Index of drugs

Pain of medium and high intensity.

1 tabl sustained release contains 100 mg of tramadol hydrochloride. The drug contains lactose.

Centrally acting analgesic - a pure agonist of mi, delta and kappa opioid receptors with high affinity for mi receptors. Other mechanisms that contribute to the analgesic effect of tramadol include inhibition of noradrenaline neuronal reuptake and increased serotonin release. Tramadol has antitussive activity. In contrast to morphine, tramadol does not induce respiratory depression in a wide range of analgesic doses. It does not affect gastrointestinal peristalsis. The effects on the cardiovascular system are insignificant. After oral administration,> 90% of tramadol is absorbed. First-pass metabolism reaches up to 30%. The average absolute bioavailability is about 70%. C_max occurs after approx. 1.2 hours. Tramadol is approximately 20% bound to plasma proteins. It penetrates the blood-brain barrier, the placenta and to a small extent into breast milk. It is metabolized mainly by N- and O-demethylation and by conjugation of O-demethylation products with glucuronic acid. Only O-demethyltramadol is pharmacologically active. Tramadol and its metabolites are excreted by the kidneys. T_0,5 tramadol is about 6 h, the active metabolite - 7.9 h; these values ​​are prolonged as the degree of renal or hepatic failure increases. In patients with liver cirrhosis, T was observed_0,5 at 13.3 +/- 4.9 h (tramadol) and 18.5 +/- 9.4 h (O-demethyltramadol), in extreme cases they were 22.3 and 36 h, respectively. In patients with insufficiency kidneys (creatinine clearance <5 ml / min), these values ​​were respectively 11 +/- 3.2 and 16.9 +/- 3 h, and in extreme cases 19.5 h and 43.2 h, respectively.

Hypersensitivity to tramadol or to any of the excipients. acute intoxication with alcohol, hypnotics, analgesics (including opioids) or psychotropic drugs. Concomitant use of MAO inhibitors or within 2 weeks after discontinuation of their use. Epilepsy which can not be treated. Treatment of opioid addiction (tramadol is an opioid receptor agonist, one can not stand the withdrawal symptoms of morphine).

The drug can only be used after careful consideration of the benefit-risk ratio and taking appropriate precautions in the event of: opioid addiction, patients with increased sensitivity to opioids, disturbances of unclear consciousness, shock, respiratory and respiratory disorders, elevated intracranial pressure, impaired liver or kidney function (in patients with severely impaired liver or kidney function should not use the drug), head injury, concurrent use of inhibitory drugs on the c and / or alcohol consumption. In patients with a history of or history of cerebral seizures, use only if it is absolutely necessary. The drug should not be used for a long time, but if the nature and severity of the disease requires long-term treatment, the patient should be checked carefully and regularly (including the necessary treatment interruptions if necessary) to determine if further treatment is necessary. During long-term use, the patient may develop tolerance to tramadol, requiring the gradual increase in doses of the drug to maintain pain control. Long-term use of the drug may lead to physical dependence. After an abrupt discontinuation of treatment, a dehydratative syndrome may occur. Due to the addictive potential of tramadol, treatment with tramadol should be short-lived and under close supervision in patients prone to drug abuse or addiction to drugs or alcohol. Use in children <12 years is not recommended. Due to the lactose content, the drug should not be used in patients with rare hereditary galactose intolerance, lactase deficiency (Lapp type) or malabsorption of glucose-galactose.

Do not use during pregnancy.Tramadol crosses the placental barrier; repeated administration of tramadol may cause an unborn child's habituation and, as a consequence, lead to withdrawal symptoms in the newborn. Tramadol administered in the period before and perinatal does not affect the uterine contractile function; in newborns, it can cause changes in respiratory rates, which are usually clinically insignificant. Tramadol in very small amounts (about 0.1% of the dose given intravenously) is excreted in human milk. Do not use tramadol while breastfeeding. In the case of a single administration of tramadol, it is usually not necessary to stop breastfeeding.

Common: dizziness, drowsiness, nausea, vomiting, constipation, dry mouth, excessive sweating, tiredness. Uncommon: allergic reactions, hypersensitivity reactions, anaphylactic shock, palpitations, tachycardia, hypotension, cardiovascular disorders (orthostatic hypotension and syncope), cognitive disorders, seizures, headache, psychomotor agitation, sensory disturbances, emotional instability, confusional states , decreased activity, drug addiction, euphoria, hallucinations, visual impairment, dyspnea, bronchospasm, wheezing, respiratory depression, retching, gastrointestinal irritation (feeling of tightness in the stomach, bloating), diarrhea, pruritus, rash, urticaria, angioneurotic edema, increased activity of liver enzymes, impaired urination, urinary retention, withdrawal reactions (agitation, anxiety, nervousness, insomnia, hyperkinesia, tremors, gastrointestinal symptoms, very rarely described withdrawal symptoms include: panic attacks, increased anxiety, hallucinations, paresthesia, noise ear and atypical disorders o.u.n.). Rarely: changes in appetite, paresthesia, tremors, involuntary muscle contractions, disturbed coordination, fainting, sleep disturbances, anxiety and nightmares, blurred vision, skeletal muscle weakness, difficulty urinating. Very rare: bradycardia, hypertension. Unknown: hypoglycaemia, mydriasis. If doses significantly higher than those recommended and concomitant use of other inhibitory substances are used, o.u.n. Breathing may occur. Convulsions like in epilepsy occur mainly after the use of high doses of tramadol and at the same time drugs that lower the seizure threshold. After using tramadol, various kinds of mental disorders may occur, varying in severity and symptoms; depending on the patient's personality and duration of treatment. The drug can cause addiction. The severity of bronchial asthma has been reported during treatment with tramadol, although no causal relationship has been established between these facts.

Orally. Adults and children> 12 years: 100 mg (1 table with delayed release) every 12 hours. It is recommended to use the lowest effective dose with analgesia. In the treatment of chronic pain, dosage according to a predefined time schedule is recommended. The maximum dose is 400 mg / day in 2 divided doses, every 12 hours.Special groups of patients. No dosage adjustment is normally required for patients up to 75 years of age who have no signs of liver or kidney failure. In patients> 75 years of age, the elimination of the drug may be prolonged. If necessary, extend the period between consecutive doses of the drug, individually for a given patient. The maximum dose for people> 75 years is 300 mg / day in divided doses. In patients with renal or hepatic failure and in patients with chronic pain T_0,5 in the elimination phase of tramadol may be prolonged and consideration should be given to extending the intervals between successive doses. Do not use in patients with severe hepatic or renal impairment (CCr <10 ml / min).Way of giving. Tablets powl. about release should be swallowed whole, without chewing and crushing, with sufficient liquid, regardless of meals. Tablets powl. about however, the release may be divided into halves along the dividing line, if required by the size of the desired dose.