Butorphanol Tartrate

Trade Names:
Stadol
- Injection 1 mg/mL (1 mg of tartrate salt is equal to 0.68 mg base)
- Injection 2 mg/mL (1 mg of tartrate salt is equal to 0.68 mg base)
- Nasal Spray 10 mg/mL

Pharmacology

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Potent analgesic that stimulates and inhibits opiate receptors in CNS. Antagonist effects decrease (but do not eliminate) abuse potential and may cause withdrawal symptoms in patients with opiate dependence.

Pharmacokinetics

Absorption

IM T _max is 20 to 40 min.

Nasal T _max is 30 to 60 min. Absolute bioavailability is 60% to 70% (oral bioavailability 5% to 17% because of extensive first pass metabolism).

Distribution

Butorphanol is about 80% protein bound. Vd is 305 to 901 L. Butorphanol crosses the blood-brain barrier and placenta; it is excreted into human milk.

Metabolism

Metabolized in liver to hydroxybutorphanol and norbutorphanol.

Elimination

70% to 80% excreted in urine (5% as unchanged drug); 15% excreted in feces. The t _½ is 2.1 to 8.8 h (IV) and 2.9 to 9.2 h (intranasal). Cl is 52 to 154 L/h.

Onset

IV A few min. IM Within 15 min. Nasal Within 15 min.

Peak

IV / IM 30 to 60 min. Nasal 1 to 2 h.

Duration

IV / IM 3 to 4 h. Nasal 4 to 5 h.

Special Populations

For those with Ccr less than 30 mL/min, the t _½ is approximately doubled and the total body Cl is approximately ½.

The t _½ may be tripled and total body Cl is approximately ½.

Elderly t _½ is increased 25%. Absolute bioavailability of nasal spray is less in elderly women (48%) than in elderly men (75%).

Indications and Usage

Management of pain when use of an opioid analgesic is appropriate (parenteral/nasal); preoperative or preanesthetic medication, as a supplement to balanced anesthesia, and for relief of pain during labor (parenteral).

Contraindications

Hypersensitivity to this medication or the preservative benzethonium chloride.

Dosage and Administration

IV 0.5 to 2 mg every 3 to 4 h as needed. IM 1 to 4 mg every 3 to 4 h as needed. Single doses should not exceed 4 mg. Nasal Initial dose is 1 mg (1 spray in 1 nostril). Wait 60 to 90 min before giving second 1 mg dose. Repeat dose sequence in 3 to 4 h after second dose of sequence if needed. For severe pain, in patient able to remain recumbent, initial dose 2 mg (1 spray in each nostril) every 3 to 4 h.

Usual dose: IM 2 mg 60 to 90 min before surgery; IV 2 mg shortly before induction. Maintenance dose in balanced anesthesia: IV 0.5 to 1 mg.

IV / IM 1 to 2 mg in early labor at term; repeat after 4 h.

IM / IV ½ normal dose. Repeat doses determined by patient's response rather than at fixed intervals, but generally no less often than at 6-h intervals. Nasal Initial dose is 1 mg (1 spray in 1 nostril). Wait 90 to 120 min before giving second 1 mg dose. Repeat dose sequence based on patient response, but generally no less often than 6-h intervals.

General Advice

• IV/IM
• When giving by IM route, use deep, slow injection.
• If accidental skin contact occurs, wash exposed area with cool water.
• Do not administer if solution is discolored, cloudy, or contains particulate matter.

• Nasal
• Pump reservoir must be primed prior to initial use; pump sprayer firmly and quickly until a fine spray appears (up to 7 to 8 strokes).
• Pump reservoir must be reprimed (1 or 2 strokes) if not used for 48 h or longer).
• Butorphanol may be aerosolized during priming process; aim pump sprayer away from yourself, the patient, and other people.
• Insert spray tip into 1 nostril, pointing tip toward back of the nose, close other nostril with finger, and pump spray unit firmly and quickly while patient is gently sniffing with mouth closed. Remove pump unit from nose and have patient tilt head backwards and continue sniffing gently for a few more seconds.
• One bottle will deliver 14 to 15 doses if no repriming is needed. With intermittent use requiring repriming before each dose, 1 bottle may deliver only 8 to 10 doses.
• Follow institutional or organizational policies and procedures to dispose of used pump units. Dispose of used units by unscrewing the cap, rinsing the bottle, and placing parts in waste container.

