buprenorphine transdermal (Rx)

Brand and Other Names:Butrans
  • Print

Dosing & Uses

AdultPediatric

Dosing Form & Strengths

transdermal patch: Schedule III

  • 5mcg/hr
  • 7.5mcg/hr
  • 10mcg/hr
  • 15mcg/hr
  • 20mcg/hr

Chronic Severe Pain

Indicated for the management of pain severe enough to require daily, around-the-clock, long-term opioid treatment and for which alternative treatment options are inadequate

Each patch is worn for 7 days (except during titration)

Opioid-naïve: Initiate with 5 mcg/hr patch; may supplement with prompt-acting opioid and nonopioid analgesic for break-through pain

Do not increase patch until patient has been exposed continually to previous dose for 72 hr

Based on requirement for supplemental short-acting analgesics, upward titration may be instituted with at a minimum interval of 72 hr  

Do not exceed dose of one 20 mcg/hr transdermal system (risk of QT prolongation with higher doses)

Conversion from other opioids

  • Oral morphine equivalent <30 mg/day: Initiate with 5 mcg/hr patch
  • Oral morphine equivalent 30-80 mg/day: Initiate with 10 mcg/hr patch
  • May supplement with prompt-acting opioid and nonopioid analgesic for break-through pain
  • Use caution when prescribing to opioid-experienced patients requiring high doses of opioids (ie, >80 mg/day oral morphine equivalent); buprenorphine transdermal 20 mcg/hr may not provide adequate analgesia for patients previously on high-dose opioids

Opioid-tolerant definition

  • Use of higher starting doses in patients who are not opioid tolerant may cause fatal respiratory depression
  • Patients who are opioid tolerant are those receiving, for 1 week or longer, at least 60 mg/day PO morphine, 25 mcg/hr transdermal fentanyl, 30 mg/day PO oxycodone, 8 mg/day PO hydromorphone, 25 mg/day PO oxymorphone, or an equianalgesic dose of another opioid

Limitations of use

  • Because of the risks of addiction, abuse, and misuse with opioids, even at recommended doses, and because of the greater risks of overdose and death with extended-release opioid formulations, reserve for patients whom alternative treatment options (eg, nonopioid analgesics or immediate-release opioids) are ineffective, not tolerated, or would be otherwise inadequate to provide sufficient management of pain
  • Not indicated as a PRN analgesic

Geriatric Dosing

Although specific dose adjustments on the basis of advanced age are not required for pharmacokinetic reasons, use caution in the elderly population to ensure safe use

Clinical trials observed that some adverse effects (ie, respiratory depression, constipation, urinary retention) occur more frequently in elderly patients

Hepatic Impairment

Only intended for 7-day application, consider use of an alternate analgesic that permits flexible dosing

Mild-to-moderate: Initiate with 5 mcg/hr dose; titrate to provide adequate analgesia and tolerable adverse effects

Severe: Not yet studied with severe hepatic impairment

Administration

Apply to hairless or nearly hairless skin site; if none available, clip hair at application site (do not shave)

Do not apply to irritated skin

Clean application site with water only; do not use soaps, alcohol, oils, lotions, or abrasive devices

Allow skin to dry completely before application

If problems with adhesion occur, may tape edges with first aid tape

If transdermal patch falls off during the 7 days, discard patch and apply new patch to different skin site

Rotate application site: after each patch removal, wait a minimum of 3 weeks before reapplying to same application site

When discontinuing patch, taper dose as part of comprehensive treatment plan; consider use of immediate-release opioid analgesics

Safety and efficacy not established

Next:

Adverse Effects

>10%

Nausea (23%)

Dizziness (16%)

Headache (16%)

Pruritus at application site (15%)

Constipation (14%)

Somnolence (14%)

Vomiting (11%)

1-10%

Peripheral edema (7%)

Xerostomia (7%)

Erythema at application site (7%)

