tapentadol and Facial-Pain

Acute orofacial pain is associated with significant disability and has a detrimental impact on quality of life. Although various origins of the pain in trigeminal territory can be identified an odontogenic pathology is the most common cause of acute orofacial pain in patients. Due to complex pathophysiology drugs with multitarget action might provide beneficial effect in pain management. The aim of the present study was to experimentally examine the anti-nociceptive effects of tapentadol, an opioid agonist and a norepinephrine reuptake inhibitor (MOR/NRI), in our animal model of orofacial pain. We tested the effect of tapentadol at gradual doses of 1, 2 and 5 mg/kg during thermal and mechanical stimulation in the trigeminal area of adult rats. We observed that tapentadol exhibits antinociceptive effect at dosages of 2 mg/kg and 5 mg/kg and only in association with mechanical stimulation.

Topics: Analgesics, Opioid; Animals; Disease Models, Animal; Facial Pain; Male; Pilot Projects; Rats; Rats, Wistar; Tapentadol

Tapentadol exhibits a synergistic dual effect effect (MOR / NRI) -agonist effect on noradrena-line reuptake inhibition (NRI). Tapentadol is effective on pain with neuropathic characteristics, therefore we decided to use it in an experimental model of acute orofacial pain.. The Orofacial Stimulation Test, developed by Ugo Basile, measures hypersensitivity to thermal or mechanical stimulation of the trigeminal area. In the experiment, rats had to voluntarily contact a thermal or mechanical stimulator with their unshaved vibrissal pad in order to access a food reward. Twenty adult laboratory rats (average weight 345 grams) were tested. Intraperitoneal tapentadol was used in doses of 1 mg/kg and 2 mg/kg.. The results of the pilot study indicate that intraperitoneal administration of tapentadol (2 mg/kg) increased mechanical anti-nociception in rats.

Topics: Acute Pain; Analgesics, Opioid; Animals; Central Amygdaloid Nucleus; Dose-Response Relationship, Drug; Facial Pain; Naloxone; Pain Measurement; Pilot Projects; Rats; Tapentadol; Yohimbine

Preclinical Research The aim of the present study was to evaluate the antinoceptive interaction between the opioid analgesic, tapentadol, and the NSAID, ketorolac, in the mouse orofacial formalin test. Tapentadol or ketorolac were administered ip 15 min before orofacial formalin injection. The effect of the individual drugs was used to calculate their ED

Topics: Analgesics; Animals; Disease Models, Animal; Drug Synergism; Drug Therapy, Combination; Facial Pain; Formaldehyde; Gene Expression Regulation; Injections, Intraperitoneal; KATP Channels; Ketorolac; Mice; Phenols; Receptors, Opioid; Tapentadol

Combination therapy with two or more analgesics is widely used for conditions associated with moderate to severe pain. Combinations of diverse analgesics with different modes of action can improve the risk-benefit ratio of analgesic treatments. The aim of this study is to evaluate the antinociceptive effect of tapentadol (TAP) and flupirtine (FLP), when administered separately or in combination, as well as their synergistic interaction in the orofacial formalin test in rats. After i.p. injection of TAP at different doses (2, 5, 10 and 15mg/kg), the biphasic nociceptive behavior was reduced in a dose-dependent manner in both phase I and II. Conversely, i.p. injection of FLP at different doses (0.6, 1.6, 3.3, 6.6, 16.6 and 22.2mg/kg) induced a dose-dependent antinociceptive effect in phase II only. TAP was found to be more effective than FLP. The interaction between TAP and FLP was synergistic in phase II with an interaction index (γ) of 0.50±0.24. The data reported in this study indicate that FLP enhances the antinociceptive effect of TAP and this drug combination might be potentially useful in the treatment of chronic pain.

Topics: Aminopyridines; Analgesics; Animals; Dose-Response Relationship, Drug; Drug Synergism; Facial Pain; Formaldehyde; Male; Nociception; Phenols; Rats; Rats, Wistar; Tapentadol

Abstract Since 2008, three new analgesic entities, tapentadol immediate release (Nucynta) diclofenac potassium soft gelatin capsules (Zipsor), and bupivacaine liposome injectable suspension (EXPAREL) were granted US Food and Drug Administration (FDA) approval to treat acute pain. Tapentadol immediate-release is a both a mu-opioid agonist and a norepinephrine reuptake inhibitor, and is indicated for the treatment of moderate to severe pain. Diclofenac potassium soft gelatin capsules are a novel formulation of diclofenac potassium, which is a nonsteroidal anti-inflammatory drug (NSAID), and its putative mechanism of action is through inhibition of cyclooxygenase enzymes. This novel formulation of diclofenac allows for improved absorption at lower doses. Liposomal bupivacaine is a new formulation of bupivacaine intended for single-dose infiltration at the surgical site for postoperative analgesia. Bupivacaine is slowly released from this liposomal vehicle and can provide prolonged analgesia at the surgical site. By utilizing NSAIDs and local anesthetics to decrease the transmission of afferent pain signals, less opioid analgesics are needed to achieve analgesia. Since drug-related adverse events are frequently dose related, lower doses from different drug classes may be employed to reduce the incidence of adverse effects, while producing synergistic analgesia as part of a multimodal analgesic approach to acute pain.

Topics: Analgesics; Animals; Anti-Inflammatory Agents, Non-Steroidal; Bupivacaine; Cyclooxygenase Inhibitors; Diclofenac; Drug Approval; Drug Combinations; Facial Pain; Humans; Phenols; Tapentadol; United States; United States Food and Drug Administration