tolmetin

Absorption: Well absorbed from the GI tract following oral administration.

Distribution: Unknown.

Protein Binding: >99%.

Metabolism/Excretion: Mostly metabolized by the liver; 20% excreted unchanged by the kidneys.

Half-Life: 1 hr.

Time/Action Profile ⬆ ⬇

(anti-inflammatory effects)

ROUTE	ONSET	PEAK	DURATION
PO	within 7 days	1–2 wk	unknown

Contraind./Precautions ⬆ ⬇

Contraindicated in:

Hypersensitivity;
Cross-sensitivity may exist with other NSAIDs, including aspirin;
Active GI bleeding or ulcer disease;
Perioperative pain from coronary artery bypass graft surgery;
OB: Avoid use of NSAIDs after 30 wk gestation (may cause premature closure of fetal ductus arteriosus);
Lactation: Lactation.

Use Cautiously in:

Cardiovascular disease or risk factors for cardiovascular disease (may ↑ risk of serious cardiovascular thrombotic events, MI, and stroke, especially with prolonged use or use of higher doses);
History of ulcer disease;
Severe renal impairment (dosage ↓ recommended);
Severe hepatic impairment (dosage ↓ recommended);
OB: Use at or after 20 wk gestation may cause fetal renal impairment leading to oligohydramnios and, possibly neonatal renal impairment; if treatment is necessary between 20 wk and 30 wk gestation, limit use to the lowest effective dose and shortest duration possible;
Pedi: Children 2 yr (safety and effectiveness not established);
Geri: Appears on Beers list. Older adults are at risk for side effects.

Adv. Reactions/Side Effects ⬆ ⬇

CV: edema, HF, hypertension, MI

Derm: rash, DRUG REACTION WITH EOSINOPHILIA AND SYSTEMIC SYMPTOMS (DRESS), EXFOLIATIVE DERMATITIS, STEVENS-JOHNSON SYNDROME (SJS), TOXIC EPIDERMAL NECROLYSIS (TEN)

EENT: tinnitus, visual disturbances

GI: abdominal pain, diarrhea, dyspepsia, GI BLEEDING, HEPATOTOXICITY, nausea, vomiting, constipation, flatulence

GU: renal failure

Hemat: prolonged bleeding time

MS: muscle weakness

Neuro: dizziness, headache, depression, drowsiness, sleep disturbances, STROKE

Misc: HYPERSENSITIVITY REACTIONS (INCLUDING ANAPHYLAXIS)

Interactions ⬆ ⬇

Drug-drug:

↑risk of bleeding with some cephalosporins, thrombolytic agents, aspirin, clopidogrel, prasugrel, apixaban, dabigatran, rivaroxaban, or warfarin.
↑GI side effects with aspirin, corticosteroids, and other NSAIDs.
May ↓ response to antihypertensives or diuretics.
May ↑ levels and risk of toxicity from lithium.
May ↑ risk of hematologic toxicity from antineoplastics or radiation therapy.
↑risk of nephrotoxicity with cyclosporine or chronic use of acetaminophen.
May ↑ risk of hypoglycemia from insulin or oral hypoglycemic agents.

Drug-Natural Products:

↑anticoagulant effect and bleeding risk with arnica, chamomile, clove, dong quai, feverfew, garlic, ginger, ginkgo, and Panax ginseng.

Route/Dosage ⬆ ⬇

PO (Adults ): 400 mg 3 times daily initially, followed by maintenance dose of 600–1800 mg/day in 3–4 divided doses (not to exceed 2000 mg/day).
PO (Children >2 yr): 20 mg/kg/day in 3–4 divided doses initially, followed by maintenance dose of 15–30 mg/kg/day in 3–4 divided doses.

Availability ⬆ ⬇

(Generic available)

Tablets: 600 mg
Capsules: 400 mg

Assessment ⬆ ⬇

Patients who have asthma, aspirin-induced allergy, and nasal polyps are at ↑ risk for developing hypersensitivity reactions. Monitor for rhinitis, asthma, and urticaria.
Assess pain and range of motion prior to and weekly during therapy.
Assess patient for skin rash frequently during therapy. Discontinue tolmetin at first sign of rash; may be life-threatening. SJS or TEN may develop. Treat symptomatically; may recur once treatment is stopped.
Monitor for signs and symptoms of DRESS (fever, rash, lymphadenopathy, facial swelling, eosinophilia) periodically during therapy. If symptoms occur discontinue tolmetin.

Lab Test Considerations:

Evaluate BUN, serum creatinine, CBC, and liver function periodically in patients receiving prolonged therapy.
- May ↑ serum potassium, BUN, AST, and ALT.
- May ↓ hemoglobin and hematocrit. Bleeding time may be prolonged for up to 2 days after discontinuation.
- May cause false-positive results for urinary protein.

Implementation ⬆ ⬇

Administration in higher than recommended doses does not provide ↑ effectiveness but may cause ↑ side effects. Use lowest effective dose for shortest period of time.
PO: May be administered with food, milk, or antacids to ↓ GI irritation. Tablets may be crushed and capsules opened and mixed with fluids or food.

Patient/Family Teaching ⬆ ⬇

Advise patient to take tolmetin with a full glass of water and to remain in an upright position for 15–30 min after administration.
Instruct patient to take medication as directed. Take missed doses as soon as remembered but not if almost time for the next dose. Do not double doses.
May cause drowsiness or dizziness. Advise patient to avoid driving or other activities requiring alertness until response to medication is known.
Caution patient to avoid the concurrent use of alcohol, aspirin, NSAIDs, acetaminophen, anticoagulants, or other OTC or herbal products without consulting health care professional.
Advise patient to use sunscreen and protective clothing to prevent photosensitivity reactions.
Advise patient to inform health care professional of medication regimen prior to treatment or surgery.
Advise patient to consult health care professional if rash, itching, visual disturbances, tinnitus, weight gain, edema, black stools, persistent headache, or influenza-like syndrome (chills, fever, muscle aches, pain) occurs.
Rep: May cause fetal harm. Advise females of reproductive potential to notify health care professional if pregnancy is planned or suspected and to avoid tolmetin starting at 20 wk gestation due to risk of oligohydramnios and 30 wk gestation because of risk of premature closing of the fetal ductus arteriosus. If NSAIDs are necessary between 20 and 30 wk gestation, limit use to the lowest effective dose and shortest duration possible. Consider ultrasound monitoring of amniotic fluid if NSAID therapy extends beyond 48 hr. Discontinue tolmetin if oligohydramnios occurs and follow up with infant. Advise women to avoid tolmetin in the 3rd trimester of pregnancy (after 29 wk); may cause premature closure of the fetal ductus arteriosus. Use during labor or delivery may delay birth and risk of stillbirth. Advise patient to notify health care professional if breastfeeding.

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Pronunciation ⬇

Classifications ⬆ ⬇

Indications ⬆ ⬇

Action ⬆ ⬇

Pharmacokinetics ⬆ ⬇