Details
Stereochemistry | ACHIRAL |
Molecular Formula | C15H14NO3.Na |
Molecular Weight | 279.2663 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
[Na+].CN1C(CC([O-])=O)=CC=C1C(=O)C2=CC=C(C)C=C2
InChI
InChIKey=QGUALMNFRILWRA-UHFFFAOYSA-M
InChI=1S/C15H15NO3.Na/c1-10-3-5-11(6-4-10)15(19)13-8-7-12(16(13)2)9-14(17)18;/h3-8H,9H2,1-2H3,(H,17,18);/q;+1/p-1
Tolmetin is a nonsteroidal anti-inflammatory agent. It was marketed as Tolectin in USA. TOLECTIN (tolmetin sodium) is indicated for the relief of signs and symptoms of
rheumatoid arthritis and osteoarthritis. TOLECTIN is indicated in the treatment of
acute flares and the long-term management of the chronic disease.
TOLECTIN is also indicated for treatment of juvenile rheumatoid arthritis. The mode of action of tolmetin is not known. However, studies in laboratory animals and man have demonstrated that the anti-inflammatory action of tolmetin is not due to pituitary-adrenal stimulation. Tolmetin inhibits prostaglandin synthetase in vitro and lowers the plasma level of prostaglandin E in man. This reduction in prostaglandin synthesis may be responsible for the anti-inflammatory action.
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL221 |
0.35 µM [IC50] | ||
Target ID: CHEMBL230 |
0.82 µM [IC50] | ||
Target ID: CHEMBL2094253 |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | Tolmetin sodium Approved UseCarefully consider the potential benefits and risks of tolmetin sodium capsules and other treatment options before deciding to use tolmetin sodium capsules. Use the lowest effective dose for the shortest duration consistent with individual patient treatment goals (see WARNINGS). Tolmetin sodium capsules are indicated for the relief of signs and symptoms of rheumatoid arthritis and osteoarthritis. Tolmetin sodium capsules are indicated in the treatment of acute flares and the long-term management of the chronic disease. Tolmetin sodium capsules are also indicated for treatment of juvenile rheumatoid arthritis. The safety and effectiveness of tolmetin sodium capsules have not been established in pediatric patients under 2 years of age. Launch Date1976 |
|||
Primary | Tolmetin sodium Approved UseCarefully consider the potential benefits and risks of tolmetin sodium capsules and other treatment options before deciding to use tolmetin sodium capsules. Use the lowest effective dose for the shortest duration consistent with individual patient treatment goals (see WARNINGS). Tolmetin sodium capsules are indicated for the relief of signs and symptoms of rheumatoid arthritis and osteoarthritis. Tolmetin sodium capsules are indicated in the treatment of acute flares and the long-term management of the chronic disease. Tolmetin sodium capsules are also indicated for treatment of juvenile rheumatoid arthritis. The safety and effectiveness of tolmetin sodium capsules have not been established in pediatric patients under 2 years of age. Launch Date1976 |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
29.3 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1126116/ |
300 mg single, oral dose: 300 mg route of administration: Oral experiment type: SINGLE co-administered: |
TOLMETIN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
AUC
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
50.5 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1126116/ |
300 mg single, oral dose: 300 mg route of administration: Oral experiment type: SINGLE co-administered: |
TOLMETIN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
T1/2
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
0.83 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1126116/ |
300 mg single, oral dose: 300 mg route of administration: Oral experiment type: SINGLE co-administered: |
TOLMETIN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
Doses
Dose | Population | Adverse events |
---|---|---|
