Tramadol, 50 mg/ml, solution for injection, 2 ml, 5 pcs.

Composition and release form

10 pcs in blister; There are 5 blisters in a box.

10 pcs in blister; There are 2 blisters in a box.

in dropper bottles of 10 or 20 ml; There is 1 dropper bottle in the box.

in ampoules of 1 ml; in a box there are 5 ampoules of 1 ml each.

in ampoules of 2 ml; in a box there are 5, 10 or 50 ampoules of 2 ml.

10 pcs in blister; There are 1 or 2 blisters in a box.

Tramadol 5%/2 ml No. 5 solution d/in.amp.

Instructions for medical use of the drug Tramadol Trade name Tramadol International nonproprietary name Tramadol Dosage form Solution for injection 5%, 1 ml and 2 ml Composition 1 ml of the drug contains the active substance - tramadol hydrochloride (in terms of 100% substance) 50.0 mg, excipients: sodium acetate trihydrate, water for injection. Description Colorless or slightly colored transparent liquid. Pharmacotherapeutic group Analgesics. Opioids. Opioids are different. Tramadol. ATC code N02AX02 Pharmacological properties Pharmacokinetics The absolute bioavailability of tramadol when administered intramuscularly is 100%. Plasma protein binding is 20%. Tramadol penetrates the blood-brain barrier and the placenta. The drug is found in breast milk only in very small quantities (0.1%). Tramadol and its metabolites are excreted through the kidneys. 11 metabolites have been identified, of which only O-demethyltramadol is pharmacologically active. The elimination half-life is approximately 6 hours, regardless of route of administration. In case of impaired liver or kidney function, a slight increase in the half-life is expected. In cases of more severe impairment (liver cirrhosis, creatinine clearance <5 ml/min), a 2-3-fold increase in elimination time is expected. Excreted by the kidneys - 90% and through the intestines - 10%. Pharmacodynamics Centrally acting analgesic (opioid + non-opioid). Non-selective agonist of opiate mu-, delta- and kappa receptors in the central nervous system with the highest affinity for mu receptors. Inhibits the activity of the nociceptive system and activates the antinociceptive system. Promotes the opening of potassium and calcium channels, causes hyperpolarization of membranes and inhibits the conduction of nerve impulses. Stimulates the adrenergic system, inhibiting the reverse neuronal uptake of norepinephrine. Enhances the release of serotonin. Has sedative and antitussive effects. In therapeutic doses, it practically does not depress respiration and does not interfere with cardiovascular activity. When administered parenterally, the analgesic effect develops within 5–10 minutes and persists for 3–5 hours. Indications for use Pain syndrome of moderate and severe intensity: - postoperative period - injuries, burns - myocardial infarction - oncological diseases - pain relief during painful diagnostic and therapeutic procedures Method of administration and dosage Tramadol is used as prescribed by a doctor, the dosage regimen of the drug is selected individually, depending on the severity of pain and sensitivity of the patient. The duration of treatment is determined individually; the drug should not be prescribed beyond the period justified from a therapeutic point of view. Due to the possible development of addiction and withdrawal syndrome, courses of treatment for chronic pain should be carried out at regular intervals. Tramadol is intended for intravenous (administer slowly!), intramuscular or subcutaneous administration. The usual single dose for intravenous administration to adults and children over 14 years of age is 50-100 mg of tramadol hydrochloride. If necessary, in case of insufficient effect, a single dose of 50 mg can be prescribed after 30-60 minutes. When performing an intravenous drip infusion, an initial dose of 50-100 mg of tramadol hydrochloride is administered intravenously over 20 minutes, then a maintenance drip infusion is started at a rate of 12 mg of tramadol hydrochloride per hour up to the maximum possible daily dose of 600 mg. Compatible solutions for tramadol infusion are: 0.9% sodium chloride solution, Ringer's solution or 5% glucose solution. When administered intramuscularly or subcutaneously, the initial dose is usually 50-100 mg, further injections are possible, if necessary, at a dose of 50 mg up to the maximum possible daily dose. The maximum daily dose of the drug should not exceed 600 mg. In elderly patients, as well as in patients with impaired liver and/or kidney function, dosage regimen adjustment is necessary: ​​reducing the dose and frequency of drug administration. The highest daily dose for patients over 75 years of age should not exceed 300 mg (6 ml). For children aged 2 to 14 years, tramadol hydrochloride is recommended to be prescribed in a single dose at the rate of 1-2 mg per 1 kg of the child’s body weight, the