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Pronunciation(TOLE met in)
U.S. Brand NamesTolectin®; Tolectin® DS [DSC]
SynonymsTolmetin Sodium
Generic AvailableYes
Canadian Brand NamesTolectin®
UseTreatment of rheumatoid arthritis and osteoarthritis, juvenile rheumatoid arthritis
Pregnancy Risk FactorC/D (3rd trimester or at term)
LactationEnters breast milk/compatible
ContraindicationsHypersensitivity to tolmetin, any component of the formulation, aspirin, or other NSAIDs; pregnancy (3rd trimester or near term)
Warnings/PrecautionsFatal asthmatic and anaphylactoid reactions have occurred in patients with "aspirin triad." Use with caution in patients with CHF, hypertension, dehydration, decreased renal or hepatic function, history of GI disease (bleeding, ulcers, or previous GI symptoms with NSAID use), or those receiving anticoagulants and/or corticosteroids. Use lowest effective dose for shortest period possible; bleeding risk has been correlated to dose and duration of therapy. Gastrointestinal bleeding may occur without prior symptoms of gastrointestinal irritation. Elderly are at a high risk for adverse effects from NSAIDs. As many as 60% of elderly can develop peptic ulceration and/or hemorrhage asymptomatically. Use of NSAIDs can compromise existing renal function especially when Clcr<30 mL/minute. CNS adverse effects such as confusion, agitation, and hallucination are generally seen in overdose or high-dose situations; however, elderly may demonstrate these adverse effects at lower doses than younger adults. Withhold for at least 4-6 half-lives prior to surgical or dental procedures.
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Adverse Reactions1% to 10%:
Cardiovascular: Chest pain, hypertension, edema
Central nervous system: Headache, dizziness, drowsiness, depression
Dermatologic: Skin irritation
Endocrine & metabolic: Weight gain/loss
Gastrointestinal: Heartburn, abdominal pain, diarrhea, flatulence, vomiting, constipation, gastritis, peptic ulcer, nausea
Genitourinary: Urinary tract infection
Hematologic: Elevated BUN, transient decreases in hemoglobin/hematocrit
Ocular: Visual disturbances
Otic: Tinnitus
<1%: CHF, hypertension, arrhythmia, tachycardia, confusion, hallucinations, aseptic meningitis, mental depression, drowsiness, insomnia, urticaria, erythema multiforme, toxic epidermal necrolysis, Stevens-Johnson syndrome, angioedema, polydipsia, hot flashes, gastritis, GI ulceration, cystitis, polyuria, agranulocytosis, anemia, hemolytic anemia, bone marrow suppression, leukopenia, thrombocytopenia, hepatitis, peripheral neuropathy, toxic amblyopia, blurred vision, conjunctivitis, dry eyes, decreased hearing, acute renal failure, allergic rhinitis, dyspnea, bronchospasm, epistaxis
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Overdosage/ToxicologySymptoms of overdose include lethargy, mental confusion, dizziness, leukocytosis, and renal failure. Management of NSAID intoxication is supportive and symptomatic. Since many NSAIDs undergo enterohepatic cycling, multiple doses of charcoal may be needed to reduce the potential for delayed toxicities.
Drug InteractionsACE inhibitors: Antihypertensive effects may be decreased by concurrent therapy with NSAIDs; monitor blood pressure.
Angiotensin II antagonists: Antihypertensive effects may be decreased by concurrent therapy with NSAIDs; monitor blood pressure.
Anticoagulants (warfarin, heparin, LMWHs) in combination with NSAIDs can cause increased risk of bleeding.
Other antiplatelet drugs (ticlopidine, clopidogrel, aspirin, abciximab, dipyridamole, eptifibatide, tirofiban) can cause an increased risk of bleeding.
Corticosteroids may increase the risk of GI ulceration; avoid concurrent use.
Cyclosporine: NSAIDs may increase serum creatinine, potassium, blood pressure, and cyclosporine levels; monitor cyclosporine levels and renal function carefully.
Hydralazine's antihypertensive effect is decreased; avoid concurrent use.
