Buprenorphine, sold under the brand name Subutex, among others, is an opioid used to treat opioid use disorder, acute pain, and chronic pain. It can be used under the tongue, in the cheek, by injection, as a skin patch, or as an implant. For opioid use disorder, it is typically started when withdrawal symptoms have begun and for the first two days of treatment under direct observation of a health care provider. The combination formulation of buprenorphine/naloxone (Suboxone) is recommended to discourage misuse by injection. Maximum pain relief is generally within an hour with effects up to 24 hours.
Side effects may include respiratory depression (decreased breathing), sleepiness, adrenal insufficiency, QT prolongation, low blood pressure, allergic reactions, and opioid addiction. Among those with a history of seizures, there is a risk of further seizures. Opioid withdrawal following stopping buprenorphine is generally less severe than with other opioids. It is unclear if use during pregnancy is safe and use while breastfeeding is not recommended. Buprenorphine affects different types of opioid receptors in different ways.Depending on the type of receptor it may be an agonist, partial agonist, or antagonist.
Buprenorphine was patented in 1965 and approved for medical use in the United States in 1981. In 2017, 14.6 million prescriptions for the medication were written in the United States. It is also a common drug of abuse, being used in place of heroin. Buprenorphine may be used recreationally by injection or in the nose for the high it produces. In the United States, it is a Schedule III controlled substance.
WHAT IS SUBOXONE
It is an opioid used to treat , acute pain, and chronic pain. It can be used under the tongue, in the cheek, by injection, as a skin patch, or as an implant.
USE FOR SUBOXONE
Buprenorphine is used to treat people with opioid use disorder. The combination formulation of buprenorphine/naloxone is generally preferred as naloxone, an opioid antagonist, has a higher bioavailability intravenously and results in acute withdrawal if the formulation is crushed and injected.Prior to starting buprenorphine, individuals should wait long enough after their last dose of opioid until they have some withdrawal symptoms to allow for the medication to bind the receptors, but if taken too soon, buprenorphine can displace other opioids bound to the receptors and precipitate an acute withdrawal. The dose of buprenorphine is then adjusted until symptoms improve, and individuals remain on a maintenance dose through treatment.
A transdermal patch is available for the treatment of chronic pain.These patches are not indicated for use in acute pain, pain that is expected to last only for a short period of time, or pain after surgery, nor are they recommended for opioid addiction.
EFFECT OF SUBOXONE
Common adverse drug reactions associated with the use of buprenorphine are similar to those of other opioids and include: nausea and vomiting, drowsiness, dizziness, headache, memory loss, cognitive and neural inhibition, perspiration, itchiness, dry mouth, shrinking of the pupils of the eyes (miosis), orthostatic hypotension, male ejaculatory difficulty, decreased libido, and urinary retention. Constipation and CNS effects are seen less frequently than with morphine.
At treatment initiation, the first dose of Suboxone should be administered only when objective and clear signs of moderate opioid withdrawal appear, and not less than 4 hours after the patient last used an opioid.
It is recommended that an adequate treatment dose, titrated to clinical effectiveness, should be achieved as rapidly as possible. The dosing on the initial day of treatment may be given in 2 mg to 4 mg increments if preferred. In some studies, gradual induction over several days led to a high rate of dropout of buprenorphine patients during the induction period.
In a one-month study, patients received 8 mg of Suboxone on Day 1 and 16 mg Suboxone on Day 2. From Day 3 onward, patients received either SUBOXONE sublingual tablet or Suboxone at the same buprenorphine dose as Day 2 based on their assigned treatment. Induction in the studies of buprenorphine solution was accomplished over 3-4 days, depending on the target dose.