Overview
An opioid receptor antagonist agonist (kappa and delta receptor agonist and mu opioid receptor antagonist). It activates the endogenous antinociceptive system through kappa-opiate receptors, disrupts the interneuronal transmission of pain impulses at various levels of the central nervous system. Acting on the higher parts of the brain, it changes the emotional coloring of pain. It inhibits conditioned reflexes, has a sedative effect, causes dysphoria, myosis, and excites the vomiting center. To a lesser extent than morphine, trimeperidine, fentanyl, depresses the respiratory center and affects the motility of the gastrointestinal tract. Does not affect hemodynamics. The risk of histamine reaction, as well as the development of addiction and opioid dependence with controlled use is significantly lower than for opioid agonists.
With the on / in the introduction of the effect develops after 2-3 minutes, with s / c or / m - after 10-15 minutes. The maximum effect is after 30-60 minutes, the duration of action in the absence of tolerance with subcutaneous or intramuscular administration is 3-6 hours, intravenous administration is 3-4 hours.
Side effects
From the nervous system and sensory organs: more often - drowsiness (36%), headache (3%); less often - dizziness, fatigue, general weakness, lethargy; rarely (less than 1%) - nervousness, euphoria, discomfort, blurred combination with this, diplopia, restless sleep, nightmares, unusual dreams, depression, confusion (hallucinations, depersonalization), in children - paradoxical agitation, anxiety; frequency unknown - tinnitus, cramps, muscle stiffness (especially respiratory), tremors, involuntary muscle twitches.
From the CCC: less often - lowering blood pressure; rarely (less than 1%) - arrhythmias (tachycardia / bradycardia), increased blood pressure.
From the respiratory system: rarely (less than 1%) - respiratory depression (decrease in minute respiratory volume).
From the digestive system: less often - dry mouth (4%), anorexia, nausea and / or vomiting (6%); rarely - gastrointestinal irritation, biliary tract spasm, inflammatory bowel disease - paralytic ileus and toxic megacolon (constipation, flatulence, nausea, stomach cramps, gastralgia, vomiting); frequency unknown - constipation, hepatotoxicity (dark urine, pale stool, icteric sclera and skin integument).
From the urinary system: rarely (less than 1%) - decreased urine output, spasm of the ureters (difficulty and pain during urination, frequent urination).
Allergic reactions: less often - urticaria, skin rash, skin itching, swelling of the face; rarely (less than 1%) - bronchospasm, angioedema, laryngospasm; in extreme cases - anaphylactic or anaphylactoid shock.
Local reactions: hyperemia, edema, burning at the injection site, pain at the injection site.
Other: less often - increased sweating; frequency unknown - drug dependence, withdrawal syndrome (abdominal pain of a spastic nature, nausea, vomiting, rhinorrhea, lacrimation, weakness, anxiety, Bifin
Overdose. Symptoms of acute and chronic overdose: cold, sticky sweat, pallor of the skin, miosis, hypothermia, confusion, dizziness, drowsiness, decreased blood pressure, cardiovascular failure, nervousness, fatigue, bradycardia, severe weakness, periodic Chain-Stokes respiration, lung hypoventilationhypothermia, anxiety, miosis, convulsions, in severe cases - loss of consciousness, respiratory center paralysis, respiratory arrest, stupor, coma.
Treatment: maintaining adequate pulmonary ventilation, systemic hemodynamics and body temperature, oxygen therapy; with respiratory depression - in / in the introduction Bifin a specific antagonist of opioid complete naloxone or nalorphine.
special instructions
The finished dosage form contains there disulfite as a preservative, which can cause asthma attacks, anaphylactic or anaphylactoid shock in patients with bronchial asthma (with increased sensitivity to sulfite).
Do not use for more than 3 days and exceed dosage due to the possibility of developing physical dependence.
The effect of the drug on the myocardium is not fully understood (caution should there exercised when prescribing for myocardial infarction).
During the treatment period, it is necessary to refrain from driving vehicles and engaging in other potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions.
The drug, introduced in oil at a dose of 10 mg, is equivalent in action to morphine with a similar dosage and route of administration.
Pregnancy and lactation
Use during pregnancy is possible only under strict indications.
