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Profiles of Drug Substances,... 2020Meloxicam, an oxicam derivative: 4-Hydroxy-2-methyl-N-(5-methyl-2-thiazolyl)-2H-1,2- benzothiazine-3-carboxamide 1,1-dioxide, is a nonsteroidal anti-inflammatory drug...
Meloxicam, an oxicam derivative: 4-Hydroxy-2-methyl-N-(5-methyl-2-thiazolyl)-2H-1,2- benzothiazine-3-carboxamide 1,1-dioxide, is a nonsteroidal anti-inflammatory drug (NSAID). It is a selective inhibitor of cyclooxygenase-2 (COX-2). It is used in the management of rheumatoid arthritis, acute exacerbations of osteoarthritis, ankylosing spondylitis and juvenile idiopathic arthritis. It is given in a single oral dose of 7.5mg, increased if necessary to a maximum of 15mg daily (7.5mg in the elderly). It may also be given by rectal suppository in doses similar to those used orally. The reported side effects of meloxicam are similar to those of nonsteroidal anti-inflammatory drugs (NSAIDs), such as abdominal pain, anemia, and edema. There is also an increased risk of serious gastrointestinal (GI) adverse events, including ulceration and bleeding. This profile is prepared to discuss and explain physical characteristics, Proprietary and nonproprietary names of meloxicam. It also includes methods of preparation, thermal and spectral behavior, methods of analysis, pharmacokinetics, metabolism, excretion and pharmacology.
Topics: Aged; Anti-Inflammatory Agents, Non-Steroidal; Arthritis; Humans; Meloxicam; Thiazines; Thiazoles
PubMed: 32164967
DOI: 10.1016/bs.podrm.2019.10.006 -
Journal of the American Association For... May 2022Several analgesics are suggested for pain management in mice. Nonsteroidal antiinflammatories (NSAIDs), such as meloxicam can be administered for the treatment of...
Several analgesics are suggested for pain management in mice. Nonsteroidal antiinflammatories (NSAIDs), such as meloxicam can be administered for the treatment of inflammation and acute pain; however, several side effects can occur which include gastrointestinal ulceration and renal and hepatic toxicity. We previously performed a pilot study to test the antinociceptive activity of meloxicam in mice, but we observed behavioral changes in unoperated control mice. These observations spurred further investigation. One hypothesis for the result was potential differences in formulation between commercial brands of meloxicam. Thus, this current study aimed to evaluate the effects of 3 different commercial brands of meloxicam (20 mg/kg) in the general activity of mice using the open field test. Our results showed that meloxicam had several effects on mouse behavior and caused the formation of skin lesions at the injection site, depending on the brand of the drug. The most significant adverse effect observed was decreased exploratory activity. Grooming frequency was reduced in all groups. These adverse effects might be related to the quality of the drugs because meloxicam formulations can contain crystal polymorphisms that affect drug quality and efficacy. This study points out the importance of drug quality variation that can affect the outcome of behavioral studies in mice.
Topics: Analgesics; Animals; Anti-Inflammatory Agents, Non-Steroidal; Meloxicam; Mice; Open Field Test; Pilot Projects; Thiazines
PubMed: 35101160
DOI: 10.30802/AALAS-JAALAS-21-000046 -
Drugs Jul 2021Prolonged-release (PR; as ascribed in the EU) or extended-release (as ascribed in the USA) bupivacaine/meloxicam (HTX-011; hereafter referred to as bupivacaine/meloxicam... (Review)
Review
Prolonged-release (PR; as ascribed in the EU) or extended-release (as ascribed in the USA) bupivacaine/meloxicam (HTX-011; hereafter referred to as bupivacaine/meloxicam PR; Zynrelef) is a synergistic fixed-dose combination (FDC) of the local anaesthetic bupivacaine and the NSAID meloxicam. It is approved in the EU and the USA to treat postoperative pain. After needle-free application at the surgical site, the novel polymer technology allows simultaneous diffusion of bupivacaine and meloxicam over 72 h. In clinical trials, bupivacaine/meloxicam PR significantly reduced postoperative pain and opioid consumption relative to bupivacaine hydrochloride (HCl) and placebo in patients undergoing bunionectomy, herniorrhaphy or total knee arthroplasty (TKA). When used as the foundation of a scheduled non-opioid multimodal analgesia (MMA) regimen, bupivacaine/meloxicam PR further improved pain control and reduced the need for opioids following surgery. Bupivacaine/meloxicam PR was generally well tolerated, with a lower incidence of opioid-related adverse events than bupivacaine HCl and placebo. Although additional data would be beneficial, current evidence indicates that bupivacaine/meloxicam PR is a promising non-opioid treatment option for the management of postoperative pain.