Lithium levels can be increased; avoid concurrent use if possible or monitor lithium levels and adjust dose. Sulindac may have the least effect. When NSAID is stopped, lithium will need adjustment again.
Loop diuretics efficacy (diuretic and antihypertensive effect) may be reduced.
Methotrexate: Severe bone marrow suppression, aplastic anemia, and GI toxicity have been reported with concomitant NSAID therapy. Avoid use during moderate or high-dose methotrexate (increased and prolonged methotrexate levels). NSAID use during low-dose treatment of rheumatoid arthritis has not been fully evaluated; extreme caution is warranted.
Thiazides antihypertensive effects are decreased; avoid concurrent use.
Warfarin's INRs may be increased by piroxicam. Other NSAIDs may have the same effect depending on dose and duration. Monitor INR closely. Use the lowest dose of NSAIDs possible and for the briefest duration.
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Ethanol/Nutrition/Herb InteractionsEthanol: Avoid ethanol (may enhance gastric mucosal irritation).
Food: Tolmetin peak serum concentrations may be decreased if taken with food or milk.
Herb/Nutraceutical: Avoid cat's claw, dong quai, evening primrose, feverfew, garlic, ginger, ginkgo, red clover, horse chestnut, green tea, ginseng (all have additional antiplatelet activity).
Mechanism of ActionInhibits prostaglandin synthesis by decreasing the activity of the enzyme, cyclooxygenase, which results in decreased formation of prostaglandin precursors
Pharmacodynamics/KineticsOnset of action: Analgesic: 1-2 hours; Anti-inflammatory: Days to weeks
Absorption: Well absorbed
Bioavailability: Reduced 16% with food or milk
Half-life elimination: Biphasic: Rapid: 1-2 hours; Slow: 5 hours
Time to peak, serum: 30-60 minutes
Excretion: Urine (as inactive metabolites or conjugates) within 24 hours
DosageOral: Children  2 years:
Anti-inflammatory: Initial: 20 mg/kg/day in 3 divided doses, then 15-30 mg/kg/day in 3 divided doses
Analgesic: 5-7 mg/kg/dose every 6-8 hours
Adults: 400 mg 3 times/day; usual dose: 600 mg to 1.8 g/day; maximum: 2 g/day
Monitoring ParametersOccult blood loss, CBC, liver enzymes, BUN, serum creatinine, periodic liver function test
Dietary ConsiderationsShould be taken with food, milk, or antacids to decrease GI adverse effects. Sodium content of 200 mg: 0.8 mEq.
Patient EducationTake this medication exactly as directed; do not increase dose without consulting prescriber. Do not crush tablets or break capsules. Take with food or milk to reduce GI distress. Maintain adequate hydration (2-3 L/day of fluids) unless instructed to restrict fluid intake. You should have regular ophthalmic evaluations when using NSAIDs for long periods of time. Do not use alcohol, aspirin or aspirin-containing medication, or any other anti-inflammatory medications without consulting prescriber. You may experience dizziness, nervousness, or headache (use caution when driving or engaging in tasks requiring alertness until response to drug is known); or nausea, vomiting, or heartburn (small, frequent meals, frequent mouth care, sucking lozenges, or chewing gum may help); or constipation (increased exercise, fluids, fruit, or fiber may help). GI bleeding, ulceration, or perforation can occur with or without pain. Discontinue medication and contact prescriber if persistent abdominal pain or cramping, or blood in stool occurs. Report chest pain or palpitations; breathlessness or respiratory difficulty; unusual bruising/bleeding; blood in urine, stool, mouth, or vomitus; unusual fatigue; skin rash or itching; unusual weight gain or swelling of extremities; change in urinary pattern; or change in vision or hearing or ringing in ears. Pregnancy precaution: Inform prescriber if you are or intend to become pregnant. This drug should not be used in the 3rd trimester of pregnancy.
