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Tramadol

What is Tramadol?

Tramadol is an opioid  synthetic analgesic, which has effects on the central nervous system and action on the spinal cord (promotes the opening of K+ and Ca2+ channels, causes hyperpolarization of membranes and inhibits the conduction of painful impulses), Tramadol enhances the effect of sedative drugs, activates opiate receptors (μ-, Δ-, κ-) on pre- and postsynaptic membranes of afferent fibers in the nociceptive system of the brain and gastrointestinal tract.

Possible Side Effects

Tramadol slows the destruction of catecholamines, stabilizing their concentration in the central nervous system. Tramadol is a racemic mixture of 2 enantiomers – right-turn (+) and left-turn (-), each of which exhibits a different affinity for the other receptor. (+) Tramadol is a selective mu-opioid receptor agonist and also selectively inhibits neuronal reuptake of serotonin. (-) Tramadol inhibits the neuronal reuptake of norepinephrine. Mono-O-desmethyltramadol (M1 metabolite) also selectively stimulates mu-opiate receptors. The affinity of tramadol for opioid receptors is 10 times lower than that of codeine and 6,000 times lower than that of morphine. The analgesic action of Tramadol is 5-10 times weaker than that of morphine (therefore Tramadol is taken in higher doses).

The analgesic action of Tramadol is caused by a decrease in nociceptive activity and an increase in the body’s antinociceptive system. In therapeutic doses, Tramadol slightly affects hemodynamics and respiration, does not change the pressure in the pulmonary artery, slightly slows intestinal peristalsis, without causing constipation. Tramadol has some sedative effect and surprises cough reflex because Tramadol suppresses the respiratory center, awakens the induction zone of the vomiting center, the nerve nucleus of the oculomotor nerve. With prolonged use, tolerance to Tramadol may develop. Analgesic action develops in 15-30 minutes after ingestion and lasts up to 6 hours.

Pharmacological action

The pharmacological action of Tramadol is analgesic (opioid). Tramadol is dispensed in many forms, from rectal suppositories to oral drip solution, but the two most popular forms are tablets and injectable, solution.

Dosage

Tramadol tablets

Bag in. The tablet should be swallowed without chewing, washed down with a small amount of liquid or dissolved in 1/2 cup of water, regardless of food intake. The drug is used as instructed by a doctor, the dosage regimen is chosen individually depending on the severity of the pain syndrome and the sensitivity of the patient.

In the absence of other prescriptions, the drug should be used in the following doses: adults and adolescents over 14 years (more than 25 kg) – 50 mg, if necessary, after 30-60 minutes, you can take another tablet; in severe pain, a single dose can be 100 mg. Depending on the intensity of the pain syndrome, the analgesic effect is usually maintained for 4-6 hours.

Precaution

A daily dose of Tramadol should not exceed 400 mg.
Higher doses may be used to treat pain in cancer patients and severe pain after surgery.

Special patient categories

The elderly. In elderly patients (over 75 years of age), the interval between administration of Tramadol may increase according to individual characteristics due to the possibility of delayed withdrawal.

Impaired renal and/or hepatic function. In patients with renal and/or hepatic disease, Tramadol may last longer. With Cl-creatinine <30 mL/min and/or patients with hepatic insufficiency,  an interval of 12 hours is required between taking regular doses of Tramadol Generic. Increasing the interval between administration of single doses is possible.

Tramadol should not be used in patients with severely impaired renal function (creatinine Cl <10 ml/min) or impaired hepatic function.
The drug should not be used for a period that is justified from a therapeutic point of view. In case of prolonged use of tramadol, due to the intensity or etiology of the pain syndrome, periodic monitoring is required (if necessary – with breaks in the administration of the drug) to determine the need for additional therapy and dose optimization.

Tramadol injection

Intravenous injection of Tramadol (injected slowly, not more than 1 ml/min, equivalent to 50 mg of tramadol). Water for injection, saline and 5% glucose solution can be used to dilute the drug.
The recommended doses below are indicative. In practice, it is necessary to choose the minimum dose with analgesic effect. Treatment time of the drug is determined individually. It must not be used for longer than the therapeutically justified period.

Adults and adolescents from 14 years: single dose of 50-100 mg, Tramadol can be used again after 4-6 hours. The maximum daily dose of Tramadol is 400 mg.

Children from 1 to 14 years: single dose of 1-2 mg/kg, the maximum daily dose is 8 mg/kg.
Tramadol is extremely popular and is one of the most prescribed analgesics in the world now, although it was invented as far back as 1964.

Frequently asked questions

Last Updated on July 20, 2021 by admin

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