ketorolac

Absorption: Rapidly and completely absorbed following all routes of administration.

Distribution: Well distributed to tissues.

Protein Binding: 99%.

Metabolism/Excretion: Primarily metabolized by the liver. Primarily by the kidneys (92%); 6% excreted in feces.

Half-Life: 4.5 hr (range 3.8–6.3 hr; ↑ in geriatric patients and patients with impaired renal function).

Time/Action Profile ⬆ ⬇

(analgesic effects)

ROUTE	ONSET	PEAK	DURATION
PO	unknown	2–3 hr	4–6 hr or longer
IM, IV	10 min	1–2 hr	6 hr or longer
IN	unknown	unknown	6–8 hr or longer

Contraind./Precautions ⬆ ⬇

Contraindicated in:

Hypersensitivity;
Cross-sensitivity with other NSAIDs may exist;
Preoperative use;
Active or history of peptic ulcer disease or GI bleeding;
Known alcohol intolerance (injection only);
Coronary artery bypass graft surgery;
Cerebrovascular bleeding;
Advanced renal impairment or at risk for renal failure due to volume depletion;
Concurrent use of pentoxifylline or probenecid;
OB: Avoid use of after 30 wk gestation; may inhibit labor and maternal bleeding at delivery.

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); avoid use in patients with recent MI or HF;
HF;
Coagulation disorders;
Mild-to-moderate renal impairment (↓ dose may be required);
Hepatic impairment;
OB: Use at or after 20 wk gestation may cause fetal or 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;
Lactation: Use while breastfeeding only if potential maternal benefit justifies potential risk to infant;
Pedi: Safety and effectiveness not established in neonates;
Geri: Appears on Beers list. risk GI bleeding or peptic ulcer disease in older adults. Avoid chronic use unless other alternatives are not effective and the patient can take a gastroprotective agent; avoid short-term use in combination with oral or parenteral corticosteroids, anticoagulants, or antiplatelet agents unless other alternatives are not effective and the patient can take a gastroprotective agent.

Adv. Reactions/Side Effects ⬆ ⬇

CV: edema, HF, MI

Derm: DRUG REACTION WITH EOSINOPHILIA AND SYSTEMIC SYMPTOMS (DRESS), EXFOLIATIVE DERMATITIS, pruritus, purpura, STEVENS-JOHNSON SYNDROME, sweating, TOXIC EPIDERMAL NECROLYSIS, urticaria

EENT: ↑lacrimation (spray), nasal discomfort (spray), throat irritation (spray)

F and E: hyperkalemia

GI: ↑liver enzymes, abdominal pain, abnormal taste, diarrhea, dry mouth, dyspepsia, GI BLEEDING, nausea

GU: oliguria, renal toxicity, urinary frequency

Hemat: prolonged bleeding time

Local: injection site pain

Neuro: drowsiness, abnormal thinking, dizziness, euphoria, headache, paresthesia, STROKE

Resp: asthma, dyspnea

Misc: HYPERSENSITIVITY REACTIONS (INCLUDING ANAPHYLAXIS)

Interactions ⬆ ⬇

Drug-drug:

Probenecid↑ levels and the risk of adverse reactions; concurrent use is contraindicated.
↑risk of bleeding when used with pentoxifylline; concurrent use is contraindicated.
Concurrent use with aspirin may ↓ effectiveness.
↑adverse GI effects with aspirin, other NSAIDs, potassium supplements, corticosteroids, or alcohol.
May ↓ effectiveness of diuretics or antihypertensives.
May ↑ serum lithium levels and ↑ risk of toxicity.
↑risk of toxicity from methotrexate.
↑risk of bleeding with anticoagulants, aspirin, clopidogrel, ticagrelor, prasugrel, corticosteroids, fibrinolytics, SNRIs, or SSRIs.
↑risk of adverse hematologic reactions with antineoplastics or radiation therapy.
May ↑ risk of nephrotoxicity from cyclosporine.

