Index of drugs

Pain of medium and high intensity.

One capsule contains 50 mg of tramadol hydrochloride. 1 ml of drops (40 drops or 8 applications from the dispenser) contains 100 mg of tramadol hydrochloride; drops contain sucrose.

Central analgesic drug - a non-selective, pure agonist at the mi, delta and kappa opioid receptors with higher affinity for mi receptors. Other mechanisms that may increase its analgesic effect include suppression of norepinephrine neuronal reuptake and support of serotonin release. In contrast to morphine, tramadol has no depressive effect on the respiratory system, does not disturb gastrointestinal motility and has no significant effect on the cardiovascular system. It works about 4-8 h. It is well absorbed from the digestive tract; the average bioavailability is about 70% and increases to about 90% at steady state. After giving the cap. C_max occurs after approx. 1.6-2 h. Plasma proteins are approximately 20% bound. It is metabolised by CYP2D6 to several metabolites; the O-desmethyl metabolite is pharmacologically active. Tramadol crosses the blood-brain barrier, across the placenta barrier and in small amounts into breast milk. Tramadol and its metabolites are almost completely excreted through the kidneys. T_0,5 tramadol is 6-7 h. In patients with renal or hepatic insufficiency the elimination of the drug is slower.

Hypersensitivity to tramadol, other opioid analgesics or to any of the excipients. acute alcohol intoxication, analgesics, hypnotics, opioid or psychotropic analgesics. Use with MAO inhibitors (a 14-day break should be observed between the use of tramadol and MAO inhibitors). Use in the treatment of opioid addiction. Uncontrolled epilepsy.

Use with caution in patients: opioid addicts; with increased sensitivity to opioids; after head injuries; in shock; with disorders of consciousness of unknown origin; with respiratory or respiratory disorders; with increased intracranial pressure; with hepatic and / or renal impairment, especially during long-term therapy, blood levels should be monitored (do not use in patients with CCr <10 ml / min). Patients with a history of epilepsy or cerebral seizures should only be used when absolutely necessary. During long-term use, the patient may develop tolerance to tramadol; long-term use of the drug may lead to physical and mental dependence; discontinuation symptoms may occur after abrupt cessation of use. Due to the addictive potential of tramadol, treatment with tramadol should be carried out under the supervision of a physician in patients prone to drug abuse and drug dependence, and in patients who have long-term therapy. The patient's condition should be checked carefully and regularly (if necessary - with interruption of treatment) to determine if further treatment is necessary. Tramadol should not be used as a substitution therapy for opioid dependence, because it does not remove the symptoms occurring after discontinuation of morphine. The use of tramadol in light general anesthesia is not recommended, because of the risk of awakening during surgery. After administration of a strong anesthetic (inhalation or intravenous), tramadol can be used during surgery in the same way as other analgesics routinely used. It is not recommended to use the drug in children <12 years. Due to the sucrose content, patients with rare hereditary fructose intolerance, sucrase-isomaltase deficiency or glucose-galactose malabsorption should not be given drops.

Do not use during pregnancy (no safety data). Tramadol is not recommended during breastfeeding (about 0.1% of the dose of the drug taken by the mother is excreted in milk).

Very common: dizziness, headache, drowsiness, nausea. Common: vomiting, constipation, diarrhea, dry mouth, excessive sweating.Uncommon: palpitations, tachycardia, orthostatic hypotension, cardiovascular collapse, rebound, irritation of the gastrointestinal tract (eg feeling of fullness in the abdomen, pressure in the stomach), skin reactions (pruritus, rash, urticaria). Rare: bradycardia, increase in blood pressure, changes in appetite, paresthesia, tremor, respiratory depression, cerebral convulsions, hallucinations, confusion, sleep disturbances, nightmares, blurred vision, weakening of skeletal muscle strength, micturition disorders (dysuria, retention) urine), allergic reactions (eg dyspnea, bronchospasm, wheezing, angioneurotic edema), anaphylactic shock. In individual cases: increase in liver enzymes. Mental disorders may occur during treatment, vary in severity and symptoms and depending on the patient's personality and time of drug administration; these may be mood disorders (usually arousal, sometimes dysphoria), changes in activity (usually a decrease, sometimes an increase), excessive fatigue and changes in the ability to cognitive and sensory perception (eg decision-making behavior, perception disorders). Addiction may occur. After discontinuation of tramadol withdrawal symptoms may occur: agitation, anxiety, nervousness, sleep disorders, hyperkinesia, tremors and gastrointestinal disorders, as well as panic attacks, severe anxiety, hallucinations, paresthesia, ringing in the ears and other symptoms from the o.u.n. At the time of treatment with tramadol, worsening of bronchial asthma was also reported, however causality was not established.

Orally. Adults and children> 12 years: individually, depending on the severity of the pain and the patient's response, usually 50-100 mg (1-2 capsules or 20-40 drops or 4-8 applications from the dosing pump) every 4-6 h (in acute pain the initial dose should be 100 mg, and in chronic pain 50 mg). Serve the smallest dose with effective pain relief. The usual dose should not exceed 400 mg / day, in divided doses, except in special clinical indications.Special groups of patients. Dose adjustment is not usually necessary in patients under 75 years of age without clinical evidence of renal or hepatic failure. In patients> 75 years of age, the time interval between doses should be extended. In patients with renal insufficiency, consideration should be given to extending the intervals between consecutive doses; in the case of CCr <30 ml / min, the gap should be extended to 12 hours; do not use the drug at CCr <10 ml / min; in patients on hemodialysis, tramadol is not required after hemodialysis. In patients with hepatic impairment, consideration should be given to increasing the intervals between consecutive doses; in severe liver failure the interval should be extended to 12 hours.Way of giving. The preparation can be taken regardless of meals. Drops should be taken with a small amount of liquid or sugar.