Butorphanol

Butorphanol Tartrate Injection is indicated - as a preoperative or pre-anesthetic medication - as a supplement to balanced anesthesia - for the relief of pain during labor, and - for the management of pain severe enough to require an opioid analgesic and for which alternative treatments are inadequate. Limitations of Use: Because of the risks of addiction, abuse, misuse, overdose, and death, which can occur at any dosage or duration and persist over the course of therapy, reserve opioid analgesics, including butorphanol tartrate, for use in patients for whom alternative treatment options are ineffective, not tolerated, or would be otherwise inadequate to provide sufficient management of pain.

Butorphanol is a partial opioid agonist at the mu opioid receptor and a full agonist at the kappa opioid receptor. The principal therapeutic action of butorphanol is analgesia. Clinically, dosage is titrated to provide adequate analgesia and may be limited by adverse reactions, including respiratory and CNS depression. The precise mechanism of the analgesic action is unknown. However, specific CNS opioid receptors for endogenous compounds with opioid-like activity have been identified throughout the brain and spinal cord and are thought to play a role in the analgesic effects of this drug.

Important Dosage and Administration Instructions Butorphanol Tartrate Injection should be prescribed only by healthcare professionals who are ‎knowledgeable about the use of opioids and how to mitigate the ‎associated risks.‎ Use the lowest effective dosage for the shortest duration of time consistent with individual patient treatment goals. Because the risk of overdose increases as opioid doses increase, reserve ‎titration to higher doses of Butorphanol Tartrate Injection for patients in whom lower ‎doses are insufficiently effective and in whom the expected benefits of ‎using a higher dose opioid clearly outweigh the substantial risks.‎ There is variability in the opioid analgesic dose and duration needed to ‎adequately manage pain due both to the cause of pain and to individual ‎patient factors.

Butorphanol Tartrate Injection is contraindicated in: • Patients with significant respiratory depression • Patients with acute of severe bronchial asthma in an unmonitored setting or in the absence of resuscitative equipment • Patients with known or suspected gastrointestinal obstruction, including paralytic ileus • Patients with hypersensitivity to butorphanol tartrate or any of the formulation excipients (e.g., anaphylaxis)

Boxed warning (serious and life-threatening risks from use of butorphanol tartrate injection): Addiction, Abuse, and Misuse Because the use of Butorphanol Tartrate Injection exposes patients and other users to the risks of opioid addiction, abuse, and misuse, which can lead to overdose and death, assess each patient’s risk prior to prescribing and reassess all patients regularly for the development of these behaviors and conditions. Addiction, Abuse, and Misuse Butorphanol Tartrate Injection is a Schedule IV controlled substance. As an opioid, butorphanol tartrate exposes users to the risks of addiction, abuse, and misuse. Although the risk of addiction in any individual is unknown, it can occur in patients appropriately prescribed butorphanol tartrate. Addiction can occur at recommended dosages and if the drug is misused or abused.

The following serious adverse reactions are described, or described in greater detail, in other sections: • Addiction, Abuse, and Misuse • Life-Threatening Respiratory Depression • Interactions with Benzodiazepines and Other CNS Depressants • Neonatal Opioid Withdrawal Syndrome • Opioid-Induced Hyperalgesia and Allodynia • Adrenal Insufficiency • Cardiovascular Effects • Gastrointestinal Adverse Reactions • Seizures • Withdrawal Clinical Trial Experience A total of 1658 patients were studied in premarketing clinical trials of Butorphanol Tartrate Injection. In nearly all cases the type and incidence of side effects with butorphanol were those commonly observed with opioid analgesics. The adverse experiences described below are based on data from short- and long-term clinical trials in patients receiving Butorphanol Tartrate Injection.

Benzodiazepines and Other Central Nervous System (CNS) Depressants Due to additive pharmacologic effect, the concomitant use of benzodiazepines or other CNS depressants such as alcohol, sedatives/hypnotics, anxiolytics, tranquilizers, muscle relaxants, general anesthetics, antipsychotics, gabapentinoids (gabapentin or pregabalin), and other opioids, can increase the risk of respiratory depression, profound sedation, coma, and death. Reserve concomitant prescribing of these drugs for use in patients for whom alternative treatment options are inadequate. Limit dosages and durations to the minimum required. Monitor patients closely for signs of respiratory depression and sedation. If concomitant use is warranted, consider ‎prescribing naloxone for the emergency treatment of opioid overdose.

Store at 20°C to 25°C (68°F to 77°F). Protect from light.