400 mg 3 times / day steady, oral (starting) Dose: 400 mg, 3 times / day Route: oral Route: steady Dose: 400 mg, 3 times / day Sources: |
unhealthy, adults n = 800 Health Status: unhealthy Condition: rheumatoid arthritis and osteoarthritis Age Group: adults Population Size: 800 Sources: |
Other AEs: Nausea, Dyspepsia... Other AEs: Nausea (11%) Sources: Dyspepsia (3-9) Distress gastrointestinal (3-9) Abdominal pain (3-9) Diarrhea (3-9) Flatulence (3-9) Vomiting (3-9) Constipation (1-3) Gastritis (1-3) Peptic ulcer (1-3) Headache (3-9) Asthenia (3-9) Chest pain (1-3) Blood pressure increased (3-9) Edema (3-9) Dizziness (3-9) Drowsiness (3-9) Depression (1-3) Weight gain (3-9) Weight loss (3-9) Skin irritation (1-3) Tinnitus (1-3) Visual disturbance (1-3) Blood urea nitrogen increased (1-3) Urinary tract infection (1-3) Gastrointestinal ulcer bleeding (<1%) Bleeding gastrointestinal (<1%) Perforation (<1%) Glossitis (<1%) Stomatitis (<1%) Hepatitis (<1%) Function liver abnormal (<1%) Anaphylactoid reaction (<1%) Fever (<1%) Lymphadenopathy (<1%) Serum sickness (<1%) Hemolytic anemia (<1%) Thrombocytopenia (<1%) Granulocytopenia (<1%) Agranulocytosis (<1%) Urticaria (<1%) Purpura (<1%) Erythema multiforme (<1%) Toxic epidermal necrolysis (<1%) Hematuria (<1%) Proteinuria (<1%) Dysuria (<1%) Renal failure (<1%) |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
Blood urea nitrogen increased | 1-3 | 400 mg 3 times / day steady, oral (starting) Dose: 400 mg, 3 times / day Route: oral Route: steady Dose: 400 mg, 3 times / day Sources: |
unhealthy, adults n = 800 Health Status: unhealthy Condition: rheumatoid arthritis and osteoarthritis Age Group: adults Population Size: 800 Sources: |
Chest pain | 1-3 | 400 mg 3 times / day steady, oral (starting) Dose: 400 mg, 3 times / day Route: oral Route: steady Dose: 400 mg, 3 times / day Sources: |
unhealthy, adults n = 800 Health Status: unhealthy Condition: rheumatoid arthritis and osteoarthritis Age Group: adults Population Size: 800 Sources: |
Constipation | 1-3 | 400 mg 3 times / day steady, oral (starting) Dose: 400 mg, 3 times / day Route: oral Route: steady Dose: 400 mg, 3 times / day Sources: |
unhealthy, adults n = 800 Health Status: unhealthy Condition: rheumatoid arthritis and osteoarthritis Age Group: adults Population Size: 800 Sources: |
Depression | 1-3 | 400 mg 3 times / day steady, oral (starting) Dose: 400 mg, 3 times / day Route: oral Route: steady Dose: 400 mg, 3 times / day Sources: |
unhealthy, adults n = 800 Health Status: unhealthy Condition: rheumatoid arthritis and osteoarthritis Age Group: adults Population Size: 800 Sources: |
Gastritis | 1-3 | 400 mg 3 times / day steady, oral (starting) Dose: 400 mg, 3 times / day Route: oral Route: steady Dose: 400 mg, 3 times / day Sources: |
unhealthy, adults n = 800 Health Status: unhealthy Condition: rheumatoid arthritis and osteoarthritis Age Group: adults Population Size: 800 Sources: |
Peptic ulcer | 1-3 | 400 mg 3 times / day steady, oral (starting) Dose: 400 mg, 3 times / day Route: oral Route: steady Dose: 400 mg, 3 times / day Sources: |
unhealthy, adults n = 800 Health Status: unhealthy Condition: rheumatoid arthritis and osteoarthritis Age Group: adults Population Size: 800 Sources: |
Skin irritation | 1-3 | 400 mg 3 times / day steady, oral (starting) Dose: 400 mg, 3 times / day Route: oral Route: steady Dose: 400 mg, 3 times / day Sources: |
unhealthy, adults n = 800 Health Status: unhealthy Condition: rheumatoid arthritis and osteoarthritis Age Group: adults Population Size: 800 Sources: |
Tinnitus | 1-3 | 400 mg 3 times / day steady, oral (starting) Dose: 400 mg, 3 times / day Route: oral Route: steady Dose: 400 mg, 3 times / day Sources: |
unhealthy, adults n = 800 Health Status: unhealthy Condition: rheumatoid arthritis and osteoarthritis Age Group: adults Population Size: 800 Sources: |
Urinary tract infection | 1-3 | 400 mg 3 times / day steady, oral (starting) Dose: 400 mg, 3 times / day Route: oral Route: steady Dose: 400 mg, 3 times / day Sources: |
