Tramadol Capsules (50 mg) Tramadol. Tramadol is a narcotic analgesic that can cause severe addiction

Tramadol

International nonproprietary name

Tramadol

Dosage form

Capsules 50 mg

Compound

1 capsule contains

active substance- tramadol hydrochloride in terms of 100% substance 50 mg

excipients: lactose monohydrate, magnesium stearate

capsule shell composition: brilliant black PN (E 151), patent blue (E 131), quinoline yellow (E 104), erythrosine (E 127), titanium dioxide

(E 171), gelatin.

Description

Hard gelatin capsules with a green body and cap, cylindrical in shape, size No. 2. The contents of the capsule are white powder.

Pharmacotherapeutic group

Analgesics. Opioids. Opioids are different. Tramadol

ATX code N02A X02

Pharmacological properties

Pharmacokinetics

When taken orally, more than 90% of tramadol is absorbed from the gastrointestinal tract. Maximum plasma concentration is achieved after 4.8 hours. Absolute bioavailability - 68%. Binding to blood plasma proteins - 20%. Penetrates through the blood-brain and placental barriers. 0.1% of the drug passes into breast milk. Metabolized in the liver. The half-life is 6 hours. Tramadol hydrochloride and its metabolites are excreted by the kidneys (25-35%) unchanged. Approximately 7% is eliminated by hemodialysis.

An increase in half-life was noted in patients over 75 years of age.

Pharmacodynamics

Tramadol is a centrally acting analgesic. It has a mixed mechanism of action. It is a non-selective agonist of opioid mu-, delta- and kappareceptors. Other mechanisms that are involved in the analgesic effect of tramadol hydrochloride are inhibition of norepinephrine reuptake in neurons and enhancement of the serotonergic response.

Opens K+ and Ca++ channels, causes hyperpolarization of membranes and inhibits the conduction of pain impulses. The analgesic effect is due to a decrease in the activity of the nociceptive system and an increase in the antinociceptive system of the body. Tramadol hydrochloride has an antitussive effect. When used in therapeutic doses, tramadol hydrochloride does not depress respiration and does not affect intestinal motility.

Indications for use

Acute and chronic pain syndrome of moderate and significant severity (pre- and postoperative periods, malignant formations, trauma, neuralgia)

Directions for use and doses

The dose and duration of treatment are determined by the doctor individually, based on the intensity of the pain syndrome.

For adults prescribed orally (with a small amount of liquid, regardless of food intake) 1 capsule (50 mg). For severe pain, a single dose can be 2 capsules (100 mg).

The daily dose should not exceed 5-6 capsules. The dosing frequency should not be more frequent than every 4 hours.

The drug should not be used longer than is justified from a therapeutic point of view. For patients with moderate liver/kidney dysfunction, as well as for the elderly, doses are selected individually.

In case of moderate liver failure, it is recommended to reduce the dose or increase the interval between doses.

In case of moderate renal failure, it is advisable to increase the interval between doses. For patients with creatinine clearance less than 30 ml/min, the interval should be increased to 12 hours. In such cases, the maximum recommended daily dose is 200 mg. Due to the possible development of dependence on tramadol, treatment should be short-term and intermittent. The possible benefits of long-term therapy should be carefully reviewed to ensure that they outweigh the risk of developing dependence.

Side effects

Often:

- increased sweating

- headache

- dizziness

Nausea

• Dry mouth

  Change in appetite

• Flatulence

  Epigastric pain

• Uncommon:

  Tachycardia

  Feeling of heartbeat

  Reduced blood pressure to the point of collapse (orthostatic collapse)

  Rarely:

  Weakness

  Lethargy

  Reduced reaction speed

  Sleep disturbance

  Nightmares

  Euphoria

  Hallucinations

  Anxiety

  Emotional lability

  Depression

  Amnesia

  Paresthesia

  Drowsiness

  Epileptiform seizures

• Respiratory depression

  Impaired coordination and speech

  Syncope

  Confusion

  Anxiety

  Impaired vision, taste

  Midriaz

  Bradycardia

  Increased blood pressure

  Muscle spasm

  Involuntary muscle contraction

  Muscle weakness

  Frequency unknown:

  Increased liver enzyme levels

  - hives

  - itching

  - exanthema

  - bullous rash

  - angioedema

  - anaphylactic reactions

  - difficulty urinating

  - dysuria

  - urinary retention

  - dyspnea

  - worsening of bronchial asthma

  - bronchospasm

  - menstrual irregularities

  - fatigue

  - drug dependence in patients prone to drug abuse, as well as with long-term use of large doses of the drug.

  Abrupt withdrawal after long-term use of the drug can cause withdrawal syndrome (manifestations similar to symptoms of drug withdrawal: psychomotor agitation, anxiety, irritability, insomnia, tremor, paresthesia, attacks of phobia, hallucinations, confusion, depersonalization, paranoia, tinnitus, disorders gastrointestinal tract).

Contraindications

Hypersensitivity to the active substance or to other components of the drug

Acute alcohol intoxication

Acute poisoning with hypnotics, analgesics or psychotropic drugs

Severe liver failure

Severe renal failure (creatinine clearance less than 10 ml/min)

Epilepsy with frequent seizures

The period of treatment with MAO inhibitors and the next 14 days after their discontinuation

Not used to treat opioid addiction

Pregnancy or lactation period

Children under 18 years of age

Drug interactions

When Tramadol is prescribed simultaneously with drugs that depress the central nervous system, a mutual enhancement of central effects, including respiratory depression, is possible.

Inducers of microsomal oxidation (carbamazepine, barbiturates) reduce the severity of the analgesic effect and duration of action. Long-term use of opioid analgesics or barbiturates stimulates the development of cross-tolerance.

Anxiolytics increase the severity of the analgesic effect, the duration of anesthesia increases when combined with barbiturates. Naloxone activates breathing, terminating analgesia after the use of opioid analgesics. When used together with MAO inhibitors and within 14 days after their discontinuation, furazolidone, procarbazine and antipsychotics, there is a risk of developing seizures.

Quinidine increases the plasma concentration of tramadol and reduces the content of the M1 metabolite due to competitive inhibition of the CYP2D6 isoenzyme.

With the simultaneous use of Tramadol and warfarin, the risk of side effects from the blood coagulation system increases. Tramadol may cause seizures and/or the development of potentially life-threatening serotonin syndrome when used with serotonergic drugs.

Ketoconazole and erythromycin may interfere with the metabolism of tramadol. The clinical significance of this interaction has not been studied.

Ondansetron increases the need for tramadol in patients with postoperative pain.

Special instructions

You should not drink alcohol during treatment with Tramadol.

With prolonged use of Tramadol, addiction and drug dependence may develop.

Tramadol should not be used to treat drug withdrawal syndrome.

