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Tolmetin Sodium

Pronunciation: TOL-met-in SOE-dee-um
Class: NSAID

Trade Names

Tolmetin Sodium
- Tablets, oral 200 mg
- Tablets, oral 600 mg
- Capsules, oral 400 mg

Pharmacology

Decreases inflammation, pain, and fever, probably through inhibition of cyclooxygenase activity and prostaglandin synthesis.

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Pharmacokinetics

Absorption

Rapidly and completely absorbed. T max is approximately 30 to 60 min. Administration with food or milk decreases bioavailability by 16% and administration with food decreases C max by 50%.

Elimination

Biphasic elimination from plasma with a rapid half-life of 1 to 2 h, followed by a slower half-life phase of 5 h. Almost all of the dose is recovered in urine (partially as inactive oxidative metabolites) in 24 h.

Indications and Usage

Treatment of chronic and acute rheumatoid arthritis (RA) and osteoarthritis; treatment of juvenile RA.

Contraindications

Known hypersensitivity to tolmetin; treatment of perioperative pain in the setting of coronary artery bypass graft surgery; patients who have experienced asthma, urticaria, or allergic-type reactions after taking aspirin or other NSAIDs.

Dosage and Administration

Osteoarthritis/Rheumatoid Arthritis
Adults

PO 400 mg 3 times daily initially; titrate to 600 to 1,800 mg/day in divided doses (max, 1,800 mg/day).

Juvenile Rheumatoid Arthritis
Children 2 y and older

PO 20 mg/kg/day in 3 to 4 divided doses initially; titrate to 15 to 30 mg/kg/day (max, 30 mg/kg/day).

General Advice

  • If GI symptoms occur, tolmetin can be administered with antacids other than sodium bicarbonate.

Storage/Stability

Store between 68° and 77°F.

Drug Interactions

ACE inhibitors (eg, enalapril)

The antihypertensive effects of ACE inhibitors may be diminished. Also, the risk of nephrotoxicity associated with ACE inhibitors or tolmetin may be increased. Closely monitor BP. If BP control deteriorates, consider stopping tolmetin. Periodic measurement of renal function is warranted.

Alcohol

The risk of GI bleeding may be increased.

Aminoglycosides (eg, tobramycin)

The risk of acute renal failure may be increased. Avoid coadministration.

Anticoagulants (eg, warfarin)

The risk of bleeding may be increased. Coadminister with caution. Monitor anticoagulant activity and adjust the warfarin dose as needed.

Antiplatelet agents (eg, clopidogrel, prasugrel), corticosteroids (eg, prednisone)

The risk of bleeding may be increased. Use with caution. Closely monitor the patient and instruct the patient to report any signs or symptoms of bleeding.

Bisphosphonates (eg, alendronate)

Synergistic action may increase the risk of GI adverse reactions (eg, gastric ulceration). Use with caution. Closely monitor for GI adverse reactions. Instruct patients to report signs of GI irritation (eg, nausea/vomiting) to their health care provider.

Cyclosporine, tacrolimus

The nephrotoxicity of tolmetin and cyclosporine or tacrolimus may be increased. Closely monitor renal function and cyclosporine or tacrolimus concentrations. If an interaction is suspected, decrease the cyclosporine or tacrolimus dose or discontinue tolmetin.

Direct thrombin inhibitors (eg, dabigatran, desirudin)

The risk of bleeding may be increased. If coadministration cannot be avoided, instruct patients to report any signs or symptoms of bleeding or gastric discomfort to their health care provider.

Food

Administration of tolmetin with milk had no effect on tolmetin C max , but decreased total tolmetin bioavailability by 16%. When tolmetin was taken immediately after a meal, tolmetin C max was reduced by 50% while total bioavailability was again decreased by 16%.

Heparin

The risk of heparin-induced bleeding may be increased. If coadministration cannot be avoided, close clinical and laboratory monitoring is warranted.

Lithium

Lithium plasma concentrations may be elevated and renal Cl reduced, increasing the risk of toxicity. Monitor lithium concentrations and the clinical response. Monitor for signs of lithium toxicity. Adjust the lithium dose as needed.

Loop diuretics (eg, furosemide), thiazide diuretics (eg, chlorothiazide)

Diuretic effects may be reduced. In addition, renal toxicity may occur. Closely observe patients for diuretic efficacy and signs of renal failure.