unhealthy, adults n = 800 Health Status: unhealthy Condition: rheumatoid arthritis and osteoarthritis Age Group: adults Population Size: 800 Sources: |
Visual disturbance | 1-3 | 400 mg 3 times / day steady, oral (starting) Dose: 400 mg, 3 times / day Route: oral Route: steady Dose: 400 mg, 3 times / day Sources: |
unhealthy, adults n = 800 Health Status: unhealthy Condition: rheumatoid arthritis and osteoarthritis Age Group: adults Population Size: 800 Sources: |
Nausea | 11% | 400 mg 3 times / day steady, oral (starting) Dose: 400 mg, 3 times / day Route: oral Route: steady Dose: 400 mg, 3 times / day Sources: |
unhealthy, adults n = 800 Health Status: unhealthy Condition: rheumatoid arthritis and osteoarthritis Age Group: adults Population Size: 800 Sources: |
Abdominal pain | 3-9 | 400 mg 3 times / day steady, oral (starting) Dose: 400 mg, 3 times / day Route: oral Route: steady Dose: 400 mg, 3 times / day Sources: |
unhealthy, adults n = 800 Health Status: unhealthy Condition: rheumatoid arthritis and osteoarthritis Age Group: adults Population Size: 800 Sources: |
Asthenia | 3-9 | 400 mg 3 times / day steady, oral (starting) Dose: 400 mg, 3 times / day Route: oral Route: steady Dose: 400 mg, 3 times / day Sources: |
unhealthy, adults n = 800 Health Status: unhealthy Condition: rheumatoid arthritis and osteoarthritis Age Group: adults Population Size: 800 Sources: |
Blood pressure increased | 3-9 | 400 mg 3 times / day steady, oral (starting) Dose: 400 mg, 3 times / day Route: oral Route: steady Dose: 400 mg, 3 times / day Sources: |
unhealthy, adults n = 800 Health Status: unhealthy Condition: rheumatoid arthritis and osteoarthritis Age Group: adults Population Size: 800 Sources: |
Diarrhea | 3-9 | 400 mg 3 times / day steady, oral (starting) Dose: 400 mg, 3 times / day Route: oral Route: steady Dose: 400 mg, 3 times / day Sources: |
unhealthy, adults n = 800 Health Status: unhealthy Condition: rheumatoid arthritis and osteoarthritis Age Group: adults Population Size: 800 Sources: |
Distress gastrointestinal | 3-9 | 400 mg 3 times / day steady, oral (starting) Dose: 400 mg, 3 times / day Route: oral Route: steady Dose: 400 mg, 3 times / day Sources: |
unhealthy, adults n = 800 Health Status: unhealthy Condition: rheumatoid arthritis and osteoarthritis Age Group: adults Population Size: 800 Sources: |
Dizziness | 3-9 | 400 mg 3 times / day steady, oral (starting) Dose: 400 mg, 3 times / day Route: oral Route: steady Dose: 400 mg, 3 times / day Sources: |
unhealthy, adults n = 800 Health Status: unhealthy Condition: rheumatoid arthritis and osteoarthritis Age Group: adults Population Size: 800 Sources: |
Drowsiness | 3-9 | 400 mg 3 times / day steady, oral (starting) Dose: 400 mg, 3 times / day Route: oral Route: steady Dose: 400 mg, 3 times / day Sources: |
unhealthy, adults n = 800 Health Status: unhealthy Condition: rheumatoid arthritis and osteoarthritis Age Group: adults Population Size: 800 Sources: |
Dyspepsia | 3-9 | 400 mg 3 times / day steady, oral (starting) Dose: 400 mg, 3 times / day Route: oral Route: steady Dose: 400 mg, 3 times / day Sources: |
unhealthy, adults n = 800 Health Status: unhealthy Condition: rheumatoid arthritis and osteoarthritis Age Group: adults Population Size: 800 Sources: |
Edema | 3-9 | 400 mg 3 times / day steady, oral (starting) Dose: 400 mg, 3 times / day Route: oral Route: steady Dose: 400 mg, 3 times / day Sources: |
unhealthy, adults n = 800 Health Status: unhealthy Condition: rheumatoid arthritis and osteoarthritis Age Group: adults Population Size: 800 Sources: |
Flatulence | 3-9 | 400 mg 3 times / day steady, oral (starting) Dose: 400 mg, 3 times / day Route: oral Route: steady Dose: 400 mg, 3 times / day Sources: |
unhealthy, adults n = 800 Health Status: unhealthy Condition: rheumatoid arthritis and osteoarthritis Age Group: adults Population Size: 800 Sources: |