Rash at application site (6%)

Fatigue (5%)

Hyperhidrosis (4%)

Pruritus (4%)

Falls (4%)

Diarrhea (3%)

Pain in extremity (3%)

Insomnia (3%)

Dyspnea (3%)

Dyspepsia (3%)

Urinary tract infection (3%)

Back pain (3%)

Joint swelling (3%)

Hypoesthesia (2%)

Arthralgia (2%)

Stomach discomfort (2%)

Rash (2%)

Anorexia (2%)

Paraesthesia (2%)

Tremor (2%)

Confusional state (2%)

Previous
Next:

Warnings

Black Box Warnings

Addiction, abuse, and misuse

  • Risk of opioid addiction, abuse, and misuse, which can lead to overdose and death
  • Assess each patient’s risk prior to prescribing and monitor all patients regularly for the development of these behaviors or conditions

Life-threatening respiratory depression

  • Serious, life-threatening, or fatal respiratory depression may occur
  • Monitor for respiratory depression, especially during initiation or following a dose increase

Accidental exposure

  • Accidental of even 1 dose, especially by children, can result in a fatal overdose

Neonatal opioid withdrawal syndrome

  • Prolonged use during pregnancy can result in neonatal opioid withdrawal syndrome, which may be life-threatening if not recognized and treated, and requires management according to protocols developed by neonatology experts
  • Syndrome presents as irritability, hyperactivity and abnormal sleep pattern, high pitched cry, tremor, vomiting, diarrhea and failure to gain weight
  • Onset, duration, and severity of neonatal opioid withdrawal syndrome vary based on the specific opioid used, duration of use, timing and amount of last maternal use, and rate of elimination of the drug by the newborn
  • If opioid use is required for a prolonged period in a pregnant woman, advise the patient of the risk of neonatal opioid withdrawal syndrome and ensure that appropriate treatment will be available

Contraindications

Hypersensitivity

Significant respiratory depression

Severe bronchial asthma

Paralytic ileus

Management of acute pain or opioid analgesia required for short period of time

Management of postoperative pain, including use after outpatient or day surgeries

Management of mild pain

Management of intermittent pain (not for PRN use)

Cautions

Respiratory depression is main hazard; may occur more frequently in elderly or debilitated patients, or in conditions associated with hypoxia or hypercapnia (even moderate therapeutic doses)

CNS depression: May cause somnolence, dizziness, altered consciousness (including coma)

Coadministration with alcohol, other CNS depressants, and illicit drugs may cause hypotension, profound sedation, and coma or respiratory depression

QTc prolongation observed in healthy individuals at 40 mcg/hr; avoid in patients with history of Long QT Syndrome or coadministration with Class IA (eg, quinidine, procainamide, disopyramide) or Class III (eg, sotalol, amiodarone, dofetilide) antiarrhythmics

Head injury: Respiratory depressant effects of opioids may include carbon dioxide retention and lead to elevated CSF pressure

Hypotensive effects: Can cause severe hypotension; caution with depleted blood volume or coadministration of drugs that that affect vasomotor tone (eg, phenothiazines), vasodilators, or antihypertensives

Misuse, abuse, diversion: Partial agonist at the mu opioid receptor and a Schedule III controlled opioids expose users to the risks of addiction, abuse, and misuse; there is a greater risk for overdose and death with extended-release opioids due to the larger amount of active opioid present (see Black Box Warnings)

Serious, life-threatening, or fatal respiratory depression reported (see Black Box Warnings)

Accidental exposure reported, including fatalities (see Black Box Warnings)

Neonatal opioid withdrawal syndrome reported with long-term use during pregnancy (see Black Box Warnings)

Interactions with CNS depressants (eg, alcohol, sedatives, anxiolytics, hypnotics, neuroleptics, other opioids) can cause additive effects and increase risk for respiratory depression, profound sedation, and hypotension

