Drug Guide
Butorphanol Tartrate
Classification
Therapeutic: Opioid analgesic, mixed agonist-antagonist
Pharmacological: Kappa-opioid receptor agonist and partial-mu-opioid receptor antagonist
FDA Approved Indications
- Management of moderate to severe pain
Mechanism of Action
Butorphanol works by activating kappa-opioid receptors and partially blocking mu-opioid receptors, providing analgesia with potentially fewer side effects related to mu-opioid receptor activation.
Dosage and Administration
Adult: Typically 1-4 mg every 3-4 hours as needed, not exceeding 8 mg per dose or 24 mg per day.
Pediatric: Use is not established; consult specific pediatric guidelines.
Geriatric: Use with caution; start at lower end of dosing range.
Renal Impairment: Adjust dose cautiously; no specific guidelines, monitor for increased effects.
Hepatic Impairment: Use with caution; dosing adjustments may be necessary. Consider lower doses.
Pharmacokinetics
Absorption: Rapidly absorbed via intranasal, IM, IV routes.
Distribution: Widely distributed, crosses the blood-brain barrier.
Metabolism: Metabolized in the liver via CYP3A4 enzymes.
Excretion: Excreted mainly in urine, small amount in feces.
Half Life: Approximately 2-3 hours.
Contraindications
- Hypersensitivity to butorphanol or other opioids.
- Acute respiratory depression.
- Shock.
Precautions
- Use with caution in patients with a history of substance abuse, head injury, increased intracranial pressure, or hepatic impairment. Not recommended in obstetrics during labor due to potential neonatal respiratory depression.
Adverse Reactions - Common
- Dizziness (Common)
- Nausea (Common)
- Drowsiness (Common)
Adverse Reactions - Serious
- Respiratory depression (Uncommon but serious)
- Hypotension (Uncommon)
- Cardiovascular collapse (Rare)
Drug-Drug Interactions
- CNS depressants (e.g., alcohol, benzodiazepines) increasing sedation risk.
- Other opioids may enhance effects or respiratory depression.
Drug-Food Interactions
N/ADrug-Herb Interactions
N/ANursing Implications
Assessment: Monitor respiratory status, level of consciousness, and pain relief.
Diagnoses:
- Risk for respiratory depression
- Ineffective airway clearance
- Risk for falls due to dizziness or sedation
Implementation: Administer IV, IM, or intranasal as prescribed. Monitor vital signs closely.
Evaluation: Assess pain relief, respiratory status, and for adverse effects.
Patient/Family Teaching
- Do not operate heavy machinery or drive.
- Avoid alcohol and sedatives.
- Report excessive drowsiness, confusion, difficulty breathing.
Special Considerations
Black Box Warnings:
- Risks of addiction, abuse, and misuse.
Genetic Factors: No specific pharmacogenetic considerations.
Lab Test Interference: May alter some laboratory test results, such as for liver function or urinalysis.
Overdose Management
Signs/Symptoms: Sedation, respiratory depression, pinpoint pupils.
Treatment: Administer naloxone for respiratory depression. Supportive care including airway management and mechanical ventilation if necessary.
Storage and Handling
Storage: Store at room temperature, away from light and moisture.
Stability: Stable until the expiration date on the package.