Butorphanolum

Butorphanolum Uses, Dosage, Side Effects, Food Interaction and all others data.

A synthetic morphinan analgesic with narcotic antagonist action. It is used in the management of severe pain.

Butorphanolum is a synthetic opioid agonist-antagonist analgesic with a pharmacological and therapeutic profile that has been well established since its launch as a parenteral formulation in 1978. The introduction of a transnasal formulation of butorphanol represents a new and noninvasive presentation of an analgesic for moderate to severe pain. This route of administration bypasses the gastrointestinal tract, and this is an advantage for a drug such as butorphanol that undergoes significant first-pass metabolism after oral administration. The onset of action and systemic bioavailability of butorphanol following transnasal delivery are similar to those after parenteral administration. Butorphanolum blocks pain impulses at specific sites in the brain and spinal cord.

Butorphanolum
Uses
Dosage
Side Effect
Precautions
Interactions
Uses during Pregnancy
Uses during Breastfeeding
Accute Overdose
Food Interaction
Half Life
Volume of Distribution
Clearance
Interaction With other Medicine
Contradiction
Storage

Trade Name	Butorphanolum
Availability	Prescription only
Generic	Butorphanol
Butorphanol Other Names	Butorfanol, Butorphanol, Butorphanolum
Related Drugs	Buprenex, aspirin, acetaminophen, tramadol, naproxen, Tylenol, oxycodone, fentanyl, lidocaine, ketamine
Type
Formula	C₂₁H₂₉NO₂
Weight	Average: 327.4605 Monoisotopic: 327.219829177
Protein binding	Serum protein binding is approximately 80%.
Groups	Approved, Illicit, Vet approved
Therapeutic Class
Manufacturer
Available Country
Last Updated:	September 19, 2023 at 7:00 am

Uses

Butorphanolum is an opioid agonist-antagonist used to treat moderate to severe pain.

For the relief of moderate to severe pain.

Butorphanolum is also used to associated treatment for these conditions: Pain, Perioperative Pain, Severe Pain

How Butorphanolum works

The exact mechanism of action is unknown, but is believed to interact with an opiate receptor site in the CNS (probably in or associated with the limbic system). The opiate antagonistic effect may result from competitive inhibition at the opiate receptor, but may also be a result of other mechanisms. Butorphanolum is a mixed agonist-antagonist that exerts antagonistic or partially antagonistic effects at mu opiate receptor sites, but is thought to exert its agonistic effects principally at the kappa and sigma opiate receptors.

Toxicity

The clinical manifestations of butorphanol overdose are those of opioid drugs in general. The most serious symptoms are hypoventilation, cardiovascular insufficiency, coma, and death.

Food Interaction

Avoid alcohol.

Butorphanolum Alcohol interaction

[Moderate] GENERALLY AVOID:

Ethanol may potentiate the central nervous system (CNS) depressant effects of opioid analgesics.

Concomitant use may result in additive CNS depression and impairment of judgment, thinking, and psychomotor skills.

In more severe cases, hypotension, respiratory depression, profound sedation, coma, or even death may occur.

Concomitant use of opioid analgesics with ethanol should be avoided.

Butorphanolum Hypertension interaction

[Moderate] Butorphanolum may increase blood pressure and rarely causes severe hypertension.

Therapy with butorphanol should be administered cautiously in hypertensive patients, particularly when given before surgery or anesthesia.

Butorphanolum Drug Interaction

Major: zolpidem, zolpidem, acetaminophen / butalbital / caffeine, acetaminophen / butalbital / caffeine, clonazepam, clonazepam, pregabalin, pregabalin, alprazolam, alprazolamModerate: duloxetine, duloxetine, promethazine, promethazine, topiramate, topiramateUnknown: esomeprazole, esomeprazole, cholecalciferol, cholecalciferol

Butorphanolum Disease Interaction

Major: impaired GI motility, infectious diarrhea, liver disease, prematurity, gastrointestinal obstruction, acute MI, drug dependence, intracranial pressure, respiratory depressionModerate: hypertension, hypotension, adrenal insufficiency, biliary spasm, hypothyroidism, renal dysfunction, seizure disorders, urinary retention

Volume of Distribution

305 to 901 L

Elimination Route

Rapidly absorbed after intramuscular injection and peak plasma levels are reached in 20-40 minutes. The absolute bioavailability is 60-70% and is unchanged in patients with allergic rhinitis. In patients using a nasal vasoconstrictor (oxymetazoline) the fraction of the dose absorbed was unchanged, but the rate of absorption was slowed. Oral bioavailability is only 5-17% because of extensive first-pass metabolism.

Half Life

The elimination half-life of butorphanol is about 18 hours. In renally impaired patients with creatinine clearances <30 mL/min the elimination half-life is approximately doubled. After intravenous administration to patients with hepatic impairment, the elimination half-life of butorphanol was approximately tripled.