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Butorphanol Tartrate


Class: Opiate Partial Agonists
VA Class: CN101
CAS Number: 58786-99-5
Brands: Stadol, Stadol NS


Opiate partial agonist; phenanthrene derivative.a b d

Uses for Butorphanol Tartrate


Relief of moderate to severe pain such as that associated with acute and chronic medical disorders including cancer, neuropathic or spastic conditions, orthopedic problems, burns, renal colic, and surgery.d

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Preoperative sedation and analgesia and as a supplement to surgical anesthesia.a

Obstetric analgesia during labor.a

Management of pain associated with migraine headache.113 114 116 122

In equianalgesic doses, parenteral butorphanol is as effective as morphine, meperidine, and pentazocine, but relative potential for abuse reportedly is less than that of codeine or propoxyphene.d

Butorphanol Tartrate Dosage and Administration


Administer IM, by IV injection, or by nasal inhalation.113

Nasal Administration

Assemble the nasal solution spray pump according to the manufacturer’s instructions.113 Prior to initial use, fully prime the spray pump; reprime pump whenever it has not been used for ≥48 hours.113

Consult the manufacturer’s patient instructions regarding use of the nasal solution spray pump.113 124

The nasal solution spray pump is an open delivery system; aim the pump spray away from the patient, other individuals, or animals to minimize environmental exposure.113

IV Administration

For drug compatibility information, see Compatibility under Stability.


Available as butorphanol tartrate; dosage expressed in terms of the salt.a b

After initial priming, the nasal solution spray pump delivers about 14–15 metered doses containing 1 mg per spray.a If repriming of the pump is necessary, the spray pump will deliver about 8–10 metered doses, depending on the extent of repriming.113



Initially, 1 mg; may repeat dose every 3–4 hours as necessary.a Usual effective dosage, depending on severity of pain, is 0.5–2 mg repeated every 3–4 hours.a


Initially, 2 mg in patients able to remain recumbent; may repeat dose every 3–4 hours as necessary.a Usual effective dosage, depending on severity of pain, is 1–4 mg repeated every 3–4 hours.a


Initially, 1 mg (1 spray in 1 nostril); if adequate analgesia is not achieved, may give an additional 1-mg dose within 60–90 minutes.113 May repeat this initial dose sequence in 3–4 hours, if needed.113

For management of severe pain: Initially, 2 mg (1 spray in each nostril) in patients who can remain recumbent if drowsiness or dizziness occurs.113 Do not administer additional 2-mg doses at intervals <3–4 hours, since the incidence of adverse effects may be increased.113

Preoperative Sedation and Analgesia

Usual dosage is 2 mg administered 60–90 minutes before surgery.a

Supplement to Surgical Anesthesia

2 mg shortly before induction of anesthesia and/or 0.5–1 mg administered during anesthesia in increments up to 0.06 mg/kg (depending on previous administration of sedatives, analgesics, and hypnotic agents).a Usual total dose is 4–12.5 mg (approximately 0.06–0.18 mg/kg).a

Obstetric Analgesia
IV or IM

1–2 mg administered in patients at full term in early labor; may repeat after 4 hours.a Use alternative analgesia if delivery expected within 4 hours.a

Prescribing Limits



Maximum 4 mg as a single dose.a

Special Populations

Hepatic Impairment


Initially, 0.5 mg.113 If necessary, repeat dose at an interval of ≥6 hours.113


Initially, 1 mg.113 If necessary, repeat dose at an interval of ≥6 hours.113


Initially, 1 mg (1 spray in 1 nostril); may give an additional 1-mg dose within 90–120 minutes, if necessary.113 May repeat this initial dose sequence at an interval of ≥6 hours.113

Renal Impairment

Patients with renal impairment may receive the same IV, IM, or intranasal dosages as patients with hepatic impairment.113

Geriatric Patients

Geriatric patients may receive the same IV, IM, or intranasal dosages as patients with hepatic impairment.113

Cautions for Butorphanol Tartrate


  • Known hypersensitivity to butorphanol or benzethonium chloride (contained in the multiple-dose vials of the injection or in the nasal solution).a b