Particular caution should be exercised when prescribing the drug to patients with head injuries, increased intracranial pressure, moderate renal or hepatic impairment, patients with a tendency to seizures, as well as patients with hypersensitivity to opiates. The risk of seizures may be higher in patients who use anti-seizure medications concomitantly with Tramadol. Patients with a history of epilepsy and a tendency to epileptic seizures should be prescribed the drug only if absolutely necessary. Use with caution to treat patients with weakened respiratory function or in case of simultaneous use of drugs that depress the activity of the central nervous system, due to the risk of further respiratory depression.

The drug contains lactose, therefore patients with rare hereditary forms of galactose intolerance, lactase deficiency or glucose-galactose malabsorption syndrome should not use the drug.

Use in pediatrics

The drug is not used to treat children under 18 years of age.

Use during pregnancy or lactation

Tramadol penetrates the placental barrier, so using the drug during pregnancy is not recommended. If there are indications for pain therapy with opiates during pregnancy, you should limit yourself to a one-time use.

A small amount of Tramadol passes into breast milk, so the drug should not be used during breastfeeding. With a one-time use, breastfeeding can not be interrupted.

Features of the effect of the drug on the ability to drive vehicles and potentially dangerous mechanisms

When using the drug, you should refrain from driving vehicles and operating other mechanisms, which require increased attention and quick mental and motor reactions.

Overdose

Symptoms: vomiting, miosis, circulatory disorders, depression of consciousness (up to coma), convulsions, depression of the respiratory center until breathing stops completely.

Treatment aimed at ensuring airway patency, maintaining breathing and cardiovascular function.

The antidote for depression of the respiratory center is naloxone, and for convulsions - benzodiazepine. Tramadol is poorly eliminated by dialysis, so separate use of hemodialysis or hemofiltration is not enough.

Release form and packaging

each tablet contains the active substance - tramadol hydrochloride (in terms of 100% substance) - 50 mg; excipients - lactose monohydrate, povidone K-25, calcium stearate, microcrystalline cellulose.

Description

tablets from white to white with a yellowish tint, flat-cylindrical, chamfered. Marbling is allowed on the surface of the tablets.

Pharmacological action

Tramadol is a centrally active opioid analgesic. It has a mixed mechanism of action. It is a non-selective pure agonist of opioid c, d and k receptors and has maximum affinity for c receptors. Other mechanisms involved in the analgesic effects of tramadol include inhibition of neuronal norepinephrine reuptake and increased serotonin release. Tramadol also has an antitussive effect. Unlike morphine, analgesic doses of tramadol over a wide range do not depress respiration; gastrointestinal motility is less inhibited. The effect on the cardiovascular system is usually weak. The activity of tramadol is estimated to range from 1/10 to 1/6 of the activity of morphine.

Pharmacokinetics

When taken orally, absorption is 90%, bioavailability is 60-65%. The maximum concentration in plasma when taking tablets orally is achieved within 2 hours. Plasma protein binding – 20%. The volume of distribution depends on the route of administration; when taken orally, it is 306 liters. Passes through the blood-brain and other histohematic barriers, including the placental, and is secreted into breast milk. Biotransformation occurs in the liver through demethylation and conjugation with the formation of 11 metabolites (1 of them is active). The formation of the active metabolite (M1) depends on the activity of the CYP2D6 isoenzyme of cytochrome P-540. T1/2 in the second phase – 6 hours (tramadol), 7.9 hours (mono-O-desmethyltramadol); in patients over 75 years old – 7.4 hours (tramadol); for liver cirrhosis – 13.3±4.9 hours (tramadol), 18.5±9.4 hours (mono-O-desmethyltramadol), in severe cases – 22.3 hours and 36 hours, respectively. T1/2 with chronic renal failure (creatinine clearance less than 5 ml/min) – 11±3.2 hours (tramadol), 16.9±3 hours (mono-O-desmethyltramadol), in severe cases – 19.5 hours and 43. 2 hours respectively. Excreted by the kidneys (25-35% unchanged), the average cumulative renal excretion rate is 94%. About 7% is eliminated by hemodialysis.

Indications for use

Pain syndrome of strong and moderate intensity in malignant neoplasms, acute myocardial infarction, injuries, during painful diagnostic and therapeutic procedures.

Contraindications

Hypersensitivity to tramadol or to any of the excipients; porphyria; asthma attack; acute intoxication with alcohol, hypnotics, analgesics, opioids or psychotropic drugs; simultaneous use of MAO inhibitors (and 2 weeks after their discontinuation); epilepsy; drug withdrawal syndrome; dysfunction of the liver and kidneys; pregnancy; breastfeeding; children up to 14 years of age.

Pregnancy and lactation

Contraindicated.

Directions for use and doses

The tablets should be swallowed whole with a little water or the tablet should be dissolved in one glass of water. The drug is taken regardless of meals.

The dose of the drug should be adjusted depending on the intensity of the pain syndrome and the sensitivity of the patient. For pain relief, the minimum effective therapeutic dose should be selected. The duration of the course of treatment is also determined individually, but the drug should not be prescribed beyond the period justified from a therapeutic point of view. If long-term treatment with tramadol is necessary, the patient's condition and the justification for continued use of the drug should be carefully and regularly assessed at short intervals.

For adults and adolescents over 14 years of age, the usual dose for a single oral dose is 50 mg (1 tablet), repeated every 4-6 hours if necessary. If pain relief does not occur within 30-60 minutes, you can repeat the dose at the same dose. For severe pain, an initial dose of 100 mg (2 tablets) may be required. Do not exceed the maximum daily dose of 400 mg (8 tablets). Depending on the nature and intensity of the pain, the duration of action of the drug is 4-8 hours.

Elderly patients

There is usually no need to adjust the dose in patients under 75 years of age without clinical evidence of hepatic/renal impairment. In patients over 75 years of age, tramadol elimination may be prolonged. Therefore, if necessary, the interval between doses of the drug should be extended in accordance with the patient's need for pain relief.

Patients with impaired renal/liver function

In patients with renal/hepatic insufficiency, the elimination of the drug is slow. Therefore, prolongation of the interval between doses of the drug must be carefully monitored in accordance with the patient's pain relief needs.

In patients with creatinine clearance<30 мл/мин интервал между приемами препарата должен быть увеличен до 12 часов. Трамадол не рекомендуется принимать пациентам с тяжелой почечной недостаточностью (клиренс креатинина <10 мл/мин).

Because very little tramadol is removed by hemodialysis, it is usually not necessary to take an additional dose of tramadol after the hemodialysis procedure.

Side effect

The frequency of possible side effects is classified as follows:

Very common (≥1/10)

Often (≥1/100 to<1/10)

Uncommon (≥1/1000 to<1/100)

Rarely (≥1/10000 to<1/1000)

Very rarely (<1/10000)

Unknown (frequency cannot be estimated from available data).

The most common side effects that may occur during treatment with tramadol are nausea and dizziness, occurring in more than 1 in 10 patients.

From the cardiovascular system: uncommon: rapid heartbeat, weakness, vascular collapse. These side effects may occur especially in an upright position and during physical activity. Rarely: bradycardia, arterial hypertension.

