Tramaklosidol (Tablets, Solution) Instructions for Use

ATC Code

N02AX02 (Tramadol)

Active Substance

Tramadol (Rec.INN registered by WHO)

Clinical-Pharmacological Group

Opioid analgesic with a mixed mechanism of action

Pharmacotherapeutic Group

Opioid analgesic agent

Pharmacological Action

An opioid analgesic, a derivative of cyclohexanol. It is a non-selective agonist of μ-, Δ-, and κ-receptors in the CNS. It is a racemate of (+) and (-) isomers (50% each), which are involved in the analgesic effect in different ways.

The (+) isomer is a pure opioid receptor agonist, has low tropism, and does not have pronounced selectivity for different receptor subtypes. The (-) isomer, by inhibiting neuronal norepinephrine reuptake, activates descending noradrenergic influences. Due to this, the transmission of pain impulses to the substantia gelatinosa of the spinal cord is disrupted.

It causes a sedative effect. In therapeutic doses, it practically does not depress respiration. It has an antitussive effect.

Pharmacokinetics

After oral administration, it is rapidly and almost completely absorbed from the gastrointestinal tract (about 90%). C_max in plasma is reached 2 hours after oral administration. Bioavailability after a single dose is 68% and increases with repeated use.

Plasma protein binding is 20%. Tramadol is widely distributed in tissues. V_d after oral administration and IV injection is 306 L and 203 L, respectively. It crosses the placental barrier in a concentration equal to the concentration of the active substance in the plasma. 0.1% is excreted in breast milk.

It is metabolized by demethylation and conjugation into 11 metabolites, only 1 of which is active.

It is excreted by the kidneys – 90% and through the intestines – 10%.

Indications

Moderate and severe pain syndrome of various origins (including in malignant tumors, acute myocardial infarction, neuralgia, injuries). Performing painful diagnostic or therapeutic procedures.

ICD codes

Dosage Regimen

Tablets, Solution

For adults and children over 14 years of age, a single oral dose is 50 mg, rectal – 100 mg, IV slowly or IM – 50-100 mg. If the effectiveness after parenteral administration is insufficient, then after 20-30 minutes, an oral dose of 50 mg is possible.

For children aged 1 to 14 years, the dose is set at 1-2 mg/kg.

The duration of treatment is determined individually.

Maximum dose for adults and children over 14 years of age, regardless of the route of administration, is 400 mg/day.

Adverse Reactions

From the CNS dizziness, weakness, drowsiness, confusion; in some cases – seizures of cerebral origin (with IV administration in high doses or with simultaneous administration of neuroleptics).

From the cardiovascular system tachycardia, orthostatic hypotension, collapse.

From the digestive system dry mouth, nausea, vomiting.

From metabolism increased sweating.

From the musculoskeletal system muscle weakness.

Contraindications

Acute intoxication with alcohol and drugs that have a depressant effect on the CNS, children under 1 year of age, hypersensitivity to tramadol.

Use in Pregnancy and Lactation

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

If it is necessary to use during lactation (breastfeeding), it should be taken into account that Tramadol is excreted in breast milk in small amounts.

Use in Hepatic Impairment

Should be used with caution in patients with impaired liver function.

Use in Renal Impairment

Should be used with caution in patients with impaired renal function.

Pediatric Use

Contraindicated in children under 1 year of age. For children aged 1 to 14 years, the dose is set at 1-2 mg/kg.

Tramadol in the form of prolonged-release dosage forms should not be used in children under 14 years of age.

Special Precautions

Should be used with caution in cases of seizures of central origin, drug dependence, confusion, in patients with impaired renal and liver function, as well as in cases of hypersensitivity to other opioid receptor agonists.

Tramadol should not be used for 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.

It is not recommended for the treatment of withdrawal syndrome from narcotic substances.

Combination with MAO inhibitors should be avoided.

Alcohol consumption should be avoided during treatment.

Tramadol in the form of prolonged-release dosage forms should not be used in children under 14 years of age.

Effect on the ability to drive vehicles and operate machinery

During the use of tramadol, it is not recommended to engage in activities that require increased attention and high speed of psychomotor reactions.

Drug Interactions

With simultaneous use with drugs that have a depressant effect on the CNS, and with ethanol, an increase in the depressant effect on the CNS is possible.

With simultaneous use with MAO inhibitors, there is a possibility of developing serotonin syndrome.

With simultaneous use with serotonin reuptake inhibitors, tricyclic antidepressants, antipsychotic drugs, and other agents that lower the seizure threshold, the risk of seizures increases.

With simultaneous use, the anticoagulant effect of warfarin and phenprocoumon is enhanced.

With simultaneous use with carbamazepine, the concentration of tramadol in the blood plasma and its analgesic effect are reduced.

Cases of serotonin syndrome and seizures have been described with simultaneous use with paroxetine.

Cases of serotonin syndrome have been described with simultaneous use with sertraline and fluoxetine.

With simultaneous use, there is a possibility of a decrease in 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.

Storage Conditions

Store at 2°C (36°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.