Headache | 3-9 | 400 mg 3 times / day steady, oral (starting) Dose: 400 mg, 3 times / day Route: oral Route: steady Dose: 400 mg, 3 times / day Sources: |
unhealthy, adults n = 800 Health Status: unhealthy Condition: rheumatoid arthritis and osteoarthritis Age Group: adults Population Size: 800 Sources: |
Vomiting | 3-9 | 400 mg 3 times / day steady, oral (starting) Dose: 400 mg, 3 times / day Route: oral Route: steady Dose: 400 mg, 3 times / day Sources: |
unhealthy, adults n = 800 Health Status: unhealthy Condition: rheumatoid arthritis and osteoarthritis Age Group: adults Population Size: 800 Sources: |
Weight gain | 3-9 | 400 mg 3 times / day steady, oral (starting) Dose: 400 mg, 3 times / day Route: oral Route: steady Dose: 400 mg, 3 times / day Sources: |
unhealthy, adults n = 800 Health Status: unhealthy Condition: rheumatoid arthritis and osteoarthritis Age Group: adults Population Size: 800 Sources: |
Weight loss | 3-9 | 400 mg 3 times / day steady, oral (starting) Dose: 400 mg, 3 times / day Route: oral Route: steady Dose: 400 mg, 3 times / day Sources: |
unhealthy, adults n = 800 Health Status: unhealthy Condition: rheumatoid arthritis and osteoarthritis Age Group: adults Population Size: 800 Sources: |
Agranulocytosis | <1% | 400 mg 3 times / day steady, oral (starting) Dose: 400 mg, 3 times / day Route: oral Route: steady Dose: 400 mg, 3 times / day Sources: |
unhealthy, adults n = 800 Health Status: unhealthy Condition: rheumatoid arthritis and osteoarthritis Age Group: adults Population Size: 800 Sources: |
Anaphylactoid reaction | <1% | 400 mg 3 times / day steady, oral (starting) Dose: 400 mg, 3 times / day Route: oral Route: steady Dose: 400 mg, 3 times / day Sources: |
unhealthy, adults n = 800 Health Status: unhealthy Condition: rheumatoid arthritis and osteoarthritis Age Group: adults Population Size: 800 Sources: |
Bleeding gastrointestinal | <1% | 400 mg 3 times / day steady, oral (starting) Dose: 400 mg, 3 times / day Route: oral Route: steady Dose: 400 mg, 3 times / day Sources: |
unhealthy, adults n = 800 Health Status: unhealthy Condition: rheumatoid arthritis and osteoarthritis Age Group: adults Population Size: 800 Sources: |
Dysuria | <1% | 400 mg 3 times / day steady, oral (starting) Dose: 400 mg, 3 times / day Route: oral Route: steady Dose: 400 mg, 3 times / day Sources: |
unhealthy, adults n = 800 Health Status: unhealthy Condition: rheumatoid arthritis and osteoarthritis Age Group: adults Population Size: 800 Sources: |
Erythema multiforme | <1% | 400 mg 3 times / day steady, oral (starting) Dose: 400 mg, 3 times / day Route: oral Route: steady Dose: 400 mg, 3 times / day Sources: |
unhealthy, adults n = 800 Health Status: unhealthy Condition: rheumatoid arthritis and osteoarthritis Age Group: adults Population Size: 800 Sources: |
Fever | <1% | 400 mg 3 times / day steady, oral (starting) Dose: 400 mg, 3 times / day Route: oral Route: steady Dose: 400 mg, 3 times / day Sources: |
unhealthy, adults n = 800 Health Status: unhealthy Condition: rheumatoid arthritis and osteoarthritis Age Group: adults Population Size: 800 Sources: |
Function liver abnormal | <1% | 400 mg 3 times / day steady, oral (starting) Dose: 400 mg, 3 times / day Route: oral Route: steady Dose: 400 mg, 3 times / day Sources: |
unhealthy, adults n = 800 Health Status: unhealthy Condition: rheumatoid arthritis and osteoarthritis Age Group: adults Population Size: 800 Sources: |
Gastrointestinal ulcer bleeding | <1% | 400 mg 3 times / day steady, oral (starting) Dose: 400 mg, 3 times / day Route: oral Route: steady Dose: 400 mg, 3 times / day Sources: |
unhealthy, adults n = 800 Health Status: unhealthy Condition: rheumatoid arthritis and osteoarthritis Age Group: adults Population Size: 800 Sources: |
Glossitis | <1% | 400 mg 3 times / day steady, oral (starting) Dose: 400 mg, 3 times / day Route: oral Route: steady Dose: 400 mg, 3 times / day Sources: |
