Tolectin, Tolectin DS
Classifications: analgesic, nonsteroidal antiinflammatory (nsaid); antipyretic; Therapeutic: nsaid, analgesic; antipyretic; disease-modifying antirheumatic drug (dmard)
Pregnancy Category: C first and second trimester; D third trimester
200 mg, 600 mg tablets; 400 mg capsules
Nonsteroidal antiinflammatory analgesic that competitively inhibits both cyclooxygenase (COX) isoenzymes, COX-1 and COX-2,
by blocking arachidonate binding to prostaglandin sites, and thus inhibits prostaglandin synthesis.
Possesses analgesic, antiinflammatory, and antipyretic and antirheumatic activity.
In acute flares and management of chronic rheumatoid arthritis. May be used alone or in combination with gold or corticosteroids.
History of intolerance or hypersensitivity to tolmetin, aspirin, and other NSAIDs; active peptic ulcer, patients with asthma, nasal polyps, rhinitis, "aspirin triad," CABG perioperative pain;
in patients with functional class IV rheumatoid arthritis (severely incapacitated, bedridden, or confined to a wheelchair).
Safety during pregnancy (category C in first and second trimester, and category D in third trimester), lactation, or children
<2 y is not established.
History of upper GI tract disease; impaired kidney function; SLE; compromised cardiac function.
Route & Dosage
Adult: PO 400 mg t.i.d. (max: 2 g/d)
Child (≥2 y): PO 20 mg/kg/d in 34 divided doses (max: 30 mg/kg/d)
- Schedule treatment (preferred) to include a morning dose (on arising) and a bedtime dose.
- Give with fluid of patient's choice; crush tablet or empty capsule to mix with water or food if patient cannot swallow tablet/capsule.
- Store at 15°30° C (59°86° F) in tightly capped and light-resistant container unless otherwise
Adverse Effects (≥1%)CNS: Headache, dizziness, vertigo, lightheadedness,
mood elevation or depression
, tension, nervousness, weakness, drowsiness, insomnia
, tinnitus. CV:
Mild edema (about 7% patients), sodium and water retention, mild to moderate hypertension. GI:
Epigastric or abdominal pain, dyspepsia, nausea,
vomiting, heartburn, constipation
, peptic ulcer
, GI bleeding. Hematologic:
Transient and small decreases in hemoglobin and hematocrit, purpura, petechiae, granulocytopenia, leukopenia. Urogenital:
Hematuria, proteinuria, increased BUN. Skin: Toxic epidermal necrolysis,
morbilliform eruptions, urticaria, pruritus. Body as a Whole: Anaphylaxis
(especially after drug is discontinued and then reinstituted).
Diagnostic Test Interference
Tolmetin prolongs bleeding time, inhibits platelet aggregation, elevates BUN, alkaline phosphatase, and AST levels; may decrease hemoglobin and hematocrit values. Metabolites may produce false-positive results for proteinuria [with tests that rely on acid precipitation (e.g., sulfosalicylic acid)].
InteractionsDrug: oral anticoagulants
may prolong bleeding time; may increase lithium
s add to ulcerogenic effects; may increase methotrexate
toxicity. Herbal: Feverfew, garlic, ginger, ginkgo
may increase bleeding potential.
Rapidly from GI tract. Peak:
3060 min. Distribution:
Crosses bloodbrain barrier and placenta; distributed into breast milk. Metabolism:
In liver. Elimination:
In urine. Half-Life:
Assessment & Drug Effects
- Monitor therapeutic effect. Therapeutic response for rheumatoid arthritis or osteoarthritis generally occurs within 1 wk
with progressive improvement in succeeding week: Reduced joint pain and swelling, reduction in duration of morning stiffness,
improved functional capacity (increase in grip strength, delayed onset of fatigue).
- Monitor patients with kidney damage closely. Evaluate I&O ratio and encourage patient to increase fluid intake to at least
8 full glasses per day.
- Lab tests: Obtain periodic kidney function tests (routine urinalysis, creatinine clearance, and serum creatinine) for patient
on long-term therapy.
- Check self-medicating habits of the patient. Sodium bicarbonate alkalinizes the urine, which increases urinary excretion
of tolmetin and may reduce degree and duration of effectiveness.
Patient & Family Education
- Take drug with meals or milk if GI disturbances occur. Notify physician if symptoms persist; dosage reduction may be necessary,
or antacid added.
- Monitor weight and report an increase >2 kg (4 lb)/wk with impaired kidney or cardiac function; check for swelling in ankles,
tibiae, hands, and feet.
- Inform surgeon or dentist before treatment if you are taking tolmetin because of possible enhanced bleeding.
- Report promptly signs of abnormal bleeding (ecchymosis, epistaxis, melena, petechiae), itching, skin rash, persistent headache,
- Avoid potentially hazardous activities until response to drug is known because dizziness and drowsiness are common adverse