Tramadol: Characteristics And Side Effects Of This Pain Reliever
Many people suffer pain in their daily lives, whether due to an illness, a psychogenic cause, poor posture, or other types of causes. When the pain is intense and does not subside with other types of drugs, tramadol, an opioid-type analgesic drug, is usually indicated (it should always be prescribed by a doctor).
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 is an opioid analgesic drug that is widely prescribed in Primary Care and Pain Units, especially when ibuprofen, paracetamol, nolotil or other pain medications are insufficient.
This drug has multiple trade names, since it has more than 70 different presentations. Some of these names are: Tioner (Gebro Farma), Ceparidin (Arafarma), Adolonta (Grünenthal), Zytram (Mundipharma), Gelpar, Dolotradol (Ferrer), Tradonal (Meda Pharma)…
For its part, let us remember that opioids are a group of analgesic medications (this means that they relieve pain), which act by interacting with the opioid receptors of the cells.
Thus, tramadol relieves pain, exerting an effect of reducing its perception ; It does so through its action on the nerve cells of the brain and spinal cord. Its action occurs on the speed of transmission of the painful signal, as well as its intensity, which results in a lower perception of pain in the patient.
Its effects last between 6 and 8 hours (depending on its concentration and release speed). If we compare it with another opioid, such as morphine, the behavior of tramadol is quite atypical.
Composition and format of this drug
The active ingredient of any drug is that essential substance of said drug, necessary for it to produce its therapeutic effects. That is, it allows it to exert its pharmacological action for which it has been designed. In the case of tramadol, its active ingredient is tramadol hydrochloride.
On the other hand, tramadol has different formats: in capsules, injectable, drops, effervescent tablets. and their concentrations also vary; 50, 100, 150, 200 mg…
Generally, when its concentration is high, its release is prolonged (also called delay); This means that its effect lasts longer over time. Extended-release tramadol is especially indicated to control a type of intense, continuous and persistent pain.
This format is usually taken every 12 hours (always under medical supervision), until the pain decreases.
Properties and characteristics as an analgesic
We are going to learn about the most notable properties of tramadol, clarifying at all times pharmacology concepts that may raise doubts.
First of all, how does tramadol work once ingested? If administered orally (in tablet or pill format) its absorption exceeds 40% of the dose. This occurs even if other medications are taken at the same time. On the other hand, the bioavailability of tramadol is 20%. Let us remember that the bioavailability of a drug refers to the percentage of the administered dose that reaches the bloodstream
On the other hand, as a notable characteristic of tramadol, it has a great muscle affinity, which means that it binds up to 20% to plasma proteins. Its concentration in plasma is maximum when the drug has been administered 3 hours ago.
On the other hand, its useful life ranges between 6 and 8 hours (The useful life of a drug is the time that said drug maintains its potency at 90% or more, without its chemical and physical properties being modified).
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 thanks to two isoenzymes (a type of enzyme), which are: CYP3A4 and CYP2D6.
Regarding its elimination, both tramadol and its metabolites are eliminated practically in their entirety (up to 90%) through the kidneys (kidneys).
Pharmacodynamics
How does tramadol act in our body? What is your mecanism of action? It is a non-selective pure agonist substance that 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 it also has others, which explain its analgesic effect, and which are inhibiting norepinephrine reuptake and enhancing serotonin release
These two neurotransmitters (norepinephrine (NA) and serotonin (SA)) are closely related to mood (specifically, their deficit is related to depressive states).
Indications
What is tramadol indicated for? Mainly, for the treatment of pain, when it has a moderate to severe intensity.
Sometimes it is also used to treat low back pain Low back pain involves pain that is located in the lower back; Its origin is generally related to alterations in the musculoskeletal structure of the spine.
It is worth mentioning, in this section, that tramadol does not have anti-inflammatory effects, as other drugs, such as ibuprofen, would have, for example. This means that it does not prevent or reduce tissue inflammation, so it should not be used for this purpose.
Contraindications
Tramadol, like any other drug, has a series of contraindications; this means that People with any of these characteristics should not take tramadol in almost any case:
Lactation
In women, if they are breastfeeding, it is known that approximately 0.1% of the dose of tramadol is secreted into the milk, so It is recommended not to administer tramadol during this period
If a single dose is administered, it is not necessary to stop breastfeeding (although you should always consult your doctor). On the other hand, if it is administered repeatedly and/or for several days (more than 2/3 days), breastfeeding should be stopped.
Side effects
Like any drug, tramadol also has side effects. The most frequent, in this case, are: vomiting, dizziness, nausea, drowsiness, dry mouth, headache, sweating, constipation, fatigue and confusion
Hollingshead, J., Dühmke, RM & Cornblath, D.R. (2006). Tramadol for neuropathic pain. Scott, L.J. & Perry, C.M. (2000). Tramadol. Drugs, 60: 139–176. Stahl, S. M. (2002). Essential psychopharmacology. Neuroscientific bases and clinical applications. Barcelona: Ariel. Vademecum. (2018). Tramadol.