unhealthy, adults n = 800 Health Status: unhealthy Condition: rheumatoid arthritis and osteoarthritis Age Group: adults Population Size: 800 Sources: |
Granulocytopenia | <1% | 400 mg 3 times / day steady, oral (starting) Dose: 400 mg, 3 times / day Route: oral Route: steady Dose: 400 mg, 3 times / day Sources: |
unhealthy, adults n = 800 Health Status: unhealthy Condition: rheumatoid arthritis and osteoarthritis Age Group: adults Population Size: 800 Sources: |
Hematuria | <1% | 400 mg 3 times / day steady, oral (starting) Dose: 400 mg, 3 times / day Route: oral Route: steady Dose: 400 mg, 3 times / day Sources: |
unhealthy, adults n = 800 Health Status: unhealthy Condition: rheumatoid arthritis and osteoarthritis Age Group: adults Population Size: 800 Sources: |
Hemolytic anemia | <1% | 400 mg 3 times / day steady, oral (starting) Dose: 400 mg, 3 times / day Route: oral Route: steady Dose: 400 mg, 3 times / day Sources: |
unhealthy, adults n = 800 Health Status: unhealthy Condition: rheumatoid arthritis and osteoarthritis Age Group: adults Population Size: 800 Sources: |
Hepatitis | <1% | 400 mg 3 times / day steady, oral (starting) Dose: 400 mg, 3 times / day Route: oral Route: steady Dose: 400 mg, 3 times / day Sources: |
unhealthy, adults n = 800 Health Status: unhealthy Condition: rheumatoid arthritis and osteoarthritis Age Group: adults Population Size: 800 Sources: |
Lymphadenopathy | <1% | 400 mg 3 times / day steady, oral (starting) Dose: 400 mg, 3 times / day Route: oral Route: steady Dose: 400 mg, 3 times / day Sources: |
unhealthy, adults n = 800 Health Status: unhealthy Condition: rheumatoid arthritis and osteoarthritis Age Group: adults Population Size: 800 Sources: |
Perforation | <1% | 400 mg 3 times / day steady, oral (starting) Dose: 400 mg, 3 times / day Route: oral Route: steady Dose: 400 mg, 3 times / day Sources: |
unhealthy, adults n = 800 Health Status: unhealthy Condition: rheumatoid arthritis and osteoarthritis Age Group: adults Population Size: 800 Sources: |
Proteinuria | <1% | 400 mg 3 times / day steady, oral (starting) Dose: 400 mg, 3 times / day Route: oral Route: steady Dose: 400 mg, 3 times / day Sources: |
unhealthy, adults n = 800 Health Status: unhealthy Condition: rheumatoid arthritis and osteoarthritis Age Group: adults Population Size: 800 Sources: |
Purpura | <1% | 400 mg 3 times / day steady, oral (starting) Dose: 400 mg, 3 times / day Route: oral Route: steady Dose: 400 mg, 3 times / day Sources: |
unhealthy, adults n = 800 Health Status: unhealthy Condition: rheumatoid arthritis and osteoarthritis Age Group: adults Population Size: 800 Sources: |
Renal failure | <1% | 400 mg 3 times / day steady, oral (starting) Dose: 400 mg, 3 times / day Route: oral Route: steady Dose: 400 mg, 3 times / day Sources: |
unhealthy, adults n = 800 Health Status: unhealthy Condition: rheumatoid arthritis and osteoarthritis Age Group: adults Population Size: 800 Sources: |
Serum sickness | <1% | 400 mg 3 times / day steady, oral (starting) Dose: 400 mg, 3 times / day Route: oral Route: steady Dose: 400 mg, 3 times / day Sources: |
unhealthy, adults n = 800 Health Status: unhealthy Condition: rheumatoid arthritis and osteoarthritis Age Group: adults Population Size: 800 Sources: |
Stomatitis | <1% | 400 mg 3 times / day steady, oral (starting) Dose: 400 mg, 3 times / day Route: oral Route: steady Dose: 400 mg, 3 times / day Sources: |
unhealthy, adults n = 800 Health Status: unhealthy Condition: rheumatoid arthritis and osteoarthritis Age Group: adults Population Size: 800 Sources: |
Thrombocytopenia | <1% | 400 mg 3 times / day steady, oral (starting) Dose: 400 mg, 3 times / day Route: oral Route: steady Dose: 400 mg, 3 times / day Sources: |
unhealthy, adults n = 800 Health Status: unhealthy Condition: rheumatoid arthritis and osteoarthritis Age Group: adults Population Size: 800 Sources: |
