What is Buprenorphine Drug?

Buprenorphine, the active ingredient in Suboxone and Subutex, is a partially analgesic opioid used to treat opioid use disorder, acute pain, and chronic pain. It is preferred that the formulation of buprenorphine medications contains naloxone as it helps reduce انسحاب symptoms.

It was approved for clinical use in October 2002 by the Food and Drug Administration (FDA) and is currently scheduled as a schedule III drug which means that it has a moderate to low potential for physical and psychological dependence. The drug is also sold under several other trade names in different countries including Cizdol, Brixadi, Ubsolv, Bunavail, and Buvidal. It comes in different forms and can be used:

  • Under the tongue (sublingual)
  • In the cheek (buccal)
  • By injection (intravenous)
  • As a skin patch (transdermal)
  • As an implant

 

Buprenorphine Depression

The drug was invented in the 1960s and was put to human trial in 1971. In 1978, buprenorphine was launched in the UK as an injection to treat severe pain from serious injuries or severe illnesses. It now regarded as the leading medication for the treatment of opioid dependency. Buprenorphine has a remarkably high potency. It is 30 to 70 times more potent than Morphine, a powerful Opioid, and when used as a patch, it can be 100 times more potent. This means that it stays in the body for a long time. Another positive characteristic is that Buprenorphine creates ceiling effects when taken in high doses. A drug ceiling effect refers to the dose beyond which there is no additional analgesic effect. This leads to lower chances of overdose.

The action mechanism of buprenorphine is complex and involves several processes. Firstly, it displaces other opioids from the receptors they occupy in the brain. Then, it binds tightly to the receptors it emptied preventing other opioids from binding to them again. Buprenorphine is an opioid partial agonist. This implies that similar to other opioids, it creates effects such as respiratory depression. With buprenorphine, however, these effects are weaker than those of full drugs such as heroin and methadone.

 

Non-medical use and side effects of Buprenorphine

Since it is an opioid, Buprenorphine can also produce a euphoric sensation which has led to it being used non medically and for recreational purposes. The International Narcotics Control Board reported there has been an 80% increase in drug abuse in Georgia since 2003, an increase it attributes to the spreading availability of illegally imported Subutex. Thousands of pills are being snapped up by so-called doctor shoppers, in countries where the drug is legal, who then sell them on to the black market. And as mentioned above, Medicines such as Subutex can lead to abuse and dependency.

39 percent of patients treated in Georgian detox centers were treated for Subutex misuse in 2005, up from 29% in 2004. Abuse of Buprenorphine can lead to dangerous consequences. Even when taken as prescribed some minor side effects can arise. These include: Common side effects of buprenorphine include:

  • Constipation, headache, nausea, and vomiting
  • دوخة
  • Drowsiness and fatigue
  • التعرق
  • Dry mouth
  • Muscle aches and cramps
  • Inability to sleep
  • Fever
  • Blurred vision or dilated pupils
  • الارتعاش
  • الخفقان
  • Disturbance in attention

In cases of abuse the effects can be more adverse :

  • Respiratory distress
  • Overdose
  • Adrenal insufficiency
  • Dependence
  • Withdrawal
  • Itching, pain, swelling, and nerve damage (implant)

 

Buprenorphine Withdrawal

Dependence can occur when the drug is taken for longer than intended or in higher doses than prescribed. The dependent person will develop a compulsive need to take the drug even if not needed. As dependency increases, tolerance is developed and the desired effects become weak. As a result, the user will increase the dose. This raises the chances of an overdose, yet as mentioned the ceiling effect can lower the rates of such incidents. In cases of overdose the following symptoms can be seen : 

  • التخدير
  • تباطأ التنفس
  • غيبوبة
  • Fainting
  • Cold, clammy skin
  • Extreme weakness
  • Hypotension

 

Buprenorphine and Alcohol

In more severe overdoses such as an overdose on Buprenorphine mixed with another drug or alcohol, the symptoms can worsen. The side effects of such overdose include:

  • Seizures or convulsions
  • Yellowing eyes or skin
  • Dark urine
  • Stomach pain or cramps
  • Unusual or increased sweating
  • Slow heartbeat
  • ضغط دم منخفض
  • Nausea or vomiting
  • Severe drowsiness
  • Severe confusion
  • Severe dizziness
  • Severe nervousness

In nearly all deadly overdose cases, the overdose was caused by mixing buprenorphine with other drugs. According to a study, ED visits involving buprenorphine increased considerably from an approximated 3,161 in 2005 to 30,135 visits in 2010. The increased availability of the drug is said to have caused this increase. Buprenorphine-related ED visits involving nonmedical use increased 255% from 2006 to 2010, with 4,440 visits to 15,778 visits, respectively. In 2010, 52% (15,778 visits) of buprenorphine-related ED visits were classified as recreational uses of the drug.

 

Buprenorphine Treatment

A person with an opioid dependency will also experience withdrawal symptoms if they quit using the drug abruptly.

Abuse of Opioids can be very dangerous and even fatal. Although Buprenorphine is one of the safer Opioids, it is not completely harmless. If you need help with Opioids dependency and recovery, have a look at our موقع الكتروني.

 

المراجع

Roberts, James R. MD Buprenorphine: Toxicity and Overdose, Emergency Medicine News: January 2009 – Volume 31 – Issue 1 – p 7-10

DOI: 10.1097/01.EEM.0000343552.62943.49 

Srivastava, A., Kahan, M., Njoroge, I., & Sommer, L. Z. (2019). Buprenorphine in the emergency department: Randomized clinical controlled trial of clonidine versus buprenorphine for the treatment of opioid withdrawal. Canadian family physician Medecin de famille canadien, 65(5), e214–e220.

https://www.samhsa.gov/data/sites/default/files/DAWN106/DAWN106/sr106-buprenorphine.htm

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https://www.webmd.com/drugs/2/drug-64748/buprenorphine-hcl-sublingual/details

“Buprenorphine Hydrochloride”. drugs.com. American Society of Health-System Pharmacists. 26 January 2017. Retrieved 17 March 2017.

“Buprenorphine Hydrochloride”. drugs.com. American Society of Health-System Pharmacists. 26 January 2017. Retrieved 17 March 2017.

“Buprenorphine Hydrochloride”. drugs.com. American Society of Health-System Pharmacists. 26 January 2017. Retrieved 17 March 2017.

Cote J, Montgomery L (July 2014). “Sublingual buprenorphine as an analgesic in chronic pain: a systematic review”. Pain Medicine. 15 (7): 1171–8. دوى:10.1111/pme.12386بميد 24995716.

Budd K, Raffa RB. (eds.) Buprenorphine – The unique opioid analgesic. Thieme, 200, رقم ISBN 3-13-134211-0

“IMPORTANT SAFETY INFORMATION”. Archived from the original on 18 March 2019. Retrieved 25 June 2016.