Methotrexate

Plasma concentrations and toxic effects of methotrexate may be increased. Severe toxicity characterized by bone marrow suppression, nephrotoxicity, and mucositis has occurred in patients receiving NSAIDs and high-dose methotrexate chemotherapy. Fatal toxicity has occurred. Avoid coadministration of high-doses of methotrexate and tolmetin. Use of low-dose methotrexate for RA, commonly used in conjunction with NSAIDs, is considerably less likely to result in a clinically important interaction.

Pemetrexed

Plasma concentrations and toxic effects of pemetrexed may be increased. A 2- to 5-day suspension of tolmetin before and 2 days after pemetrexed administration is recommended in the pemetrexed package labeling. Alternatively, ibuprofen may be an acceptable alternative to tolmetin in patients with healthy renal function who are receiving pemetrexed. Consult pemetrexed package labeling.

Probenecid

Pharmacologic and toxic effects of tolmetin may be increased by probenecid. Monitor for signs of tolmetin toxicity.

Quinolones (eg, ciprofloxacin)

Risk of CNS stimulation and seizures from quinolones may be increased. In addition, plasma concentrations of quinolones may be increased. Coadminister with caution.

Rivaroxaban

Because of additive effects on the inhibition of normal clotting mechanisms, the risk of bleeding may be increased. Coadminister with caution. Careful clinical monitoring is warranted.

Salicylates (eg, aspirin)

The risk of serious GI events and salicylate toxicity may be increased. Coadministration is not recommended.

Serotonin reuptake inhibitors (eg, fluoxetine, venlafaxine)

The risk of upper GI bleeding may be increased. If coadministration cannot be avoided, close clinical monitoring for signs of GI bleeding is warranted. Consider the use of acid suppression therapy. Instruct patients to report any signs or symptoms of bleeding.

Smoking

The risk of GI bleeding may be increased.

Triamterene

The risk of acute renal failure may be increased. If coadministration cannot be avoided, closely monitor renal function. If renal function decreases, consider stopping one or both drugs.

Laboratory Test Interactions

The metabolites of tolmetin in urine have been found to give positive tests for proteinuria using tests that rely on acid precipitation as their end point (eg, sulfosalicylic acid).

Adverse Reactions

Cardiovascular

Elevated BP (3% to 9%).

CNS

Asthenia, dizziness, headache (3% to 9%); depression, drowsiness (more than 1% to less than 3%).

Dermatologic

Skin irritation (more than 1% to less than 3%).

EENT

Tinnitus, visual disturbance (more than 1% to less than 3%).

GI

Nausea (11%); abdominal pain, diarrhea, dyspepsia, flatulence, GI distress, vomiting (3% to 9%); constipation, gastritis, peptic ulcer (more than 1% to less than 3%).

Genitourinary

Elevation in BUN, UTI (more than 1% to less than 3%).

Hematologic

Decrease in Hgb or Hct.

Metabolic-Nutritional

Edema, weight gain or loss (3% to 9%).

Miscellaneous

Chest pain (more than 1% to less than 3%).

Precautions

Warnings

NSAIDs may cause an increased risk of serious CV thrombotic events, MI, and stroke, which can be fatal. This risk may increase with length of therapy. Patients with CV disease or risk factors for CV disease may be at greater risk. NSAIDs cause an increased risk of serious GI adverse reactions, including bleeding, inflammation, perforation of the stomach or intestines, and ulceration, which can be fatal. These events can occur any time during use and without warning symptoms. Elderly patients are at greater risk of serious GI events.


Monitor

Monitor for signs or symptoms of GI tract ulcerations and bleeding. In patients on long-term treatment, periodically check CBC and chemistry profile. Check Hgb or Hct in patients on long-term treatment if they exhibit signs or symptoms of anemia. Monitor renal function in patients with compromised kidney function. Perform eye examinations if patients experience visual disturbances. Closely monitor BP during the initiation of treatment and throughout the course of therapy. Carefully monitor patients who may be adversely affected by alterations in platelet function (eg, patients with coagulation disorders or receiving anticoagulant therapy).


Pregnancy

Category C . Avoid late in pregnancy.

Lactation

Excreted in breast milk.

Children

Safety and efficacy not established in pediatric patients younger than 2 y.