From the central nervous system: very often: dizziness; often: headache; rarely: loss of coordination, fainting, speech disorders, changes in appetite, paresthesia, tremor, decreased breathing, epileptic seizures.

Epileptiform seizures have been observed mainly after the administration of high doses of tramadol or after the simultaneous use of drugs that can provoke seizures or lower the seizure threshold.

From the mental side: rarely: hallucinations, confusion, insomnia and nightmares.

Mental disorders may vary in manifestation (depending on the individual and duration of use of the drug). These may include changes in mood (usually high spirits, sometimes irritability), changes in cognitive and sensory abilities (changes in sensory perception and consciousness, which can lead to errors in decision making).

Dependence, abuse and withdrawal reactions may develop. Withdrawal reactions after stopping the drug are typical for opiates and include: agitation, anxiety, nervousness, insomnia, hyperkinesia, tremor, gastrointestinal symptoms. Very rarely, attacks of panic, anxiety, hallucinations, paresthesia, tinnitus, confusion, delirium, depersonalization, loss of sense of reality, and paranoia are observed.

From the organ of vision: rarely: blurred vision, miosis, mydriasis.

From the gastrointestinal tract: very often: nausea; often: vomiting, constipation, dry mouth; infrequently: diarrhea, stomach problems (for example, feeling of fullness in the stomach, flatulence).

From the respiratory system and mediastinal organs: rarely: shortness of breath, respiratory depression; unknown: worsening of existing asthma, although a cause-and-effect relationship has not been established.

From the skin: often: sweating; infrequently: itching, rash, redness of the skin. From the musculoskeletal system: rarely: decreased muscle strength.

From the liver and biliary tract: very rarely: increased transaminases.

From the urinary system: rarely: difficulty urinating, dysuria, urinary retention.

From the reproductive system: unknown: decreased libido, impotence, erectile dysfunction, lack of menstruation, infertility. If these adverse reactions develop, it is necessary to evaluate the level of sex hormones.

Other: rarely: allergic reactions (such as difficulty breathing, wheezing, swelling of the skin) and shock reactions (sudden circulatory failure).

When taking tramadol concomitantly with serotonergic drugs, patients should be carefully monitored if the following symptoms develop: agitation, hallucinations, rapid heartbeat, fever, increased sweating, chills or tremors, muscle twitching (muscle cramps) or rigidity (stiffness), loss of coordination, nausea, vomiting or diarrhea (see Precautions section - Serotonin syndrome).

Overdose

Symptoms: specific miosis, vomiting, cardiovascular collapse, impaired consciousness up to coma, convulsions and respiratory depression up to respiratory arrest.

Treatment: General first aid measures should be taken. Ensure airway patency (aspiration is possible), respiratory and circulatory support depending on symptoms.

In case of overdose with oral forms, gastric lavage and the use of activated charcoal are recommended within 2 hours after using tramadol; at a later date, cleansing the digestive system may be useful only if high doses are used.

The antidote for respiratory depression is naloxone. In animal studies, naloxone was found to have no effect on seizures. In this case, diazepam is administered.

Tramadol is excreted only in minimal quantities from the blood serum by hemodialysis or hemofiltration. Therefore, treatment of acute tramadol overdose with hemodialysis or hemofiltration is not sufficient to eliminate intoxication.

Interaction with other drugs

Tramadol should not be taken together with MAO inhibitors. Life-threatening reactions affecting the central nervous, respiratory, and cardiovascular systems have been observed in patients receiving MAO inhibitors within 14 days of use of the opioid pethidine. A similar interaction with MAO inhibitors when using tramadol cannot be excluded.

The simultaneous use of tramadol and drugs that depress the central nervous system, including alcohol, may enhance their effect on the central nervous system.

The results of pharmacokinetic studies have shown that concomitant or prior use of cimetidine (an enzyme inhibitor) is unlikely to lead to a clinically significant interaction. Concomitant or prior use of carbamazepine (an enzyme inducer) may reduce the analgesic effect and shorten the duration of action of tramadol.

The combination of mixed agonists/antagonists (eg, buprenorphine, nalbuphine, pentazocine) and tramadol is not recommended because the combination may theoretically reduce the analgesic effect of the pure agonist.

Caution should be exercised when using tramadol with coumarin derivatives (eg, warfarin) as there are reports of increased INR with severe bleeding and hemorrhage in some patients.

Drugs that inhibit CYP3A4, including ketoconazole and erythromycin, may inhibit the metabolism of tramadol (O-demethylation) and its active O-demethylated metabolite. The clinical significance of this interaction has not been studied.

A small number of studies have shown that pre- or postoperative use of selective 5HT3 serotonin receptor antagonists (ondansetron) increases the need for tramadol in patients with postoperative pain.

Long-term use of opioid analgesics and barbiturates stimulates the development of cross-tolerance. Quinidine increases the plasma concentration of tramadol and reduces the concentration of the M1 metabolite due to competitive inhibition of the CYP2D6 coenzyme. There is evidence of a decrease in plasma concentrations of fluoroquinolones (ciprofloxacin, ofloxacin) when premedicated with tramadol during surgical interventions.

Tramadol may stimulate the development of seizures and increase the ability of selective serotonin reuptake inhibitors, serotonin-norepinephrine reuptake inhibitors, tricyclic antidepressants, antipsychotics and other drugs that lower the seizure threshold, such as bupropion, mirtazapine, tetrahydrocannabinol, to cause seizures.

Concomitant use of tramadol and serotonergic drugs, such as selective serotonin reuptake inhibitors, serotonin-norepinephrine reuptake inhibitors, tricyclic antidepressants, MAO inhibitors and mirtazapine, may contribute to the development of serotonin syndrome (see Precautions - Serotonin syndrome).

There is a risk of developing serotonin syndrome when one of the following symptoms occurs:

Spontaneous muscle clonus;

Inducible or ocular clonus with agitation or sweating;

Tremor and hyperreflexia;

Hypertension, body temperature >38°C, inducible or ocular clonus.

Discontinuation of all serotonergic drugs is the first and main intervention for serotonin syndrome. In most patients, this leads to a rapid decrease in symptoms over 6-12 hours and their complete disappearance within 24 hours. Other necessary measures are symptomatic therapy and individual care.

Precautions

The drug is prescribed with caution for opioid addiction, traumatic brain injury, shock, loss of consciousness of unknown origin, dysfunction of the respiratory center, increased intracranial pressure in traumatic brain injury, brain diseases, impaired renal and liver function, and patients with epilepsy. The use of tramadol may complicate the diagnosis of acute pain in the abdominal region.

Tramadol is used with extreme caution in patients sensitive to opiates. Seizures have been reported in patients receiving tramadol at the recommended dosage. The risk may increase with doses greater than the recommended maximum daily dose (400 mg). When used together with drugs that lower the seizure threshold, tramadol may increase the risk of epileptic seizures. In patients with epilepsy or prone to epileptic seizures, tramadol is used only for health reasons.

