia (14%)

Infection (20%)

Abdominal pain (11.7%)

1-10%:

Rhinitis (9.7%)

Chills (6-7.8%)

Flu syndrome (6%)

Nervousness (6%)

Diarrhea (4.9-5%)

Asthenia (4.9%)

Fever (3%)

Dyspepsia (3%)

Vomiting (5-7.8%)

Runny eyes (5%)

Accidental injury (2-3%)

Abscess (2%)

Vasodilation (3.9%)

<1%:

Dyspnea

Constipation

Pruritis

Psychosis

Urinary retention

Tinnitus

Tremor

Pallor

Flatulence

Dyspepsia

Apnea

Black Box Warning

Black Box Warning:

The Food and Drug Administration (FDA) has implemented a Risk Evaluation and Mitigation Strategy (REMS) for opioid analgesics to help ensure that the benefits of these drugs for pain management outweigh the risks associated with addiction, abuse, and misuse. The REMS program was established as a response to the opioid epidemic in the United States and aims to improve the safe use of these medications.

Contraindication / Caution

Contraindication/Caution:

Contraindications:

Allergic reactions: buprenorphine should not be used in individuals who have previously had an allergic reaction to buprenorphine or any of its ingredients.

Respiratory depression: buprenorphine should not be used in individuals with severe respiratory depression, as it may worsen their breathing.

Acute pain: buprenorphine should not be used for the treatment of acute pain, as it is not a suitable medication for this type of pain.

Alcohol or sedative withdrawal: buprenorphine should not be used in individuals undergoing alcohol or sedative withdrawal, as it may worsen their symptoms.

Cautions:

Pregnancy: buprenorphine should be used with caution in pregnant women, as it may cause harm to the fetus. Women taking buprenorphine should use effective contraception to prevent pregnancy.

Liver or kidney disease: buprenorphine should be used with caution in individuals with liver or kidney disease, as it may cause additional strain on these organs.

Depression: buprenorphine may cause depression or worsen pre-existing depression. Patients taking buprenorphine should inform their healthcare provider if they experience symptoms of depression.

Interactions with other medications: buprenorphine may interact with other medications, including benzodiazepines, alcohol, and other opioids. Patients taking buprenorphine should inform their healthcare provider about all the medications they are taking.

Pregnancy / Lactation

Pregnancy consideration:

Limited data available regarding the use in pregnant women.

Breastfeeding warnings:

The developmental and health benefits of both infant and mother should be considered.

Pregnancy category:

Category A: well-controlled and satisfactory studies do not show risk to the fetus in the first/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 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: No data is available for the drug under this category.

Pharmacology

Pharmacology:

buprenorphine is a partial opioid agonist that is used in the treatment of opioid addiction and chronic pain. It works by binding to the mu-opioid receptors in the brain, which are the same receptors that are targeted by full opioid agonists such as morphine and fentanyl.

Pharmacodynamics:

Opioid agonism: buprenorphine is a partial agonist at the mu-opioid receptors, which means it activates these receptors to produce a certain level of pain relief, but it does not activate them to the same extent as a full opioid agonist. This results in a lower risk of overdose, respiratory depression, and addiction compared to full opioid agonists.

Ceiling effect: buprenorphine has a ceiling effect, which means that as the dose of the drug increases, its effects will plateau, and further increases in the dose will not produce a proportionate increase in effects. This reduces the risk of overdose and toxicity associated with buprenorphine use.

Pharmacokinetics:

Absorption:

buprenorphine is absorbed well following sublingual (under the tongue) administration and intramuscular injection.

Distribution:

buprenorphine distributes throughout the body, including the brain and other organs.

Metabolism:

buprenorphine is metabolized in the liver by the cytochrome P450 system, and its metabolites are excreted in the urine.

Half-life:

buprenorphine has a long half-life, which allows for once-daily dosing in most patients

Adminstartion

Administration:

Sublingual administration:

buprenorphine sublingual tablets or films are placed under the tongue and allowed to dissolve.
This form of administration is used for the treatment of opioid addiction and provides rapid onset of action within 15-30 minutes.
The sublingual form is the most used form of buprenorphine and is the safest and most effective form of the medication.

Transdermal administration:

buprenorphine transdermal patches are applied to the skin and deliver the medication through the skin and into the bloodstream over a period of 72 hours.
This form of administration is used for the treatment of chronic pain and provides a steady, continuous level of buprenorphine in the bloodstream.
The transdermal form is less commonly used than the sublingual form, as it may cause skin irritation and other side effects.

Intramuscular injection:

buprenorphine intramuscular injections are given into a muscle, typically in the upper arm or thigh.
This form of administration is used for the treatment of severe pain and provides rapid onset of action within 5-10 minutes.
The intramuscular form is less commonly used than the sublingual form, as it may cause local pain and discomfort at the injection site.

Patient Information Leaflet

Patient information leaflet

Generic Name: buprenorphine

Pronounced: BUE-pre-NOR-feen

Why do we use buprenorphine?

Opioid Addiction: buprenorphine is used as part of a comprehensive treatment program for individuals with opioid addiction. When used as directed, it can help to reduce cravings, prevent withdrawal symptoms, and improve overall functioning.

Chronic Pain: buprenorphine is used for the treatment of chronic pain, such as low back pain, osteoarthritis, or chronic pain from cancer. It works by reducing pain and improving quality of life for patients who have not responded to other pain medications.

Pain Management: buprenorphine is used for the management of pain in the hospital or pre-operative setting. It can be used alone or in combination with other medications to provide pain relief for patients undergoing surgery or other medical procedures.

Neonatal Abstinence Syndrome: buprenorphine is used to treat neonatal abstinence syndrome (NAS), a condition that affects new-borns exposed to opioids in utero. NAS can cause symptoms such as tremors, seizures, and excessive crying, and buprenorphine can help to reduce these symptoms and improve the health of affected new-borns.

buprenorphine

No data available for drug.

DRUG INTERACTION

buprenorphine

&

buprenorphine +

Contraindicated

Serious Use Alternative

Monitor Closely

Minor

buprenorphine

No data available for drug.

DRUG INTERACTION

buprenorphine

&

buprenorphine +

Contraindicated

Serious Use Alternative

Monitor Closely

Minor

medtigo

buprenorphine

Brand Name :

Synonyms :

Class :

Action and Spectrum

Dosing & Uses

Drug Interaction

Adverse Reaction

Black Box Warning

Contraindication / Caution

Pregnancy / Lactation

Pharmacology

Adminstartion

Patient Information Leaflet

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