Butorphanol

Table of contents

  • Brand Names
  • Chemistry
  • Pharmacologic Category
  • Mechanism of Action
  • Therapeutic Use
  • Pregnancy and Lactation Implications
  • Contraindications
  • Warnings and Precautions
  • Adverse Reactions
  • Toxicological Effects
  • Caution and personalized dose adjustment in patients with the following genotypes
  • Other genes that may be involved
  • Drug Interactions
  • Nutrition/Nutraceutical Interactions
  • Dosage
  • Pharmacokinetics and Pharmacodynamics
  • Special Considerations

Brand Names

Europe

Denmark: Dolorex; Finland: Butordol; Greece: Anpiral, Stadol; Poland: Beforal, Moradol, Stadol.

North America

Canada: Butorphanol; USA: Butorphanol, Stadol.

Latin America

Mexico: Stadol.

Asia

Japan: Stadol.

Drug combinations

Chemistry

Butorphanol Tartrate: C~21~H~29~NO~2~ C~4~H~6~O~6~. Mw: 477.55. (1) Morphinan-3,14-diol, 17-(cyclobutylmethyl)-, (-)-, [S-(R*,R*)]-2,3-dihydroxybutanedioate (1:1); (2)(-)-17-(Cyclobutylmethyl)morphinan-3,14-diol D-(-)-tartrate (1:1). CAS-58786-99-5; CAS-42408-82-2 (butorphanol)(1976).

Pharmacologic Category

Analgesics and Antipyretics; Opiate Partial Agonists. (ATC-Code: N02AF01).

Mechanism of action

Mixed narcotic agonist-antagonist with central analgesic actions. Binds to opiate receptors in the CNS (limbic system), causing inhibition of ascending pain pathways, altering the perception of and response to pain. Produces generalized CNS depression. Opiate antagonistic effect may result from competitive inhibition at the opiate receptor, but other mechanisms are probably also involved. It appears to exert agonistic effects principally at κ- and Σ- opiate receptors.

Therapeutic use

Management of moderate-to-severe pain (cancer, neuropathic or spastic conditions, orthopedic problems, burns, renal colic). Preoperative medication. Supplement to balanced anesthesia. Management of pain during labor.

Pregnancy and lactiation implications

There are no adequate studies using butorphanol in pregnant women, and the drug should be used during pregnancy only when the potential benefits justify the possible risk to the fetus. Use of the nasal preparation is not recommended during labor and delivery (absence of clinical experience). Use caution during lactation.

Unlabeled use

Contraindications

Hypersensitivity to butorphanol or any component of the formulation. Avoid use in opiate-dependent patients who have not been detoxified (may precipitate opiate withdrawal). Pregnancy (prolonged use or high doses at term).

Warnings and precautions

May cause CNS depression. May cause hypotension (caution in hypovolemia, cardiovascular disease, or drugs which may exaggerate hypotensive effects). May obscure diagnosis or clinical course of acute abdominal conditions. Use with caution in adrenal insufficiency, including Addison’s disease. Use with caution in biliary tract dysfunction. Use with caution in history of drug abuse or acute alcoholism (risk of drug dependency; tolerance, psychological and physical dependence may occur). Use with extreme caution in head injury, intracranial lesions, or elevated intracranial pressure (may elevate intracranial pressure). Use with caution in hepatic and renal impairment. Use with caution in prostatic hyperplasia and/or urinary stricture. Use with caution in morbidly obese patients. Use with caution in pre-existing respiratory compromise (hypoxia and/or hypercapnia), COPD or other obstructive pulmonary disease, and kyphoscoliosis or other skeletal disorder which may alter respiratory function (critical respiratory depression may occur). Use with caution in thyroid dysfunction. Concurrent use of sumatriptan nasal spray and butorphanol nasal spray may increase risk of transient high blood pressure. Use with caution in debilitated patients (risk of critical respiratory depression). Caution in the elderly (higher sensitivity to adverse effects). Concurrent use of agonist/antagonist analgesics may precipitate withdrawal symptoms and/or reduced analgesic efficacy following prolonged therapy with µ-opioid agonists. Abrupt discontinuation following prolonged use may also lead to withdrawal symptoms. Episodes of abuse associated with all routes of administration, especially nasal administration. Use with caution in patients who recently received repeated doses of opiate analgesics. Possible increased myocardial workload (use in patients with acute myocardial infarction, ventricular dysfunction, or coronary insufficiency only if the potential benefits justify the possible risks). Severe hypertension reported rarely. Use cautiously before surgery or anesthesia in hypertensive patients. Possible hypotension associated with syncope in patients receiving nasal solution.

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