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/mLApo-Butorphanol (Canada)PMS-Butorphanol (Canada)
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.
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).
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.
Metabolized in liver to hydroxybutorphanol and norbutorphanol.
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.
IV A few min. IM Within 15 min. Nasal Within 15 min.
IV / IM 30 to 60 min. Nasal 1 to 2 h.
IV / IM 3 to 4 h. Nasal 4 to 5 h.
For those with Ccr less than 30 mL/min, the t ½ is approximately doubled and the total body Cl is approximately ½.Hepatic Function Impairment
The t ½ may be tripled and total body Cl is approximately ½.Elderly
Elderly t ½ is increased 25%. Absolute bioavailability of nasal spray is less in elderly women (48%) than in elderly men (75%).
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).
Hypersensitivity to this medication or the preservative benzethonium chloride.
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.Preoperative/PreanestheticAdults
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.LaborAdults
IV / IM 1 to 2 mg in early labor at term; repeat after 4 h.Kidney or Liver Impairment and ElderlyAdults
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.
Store at controlled room temperature (59° to 86°F).
Additive CNS depression.
None well documented.
Palpitations, vasodilation (at least 1%).
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).
Pruritus, sweating/clamminess (at least 1%).
Nasal congestion (nasal spray; 13%); blurred vision, ear pain, pharyngitis, rhinitis, tinnitus, unpleasant taste (at least 1%).
Nausea, vomiting (nasal spray; 13%); anorexia, constipation, dry mouth, stomach pain (at least 1%).
Bronchitis, cough, dyspnea, epistaxis, nasal congestion, nasal irritation, sinus congestion, sinusitis, upper respiratory infection (at least 1%).
Sensation of heat (at least 1%); apnea (postmarketing).
Take vital signs and auscultate heart and lungs before administration.
Category C .
Excreted in breast milk.
Safety and efficacy not established.
More sensitive to effects; reduce dose.
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.
May cause drowsiness, dizziness, or hypotension during first hour of dosing.
Drug increases cardiac workload. Severe hypertension has occurred.
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.
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.
May occur, especially in patients on other CNS drugs or in patients with CNS disease or respiratory impairment.
Use with caution in patients with hepatic or renal disease.
CV insufficiency, coma, death, hyperventilation.
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