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Pronunciation |
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(TOLE
met
in) |
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U.S. Brand
Names |
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Tolectin®; Tolectin®
DS |
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Generic
Available |
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No |
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Canadian Brand
Names |
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Novo-Tolmetin |
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Synonyms |
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Tolmetin Sodium |
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Pharmacological Index |
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Nonsteroidal Anti-Inflammatory Agent (NSAID) |
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Use |
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Treatment of rheumatoid arthritis and osteoarthritis, juvenile rheumatoid
arthritis |
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Pregnancy Risk
Factor |
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C (D in 3rd trimester or near delivery) |
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Contraindications |
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Known hypersensitivity to tolmetin or any component, aspirin, or other
nonsteroidal anti-inflammatory drugs (NSAIDs) |
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Warnings/Precautions |
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Use with caution in patients with upper GI disease, impaired renal function,
congestive heart failure, dehydration, hypertension, and patients receiving
anticoagulants; if GI upset occurs with tolmetin, take with antacids other than
sodium bicarbonate |
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Adverse
Reactions |
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>10%:
Central nervous system: Dizziness
Dermatologic: Rash
Gastrointestinal: Abdominal cramps, heartburn, indigestion, nausea
1% to 10%:
Central nervous system: Headache, nervousness
Dermatologic: Itching
Endocrine & metabolic: Fluid retention
Gastrointestinal: Vomiting
Otic: Tinnitus
<1%: Congestive heart failure, hypertension, arrhythmias, 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, shortness of breath, epistaxis
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Overdosage/Toxicology |
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Symptoms of overdose include lethargy, mental confusion, dizziness,
leukocytosis, renal failure
Management of a nonsteroidal anti-inflammatory drug (NSAID) intoxication is
primarily supportive and symptomatic. Fluid therapy is commonly effective in
managing the hypotension that may occur following an acute NSAID overdose,
except when this is due to an acute blood loss. Seizures tend to be very
short-lived and often do not require drug treatment; although, recurrent
seizures should be treated with I.V. diazepam. Since many of the NSAID undergo
enterohepatic cycling, multiple doses of charcoal may be needed to reduce the
potential for delayed toxicities. |
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Drug
Interactions |
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Decreased effect with aspirin; decreased effect of thiazides, furosemide, ACE
inhibitors
Increased toxicity of digoxin, methotrexate, cyclosporine, lithium, insulin,
sulfonylureas, potassium-sparing diuretics, aspirin |
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Mechanism of
Action |
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Inhibits prostaglandin synthesis by decreasing the activity of the enzyme,
cyclo-oxygenase, which results in decreased formation of prostaglandin
precursors |
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Pharmacodynamics/Kinetics |
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Onset of effect: Analgesic: 1-2 hours; Anti-inflammatory: Days - weeks
Absorption: Oral: Well absorbed
Bioavailability: Food/milk decreases total bioavailability by 16%
Time to peak serum concentration: Within 30-60 minutes |
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Usual Dosage |
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Oral:
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
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Dietary
Considerations |
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Should be administered with food, milk, or antacids to decrease GI adverse
effects; food or milk may decrease the extent of oral
absorption |
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Monitoring
Parameters |
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Occult blood loss, CBC, liver enzymes, BUN, serum creatinine, periodic liver
function test |
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Mental Health: Effects
on Mental Status |
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Dizziness is common; may cause nervousness; may rarely cause drowsiness,
confusion, insomnia, hallucinations, or depression |
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Mental Health:
Effects on Psychiatric
Treatment |
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May 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 |
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Dental Health: Local
Anesthetic/Vasoconstrictor
Precautions |
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No information available to require special precautions |
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Dental Health:
Effects on Dental Treatment |
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NSAID 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®). |
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Patient
Information |
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Take 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 fluid intake (2-3 L/day of fluids
unless instructed to restrict fluid intake). Do not use alcohol, aspirin, or
aspirin-containing medication, and all 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); nausea, vomiting, or heartburn (frequent small
meals, frequent mouth care, sucking lozenges, or chewing gum may help);
constipation (increased exercise, fluids, or dietary fruit and 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 difficulty breathing; 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 precautions: Inform
prescriber if you are or intend to be pregnant. |
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Nursing
Implications |
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Monitor occult blood loss, CBC, liver enzymes, BUN, serum creatinine,
periodic liver function test |
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Dosage Forms |
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Capsule, as sodium (Tolectin® DS): 400 mg
Tablet, as sodium (Tolectin®): 200 mg, 600 mg
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References |
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Berde 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, Ostick G,
"Absence of Abdominal Pain in Elderly Patients With Peptic Ulcer," Age
Ageing, 1984, 13:120-3.
Clive DM, Stoff JS,
"Renal Syndromes Associated With Nonsteroidal Anti-inflammatory Drugs," N
Engl J Med, 1984, 310(9):563-72.
Court H and Volans GN,
"Poisoning After Overdose With Nonsteroidal Anti-inflammatory Drugs," Adverse
Drug React Acute Poisoning Rev, 1984, 3(1):1-21.
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, Szczepanski L, et al,
"Omeprazole Compared With Misoprostrol for Ulcers Associated With Nonsteroidal Anti-inflammatory Drugs,"
N Engl J Med, 1998, 338(11):727-34.
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.
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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