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Drugs Affecting the Musculoskeletal System
Published in Radhwan Nidal Al-Zidan, Drugs in Pregnancy, 2020
Risk Summary: It is better to be avoided during the 1st and 3rd Trimesters because the pregnancy experience in humans suggests a risk of pulmonary hypertension of the newborn, SABs, and congenital malformations linked to the use of Tolmetin.
Pharmacokinetic-Pharmacodynamic Correlations of Analgesics
Published in Hartmut Derendorf, Günther Hochhaus, Handbook of Pharmacokinetic/Pharmacodynamic Correlation, 2019
Although synovial cyclooxygenase remains suppressed for at least 24 h after a dose of tolmetin, no clear relationship between synovial fluid PGE and tolmetin concentrations could be established.167 This was explained on the basis that the observed concentrations of tolmetin were much higher than those needed to completely inhibit cyclooxygenase and perhaps the drug should be administered less frequently.
Muscular dystrophy and arthritis
Published in Michael Horvat, Ronald V. Croce, Caterina Pesce, Ashley Fallaize, Developmental and Adapted Physical Education, 2019
Michael Horvat, Ronald V. Croce, Caterina Pesce, Ashley Fallaize
Nonsteroidal anti-inflammatory drugs (NSAIDs) have become the preferred initial therapy in treating JRA. Within the NSAID family of medications, ibuprofen, naproxen (Naprosyn), and tolmetin sodium (Tolectin) have been approved for use in children 12 and under by the Food and Drug Administration (FDA). Six to 8 weeks often are required to fully determine NSAID efficacy, and laboratory tests should be administered to determine possible medication toxicity. Possible side effects of NSAID ingestion include stomach pain, nausea and vomiting, anemia, headache, blood in the urine, severe abdominal pain and peptic ulcer, fragility and scarring of the skin (especially with Naprosyn), and difficulty concentrating in school (Arthritis Foundation, 2017).
Tolmetin sodium-loaded thermosensitive mucoadhesive liquid suppositories for rectal delivery; strategy to overcome oral delivery drawbacks
Published in Drug Development and Industrial Pharmacy, 2019
Mohamed A. Akl, Hatem R. Ismael, Fathy I. Abd Allah, Alla A. Kassem, Ahmed M. Samy
Tolmetin sodium (TS) is a pyrrole-acetic acid derivative belonging to the class of NSAIDs. It acts by inhibition of cyclooxygenase enzymes that produce prostaglandins such as PGF and PGE2 [1]. It exhibited potent anti-inflammatory, analgesic, and antipyretic activity more than of aspirin and has been widely used for treatment of chronic rheumatoid arthritis, osteoarthritis and ankylozing spondylitis for the relief of mild to moderate pain. In clinical contexts, TS is administered orally in a dose equal to 600–1800 mg/daily in two, three or four divided doses depending on patient response and the severity of the disease. TS is rapidly and almost completely absorbed within 30–60 min after an oral therapeutic dose. It undergoes aggressive hepatic first-pass metabolism after oral administration [2]. A rectal dosage form of TS is not out in the market, although it is of particular interest when oral administration is impossible.
The influence of physicochemical properties on the reactivity and stability of acyl glucuronides†
Published in Xenobiotica, 2018
Patrick Camilleri, Akshay Buch, Brandi Soldo, Andrew J. Hutt
The development and marketing of both zenarestat and zomepirac were terminated due to serious concerns about hepatotoxicity and hypersensitivity reactions including bronchospasm and anaphylactic shock toxicity shown by the two drugs. The short half-lives of their acyl glucuronide metabolites (8) and (9), a good indication of their high reactivity, and has been considered to play a major role in their hepatotoxicity. In contrast to these outcomes, although tolmetin acyl glucuronide (2) is even more reactive as illustrated by a shorter half-life than those of (8) and (9), the occurrence of liver damage due to tolmetin at recommended dosages has not been reported. Thus, although the short half-life of an acyl glucuronide may give an indication of reactivity and possible toxicity, other factors, including dose, may also contribute to their observed toxicity.
Pharmaceuticals agents for preventing NSAID-induced gastric ulcers: a patent review
Published in Expert Review of Clinical Pharmacology, 2021
Daiane Franco Teixeira, Anamaria Mendonça Santos, Ana Maria Santos Oliveira, José Adão Carvalho Nascimento Júnior, Luiza Abrahão Frank, Marilia Trindade De Santana Souza, Enilton Aparecido Camargo, Mairim Russo Serafini
Tolmetin, for example, is an NSAID used to treat pain in rheumatoid arthritis or juvenile rheumatoid arthritis. The drug’s commercial name is Tolectin®, and it is available in a capsule or tablet form. This medication showed anti-inflammatory, antipyretic, and analgesic activity in animals and produced less gastrointestinal damage when compared to controls such as indomethacin and aspirin [50,51]. Monocordil (isosorbide dinitrate), a well-known vasodilator, was used as a nitric oxide donor and presented a cytoprotective effect on the gastric mucosal defensive mechanisms, thus reducing local inflammation and the formation of gastric lesions [52].