maximum daily dose should not exceed 4-8 mg per 1 kg of the child’s body weight. Side effects Very often (>1/10) - nausea, vomiting - dizziness Often (from 1/100 to 1/10) - headache, drowsiness - constipation, dry mouth - increased sweating - weakness, increased fatigue Uncommon (from 1 /1000 to 1/100) - urge to vomit, irritation of the gastrointestinal tract (feeling of tension in the abdomen, bloating) - skin reactions (urticaria, itching, rash) - disturbance of cardiovascular regulation (palpitation, tachycardia, orthostatic hypotension or cardiovascular collapse) - mainly with intravenous administration of the drug and in physically weakened patients Rarely (from 1/10000 to 1/1000) - bradycardia, increased blood pressure - changes in appetite, paresthesia, tremor, respiratory depression, epileptiform convulsions (with significant exceeding the dose or after the concomitant use of drugs that lower the seizure threshold or cause convulsions), involuntary muscle contractions, loss of coordination, fainting - respiratory failure (if the recommended dose is significantly exceeded and while taking drugs that suppress the central nervous system) - decreased clarity of vision - muscle weakness - urinary disorders (difficulty urinating, dysuria and urinary retention) - allergic reactions (dyspnea, bronchospasm, wheezing, angioedema), anaphylaxis, worsening of bronchial asthma - increased levels of liver enzymes - hallucinations, confusion, sleep disturbances, nightmares - changes in mood (usually elation, less commonly dysphoria), changes in activity (usually depression, less often increase) and changes in cognitive and sensory abilities (for example, decision-making behavior, disturbances in perception of reality) - these side effects may appear after administration tramadol and vary in nature and intensity depending on the duration of therapy and the individual characteristics of the patient - development of dependence Frequency unknown - mydriasis - withdrawal syndrome Symptoms of withdrawal syndrome: agitation, anxiety, nervousness, insomnia, hyperkinesia, tremor and gastrointestinal symptoms ; very rare: panic attacks, severe anxiety, hallucinations, paresthesia, tinnitus, confusion, delirium, depersonalization, paranoia. Contraindications - hypersensitivity to tramadol hydrochloride or other opiates - conditions accompanied by respiratory depression or severe depression of the central nervous system (poisoning with alcohol, sedatives, hypnotics, narcotic analgesics, psychotropic drugs) - simultaneous use of monoamine oxidase inhibitors and a two-week period after their withdrawal - violation consciousness of unknown origin - dysfunction of the respiratory center, impaired respiratory function - conditions accompanied by increased cranial pressure, without artificial respiration - narcotic, opioid addiction - severe renal failure (creatinine clearance less than 10 ml/min) - severe liver failure - patients suffering from epilepsy, the course of which cannot be adequately controlled - pregnancy and lactation - children under 2 years of age Drug interactions Tramadol solution is incompatible in the same syringe with solutions of diclofenac, indomethacin, phenylbutazone, diazepam, flunitrazepam, nitroglycerin, midazolone. Tramadol is not prescribed simultaneously with monoamine oxidase inhibitors; its use is possible 2 weeks after their discontinuation. Combined use with neuroleptics, furazolidone, procarbazine, serotonin reuptake inhibitors, tricyclic antidepressants is not recommended due to the possible risk of developing seizures. Tramadol enhances (mutually) the effects of tranquilizers, sleeping pills, sedatives, alcohol and other substances that depress the central nervous system. Long-term use of opioid analgesics or barbiturates stimulates the development of cross-tolerance. When used together with carbamazepine, analeptics and psychostimulants, the analgesic effect of the drug is weakened. Direct antagonists of Tramadol, completely blocking its action, are naloxone and naltrexone. The drug is not prescribed for the treatment of drug withdrawal syndrome. Quinidine increases the plasma concentration of tramadol and reduces the content of the metabolite mono-O-demethyltramadol due to competitive inhibition of the CYP2D6 isoenzyme. Combining opioid agonists/antagonists (eg, buprenophine, nalbuphine, pentazocine) and tramadol is not recommended as the analgesic effect of the pure agonist is reduced in these conditions. The development of serotonin syndrome is possible when tramadol is used in combination with other serotonergic substances, such as selective serotonin reuptake inhibitors. Symptoms of serotonin syndrome include confusion, dysphoria, hyperthermia, diaphoresis, ataxia, hyperreflexia, myoclonus, and diarrhea. Withdrawal of serotonergic drugs causes rapid relief of symptoms. With