Opioid analgesic with central effect. It is a pure non-selectively active mi, delta and kappa opioid receptor agonist with particular affinity for the mi receptor. Other mechanisms of analgesia include suppression of norepinephrine neuronal uptake and support of serotonin release. In contrast to morphine, tramadol does not inhibit respiratory function, does not disturb gastrointestinal motility and has no significant effect on the cardiovascular system. The strength of tramadol is determined to be 1/10 to 1/6 of the strength of morphine. The action time is 4-8 h. Tramadol binds to approximately 20% of plasma proteins. It is metabolized by N- and O-demethylation. Only O-demethyltramadol is pharmacologically active. The half-life is about 6 hours. Tramadol and its metabolites are almost completely (90%) excreted in the urine. In the case of liver or kidney disorders, the half-life of tramadol may be prolonged.
Contraindications:
Hypersensitivity to tramadol or other ingredients of the preparation or other opioid analgesics. acute poisoning: alcohol or drugs that act on the CNS (hypnotic, psychotropic, analgesic). Do not use in patients treated in the last 2 weeks with MAO inhibitors. Do not use in the treatment of addiction to opioids and in patients with epilepsy inadequately controlled medicines. Tramadol should not be used in patients with severe renal impairment (creatinine clearance below 10 ml / min). Use in children under 12 years is not recommended.
Precautions:
The preparation should be used with extreme caution: in cases of opioid addiction, head injury, shock, in consciousness of unknown origin, in the case of respiratory disorders or respiratory center disorders and in the case of increased intracranial pressure. Caution should be used in patients with increased sensitivity to opioid medicines. Patients with a history of epilepsy and persons susceptible to cerebral seizures should be treated with tramadol only when it is absolutely necessary. Treatment, due to the possibility of addiction, should be short-lived and under close supervision, especially in patients with a tendency to abuse drugs or addiction. The use of the drug in light general anesthesia is not recommended.
Pregnancy and lactation:
The preparation should not be used during pregnancy due to lack of safety data. Tramadol is not recommended during breastfeeding.
Side effects:
Very common: nausea, drowsiness, pain and dizziness. Common: vomiting, constipation, excessive sweating, dry mouth, diarrhea. Uncommon: cardiovascular dysfunction (palpitations, tachycardia, orthostatic hypotension, cardiovascular collapse) - especially during intravenous administration and in patients after physical exercise; gastrointestinal disorders, skin reactions (pruritus, rash, urticaria). Rare: bradycardia, increase in blood pressure, changes in appetite, paresthesia, tremors, inhibition of breathing, cerebral convulsions, hallucinations, confusion, sleep disturbances, nightmares, blurred vision, weakening skeletal muscle strength, urination disorders, urinary retention, allergic reactions ( dyspnoea, bronchospasm, angioneurotic edema), anaphylactic shock, withdrawal reactions similar to those observed after discontinuation of opioids (agitation, anxiety, nervousness, sleep disorders, hyperkinesia, tremors, gastrointestinal symptoms, panic attacks, severe anxiety, hallucinations, paresthesia, noise ear and CNS disorders).
Dosage:
The dose should be determined individually depending on the intensity of pain and individual patient response. Adults and children over 12 years: 50-100 mg every 4-6 h. The recommended maximum daily dose is 400 mg, except for specific clinical indications.In postoperative pain, the starting dose is usually 100 mg. If necessary, further doses of the drug may be used within 60 min of the first dose - 50 mg at 10-20 min intervals up to a maximum dose of 250 mg (including the starting dose). Subsequent doses of 50 mg or 100 mg should be administered at intervals of 4-6 h. The maximum daily dose is 600 mg. In patients with impaired renal or hepatic function, the time intervals between subsequent doses should be increased, depending on the degree of impairment of these organs - with a creatinine clearance below 30 ml / min or in severe hepatic insufficiency - the interval between consecutive doses should be increased to 12 h In patients over 75 years of age, subsequent doses should be used at longer intervals. The solution should be injected slowly intravenously (for 2-3 min), intramuscularly or after dilution in 0.9% NaCl solution or 5% Glucose solution and infused intravenously.