SUBOXONE

 

DESCRIPTION / DEFINITIONS: Suboxone is a combination of three parts Buprenorphine to one part Naloxone. It is a prescription drug approved to help someone through the withdrawal symptoms when quitting opiates and opioids including methadone, heroin, prescription painkillers like morphine, oxycodone, and hydrocodone, and other similar drugs. It is also prescribed for pain.

ABUSE: Although Buprenorphine itself can be abused, the addition of Naloxone to Suboxone makes it difficult. See more information under Abuse.

ADDICTION / DEPENDENCE: As with other opiates and opioids, becoming dependant on or addicted to Suboxone is not uncommon. See more information below.

SIDE EFFECTS: The side effects of Suboxone can include: abdominal pain, anxiety, pain in the joints, abnormal physical weakness or lack of energy, low blood pressure, and infertility. See more complete list below.

WITHDRAWAL SYMPTOMS: Withdrawal symptoms can include abdominal cramps, agitation, anxiety, dehydration, insomnia, and vomiting. See more information below.

TREATMENT: Quitting Suboxone is best done in a medically-supervised detox program for safety and comfort. Call us to talk to a Detox Advisor.

 

DESCRIPTION / DEFINITIONS

Suboxone is a combination of three parts Buprenorphine to one part Naloxone. It is a prescription drug approved to help people though withdrawal from opiates and opioids, including heroin, prescription painkillers like morphine, oxycodone, hydrocodone, methadone, and other similar drugs. It is also prescribed for pain.

Buprenorphine was first approved by the Food and Drug Administration (FDA) as a lower-risk alternative to methadone in Medication- Assisted Treatment (MAT) of opioid abuse.

Buprenorphine is an opioid, but it’s basically not as strong as heroin, morphine, oxycodone, and other opioid drugs. It’s enough to prevent the person from having withdrawal symptoms, but not enough to get the person ‘high’. Some people say it makes them feel ‘normal’. The effects of Buprenorphine – such as sedation and respiratory depression also tend to plateau.

Nevertheless, Buprenorphine can be abused – primarily by liquefying and injecting it so someone can actually get the euphoria and other opioid effects.

That’s where the Naloxone, the second ingredient in Suboxone, comes into play. Naloxone – also known as Narcan, and used to reverse the effects of opioid overdose – blocks the effects that could be caused by the buprenorphine and immediately causes withdrawal symptoms.

Suboxone can be dangerous, as is covered in the Warnings and Precautions on the label.

WARNINGS AND PRECAUTIONS

  • Addiction, Abuse, and Misuse: Buprenorphine can be abused in a similar manner to other opioids. Monitor patients for conditions indicative of diversion or progression of opioid dependence and addictive behaviors. Multiple refills should not be prescribed early in treatment or without appropriate patient follow‐up visits.
  • Respiratory Depression: Life‐threatening respiratory depression and death have occurred in association with buprenorphine use. Warn patients of the potential danger of self‐administration of benzodiazepines or other CNS depressants while under treatment with SUBOXONE sublingual film, or both in situations of concomitant.
  • Unintentional Pediatric Exposure: Store SUBOXONE sublingual film safely out of the sight and reach of children. Buprenorphine can cause severe, possibly fatal, respiratory depression in children.
  • Neonatal Opioid Withdrawal Syndrome: Neonatal opioid withdrawal syndrome (NOWS) is an expected and treatable outcome of prolonged use of opioids during pregnancy.
  • Adrenal Insufficiency: If diagnosed, treat with physiologic replacement of corticosteroids, and wean patient off of the opioid.
  • Risk of Opioid Withdrawal with Abrupt Discontinuation: If treatment is temporarily interrupted or discontinued, monitor patients for withdrawal and treat appropriately.
  • Risk of Hepatitis, Hepatic Events: Monitor liver function tests prior to initiation and during treatment and evaluate suspected hepatic events.
  • Precipitation of Opioid Withdrawal Signs and Symptoms: An opioid withdrawal syndrome is likely to occur with parenteral misuse of SUBOXONE sublingual film by individuals physically dependent on full opioid agonists, or by sublingual or buccal administration before the agonist effects of other opioids have subsided.
  • Risk of Overdose in Opioid‐Naïve Patients: SUBOXONE sublingual film is not appropriate as an analgesic. There have been reported deaths of opioid naïve individuals who received a 2 mg sublingual dose.

 

ABUSE

Because Suboxone contains Buprenorphine, an opioid, some people may expect that if you take more of it, the effect will be greater – as it is with other opioids. The Naloxone helps prevent that and causes withdrawal symptoms, which could be dangerous.

 

ADDICTION / DEPENDENCE

One can become dependent on or addicted to Suboxone in an effort to continue to feel ‘normal’ and not go through the withdrawal symptoms one experiences when getting off opioids.