the simultaneous administration of tramadol and coumarin derivatives (for example, warfarin), patients must be carefully monitored, since in some patients prothrombin time values ​​decrease with the development of bleeding and ecchymosis. Other CYP3A4 inhibitors, such as ketoconazole and erythromycin, may inhibit the metabolism of tramadol (N-demethylation) and the active metabolite O-demethyltramadol. CYP2D6 isoenzyme inhibitors (such as fluoxetine, paroxetine and aminotriptyline) reduce the metabolism of tramadol. A limited number of studies have found that pre- or postoperative use of the antiemetic 5-HT3 antagonist ondansetron increased the need for tramadol for postoperative pain. Special instructions If Tramadol is used together with other drugs, the patient should inform the doctor about this. Observe precautions when taking the drug in the following conditions: - with convulsions of central origin - with traumatic brain injuries - in patients with impaired liver and kidney function - with shock - with pain in the abdominal cavity of unknown origin (“acute abdomen”) - with disorders on the part of the respiratory center and respiratory function Tramadol should not be used longer than is justified from a therapeutic point of view. In the case of long-term treatment, the possibility of developing drug dependence cannot be excluded; therefore, courses of treatment should be short-term and under strict medical supervision. The patient should be warned about the need to strictly adhere to the dose and duration of treatment prescribed by the doctor and not to transfer the drug to others. Long-term treatment for chronic pain syndrome should be carried out only according to strict indications. Tramadol is used at increased intervals in elderly patients. Under close medical supervision and in reduced doses, tramadol hydrochloride should be used against the background of the effects of anesthesia, hypnotics and psychotropic drugs. The drug should not be combined with narcotic analgesics due to poor predictability of interaction effects. It is not recommended for use in the treatment of drug withdrawal syndrome. Combination with monoamine oxidase inhibitors should be avoided. Patients with epilepsy or patients susceptible to developing seizures should take Tramadol only for health reasons. During treatment with the drug, alcohol consumption is not allowed. The incidence of side effects increases with increasing duration of drug use. Features of the effect of the drug on the ability to drive a vehicle or operate potentially dangerous mechanisms It is not recommended to engage in activities that require increased attention and high speed of psychomotor reactions (driving vehicles and operating machinery) due to the possible occurrence of adverse reactions. Overdose Symptoms: nausea, vomiting, constriction of the pupils, dilation of the pupils, depression of consciousness, up to a coma, drop in blood pressure. The most dangerous consequences of an overdose of tramadol hydrochloride are respiratory depression and even stopping, convulsions. Treatment: maintaining adequate pulmonary ventilation and symptomatic therapy in the intensive care unit. The antidote for respiratory depression is naloxone; for convulsions, it is advisable to use diazepam. Hemodialysis is ineffective. Release form and packaging 1 ml or 2 ml of the drug in neutral glass ampoules for syringe filling or imported sterile ampoules for syringe filling, with a break point or break ring. A label made of label or writing paper is affixed to each ampoule. 5 ampoules are packed in blister packs made of polyvinyl chloride film and aluminum or imported foil. 2 contour packages together with approved instructions for medical use in the state and Russian languages ​​are placed in a pack of boxed cardboard or ersatz chrome. It is allowed to place blister packs (without being included in a pack), together with approved instructions for medical use in the state and Russian languages, in boxes made of cardboard or corrugated cardboard. The number of instructions is nested according to the number of packages. Storage conditions Store in a dry place, protected from light, at a temperature not exceeding 30°C. Keep out of the reach of children! Shelf life: 3 years Do not use the drug after the expiration date. Conditions for dispensing from pharmacies By prescription Name and country of the organization - manufacturer/packer JSC "Khimpharm", Shymkent, Republic of Kazakhstan Owner of the registration certificate JSC "Khimpharm", Shymkent, Republic of Kazakhstan Address of the organization accepting claims from consumers in the territory of the Republic of Kazakhstan on the quality of products (goods) JSC "Khimpharm", Republic of Kazakhstan Shymkent, st. Rashidova, 81, Phone number +7 7252 (561342) Fax number +7 7252 (561342) Email address

