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Tramadol | Facts You Should Remember

Tramadol has an analgesic (opioid) effect. Activates opiate receptors (mu, delta, and kappa) on the pre- and postsynaptic membranes of the afferent fibers of the nociceptive system, in the brain and the gastrointestinal tract; promotes the discovery of potassium and calcium channels, causes hyperpolarization of the membranes and inhibits the conduction of nerve impulses. Slows down the destruction of catecholamines and stabilizes their content in the central nervous system.

The analgesic effect is due to a decrease in the activity of nociceptive and an increase in the antinociceptive systems of the body. Sedative impact on the cerebral cortex inhibits a cough and respiratory centers, stimulates the starting area of the vomiting center, the nucleus of the oculomotor nerve; causes spasm of sphincter smooth muscle. When administered parenterally, the analgesic effect develops in 5-10 minutes and lasts 4-6 hours.

Pharmacokinetics
Plasma protein binding – 20%. The amount of distribution depends on the method of administration; with a / in the introduction of 203 liters. Passes through the hematoencephalic and other histohematogenous barriers, including the placenta, is secreted into breast milk. Biotransformation is carried out in the liver by demethylation and conjugation with the formation of 11 metabolites (1 of them is active). The structure of an active metabolite (M1) depends on the activity of the CYP2D6 cytochrome P-540 isoenzyme.

Excreted mainly by the kidneys (90%) and intestines (about 10%). The kidneys excrete approximately 30% of the administered dose of the drug in unchanged form, 60% – in the formation of metabolites and glucuronic conjugates. In violation of the functions of the liver and kidneys (Cl creatinine less than 80 ml/min), the elimination of tramadol slows down.

Indications for use
Medium intensity pain syndrome in malignant tumors, acute myocardial infarction, injuries, diagnostic and therapeutic procedures; neuralgia

Contraindications
Hypersensitivity, acute alcohol poisoning and intoxication with depriving drugs and drugs that depress the central nervous system, epilepsy, suicide risk, susceptibility to substance abuse, impaired liver and kidney function, breastfeeding. Children’s age up to 1 year. The use of tramadol is contraindicated in patients taking drugs inhibitors of MAO.

Carefully. In children older than one year, the only indication for the use of tramadol is a pronounced pain syndrome caused by acute or chronic pain.

Pregnancy and lactation
Use during pregnancy is allowed if the expected effect of therapy outweighs the potential risk to the fetus. At the time of treatment should stop breastfeeding. In the case of a single dose, there is no need to interrupt breastfeeding.

Dosage and administration
Designed for intravenous, intramuscular, subcutaneous administration. In/to the introduction is carried out by slow injection, preferably in the superficial brachial vein, with a speed of 1 ml/min.
The dose of the drug should be adjusted depending on the intensity of pain and sensitivity of the patient, for anesthesia should choose the minimum effective therapeutic dose. 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.

For adults and adolescents over the age of 14, the usual single dose for IV administration is 0.05-0.1 g (50-100 mg). If necessary, in case of insufficient effect, further injections are possible in 30-60 minutes, up to the maximum possible daily dose. When conducting intravenous drip infusion, the initial dose of 0.05-0.1 g (50-100 mg) is administered intravenously slowly (over 20 minutes), then the supporting drip infusion is started at a rate of 12 mg / h to the maximum possible daily dose, which is 0.4 g (400 mg). The effect lasts an average of 4-8 hours, depending on the nature and intensity of the pain.

With the / m and s / c administration, the initial dose for adults and children over 14 years old is usually 0.05-0.1 g (50-100 mg), further injections are possible, if necessary, at a dose of 0.03 g (30 mg) to the maximum possible daily dose.
The maximum daily dose of the drug should not exceed 0.4 g (400 mg).
For children aged 1 to 14 years, tramadol is recommended to be administered in a single dose at the rate of 1-2 mg/kg, and the maximum daily dose should not exceed 4-8 mg/kg. The drug should be diluted with water for injection; it is necessary to consider what concentrations of the drug can be obtained (1 ml of the drug contains 0.05 g (50 mg), 2 ml – 100 mg of tramadol).

For dilution of the drug, you can use water for injection, saline, and 5% glucose solution. It is recommended to use freshly prepared solutions. Tramadol solutions can be applied within 24 hours from the moment of preparation, provided they are stored in a refrigerator at a temperature of 1 to 5 ° C.

Elderly patients:
Usually, there is no need to adjust the dose in patients under 75 years of age without clinical manifestations of hepatic/renal failure. In patients older than 75 years, the elimination of tramadol may be extended. Therefore, if necessary, the interval between doses of the drug should be lengthened following the need for patient pain relief.

Patients with impaired renal / liver function:
In patients with renal/hepatic insufficiency, drug excretion is delayed. Therefore, the lengthening of the interval between doses of the drug must be carefully controlled per the need for patient pain relief.

Side effect
Tramadol is relatively well tolerated, in therapeutic doses does not cause pronounced respiratory depression. May cause dizziness, euphoria, dysphoria, nervousness, agitation, anxiety, tremor, muscle spasms, emotional lability, hallucinations, collapse, lethargy, drowsiness, sleep disturbances, confusion, movement coordination, depression, amnesia, impaired cognitive function, sleep disorders, confusion instability of gait, convulsions, nausea, pain in the epigastric region, vomiting, constipation, diarrhea, difficulty in swallowing, blurred vision, taste, tachycardia, manifestation of vasodilation – tachycardia, orthostatic hypotension , fainting, difficulty urinating, irregular menstruation.