In patients with respiratory depression or concomitant use of CNS depressants, or if the maximum recommended daily dose is significantly exceeded, the drug is prescribed with caution as respiratory depression may occur. Tramadol has a low addiction potential. With prolonged use, tolerance, mental and physical dependence may develop. In patients prone to drug abuse or dependence, treatment with tramadol should be carried out only for a short period and under strict medical supervision.

Tramadol is not suitable for replacement therapy in opioid-dependent patients. Although tramadol is an opioid agonist, it does not suppress morphine withdrawal symptoms.

The drug contains lactose, so patients with rare hereditary forms of galactose intolerance, lactase deficiency or glucose-galactose malabsorption syndrome should not use the drug.

Serotonin syndrome: When taking tramadol concomitantly with serotonergic drugs, patients should be carefully monitored if the following symptoms develop: agitation, hallucinations, rapid heartbeat, fever, increased sweating, chills or tremors, muscle twitching (muscle cramps) or rigidity (stiffness), loss of coordination, nausea, vomiting or diarrhea. Symptoms typically develop within hours to several days of starting concomitant opioid therapy with other drugs. However, symptoms may develop later, especially after increasing the dose of drugs. If serotonin syndrome is suspected, discontinue opioids and/or other concomitant medications.

Adrenal insufficiency: Patients should be closely monitored if symptoms of adrenal insufficiency occur, such as nausea, vomiting, loss of appetite, fatigue, weakness, dizziness, or low blood pressure. If adrenal insufficiency is suspected, diagnostic testing should be performed. If necessary, if the test result is positive, it is necessary to prescribe treatment with corticosteroids and discontinue opioids. If opioids are discontinued, a follow-up evaluation of adrenal function should be performed to determine the need to continue or discontinue corticosteroid therapy.

Androgen deficiency: Chronic use of opioids can affect the hypothalamic-pituitary-gonadal axis, which can lead to androgen deficiency, which manifests as low libido, impotence, erectile dysfunction, amenorrhea and infertility. If symptoms or signs of androgen deficiency appear, laboratory diagnosis should be performed.

Best before date

Do not use after the expiration date stated on the package.

Active ingredient

Tramadol hydrochloride (tramadol)

Release form, composition and packaging

Pills white with faintly noticeable inclusions, round, flat, slightly rough, chamfered, with a characteristic strawberry smell.

Excipients: lactose, microcrystalline cellulose, magnesium stearate, crospovidone, macrogol 4000, sodium saccharin, colloidal silicon oxide, flavoring.

10 pcs. - blisters (1) - cardboard packs.
10 pcs. - blisters (2) - cardboard packs.
10 pcs. - blisters (3) - cardboard packs.
10 pcs. - blisters (5) - cardboard packs.

Capsules hard gelatin, with a yellow body and a green cap; the contents of the capsules are white or almost white powder.

Excipients: calcium hydrogen phosphate, sodium starch glycolate, magnesium stearate.

Composition of the capsule shell: gelatin, titanium dioxide, yellow iron oxide, indigotine (E132).

10 pcs. - contour cell packaging (1) - cardboard packs.
10 pcs. - contour cell packaging (2) - cardboard packs.
10 pcs. - contour cell packaging (3) - cardboard packs.
10 pcs. - contour cell packaging (5) - cardboard packs.
10 pcs. - contour cell packaging (10) - cardboard packs.

10 ml - dark glass dropper bottle (1) - cardboard packs.
20 ml - dark glass dropper bottle (1) - cardboard packs.
50 ml - dark glass dropper bottle (1) - cardboard packs.
100 ml - dark glass dropper bottle (1) - cardboard packs.

Pharmacological action

Opioid analgesic with a mixed mechanism of action. Refers to centrally acting analgesics. Has a pronounced analgesic effect. Non-selective antagonist of opioid mu-, delta- and kappa receptors in the central nervous system with the highest affinity for mu receptors. Inhibits neuronal reuptake and enhances the release of serotonin. It also has an antitussive effect and does not interfere with gastrointestinal motility.

Duration of action is about 4-8 hours.

Pharmacokinetics

Suction

After administration, tramadol is quickly and almost completely absorbed from the gastrointestinal tract (about 90%). Cmax in the blood is determined after approximately 2 hours. Bioavailability is about 70%, does not depend on food intake and increases with repeated use of the drug.

Distribution

Plasma protein binding is about 20%. Tramadol penetrates the BBB and placental barrier. Approximately 0.1% is excreted in breast milk.

Metabolism

Metabolized by demethylation and conjugation to 11 metabolites, only one of which (O-demethyltramadol) has pronounced pharmacological activity (2-4 times higher than the activity of Tramadol).

Removal

Tramadol and its metabolites are excreted mainly by the kidneys (up to 90%) and through the intestines (about 10%). T1/2, regardless of the route of administration, is about 6 hours. In elderly patients, with and with renal failure, the T1/2 value increases.

Indications

— pain syndrome of moderate and severe intensity of various etiologies (postoperative period, trauma, pain in cancer patients);

— for the purpose of pain relief during painful diagnostic or therapeutic procedures.

Contraindications

- conditions accompanied by respiratory depression or severe depression of the central nervous system (poisoning with alcohol, sleeping pills, narcotic analgesics, psychotropic drugs);

- simultaneous use of MAO inhibitors (and 2 meals after their withdrawal);

- pregnancy;

- lactation period (use is possible only for health reasons);

- age up to 14 years;

- hypersensitivity to the drug.

Dosage

Pills

initial dose - 1 tablet. (50 mg) orally with a small amount of liquid, regardless of meals; if there is no effect within 30-60 minutes, you can take 1 more tablet; at strong pain a single dose can immediately be 100 mg (2 tablets). The effect, depending on the severity of pain, lasts for 4-8 hours. The daily dose of Tramadol should not exceed 400 mg (8 tablets).

The duration and regimen of use are determined by the attending physician

The tablets can be swallowed without chewing, washed down with the required amount of liquid, regardless of meals, or pre-dissolved in 1/2 glass of water.

Capsules

The dose of the drug is selected by the doctor individually depending on the intensity and nature of the pain.

Adults and teenagers over 14 years of age: initial dose - 1 capsule (50 mg) orally with a small amount of liquid, regardless of meals; if there is no effect within 30-60 minutes, you can take 1 more capsule; at severe pain a single dose can immediately be 100 mg (2 capsules). The effect, depending on the severity of pain, lasts for 4-8 hours. The daily dose of tramadol should not exceed 400 mg (8 capsules).

This dosage form should not be prescribed children weighing less than 25 kg and aged less than 14 years.

Elderly patients, patients with impaired liver and kidney function if necessary, the interval between doses of the drug should be increased.

The duration and regimen of use are determined by the attending physician.

Capsules should be swallowed without chewing, with the required amount of liquid, regardless of meals.

Oral solution

The dose of the drug is selected by the doctor individually depending on the intensity and nature of the pain.