Directions for use and doses

The dosage is individual, depending on the intensity and nature of the pain, the duration and treatment regimen are determined by the doctor.

Tablets, capsules: orally, regardless of food intake, without chewing, with a small amount of liquid, or after dissolving in 1/2 glass of water, usually 1 tablet. or caps. (50 mg). If there is no effect within 30–60 minutes, the same dose can be repeated. For severe pain - 2 tables. or 2 caps. (100 mg) once.

Oral solution: with a small amount of liquid or with sugar, for adults and children over 14 years of age with a body weight over 50 kg, the initial dose is 20 drops, if the effect is insufficient, you can take the next dose after 30–60 minutes, repeat administration is possible after 4 –6 hours. The daily dose should not exceed 400 mg (160 drops). A single dose for children over 1 year of age is 1–2 mg/kg body weight. Approximate dosages for children: 1 year (10 kg) - 4-8 drops, 3 years (15 kg) - 6-12 drops, 6 years (20 kg) - 8-16 drops, 9 years (30 kg) - 12- 24 drops, 12 years (45 kg) - 18–36 drops.

Solution for injection: IV, IM, SC, for adults and adolescents over 14 years of age, a single dose is 1 ml; if there is no effect, the same dose can be repeated after 30–60 minutes. For severe pain - 50 mg every 4 hours, the daily dose should not exceed 400 mg, higher dosages are possible in the presence of a tumor or during surgery. For children from 1 to 13 years old, a single dose is 1–2 mg/kg body weight.

Suppositories: rectally, adults and adolescents over 14 years old, 1 suppository. (100 mg) depending on the intensity of pain, but not more than 400 mg (4 supp.).

In the presence of impaired liver and/or kidney function, as well as in elderly patients, an increase in the interval between doses is required.

TRAMADOL RETARD TAB. P/P/O PROLONG.HIGH. 200MG No. 10

In patients with opioid dependence, head injuries, shock, impaired consciousness of unknown etiology, breathing disorders or damage to the respiratory center, increased intracranial pressure, tramadol should be used only with extreme caution.

The drug should be used with caution in patients with known cases of severe opioid intolerance of allergic and non-allergic origin. Cases of seizures have been reported in patients taking tramadol at recommended doses. The risk of developing seizures may increase if the maximum recommended daily dose of the drug (400 mg) is exceeded. Taking tramadol may increase the risk of seizures in patients taking drugs that lower the seizure threshold. Patients with epilepsy and patients susceptible to seizures should take tramadol only for health reasons.

Concomitant use of tramadol and sedatives such as benzodiazepines or similar drugs may result in sedation, respiratory depression, coma and death. As a result, the concomitant use of tramadol with sedatives should only be considered when alternative treatment options are not available. When using tramadol and sedatives simultaneously, the minimum effective dose should be selected over the shortest possible course.

Close monitoring is necessary for signs and symptoms of respiratory depression and sedation. Therefore, it is strongly recommended that patients and their caregivers be informed about such symptoms.

When stopping treatment with tramadol, it is advisable to gradually reduce the dose to prevent withdrawal symptoms.

Tramadol is metabolized in the liver with the participation of the CYP2D6 isoenzyme. If there is insufficiency or absence of the CYP2D6 isoenzyme, it is impossible to obtain an adequate analgesic effect. It is estimated that approximately 7% of Caucasians may have CYP2D6 deficiency. In contrast, patients with high metabolic activity have an increased risk of developing adverse effects of opioid toxicity, even when taken at recommended doses.

Common symptoms of opioid toxicity include: confusion, drowsiness, shallow breathing, constricted pupils, nausea, vomiting, constipation and lack of appetite. In severe cases, symptoms of circulatory failure and respiratory depression are observed, which can be life-threatening and, in extremely rare cases, lead to death.

