Index of drugs

Treatment of moderate to severe pain.

1 suppository contains 100 mg of tramadol hydrochloride.

Opioid analgesic with central effect. A pure, non-selective, agonist at the mi, delta and kappa opioid receptors, with particular affinity for the mi receptor. Other mechanisms of analgesia include inhibition of norepinephrine neuronal reuptake and the severity of serotonin release. Tramadol also works antitussive. In contrast to the morphine tramadol used in the recommended doses does not inhibit respiratory function, it also has a smaller impact on the motility of the digestive system and the circulatory system. The strength of tramadol is determined to be 1/10 to 1/6 of the strength of morphine. After rectal administration, the bioavailability is 78% ± 10%. It binds about 20% of plasma proteins. It penetrates the blood-brain barrier. It is metabolized mainly in the N- and O-demethylation process and the coupling of O-demethylated derivatives with glucuronic acid. Only O-demethyltramadol is pharmacologically active. T_0,5 is about 6 hours. Tramadol and its metabolites are almost completely excreted in the urine. In patients over 75 years and in renal or hepatic impairment, the half-life may be prolonged.

Hypersensitivity to tramadol or other ingredients of the preparation. acute intoxication with alcohol, hypnotics, painkillers, opioids or psychotropic drugs. The drug is contraindicated in patients who are currently taking or who have taken MAO inhibitors within 14 days prior to treatment with the product. Epilepsy which can not be treated. Do not use in the treatment of opioid addiction.

The product should be used with extreme caution: in cases of opioid addiction, head injury, shock, unconsciousness consciousness disorders, respiratory disorders or its function, and in the case of increased intracranial pressure. Caution should be used in patients with increased sensitivity to opioid medicines. Trials have been reported in patients treated with tramadol at the recommended doses. This risk may be greater if the dose of tramadol hydrochloride exceeds the recommended maximum daily dose (400 mg). In addition, tramadol may increase the risk of seizures in patients receiving concomitant medications lowering the seizure threshold. Patients with a history of epilepsy and persons susceptible to cerebral seizures should be treated with tramadol only when it is absolutely necessary. The drug has low addictive potential; prolonged use may develop tolerance, mental and physical dependence. In patients with a tendency to abuse drugs or addiction, treatment should be short-lived and under close supervision. Tramadol should not be used in substitution therapy in patients addicted to opioids (although it is an opioid receptor agonist, it does not abrogate the withdrawal symptoms of morphine). The preparation is not recommended in children under 12 years of age, due to the form that prevents precise dosing.

The drug should not be used in pregnant women. Tramadol crosses the placental barrier. Administration in the pre- and perinatal period does not interfere with the uterine contractile function. In newborns, it can cause changes in the respiratory rate. Prolonged use in pregnancy may lead to withdrawal syndrome in the newborn. During breastfeeding, about 0.1% of the dose of the drug taken by the mother is excreted in milk - therefore, tramadol should not be used during breastfeeding, but in the case of a single administration of the drug, it is not necessary to stop breastfeeding.

Very common: nausea, dizziness. Common: headache, drowsiness, vomiting, constipation, dry mouth, excessive sweating, tiredness.Uncommon: palpitations, tachycardia, orthostatic hypotension, cardiovascular collapse (especially during intravenous administration and in patients after physical exertion), retching, feeling of pressure in the stomach, bloating, diarrhea, skin reactions (pruritus, rash, urticaria). Rare: bradycardia, increase in blood pressure, changes in appetite, suppression of breathing, dyspnea (when doses significantly higher than recommended and concomitant use of other substances inhibiting the cortex), speech disorders, paresthesia, tremors, seizures of the epileptic type (mainly after high doses of tramadol or simultaneously with drugs that can lower the seizure threshold), involuntary muscle spasms, abnormal coordination, fainting, hallucinations, confusion, sleep disturbances, delirium, anxiety, nightmares, miosis, blurred vision, excessive mydriasis, skeletal muscle weakness, diarrhea, urinary retention, allergic reactions (including dyspnoea, bronchospasm, wheezing, angioedema), anaphylaxis. In individual cases: increase in liver enzymes. There may be various types of mental disorders, including mood disorders (usually arousal, sometimes dysphoria), changes in activity (usually a decrease, sometimes an increase) and changes in the ability to feel and recognize (eg decision making, perception disorders). The preparation can cause addiction. Symptoms of withdrawal reactions may occur, similar to those occurring after discontinuation of opioids, e.g. agitation, anxiety, nervousness, insomnia, hyperkinesia, tremors and gastrointestinal symptoms. Other symptoms that occurred after discontinuation of tramadol were very rarely observed: panic attacks, severe anxiety, hallucinations, paresthesia, tinnitus and unusual abnormalities o.u.n. (eg confusion, delusion, depersonalization, derealization, paranoia). The severity of bronchial asthma has been reported, although no causal relationship has been established.

Rectally. The lowest effective pain relief should be given. In addition to exceptional clinical situations, a dose of> 400 mg of tramadol hydrochloride per day should not be used. Adults and adolescents> 12 years: 100 mg (1 suppository) every 4-6 h. Do not use tramadol longer than is absolutely necessary. If long-term analgesia is needed, the patient's condition should be carefully and regularly monitored (if treatment is interrupted for a period of time if necessary) to assess whether and in what dose the treatment should be continued. In patients under 75 years of age who do not have clinical signs of liver or kidney failure, dosage adjustment is not usually necessary. In patients> 75 years and in patients with renal insufficiency and / or dialysis and with hepatic insufficiency the elimination may be prolonged; the time interval between doses should be extended depending on the patient's needs. In cases of severe renal failure and / or severe hepatic insufficiency, the use of the preparation is not recommended.