Many people experience pain in their day-to-day life, whether from illness, psychogenic cause, poor posture, or other causes. When the pain is severe and does not involve another type of medicine, tramadol, an opioid-type pain reliever (usually prescribed by a doctor), is usually indicated.
In this article we will see what are the most relevant properties and characteristics of tramadol, As well as its composition, format, indications, contraindications, mechanism of action and possible adverse effects.
Tramadol: What is it and what is it for?
Tramadol is an opioid-type analgesic widely prescribed in primary care and pain treatment units, especially when ibuprofen, paracetamol, nolotil, or other pain relievers are insufficient.
this medicine he has several trade names, As it has over 70 different presentations. Some of these names are: Tioner (Gebro Farma), Ceparidin (Arafarma), Adolonta (Grünenthal), Zytram (Mundipharma), Gelpar, Dolotradol (Ferrer), Tradonal (Meda Pharma) …
For their part, remember that opioids are a group of analgesic (that is, pain reliever) drugs, which work by interacting with opioid receptors in cells.
Thus, tramadol relieves pain, exerting a diminishing effect on their perception; it does so by its action on the nerve cells of the brain and the spinal cord. Its action occurs on the speed of transmission of the pain signal, as well as on its intensity, which results in a lesser perception of pain in the patient.
Its effects last between 6 and 8 hours (depending on its concentration and rate of release). When compared to another opioid, such as morphine, the behavior of tramadol is quite atypical.
Composition and format of this medication
The active ingredient in any medicine is that essential substance of that medicine, which is necessary for it to produce its therapeutic effects. That is to say, it allows it to exert its pharmacological action for which it was designed. In the case of tramadol, its active ingredient is tramadol hydrochloride.
On the other hand, tramadol has different formats: in capsules, injectables, drops, effervescent tablets … and their concentrations also vary; 50, 100, 150, 200 mg …
Usually, when their concentration is high, their release is prolonged (Also called delay); this means that its effect lasts longer. Prolonged-release tramadol is particularly indicated for controlling a type of intense, continuous and persistent pain.
This format is usually taken every 12 hours (always under medical supervision), until the pain subsides.
Properties and characteristics as an analgesic
We will discover the most remarkable properties of tramadol, clarifying at any time the concepts of pharmacology that may raise doubts.
First of all, how does tramadol work when ingested? If administered orally (in tablet format or in tablet form), its absorption exceeds 40% of the dose. This happens even if other drugs are taken at the same time. In contrast, the bioavailability of tramadol is 20%. Remember that the bioavailability of a drug refers to percentage of the administered dose of the same, which happens until the blood flow.
On the other hand, as a notable feature of tramadol, it has high muscle affinity, which means that it binds to plasma proteins up to 20%. Its plasma concentration is highest when the drug has been administered for 3 hours.
On the other hand, its useful life varies from 6 to 8 hours. (The shelf life of a drug is the time that the drug maintains its potency at 90% or more, without its chemical and physical properties being changed).
As for its half-life, it is approximately 6 hours (the half-life of a drug is the time it takes to lose half of its pharmacological activity).
Metabolism and elimination
At the metabolic level, tramadol is metabolized in the liver. This process occurs through two isoenzymes (a type of enzyme), which are: CYP3A4 and CYP2D6.
As for its elimination, tramadol and its metabolites are eliminated almost completely (up to 90%) by the kidneys (kidneys).
How does tramadol work in our body? What is its mechanism of action? It is a pure, non-selective agonist, which acts on three types of opioid receptors, Which are: μ, δ (delta) and κ (kappa). Its greatest affinity occurs with μ receptors.
This is its main mechanism of action, although there are also others, which explain its analgesic effect, and which are norepinephrine reuptake inhibition and potentiation of serotonin release.
These two neurotransmitters (noradrenaline [NA] and serotonin [SA]) They are closely linked to mood (in particular, their deficit is linked to depressive states).
What is tramadol used for? Primarily for the treatment of pain, when it is of moderate to severe intensity.
It is also sometimes used to treat low back pain. Low back pain involves pain in the lower back; its origin is generally linked to alterations in the musculoskeletal structure of the spine.
It should be mentioned in this section that tramadol has no anti-inflammatory effect, for example if it had other drugs, like ibuprofen. This means that it does not prevent or reduce tissue inflammation, so it should not be used for this purpose.
Tramadol, like any other medicine, has a number of contraindications; That means people with any of these characteristics should not take tramadol in almost all cases:
- People with hypersensitivity.
- People who have been intoxicated (acutely) by alcohol, hypnotics, opioids, psychotropic drugs, pain relievers.
- People being treated with MAO inhibitors (MAOIs, a type of antidepressant).
- People with epilepsy who cannot be controlled with any treatment.
- People being treated for morphine (morphine) withdrawal syndrome.
- People under 12 years old.
- People with renal or hepatic insufficiency (in this case, its use is allowed, although under medical supervision).
In women, when breastfeeding, it is known that about 0.1% of the dose of tramadol is secreted in the milk, so that it is recommended not to administer tramadol during this time.
If you are receiving a single dose of yourself, you should not stop breast-feeding (although you should always consult your doctor). On the other hand, if it is administered repeatedly and / or over several days (more than 2/3 days), breast-feeding should be stopped.
Like all medicines, tramadol also has side effects. The most common, in this case, are: vomiting, dizziness, nausea, drowsiness, dry mouth, headache, sweating, constipation, fatigue and confusion.
Hollingshead, J., Dühmke, RM and Cornblath, DR (2006). Tramadol for neuropathic pain. Scott, LJ and Perry, CM (2000). Tramadol. Drugs, 60: 139-176. Stahl, SM (2002). Essential psychopharmacology. Neuroscientific bases and clinical applications. Barcelona: Ariel. Vade mecum. (2018). Tramadol.