An estimate of the prevalence of rapid metabolizers in different populations is given below.

According to data published in the literature, the use of tramadol in the postoperative period in children with obstructive sleep apnea syndrome after tonsillectomy and/or adenoidectomy led to the development of rare but life-threatening adverse events. Particular caution should be exercised when tramadol is used in children for postoperative pain management and close monitoring for symptoms of opioid toxicity, including respiratory depression.

Tramadol is not recommended for use in children with respiratory problems, including neuromuscular disorders, severe heart or respiratory disease, upper respiratory or lung infections, multiple traumas, or major surgery. These factors may increase symptoms of opioid toxicity.

It is possible to develop addiction, physical and mental dependence, especially with prolonged use.

In patients prone to drug abuse or the development of drug dependence, treatment with Tramadol retard should be carried out only in short courses and under medical supervision. Tramadol retard is not suitable as a replacement therapy for patients with opioid addiction. Although tramadol is an opioid agonist, it does not suppress morphine withdrawal symptoms.

Products

Composition: 1 tablet (50 mg) contains: active substance: tramadol hydrochloride 50 mg excipients: potato starch, lactose, magnesium stearate

DESCRIPTION

Tablets are white or white with a slight yellowish tint.

Pharmacotherapeutic group

An analgesic with a mixed mechanism of action.

ATX code

N02AX02

Belongs to list 1 of potent substances.

pharmachologic effect

Tramadol is a cyclohexanol derivative with opiate-agonist properties. Refers to centrally acting analgesics. It has weak affinity for opiate receptors without preferential selectivity for certain receptor populations. It has analgesic, antitussive and sedative effects. The activity of tramadol is 1/10-1/6 of the activity of morphine. Unlike morphine, tramadol in therapeutic doses does not depress respiration, does not suppress gastrointestinal motility and does not affect cardiovascular activity.

Pharmacokinetics

When taken orally, it is quickly absorbed, the therapeutic effect occurs within 15-30 minutes. The therapeutic effect lasts for 4-8 hours. The maximum concentration in blood plasma after oral administration is observed after 1.5-2 hours. Plasma protein binding is about 20%. Penetrates through the placental barrier (the concentration in the blood of the umbilical vein is 80% of the concentration in the mother's blood). Biotransformation occurs in the liver through demethylation and conjugation with the formation of 11 metabolites (1 of them is active). It is excreted mainly by the kidneys (90%) and intestines (about 10%). If the functions of the liver and kidneys are impaired (creatinine clearance less than 80 ml/min), excretion slows down.

Indications for use

• Acute and chronic pain syndrome of strong and moderate intensity of various origins (malignant tumors, injuries, severe neurology, etc.); • Painful diagnostic and therapeutic manipulations.

Contraindications

• Hypersensitivity to any of the components of the drug; • Acute poisoning with alcohol, analgesics, sleeping pills and psychopharmacological drugs; • Treatment with MAO inhibitors and for 14 days after the end of this treatment; • Children under 14 years of age. Tramadol cannot be used as replacement therapy for drug addiction.

Carefully

• opioid addiction (dependence on opioids); • disturbances of consciousness of unknown origin; • disorders of the respiratory center and respiratory functions, as well as in conditions accompanied by increased intracranial pressure, if the patient is not on artificial respiration; • brain diseases; • shock; • epilepsy or tendency to seizures. In patients with epilepsy or prone to seizures, the drug is used only in exceptional cases; • patients with hypersensitivity to opioids.

Use during pregnancy and lactation

Tramadol penetrates the placental barrier. In small quantities (0.1% of the concentration in the blood plasma) it enters breast milk. In this regard, therapy during pregnancy should be limited to individual single doses. Long-term use during pregnancy should be avoided due to the risk of developing addiction in the fetus and the possibility of withdrawal syndrome in the neonatal period. The use of tramadol immediately before or during labor does not affect the contractile function of the uterus. In these cases, the newborn may experience a change in the frequency of respiratory movements, which is insignificant for clinical practice. The use of tramadol during lactation in the form of single doses does not require interruption of breastfeeding.

Directions for use and doses

Inside. The dosages used depend on the severity of the pain syndrome and the individual sensitivity of the patient. The time of taking the drug does not depend on the time of meals.

