Opioid analgesic with central effect. Non-selective opioid receptor agonist (mainly kappa type, weaker type delta and mi). Other mechanisms that may increase its analgesic effect include suppression of noradrenaline reversion and an increase in the release of serotonin. At therapeutic doses, tramadol does not have a depressive effect on the respiratory system, it does not disturb gastrointestinal motility and has little effect on the cardiovascular system. It works antitussive. After oral administration, it is absorbed in about 90% (average total bioavailability about 70%), about 20% bound to plasma proteins. Subject to the first-pass effect (up to 30%). After a 100 mg dose, the maximum concentration in blood (Cmax= 141 ± 40 ng / ml) reaches after 4.9 hours; after a dose of 200 mg - Cmax= 260 ± 62 ng / ml reached after approx. 4.8 h. In the therapeutic dose range, it is characterized by a linear pharmacokinetic profile, with analgesic effect dependent on serum concentration. Typically, the optimal analgesic effect is achieved at concentrations of 100-300 ng / ml. Metabolized mainly by N- and O-demethylation and coupling of O-demethylation products with glucuronic acid. Only O-demethyltramadol is pharmacologically active and shows 2-4 times stronger activity than the parent substance, its half-life T0,5 β = 5.4-9.6 h, for tramadol T0,5β = 6 h. Inhibition of one or both of the cytochrome C450 isoenzymes CYP3A4 and CYP2D6 may affect the concentration of tramadol or its metabolites in the plasma. Both tramadol and its metabolites are excreted by the kidneys (approximately 90% of the dose). In cirrhotic patients, the half-life of tramadol and O-desmethyltramadol may be prolonged (13.3 ± 4.9 h and 18.5 ± 9.4 h respectively, up to the extreme cases of 22.3 h and 36 h respectively). In patients with severe renal impairment (creatinine clearance <5 ml / min), these values are 11 ± 3.2 and 16.9 ± 3 h, respectively, up to the extreme values of 19.5 and 43.2 h. It passes through the blood barrier. the brain, through the placenta and into breast milk.
Contraindications:
Hypersensitivity to tramadol, other ingredients of the preparation or other opioid analgesics. acute intoxication with alcohol, hypnotics, painkillers, opioids or psychotropic drugs. Co-administration with MAO inhibitors and up to 2 weeks from the end of their use. Epilepsy resistant to treatment. Do not use in the treatment of opioid addiction. Children under 12 years.
Precautions:
The drug should be used with caution after assessing the potential risk in patients: opioid addicts, head injuries, those in shock, with consciousness disorders of unknown origin, with respiratory or respiratory disorders, with increased intracranial pressure, in patients with moderate or severe hepatic or renal failure, with increased sensitivity to opioid medicines. In patients with a history of epilepsy or who have had seizures of a cerebral origin, the drug can only be used when absolutely necessary. In patients with a tendency to abuse drugs or addiction, treatment should be short-lived and under strict control.
Pregnancy and lactation:
Tramadol crosses the placenta. Long-term use of tramadol during pregnancy may lead to increased tolerance and withdrawal symptoms in the newborn after birth. Do not use during pregnancy. Administered before or during labor - does not interfere with uterine contractions. Approx. 0.1% of the dose is excreted in breast milk. The drug is not recommended during breastfeeding. One-time administration of the drug during breastfeeding does not require discontinuation of feeding.
Side effects:
Very common: nausea and dizziness. Common: headache, lethargy, vomiting, constipation, sweating, dryness of the oral mucosa, fatigue.Uncommon: palpitations, tachycardia, orthostatic hypotension, cardiovascular collapse (especially after intravenous administration and in patients after physical exertion), nausea, irritation of the stomach and intestines, skin reactions (pruritus, rash, urticaria). Rare: elevated blood pressure, bradycardia, changes in appetite, paresthesia, tremors, respiratory depression, seizures, myoclonus, fainting, hallucinations, confusion, anxiety, sleep disturbances, nightmares, blurred vision, muscle weakness, difficulty urinating, retention urine, allergic reactions (dyspnea, bronchospasm, wheezing, angioneurotic edema, anaphylactic shock). Very rare: increased liver enzymes, atypical withdrawal symptoms (panic attacks, acute anxiety, hallucinations, paresthesia, tinnitus, other unusual symptoms from the o.u.n.).
Dosage:
Orally. The dose should be determined individually depending on the intensity of pain and the patient's response. Adults and children over 12 years of age: initially 100 mg 2 times a day (morning and evening). If the analgesic effect is insufficient, the dose may be increased to 150 mg twice daily or 200 mg twice daily. Exceptionally, subsequent doses can be administered at intervals of less than 12 h (not more often than every 8 h). Use the lowest effective dose. The drug should not be used for longer than is absolutely necessary. In patients over 75 years of age due to the delayed excretion of the drug - intervals between doses can be extended depending on the patient's needs. In patients with moderate hepatic impairment, careful use of the preparation may be considered, provided that the intervals between individual doses are prolonged. The tablets should be swallowed whole with water (without breaking or crushing).
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