One extended-release capsule contains 50 mg, 100 mg, 150 mg or 200 mg tramadol hydrochloride.
Action:
Opioid centrally acting analgesic, opioid receptor agonist: (+) - isomer shows opiod activity by affinity to the mi receptor (-) - isomer enhances analgesic activity of (+) - isomer and is a norepinephrine and serotonin reuptake inhibitor, thereby modifying transmission of pain impulses. Tramadol also works antitussive. At the recommended doses, it does not inhibit respiratory function and has no significant effect on the cardiovascular system. After oral administration, approximately 90% of the drug is absorbed from the gastrointestinal tract. Bioavailability is about 70%, regardless of the meal. It binds to plasma proteins in about 20%. The only pharmacologically active metabolite is O-demethyltramadol, with a potency of 2-4-fold greater than the starting material. Tramadol and its metabolites are almost completely excreted in the urine (90%). T0,5 tramadol is about 6 h, the active metabolite is about 7.9 h. In patients with hepatic and renal failure, the half-life is prolonged. In patients over 75 years old, tramadol bioavailability is increased by 17% and the half-life is prolonged. It penetrates the blood-brain barrier and through the placenta.
Contraindications:
Hypersensitivity to tramadol or other ingredients of the preparation. acute intoxication with alcohol or drugs: hypnotics, psychotropic drugs, central analgesics, opioids. Concomitant use of MAO inhibitors and 2 weeks after discontinuation. Simultaneous treatment of opioid addiction.
Precautions:
Use cautiously in patients with consciousness disorders of unknown aetiology, severe liver and / or kidney failure, diseases associated with increased intracranial pressure (head injuries, brain diseases), impaired respiratory center function, respiratory function or excessive bronchial secretion or concurrently with drugs inhibiting the function of CNS (risk of breath suppression). Patients with epilepsy or a tendency to convulsions should use tramadol only if absolutely necessary. In patients with a tendency to abuse drugs and addictions, the treatment should be carried out intermittently, under close medical supervision. In patients with severe hepatic and / or renal impairment, the use of the preparation is not recommended. Due to the lack of safety and efficacy studies, the use of the preparation in children below 12 years is not recommended. Due to the sucrose content, patients with fructose intolerance, glucose-galactose malabsorption or sucrose-isomaltase deficiency should not use the preparation.
Pregnancy and lactation:
During pregnancy, the preparation must not be used if it is not absolutely necessary. Applied before delivery or during labor, it does not impair the contractility of the uterus; it may cause the newborn to change the frequency of breaths to a degree that is not clinically relevant. During lactation, about 0.1% of the administered dose is excreted in milk - therefore, tramadol should not be used during breast-feeding.
Side effects:
Very common (1/10): dizziness, nausea. Common (1/100, <1/10): headache, drowsiness, vomiting, constipation, dry mouth, excessive sweating. Uncommon (1/1000, <1/100): arrhythmia, tachycardia, circulatory collapse, orthostatic hypotension, retching, gastrointestinal disturbances, pruritus rash, urticaria. Rarely (1 / 10,000, <1/1000): changes in appetite, changes in mood (mainly elevation of mood, sporadic dysphoria), changes in activity (usually limiting, occasionally increasing), changes in cognitive and sensory functions (decision making, perception disorders), blurred vision, bradycardia, hypertension, motor weakness, urinary disorders (including urinary retention). Very rare (<1 / 10,000): hypersensitivity reactions (incl.dyspnoea, bronchospasm, wheezing, angioneurotic edema, anaphylactic reactions), epileptic seizures (mainly at high doses or after simultaneous administration of preparations lowering the seizure threshold or with potential action inducing seizure - for example, medicines used to treat mental disorders). In individual cases: increase in liver enzymes. In addition, asthma may be exacerbated. Breathing suppression was observed after using a significantly exceeded the recommended dose of the preparation and after simultaneous use of drugs inhibiting the activity o.u.n. Prolonged use of the preparation may cause addiction. You may experience symptoms associated with withdrawal reactions, similar to those observed after discontinuation of opioids: agitation, anxiety, nervousness, insomnia, hyperkinesia, muscle tremors, gastrointestinal disorders.
Dosage:
Orally. Adults and children over 12 years of age. The dose should be selected depending on the intensity of pain and the individual sensitivity of the patient. The starting dose is 50-100 mg 2 times a day (morning and evening), depending on the severity of pain, the dose can be increased to 150-200 mg 2 times a day. The maximum daily dose is 400 mg. If long-term treatment with tramadol is necessary, the patient should be carefully monitored (if necessary with interruption of treatment) to determine any changes in dosage.Special groups of patients. In patients> 75 years, it may be necessary to reduce the dose and prolong the interval between consecutive doses. In patients with moderate hepatic and / or renal impairment, the interval between consecutive doses should be increased. For patients with dysphagia, you can carefully open the capsule, pour the contents (granules) on a spoon and give to swallow; washed down with water; The granules should not be chewed or crushed.Way of giving. The capsules can be taken with or without food, swallowed whole with water.
(C)