In rare cases, as a rule, with prolonged use of tramadol, addiction, dependence, “cancellation” syndrome are possible; pronounced respiratory depression, hypotension, collapse.

When using tramadol in patients with aggravated allergic history, allergic reactions are possible: urticaria, pruritus, exanthema, bullous rash, intense itching in the nasal cavity, marked redness of the wings of the nose, itching in the lower extremities.
The incidence of side effects increases with increasing duration of the drug.

Overdose
Symptoms: miosis, convulsions, collapse, coma, depression of the respiratory center, apnea. Treatment: ensuring airway patency, maintaining adequate pulmonary ventilation, maintaining the cardiovascular system, symptomatic therapy (opiate effects can be stopped by naloxone; convulsions by benzodiazepines (diazepam)). In chronic poisoning with tramadol may develop withdrawal syndrome.

Interaction with other drugs
Enhances the effects of tranquilizers, sleeping pills, sedatives and anesthetics, anxiolytics, alcohol. Analeptics and psychostimulants reduce activity, naloxone, and naltrexone (direct antagonists) completely block. In combination with selective serotonin reuptake inhibitors (some antidepressants and JIC, reducing appetite), tricyclic antidepressants, other tricyclic compounds (for example, with promethazine), anti-migraine drugs (triptanami), narcotic analgesics, MAO inhibitors, neuroleptics, and other anti-depressant drugs (triptanami), narcotic analgesics, MAO inhibitors, neuroleptics, and anti-depressants; threshold convulsive readiness, such as bupropion, mirtazapine, tetrahydrocannabinol, increases the risk of seizures.

In patients treated with carbamazepine for a long time, the metabolism of tramadol is significantly increased, which may require an increase in the analgesic dosage.

The drug should not be combined with narcotic analgesics from the group of complete (promedol, fentanyl) or partial agonists (buprenorphine), as well as antagonist agonists (nalbuphine, butorphanol) opioid receptors. Inductors of microsomal oxidation (including carbamazepine, barbiturates) reduce the duration of the analgesic effect.

Prolonged use of opioid analgesics and barbiturates stimulates the development of cross-tolerance plasma concentrations of tramadol and reduces the level of Ml metabolite due to competitive inhibition of coenzyme CYP2D6. There is evidence of a decrease in plasma concentrations of fluoroquinolones (ciprofloxacin, ofloxacin) during premedication with tramadol during surgical interventions. Tramadol is pharmaceutically incompatible “in one syringe” with solutions of nonsteroidal anti-inflammatory drugs, nitroglycerin.

The simultaneous use of tramadol and serotonergic drugs such as selective serotonin reuptake inhibitors, serotonin-noradrenaline reuptake inhibitors, tricyclic antidepressants, MAO inhibitors, and mirtazapine can contribute to the development of serotonin syndrome.

There is a possibility of developing serotonin syndrome when one of the following symptoms is observed:
• spontaneous muscle clonus;
• induced or ocular clonus with agitation or sweating;
• tremor and hyperreflexia;
• hypertension, body temperature> 38 ° C, induced or ocular clonus.
Withdrawal of serotonergic drugs usually leads to quick recovery. Treatment depends on the type and severity of the symptoms.

Application features
Do not use for the treatment of drug withdrawal syndrome. Do not use ethanol at the same time.
Precautionary measures
With caution, the drug is prescribed to patients with impaired renal function and liver, with head injuries, increased intracranial pressure, patients with epilepsy, with loss of consciousness of unknown origin, impaired function of the respiratory center. The use of tramadol can complicate the diagnosis of acute pain in the abdominal region.

Under careful observation in reduced doses, tramadol should be used against the background of the action of anesthetics, hypnotic drugs, anxiolytics, and antidepressants to avoid excessive depression of the central nervous system and suppressing the activity of the respiratory center.
The use of tramadol makes it difficult to perform work that requires a high rate of mental and physical reactions and increased concentration of attention (driving vehicles, controlling machinery, instruments, etc.).

The use of tramadol makes it difficult to perform work that requires a high rate of mental and physical reactions and increased concentration of attention (driving vehicles, controlling machinery, instruments, etc.).
Do not use for the treatment of drug withdrawal syndrome. Do not use ethanol at the same time.

Precautionary measures
With caution, the drug is prescribed to patients with impaired renal function and liver, with head injuries, increased intracranial pressure, patients with epilepsy, with loss of consciousness of unknown origin, impaired function of the respiratory center. The use of tramadol can complicate the diagnosis of acute pain in the abdominal region.

Under careful observation in reduced doses, tramadol should be used against the background of the action of anesthetics, hypnotic drugs, anxiolytics, and antidepressants to avoid excessive depression of the central nervous system and suppressing the activity of the respiratory center.
The use of tramadol makes it difficult to perform work that requires a high rate of mental and physical reactions and increased concentration of attention (driving vehicles, controlling machinery, instruments, etc.).


Do not use for the treatment of drug withdrawal syndrome. Do not use ethanol at the same time.
Precautionary measures
With caution, the drug is prescribed to patients with impaired renal function and liver, with head injuries, increased intracranial pressure, patients with epilepsy, with loss of consciousness of unknown origin, impaired function of the respiratory center. The use of tramadol can complicate the diagnosis of acute pain in the abdominal region.

Under careful observation in reduced doses, tramadol should be used against the background of the action of anesthetics, hypnotic drugs, anxiolytics, and antidepressants to avoid excessive depression of the central nervous system and suppressing the activity of the respiratory center.
The use of tramadol makes it difficult to perform work that requires a high rate of mental and physical reactions and increased concentration of attention (driving vehicles, controlling machinery, instruments, etc.).

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