Hepatoxicity: Although not observed in buprenorphine transdermal chronic pain clinical trials, cases of cytolytic hepatitis and hepatitis with jaundice observed in individuals receiving buprenorphine SL for opioid dependence treatment

Fever: If fever or increased core body temperature occurs following strenuous exertion, monitor for increased opioid adverse effects; adjust dose if necessary

Similar to other opioids, may aggravate seizure disorders by lowering seizure threshold

Special risk groups may experience increased adverse reactions; caution with alcoholism, delirium tremens, adrenocortical insufficiency, CNS depression, debilitation, kyphoscoliosis associated with respiratory compromise, myxedema or hypothyroidism, prostatic hypertrophy or urethral stricture, severe impairment of hepatic, pulmonary or renal function, and toxic psychosis

May cause sphincter of Oddi spasm and aggravate abdominal conditions, including ileus

Not recommended for use within 14 days of MAO inhibitors; severe and unpredictable potentiation by MAO inhibitors reported

Previous
Next:

Pregnancy & Lactation

Pregnancy Category: C

Opioids cross the placenta and may produce respiratory depression and psychophysiologic effects in neonates; not recommended for use in women immediately prior to and during labor, when use of shorter-acting analgesics or other analgesic techniques are more appropriate

Neonates whose mothers have been taking opioids chronically may also exhibit withdrawal signs, either at birth and/or in the nursery, because they have developed physical dependence; neonatal opioid withdrawal syndrome, unlike opioid withdrawal syndrome in adults, may be life-threatening and should be treated according to protocols developed by neonatology experts

Lactation: Detected in low concentrations in human milk; breastfeeding not advised

Pregnancy Categories

A:Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

B:May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

C:Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

D:Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

X:Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

NA:Information not available.

more...
Previous
Next:

Pharmacology

Mechanism of Action

Semisynthetic narcotic mixed agonist-antagonist analgesic; exerts agonistic effects at the mu and delta opioid receptors in the CNS, and antagonistic effects at the kappa opioid receptor

Absorption

17 hr is the median time for 10mcg/hr to deliver quantifiable concentration (ie, >25 pg/mL)  

Peak plasma concentration: 176 pg/mL (5 mcg/hr); 191 pg/mL (10 mcg/hr); 471 pg/mL (20 mcg/hr)  

AUC: 12,087 pg•h/mL (5 mcg/hr); 27,035 pg•h/mL (10 mcg/hr); 54,294 pg•h/mL (20 mcg/hr)

Absolute bioavailability: 15%

Distribution

Vd: 430 L (after IV administration)

Protein bound: 96%  

Metabolism

Metabolism: via hepatic metabolism, with subsequent biliary excretion and renal excretion of soluble metabolites

Pharmacokinetics

Half-life, terminal: 26 hr (after patch removal)

Clearance: 55 L/hr

Excretion (within 7 days): Feces (70%), urine (27%)

Previous
Next:

Images

Previous
Next:

Formulary

FormularyPatient Discounts

Adding plans allows you to compare formulary status to other drugs in the same class.

To view formulary information first create a list of plans. Your list will be saved and can be edited at any time.

Adding plans allows you to:

  • View the formulary and any restrictions for each plan.
  • Manage and view all your plans together – even plans in different states.
  • Compare formulary status to other drugs in the same class.
  • Access your plan list on any device – mobile or desktop.

The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

Tier Description
1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
NC NOT COVERED – Drugs that are not covered by the plan.
Code Definition
PA Prior Authorization
Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
QL Quantity Limits
Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
ST Step Therapy
Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
OR Other Restrictions
Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
Additional Offers
Email to Patient

From:

To:

The recipient will receive more details and instructions to access this offer.

By clicking send, you acknowledge that you have permission to email the recipient with this information.

Email Forms to Patient

From:

To:

The recipient will receive more details and instructions to access this offer.

By clicking send, you acknowledge that you have permission to email the recipient with this information.

Previous