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Nursing ImplicationsMonitor occult blood loss, CBC, liver enzymes, BUN, serum creatinine, periodic liver function test
Anesthesia and Critical Care Concerns/Other ConsiderationsThe 2002 ACCM/SCCM guidelines for analgesia (critically-ill adult) suggest that NSAIDs may be used in combination with opioids in select patients for pain management. Concern about adverse events (increased risk of renal dysfunction, altered platelet function and gastrointestinal irritation) limits its use in patients who have other underlying risks for these events. In short-term use, NSAIDs vary considerably in their effect on blood pressure. When NSAIDs are used in patients with hypertension, appropriate monitoring of blood pressure responses should be completed and the duration of therapy, when possible, kept short. The use of NSAIDs in the treatment of patients with congestive heart failure may be associated with an increased risk for fluid accumulation and edema; may precipitate renal failure in dehydrated patients.
Cardiovascular ConsiderationsIn short-term use, NSAIDs vary considerably in their effect on blood pressure. A recent meta-analysis (see References) showed that indomethacin and naproxen had the largest effect on blood pressure. Other NSAIDs, including piroxicam, ibuprofen, and sulindac had less of an effect. Ibuprofen combined with captopril or losartan may attenuate the antihypertensive effects of ACE inhibition or receptor blockade on sitting or 24-hour ambulatory diastolic blood pressure. When NSAIDs are used in patients with hypertension, appropriate monitoring of blood pressure responses should be completed and the duration of therapy, when possible, kept short. The use of NSAIDs in the treatment of patients with congestive heart failure may be associated with an increased risk for fluid accumulation and edema. One study showed that NSAID use in elderly patients had an increased risk of hospitalization for heart failure. This study gives compelling reasons to avoid or limit the use of NSAIDs in patients with congestive heart failure, particularly in the elderly population.
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Dental Health: Effects on Dental TreatmentNSAID formulations are known to reversibly decrease platelet aggregation via mechanisms different than observed with aspirin. The dentist should be aware of the potential of abnormal coagulation. Caution should also be exercised in the use of NSAIDs in patients already on anticoagulant therapy with drugs such as warfarin (Coumadin®).
Dental Health: Vasoconstrictor/Local Anesthetic PrecautionsNo information available to require special precautions
Mental Health: Effects on Mental StatusDizziness is common; may cause nervousness; may rarely cause drowsiness, confusion, insomnia, hallucinations, or depression
Mental Health: Effects on Psychiatric TreatmentMay rarely cause agranulocytosis; use caution with clozapine and carbamazepine; may decrease lithium clearance resulting in an increase in serum lithium levels and potential lithium toxicity; monitor serum lithium levels
Dosage Forms[DSC] = Discontinued product Capsule, as sodium: 400 mg
Tolectin® DS: 400 mg [DSC]
Tablet, as sodium: 200 mg, 600 mg
Tolectin®: 600 mg
ReferencesBerde C, Ablin A, Glazer J, et al, "American Academy of Pediatrics Report of the Subcommittee on Disease-Related Pain in Childhood Cancer,"Pediatrics, 1990, 86(5 Pt 2):818-25.
Brooks PM and Day RO, "Nonsteroidal Anti-inflammatory Drugs - Differences and Similarities,"N Engl J Med, 1991, 324(24):1716-25.
Clinch D, Banerjee AK, and Ostick G, "Absence of Abdominal Pain in Elderly Patients With Peptic Ulcer,"Age Ageing, 1984, 13(2):120-3.
Clive DM and Stoff JS, "Renal Syndromes Associated With Nonsteroidal Anti-inflammatory Drugs,"N Engl J Med, 1984, 310(9):563-72.
Conlin P, Moore T, Swartz S, et al, "Effect of Indomethacin on Blood Pressure Lowering by Captopril and Losartan in Hypertensive Patients,"Hypertension, 2000, 36(3):461-5.
Court H and Volans GN, "Poisoning After Overdose With Nonsteroidal Anti-inflammatory Drugs,"Adverse Drug React Acute Poisoning Rev, 1984, 3(1):1-21.
"Drugs for Pain,"Med Lett Drugs Ther, 2000, 42(1085):73-8.
Graham DY, "Prevention of Gastroduodenal Injury Induced by Chronic Nonsteroidal Anti-inflammatory Drug Therapy,"Gastroenterology, 1989, 96(2 Pt 2 Suppl):675-81.