Adults and teenagers over 14 years of age: the dose is 50 mg (20 drops). If there is no desired effect, you can take another 20 drops after 30-60 minutes. If necessary, the drug can be taken again after 4-6 hours. The daily dose should not exceed 400 mg (160 drops).

For children aged 1 to 14 years a single dose is 1-2 mg/kg body weight. Approximate dosages for children are given in the table (1 drop of solution corresponds to approximately 2.5 mg of tramadol g/x).

Elderly

patients, patients with impaired liver and kidney function if necessary, increase the interval between doses of the drug. The prescribed number of drops should be taken with a small amount of liquid or with sugar, regardless of meals. The duration and regimen of use are determined by the attending physician.

The bottle with the dispensing device is equipped with a child-proof cap. To open the bottle, press on the cap and rotate from left to right.

Side effects

The most common symptoms are dizziness, nausea, constipation, headache, drowsiness (in 15-30% of patients), vomiting, itching, symptoms of psychostimulant action, asthenia, sweating, dyspepsia, dry mouth, diarrhea (5-15% of patients).

With a frequency of less than 5%, weight loss, hypotension and tachycardia, paresthesia, hallucinations, tremor, abdominal pain, visual disturbances, and urinary retention are possible.

The incidence of side effects increases with increasing duration of drug use. With long-term use in large doses, the possibility of developing drug dependence cannot be ruled out.

About all side effects, incl. not listed above should be reported to your doctor.

Overdose

Symptoms: constriction of the pupils, vomiting, respiratory depression and convulsions.

Treatment: first aid for poisoning is maintaining adequate pulmonary ventilation and symptomatic therapy in a specialized department. In mild cases, gastric lavage is sufficient. The application is not decisive, because does not eliminate all symptoms of poisoning and may cause convulsions. Hemodialysis is not very effective. For convulsions, intravenous administration of diazepam is advisable.

Drug interactions

With the simultaneous use of Tramadol with drugs that have a depressant effect on the central nervous system, as well as with ethanol, their effect may be enhanced.

With simultaneous use of Tramadol with other inducers of metabolic enzymes, the analgesic effect of Tramadol may be weakened.

With systematic use of barbiturates, especially phenobarbital, there is a possibility of reducing the analgesic effect of opioid analgesics.

Long-term use of opioid analgesics or barbiturates stimulates the development of cross-tolerance.

Naloxone activates respiration, eliminating analgesia after the use of opioid analgesics.

Special instructions

In elderly patients, Tramadol is used at increased intervals.

The drug should be used with caution and under the supervision of a physician in patients with impaired renal and liver function, with traumatic brain injuries, increased intracranial pressure, patients with epilepsy, as well as persons with drug dependence on opioids.

Under close medical supervision and in reduced doses, Tramadol 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 the interaction effect.

With long-term use of carbamazepine, the effect of Tramadol may be weaker.

Impact on the ability to drive vehicles and operate machinery

While using tramadol, you should not drive a car or do other work that requires increased alertness.

Pregnancy and lactation

During pregnancy, long-term use of Tramadol should be avoided due to the risk of developing addiction in the fetus and withdrawal syndrome in the neonatal period.

If it is necessary to take it during lactation, it should be taken into account that Tramadol is excreted in breast milk in small quantities.

Tramadol is a narcotic analgesic that is used to relieve pain from serious injuries and tumors. The drug quickly eliminates pain, but is less effective than morphine.

Release form

Tramadol is mainly available as an injection solution. Other forms of the drug are also produced (tablets, capsules, rectal suppositories), but they are less easily absorbed by the body, and therefore are less often used in medical practice.

Tramadol injection solution is packaged in sterile glass bottles hidden in cardboard packaging.

Effect of the drug

Tramadol injections have the effect of an opium analgesic. They produce the following effect on the patient’s body:

• inhibits the conduction of pain impulses through the nervous system;
• opens calcium and potassium channels;
• increases the effect of sedatives;
• activates opioid receptors in the brain and spinal cord.

Important! The complex effect helps to almost completely get rid of pain, because even the spinal cord is susceptible to the influence of the opium analgesic.

Due to its strong narcotic effects, the drug is included in the priority list for drug control in the Russian Federation.

Composition of the substance

For production, auxiliary substances are used to create an injection solution, and the main active component is tramadol hydrochloride.

Pharmacokinetics

The substance is absorbed by cellular tissues by 90%. Of the absorbed tramadol hydrochloride, only 68% is absorbed. With constant use of the drug, the body begins to better perceive the drug and absorb large doses of the substance.

The medication penetrates the placental barrier and affects the embryo, so use during pregnancy is carried out with extreme caution. The active substance also reaches 0.1% into the breast milk of nursing mothers.

At the end of the journey, the substance is excreted by the kidneys, about 35% of tramadol hydrochloride is removed unchanged from its original form.

In general, the analgesic effect lasts no more than 4-8 hours, after which a repeated injection of the drug is required.

Indications for use of the drug

Tramadol is intended to combat severe pain. Therefore, it can be prescribed for any severe pain. Main areas of application:

• pain relief during operations;
• reduction of discomfort during endoscopy;
• combating pain in malignant tumors and cancer;
• decreased sensitivity of the chronically inflamed area;
• treatment of purulent inflammations accompanied by severe pain;
• relief of pain in patients who have suffered serious trauma;
• any other situations when a therapeutic or diagnostic procedure is accompanied by severe pain.

Since the substance is considered a narcotic and its release is strictly controlled in the Russian Federation, the analgesic cannot be used for any mild pain. "Tramadol" is aimed at getting rid of severe pain, which significantly reduces the quality of life, causes insomnia, moral and nervous exhaustion.

Method of use of solution for injection

The dosage should first be determined by the attending physician who prescribed the drug to the patient. The size of the daily dose of the drug depends on the following factors:

• patient weight;
• age;
• level of sensitivity to pain;
• the degree of pain that engulfs him.

Important! The more severe the pain and the harder it is for the patient to cope with it, the higher the dosage of Tramadol will be.

The course of therapy and its duration are also chosen by the doctor. You should not violate the recommendations given to them, as this may result in side effects or a decrease in the effectiveness of treatment.

You can administer the drug:

• subcutaneously;
• intravenously (you need to press the syringe slowly);
• intramuscularly.

To properly administer injections, you must have minimal medical skills.

If the doctor has not prescribed the patient a different course of the drug, the following instructions for using Tramadol injections should be followed:

1. Use 50-100 mg as an initial dose (this corresponds to 1-2 ml of solution).
2. If the effect of using the above dosage is insufficient, then increase the dose. Repeatedly (no earlier than 60 minutes) another 1 ml of solution for injection should be administered.
3. During the day, you can use up to 400 mg (8 ml of solution), if reduced dosages do not allow you to completely get rid of pain. Then the initial dose of the drug is 100 mg.
4. If the drug is used for elderly patients, the interval between doses of the substance should be greater than 60 minutes. This is due to the fact that the metabolism of older people slows down, which is why an overdose can occur if an analgesic is administered frequently.
5. When treating cancer, a dosage of more than 400 mg per day is allowed, but only with the permission of a specialist.