Abuse Potential

Possible tolerance, psychologic dependence, and physical dependence.a b d Episodes of abuse associated with all routes of administration, especially nasal administration.a b

Patients with a history of drug or alcohol dependence or abuse are at risk of habituation or dependence; use only with careful surveillance in such patients.a b

Patients Dependent on Opiates

Partial opiate antagonist; not recommended for use in patients physically dependent on opiatesa because of the potential to precipitate symptoms of withdrawal (e.g., anxiety, agitation, mood changes, hallucinations, dysphoria, weakness, diarrhea).128 129

Use with caution in patients who recently received repeated doses of opiate analgesics; allow an adequate period of withdrawal from opiates before initiation of butorphanol therapy.128 129

General Precautions

Head Injury and Increased Intracranial Pressure

Adverse effects of opiates may obscure the existence, extent, or course of intracranial pathology.113 Use in patients with head injury only if the potential benefits justify the possible risks.113

Respiratory Effects

Possible respiratory depression, especially in patients with impaired respiration caused by other drugs, uremia, severe infection, severely limited respiratory reserve, bronchial asthma, respiratory obstruction, or cyanosis.a b d Use with caution and in lower dosages in these patients.a b d

Cardiovascular Effects

Possible increased myocardial workload; use in patients with AMI, ventricular dysfunction, or coronary insufficiency only if the potential benefits justify the possible risks.a b

Severe hypertension reported rarely.a b If hypertension occurs, discontinue and administer a hypotensive agent as necessary; butorphanol-induced hypertension reportedly has been managed with naloxone in patients who were not opiate dependent.113

Use cautiously before surgery or anesthesia in hypertensive patients.d

Possible hypotension associated with syncope in patients receiving nasal solution; caution patients against performing activities that may pose risks if hypotension were to occur.113

CNS Depression

Performance of activities requiring mental alertness and physical coordination may be impaired.a b

Concurrent use of other CNS depressants may potentiate CNS depression.a b (See Specific Drugs under Interactions.)

Biliary Tract Surgery

Safe use in patients about to undergo biliary tract surgery has not been established; use with caution.d

Specific Populations


Category C.a b

Use of intranasal spray not recommended during labor and delivery.


Distributed into milk following parenteral administration, but not in clinically important amounts at usual therapeutic dosages.113

No experience with use of nasal solution in nursing women; estimated that amount of drug distributed into milk will be similar to that when administered parenterally.113 b

Pediatric Use

Safety and efficacy not established in children <18 years of age.a b

Geriatric Use

Select dosage with caution.113 (See Geriatric Patients under Dosage and Administration.)

Possible increased sensitivity to the drug in some geriatric individuals.113

Insufficient experience with the nasal solution in patients ≥65 years of age to determine whether geriatric patients respond differently than younger adults.b

Hepatic Impairment

Use with caution.a b (See Hepatic Impairment under Dosage and Administration.)

Renal Impairment

Use with caution.a b (See Renal Impairment under Dosage and Administration.)

Common Adverse Effects

Sedation, dizziness, nausea and/or vomiting.a b

Interactions for Butorphanol Tartrate

Not known whether drugs that affect hepatic microsomal enzymes may interfere with metabolism of butorphanol.113

Specific Drugs





Pharmacokinetic interaction unlikelyb

CNS depressants (e.g., alcohol, antihistamines, general anesthetics, hypnotics, phenothiazines, sedatives, tranquilizers, barbiturates)

Additive CNS effectsa b

Reduce dose and frequency of butorphanol administration113


Potential for decreased metabolism of butorphanol is unknown113 a b

Consider reducing dose and increasing interval between doses of butorphanol113 a b


Possible decreased rate of absorption of intranasal butorphanol; extent of absorption appears to be unchanged113 b

Slower onset of analgesic action if butorphanol is administered intranasally with or immediately after oxymetazoline113


Increased conjunctival changesd


Reduced analgesic effect of butorphanol nasal spray when administered shortly after sumatriptan nasal spray; possible increased BPb

Reduction in analgesic effect is minimal if butorphanol is administered≥30 minutes after sumatriptanb