Gurwitz JH, Avorn J, Ross-Degnan D, et al, "Nonsteroidal Anti-Inflammatory Drug-Associated Azotemia in the Very Old,"JAMA, 1990, 264(4):471-5.
Hawkey CJ, Karrasch JA, Szczepañski L, et al, "Omeprazole Compared With Misoprostrol for Ulcers Associated With Nonsteroidal Anti-inflammatory Drugs,"N Engl J Med, 1998, 338(11):727-34.
Heerdink ER, Leufkens HG, Herings RM, et al, "NSAIDs Associated With Increased Risk of Congestive Heart Failure in Elderly Patients Taking Diuretics,"Arch Intern Med, 1998, 158(10):1108-12.
Hollingworth P, "The Use of Nonsteroidal Anti-inflammatory Drugs in Paediatric Rheumatic Diseases,"Br J Rheumatol, 1993, 32(1):73-7.
Hoppmann RA, Peden JG, and Ober SK, "Central Nervous System Side Effects of Nonsteroidal Anti-inflammatory Drugs. Aseptic Meningitis, Psychosis, and Cognitive Dysfunction,"Arch Intern Med, 1991, 151(7):1309-13.
Jacobi J, Fraser GL, Coursin DB, et al, "Clinical Practice Guidelines for the Sustained Use of Sedatives and Analgesics in the Critically Ill Adult,"Crit Care Med, 2002, 30(1):119-41. Available at: http://www.sccm.org/pdf/sedatives.pdf. Accessed August 2, 2003.
Knodel LC, "Preventing NSAID-Induced Ulcers: The Role of Misoprostol,"Consult Pharm, 1989, 4:37-41.
Morgan TO, Anderson A, and Bertram D, "Effect of Indomethacin on Blood Pressure in Elderly People With Essential Hypertension Well Controlled on Amlodipine or Enalapril,"Am J Hypertens, 2000, 13(11):1161-7.
Page J and Henry D, "Consumption of NSAIDs and the Development of Congestive Heart Failure in Elderly Patients: An Underrecognized Public Health Problem,"Arch Intern Med, 2000, 160(6):777-84.
Pope JE, Anderson JJ, and Felson DT, "A Meta-analysis of the Effects of Nonsteroidal Anti-inflammatory Drugs on Blood Pressure,"Arch Intern Med, 1993, 153(4):477-84.
Pounder R, "Silent Peptic Ulceration: Deadly Silence or Golden Silence?"Gastroenterology, 1989, 96(2 Pt 2 Suppl):626-31.
Rose CD and Doughty RA, "Pharmacological Management of Juvenile Rheumatoid Arthritis,"Drugs, 1992, 43(6):849-63.
Smolinske SC, Hall AH, Vandenberg SA, et al, "Toxic Effects of Nonsteroid Anti-inflammatory Drugs in Overdose. An Overview of Recent Evidence on Clinical Effects and Dose-Response Relationships,"Drug Saf, 1990, 5(4):252-74.
Vale JA and Meredith TJ, "Acute Poisoning Due to Nonsteroidal Anti-inflammatory Drugs,"Med Toxicol, 1986, 1(1):12-31.
Verbeeck RK, "Pharmacokinetic Drug Interactions With Nonsteroidal Anti-inflammatory Drugs,"Clin Pharmacokinet, 1990, 19(1):44-66.
Yeomans ND, Tulassay Z, Juhasz L, et al, "A Comparison of Omeprazole With Ranitidine for Ulcers Associated With Nonsteroidal Anti-inflammatory Drugs,"N Engl J Med, 1998, 338(11):719-26.
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International Brand NamesArtocaptin® (ES); Artrocaptin® (ES); Safitex® (AR); Tolectin® (AT, BE, BG, CA, CY, CZ, EG, IT, JO, LB, LU, MT, MX, NL, SY, TR, ZA)
The information provided herein should not be used during any medical emergency or for the diagnosis or treatment of any medical condition. A licensed medical professional should be consulted for diagnosis and treatment of any and all medical conditions. Call 911 for all medical emergencies. Links to other sites are provided for information only -- they do not constitute endorsements of those other sites. © 1997-
A.D.A.M., Inc. Any duplication or distribution of the information contained herein is strictly prohibited. |
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