Contraindications for use

The medication has a number of contraindications for use. The main prohibition is under 14 years of age. Children do not tolerate opium analgesics well; they quickly develop dependence, which can result in serious health problems.

Other contraindications:

• use of MAO inhibitors while using an analgesic or 2 weeks before its prescription;
• allergic reactions characteristic of the use of opium drugs;
• risk of respiratory depression in bronchial asthma and similar conditions;
• severe liver and kidney dysfunction;
• CNS disorders.

It is strictly prohibited to prescribe the drug if the patient has recently suffered poisoning with sleeping pills, drugs or alcoholic beverages.

Side effects from using Tramadol

Since the drug is opium, the list of side effects on the patient’s body is quite extensive. The main problems that may arise during the use of an analgesic:

1. Increased sweating of the body. It is expressed even with moderate physical activity.
2. Confusion, slowness or acceleration of thoughts.
3. Headaches and migraines of a prolonged nature.
4. Increased stimulation of the nervous system, which is expressed by a number of side effects - hand tremors, confused speech, pronounced emotions, euphoria.
5. Fatigue quickly even when performing basic actions.
6. Tendency to constant drowsiness (if the opposite effect is not observed - hyperexcitability).
7. Insomnia.
8. Incorrect coordination of movements and limbs.
9. Attacks of rapid heartbeat.
10. Nausea progressing to vomiting.
11. Diarrhea and other temporary gastrointestinal disorders.
12. Depressive or manic states.
13. Memory impairment: amnesia, in which current events are poorly remembered.
14. Allergic reactions - skin itching, redness, rash and hives.
15. Dysfunctions of visual and taste perception, including hallucinations; sometimes - a violation of tactile perception.
16. Urinary excretion disorders: incontinence, painful urination, etc.
17. Changes in the menstrual cycle. Displacement or complete absence of menstruation (temporary).

Due to the wide range of side effects, Tramadol is prescribed only when the benefits of using the drug outweigh the possible harm. A striking example is cases where severe cancer pain does not allow one to move, work, or even eat food.

In case of prolonged use of the drug, which is not recommended for moderate pain, drug dependence may develop. It is expressed by a number of typical symptoms - irritability, sleep disturbances, excessive sweating, withdrawal symptoms, etc. When using Tramadol, you must constantly monitor the patient's condition and try to avoid addiction.

Admissibility of the drug during pregnancy and breastfeeding

Doctors allow the use of the medication both when carrying a child and when breastfeeding the baby. However, in both cases it is important to be careful.

Tramadol affects the baby to a lesser extent during breastfeeding. Then the percentage of the substance that reaches the baby does not exceed 0.1%. However, this percentage can negatively affect the child’s condition. If allergic reactions are noticed in the absence of complementary foods, obvious disturbances in the functioning of the nervous system (insomnia, apathy or increased activity), it is important to consult a specialist.

It is not recommended to use the drug during pregnancy, because in small doses it enters the placenta and can cause addiction in the embryo. A short course of the drug is allowed if the pain causes severe stress in the mother, which is even more dangerous for the child.

Interaction with alcohol

• hallucinations;
• disturbances of consciousness;
• coordination disorders;
• hypertension;
• increased nervous excitability;
• and other effects that are characteristic of a person in a state of alcohol or drug intoxication.

If the patient uses alcohol-based vital medications, it is recommended, if possible, to replace them with alcohol-free analogues. If this cannot be done, you should seek advice from the doctor who prescribed the drug or a similar specialist. He can make one of the following decisions:

• temporarily reduce the dosage of the alcohol-based drug;
• reduce the number of drug doses per month;
• temporarily discontinue the medication and replace it with a similar one.

It is impossible to completely cancel important medications, as this can lead to a sharp deterioration in health and even poses a risk of death.

If a patient who is prescribed Tramadol injections is prone to alcoholism, it is very important to monitor his behavior and not allow him to drink alcohol.

Interaction with other drugs

Do not use simultaneously with drugs that depress the central nervous system (sedatives). Tramadol causes increased sedation, especially if the drug contains ethanol.

It should also not be used simultaneously with Quinidine, as this drug can cause an increase in the concentration of Tramadol and an overdose.

With constant use of a narcotic analgesic simultaneously with a barbiturate, the effectiveness of both drugs may decrease.

Use while driving

It is not recommended to use the drug if the patient is about to drive or will soon perform life-threatening activities (interact with cutting machines in factories, etc.). During the period of use of the medication, it is recommended to take sick leave, abandon mental professional activities and hard work requiring fine motor skills and attention.

When using the medication, the following decreases:

• reaction speed;
• level of concentration;
• coordination of movements;
• fine motor skills of hands.

Overdose

An overdose can be achieved if you consume more than 8 mg of the drug per kilogram of body weight. Thus, the maximum permissible dosage of 400 mg, which is used for pain of moderate severity, is contraindicated in patients weighing up to 50 kg: it can cause an overdose.

If the dosages specified by the specialist are observed, only too frequent administration of the drug can lead to an overdose. This is especially true for older people, for whom the duration of removal of the medication from the body is increased (more than 8 hours).

The medication does not immediately lead to the maximum degree of overdose; at first, you may not notice the symptoms of the disorder at all. Depending on how much the permissible dose was exceeded, symptoms of three stages of poisoning develop:

1. First stage. It is expressed by typical symptoms of poisoning: nausea and increased sweating, decreased heart rate and decreased blood pressure. Mild fever rarely occurs. The patient may notice dizziness, headaches, “spots” - black spots, blurred vision.
2. Second stage. Breathing problems begin. The patient breathes shallowly and heavily. The heartbeat continues to worsen, and constriction of the pupils is observed. Severe pain occurs in the abdominal area. Diarrhea may occur. It becomes difficult to move, and the body’s reactions noticeably slow down.
3. Third stage. Seizures and other symptoms of epilepsy may occur, and swelling of the lungs or larynx often occurs. Choking or spasm of the lungs begins, which can lead to loss of consciousness. CNS depression often results in coma. If the patient is not helped, death may occur.

This overdose cannot be compensated for by gastric lavage. If you notice symptoms of exceeding the permissible dose, you must consult a doctor so that he can quickly compensate for the dangerous condition with the help of detoxification and special medications.

Since an overdose can lead to coma and death, you must carefully follow the doctor’s instructions and carefully measure the required dose of the drug. This is especially true for older people. They cannot simply follow the instructions in the package: it is important to visit a specialist so that he can professionally and individually prescribe a course of therapy.

Analogues of the drug

The drug can be changed to similar narcotic analgesics. The use of non-narcotic painkillers for severe pain is not justified.

Possible analogues:

• Tramal;
• Protradon;
• Sintradon;
• Tramolin;
• Tramundin retard;
• Tramolin retard.

Tramadol can be replaced with analogues only with the permission of a doctor.

You can also use different forms of the drug:

• capsules;
• pills;
• solution for internal use.