Topics: Analgesics, Opioid; Anesthetics, Local; Anti-Inflammatory Agents, Non-Steroidal; Bupivacaine; Delayed-Action Preparations; Drug Combinations; Drug Interactions; Humans; Meloxicam; Pain, Postoperative
PubMed: 34228280
DOI: 10.1007/s40265-021-01551-9 -
Zhurnal Nevrologii I Psikhiatrii Imeni... 2022Pain syndromes, acute and chronic, against the background of inflammatory diseases (such as osteoarthritis (OA)), degenerative-dystrophic changes (involutive process,...
Pain syndromes, acute and chronic, against the background of inflammatory diseases (such as osteoarthritis (OA)), degenerative-dystrophic changes (involutive process, trauma) or systemic diseases (rheumatoid arthritis, etc.) dictate a steady increase in the intake of nonsteroidal anti-inflammatory drugs (NSAIDs). The choice of the most «safe NSAID» is based on the assessment of the toxicity index (the ratio when blocking cyclooxygenase (COX)) and the development of relative risks (the benefit/risk ratio). As well as those adverse events that can be detected with individual sensitivity to a specific NSAIDs, taking into account the anamnesis of previous diseases and intolerance to NSAIDs, existing chronic diseases (gastrointestinal tract, cardiovascular system, type 2 diabetes mellitus), limiting the appointment of NSAIDs. Considering these circumstances, the NSAID meloxicam (Amelotex) can be recommended for the treatment of various genesis pain syndromes. A number of studies have demonstrated the efficacy and safety of meloxicam with different methods of its administration (per oral (p/o), intramuscularly (i/m)) in the treatment of pain syndrome in the lower back, with OA, etc. Recent studies concern intravenous (i/v) meloxicam (30 mg) administration with moderate and severe postoperative pain syndrome. Today, the most commonly pain therapy scheme using meloxicam includes step-by-step administration of injectable and oral forms: meloxicam i/m (1.5 ml) for 3-5 days, followed by a transition to p/o (7.5-15 mg) intake for 14 days, or complex therapy with meloxicam (Amelotex), with muscle relaxant and B vitamins.
Topics: Anti-Inflammatory Agents, Non-Steroidal; Arthritis, Rheumatoid; Diabetes Mellitus, Type 2; Humans; Meloxicam; Osteoarthritis
PubMed: 35175701
DOI: 10.17116/jnevro202212201136 -
The Annals of Pharmacotherapy Jan 2023To review data for bupivacaine/meloxicam extended-release (ER) solution for management of postoperative pain and opioid-sparing effects. (Review)
Review
OBJECTIVE
To review data for bupivacaine/meloxicam extended-release (ER) solution for management of postoperative pain and opioid-sparing effects.
DATA SOURCES
Literature search of PubMed (1946 to August 2021) and ProQuest (1946 to August 2021) was performed using the terms: Zynrelef, HTX-011, and "bupivacaine AND meloxicam." Additional information sources include ClinicalTrials.gov, prescribing information, Heron Therapeutics' Clinical and Economic Evidence Dossier, meeting abstracts, and references of identified articles.
STUDY SELECTION AND DATA EXTRACTION
Clinical trials and articles evaluating bupivacaine/meloxicam ER for postoperative pain management.
DATA SYNTHESIS
Bupivacaine is a short-acting local anesthetic. Its efficacy is negatively impacted by the acidic environment of surgical sites. Meloxicam, a nonsteroidal antiinflammatory, reduces inflammation at the surgical site and increases pH propagating bupivacaine movement into the neurons. In Phase 2 and Phase 3 clinical trials, bupivacaine/meloxicam ER was compared with bupivacaine HCl, bupivacaine ER, and meloxicam ER with and without scheduled nonopioid multimodal analgesia (MMA) in bunionectomies, herniorrhaphies, total knee arthroplasty and abdominoplasty. Postoperative pain was well controlled for 72 hours and consistently superior to placebo, with minimal or no opioid use. Wound healing was not impacted and adverse effects were similar to placebo (most commonly nausea, dizziness, constipation, and headaches).
