Tramadol: An Opioid Drug In Common Use
Tramadol, an opioid drug, is a centrally acting painkiller that belongs to the family of opioid drugs. It acts on your central nervous system. However, it doesn’t act in the same way as other opioids. It’s marketed as Adolonta, Gelotradol, Dolpar, and Zytram, among other brand names. Its active substance is tramadol hydrochloride. Chemically, it’s similar to codeine.
You might use tramadol combined with paracetamol if you have chronic pain. You use them together because they’re more effective when you combine them rather than taking them separately. This also means you’re taking less of each drug. Therefore, you’re less likely to suffer side effects.
What’s the opioid drug tramadol used for?
Tramadol treats moderate to severe pain in adults and adolescents from the age of twelve. Its potency is considered to be between one-sixth and one-tenth that of morphine.
The World Health Organization (WHO) states that tramadol is on the second rung of the pain ladder. In other words, it’s used for moderate pain. On this particular scale, weak opioids are classed as analgesics.
Tramadol causes fewer gastrointestinal and cardiovascular side effects. Therefore, you can take it if you can’t tolerate nonsteroidal anti-inflammatory drugs (NSAIDs).
You can use it in combination with paracetamol to treat chronic pain. With this option, your levels of pain will improve. Furthermore, it has good results in terms of patient adherence. This means you’re more likely to stick with it.
Data on opioid use
The Spanish Medicines Agency (AEMPS) published a report on the use of opioids for the period 2010-2017. The statistics showed that opioid use has almost doubled in recent years. In fact, the daily dosage has increased from 9.9 to 17.7.
The most commonly consumed group of opioids is opioids combined with other painkillers. The most common combination is tramadol and paracetamol (34.89 percent). The second most common is tramadol alone (22.53 percent).
These figures are clearly worrying. You shouldn’t use opioids as the first line in analgesic treatment. In fact, you should only take them for moderate to severe pain that hasn’t responded to previous treatments.
Furthermore, you shouldn’t use tramadol for any chronic non-cancer pain at a high dosage and over a prolonged period. In addition, opioids are addictive.
Mechanism of action of the opioid tramadol
Tramadol is composed of two enantiomers. Each of them acts in a different way. This is what makes it an atypical opioid.
- The isomer (+) has preferential activity by the opioid receptor μ.
- The isomer (-) works by inhibiting the reuptake of norepinephrine and serotonin. Thus, it enhances the analgesic effect of the isomer (+).
Tramadol is a pure opioid receptor agonist. It isn’t selective. However, it has a higher affinity for opioid receptors of type μ. The inhibition of the neuronal reuptake of norepinephrine and serotonin contributes to its analgesic effect.
Tramadol has an active metabolite. This is O-desmethyl tramadol. Several studies show that the potency of this metabolite is several times greater than the original tramadol. Its analgesic activity is, therefore, critical for tramadol’s analgesic effects.
It also has an antitussive effect. Codeine has the same effect.
Side effects of the opioid tramadol
The most common adverse side effects you might suffer are nausea and dizziness. You could also suffer from:
- Hyperhidrosis – increased sweating.
Due to its serotonergic effects, you shouldn’t combine tramadol with other drugs that also act on serotonin. For example, anti-depressants like SSRIs or amphetamine-type drugs.
Tramadol lowers the threshold for the occurrence of seizures. For this reason, you shouldn’t generally use it if you suffer from epilepsy. Nor should you use it in combination with other medications that also lower this threshold.
You’re less likely to suffer respiratory depression with tramadol than with other opioids. However, it’s a side effect that you could still suffer. In fact, you should always consider this factor when using it as an anesthetic.
If you take tramadol long-term, you might become both mentally and physically dependent upon it. Therefore, you should always take this into account. Furthermore, you should never take it in an uncontrolled way. If you discontinue the treatment, you must withdraw from it gradually. Finally, you must adjust your dosage to your individual levels of pain and sensitivity. In fact, you should always take the lowest dose possible.It might interest you...
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- Agencia Española de Medicamentos y Productos sanitarios (2018). Ficha técnica. Adolonta. [Online] Disponible en: https://cima.aemps.es/cima/dochtml/ft/59088/FT_59088.html
- Tornero-Tornero, C., Galván, J., García, I., Boyer, M., & Orduña-Valls, J.. (2017). Paxiflas(r): nueva combinación bucodispersable de tramadol/paracetamol para el tratamiento del dolor moderado a intenso. Revista de la Sociedad Española del Dolor, 24(2), 59-67.
- Bravo, L., Mico, J. A., & Berrocoso, E. (2017). Discovery and development of tramadol for the treatment of pain. Expert opinion on drug discovery, 12(12), 1281-1291.