If it is inconvenient to make constant injections, you can replace the release form with one of the above. But to do this, you need to visit the doctor again and ask for a prescription, otherwise the drug will not be sold even if you have a prescription for the purchase of ampoules.

When changing the form of release of the drug, you need to take into account that the degree of absorption of different versions of the drug is different. Therefore, the dosage is slightly different. The doctor will make any necessary changes to the prescription.

Storage conditions, expiration date and release from pharmacies

The drug is released strictly according to prescription. Purchasing without a prescription or using counterfeit prescriptions is punishable by law.

Storage conditions: at temperatures up to 20 degrees, in a dry and dark place. It is advisable not to remove the ampoules from the packaging. Keep away from children.

Shelf life – 2 years.

General characteristics. Compound:

Active substance: tramadol hydrochloride 100.0 mg

Excipients: lactose monohydrate (milk sugar) - 225.0 mg; potato starch - 85.0 mg; magnesium stearate - 5.0 mg; talc - 5.0 mg; microcrystalline cellulose - 60.0 mg; povidone (polyvinylpyrrolidone) - 20.0 mg.

Pharmacological properties:

Pharmacodynamics. Tramadol is an opioid analgesic with a central mechanism of action. It is a non-selective full agonist of |>, 5- and k-opioid receptors with high affinity for beta-opioid receptors. The second mechanism of action of tramadol, which enhances its analgesic effect, is the suppression of the reuptake of norepinephrine by neurons and increased release of serotonin.
Tramadol has an antitussive effect. In therapeutic doses it does not depress respiration and has virtually no effect on intestinal motility. The effect on the cardiovascular system is weak. The analgesic potential of tramadol is 1/10-1/6 of the activity of morphine.

Pharmacokinetics. When taken orally, absorption is about 90%. The half-absorption period is about 0.4 hours. After oral administration, bioavailability is about 68%. Compared to other opioid analgesics, the absolute bioavailability of tramadol is high. The time to reach maximum plasma concentration after oral administration is 2 hours.
Plasma protein binding is about 20%. Penetrates through the blood-brain and placental barriers. Minor amounts of tramadol and its desmethylated derivative (0.1% and 0.02%, respectively) pass into breast milk.
The isoenzymes CYP3A4 and CYP2D6 are involved in the metabolism of tramadol, the suppression of which by other substances may affect the concentration of tramadol and its active metabolite in the blood. To date, clinically significant interactions with other drugs mediated by this mechanism have not been identified.
Tramadol and its metabolites are excreted primarily in the urine, with an average cumulative renal excretion rate of 90%.
The half-life of tramadol (T) is approximately 6 hours, regardless of the route of administration. In patients over 75 years of age, the half-life may be increased by 1.4 times; for liver cirrhosis up to 13.3±4.9 hours (tramadol), 18.5±9.4 hours (O-desmethyltramadol), in severe cases - up to 22.3 hours and 36 hours, respectively. T1/2 at (creatinine clearance less than 5 ml/min) - 11±3.2 hours (tramadol), 16.9±3 hours (O-desmethyltramadol), in severe cases - up to 19.5 hours and 43. 2 hours respectively.
Metabolized in the liver by N- and O-demethylation followed by conjugation with glucuronic acid. Only O-desmethyltramadol has pharmacological activity. There are significant individual differences in the concentrations of other metabolites. 11 tramadol metabolites were detected in urine. At therapeutic doses, the pharmacokinetics of tramadol are linear. The relationship between tramadol serum concentration and analgesic effect is dose-dependent, varying among individuals. Tramadol serum concentrations of 100-300 ng/ml are usually effective.

Indications for use:

Moderate and severe pain syndrome of various etiologies (for example, pain in cancer patients, with injuries and in the postoperative period). Painful diagnostic and therapeutic procedures.

Important! Get to know the treatment

Directions for use and dosage:

Inside. The tablets are swallowed whole, regardless of food intake, without chewing, with a sufficient amount of liquid.
The dose should be selected individually depending on the intensity of the pain syndrome and the individual sensitivity of the patient. Recommended doses are approximate. The duration of treatment with the drug is determined individually. When treating, it is always necessary to select the minimum effective dose of the drug. When treating chronic pain syndrome, you should adhere to a specific schedule for taking the drug. Adults and adolescents over 14 years of age The single dose is 50 mg of tramadol. If the analgesic effect is insufficient, 50 mg of tramadol is taken again after 30-60 minutes. For intense pain, the recommended single dose is 100 mg of tramadol.
Depending on the intensity of the pain syndrome, the analgesic effect usually lasts for 4-6 hours. In the postoperative period, short-term use of higher doses of the drug is possible (in the early stages after surgery). The daily dose of tramadol should not exceed 400 mg, except in special circumstances (for example, cancer pain or severe post-operative pain).
Patients over 75 years of age
In patients over 75 years of age without clinical evidence of hepatic or renal impairment, no dose adjustment of tramadol is usually required. In patients in this age group, the elimination of tramadol may be slower. Therefore, if it seems necessary, the interval between doses of the drug can be increased according to the patient's condition. Patients with renal failure or on dialysis and patients with liver failure
If renal and/or liver function is impaired, the elimination of tramadol from the body is slowed down. If necessary, the interval between doses of the drug should be increased.
Duration of therapy
Tramadol should under no circumstances be used for longer than necessary. With long-term use of tramadol, depending on the intensity or etiology of the pain syndrome, periodic monitoring is necessary (if necessary, with breaks in taking the drug) to determine the need for further therapy and dose optimization.

Features of application:

In patients with opioid dependence, head injuries, shock, in patients with disturbances of 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 severe intolerance to opioids of allergic and non-allergic origin.
In patients taking tramadol in recommended doses, side effects were observed. 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 prone to developing seizures should take tramadol only for health reasons. Tramadol has a lower potential for drug dependence. However, with prolonged use, addiction, physical and mental dependence are possible. In patients prone to drug abuse or drug dependence, treatment with tramadol should be carried out only in short courses and under medical supervision.
Tramadol is not suitable for substitution therapy in patients with opioid dependence. Although tramadol is an opioid agonist, it cannot reverse opioid withdrawal.

INFLUENCE ON THE ABILITY TO DRIVE A VEHICLE AND WORK WITH MECHANISMS
Even at recommended doses, tramadol can cause drowsiness and other adverse drug reactions from the central nervous system, so it can impair the ability to drive vehicles and engage in other activities that require increased concentration and speed of psychomotor reactions. When taking tramadol, it is necessary to refrain from driving vehicles and engaging in potentially hazardous activities that require increased concentration and speed of psychomotor reactions, especially when used simultaneously with other psychotropic drugs.

