Butorphanol (Solution) Instructions for Use

ATC Code

N02AF01 (Butorphanol)

Active Substance

Butorphanol (Rec.INN registered by WHO)

Clinical-Pharmacological Group

Opioid receptor agonist-antagonist. Analgesic

Pharmacotherapeutic Group

Opioid analgesic agent: opioid receptor agonist-antagonist

Pharmacological Action

Opioid analgesic, agonist-antagonist of opioid receptors. It is an agonist of kappa- and an antagonist of mu-opioid receptors.

It activates the endogenous antinociceptive system, mainly through kappa-opioid receptors, and thus disrupts interneuronal transmission of pain impulses at various levels of the CNS, and also changes the emotional coloring of pain by affecting the higher parts of the brain. The influence on sigma receptors causes some psychotomimetic action and the ability to sometimes cause dysphoria.

It has a sedative and central antitussive effect, excites the vomiting center, and causes miosis. To a lesser extent than mu-opioid receptor agonists (morphine, promedol, fentanyl), it depresses the respiratory center and affects gastrointestinal motility. An effect on hemodynamics (increased systolic and decreased diastolic pressure, increased pressure in the pulmonary artery), increased intracranial pressure is possible.

The drug has a rapid analgesic effect: with IV administration, the effect develops in 2-3 minutes, with IM administration – in 10-30 minutes. The maximum analgesic effect is achieved in 30-60 minutes, the duration of action with IM administration is 3-4 hours, with IV administration – 2-4 hours.

With controlled use, the likelihood of developing habituation and drug (opioid) dependence is very low.

Pharmacokinetics

It binds 80% to plasma proteins. C_max in blood plasma is 2.2 mg/ml. T_1/2 is 2.5-4 hours, in the elderly – 6.6 hours, in patients with severe renal impairment – 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 eliminated in feces. It penetrates the placental barrier and is found in breast milk.

Indications

• Severe pain syndrome of various origins (including in the pre-, intra-, and postoperative periods);
• For malignant neoplasms;
• During childbirth (in the absence of signs of intrauterine pathology in the fetus).

ICD codes

Dosage Regimen

Solution

It is prescribed IV or IM. Doses are selected individually depending on the age and condition of the patient.

For pain syndrome, 1 mg of the drug is administered IV or 2 mg IM every 3-4 hours as needed.

For premedication, 2 mg is administered IM 60-90 minutes before the start of surgery or the same dose IV immediately before surgery. When performing IV general anesthesia, 2 mg is administered IV before the administration of sodium thiopental, and then 0.5-1 mg is added to maintain the required depth of anesthesia. The total dose of analgesic required for general anesthesia ranges from 4 to 12.5 mg.

During childbirth, 1 mg or 2 mg of the drug is administered IM or IV to women in labor with a pregnancy of at least 37 weeks in the absence of signs of intrauterine pathology in the fetus.

It should not be administered more often than once every 4 hours, the last injection should be made no less than 4 hours before delivery.

In elderly patients, the dose is halved, and the interval between injections is increased to 6 hours.

Adverse Reactions

Drowsiness, dizziness, confusion, headache, feelings of anxiety, agitation, euphoria or dysphoria, hallucinations, tachycardia, decreased blood pressure, nausea, less often vomiting, dry mouth, decreased visual acuity, urinary retention, profuse sticky sweat, skin itching, slowed reaction speed.

Paresthesia, tremor, unusual dreams, increased blood pressure, rash. With repeated use in high doses, the possibility of drug dependence cannot be ruled out.

Contraindications

• Respiratory depression;
• CNS depression;
• Convulsions;
• Increased intracranial pressure;
• Traumatic brain injuries;
• Acute alcohol conditions and alcoholic psychosis;
• Hepatic and renal failure;
• Bronchial asthma;
• Heart failure;
• Acute myocardial infarction;
• Heart rhythm disturbances;
• Arterial hypertension;
• Acute surgical diseases of the abdominal organs before diagnosis;
• During treatment with MAO inhibitors and for another 14 days after their withdrawal;
• Drug dependence on morphine-like drugs (morphine, promedol, fentanyl).
• Age under 18 years;
• Pregnancy (except for preparation for childbirth and pain syndrome during childbirth);
• Lactation period;
• Hypersensitivity to butorphanol.

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

Use in Pregnancy and Lactation

Contraindicated in pregnancy (except for preparation for childbirth and pain syndrome during childbirth).

Pediatric Use

Contraindicated in children under 18 years of age.

Geriatric Use

In elderly patients, the dose is halved, and the interval between injections is increased to 6 hours.

With caution – elderly age (over 65 years).

Special Precautions

Emotionally unstable individuals, patients with a history of drug dependence should take measures aimed at complete elimination of the narcotic substance from the body before starting treatment with butorphanol.

During preparation for childbirth, it is prescribed subject to careful medical supervision.

Effect on ability to drive vehicles and mechanisms

During treatment, one should not engage in potentially hazardous activities requiring increased attention, speed of mental and motor reactions, and one should not consume ethanol.

Overdose

Symptoms: hypoventilation, hypothermia, arterial hypotension, cardiovascular insufficiency, stuporous or comatose state.

Treatment: maintaining adequate pulmonary ventilation, systemic hemodynamics and body temperature. In case of respiratory depression, IV administration of the specific opioid antagonist naloxone at a dose of 0.4-2 mg is possible. Patients should be under continuous observation. If necessary – artificial ventilation of the lungs.

Drug Interactions

Should not be combined with other opioid analgesics due to the danger of weakening analgesia and the possibility of provoking withdrawal syndrome in patients dependent on opioids.

Under careful observation and in reduced doses, it should be used against the background of general anesthetics, hypnotic drugs to avoid increased excessive CNS depression and suppression of respiratory center activity.

It enhances the effect of drugs that depress the CNS (barbiturates, anxiolytics, antipsychotic agents, histamine H₁-receptor blockers, ethanol).

Pharmaceutically incompatible with diazepam, barbiturates.

Local vasoconstrictors reduce the effectiveness of butorphanol with intranasal use.

Storage Conditions

List A. Store in a light-protected place, out of reach of children, at a temperature of 5°-30°C (41°-86°F). Do not allow freezing.

Shelf Life

Shelf life – 2 years.

Dispensing Status

The drug is dispensed by prescription.

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.