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

Composition:1 ml of the solution contains 2 mg of butorphanol tartrate as the active substance; auxiliary substances - citric acid, sodium citrate, sodium chloride, disodium edetate (Trilon B), water for injection.

Description:

Transparent colorless liquid.

Pharmacotherapeutic group:An analgesic opioid: an opioid receptor agonist-antagonist

ATX: & nbsp

N.02.A.F.01 Butorphanol

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. Has antitussive and sedative effect, stimulates the vomiting center, causes a narrowing of the pupils, raises blood pressure, the end diastolic pressure in the left ventricle, and the general peripheral vascular resistance.

Pharmacokinetics:Absorption from the site of intramuscular injection is high. The maximum concentration in the plasma after 20-40 min; connection with plasma proteins - 80%. Penetrates through blood-brain and placental barriers, excreted in breast milk (concentration in the breast milk of the mother, after intramuscular injection of 2 mg 4 times a day - 4 μg / l). Metabolized in the liver, excreted by the kidneys, mainly in the form of metabolites - 70-80% (5% unchanged), through the intestine - 15%. 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.

Indications:Pain syndrome of different genesis of moderate to severe severity, resistant to non-narcotic analgesics; premedication before general anesthesia; as a component of intravenous general anesthesia; anesthesia of childbirth.

Contraindications:Hypersensitivity, pregnancy (except for the preparation for childbirth and pain during labor), lactation.

Carefully:Drug dependence, intracranial hypertension, craniocerebral trauma, respiratory failure, hepatic and / or renal insufficiency, bronchial asthma, age under 18, elderly age (over 65 years), chronic heart failure, acute myocardial infarction, cardiac rhythm disturbances, arterial hypertension.

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.

In the general anesthesia - 2 mg before the introduction of 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 intravenously or intramuscularly are given to women with a gestation period of at least 37 weeks (in the absence of signs of intrauterine pathology in the fetus) no more than once in 4 hours, less than 4 hours before the expected delivery period.

Side effects:

From the nervous system and sensory organs: drowsiness, general weakness, confusion, dizziness, headache, ringing in the ears, blurred vision, diplopia, convulsions, tremor, paresthesia, dysphoria, euphoria, anxiety, nightmares or unusual dreams.

From the cardiovascular system: decrease or increase in blood pressure, tachycardia, arrhythmia.

From the gastrointestinal tract: anorexia, nausea, vomiting, constipation, dry mouth, with inflammatory bowel diseases - paralytic intestinal obstruction and toxic megacolon, liver function abnormalities.

From the side of the urinary system: decreased diuresis, spasm of ureters.

Allergic reactions: skin rash, skin itching, flushing of the face, bronchospasm.

Local reactions: hyperemia, edema, burning at the injection site.

Other: increased sweating, drug dependence, withdrawal syndrome.

Overdose:

Symptoms: respiratory depression, cardiovascular failure, depression of consciousness (up to coma).

Treatment: continuous monitoring, maintenance of adequate pulmonary ventilation, indicators of systemic hemodynamics, body temperature. If necessary, the use of naloxone (a specific opioid antagonist).

Interaction:

Enhances the effect of drugs that depress the central nervous system (barbiturates, anxiolytics, antipsychotic JIC, H1-histamine receptor blockers, ethanol). Pharmaceutically incompatible with diazepam, barbiturates. Means with anticholinergic activity, antidiarrhoeal preparations (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).

Buprenorphine (incl.previous therapy) reduces the effect of opioid analgesics. Reduces the effect of metoclopramide.

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

Naloxone reduces the effect of opioid analgesics, as well as the respiratory and central nervous system caused by them.

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.

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

Form release / dosage:Solution for intravenous and intramuscular injection 2 mg / ml.

Packaging:Solution for intravenous and intramuscular injection 2 mg / ml in ampoules of 1 ml. 5 ampoules per contour cell pack.1 or 2 contour packs together with instructions for use, with a knife ampoule or scarifier, if necessary for ampoules of this type, in a pack of cardboard.

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

Shelf life:

2 years. Do not use after the expiration date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LSR-002174/07

Date of registration:15.08.2007

Expiration Date:Unlimited

The owner of the registration certificate:STATE FACTORY OF MEDICAL PREPARATIONS, FSUE STATE FACTORY OF MEDICAL PREPARATIONS, FSUE Russia

Manufacturer: & nbsp

STATE FACTORY OF MEDICAL PREPARATIONS, FSUE Russia

Information update date: & nbsp14.03.2017

Illustrated instructions

Instructions

Butorphanol tartrate (Butorphanol tarthrati)