Index of drugs

Symptomatic treatment of moderate to severe pain.

1 tabl Effervescent contains 37.5 mg of tramadol hydrochloride and 325 mg of paracetamol.

Tramadol is a centrally acting opioid analgesic. It is a pure non-selectively active mi, delta and kappa opioid receptor agonist with particular affinity for the mi receptor. Other mechanisms of analgesia include suppression of norepinephrine neuronal uptake and increased serotonin release. Tramadol also works antitussive. In contrast to the morphine tramadol used in the recommended doses does not inhibit respiratory function, does not disturb gastrointestinal motility and has no significant effect on the cardiovascular system. The strength of tramadol is determined to be 1/10 to 1/6 of the strength of morphine. Paracetamol is a painkiller (the exact mechanism of action is unknown). Tramadol is used as a racemic form and the [-] and [+] tramadol isomers and its metabolite M1 are detected in the blood. Although tramadol is absorbed quickly after ingestion, its absorption is slower (and the half-life longer) than paracetamol. After a single oral dose of 1 tablet, the maximum blood concentrations are achieved after 1.1 h (+/- tramadol) and 0.5 h (paracetamol) respectively. The average half-lives are 5.7 h for +/- tramadol and 2.8 h for paracetamol. Tramadol in the form of a racemic mixture is absorbed quickly and almost completely after oral administration. The mean absolute bioavailability of a 100 mg oral single dose is about 75%; during long-term bioavailability increases to about 90%. After oral administration of the preparation, paracetamol is absorbed quickly and almost completely, mainly in the small intestine. Paracetamol reaches its maximum concentration in blood within 1 h and this time does not change when used with tramadol. Tramadol is rapidly metabolised after oral administration. Approximately 30% of the administered dose is excreted in the urine in unchanged form, while 60% is excreted as metabolites. Paracetamol is mainly metabolised in the liver in two metabolic pathways: glucuronidation and sulphate conjugation. The hepatotoxic intermediate metabolite N-acetyl-p-benzoquinimine formed in a small amount is rapidly coupled to reduced glutathione and excreted in the urine after conjugation with cysteine ​​or mercapturic acid. Tramadol and its metabolites are mainly excreted in the urine. The half-life of paracetamol is 2-3 hours in adults; it is shorter in children and slightly longer in newborns and patients with liver cirrhosis. Paracetamol is mainly excreted in the urine as glucuronides and sulphates. Less than 9% of paracetamol is excreted unchanged in the urine. In the case of renal failure, the half-life of both tramadol and paracetamol is prolonged.

Hypersensitivity to tramadol hydrochloride, Paracetamol, sunset yellow or any of the excipients. acute intoxication with alcohol, hypnotics, centrally acting analgesics, opioids or psychotropic drugs. Use in patients who take or have taken MAO inhibitors within 14 days prior to treatment with the product. Severe hepatic failure. Epilepsy resistant to treatment.

It is not recommended for patients with severe renal insufficiency (creatinine clearance <10 ml / min). It is not recommended for patients with severe respiratory insufficiency. Do not use in the treatment of opioid addiction. Patients with epilepsy treated successfully and patients prone to convulsions should be treated with the preparation only when absolutely necessary. The preparation should be used with extreme caution in patients addicted to opioids, patients with head injuries, susceptible to convulsions, biliary disorders, shock, impaired consciousness of unexplained etiology, central or peripheral respiratory disorders, increased intracranial pressure.Overdose of paracetamol may cause toxic liver damage in some patients. Therapy with withdrawal symptoms may occur after the therapeutic doses of tramadol. Addiction and abuse cases have rarely been reported. There may be withdrawal symptoms similar to those occurring after discontinuation of opioids. The use of tramadol during shallow anesthesia with enflurane and nitrous oxide should be avoided. The safety and efficacy of the medicine in children under 15 years has not been studied, therefore it is not recommended for use in this age group. An orange yellow dye may cause allergic reactions. The preparation contains 7.8 mmol (179.4 mg) sodium in one tablet, which should be taken into account in patients who control the sodium content of the diet.

Use during pregnancy and breastfeeding is contraindicated.

Very common: dizziness, drowsiness, nausea. Common: confusion, mood swings, anxiety, nervousness, euphoria, sleep disturbances, headache, tremors, vomiting, constipation, dry mouth, diarrhea, abdominal pain, dyspepsia, bloating, excessive sweating, pruritus. Uncommon: depression, hallucinations, nightmares, amnesia, involuntary muscle spasms, paresthesia, tinnitus, arrhythmias, tachycardia, palpitations, hypertension, hot flushes, shortness of breath, swallowing disorders, tarry stools, skin reactions (eg rash , urticaria), impaired urination (painful or difficult urination and retention of urine), albuminuria, chills, chest pain, elevation of transaminases. Rarely: addiction to the drug, convulsions, ataxia, blurred vision. Although during the clinical trials the following adverse reactions related to the use of tramadol or paracetamol have not been observed, their occurrence can not be ruled out. During the use of tramadol may occur: orthostatic hypotension, bradycardia, collapse; rare cases of coagulation disorder, including prolongation of prothrombin time; hypersensitivity reactions from the respiratory system (eg dyspnea, bronchospasm, wheezing, angioneurotic edema) and anaphylaxis; rare cases of changes in appetite, weakening of the musculoskeletal system and inhibition of breathing; differing in terms of severity and type, psychiatric disorders, such as mood changes (usually euphoria, sporadic dysphoria), changes in activity (usually a decrease, occasionally increase), and changes in cognitive abilities and the reception of stimuli; worsening bronchial asthma, although no causal relationship has been established; symptoms of withdrawal syndrome, similar to those occurring after discontinuation of opioids, such as agitation, anxiety, nervousness, insomnia, excessive mobility, tremors and dyspeptic discomfort. Very rarely after abrupt discontinuation of tramadol administration: panic attacks, severe anxiety, hallucinations, paresthesia, tinnitus and unusual CNS disorders. During the use of paracetamol: hypersensitivity reactions with rash, agranulocytosis, thrombocytopenia (but without a proven causal relationship) may occur; Several reports suggest the possibility of hypoproyrombinemia when co-administered with Warfarin or warfarin preparations, although other studies have not shown changes in prothrombin time.

Orally. The dose should be determined individually depending on the intensity of pain and the patient's response.Adults and adolescents> 15 years: it is recommended to start treatment with a dose of 2 tablets. sparkling. An additional dose can be accepted if necessary. Do not use a daily dose of more than 8 tablets. sparkling. The product should be taken no more than every 6 hours, especially in the elderly. In patients with moderate renal impairment (creatinine clearance 10-30 ml / min), the drug should be taken every 12 hours. In patients with moderate hepatic impairment, caution may be considered, provided that the intervals between individual doses are prolonged. The tablets should be taken after reconstitution in a glass of water.