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

Opioid analgesic, opioid receptor antagonist agonist. It is an agonist kappa and antagonist of mu-opioid receptors. Activates the endogenous antinociceptive system mainly through cap-pa-opioidreceptors and thus violates the inter-neural transmission of pain impulses at various levels of the central nervous system (CNS), and also changes the emotional color of the pain, affecting the higher parts of the brain.

The effect on sigma-receptors is due to some psychomimetic action, and the ability to sometimes cause dysphoria.

Has a sedative and central antitussive action, excites the vomiting center, causes miosis. To a lesser extent, than agonists of mu-opioid receptors (morphine, trimeridine, fentanyl) depresses the respiratory center and affects the motility of the gastrointestinal tract. Possible influence on hemodynamics (increased systolic and reduced diastolic pressure, increased pulmonary artery pressure), increased intracranial pressure. The drug has a rapid analgesic effect: with intravenous administration, the effect develops in 2-3 minutes, with intramuscular injection after 10-30 minutes. The maximum analgesic effect is achieved in 30-60 minutes, the duration of action is at an IV injection 3-4 hours, with iv introduction 2-4 hours.With controlled use, the likelihood of developing addiction and drug (opioid) dependence is very small.

Pharmacokinetics:80% of the drug binds to plasma proteins. The maximum concentration in the blood plasma is 2.2 mg / ml. Half-life is 2.5-4 hours, in elderly patients - 6.6 hours, in patients with severe renal dysfunction - more than 10 hours. About 5% of the drug is excreted unchanged in urine, 70-80% - in the form of metabolites, the remaining part is excreted with bile and excreted with feces. It penetrates the placental barrier and is found in breast milk.

Indications:Severe pain syndrome of various origins (including preoperative, operational and postoperative periods), with malignant neoplasms (with intolerance to other opioids), during labor (in the absence of fetal signs of intrauterine pathology).

Contraindications:

Hypersensitivity to the components of the drug. Inhibition of respiration, CNS; convulsions. Increased intracranial pressure. Craniocerebral injury. Acute alcohol intoxication and alcoholic psychosis.Hepatic and renal failure, bronchial asthma, heart failure, acute myocardial infarction, heart rhythm disturbance, arterial hypertension.

Acute surgical diseases of the abdominal cavity before diagnosis.

Against the background of treatment with monoamine oxidase inhibitors and for another 14 days after their withdrawal. Age to 18 years.

Pregnancy (except for pain during labor), the period of breastfeeding.

Drug addiction to morphine-like drugs (morphine, trimeridine, fentanyl).

Carefully:Patients with general exhaustion, elderly age (over 65 years).

Dosing and Administration:

Assign intravenously or intramuscularly. Doses are selected individually depending on the age and condition of the patient.

With pain syndrome, 1 mg of the drug is administered intravenously or 2 mg intramuscularly every 3-4 hours as needed. For premedication, inject 2 mg of the drug intramuscularly for 60-90 minutes before the operation or the same dose intravenously immediately before the operation.

When intravenous general anesthesia is administered, 2 mg is administered intravenously before administration of the general anesthetic agent, and then 0.5-1.0 mg of the drug is added to maintain the necessary depth of anesthesia.The total dose of analgesic, required for general anesthesia, is 4 to 12.5 mg.

At the time of delivery, 1 mg or 2 mg of the drug is administered intramuscularly or intravenously to parturient women with a gestation period of at least 37 weeks if the fetus lacks signs of intrauterine pathology. Do not administer more than once in 4 hours, the last injection should be done at least 4 hours before the delivery.

In elderly patients, the dose is reduced by half, and the interval between injections increases to 6 hours.

Side effects:

Most often: drowsiness, dizziness, nausea, or vomiting.

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

From the cardiovascular system: symptoms of vasodilation, palpitations, rarely: lowering blood pressure, fainting; communication with taking the drug is not established - increased blood pressure, tachycardia, pain in the chest.

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, rash, hives.

From the urinary system: decrease in urination.

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

Other: apnea, seizures, asthenia, lethargy, headache, fever, delirium, drug dependence, transient difficulty in speech and movement (associated with excessive drug effects).

Overdose:

Symptoms: cold sticky sweat, confusion, dizziness, drowsiness, decreased blood pressure, nervousness, fatigue, bradycardia, severe weakness, slow labored breathing, hypothermia, anxiety, miosis, seizures, 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; use of opioid receptor antagonist - naloxone.

Interaction:

It should not be combined with other narcotic analgesics because of the danger of weakening analgesia and the possibility of provoking a withdrawal syndrome in patients with opioid dependence.

Under careful supervision and in reduced doses should be used against the background of the means for general anesthesia, hypnotics in order to avoid the increase of excessive CNS suppression and suppression of the activity of the respiratory center.

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. Medicines (JIC) with anticholinergic activity, antidiarrheal JIC (incl. loperamide) increase the risk of constipation up to intestinal obstruction, urinary retention and CNS depression.

Strengthens the hypotensive effect of JIC, reducing blood pressure (including ganglion blockers, diuretics).

Buprenorphine (including 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 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 depression and central nervous system caused by them; higher doses may be required to level the effects of butorphanol, nalbuphine and pentazocine, which have been prescribed to eliminate the undesirable effects of other opioids; can accelerate the appearance of symptoms of the syndrome of "withdrawal" against the background of drug dependence. Naltrexone accelerates the appearance of symptoms of the "cancellation" 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.

Effect on the ability to drive transp. cf. and fur:During the treatment period it is recommended to refrain from driving. Butorphanol complicates the performance of work that requires increased attention, high speed of mental and motor reactions (driving vehicles, controlling mechanisms, devices and other potentially hazardous activities).

Form release / dosage:

Solution for intravenous and intramuscular injection 2 mg / ml.

Packaging:

1 ml of the drug in ampoules of syringe filling with a capacity of 2 ml of amber glass or ampoules from the light-protective glass. On the ampoule, paint can be marked with a dot or a break ring. Five ampoules are placed in a contour mesh package made of a polyvinyl chloride film. The contourcell is not covered with foil. For 1 or 2 contour mesh packaging with an ampull ceramic ceramic scriber and instructions for use are put in a pack of cardboard.

When using ampoules with a dot or a ring of fracture, the scarifier is not inserted.

Storage conditions:List A. In the dark place at a temperature of 5 to 30 ° C. Keep out of the reach of children.

Shelf life:

3 years.

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

Terms of leave from pharmacies:On prescription

Registration number:P N001327 / 01

Date of registration:10.03.2009

Expiration Date:Unlimited

The owner of the registration certificate:MOSHIMFARM PREPARATES them. N.А.Semashko, OJSC MOSHIMFARM PREPARATES them. N.А.Semashko, OJSC Russia

Manufacturer: & nbsp

MOSHIMFARM PREPARATES them. NA Semashko OJSC Russia

Information update date: & nbsp14.03.2017

Illustrated instructions

Instructions

Butorphanol (Butorphanol)