ketorolac tromethamine

Acular, Acular LS, Apo-Ketorolac (CA)

Pharmacologic class: Nonsteroidal anti-inflammatory drug (NSAID)

Therapeutic class: Analgesic, antipyretic, anti-inflammatory

Pregnancy risk category C (first and second trimesters), D (third trimester)

FDA Box Warning

• Drug is indicated for short-term management (up to 5 days in adults) of moderately severe acute pain that requires opioid-level analgesia. It's not indicated for minor or chronic painful conditions. Drug carries many risks; NSAID-related adverse events can be serious in certain patients, especially when used inappropriately. Raising dosage beyond recommendations increases risk of serious adverse events and won't provide better efficacy.

• Drug can cause peptic ulcers, GI bleeding, and perforation and is contraindicated in patients with active peptic ulcer disease, recent GI bleeding or perforation, or history of peptic ulcer disease or GI bleeding.

• Drug is contraindicated in advanced renal impairment and patients at risk for renal failure.

• Drug inhibits platelet function and is contraindicated in patients with suspected or confirmed cerebrovascular bleeding, hemorrhagic diathesis, incomplete hemostasis, or high risk of bleeding.

• Drug is contraindicated as prophylactic analgesic before major surgery, and intraoperatively when hemostasis is critical.

• Hypersensitivity reactions ranging from bronchospasm to anaphylactic shock have occurred. Ensure that appropriate counteractive measures are available when giving first dose of injection form. Drug is contraindicated in known hypersensitivity to ketorolac or allergic reaction to aspirin or other NSAID.

• Drug is contraindicated for intrathecal or epidural administration (due to alcohol content), during labor and delivery (may impede fetal circulation and inhibit uterine contractions), in breastfeeding women (due to potential adverse effects of prostaglandin-inhibiting drugs on neonates), and in patients currently receiving aspirin or NSAIDs (due to cumulative risk of serious NSAID-related adverse effects).

• Tablet form is indicated only as continuation therapy to injection form, and combined duration of use of both forms mustn't exceed 5 days.

• For tablets, recommended total daily dose (maximum 40 mg) is significantly lower than for injection (maximum 120 mg).

• Adjust dosage in patients age 65 and older, those weighing less than 50 kg (110 lb), and those with moderately elevated serum creatinine level. With injection form, don't exceed 60 mg (total daily dose) in these patients. Injection form is indicated as single-dose therapy in pediatric patients, not to exceed 30 mg for I.M. use or 15 mg for I.V. use.

Action

Interferes with prostaglandin biosynthesis by inhibiting cyclooxygenase pathway of arachidonic acid metabolism; also acts as potent inhibitor of platelet aggregation

Availability

Injection: 15 mg/ml in 1-ml preloaded syringes, 30 mg/ml in 1- and 2-ml preloaded syringes

Ophthalmic solution: 0.4%, 0.5%

Tablets: 10 mg

Indications and dosages

➣ Moderately severe acute pain

Adults younger than age 65: Initially, 30 mg I.V. or 60 mg I.M. as a single dose, or 30 mg I.M. or I.V. q 6 hours, not to exceed 120 mg/day. To switch to P.O. therapy, give 20 mg P.O. initially for patients who received single 30-mg I.V. or 60-mg I.M. dose, followed by 10 mg P.O. q 4 to 6 hours as needed (not to exceed 40 mg/day or 5 days).

Children ages 2 to 16: 1 mg/kg I.M. as a single dose, to a maximum of 30 mg; or one dose of 0.5 mg/kg I.V., to a maximum of 15 mg

➣ Ocular itching caused by seasonal allergic conjunctivitis

Adults and children ages 3 and older: One drop of 0.5% ophthalmic solution (Acular) instilled into affected eye q.i.d.

➣ Postoperative ocular inflammation related to cataract extraction

Adults and children ages 3 and older: One drop of 0.5% ophthalmic solution (Acular) instilled into operative eye q.i.d., starting 24 hours after surgery and continuing for 2 weeks

➣ To reduce ocular pain, burning, or stinging after corneal refractive surgery

Adults and children ages 3 and older: One drop of 0.4% ophthalmic solution (Acular LS) instilled into operative eye q.i.d. for up to 4 days

Dosage adjustment

• Mild to moderate renal impairment

• Elderly patients

• Patients weighing less than 50 kg

Contraindications

• Hypersensitivity to drug, its components, aspirin, or other NSAIDs

• Concurrent use of aspirin, other NSAIDs, or probenecid

• Peptic ulcer disease

• GI bleeding or perforation

• Advanced renal impairment, risk of renal failure

• Increased risk of bleeding, suspected or confirmed cerebrovascular bleeding, hemorrhagic diathesis, incomplete hemostasis

• Prophylactic use before major surgery, intraoperative use when hemostasis is critical

• Labor and delivery

• Breastfeeding

Precautions

Use cautiously in:

• mild to moderate renal impairment, cardiovascular disease

• elderly patients

• pregnant patients

• children.

Administration

• Be aware that oral therapy is indicated only as continuation of parenteral therapy.

See Know that parenteral therapy shouldn't exceed 20 doses in 5 days.

• For I.V. use, dilute with normal saline solution, dextrose 5% in water, dextrose 5% and normal saline solution, Ringer's solution, or lactated Ringer's solution.

• Administer single I.V. bolus over 1 to 2 minutes.

• Inject I.M. dose slowly and deeply.

• Don't give by epidural or intrathecal injection.

Adverse reactions

CNS: drowsiness, headache, dizziness

CV: hypertension

EENT: tinnitus

GI: nausea, vomiting, diarrhea, constipation, flatulence, dyspepsia, epigastric pain, stomatitis

Hematologic: thrombocytopenia

Skin: rash, pruritus, diaphoresis

Other: excessive thirst, edema, injection site pain

Interactions

Drug-drug. Angiotensin-converting enzyme inhibitors, beta-adrenergic blockers: decreased antihypertensive effect

Anticoagulants: prolonged prothrombin time

Aspirin: altered ketorolac distribution, metabolism, and excretion; increased risk of serious adverse reactions

Cholestyramine: decreased ketorolac absorption

Corticosteroids, other NSAIDs: additive adverse GI effects

Diuretics: decreased diuretic effect

Hydantoins, lithium: increased blood levels and greater risk of toxicity of these drugs

Methotrexate: increased risk of methotrexate toxicity

Probenecid: increased risk of ketorolac toxicity

Drug-diagnostic tests. Bleeding time: prolonged for 24 to 48 hours after therapy ends

Drug-herbs. Anise, arnica, chamomile, clove, dong quai, feverfew, garlic, ginger, ginkgo, ginseng: increased risk of bleeding

Patient monitoring

• Monitor for adverse reactions, especially prolonged bleeding time and CNS reactions.

• Check I.M. injection site for hematoma and bleeding.

• Monitor fluid intake and output.

Patient teaching

• Inform patient that drug is meant only for short-term pain management.

See Tell patient to immediately report bleeding and adverse CNS reactions.

• Advise patient to minimize GI upset by eating small, frequent servings of healthy foods.

• Instruct patient to avoid aspirin products and herbs during therapy.

• Teach patient how to use eye drops, if prescribed.

• Caution female patient not to take drug if she is breastfeeding.

• Advise patient to avoid driving and other hazardous activities until he knows how drug affects concentration and alertness.

• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs, tests, and herbs mentioned above.

l