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Details

Stereochemistry ACHIRAL
Molecular Formula C17H18N2O4
Molecular Weight 314.3358
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of AMTOLMETIN

SMILES

CN1C(CC(=O)NCC(O)=O)=CC=C1C(=O)C2=CC=C(C)C=C2

InChI

InChIKey=IYNXNYQOVKPFMM-UHFFFAOYSA-N
InChI=1S/C17H18N2O4/c1-11-3-5-12(6-4-11)17(23)14-8-7-13(19(14)2)9-15(20)18-10-16(21)22/h3-8H,9-10H2,1-2H3,(H,18,20)(H,21,22)

HIDE SMILES / InChI

Molecular Formula C17H18N2O4
Molecular Weight 314.3358
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

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

TargetsConditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Tolmetin sodium

Approved Use

Carefully 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 Date

1976
Primary
Tolmetin sodium

Approved Use

Carefully 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 Date

1976
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
29.3 μg/mL
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

AUC

ValueDoseCo-administeredAnalytePopulation
50.5 μg × h/mL
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

T1/2

ValueDoseCo-administeredAnalytePopulation
0.83 h
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

Doses

DosePopulationAdverse 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%)
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%)
Sources:
AEs

AEs

AESignificanceDosePopulation
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:
Overview

Overview

CYP3A4CYP2C9CYP2D6hERG

OverviewOther

Other InhibitorOther SubstrateOther Inducer



Drug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
yes [IC50 20.5 uM]
yes [IC50 494 uM]
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
yes
yes
PubMed

PubMed

TitleDatePubMed
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
Patents

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
Tolmetin inhibited the activity of human COX-1 and -2 with IC50 values of 0.35 and 0.82 uM, respectively
Substance Class Chemical
Created
by admin
on Sat Dec 16 01:46:13 GMT 2023
Edited
by admin
on Sat Dec 16 01:46:13 GMT 2023
Record UNII
3RS348SV6U
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
AMTOLMETIN
Common Name English
GLYCINE, N-(2-(1-METHYL-5-(4-METHYLBENZOYL)-1H-PYRROL-2-YL)ACETYL)-
Systematic Name English
N-((1-METHYL-5-P-TOLUOYLPYRROL-2-YL)ACETYL)GLYCINE
Common Name English
TOLMETIN GLYCINE AMIDE
Common Name English
MCN-4366
Code English
MCN 4366
Code English
Code System Code Type Description
FDA UNII
3RS348SV6U
Created by admin on Sat Dec 16 01:46:13 GMT 2023 , Edited by admin on Sat Dec 16 01:46:13 GMT 2023
PRIMARY
PUBCHEM
135911
Created by admin on Sat Dec 16 01:46:13 GMT 2023 , Edited by admin on Sat Dec 16 01:46:13 GMT 2023
PRIMARY
CAS
87344-05-6
Created by admin on Sat Dec 16 01:46:13 GMT 2023 , Edited by admin on Sat Dec 16 01:46:13 GMT 2023
PRIMARY
EPA CompTox
DTXSID90236290
Created by admin on Sat Dec 16 01:46:13 GMT 2023 , Edited by admin on Sat Dec 16 01:46:13 GMT 2023
PRIMARY
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