HALF LIFE AND METABOLISM
The biological half-life of a substance is the time it takes for a drug to lose half of its pharmacologic activity. This is significant because it affects how soon withdrawal symptoms may appear.

When Suboxone sublingual film is administered under the tongue or in the cheek, buprenorphine has a half-life ranging from 24 to 42 hours. Naloxone’s half life ranges from 2 to 12 hours.

Suboxone metabolism is mediated primarily by the CYP2D6 enzyme.

The CYP enzymes are the major enzymes involved in drug metabolism, and since many drugs may increase or decrease the activity of various CYP isozymes, this is a major source of adverse drug interactions, since changes in CYP enzyme activity may affect the metabolism and clearance of various drugs. For example, if one drug inhibits the CYP-mediated metabolism of another drug, the second drug may accumulate within the body to toxic levels, possibly causing an overdose.

Naloxone is metabolized in the liver, primarily by glucuronide conjugation. Naloxone-3-glucoronide as the major metabolite.

OPIOID INDUCED HYPERALGESIA
When you’ve taken Suboxone – or other opioids or opioid-containing drugs – for an extended period of time, six months or so, the body can become more sensitive to pain. If you’re using Suboxone for pain relief, you may find the pain eventually becomes worse and is no longer relieved by taking Suboxone. This is a sign that you are experiencing Opioid-Induced Hyperalgesia.

 

SIDE EFFECTS

Because the Buprenorphine in Suboxone does not act as strongly on the body as other opioids such as oxycodone, hydrocodone, heroin, methadone, Lorcet, and Norco, among others, the side effects tend to be less severe than with the full agonists if taken at the recommended dose for a short period of time.

However, the side effects can still be severe and medically dangerous since many factors other than the drug itself can come into play. These include one’s age and health, which other drugs are being taken and for how long and at what dosage, how you react to the Suboxone and withdrawal, and your specific metabolism.

They can also be more severe if Suboxone is abused. Side effects include:

  • abdominal pain
  • abscess
  • adrenal insufficiency – a potentially life-threatening condition which may include non‐specific symptoms and signs including nausea, vomiting, anorexia, fatigue, weakness, dizziness, and low blood pressure.
  • allergic reaction – you may have a rash, hives, swelling of the face, wheezing, or a loss of blood pressure and consciousness
  • anaphylaxis – an acute allergic reaction that prompts the immune system to respond. The symptoms can include: fainting, lightheadedness, low blood pressure, dizziness, flushing, difficulty breathing, rapid breathing, shortness of breath, wheezing, hives, swelling under the skin, blue skin from poor circulation, rashes, nausea, vomiting, fast heart rate, feeling of impending doom, itching, tongue swelling, difficulty swallowing, facial swelling, mental confusion, nasal congestion, or impaired voice.
  • androgen deficiency – with chronic use, lower levels of male sex hormones, particularly testosterone, than is needed for health. This may cause hot flashes, sweating, insomnia, nervousness, irritability, tiredness, loss of motivation, short-term memory problems, declining self-esteem, depression, decreased energy levels, diminished muscle strength, decline or loss of libido or sexual desire, poor erections, reduced orgasmic quality, reduced volume of semen, diminished muscle mass, hair loss, abdominal obesity, reduction in high-density lipoprotein (HDL) cholesterol, an increase in total body fat, and osteoporosis that may manifest as low libido, impotence, erectile dysfunction, amenorrhea, or infertility.
  • anxiety
  • arthralgia – pain in the joints
  • asthenia – abnormal physical weakness or lack of energy
  • back pain
  • blistering and ulceration of the mouth or tongue
  • blurred vision
  • chills
  • cold sweat
  • constipation
  • cough increase
  • hepatitis – symptoms range from inflamed or injured liver cells that leak liver enzymes to reports of death, liver failure, hepatic necrosis (an acute, toxic injury to the liver), hepatorenal syndrome (the liver gradually loses ability to function, eventually leading to liver failure), and hepatic encephalopathy (a disorder caused by a buildup of toxins in the brain that can happen with advanced liver disease. It affects a lot of things, like your behavior, mood, speech, sleep, or the way you move.)
  • low blood pressure. You may feel dizzy if you get up too fast from sitting or lying down.
  • dependency
  • depression
  • diarrhea
  • loss of attention or focus
  • dizziness
  • drug withdrawal syndrome
  • dyspepsia – indigestion
  • erythema – superficial reddening of the skin, usually in patches
  • fainting
  • fever
  • flu syndrome
  • glossitis – inflammation of the tongue
  • glossodynia – a sore or burning tongue
  • headache
  • hyperhidrosis-excessive sweating
  • hypersensitivity reactions – to buprenorphine, naloxone, or both. The symptoms could be rashes, hives, and pruritus (severe itching) or bronchospasm (spasm of bronchial smooth muscle, leading to wheezing or shortness of breath), angioneurotic edema (an area of swelling in the lower layer of skin and tissue just under the skin or mucous membranes. Other symptoms may include stomach cramping and discolored patches or rash on the hands, arms, and feet, swollen throat, hoarseness, and difficulty breathing), and anaphylactic shock (an acute allergic reaction that prompts the immune system to respond. The symptoms can include: fainting, lightheadedness, low blood pressure, dizziness, flushing, difficulty breathing, rapid breathing, shortness of breath, wheezing, hives, swelling under the skin, blue skin from poor circulation, rashes, nausea, vomiting, fast heart rate, feeling of impending doom, itching, tongue swelling, difficulty swallowing, facial swelling, mental confusion, nasal congestion, or impaired voice.).
  • impairment of ability to drive or operate machinery
  • infection
  • infertility
  • injury accidental
  • insomnia
  • intoxication (feeling lightheaded or drunk)
  • irregular heart beat (palpitations)
  • irritability
  • watery eyes
  • liver problems – symptoms can include your skin or the white part of your eyes turning yellow (jaundice), urine turning dark, stools turning light in color, decreased appetite, stomach, pain, or nausea.
  • may obscure the diagnosis of patients with acute abdominal conditions
  • nausea
  • nervousness
  • numb mouth
  • opioid withdrawal – this can include: shaking, sweating more than normal, feeling hot or cold more than normal, runny nose, watery eyes, goose bumps, diarrhea, vomiting, and muscle aches.
  • oral mucosal erythema – abnormal redness of the mucous membrane lining the inside of the mouth
  • orthostatic hypotension – a drop in blood pressure upon standing, causing dizziness and possible fainting
  • pain
  • peripheral edema – swelling, usually in the lower limbs, caused by accumulation of fluid
  • pharyngitis – sore throat, often accompanied by sneezing, runny nose, headache, cough, fatigue, body aches, chills, and a fever.
  • piloerection – hair standing on end or goosebumps
  • pregnant women may be putting their baby at risk for low birth weight, preterm birth, fetal death, and opioid dependence. An opioid-dependent newborn could experience Neonatal Opioid Withdrawal Syndrome – the baby has a high pitched cry, tremor, vomiting, diarrhea, hyperactivity, abnormal sleep pattern and, possibly, failure to gain weight. Breast feeding mothers also risk their baby becoming dependent on Suboxone.
  • problems with coordination
  • respiratory problems
  • a higher risk of coma and death if Suboxone is taken with other drugs such as benzodiazepines.
  • restlessness
  • rhinitis – chronic sneezing or a congested, drippy nose with no apparent cause
  • rhinorrhea – runny nose
  • risk of going through opioid withdrawal especially when you try to quite suboxone quickly.
  • overdose in those who do not receive opioids regularly. Deaths have been reported in individuals who take only 2 mg of buprenorphine – ¼ of the usual dose for the first day of addressing opioid dependence, and 1/8th that of the second day on – as a sublingual tablet.
  • runny eyes
  • serotonin syndrome – (when taken in combination with serotonergic drugs) – serotonin syndrome is a group of potentially life-threatening symptoms that include high body temperature, agitation, increased reflexes, tremor, sweating, dilated pupils, and diarrhea, associated with serotonergic drugs. Serotonergic drugs are used to treat migraine, depression, and other mood disorders.
  • sleepiness
  • stomach discomfort
  • stomatitis – pain or inflammation of the inside of the lips, cheeks, gums, tongue, and throat
  • sweating
  • swollen and/or painful tongue
  • vomiting

 

WITHDRAWAL SYMPTOMS

Suboxone withdrawal symptoms tend to be milder than those of other opiates. But even when taken as directed and for a short period of time, withdrawal should be medically supervised. Withdrawal symptoms include:

  • abdominal cramps
  • agitation
  • anxiety
  • dehydration
  • diarrhea
  • drug cravings
  • feeling hot or cold more than normal
  • feelings of being on edge
  • flu symptoms – severe – including muscle aches, dizziness, tremors, excessive tearing, runny nose, abdominal cramps, diarrhea, nausea, vomiting, chills, loss of appetite, fatigue, sweats, and trouble regulating temperature.
  • goose bumps
  • insomnia
  • irritability
  • muscle aches
  • runny nose
  • severe vomiting
  • shaking
  • sweating more than normal
  • vomiting
  • watery eyes
  • withdrawal syndrome if you stop taking it suddenly or if you taper off it too quickly

 

TREATMENT

Suboxone can be uncomfortable and painful enough to make it difficult for people stop taking it. Withdrawal from Suboxone – and any drug that can cause dependence or addiction – is safer and more comfortable when done in a medical detox facility. Call us for help.