Adults and adolescents over 14 years of age: A single dose is 50 mg of tramadol. In case of insufficiency or absence of analgesic effect, 50 mg of tramadol is taken again after 30-60 minutes. For severe pain, a single dose of 100 mg of tramadol. The analgesic effect usually lasts for 4-8 hours. The maximum daily dose is 400 mg.

Patients with impaired renal and/or liver function: In patients with impaired renal and/or liver function, it is difficult to eliminate tramadol from the body. In the case of treatment of acute pain syndromes in such patients, when a rare or one-time prescription of tramadol is necessary, no special dosage changes are required. However, in cases of treatment of chronic pain, it is necessary to remember the danger of accumulation of the drug in the body, therefore it is advisable to increase the intervals between its individual doses. The drug should be prescribed with caution to patients with impaired renal function (50-100 mg 2 times a day), as well as to persons with cirrhosis of the liver (in this group of patients, T1/2 of tramadol increases almost 3 times).

Elderly patients: In elderly patients (over 75 years of age), the elimination of tramadol from the body slows down even when there are no clinical manifestations of impaired renal and/or liver function. In these patients, it is also necessary to increase the intervals between individual doses of the drug. It is recommended not to exceed the daily dose of 300 mg.

Side effect

Cardiovascular system: tachycardia, decreased blood pressure (up to orthostatic collapse), syncope. Gastrointestinal tract: nausea, vomiting, dry mouth, abdominal pain, anorexia, flatulence, constipation.

Nervous system and mental sphere: anxiety, lack of coordination, euphoria or depression, miosis, sleep disorders, increased nervous excitability, cognitive impairment, paresthesia, tremor, amnesia, convulsions, hallucinations, respiratory depression, sedation of varying severity, dizziness, headache , increased muscle tone. Urinary system: difficulty or frequent urination.

Other: skin reactions (exanthema, itching) up to anaphylactic shock, Steven-Johnson syndrome, excessive sweating, dyspnea. Long-term use - drug dependence, with sudden o. A worsening of bronchial asthma has been reported, however, there has been no evidence of a negative effect of tramadol on asthma.

Overdose

Symptoms: miosis or mydriasis, vomiting, tachycardia, increased blood pressure, collapse, depression of consciousness, up to coma, respiratory depression (up to apnea).

Treatment: when administered orally, first of all, it is necessary to ensure that the stomach is cleared of the drug that has not yet been absorbed (artificial vomiting, gastric lavage). The main emergency measures in more severe cases are ensuring airway patency (intubation), maintaining breathing and the cardiovascular system. The antidote for depression of the respiratory center is naloxone, which is administered in repeated doses, because Its duration of action is shorter than that of tramadol. Benzodiazepines are used to relieve convulsive syndrome.

Interaction with other drugs

With the simultaneous use of tramadol and: • drugs that depress the central nervous system, especially antidepressants, as well as alcohol, the side effects of tramadol on the central nervous system increase; • drugs that can provoke seizures or increase seizure readiness (for example, antipsychotics and antidepressants), in very rare cases epileptic seizures can be observed. The risk of seizures increases with the use of high doses of tramadol - over 400 mg per day; • carbamazepine decreases and the analgesic effect of tramadol is reduced; • quinidine increases the plasma concentration of tramadol; • barbiturates and tranquilizers may enhance and increase the duration of the analgesic and sedative effects of tramadol. Long-term use of opioid analgesics or barbiturates stimulates the development of cross-tolerance.

special instructions

Recommended doses are approximate. In practice, it is necessary to select the minimum analgesically effective dose. The duration of treatment with the drug is determined individually. Do not use longer than is justified from a therapeutic point of view. When treating long-term pain syndrome, it is advisable to take short-term breaks in the use of tramadol in order to re-determine the required therapeutic dose. During the treatment period, it is necessary to avoid drinking alcohol and refrain from engaging in potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Release form

10 or 20 tablets in blister packs. 1 or 2 blister packs along with instructions for use are placed in a cardboard pack.

Best before date

3 years. Do not use after the expiration date stated on the packaging.

Best before date

Belongs to list 1 of potent substances. In a dry place, protected from light, at a temperature not exceeding 25°C, out of the reach of children.