Tramadol represents the category of synthetic analgesics and is referred to the group of opioids. The medication provides a noteworthy effect on the CNS and spinal cord, causing membrane hyperpolarization and braking pain impulses. It produces a powerful analgesic effect that lasts for a relatively long time (roughly 6 hours). The drug activates the brain’s and gastrointestinal tract opiate receptors, decreasing the decay of catecholamines and stabilizing their concentration in the CNS.
Tramadol, based on the active substance of the same name, is a selective agonist of the mu-opioid receptor; its action aims at inhibiting the reverse neuronal uptake of serotonin and norepinephrine. The analgesic effect of tramadol is clinically up to 10 times less pronounced than that in morphine at the same doses. Considering the dosage options specified in the insert, the drug does not produce significant effects on respiration and hemodynamics, neither it changes the parameters of pulmonary artery pressure, and finally, it has no significant inhibitory effect on intestinal motility. The preparation has proved its sedative and mild antitussive effect in numerous clinical trials; however, in the long-term therapy development of tolerance should be taken into account. The onset of analgesic effect is observed within up to 30 minutes after the reception, it is maintained for approximately 6 hours.
How it works
Tramadol is used in treatment of severe to moderate inflammatory pain sensations, traumatic and vascular etiologies, as well as in conducting diagnostic or therapeutic procedures associated with painful sensations. It may also be assigned in the postoperative period, and in patients with cancer. The use of the drug is not recommended for the elimination of weak pain.
The drug is designed for oral administration, almost 90% of its content is absorbed from the gastrointestinal tract. The maximum concentration in blood is attained within two hours after the intake. The drug binds to the plasma protein at 20%. Tramadol can pass through the placental barrier in similar concentrations as in plasma concentration.
According to Effects on Weight Reduction and Safety of Short-Term Tramadol Administration study conducted by Korean scientists in 2006, the long term treatment (12 weeks therapy, 2 weeks run-in) produced at least 5% weight reduction results in 80% of tramadol control group participants; importantly, more than a half of those participants achieved 10% or more significant weight reduction. However, the medication is not intended for long-term use: the average treatment course ranges from 4 to 6 weeks with the approximate weight loss results of 3.2 – 3.8%.
According to the insert, Tramadol can be administered intravenously, intramuscularly, subcutaneously, orally, and rectally. In oral administration adults and children older than 14 years are typically prescribed a single daily application of one tablet or capsule 0.05g or 20 drops of the solution with a liquid or sugar. Repeated reception is possible after 30-60 minutes, at the same dosage, but no more than 8 times per day. In rectal application 0.1 gram of the drug is used up to 4 times per day. In intravenous, subcutaneous and intramuscular injections: 0.05 – 0.1 g of Tramadol is used (the total dose must not exceed 0.4g daily).
In children older than one year, the drug is suitable only in the form of droplets or parenteral administration at a dosage 1 – 2mg per body of weight, but not exceeding the daily dosage of 8 mg per kg. The elderly and patients with renal insufficiency are prescribed the drug basing on individual characteristics and severity of condition.
Tramadol should not be considered as a method of cancellation syndrome treatment. Taking it with ethanol is not recommended as well. In the event of single application maintaining breastfeeding is allowed. The medication should be used with caution in persons engaged in potentially hazardous work, including driving motor vehicles.