RELEVANCE TO PATIENT CARE AND CLINICAL PRACTICE
Bupivacaine/meloxicam ER is a viable, safe, nonopioid local anesthetic for sustained 72-hour postoperative pain management mitigating opioid consumption.
CONCLUSION
Bupivacaine/meloxicam ER is the only dual-acting, extended-release local anesthetic available. It provides effective analgesia in the postoperative setting and successfully reduces or eliminates postoperative opioid consumption.
Topics: Humans; Anesthetics, Local; Analgesics, Opioid; Meloxicam; Bupivacaine; Pain, Postoperative
PubMed: 35536151
DOI: 10.1177/10600280221086639 -
American Journal of Health-system... Oct 2021
Topics: Anesthetics, Local; Anti-Inflammatory Agents, Non-Steroidal; Bupivacaine; Humans; Meloxicam; Pain, Postoperative
PubMed: 34398228
DOI: 10.1093/ajhp/zxab304 -
The Medical Letter on Drugs and... Sep 2019
Review
Topics: Administration, Oral; Anti-Inflammatory Agents, Non-Steroidal; Arthritis; Humans; Meloxicam; Solubility; Tablets
PubMed: 31599868
DOI: No ID Found -
PloS One 2020In veterinary medicine, the administration of nonsteroidal anti-inflammatory analgesics (NSAIDs) for the control of postsurgical pain in dogs and cats is common given... (Comparative Study)
Comparative Study
Clinical evaluation of postoperative analgesia, cardiorespiratory parameters and changes in liver and renal function tests of paracetamol compared to meloxicam and carprofen in dogs undergoing ovariohysterectomy.
BACKGROUND
In veterinary medicine, the administration of nonsteroidal anti-inflammatory analgesics (NSAIDs) for the control of postsurgical pain in dogs and cats is common given the anti-inflammatory, analgesic, and antipyretic effects of these drugs. This study compared the serum biochemical changes and postoperative analgesic effects of paracetamol, meloxicam, and carprofen in bitches submitted to an ovariohysterectomy using the Dynamic Interactive Visual Analog Scale (DIVAS) and Pain Scale of the University of Melbourne (UMPS) scoring systems.
METHODS
Thirty bitches of different breeds underwent elective ovariohysterectomies and were randomly assigned to one of three treatment groups: a paracetamol group [15 mg kg-1 intravenous (IV)], a carprofen group (4 mg kg-1 IV), and a meloxicam group (0.2 mg kg-1 IV). All treatments were administered 30 minutes prior to surgery. Paracetamol was administered every 8 hours postoperatively for 48 hours total, while carprofen and meloxicam were intravenously administered every 24 hours. An evaluation of post-surgical pain was done with the DIVAS and the UMPS. The first post-surgical pain measurement was performed 1 hour after surgery and then 2, 4, 6, 8, 12, 16, 20, 24, 36, and 48 hours after surgery.
RESULTS
All groups exhibited a gradual reduction in pain throughout the postoperative period in both scales; however, neither scale significantly differed between the three treatment groups (P > 0.05) during the 48 postoperative hours.
CONCLUSIONS
Paracetamol was as effective as meloxicam and carprofen for post-surgical analgesia in bitches subjected to elective ovariohysterectomy. The present study demonstrates that paracetamol may be considered a tool for the effective treatment of acute perioperative pain in dogs. Furthermore, this drug led to no adverse reactions or changes in the parameters assessed in the present study, indicating its safety.
Topics: Acetaminophen; Analgesia; Animals; Anti-Inflammatory Agents, Non-Steroidal; Carbazoles; Cardiorespiratory Fitness; Dogs; Female; Hysterectomy; Kidney Function Tests; Liver Function Tests; Meloxicam; Ovariectomy; Pain, Postoperative
PubMed: 32059002
DOI: 10.1371/journal.pone.0223697 -
British Journal of Clinical Pharmacology Nov 2023
Topics: Humans; Meloxicam; Anti-Inflammatory Agents, Non-Steroidal; Thiazoles; Capillaries; Thiazines
PubMed: 37653568
DOI: 10.1111/bcp.15892 -
The Veterinary Record Jan 2020
Review
Topics: Animals; Carbazoles; Dog Diseases; Dogs; Meloxicam; Osteoarthritis; Randomized Controlled Trials as Topic; Treatment Outcome
PubMed: 31974182
DOI: 10.1136/vr.m50