Universal reference book for medicines

Active substance: tramadol

Type: Opioid analgesic with mixed mechanism of action

Description of the active substance:
This information is a reference and it is not enough that the drug has been prescribed by a doctor ..

Opioid analgesic, a cyclohexanol derivative.
A non-selective agonist of? -,? - and? -receptors in the central nervous system. It is a racemate of (+) and (-) isomers (50% each), which are involved in various ways in the analgesic effect. The isomer (+) is a pure agonist of opioid receptors, has low tropism and does not have a pronounced selectivity for various receptor subtypes. The isomer (-), suppressing the neuronal capture of norepinephrine, activates the descending noradrenergic influences. Due to this, transmission of pain impulses to the gelatinous substance of the spinal cord is disrupted.
Causes sedation.
In therapeutic doses, breathing is almost not depressed. Has antitussive effect.
After oral administration, it is quickly and almost completely absorbed from the digestive tract (about 90%).
C max in plasma is achieved 2 hours after ingestion.Bioavailability in a single admission is 68% and increases with repeated use.
Binding to plasma proteins - 20%.
Tramadol is widely distributed in tissues. V d after intake and in / in the introduction of 306 liters and 203 liters, respectively.Penetrates through the placental barrier in a concentration equal to the concentration of the active substance in the plasma. 0.1% excreted in breast milk.
Metabolized by demethylation and conjugation up to 11 metabolites, of which only 1 is active.

It is excreted by the kidneys - 90% and through the intestine - 10%.

Moderate and strong pain syndrome of various genesis (including with malignant tumors, acute myocardial infarction, neuralgia, trauma).
Conducting painful diagnostic or therapeutic procedures.
Adults and children over 14 years of age receive a single dose when administered orally - 50 mg, rectally - 100 mg, iv / slow or / m - 50-100 mg.
If the effectiveness of parenteral administration is insufficient, then in 20-30 minutes, oral administration in a dose of 50 mg is possible.
Children aged 1 to 14 years of age are given a dose of 1-2 mg / kg.

The duration of treatment is determined individually.

The maximum dose: adults and children over 14 years regardless of the mode of administration - 400 mg / day.

From the side of the central nervous system: dizziness, weakness, drowsiness, confusion;
in some cases - seizures of cerebral cramps (with iv introduction in high doses or with the simultaneous appointment of neuroleptics).
From the cardiovascular system: tachycardia, orthostatic hypotension, collapse.

On the part of the digestive system: dry mouth, nausea, vomiting.

From the side of metabolism: increased sweating.

From the musculoskeletal system: miosis.

Acute intoxication with alcohol and drugs that have a depressing effect on the central nervous system, children under 1 year of age, increased sensitivity to tramadol.

In pregnancy, long-term use of tramadol should be avoided because of 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 released in small amounts with breast milk.

Caution should be used in patients with impaired renal function.

Caution should be used in patients with impaired liver function.

Contraindicated in children under 1 year.
Children aged 1 to 14 years of age are given a dose of 1-2 mg / kg.
Tramadol in the form of long-acting dosage forms should not be used in children under 14 years of age.

With caution should be used for convulsions of central genesis, drug dependence, confused consciousness, in patients with impaired renal and hepatic function, as well as with increased sensitivity to other opioid receptor agonists.

Tramadol should not be used for longer than the term justified from a therapeutic point of view.
In the case of long-term treatment, the possibility of developing drug dependence can not be ruled out.
It is not recommended to use for the treatment of withdrawal syndrome.

It is necessary to avoid combination with MAO inhibitors.

During the treatment period, do not drink alcohol.

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

Impact on the ability to drive vehicles and manage mechanisms

During the period of application of tramadol it is not recommended to engage in activities requiring high attention, high speed of psychomotor reactions.

With simultaneous use with drugs that exert a depressing effect on the central nervous system, it is possible to increase the inhibitory effect on the central nervous system with ethanol.

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

When used simultaneously with serotonin reuptake inhibitors, tricyclic antidepressants, antipsychotics, other drugs that reduce the threshold of convulsive readiness, the risk of seizures increases.

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

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

With simultaneous use with paroxetine, there are cases of the development of serotonin syndrome, seizures.

At simultaneous application with sertralinom, fluoxetine cases of development of a serotonin syndrome are described.

With simultaneous application, there is a likelihood of reducing the analgesic effect of opioid analgesics.
Long-term use of opioid analgesics or barbiturates stimulates the development of cross tolerance.
Naloxone activates breathing, eliminating analgesia after the use of opioid analgesics.

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