Potential for decreased metabolism of butorphanol is unknown113 b

Consider reducing dose and increasing interval between doses of butorphanol113 b

Butorphanol Tartrate Pharmacokinetics



Rapidly absorbed following IM injection; peak plasma concentrations usually attained within 30–60 minutes.a d

Following nasal inhalation, peak blood concentrations are achieved in about 30–60 minutes.113 114 Absolute bioavailability of nasally administered butorphanol is 60–70% and appears to be unchanged in patients with allergic rhinitis.a

Completely absorbed from the GI tract following oral administration; however, after first-pass metabolism, bioavilability is only 5–17%.a b


Onset of analgesic activity occurs in a few minutes after IV administration or within 15 minutes after IM administration;a b peak analgesic effect achieved within 30–60 minutes after IV or IM administration.a

After nasal inhalation in postoperative patients, onset of analgesia occurs within 15 minutes;113 114 125 peak analgesic effect achieved within 1–2 hours.b


After IV or IM administration, duration of analgesia is 3–4 hours.a b

After nasal inhalation in postoperative patients, duration of analgesia is approximately 2.5–5 hours.113 114 125



Highest concentrations of butorphanol and its metabolites in animals are found in the liver, kidneys, and intestine; drug concentrations are higher in the lungs, spleen, heart, endocrine tissues, blood cells, and fat tissue than in plasma; brain concentrations are lower than plasma concentrations.d

Rapidly crosses the placenta and is distributed into milk.a b

Plasma Protein Binding

About 80%.a b



Extensively metabolized in the liver, principally by hydroxylation; N-dealkylation and conjugation of butorphanol and its metabolites also occur.a b d Metabolites have no analgesic activity.d

Elimination Route

Excreted prinicipally in urine (70–80%) mainly as metabolites; also excreted in feces (15%).a b


About 4.6–4.7 hours following intranasal or IV administration.113 114

Special Populations

In patients with hepatic impairment, elimination half-life of 16.8 hours reported.b

In patients with renal impairment (Clcr <30 mL/minute), elimination half-life of 10.5 hours reported.113

In geriatric individuals, elimination half-life reported to be about 5.6 hours (range 3.3–8.8 hours) or 6.6 hours (range: 3.8–9.2 hours) following IV or intranasal administration, respectively.113








15–30°C; protect from light.a


For information on systemic interactions resulting from concomitant use, see Interactions.

Drug Compatibility

Y-Site CompatibilityHID


Allopurinol sodium




Cefepime HCl


Dexmedetomidine HCl


Doxorubicin HCl liposome injection


Esmolol HCl

Etoposide phosphate

Fenoldopam mesylate


Fludarabine phosphate

Gemcitabine HCl

Granisetron HCl

Hetastarch in lactated electrolyte injection (Hextend)

Labetalol HCl


Melphalan HCl

Nicardipine HCl



Pemetrexed disodium

Piperacillin sodium–tazobactam sodium


Remifentanil HCl




Vinorelbine tartrate


Amphotericin B cholesteryl sulfate complex


Midazolam HCl


  • Analgesic effect is believed to result from an interaction with an opiate receptor site in the CNS (probably in or associated with the limbic system).a

  • Opiate antagonistic effect may result from competitive inhibition at the opiate receptor, but other mechanisms probably also are involved.d Butorphanol exerts antagonistic114 115 126 or partially antagonistic113 effects at μ opiate receptor sites; it appears to exerts agonistic effects principally at κ and Σ opiate receptors.101 102 103 104

  • Produces respiratory depression, sedation, miosis and, in animals, antitussive effect.a

  • Slightly increases pulmonary artery pressure, pulmonary wedge pressure, left ventricular end-diastolic pressure, systemic arterial pressure, pulmonary vascular resistance, and cardiac index.a

  • In animals, inhibits GI motility slightly, causes little increase in duodenal smooth muscle activity, and has little or no effect on bile duct flow.d

Advice to Patients

  • Potential for butorphanol to impair mental alertness or physical coordination; do not drive or operate machinery for ≥1 hour after receiving the drug or until effects on individual are known.a b

  • Patients receiving the nasal solution should not perform activities that may pose risks if hypotension were to occur.113

  • Importance of taking only as prescribed; do not increase dosage or duration of therapy unless otherwise instructed by a clinician.a b

  • Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs and alcohol consumption.a b Importance of avoiding alcohol while receiving the drug.a b

  • Importance of women informing their clinician if they are or plan to become pregnant or to breast-feed.a b

  • Importance of advising patients of other important precautionary information.a b (See Cautions.)


Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Subject to control under the Federal Controlled Substances Act of 1970 as a schedule IV (C-IV) drug.127 128 129

* available from one or more manufacturer, distributor, and/or repackager by generic (nonproprietary) name

Butorphanol Tartrate


Dosage Forms


Brand Names




1 mg/metered spray (10 mg/mL)*

Butorphanol Tartrate Nasal Spray (C-IV)

Mylan, Novex, Roxane

Stadol NS (C-IV)

Bristol-Myers Squibb, (also promoted by Cephalon)



1 mg/mL*

Butorphanol Tartrate Injection (C-IV; available as single-dose vials and prefilled syringes)

Apotex, Baxter, Bedford, Hospira, Mayne

Stadol (C-IV)


2 mg/mL*

Butorphanol Tartrate Injection (C-IV; available as single-dose vials, multiple-dose vials, and pre-filled syringes)

Apotex, Baxter, Bedford, Hospira, Mayne

Stadol (C-IV)


Comparative Pricing

This pricing information is subject to change at the sole discretion of DS Pharmacy. This pricing information was updated 02/2014. Actual costs to patients will vary depending on the use of specific retail or mail-order locations and health insurance copays.

Butorphanol Tartrate 10MG/ML Solution (MYLAN): 3/$56.99 or 8/$156.99

AHFS DI Essentials. © Copyright, 2004-2016, Selected Revisions August 1, 2007. American Society of Health-System Pharmacists, Inc., 7272 Wisconsin Avenue, Bethesda, Maryland 20814.


Only references cited for selected revisions after 1984 are available electronically.

100. The United States pharmacopeia, 21st rev, and The national formulary, 16th ed. Rockville, MD: The United States Pharmacopeial Convention, Inc; 1985:141-2.

101. Jaffe JH, Martin WR. Opioid analgesics and antagonists. In: Gilman AG, Goodman LS, Rall TW et al, eds. Goodman and Gilman’s the pharmacological basis of therapeutics. 7th ed. New York: Macmillan Publishing Company; 1985:491-531.

102. Martin WR. Pharmacology of opioids. Pharmacol Rev. 1983; 35:283-323. [IDIS 182771] [PubMed 6144112]

103. Zola EM, McLeod DC. Comparative effects and analgesic efficacy of the agonist-antagonist opioids. Drug Intell Clin Pharm. 1983; 17:411-7. [IDIS 171471] [PubMed 6861632]

104. Lewis JR. Evaluation of new analgesics: butorphanol and nalbuphine. JAMA. 1980; 243:1465-7. [IDIS 112206] [PubMed 7359723]

105. Evans WS, Bowen JN, Giordano FL et al. A case of Stadol dependence. JAMA. 1985; 253:2191-2. [IDIS 198247] [PubMed 3974108]

106. Smith SG, Davis WM. Nonmedical use of butorphanol and diphenhydramine. JAMA. 1984; 252:1010. [IDIS 188728] [PubMed 6748202]

107. Brown GR. Stadol dependence: another case. JAMA. 1985; 254:910. [IDIS 203557] [PubMed 4021020]

108. Austin RP. Diversion of butorphanol. Am J Hosp Pharm. 1983; 40:1306. [PubMed 6614013]

109. Hoover RC, Williams RB. Survey of butorphanol and nalbuphine diversion in U.S. hospitals. Am J Hosp Pharm. 1985; 42:1111-3. [PubMed 4003423]

110. Butorphanol. In: WHO Expert Committee on Drug Dependence. 25th report. Technical report series 775. Geneva: World Health Organization; 1989:24-6.

111. Preston KL, Bigelow GE, Liebson IA. Butorphanol-precipitated withdrawal in opioid-dependent human volunteers. J Pharmacol Exp Ther. 1988; 246:441-8. [IDIS 245408] [PubMed 2457074]

112. Preston KL, Bigelow GE, Liebson IA. Butorphanol-precipitated withdrawal in opioid-dependent human volunteers. NIDA Res Monogr. 1987; 76:157-61. [PubMed 2449617]

113. Mead Johnson. Stadol (butorphanol tartrate) injectable and Stadol NS (butorphanol tartrate) nasal spray prescribing information. Princeton, NJ; 1995 Jan.

