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Tramadol: the most consumed opioid

Tramadol is an opioid indicated as an analgesic for the treatment of moderate to severe pain. Today, it is the most consumed opioid drug in our country.

Tramadol is a centrally acting analgesic. It belongs to the family of opioid drugs and acts on the central nervous system. However, its behavior is atypical compared to other opioids. It is also marketed as Adolonta, Gelotradol, Dolpar or Zytram, among other brands. The active ingredient is called tramadol hydrochloride and is an analogue of codeine.

Often used in combination with paracetamol for the treatment of chronic pain. They are used in combination because they have been shown to be more effective together than separately. This is also because the dose of both is reduced and, with it, the risk of side effects.

What is it for?

Tramadol is indicated for the treatment of moderate to severe pain. in adults and adolescents from 12 years of age. The potency of tramadol is considered to be one-tenth to one-sixth that of morphine.

According to the world health organization -WHO-, Tramadol is on step II of the pain ladder. That is, in the moderate pain range. In it, weak opioids are classified as analgesics.

The absence of important gastrointestinal and cardiovascular effects is a fact worth highlighting. For this reason, tramadol is a alternative for patients who do not tolerate non-steroidal anti-inflammatory analgesics -AINES-.

Tramadol is also used in combination with paracetamol for the treatment of chronic pain. It is a therapeutic option that improves patient comfort and adherence.

Opioid consumption data

The Spanish medicines agency -AEMPS- has published the report on opioid consumption in the period 2010-2017. These statistics show that Opioid consumption has almost doubled in recent years. The defined daily dose has gone from 9.9 to 17.7.

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The group of opioids most commonly consumed is opioids combined with other pain relievers. The most consumed active ingredient is the combination of tramadol and paracetamol (34.89%). And the second, tramadol alone (22.53%).

These data are, without a doubt, an alarm signal. Opioid use should not be the first line of analgesic treatment. They are indicated only in moderate to severe pain that has not responded to other treatments.

The use of tramadol in chronic non-cancer pain in very high doses and for a long time is a questioned issue. We must not forget that it is an opiate that has addictive potential.

Tramadol mechanism of action

Tramadol is composed of two enantiomers. Each of them acts through a different mechanism of action. And this is what makes it an atypical opioid:

He (+) isomer It presents preferential activity by the μ-opioid receptor. (-) isomer It acts by inhibiting the reuptake of norepinephrine and serotonin. Thus, it enhances the opioid analgesic effect of the (+) isomer.

Tramadol is a pure opioid receptor agonist.. It is not selective, but has greater affinity for μ-type opioid receptors. The inhibition of neuronal reuptake of norepinephrine and serotonin also contributes, on the other hand, to its analgesic effect.

Tramadol It has an active metabolite: O-desmethyltramadol. Various studies show that the potency of this metabolite is several times greater than the original tramadol. Its analgesic activity is, therefore, critical for the analgesia of tramadol.

Tramadol also has an antitussive effect, like codeine.

Side effects

The most common adverse reactions in treatment with tramadol are nausea and dizziness.. Other side effects that may also occur are:

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Headache.Drowsiness.Fatigue.Hyperhidrosis -increased sweating.

Due to its serotonergic effect, It is important not to combine it with other drugs that also act on serotonin. For example, some antidepressants such as SSRIs or amphetamine-type drugs.

It must also be taken into account that Tramadol lowers seizure threshold. Generally, it is not recommended in epileptic patients. Nor in combination with other medications that similarly reduce this threshold.

Tramadol has a much lower potential than other opioids to induce respiratory depression. However, it is an adverse effect that can occur. In fact, it is an important point to consider when using tramadol as an anesthetic.

Especially in long-term treatment, Tolerance and psychological and physical dependence can develop. It is advisable to take this into account and not use it without control. In the case of discontinuing treatment, it should be done gradually. Finally, it is important to keep in mind that the dose must be adjusted to the intensity of the pain and the individual sensitivity of each patient. The lowest effective dose should always be used.

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All cited sources were reviewed in depth by our team to ensure their quality, reliability, validity and validity. The bibliography in this article was considered reliable and of academic or scientific accuracy.

Spanish Agency for Medicines and Health Products (2018). Data sheet. Adolonta. Available at: https://cima.aemps.es/cima/dochtml/ft/59088/FT_59088.htmlTornero-Tornero, C., Galván, J., García, I., Boyer, M., & Orduña-Valls, J.. (2017). Paxiflas(r): new orodispersible combination of tramadol/paracetamol for the treatment of moderate to severe pain. Journal of the Spanish Pain Society, 24(2), 59-67. Bravo, L., Mico, JA, & Berrocoso, E. (2017). Discovery and development of tramadol for the treatment of pain. Expert opinion on drug discovery, 12(12), 1281-1291.

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