Butrans

Generic name: buprenorphine transdermal (skin patch)
Drug class: Narcotic analgesics

Medically reviewed by  A Ras MD.

What is Butrans?

Butrans is a strong prescription pain medicine that contains an opioid (narcotic) that is used to manage pain severe enough to require daily, around-the-clock, long-term treatment with an opioid, when other pain treatments such as non-opioid pain medicines or immediate-release opioid medicines do not treat your pain well enough or you cannot tolerate them.

It is a  long-acting (extended-release) opioid pain medicine that can put you at risk for overdose and death. Even if you take your dose correctly as prescribed you are at risk for opioid addiction, abuse, and misuse that can lead to death.

Not for use to treat pain that is not around-the-clock.

Description

BUTRANS is a transdermal system providing systemic delivery of buprenorphine, a mu opioid partial agonist analgesic, continuously for 7 days. The chemical name of buprenorphine is 6,14-ethenomorphinan-7-methanol, 17-(cyclopropylmethyl)- α-(1,1-dimethylethyl)-4, 5-epoxy-18, 19-dihydro-3-hydroxy-6-methoxy-α-methyl-, [5α, 7α, (S)]. The structural formula is:

The molecular weight of buprenorphine is 467.6; the empirical formula is C29H41NO4. Buprenorphine occurs as a white or almost white powder and is very slightly soluble in water, freely soluble in acetone, soluble in methanol and ether, and slightly soluble in cyclohexane. The pKa is 8.5 and the melting point is about 217°C.

System Components and Structure
Five different strengths of BUTRANS are available: 5, 7.5, 10, 15, and 20 mcg/hour (Table 6). The proportion of buprenorphine mixed in the adhesive matrix is the same in each of the five strengths. The amount of buprenorphine released from each system per hour is proportional to the active surface area of the system. The skin is the limiting barrier to diffusion from the system into the bloodstream.

Table 6: BUTRANS Product Specifications

BUTRANS is a rectangular or square, beige-colored system consisting of a protective liner and functional layers. Proceeding from the outer surface toward the surface adhering to the skin, the layers are (1) a beige-colored web backing layer; (2) an adhesive rim without buprenorphine; (3) a separating layer over the buprenorphine-containing adhesive matrix; (4) the buprenorphine-containing adhesive matrix; and (5) a peel-off release liner. Before use, the release liner covering the adhesive layer is removed and discarded.

Figure 1: Cross-Section Diagram of BUTRANS (not to scale).

The active ingredient in BUTRANS is buprenorphine. The inactive ingredients in each system are: levulinic acid, oleyl oleate, povidone, and polyacrylate cross-linked with aluminum.

 Mechanism of Action

Buprenorphine is a partial agonist at the mu-opioid receptor and an antagonist at the kappa-opioid receptors, an agonist at delta-opioid receptors, and a partial agonist at ORL-1 (nociceptin) receptors. The contributions of these actions to its analgesic profile are unclear.

What is the most important information I should know about Butrans?

• Get emergency help right away if you take too much Butrans (overdose). When you first start taking Butrans, when your dose is changed, or if you take too much (overdose), serious or life-threatening breathing problems that can lead to death may occur.
• Taking Butrans with other opioid medicines, benzodiazepines, and alcohol, or other central nervous system depressants (including street drugs) can cause severe drowsiness, decreased awareness, breathing problems, coma, and death.
• Never give anyone else your Butrans. They could die from taking it. Selling or giving away Butrans is against the law.
• Store Butrans securely, out of sight and reach of children, and in a location not accessible by others, including visitors to the home.

Who should not use Butrans?

Do not use Butrans if you have:

• severe asthma, trouble breathing, or other lung problems.
• a bowel blockage or have narrowing of the stomach or intestines.

What should I tell my healthcare provider before using Butrans?

Before applying Butrans, tell your healthcare provider if you have a history of:

• head injury, seizures
• liver, kidney, thyroid problems
• problems urinating
• pancreas or gallbladder problems
• heart rhythm problems (Long QT syndrome)
• abuse of street or prescription drugs, alcohol addiction, or mental health problems.

Tell your healthcare provider if you:

• have a fever
• are pregnant or planning to become pregnant. Prolonged use of Butrans during pregnancy can cause withdrawal symptoms in your newborn baby that could be life-threatening if not recognized and treated.
• are breastfeeding. Not recommended during treatment with Butrans. It may harm your baby.
• are taking prescription or over-the-counter medicines, vitamins, or herbal supplements. Taking Butrans with certain other medicines can cause serious side effects.

How should I use Butrans?

When using Butrans:

• Do not change your dose. Apply Butrans exactly as prescribed by your healthcare provider. Use the lowest effective dose for the shortest time needed.
• See the detailed Instructions for Use for information about how to apply the Butrans patch.
• Do not apply a Butrans patch if the pouch seal is broken, or the patch is cut, damaged, or changed in any way.
• Do not apply more than 1 patch at the same time unless your healthcare provider tells you to.
• You should wear 1 Butrans patch continuously for 7 days.
• Call your healthcare provider if the dose you are using does not control your pain.
• Do not stop using Butrans without talking to your healthcare provider.
• Dispose of expired, unwanted, or unused Butrans by using the Patch-Disposal Unit. Alternatively, Butrans can be disposed of by folding the patch in half and promptly flushing down the toilet, if a drug take-back option is not readily available [see Instructions for Use]. Visit www.fda.gov/drugdisposal for additional information on disposal of unused medicines.

What should I avoid while using Butrans?

While using Butrans do not:

• Take hot baths or sunbathe, use hot tubs, saunas, heating pads, electric blankets, heated waterbeds, or tanning lamps. These can cause an overdose that can lead to death.
• Drive or operate heavy machinery, until you know how Butrans affects you. Butrans can make you sleepy, dizzy, or lightheaded.
• Drink alcohol or use prescription or over-the-counter medicines containing alcohol. Using products containing alcohol during treatment with Butrans may cause you to overdose and die.

What are the possible side effects of Butrans?

The possible side effects of Butrans are:

• constipation,
• nausea,
• sleepiness,
• vomiting,
• tiredness,
• headache,
• dizziness,
• itching,
• redness or rash where the patch is applied.

Call your healthcare provider if you have any of these symptoms and they are severe.

Get emergency medical help if you have:

• trouble breathing,
• shortness of breath,
• fast heartbeat,
• chest pain,
• swelling of your face, tongue or throat,
• extreme drowsiness,
• light-headedness when changing positions feeling faint,
• agitation,
• high body temperature,
• trouble walking,
• stiff muscles,
• mental changes such as confusion.

These are not all the possible side effects of Butrans. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

How should I store Butrans?

Store Butrans securely, out of sight and reach of children, and in a location not accessible by others, including visitors to the home.

Store at Butrans at room temperature 25°C (77°F).

What are the ingredients in Butrans?

Active ingredients: buprenorphine

Inactive ingredients: levulinic acid, oleyl oleate, povidone, and polyacrylate cross-linked with aluminum.

Label

• PRINCIPAL DISPLAY PANEL

  Butrans® 5 mcg Carton
  NDC: 59011–750–04

  

  SRC: NLM .