Overview
When iv is administered in general anesthesia - 2 mg before administration of sodium thiopental, then anesthesia is supported by repeated iv injections of 0.5-1 mg. The total dose required for anesthesia is 4-12.5 mg.
During childbirth, 1–2 mg i / m or iv is administered to women in labor with a gestational age of at least 37 weeks (in the absence of signs of intrauterine pathology in the fetus) and not more than once every 4 hours, the last injection should be made no later than 4 hours before the estimated delivery time.
Doses of the drug for children under 18 years of age not established.
pharmachologic effect
An opioid analgesic for parenteral administration from the group of mixed agonists-antagonists of opioid receptors (stimulates kappa and sigma receptors, blocks mu receptors). The severity of the analgesic effect is similar to morphine. After iv administration, the effect occurs immediately, the maximum effect - after a few minutes; after i / m administration, the effect occurs in 10-15 minutes, maximum activity - in 30-60 minutes, duration of action - 3-4 hours. To a lesser extent than morphine, it depresses breathing, has a lower narcogenic potential, less often than others Opioids cause constipation. It has an antitussive and sedative effect, stimulates the vomiting center, causes pupil constriction, increases systemic blood pressure, pulmonary artery pressure, LV BW and OPSS.
The onset of effect after intramuscular administration is 10-30 minutes, intravenous administration is 2-3 minutes, the time to achieve maximum effect after intramuscular administration is 30-60 minutes, intravenous administration is 30 minutes, duration of effect in the absence of tolerance with a / m introduction - 3-4 hours, a / in the introduction - 2-4 hours.
Side effects
From the side of the central nervous system and sensory organs: more often - drowsiness (40%); less often - dizziness, fatigue, general weakness, headache (3%), dysphoria; rarely (less than 1%) - anxiety, nightmares, unusual dreams, restless sleep, euphoria, central nervous system depression, confusion (hallucinations, depersonalization), tinnitus, blurred visual perception, diplopia, in children - paradoxical agitation, anxiety; frequency unknown - cramps, muscle stiffness (especially respiratory), tremors, involuntary muscle twitches, paresthesias.
From the CCC: less often - lowering blood pressure, tachycradia; rarely (less than 1%) - arrhythmia, increased blood pressure.
From the digestive system: less often - anorexia, nausea and / or vomiting (6%); rarely (less than 1%) - constipation, dry mouth, gastrointestinal irritation, with inflammatory bowel disease - paralytic intestinal obstruction and toxic megacolon (constipation, flatulence, nausea, stomach cramps, gastralgia, vomiting); frequency unknown - hepatotoxicity (dark urine, pale stools, icteric sclera and skin integument).
From the urinary system: less often - decreased urine output, spasm of the ureters (difficulty and pain during urination, frequent urination).
Allergic reactions: rarely (less than 1%) - skin rash (including on the face), urticaria, facial flushing, bronchospasm, skin itching.
Local reactions: hyperemia, edema, burning at the injection site.
Other: less often - sweating.
Overdose. Symptoms of acute and Butador overdose: cold, sticky sweat, confusion, dizziness, drowsiness, decreased blood Butador, nervousness, fatigue, bradycardia, severe weakness, slow labored breathing, hypothermia, natural, miosis, cramps, hypoventilation, cardiovascular failure, in severe cases - loss of consciousness, respiratory arrest, coma.
Treatment: maintaining adequate pulmonary ventilation, systemic hemodynamics, normal body temperature. Patients should be under continuous monitoring; if necessary - carrying out mechanical ventilation; the use of a specific opioid antagonist - naloxone.
special instructions
In patients with drug addiction, prior to treatment, measures should be taken to completely eliminate the drug from the body.
In experimental studies, there was no teratogenic effect of the drug, but the risk of fetal death in rats and rabbits increased.
In the period of preparation for childbirth, it is prescribed subject to careful medical supervision.
It should be borne in mind that children under 2 years old are more sensitive to the effects of opioid analgesics, and that they may experience paradoxical reactions.
The drug, administered at a dose of 2 mg / m, is equivalent to the introduction of 10 mg of morphine / m.
It does not affect biliary tract imaging.
Does not cause a change in plasma amylase and lipase activity.
Stimulates myocardial function (caution should be exercised in case of myocardial infarction).
During treatment with the drug should not engage in potentially hazardous activities requiring increased attention, speed of mental and motor reactions, ethanol should not be used.
Interaction
The use of the drug enhances the effect of drugs that depress the central nervous system (barbiturates, anxiolytics, antipsychotic drugs, H1-histamine Butador blockers, ethanol, muscle relaxants, and other opioids).
Pharmaceutically Butador with diazepam, barbiturates.