Elderly

Use with caution.

Renal Function

Not recommended in patients with advanced renal disease.

Special Risk Patients

Use with caution in patients with fluid retention, heart failure, or hypertension.

Anaphylactoid reactions

Anaphylactoid reactions may occur. Do not give tolmetin to patients with the aspirin triad, which typically occurs in patients with asthma who experience rhinitis with or without nasal polyps, or those who exhibit severe, potentially fatal bronchospasm after taking aspirin or other NSAIDs.

Asthma

Patients with asthma may have aspirin-sensitive asthma, which may be associated with severe and sometimes fatal bronchospasm when these patients use aspirin. Do not administer tolmetin to patients with this type of aspirin sensitivity because of possible cross-reactivity.

Dermatologic effects

Serious and sometimes fatal skin adverse reactions, including exfoliative dermatitis, Stevens-Johnson syndrome, and TEN, may occur.

Edema

Fluid retention and edema have been observed in patients taking NSAIDs.

Hematologic effects

Anemia has been reported and may be the result of fluid retention, occult or gross GI bleeding, or an incompletely described effect on erythropoiesis.

Hepatic effects

Elevations of 1 or more LFTs may occur in patients taking tolmetin. Cases of severe hepatic reactions, including liver necrosis, jaundice, fulminant hepatitis, and liver failure, have been reported.

Hypertension

New hypertension or worsening of preexisting hypertension, either of which may contribute to increased risk of CV events, may occur.

Inflammation and fever

The activity of tolmetin in reducing fever and inflammation may diminish the utility of these diagnostic signs in detecting complications of presumed noninfectious, painful conditions.

Platelet aggregation

May inhibit platelet aggregation; use with caution in patients with coagulation disorders or those on anticoagulant therapy.

Renal effects

Renal papillary necrosis and other renal injury may occur with long-term use. Acute interstitial nephritis with hematuria, proteinuria, and, occasionally, nephrotic syndrome has been reported. Patients at greatest risk for renal toxicity are those with impaired renal function, heart failure, or liver dysfunction; those taking diuretics or ACE inhibitors; and elderly patients.

Overdosage

Symptoms

No data available.

Patient Information

  • Encourage patients to read the NSAID Medication Guide that accompanies each prescription dispensed.
  • Tell patients to avoid taking with food or milk or immediately after a meal. If medication causes stomach upset, tell patients to take with antacids that do not contain sodium bicarbonate.
  • Explain that if drowsiness, dizziness, or blurred vision occurs, patients should observe caution while driving or performing other tasks requiring alertness.
  • Explain that photosensitivity may occur and to use sunscreens and wear protective clothing when exposed to UV or sunlight until tolerance is determined.
  • Caution patients to avoid taking other NSAIDs, aspirin, alcohol, or other OTC medications unless advised to do so by their health care provider.
  • Advise patients to discontinue tolmetin and to notify their health care provider if any of the following occur: persistent GI upset, headache, itching, visual disturbances, unusual bleeding or bruising, black stools, weight gain or edema, changes in urine pattern, joint pain, fever, or blood in their urine.
  • Inform patients that NSAIDs can cause serious skin adverse reactions, such as exfoliative dermatitis, Stevens-Johnson syndrome, and TEN, which may result in hospitalization and even death. Advise patients to be alert for skin rash, skin blisters, fever, and itching, and to seek medical advice if any of these occur. Advise patients to stop tolmetin immediately and contact their health care provider if any type of skin rash develops.
  • Inform patients of the warning signs and symptoms of hepatotoxicity (eg, nausea, fatigue, lethargy, pruritus, jaundice, flu-like symptoms). If these occur, instruct patients to stop therapy and seek immediate medical attention.
  • Inform patients that tolmetin, like other NSAIDs, may cause serious CV events, such as MI or stroke. Alert patients to the signs and symptoms of chest pain, shortness of breath, weakness, and slurring of speech. They should seek medical advice immediately if any of these symptoms are observed.
  • Instruct patients to seek immediate emergency help in the case of an anaphylactoid reaction (eg, difficulty breathing, swelling of the face or throat).
  • Advise women of childbearing potential to avoid use of tolmetin in late pregnancy because of the risk of premature closure of the ductus arteriosus.

Copyright © 2009 Wolters Kluwer Health.

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