Toxic epidermal necrolysis | <1% | 400 mg 3 times / day steady, oral (starting) Dose: 400 mg, 3 times / day Route: oral Route: steady Dose: 400 mg, 3 times / day Sources: |
unhealthy, adults n = 800 Health Status: unhealthy Condition: rheumatoid arthritis and osteoarthritis Age Group: adults Population Size: 800 Sources: |
Urticaria | <1% | 400 mg 3 times / day steady, oral (starting) Dose: 400 mg, 3 times / day Route: oral Route: steady Dose: 400 mg, 3 times / day Sources: |
unhealthy, adults n = 800 Health Status: unhealthy Condition: rheumatoid arthritis and osteoarthritis Age Group: adults Population Size: 800 Sources: |
PubMed
Title | Date | PubMed |
---|---|---|
Immune hemolytic anemia associated with tolmetin and suprofen. | 1989 Sep |
|
Multisystem failure and hepatic microvesicular fatty metamorphosis associated with tolmetin ingestion. | 1991 Aug |
|
Naproxen-induced recurrent aseptic meningitis. | 1991 Nov |
|
I almost crossed over. | 2005 Oct |
|
Non-steroidal anti-inflammatory agents, tolmetin and sulindac, inhibit liver tryptophan 2,3-dioxygenase activity and alter brain neurotransmitter levels. | 2006 Nov 10 |
|
In vivo effects of amtolmetin guacyl on lipid peroxidation and antioxidant defence systems. Comparison with non-selective and COX-2 selective NSAIDs. | 2007 Apr |
|
One center's experience: the serology and drugs associated with drug-induced immune hemolytic anemia--a new paradigm. | 2007 Apr |
|
Determination of non-steroidal anti-inflammatory drugs in urine by combining an immobilized carboxylated carbon nanotubes minicolumn for solid-phase extraction with capillary electrophoresis-mass spectrometry. | 2007 Aug 3 |
|
In vivo effects of amtolmetin guacyl on lipid peroxidation and antioxidant defence systems in different models of gastrointestinal injury. | 2007 Jan |
|
Potential antioxidant activity of celecoxib and amtolmetin guacyl: in vitro studies. | 2007 Jan |
|
Interaction of nonsteroidal anti-inflammatory drugs with multidrug resistance protein (MRP) 2/ABCC2- and MRP4/ABCC4-mediated methotrexate transport. | 2007 Jan |
|
Polyproline-rod approach to isolating protein targets of bioactive small molecules: isolation of a new target of indomethacin. | 2007 Jan 31 |
|
Determination of degradation pathways and kinetics of acyl glucuronides by NMR spectroscopy. | 2007 Jun |
|
A peripatetic pediatrician's journey into pediatric rheumatology: Part II. | 2007 Jun 21 |
|
Non-steroidal anti-inflammatory agents, tolmetin and sulindac attenuate quinolinic acid (QA)-induced oxidative stress in primary hippocampal neurons and reduce QA-induced spatial reference memory deficits in male Wistar rats. | 2007 Mar 20 |
|
Studies on the metabolism of tolmetin to the chemically reactive acyl-coenzyme A thioester intermediate in rats. | 2007 May |
|
Improving adherence to medical regimens for juvenile rheumatoid arthritis. | 2007 May 18 |
|
Idiopathic chondrolysis of the hip: a case report. | 2007 Oct |
|
Singlet oxygen scavenging activity of non-steroidal anti-inflammatory drugs. | 2008 |
|
Role of biotransformation studies in minimizing metabolism-related liabilities in drug discovery. | 2008 |
|
Cyclooxygenase inhibitors affect bone mineralization in rat fetuses. | 2008 |
|
Modulation of dopaminergic neurotransmission in rat striatum upon in vitro and in vivo diclofenac treatment. | 2008 Apr |
|
Ionic liquid-based dynamic liquid-phase microextraction: application to the determination of anti-inflammatory drugs in urine samples. | 2008 Aug 15 |
|
Topical ocular delivery of NSAIDs. | 2008 Jun |
|
The effect of piroxicam on the formation of postoperative, intraabdominal adhesion in rats. | 2008 Oct |
|
A novel high-throughput screening assay for putative antidiabetic agents through PPARalpha interactions. | 2008 Oct |
|
Methotrexate for the treatment of juvenile idiopathic arthritis: process to approval for JIA indication in Japan. | 2009 |
|
Glycerolysis of acyl glucuronides as an artifact of in vitro drug metabolism incubations. | 2009 Aug |
