Universal reference book for medicines
Product name: BUTORPHANOL

Active substance: butorphanol

Type: Opioid receptor antagonist.
N.А. Semashko OJSC (Russia)
Composition, form of production and packaging
Solution for injection 0.2%
colorless, transparent or slightly opalescent.

1 ml

Butorphanol tartrate 2 mg

Excipients: citric acid, sodium citrate, sodium chloride, trilon B, water d / u.

1 ml - ampoules (5) - packings of cellular contour (1) - packs cardboard.

1 ml - ampoules (5) - packings the cellular contour (2) - packs cardboard.


The product description was approved by the manufacturer for the 2009 print edition.


Opioid analgesic, opioid receptor antagonist agonist.
It is an agonist kappa and antagonist of mu-opioid receptors.
Activates the endogenous antinociceptive system, mainly through the kappa-opioid receptors, and thus disrupts the interneuronal transmission of pain impulses at various levels of the central nervous system, and also changes the emotional color of the pain, affecting the higher parts of the brain.
The effect on sigma-receptors is due to some psychotomimetic action and the ability to sometimes cause dysphoria.
Has a sedative and central antitussive action, excites the vomiting center, causes miosis.
To a lesser extent than agonists of mu-opioid receptors (morphine, promedol, fentanyl) depresses the respiratory center and affects the motility of the gastrointestinal tract. Possible influence on hemodynamics (increased systolic and reduced diastolic pressure, increased pulmonary artery pressure), increased intracranial pressure.
The drug has a rapid analgesic effect: with IV introduction, the effect develops in 2-3 minutes, with the / m introduction - after 10-30 minutes.
The maximum analgesic effect is achieved in 30-60 minutes, the duration of action is at iv injection 3-4 hours, with iv introduction - 2-4 hours.
With controlled use, the likelihood of developing addiction and drug (opioid) dependence is very small.


With blood plasma proteins 80% are associated.
C max in blood plasma is 2.2 mg / ml. T 1/2 is 2.5-4 h, in the elderly it is -6.6 h, in patients with severe renal dysfunction is more than 10 hours. About 5% of the drug is excreted in the urine unchanged, 70-80% - in the form of metabolites, the remainder is excreted with bile and is excreted with feces. It penetrates the placental barrier and is found in breast milk.

- pronounced pain syndrome of different origin (including preoperative, operational and postoperative periods);

- with malignant neoplasms;

- at delivery (in the absence of fetus signs of intrauterine pathology).


Assign IV or IM.
Doses are selected individually depending on the age and condition of the patient.
With pain syndrome , 1 mg of IV preparation or 2 mg IM is administered every 3-4 hours as needed.

For premedication, 2 mg IM is administered 60-90 minutes before surgery or the same dose of IV immediately before surgery.
In an IV general anesthetic, 2 mg is administered iv before sodium thiopental, and then 0.5-1 mg is added to maintain the necessary anesthetic depth. The total dose of analgesic required for general anesthesia is 4 to 12.5 mg.
At the time of delivery, 1 mg or 2 mg of the drug is injected in / m or intravenously into the parturient women with a gestation period of at least 37 weeks if the fetus has no signs of intrauterine pathology.

Do not administer more than 1 time in 4 hours, the last injection should be done at least 4 hours prior to delivery.

In elderly patients, the dose is reduced by half, and the interval between injections increases to 6 hours.


Drowsiness, dizziness, confusion, headache, feelings of anxiety, excitement, euphoria or dysphoria, hallucinations, tachycardia, decreased blood pressure, nausea, less often vomiting, dry mouth, decreased visual acuity, impaired urination, copious sweat, itchy skin, slowing reaction rate.

Paresthesia, tremor, unusual dreams, increased blood pressure, rash.
At repeated application in high doses the possibility of development of drug dependence is not excluded.

- respiratory depression;

- depression of the central nervous system;

- convulsions;

- increased intracranial pressure;

- craniocerebral trauma;

- acute alcoholic conditions and alcoholic psychosis;

- hepatic and renal insufficiency;

- bronchial asthma;

- heart failure;

acute myocardial infarction;

- violation of the rhythm of the heart;

- arterial hypertension;

- acute surgical diseases of the abdominal cavity before diagnosis;

- against treatment with MAO inhibitors and for another 14 days after their withdrawal;

- drug dependence on morphine-like drugs (morphine, promedol, fentanyl).

- age up to 18 years;

- Pregnancy (except preparation for childbirth and pain in labor);

- lactation period;

- hypersensitivity to butorphanol.

With caution - patients with general exhaustion, elderly age (over 65 years).


Contraindicated in pregnancy (except for the preparation for childbirth and pain in labor).


Contraindicated in children under the age of 18 years.


In elderly patients, the dose is reduced by half, and the interval between injections increases to 6 hours.

With caution - the elderly (over 65 years).


Emotionally unstable people, patients with drug dependence in history before starting treatment with butorphanol should take measures aimed at complete removal of the drug from the body.

In the period of preparation for childbirth appoint, subject to careful medical supervision.

Impact on the ability to drive vehicles and manage mechanisms

During treatment, do not engage in potentially hazardous activities that require increased attention, speed of mental and motor reactions, do not use ethanol.


Symptoms: hypoventilation, hypothermia, arterial hypotension, cardiovascular failure, stupor or coma.

Treatment: maintenance of adequate pulmonary ventilation, systemic hemodynamics and body temperature.
With respiratory depression, the administration of a specific opioid naloxone antagonist at a dose of 0.4-2mg is possible. Patients should be under continuous supervision. If necessary, ventilation.

It should not be combined with other opioid analgesics because of the danger of weakening analgesia and the possibility of provoking a withdrawal syndrome in patients with opioid dependence.

Under careful supervision and in reduced doses should be used against the background of the means for general anesthesia, hypnotics in order to avoid the increase of excessive CNS suppression and suppression of the activity of the respiratory center.

Enhances the effect of drugs that depress the central nervous system (barbiturates, anxiolytics, antipsychotics, blockers of histamine H 1 -receptors, ethanol).

Pharmaceutically incompatible with diazepam, barbiturates.

Local vasoconstrictors decrease the efficacy of butorphanol with intranasal application.


The drug is released by prescription.


List A. Store in a place protected from light, out of reach of children, at a temperature of 5 ° -30 ° C.
Do not freeze. Shelf life - 2 years.
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