Storage/Stability

Store at controlled room temperature (59° to 86°F).

Drug Interactions

Additive CNS depression.

Laboratory Test Interactions

None well documented.

Adverse Reactions

Cardiovascular

Palpitations, vasodilation (at least 1%).

CNS

Somnolence (43%); dizziness (19%); insomnia (nasal spray; 11%); anxiety, asthenia, confusion, euphoria, floating feeling, headache, lethargy, nervousness, paresthesia, tremor (at least 1%); convulsions, delusions, difficulty speaking, difficulty executing purposeful movements, drug dependence, vertigo (postmarketing).

Dermatologic

Pruritus, sweating/clamminess (at least 1%).

EENT

Nasal congestion (nasal spray; 13%); blurred vision, ear pain, pharyngitis, rhinitis, tinnitus, unpleasant taste (at least 1%).

GI

Nausea, vomiting (nasal spray; 13%); anorexia, constipation, dry mouth, stomach pain (at least 1%).

Respiratory

Bronchitis, cough, dyspnea, epistaxis, nasal congestion, nasal irritation, sinus congestion, sinusitis, upper respiratory infection (at least 1%).

Miscellaneous

Sensation of heat (at least 1%); apnea (postmarketing).

Precautions

Pregnancy

Category C .

Lactation

Excreted in breast milk.

Children

Safety and efficacy not established.

Elderly

More sensitive to effects; reduce dose.

Labor and Delivery

Rare reports of infant respiratory distress/apnea following butorphanol administration within 2 h of delivery, multiple butorphanol doses, use with other analgesic/sedative drugs, or in preterm pregnancies. Use with caution in presence of abnormal fetal heart rate patterns.

Hazardous Tasks

May cause drowsiness, dizziness, or hypotension during first hour of dosing.

CV disease

Drug increases cardiac workload. Severe hypertension has occurred.

Drug dependency

Although potential for physical dependence is low, abuse may occur. Tolerance and psychological and physical dependence may occur with long-term use. Use in patients physically dependent on opiate agonists may precipitate withdrawal symptoms.

Head injury and increased intracranial pressure

May cause C0 ₂ retention and secondary elevation of CSF pressure, drug-induced miosis, and alterations in mental status that could obscure interpretation of clinical course of patients with head injuries.

Respiratory depression

May occur, especially in patients on other CNS drugs or in patients with CNS disease or respiratory impairment.

Special populations

Use with caution in patients with hepatic or renal disease.

Overdosage

Symptoms

CV insufficiency, coma, death, hyperventilation.

Patient Information

• Advise patient to review the Medication Guide carefully before starting therapy and to read and check for new information each time the medication is refilled.
• Advise patient that medication may be habit forming and to take exactly as prescribed and not increase the dose or frequency of use unless advised by health care provider. Instruct patient to notify health care provider if prescribed dose does not adequately control pain.
• Review dosing schedule for 1 mg dose: 1 spray into 1 nostril only. Dose may be repeated after 60 to 90 min if prescribed by health care provider. Sequence may be repeated after 3 to 4 h if prescribed and needed for pain.
• Review dosing schedule for 2 mg dose: 1 spray into each nostril. Dose may be repeated every 3 to 4 h if prescribed and needed for pain.
• Ensure patient understands how to use nasal spray: prime pump prior to initial use (7 to 8 strokes or until fine mist appears) or reprime (1 or 2 strokes) if unit has not been used for 48 h or longer); insert spray tip into 1 nostril, pointing tip toward back of the nose, close other nostril with finger, and pump spray unit firmly and quickly while gently sniffing with mouth closed; remove pump unit from nose, tilt head backwards, and continue sniffing gently for a few more seconds.
• Caution patient that butorphanol may be aerosolized during priming process and to aim pump sprayer away from themselves, other people, and animals.
• Advise patient that 1 bottle will deliver 14 to 15 doses if no repriming needed but with intermittent use requiring repriming before each dose; 1 bottle may deliver only 8 to 10 doses.
• Instruct patient regarding proper disposal of used spray units: unscrew cap, rinse bottle, and place parts in waste container.
• Caution patient that medication may cause drowsiness or dizziness and to use caution while performing potentially hazardous tasks (eg, driving, operating machinery) until tolerance is determined.
• Caution patient to avoid alcohol and other depressants (eg, sleep medications, tranquilizers) because dangerous additive effects may occur.

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