|
Drug-organic electrolyte complexes as controlled release systems. | 2009 Jan |
|
A study of the intermolecular interactions of tolmetin/N-acetyl-L-tyrosine ethyl ester complex. | 2009 Jun |
|
Entrapment of ketorolac tromethamine in polymeric vehicle for controlled drug delivery. | 2009 Nov |
|
Maternal toxicity of nonsteroidal anti-inflammatory drugs as an important factor affecting prenatal development. | 2009 Sep |
|
Sequential injection system for phospholipase A2 activity evaluation: studies on liposomes using an environment-sensitive fluorescent probe. | 2009 Sep 15 |
|
An evaluation of the utility of routine laboratory monitoring of juvenile idiopathic arthritis (JIA) patients using non-steroidal anti-inflammatory drugs (NSAIDs): a retrospective review. | 2010 Apr 14 |
|
Accuracy of rapid urease test in diagnosing Helicobacter pylori infection in patients using NSAIDs. | 2010 Apr-Jun |
|
Friedel-Crafts acylation of pyrroles and indoles using 1,5-diazabicyclo[4.3.0]non-5-ene (DBN) as a nucleophilic catalyst. | 2010 Dec 17 |
|
Selected pharmacokinetic issues of the use of antiepileptic drugs and parenteral nutrition in critically ill patients. | 2010 Dec 31 |
|
Nonsteroidal Anti-Inflammatory Drugs: A survey of practices and concerns of pediatric medical and surgical specialists and a summary of available safety data. | 2010 Feb 4 |
|
Development of theophylline floating microballoons using cellulose acetate butyrate and/or Eudragit RL 100 polymers with different permeability characteristics. | 2010 Jan |
|
Evaluation of Wound Healing Potential of Bauhinia purpurea Leaf Extracts in Rats. | 2010 Jan |
|
Effect of formulation and processing variables on the characteristics of tolmetin microspheres prepared by double emulsion solvent diffusion method. | 2010 Jan |
|
Unusual interleukin-1 and -6 expression in fetal cartilage is associated with placental abnormalities. | 2010 Jan 1 |
|
Control of encapsulation efficiency in polymeric microparticle system of tolmetin. | 2010 Jan-Feb |
|
Determination of actarit from human plasma for bioequivalence studies. | 2010 Nov |
|
Validation and clinical application of an LC-ESI-MS/MS method for simultaneous determination of tolmetin and MED5, the metabolites of amtolmetin guacil in human plasma. | 2010 Oct |
|
Diclofenac hypersensitivity: antibody responses to the parent drug and relevant metabolites. | 2010 Oct 28 |
|
Effect of ketorolac and diclofenac on the impairment of endothelium-dependent relaxation induced by reactive oxygen species in rabbit abdominal aorta. | 2010 Sep |
|
Identification of old drugs as potential inhibitors of HIV-1 integrase - human LEDGF/p75 interaction via molecular docking. | 2012 Dec |
|
A correlation between the in vitro drug toxicity of drugs to cell lines that express human P450s and their propensity to cause liver injury in humans. | 2014 Jan |
|
Systems pharmacological analysis of drugs inducing stevens-johnson syndrome and toxic epidermal necrolysis. | 2015 May 18 |
Sample Use Guides
For the relief of rheumatoid arthritis or osteoarthritis, the recommended starting dose
for adults is 400 mg three times daily (1200 mg daily), preferably including a dose on
arising and a dose at bedtime. To achieve optimal therapeutic effect the dose should
be adjusted according to the patient’s response after one or two weeks. Control is
15
usually achieved at doses of 600-1800 mg daily in divided doses (generally t.i.d.).
Doses larger than 1800 mg/day have not been studied and are not recommended.
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/10377455
Tolmetin inhibited the activity of human COX-1 and -2 with IC50 values of 0.35 and 0.82 uM, respectively
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35711-34-3
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23665411
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252-687-3
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