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Tramadol was first synthesized in 1962 and introduced to the market in 1977. Traditionally, it has been classified as a centrally acting opioid, although more recent literature refers to it as an “atypical opioid.” Its pharmacological activity is mainly explained by μ-opioid receptor (MOR) agonism combined with inhibition of serotonin and noradrenaline reuptake, leading to increased monoamine concentrations in the central nervous system. However, as Minami et al. have pointed out, these mechanisms alone are not sufficient to fully account for its clinical effects.
Pharmacologically, tramadol is a racemic mixture composed of two enantiomers, (+) and (−), each exerting distinct effects. After hepatic metabolism via cytochrome P450 2D6, tramadol is converted into two major metabolites, M1 and M2. Because O-demethylation is the predominant pathway, higher plasma levels of (−)M1 and (+) tramadol are expected. It should be emphasized that this metabolic activation occurs only after absorption and is dependent on hepatic function. Table 1 summarizes the specific roles of each enantiomer and its metabolites.
From a peripheral perspective, the pharmacokinetics of subcutaneous tramadol remain poorly characterized, with only limited preclinical and clinical data available on its peripheral effects and underlying mechanisms.
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Current approaches to pain management rely largely on systemic administration—oral, transdermal, parenteral, intranasal, or rectal. By their nature, systemic routes expose the entire body to the active drug, which increases the likelihood of adverse effects occurring in tissues unrelated to the pain source. For this reason, the development and use of peripheral or locally acting analgesics is regarded as a promising alternative.
The direct administration of analgesics at the site of pain allows for higher local drug concentrations while reducing systemic exposure, thereby minimizing adverse effects. For patients receiving multiple pharmacological treatments, this approach also helps to avoid potential drug interactions. In cases where tolerance or dependence may develop, local application can be particularly advantageous.
Basic research has identified several peripheral mechanisms of tramadol online. These include weak agonism at μ-opioid receptors, activation of adrenergic receptors, inhibition of transient receptor potential vanilloid 1 (TRPV1) activation, blockade of N-methyl-D-aspartate (NMDA) receptors, facilitation of voltage-dependent potassium channel opening, modulation of the nitric oxide pathway, and direct sodium channel blockade. Experimental studies in animal nociception models confirm tramadol’s efficacy in controlling peripheral pain.
Why is local administration of tramadol considered a promising alternative compared to systemic use?
Clinical research in humans has also demonstrated the utility of tramadol as an anesthetic adjuvant. It has been shown effective in brachial plexus blocks, tendon repair surgery, and as a subcutaneous alternative to conventional local anesthetics.
Dentistry represents a promising field where “old tramadol” has found novel applications, particularly in oral surgery and endodontics. In third molar surgery, tramadol has demonstrated clear benefits. For example, combined oral administration and local infiltration have been shown to prolong anesthetic duration and improve postoperative analgesia in the first six hours after surgery. Other studies, such as those evaluating the combination of submucosal tramadol with oral ketorolac, report enhanced pre-emptive analgesia, reduced pain intensity, and decreased postoperative analgesic requirements.
Another promising approach in dentistry is the use of tramadol in combination with local anesthetic solutions to enhance both efficacy and duration of anesthesia. Isiordia et al. investigated the association of tramadol with mepivacaine in healthy volunteers undergoing inferior alveolar nerve blockade. Their findings demonstrated stronger anesthetic effects during the first two hours and prolonged soft tissue anesthesia.
A similar design was applied to study tramadol combined with articaine in patients requiring impacted third molar extraction. In this case, the tramadol–articaine mixture produced a longer anesthetic duration compared with articaine alone. More recently, researchers tested tramadol with mepivacaine for inferior alveolar nerve blockade in patients experiencing acute pain from symptomatic irreversible pulpitis. While the combination did not improve the overall success rate of the blockade, it did extend the anesthetic duration.
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Taken together, these results raise the question of whether local buying tramadol could become a routine option in dental procedures. Current evidence suggests a favorable profile, with no significant adverse effects reported; however, further research is necessary to clarify the mechanisms of action, optimal dosing, and clinical applicability in different scenarios. Insights from patients in real pain conditions will be particularly valuable. It is possible that this “old drug” may once again prove to be revolutionary — truly an example of old drugs, new uses.