Tramadol

Tramadol composition

Tramadol – active ingredient – tramadol hydrochloride – 50.0 mg / 100.0 mg excipients: sodium acetate tree hydrate – 4.98 mg / 9.96 mg, water for injection – up to 1 ml / 2 ml.

Description

Clearcolourless or slightly yellowish solution.

Pharmacologic effect

It has an analgesic (opioid) effect. Activates opiate receptors (mu-, delta- and kappa-) on the pre- and postsynaptic membranes of the afferent fibres 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 effect on the cerebral cortex, inhibits the cough and respiratory centers, stimulates the starting area of ​​the vomiting center, the nucleus of the oculomotor nerve; causes spasm of sphincter smooth muscles. 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 litres. Passes through the hematoencephalic and other histohematogenous barriers, including the placental, 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 formation of an active metabolite (M1) depends on the activity of CYP2D6 isoenzyme cytochrome P-540. Excreted mainly by the kidneys (90%) and the intestines (about 10%). The kidneys in unchanged form, 60% – as metabolites and glucuronic conjugates, excrete about 30% of the administered dose of the drug. 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 neoplasms, acute myocardial infarction, injuries, diagnostic and therapeutic procedures; neuralgia

Contraindications

Hypersensitivity, acute alcohol poisoning and intoxication with depriving agents 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. For children older than 1 year, the only indication for the use of tramadol is a pronounced pain syndrome caused by acute or chronic pain.

Pregnancy and lactation period

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.

About Gabriella Lucas