Butorphanol tartrate (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

An opioid analgesic from the group of opioid receptor agonist-antagonists, a phenanthrene derivative. It is an agonist of κ-class opioid receptors and a mixed antagonist of μ-opioid receptors.

It has an antitussive and sedative effect, stimulates the vomiting center, causes pupil constriction, and affects hemodynamics (increases systemic blood pressure, pulmonary artery pressure, left ventricular end-diastolic pressure, and systemic vascular resistance).

The analgesic effect occurs within minutes after intravenous administration, and within 10-15 minutes after intramuscular administration. The maximum effect develops within 30-60 minutes. The duration of action is 3-4 hours. In terms of intensity and duration of analgesic action, it is similar to morphine. Compared to morphine, it causes less respiratory depression and has a lower addictive potential.

With intranasal administration, the analgesic effect develops within 1-2 hours, and the duration of action is 4-5 hours.

Pharmacokinetics

After intramuscular administration, Butorphanol is well absorbed from the injection site. The maximum plasma concentration (C_max) is reached within 0.5-1 hour after intramuscular or intranasal administration. Plasma protein binding is about 80%. The elimination half-life (T_1/2) is about 3 hours. It is intensively metabolized in the liver by hydroxylation, N-dealkylation, and conjugation. It is excreted mainly in the urine, 5% unchanged, the rest as metabolites; 11-14% is excreted in the bile. It crosses the placental barrier and is excreted in breast milk.

Indications

Moderate and severe pain syndromes of various etiologies (including postoperative pain, during labor), premedication for general anesthesia, as a component of intravenous anesthesia.

ICD codes

Dosage Regimen

Determine the dosage individually based on the patient’s weight, severity of pain, and clinical response.

For intramuscular administration, the usual single dose is 2 mg. Administer every 3-4 hours as needed for pain relief. The dose may be increased to 4 mg for severe pain.

For intravenous administration, the usual single dose is 1 mg to 2 mg. Administer slowly over 3-5 minutes. Repeat doses every 3-4 hours as necessary.

For intranasal administration, the usual single dose is 1 mg (one spray in one nostril). For insufficient analgesia, a 2 mg dose (one spray in each nostril) may be used. The dosing interval is 3-4 hours.

For all routes, the maximum daily dose should generally not exceed 12 mg to 16 mg.

Reduce the initial dose by 50% in patients with renal impairment or hepatic impairment.

Initiate therapy at the lower end of the dosage range for elderly and debilitated patients.

Do not use in patients under 18 years of age.

Adverse Reactions

From the central and peripheral nervous system: drowsiness, dizziness, confusion; rarely – headaches, feeling of anxiety, euphoria, nervousness, paresthesia; in isolated cases – agitation, dysphoria, hallucinations, unusual dreams; with intranasal use, insomnia is possible.

From the digestive system: nausea, vomiting, dry mouth; rarely – epigastric pain.

From the cardiovascular system: rarely – increased heart rate, arterial hypotension; in isolated cases – arterial hypertension.

Allergic reactions: rarely – skin itching; in isolated cases – skin rash.

Other: increased sweating; rarely – blurred vision; in isolated cases – urination disorder; with intranasal use, swelling of the nasal mucosa is possible.

Contraindications

Severe impairment of liver and/or kidney function, pregnancy (except for preparation for childbirth), lactation (breastfeeding), hypersensitivity to butorphanol.

Use in Pregnancy and Lactation

Contraindicated during pregnancy and during lactation (breastfeeding).

During preparation for childbirth, it should be used with caution and under the condition of careful medical supervision. Data on the safety of butorphanol use during pregnancy before 37 weeks and during lactation are not available.

Butorphanol is excreted in breast milk.

Use in Hepatic Impairment

Contraindicated in severe liver function impairment.

In case of liver function impairment, dosage adjustment is required.

Use in Renal Impairment

Contraindicated in severe kidney function impairment.

In case of kidney function impairment, dosage adjustment is required.

Pediatric Use

Butorphanol is not recommended for use in patients under 18 years of age.

Geriatric Use

Dosage adjustment is required for elderly patients.

Special Precautions

Should not be used for abdominal pain of unclear etiology.

Not recommended for use in patients with drug dependence, as well as immediately after the use of narcotic drugs. In cases of extreme necessity, before using butorphanol in such patients, measures should be taken to completely remove the narcotic substance from the body.

Use with particular caution in patients with head injuries due to the threat of increased intracranial pressure.

In patients with respiratory depression of various origins, Butorphanol is used in low doses, only in case of extreme necessity and under the condition of careful monitoring by medical personnel.

In patients with arterial hypertension, Butorphanol may contribute to a moderate increase in systolic pressure.

Intranasal use of butorphanol at an initial dose of 2 mg is possible provided that the patient can be in a horizontal position due to the risk of drowsiness or dizziness (in such cases, Butorphanol should not be used additionally for 3-4 hours).

Butorphanol is not recommended for use in patients under 18 years of age.

In case of impaired liver and/or kidney function, as well as in elderly patients, dosage adjustment is required.

Avoid simultaneous consumption of alcohol.

Effect on ability to drive vehicles and operate machinery

During treatment, one should not engage in potentially hazardous activities that require increased attention and speed of psychomotor reactions.

Drug Interactions

With simultaneous use, Butorphanol enhances the effect of drugs that depress the central nervous system (barbiturates, tranquilizers, histamine H₁-receptor blockers, ethanol and ethanol-containing drugs).

With simultaneous use with MAO inhibitors, there is a high risk of developing severe adverse reactions.

Vasoconstrictor agents for topical use reduce the effectiveness of butorphanol when administered intranasally.

Butorphanol is pharmaceutically incompatible with diazepam and barbiturates.

Storage Conditions

Store at 2°C (36°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

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.