114. Gillis JC, Benfield P, Goa KL. Transnasal butorphanol: a review of its pharmacodynamic and pharmacokinetic properties, and therapeutic potential in acute pain management. Drugs. 1995; 50:157-75. [PubMed 7588085]

115. Jaffe JH, Martin WR. Opioid analgesics and antagonists. In: Gilman AG, Rall TW, Nies AS et al, eds. Goodman and Gilman’s the pharmacological basis of therapeutics. 8th ed. New York: Pergamon Press; 1990:485-521.

116. Anon. Drugs for migraine. Med Lett Drugs Ther. 1995; 37:17-20. [PubMed 7862023]

117. Joyce TH, Kubicek MF, Skjonsby BS et al. Efficacy of transnasal butorphanol tartrate in postepisiotomy pain: a model to assess analgesia. Clin Ther. 1993; 15:160-7. [PubMed 8458045]

118. Shyu WC, Morgenthien EA, Pittman KA et al. The effects of age and sex on the systemic availability and pharmacokinetics of transnasal butorphanol. Eur J Clin Pharmacol. 1994; 47:57-60. [IDIS 339323] [PubMed 7988625]

119. Shyu WC, Pittman KA, Robinson DS et al. The absolute bioavailability of transnasal butorphanol in patients experiencing rhinitis. Eur J Clin Pharmacol. 1993; 45:559-62. [IDIS 326431] [PubMed 8157043]

120. Shyu WC, Mayol RF, Pfeffer M et al. Biopharmaceutical evaluation of transnasal, sublingual, and buccal disk dosage forms of butorphanol. Biopharm Drug Dispos. 1993; 14:371-9. [IDIS 317491] [PubMed 8218955]

121. Shyu WC, Pittman KA, Robinson D et al. Multiple-dose phase I study of transnasal butorphanol. Clin Pharmacol Ther. 1993; 54:34-41. [IDIS 319110] [PubMed 8330463]

122. Hoffert MJ, Couch JR, Diamond S et al. Transnasal butorphanol in the treatment of acute migraine. Headache. 1995; 35:65-9. [PubMed 7737863]

123. Bristol-Myers Squibb, Princeton, NJ: Personal communication.

124. Mead Johnson. Stadol NS (butorphanol tartrate) nasal spray patient instructions. Princeton, NJ; 1992.

125. Schwesinger WH, Reynolds JC, Harshaw DH et al. Transnasal butorphanol and intramuscular meperidine in the treatment of postoperative pain. Adv Ther. 1992; 9:123-9.

126. Chen JC, Smith ER, Cahill M et al. The opioid receptor binding of dezocine, morphine, fentanyl, butorphanol and nalbuphine. Life Sci. 1992; 52:389-96.

127. Code of federal regulations. Part 1308. Schedules of controlled substances, revised as of April 1, 1998.

128. Bristol-Myers Squibb. Stadol NS (butorphanol tartrate) nasal spray prescribing information. Priceton, NJ; 1999 May.

129. Bristol-Myers Squibb, Priceton, NJ: Personal communication.

130. Matchar DB, Young WB, Rosenberg JH et al. Evidence-based guidelines for migraine headache in the primary care setting: pharmacological management of acute attaks. St. Paul, MN; 2001. From the American Academy of Neurology web site: ().

a. Bedford Laboratories. Butorphanol tartrate injection prescribing information. Bedford OH; 1999 Dec.

b. Bristol-Myers Squibb. Stadol NS (butorphanol tartrate) nasal spray prescribing information. Priceton, NJ; 2002 Mar

HID. Trissel LA. Handbook on injectable drugs. 14th ed. Bethesda, MD: American Society of Health-System Pharmacists; 2007:233-7.

d. AHFS Drug Information 2004. McEvoy GK, ed. Butorphanol. Bethesda, MD: American Society of Health-System Pharmacists; 2004:2075-7.