Side effects:

The most common side effects are dizziness, noted in more than 10% of patients.
The frequency is determined as follows:
Very often: 21/10;
Often: 21/100,<1/10;
Uncommon: 21/1000,<1/100;
Rare: >1/10,000<1/1000;
Very rarely:<1/10 000;
Frequency unknown: cannot be determined from available data.
- From the cardiovascular system: Uncommon: effects on cardiovascular regulation (palpitations, orthostatic hypotension or). These side effects are mainly observed with intravenous administration of the drug or with significant physical exertion. Rarely: increased blood pressure.
- Metabolic and nutritional disorders Rare: changes in appetite.
- From the respiratory system Rarely: respiratory depression, . If recommended doses are significantly exceeded with the simultaneous use of other drugs that depress the central nervous system (CNS), respiratory depression is possible.
A deterioration in bronchial asthma was noted, however, a cause-and-effect relationship with the use of the drug has not been established. Nervous system disorders Very common: dizziness. Often: drowsiness. Rarely: convulsions, involuntary muscle contractions, loss of coordination, fainting.
Convulsions are possible after the use of high doses of tramadol and when used simultaneously with drugs that lower the seizure threshold. Frequency unknown: speech disorders.
-Psychological disorders: Rarely: confusion, and nightmares. After using tramadol, various rarely observed adverse reactions from the psyche are possible (depending on the personal characteristics of the patient and the duration of treatment). These adverse drug reactions include changes in mood (usually, sometimes), changes in motor activity (usually decreased, sometimes increased), and cognitive and perceptual disturbances (eg, decision-making, perceptual disturbances). Drug dependence may develop. Possible withdrawal symptoms are similar to those of opioid withdrawal: anxiety, nervousness, sleep disturbances, hyperkinesia, tremor, and gastrointestinal symptoms. Other symptoms that are very rare during tramadol withdrawal include: severe anxiety, hallucinations, paresthesia, tinnitus and other very rare central nervous system symptoms (disorientation in time and space, hallucinations, depersonalization, derealization, paranoia).
-On the part of the organ of vision Rarely: blurred vision. Frequency unknown: .
-Digestive system disorders Very common: nausea. Common: , dry mouth, . Uncommon: gagging, feeling of heaviness in the epigastrium,.
-Skin and subcutaneous tissue disorders Common: sweating. Uncommon: itching, rash.
- From the musculoskeletal system Rarely: muscle weakness.
-On the part of the liver and biliary tract. In some cases, there was an increase in the activity of “liver” enzymes that coincided with tramadol therapy.
- From the kidneys and urinary system Rarely: urinary disorders (difficulty urinating and urinary retention).
-On the part of the immune system
Rarely: allergic reactions (shortness of breath, wheezing, angioedema) and anaphylaxis.
-General disorders. Often: increased fatigue.

Interaction with other drugs:

Tramadol should not be used simultaneously or within 14 days after discontinuation of MAO inhibitors. Life-threatening drug interactions involving central nervous system, respiratory and cardiovascular symptoms have been reported in patients treated with MAO inhibitors within 14 days prior to initiation of the opioid analgesic pethidine. Similar interactions with MAO inhibitors are possible when using tramadol. Concomitant use of tramadol and CNS depressants, including alcohol, may increase CNS adverse reactions. It is noted that with simultaneous or previous use of cimetidine (an inhibitor of microsomal liver enzymes), clinically significant interactions are unlikely. Simultaneous or previous use of carbamazepine (an inducer of microsomal liver enzymes) may reduce the analgesic effect of tramadol and shorten its duration of action.
It is not recommended to combine tramadol with opioid agonists-antagonists (eg, buprenorphine, nalbuphine, pentazocine), as the analgesic effect of tramadol as a full opioid agonist may be reduced. Tramadol can cause seizures and enhance the effect of selective serotonin reuptake inhibitors (SSRIs) and tricyclic antidepressants. antipsychotics and other drugs that lower the seizure threshold, thus leading to the development of seizures.
In isolated cases, the development of serotonin syndrome has been observed in association with the use of tramadol in combination with other serotonergic drugs, such as selective serotonin reuptake inhibitors (SSRIs) or MAO inhibitors. Possible symptoms of serotonin syndrome include confusion, agitation, pyrexia, sweating, ataxia, hyperreflexia, myoclonus, and diarrhea. Withdrawal of serotonergic drugs causes rapid resolution of symptoms. The necessary therapy is determined by the clinical picture and severity of symptoms.
With the simultaneous use of tramadol and indirect anticoagulants - coumarin derivatives (for example, warfarin), it is necessary to carefully monitor patients, as some of them have experienced an increase in the international normalized ratio (INR) with the development of bleeding and ecchymosis.
Other inhibitors of the CYP3A4 isoenzyme, for example, ketoconazole and erythromycin, may inhibit the metabolism of tramadol (N-demethylation) and possibly the active O-desmethyltramadol. The clinical significance of this interaction has not been studied.
There is limited evidence that pre- or postoperative use of antiemetics of the 5-HT3-serotonin receptor blocker group (eg, ondansetron) increased the need for tramadol in patients with postoperative pain syndrome.

Contraindications:

Hypersensitivity to tramadol or other components of the drug. Acute with alcohol, hypnotics, analgesics, opioids or other psychotropic drugs. The simultaneous use of tramadol with monoamine oxidase inhibitors (MAOIs), as well as within 14 days after stopping their use, is contraindicated. , not amenable to adequate drug control. As a drug for the treatment of opioid withdrawal syndrome. Age up to 14 years. Lactase deficiency, lactose intolerance, glucose-galactose malabsorption.

WITH CAUTION
In patients with drug dependence on opioids. With traumatic brain injury, in patients in a state of shock, in patients with impaired consciousness of unknown origin, in patients with breathing disorders and impaired activity of the respiratory center, with increased intracranial pressure.
In patients with established severe intolerance to opioids of allergic and non-allergic origin.
In case of epilepsy that can be adequately controlled with medication, or in patients susceptible to the development of seizures, tramadol can be used only for health reasons (see section “Special Instructions”).
In patients with a history of drug abuse or opioid dependence, tramadol treatment should be administered in short courses and under medical supervision (see section "Special Instructions").

Overdose:

In case of an overdose of tramadol, symptoms characteristic of narcotic analgesics should be expected. Possible symptoms: vomiting, collapse, depression of consciousness up to coma, convulsions, depression of the respiratory center to apnea.
Treatment: ensuring airway patency. Maintaining breathing and activity of the cardiovascular system, depending on the symptoms. If breathing is impaired, naloxone is administered. For seizures, diazepam should be administered intravenously. In case of an overdose of the drug in dosage forms for oral administration, activated charcoal must be administered and administered within the first two hours after the overdose. After taking particularly large doses of the drug in tablets, removal of stomach contents can be effective at a later date. and are ineffective.

Storage conditions:

Store in a dry place, protected from light, at a temperature not exceeding 25 °C. Keep out of the reach of children.

Vacation conditions:

By prescription

Package:

Tablets 100 mg.
10, 20 tablets in a blister pack made of polyvinyl chloride film and printed varnished aluminum foil.
10, 20, 30, 40, 50 or 100 tablets in a polymer container for medicines. One container or 1, 2, 3, 4, 5, 6, 8 or 10 blister packs along with instructions for use are placed in a cardboard pack.