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

Excipients: citric acid - 3,3 mg / ml, sodium citrate pentasecovihydrate - 6.4 mg / ml, sodium chloride - 6.4 mg / ml, water for injection up to 1.0 ml.

Description:A clear, 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 agonists - opioid receptor 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%. Half-life in young patients - 4.7 hours, in the elderly - 6.6 hours, in patients with renal insufficiency -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), the period to lactation, the age of 18 years.

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

Dosing and Administration:With a pain syndrome of 2 mg intramuscularly every 3-4 hours (or as needed). In elderly patients and patients with hepatic-renal insufficiency, the dose is reduced by half, and the interval between injections increases to 6 hours. For premedication, 2 mg intramuscularly administered for 60-90 min before the operation. During childbirth, 2 mg intramuscularly injections with at least 37 weeks gestation (in the absence of signs of intrauterine pathology) are given no more often than once in 4 hours,less than 4 hours before the estimated time of delivery.

Side effects:

From the nervous system and sensory organs: drowsiness, general weakness, confusion of consciousness, dizziness, headache, ringing in the ears, blurred vision, diplopia, cramps, tremor, paresthesia, dysphoria, euphoria, anxiety, nightmares or unusual dreams, eye pain, hallucinations, hostility, delirium , transient speech difficulty, fainting.

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, apnea, asthenia, lethargy, sensation of fever.

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:

Strengthens the effect of drugs that depress the central nervous system (barbiturates, anxiolytics, antipsychotic drugs, 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 (including the 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 withoccurrence of hyper- or hypotensive crises (in the beginning to assess the effect of interaction, the dose should be reduced to ¼ of the recommended).

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

Naltrexone accelerates the appearance of symptoms of "withdrawal syndrome" against the background of drug dependence (symptoms may appear as early as 5 minutes after drug administration, continue for 48 hours, are resistant and difficult to resolve); 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.

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 intramuscular injection 2 mg / ml.

Packaging:

A 1 ml syringe containing 2 mg of butorphanol. Each syringe tube in a bag of two-layer film.

For 1, 5 or 10 packs, together with instructions for medical use, put in a pack of cardboard.

Storage conditions:

List A.

Store in a dry, 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 the product after the expiration date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:П N014372 / 01

Date of registration:12.09.2008

Expiration Date:Unlimited

The owner of the registration certificate:STIROLBIOFARM, LLC STIROLBIOFARM, LLC Ukraine

Manufacturer: & nbsp

STIROLBIOFARM, LLC Ukraine

Information update date: & nbsp14.03.2017

Illustrated instructions

Instructions

Butorphanol tartrate (Butorphanol tarthrati)