Vero-Butorphanol (Solution) Instructions for Use

Marketing Authorization Holder

Veropharm, JSC (Russia)

ATC Code

N02AF01 (Butorphanol)

Active Substance

Butorphanol (Rec.INN registered by WHO)

Dosage Form

Vero-Butorphanol

Solution for intravenous and intramuscular administration 2 mg/1 ml: amp. 10 pcs.

Dosage Form, Packaging, and Composition

1 ml – ampoules (5) – contour cell packaging (2) – cardboard packs.

Clinical-Pharmacological Group

Opioid receptor agonist-antagonist. Analgesic

Pharmacotherapeutic Group

Opioid analgesic agent: opioid receptor agonist-antagonist

Pharmacological Action

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

It has an antitussive and sedative effect, stimulates the vomiting center, causes pupillary 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 a few 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 close to morphine. Compared to morphine, it causes less respiratory depression and has a lower addictive potential.

With intranasal use, 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. C_max in blood plasma is reached 0.5-1 hour after intramuscular or intranasal administration. Plasma protein binding is about 80%. 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 syndrome 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 clinical situation and pain severity.

For intramuscular administration, administer a single dose of 2 mg. If analgesia is inadequate, increase the single dose to a maximum of 4 mg.

For intravenous administration, administer a single dose of 1 mg to 2 mg.

Repeat doses as needed, maintaining an interval of 3 to 4 hours between administrations.

For premedication before anesthesia, administer 2 mg intramuscularly 60-90 minutes before surgery.

As a component of balanced anesthesia, administer an initial intravenous dose of 2 mg, with supplemental doses of 1 mg as required.

For intranasal use, administer a single dose of 1 mg to 2 mg.

Adjust the dose for elderly patients and for patients with impaired hepatic or renal function; initiate therapy at the lower end of the dosing range.

Do not exceed the maximum recommended single and daily doses. Monitor patients for respiratory depression, especially during the initial dosing period and after dose increases.

Adverse Reactions

From the central nervous system 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 – urinary 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. There are no data on the safety of butorphanol use during pregnancy before 37 weeks and during lactation.

Butorphanol is excreted in breast milk.

Use in Hepatic Impairment

Contraindicated in severe liver function impairment.

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

Use in Renal Impairment

Contraindicated in severe kidney function impairment.

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

Pediatric Use

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

Geriatric Use

Elderly patients require dose adjustment.

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 extreme caution in patients with traumatic brain injury due to the threat of increased intracranial pressure.

In patients with respiratory depression of various origins, Butorphanol is used in low doses, in case of extreme necessity and under the condition of careful supervision 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 applied 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, dose adjustment is required.

Avoid simultaneous consumption of alcohol.

Effect on the 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.