Butorphanol - instructions for use, dose, side effects, contraindications

Butorphanol is an opioid analgesic for parenteral administration from the group of mixed opioid receptor agonist-antagonists (stimulates kappa and sigma receptors, blocks mu receptors). By the expression of analgesic action is similar to morphine.After intravenous administration, the effect occurs immediately, the maximum effect is 10-15 minutes, the maximum activity is 30-60 minutes, the duration of the action is 3-4 hours. To a lesser extent than morphine, depresses breathing, has a lower narcogenic potential, less often than other opioids, causes constipation. It has antitussive and sedative action, stimulates the vomiting center, causes pupils to narrow, increases systemic arterial pressure, pulmonary artery pressure, left ventricular end-diastolic volume and overall peripheral vascular resistance.

Pharmacokinetics:The drug is rapidly absorbed into the systemic bloodstream from the site of intramuscular injection. The maximum concentration in plasma is reached in 20-40 minutes. The binding with plasma proteins is 80%. The drug penetrates through blood-brain and placental barriers, and also excretes in breast milk; is metabolized in the liver. It is excreted mainly in the form of metabolites with urine (70-80%) and with feces (15%); in unchanged form - with urine (5%). The half-life in young patients is 4.7 hours, in the elderly - 6.6 hours, in patients with severe renal dysfunction - 10.5 hours.

Indications:Pain syndrome of different genesis (medium and strong intensity); premedication before general anesthesia; as a component for intravenous general anesthesia; anesthesia during childbirth.

Contraindications:Hypersensitivity, pregnancy (except for anesthesia of childbirth), lactation.

Carefully:Drug addiction, craniocerebral trauma, intracranial hypertension, respiratory failure, hepatic and / or renal failure, chronic heart failure, acute myocardial infarction, coronary insufficiency, arterial hypertension, age 18 years (efficacy and safety not established), advanced age ( over 65 years of age).

Dosing and Administration:

With pain syndrome it is recommended to administer 1 mg intravenously or 2 mg intramuscularly every 3-4 hours as needed. In elderly patients, as well as in patients with impaired liver and kidney function, the dose should be reduced by half, and the interval between injections should be at least 6 hours. The usual dose prescribed for premedication, is 2 mg intramuscularly for 60-90 min before surgery or 2 mg intravenously immediately before surgery.

When conducting intravenous general anesthesia Enter 2 mg of butorphanol intravenously before administering drugs for general anesthesia, and then add 0.5-1.0 mg of the drug to maintain the necessary depth of anesthesia. The total dose required for general anesthesia is usually from 4 mg to 12.5 mg.

During childbirth recommend injecting 1 mg or 2 mg intramuscularly or intravenously to parturient women with a gestation period of at least 37 weeks (if the fetus lacks signs of intrauterine pathology). Butorphanol Do not enter more often than once in 4 hours, the last injection should be done at least 4 hours before the delivery.

Doses for children under 18 years are not established.

Side effects:

From the nervous system: anxiety, dizziness, confusion, euphoria, insomnia, nervousness, paresthesia, drowsiness, tremor, unusual dreams, agitation, dysphoria, hallucinations, hostility, vertigo, withdrawal syndrome.

From the cardiovascular system: decrease in blood pressure (1%), fainting.

From the digestive system: anorexia, constipation, dryness of the oral mucosa, pain in the epigastric region.

From the urinary system: decrease in urination.

From the respiratory system: possible difficulty breathing.

From the sense organs: blurred vision, pain in the eyes, ringing in the ears.

From the skin: increased sweating, itching.

Other: asthenia, lethargy, headache, a feeling of heat.

With prolonged repeated use of butorphanol in high doses, the possibility of developing drug dependence is not ruled out.

Overdose:Symptoms: cold sticky sweat, confusion, dizziness, drowsiness, lowering of blood pressure, nervousness, fatigue, bradycardia, severe weakness, slow labored breathing, hypothermia, anxiety, miosis, convulsions, hypoventilation, cardiovascular failure, in severe cases - loss consciousness, stopping breathing, coma.

Treatment: maintenance of sufficient pulmonary ventilation, systemic hemodynamics, normal body temperature. Patients should be under continuous supervision; If necessary - carrying out artificial ventilation (IVL); the use of specific antagonists of opioid receptors (for example, naloxone in a dose of 0.4 to 2 mg).

Interaction:Enhances the effect of drugs that depress the central nervous system (barbiturates, anxiolytics, antipsychotic drugs, H1-histamine receptor blockers, ethanol, muscle relaxants, other opioids). Pharmaceutically incompatible with diazepam, barbiturates. Antidiarrhoeal medicines (incl. loperamide) increase the risk of constipation up to intestinal obstruction, urinary retention and central nervous system depression. Strengthens the hypotensive effect of drugs that reduce blood pressure (including ganglioblocators, diuretics). Reduces the effect of metoclopramide. Caution should be applied simultaneously with monoamine oxidase (MAO) inhibitors because of the possibility of hyper or hypotensive crises (first, to assess the interaction effect, the dose of butorphanol should be reduced to 1/4 of the recommended one). The drug should not be combined with other narcotic analgesics because of the possibility of provoking a withdrawal syndrome in patients with dependence on opioids.

Special instructions:

In patients with drug dependence before the start of treatment should take action,aimed at the complete elimination of the drug from the body.

During treatment should not be consumed ethanol.

Effect on the ability to drive transp. cf. and fur:During treatment, do not engage in potentially hazardous activities that require increased attention, rapidity of mental and motor reactions.

Form release / dosage:

Solution for intravenous and intramuscular injection 2 mg / ml.

Packaging:

1 ml in the ampoules are glass.

5 ampoules are placed in a contour mesh box made of a polyvinylchloride film and aluminum foil.

For 1 or 2 contour mesh packages together with the instruction for use and the ampoule scarifier are placed in a pack of cardboard.

When using ampoules with a break ring, it is allowed to pack the ampoules without an ampoule scarifier.

Storage conditions:In a dark place at a temperature of no higher than 25 ° C. Keep out of the reach of children.

Shelf life:

3 years.

Do not use after the expiration date stated on the package.

Terms of leave from pharmacies:On prescription

Registration number:П N016247 / 01

Date of registration:25.02.2010 / 03.06.2015

Expiration Date:Unlimited

The owner of the registration certificate:BELMEDPREPARATY, RUP BELMEDPREPARATY, RUP Republic of Belarus

Manufacturer: & nbsp

BELMEDPREPARATY, RUP Republic of Belarus

Information update date: & nbsp13.03.2017

Illustrated instructions

Instructions

Butorphanol (Butorphanol)