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

Pharmacodynamics:Opioid analgesic 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 comes immediately, the maximum effect - in a few minutes; after intramuscular injection, the effect occurs after 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 frequently than other narcotic analgesics causes constipation. Has antitussive and sedative effect, stimulates the vomiting center, causes a narrowing of the pupils, increases systemic arterial pressure, pressure in the pulmonary artery, the diastolic volume of the left ventricle and the overall peripheral vascular resistance.

Pharmacokinetics:Absorption from the site of intramuscular injection is high. The time required to reach the maximum concentration in the plasma is 20-40 min, the maximum concentration is 2.2 ng / ml; connection with plasma proteins - 80%. Penetrates through blood-brain and placental barriers, penetrates into breast milk (concentration in the breast milk of the mother, after intramuscular injection 2 mg 4 times a day - 4 μg / l). Metabolised in the liver. The half-life in young patients is 4.7 hours, in the elderly it is 6.6 hours, in patients with renal insufficiency it is 10.5 hours.

It is excreted by the kidneys, mainly in the form of metabolites - 70-80% (5% unchanged), through the intestine - 15%.

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, age under 18 years (efficacy and safety not established).

Carefully:Drug dependence, craniocerebral trauma, intracranial hypertension, respiratory failure, hepatic and / or renal failure, chronic heart failure, acute myocardial infarction, coronary insufficiency, arterial hypertension, advanced age (over 65 years).

Dosing and Administration:

With pain syndrome - 1 mg intravenously or 2 mg intramuscularly every 3-4 hours (or as needed). In elderly patients and in patients with hepatic renal failure, the dose is reduced by a factor of 2, and the interval between injections increases to 6 hours.

For premedication appoint 2 mg intramuscularly for 60-90 min before the operation or 2 mg intravenously immediately before surgery.

When conducting an intravenous general anesthesia - 2 mg before the administration of sodium thiopental, then the anesthesia is maintained by repeated intravenous injections of 0.5-1 mg. The total dose required for anesthesia is 4-12.5 mg. During labor, 1-2 mg intramuscularly or intravenously to women with a gestation period of at least 37 weeks (in the absence of signs of intrauterine pathology in the fetus) and no more than once in 4 hours, the last injection should be made no later than 4 hours before estimated time of delivery.

Side effects:

Most often: drowsiness (43%), dizziness (19%), nausea or vomiting (13%).

FROM frequency of 1% or more: from the cardiovascular system - symptoms of vasodilation, palpitations.

From the nervous system: anxiety, confusion, euphoria, insomnia, nervousness, paresthesia, drowsiness, tremor.

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

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

From the skin: increased sweating, itching.

Other: asthenia, lethargy, headache; feeling of hot.

With a frequency of less than 1%: from the cardiovascular system - lowering blood pressure, fainting; communication with taking the drug is not established - increased blood pressure, tachycardia, pain in the chest.

From the nervous system: unusual dreams, agitation, dysphoria, hallucinations, hostility, vertigo, withdrawal syndrome, communication with the drug is not established - depression.

From the skin: rash, hives.

From the urinary system: decrease in urination.

From the respiratory system: communication with the drug is not established - shallow breathing.

The frequency is unknown (postmarketing observations, in addition): apnea, convulsions, delirium, drug dependence, transient difficulty in speech and movement (associated with excessive drug effects).

Overdose:

Symptoms of acute and chronic overdose: 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 of consciousness, respiratory arrest, coma.

Treatment: maintenance of sufficient pulmonary ventilation, systemic hemodynamics, normal body temperature. Patients should be under continuous supervision; If necessary, performing artificial ventilation; application of an opioid receptor antagonist - naloxone.

Interaction:

Strengthens the effect of drugs that depress the central nervous system (barbiturates, anxiolytics, antipsychotic drugs, H1-histamine receptor blockers, ethanol, muscle relaxants, other narcotic analgesics).

Pharmaceutically incompatible with diazepam, barbiturates. Medicines with anticholinergic activity, antidiarrhoeal drugs (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 ganglion blockers, diuretics).

Buprenorphine (incl.previous therapy) reduces the effect of other opioid analgesics; against the background of the use of low doses of agonists mu-or kappa-opioid receptors can enhance respiratory depression. Reduces the effect of metoclopramide.

With caution should be used simultaneously with monoamine-sidase inhibitors because of possible overexcitation or inhibition with the occurrence of hyper- or hypotensive crises (first, to assess the interaction effect, the dose should be reduced to 1/4 of the recommended one).

Naloxone reduces the effect of opioid analgesics, as well as the respiratory depression caused by them by the noncentral nervous system; may require large doses to level the effects of butorphanol, nalbuphine and pentazocine, which have been prescribed to eliminate the undesirable effects of other opioid analgesics; can accelerate the appearance of symptoms of "withdrawal syndrome" against the background of drug dependence.

Naltrexone accelerates the appearance of symptoms of "withdrawal syndrome" against the background of drug dependence (symptoms can appear only 5 minutes after drug administration, continue for 48 hours, are characterized by persistence and difficulty of their elimination); reduces the effect of opioid analgesics(analgesic, antidiarrheal, antitussive); does not affect the symptoms caused by the histamine reaction.

It does not prevent or alleviate the symptoms of the withdrawal syndrome with drug dependence (including fentanyl).

Special instructions:

In patients with drug dependence before the start of treatment should take measures aimed at complete removal of the drug from the body. In experimental studies, there was no teratogenic effect, but the risk of intrauterine fetal death in rats and rabbits increased.

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

It should be borne in mind that children under 2 years are more sensitive to the effects of opioid analgesics, and that they may experience paradoxical reactions. Butorphanol, administered at a dose of 2 mg intramuscularly, is equivalent to the administration of 10 mg of morphine by intramuscular injection.

Does not affect the reception of images of bile ducts. Does not cause a change in the activity of plasma amylase and lipase. Stimulates the work of the myocardium (caution should be used in case of myocardial infarction).

While using butorphanol, alcohol intake is not recommended.

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 per ampoule of light-protective glass brand SNS-1 (light-protective neutral glass, corresponding to the brand SNS-1). 10 ampoules are placed in a box of cardboard

5 ampoules are placed in a contour mesh box made of a polyvinylchloride film and foil of aluminum printed lacquered or without foil. 1 or 2 contour squares are placed in a pack of cardboard. In each pack, the box is attached instructions for use, the ampullar scarifier.

When using ampoules with a kink ring or with a notch and a dot the ampoule scaper is not inserted.

Storage conditions:List A. In the dark place at a temperature of 10 to 25 ° C. Keep out of the reach of children.

Shelf life:

2 years.

Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LS-000703

Date of registration:07.07.2010

Expiration Date:Unlimited

The owner of the registration certificate:SYNTHESIS, OJSC SYNTHESIS, OJSC Russia

Manufacturer: & nbsp

SYNTHESIS, OJSC Russia

Information update date: & nbsp13.03.2017

Illustrated instructions

Instructions

Butorphanol (Butorphanol)