Nalbuphine Hydrochloride

Pronunciation

Pronunciation: NAL-byoo-FEEN HIGH-droe-KLOR-ide
Class: Opioid agonist-antagonist analgesic

Trade Names

Nubain
- Injection 10 mg/mL
- Injection 20 mg/mL

Nubain (Canada)

Pharmacology

An opiate analgesic with both narcotic agonist and antagonist actions. Analgesic potency is about equal to that of morphine, and antagonist potency is about 1/ 25 that of naloxone. May cause sphincter of Oddi spasm. Does not increase pulmonary artery pressure, systemic vascular resistance, or myocardial work load.

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Pharmacokinetics

Absorption

When nalbuphine is taken orally, it is not as effective for pain relief as when given IM, mainly because of first-pass metabolism in GI and liver. T max is 30 min (IM).

Distribution

Nalbuphine is not bound to plasma proteins. Nalbuphine crosses the placenta.

Metabolism

Metabolized in the liver.

Elimination

Approximately 7% eliminated in urine unchanged and in feces. Plasma t 1/ 2 is 5 h and t 1/ 2 is 2.4 h.

Onset

Onset of IV nalbuphine is 2 to 3 min. Onset of subcutaneous and IM nalbuphine is less than 15 min.

Duration

Duration of analgesic activity is 3 to 6 h.

Indications and Usage

Management of moderate to severe pain; preoperative and postoperative analgesia; supplement to balanced anesthesia; obstetrical analgesia during labor and delivery.

Unlabeled Uses

Prevention and treatment of intrathecal morphine-induced pruritus after cesarean delivery.

Contraindications

Standard considerations.

Dosage and Administration

Adults

Subcutaneous / IM / IV 10 mg per 70 kg q 3 to 6 h as needed. Individualize dosage. In nontolerant patients, do not exceed 20 mg/dose or 160 mg/day.

General Advice

  • For subcutaneous, IM, or IV administration. Not for intradermal or intra-arterial administration.
  • Do not administer if particulate matter or discoloration noted.
  • Discard any unused medication per institutional policy and procedure.
  • Ensure naloxone, oxygen, and resuscitation and intubation equipment are available for use if needed.

Storage/Stability

Store ampules and vials at controlled room temperature (59° to 86°F). Protect from excessive light. Store ampules and vials in carton until contents have been used.

Drug Interactions

CNS depressants, including barbiturate anesthetics

Increased respiratory and CNS depression.

Incompatibility

Nafcillin, ketorolac.

Laboratory Test Interactions

May interfere with enzymatic methods for detection of opioids, depending on the specificity of test.

Adverse Reactions

Cardiovascular

Bradycardia, hypertension, hypotension, tachycardia (1% or less).

CNS

Sedation (36%); dizziness, vertigo (5%); headache (3%); agitation, confusion, crying, depression, dysphoria, euphoria, faintness, floating feeling, hallucinations, heaviness feeling, hostility, nervousness, numbness, restlessness, seizures, tingling, unreality, unusual dreams (1% or less).

Dermatologic

Flushing (1% or less).

EENT

Blurred vision (1% or less).

GI

Nausea, vomiting (6%); dry mouth (4%); bitter taste, cramps, dyspepsia (1% or less).

Genitourinary

Urinary urgency (1% or less).

Hypersensitivity

Anaphylactic or anaphylactoid and other hypersensitivity reactions (including shock, respiratory distress, respiratory arrest, bradycardia, cardiac arrest, hypotension, or laryngeal edema), stridor, bronchospasm, wheezing, edema, rash, pruritus, nausea, vomiting, diaphoresis, weakness, shakiness (1% or less).

Local

Injection site reactions including burning, hot sensations, pain, redness, swelling (postmarketing).

Respiratory

Pulmonary edema (postmarketing).

Miscellaneous

Sweaty/clammy feeling (9%); speech difficulty, warmth (1% or less).

Precautions

Pregnancy

Category B .

Lactation

Excreted in breast milk.

Children

Safety and efficacy not established.

Renal Function

Duration of action may be prolonged in patients with renal function impairment; may need to reduce dose.

Hepatic Function

Duration of action may be prolonged in patients with hepatic function impairment; may need to reduce dose.

Special Risk Patients

Use drug with caution in patients with impaired respiration, head injury, increased intracranial pressure, or MI with nausea or vomiting, and in patients about to undergo biliary tract surgery.

Sulfite Sensitivity

Contains sodium metabisulfite, which may cause allergic-type reactions including anaphylactic symptoms and life-threatening asthma.

Dependence

Low abuse potential; however, withdrawal symptoms can occur after long-term use. Use drug with caution in patients who are emotionally unstable or have history of narcotic abuse.

Opiate-dependent patients

Nalbuphine can precipitate withdrawal; small doses of morphine can be given to relieve discomfort. If patient has received morphine, meperidine, codeine, or other opiate of similar duration, give 25% of normal nalbuphine dose first. Observe for signs of withdrawal and increase nalbuphine dose slowly.

Overdosage

Symptoms

Respiratory depression, hypoxemia, sedation.

Patient Information

  • Advise patient or caregiver that medication will usually be prepared and administered by a health care provider in a health care setting.
  • Caution patient or caregiver that medication may be habit forming and, if used at home, to use exactly as prescribed and not to change the dose or discontinue therapy unless advised by health care provider. Advise patient or caregiver to notify health care provider if medication does not adequately control pain.
  • Advise patient or caregiver that if medication needs to be discontinued after prolonged use that it will usually slowly be withdrawn unless safety concerns (eg, rash) require a more rapid withdrawal.
  • Advise patient or caregiver to notify health care provider if any of the following occur: excessive sedation or drowsiness; slow or shallow breathing; low BP; slow heart rate; severe constipation.
  • Instruct patient to get up slowly from lying or sitting position and to avoid sudden position changes to prevent postural hypotension.
  • Advise patient to report dizziness with position changes to health care provider.
  • Caution patient that hot tubs and hot showers or baths may make dizziness worse.
  • Caution patient that drug may cause dizziness or drowsiness and to use caution while driving or performing other tasks requiring mental alertness or coordination until tolerance is determined.
  • Caution patient to avoid alcohol and other CNS depressant medications while using this medication.

Copyright © 2009 Wolters Kluwer Health.

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