TOLMETIN SODIUM

TOLMETIN SODIUM (tole'met-in) Tolectin, Tolectin DS Classifications: analgesic, nonsteroidal antiinflammatory (nsaid); antipyretic; Therapeutic: nsaid, analgesic; antipyretic; disease-modifying antirheumatic drug (dmard) Prototype: Ibuprofen Pregnancy Category: C first and second trimester; D third trimester

Availability

200 mg, 600 mg tablets; 400 mg capsules

Action

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.

Therapeutic Effect

Possesses analgesic, antiinflammatory, and antipyretic and antirheumatic activity.

Uses

In acute flares and management of chronic rheumatoid arthritis. May be used alone or in combination with gold or corticosteroids.

Contraindications

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.

Cautious Use

History of upper GI tract disease; impaired kidney function; SLE; compromised cardiac function.

Route & Dosage

Arthritis Adult: PO 400 mg t.i.d. (max: 2 g/d) Child (≥2 y): PO 20 mg/kg/d in 3–4 divided doses (max: 30 mg/kg/d)

Administration

Oral

• 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 instructed.

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)].

Interactions

Drug: oral anticoagulants, heparin may prolong bleeding time; may increase lithium toxicity; aspirin, other nsaids add to ulcerogenic effects; may increase methotrexate toxicity. Herbal: Feverfew, garlic, ginger, ginkgo may increase bleeding potential.

Pharmacokinetics

Absorption: Rapidly from GI tract. Peak: 30–60 min. Distribution: Crosses blood–brain barrier and placenta; distributed into breast milk. Metabolism: In liver. Elimination: In urine. Half-Life: 60–90 min.

Nursing Implications

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, edema.
• Avoid potentially hazardous activities until response to drug is known because dizziness and drowsiness are common adverse effects.

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Common adverse effects in italic, life-threatening effects underlined; generic names in bold; classifications in SMALL CAPS; Canadian drug name; Prototype drug