Drug-Natural Products:

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

Route/Dosage ⬆ ⬇

Oral therapy is indicated only as a continuation of parenteral therapy. Total duration of therapy by all routes should not exceed 5 days
PO (Adults <65 yr): 20 mg initially, followed by 10 mg every 4–6 hr (not to exceed 40 mg/day).
PO (Adults ≥65 yr, <50 kg, or with renal impairment): 10 mg every 4–6 hr (not to exceed 40 mg/day).
PO (Children 2–16 yr, <50 kg): 1 mg/kg as a single dose. No data available for multiple doses.
IM (Adults <65 yr): Single dose: 60 mg. Multiple dosing: 30 mg every 6 hr (not to exceed 120 mg/day).
IM (Adults ≥65 yr, <50 kg, or with renal impairment): Single dose: 30 mg. Multiple dosing: 15 mg every 6 hr (not to exceed 60 mg/day).
IM (Children 2–16 yr, <50 kg): Single dose: 0.4–1 mg/kg (maximum: 30 mg/dose). Multiple dosing: 0.5 mg/kg every 6 hr.
IV (Adults <65 yr): Single dose: 30 mg. Multiple dosing: 30 mg every 6 hr (not to exceed 120 mg/day).
IV (Adults ≥65 yr, <50 kg, or with renal impairment): Single dose: 15 mg. Multiple dosing: 15 mg every 6 hr (not to exceed 60 mg/day).
IV (Children 2–16 yr, <50 kg): Single dose: 0.4–1 mg/kg (maximum: 15 mg/dose). Multiple dosing: 0.5 mg/kg every 6 hr.
(Adults <65 yr): 1 spray in each nostril every 6–8 hr (not to exceed 4 sprays in each nostril/day).
(Adults ≥65 yr, <50 kg, or with renal impairment): 1 spray in only one nostril every 6–8 hr (not to exceed 4 sprays in one nostril/day).

Availability ⬆ ⬇

(Generic available)

Tablets: 10 mg
Nasal spray (Sprix): 15.75 mg/spray in 1.7-g bottle (delivers 8 sprays)
Solution for injection: 15 mg/mL; 30 mg/mL

Assessment ⬆ ⬇

Assess pain (note type, location, and intensity) prior to and 1–2 hr following administration.
Patients who have asthma, aspirin-induced allergy, and nasal polyps are at increased risk for developing hypersensitivity reactions. Assess for rhinitis, asthma, and urticaria.
Assess for rash periodically during therapy. May cause Stevens-Johnson syndrome or toxic epidermal necrolysis. Discontinue therapy if severe or if accompanied with fever, general malaise, fatigue, muscle or joint aches, blisters, oral lesions, conjunctivitis, hepatitis, and/or eosinophilia.
Monitor BP during initiation and periodically during therapy. May cause fluid retention and edema leading to new onset or worsening hypertension.
Monitor for signs and symptoms of DRESS (fever, rash, lymphadenopathy, facial swelling) periodically during therapy. Discontinue therapy if symptoms occur.

Lab Test Considerations:

Evaluate liver function tests, especially AST and ALT, periodically in patients receiving prolonged therapy. May cause ↑ levels.
- May cause prolonged bleeding time that may persist for 24–48 hr following discontinuation of therapy.
- May cause ↑ BUN, serum creatinine, or potassium concentrations.

Implementation ⬆ ⬇

Do not confuse ketorolac with Ketalar, ketamine, or methadone.
- Administration in higher-than-recommended doses does not provide increased effectiveness but may cause increased side effects. Duration of ketorolac therapy, by all routes combined, should not exceed 5 days. Use lowest effective dose for shortest period of time to minimize risk of cardiovascular thrombotic events.
- Coadministration with opioid analgesics may have additive analgesic effects and may permit lower opioid doses.
- Avoid concurrent administration with other NSAIDs.
PO: Ketorolac therapy should always be given initially by the IM or IV route. Use oral therapy only as a continuation of parenteral therapy.
Activate pump before first use by holding bottle arm’s length away with index finger and middle finger resting on top of finger flange and thumb supporting base. Press down evenly and release pump 5 times to activate. Prior to each use, blow nose gently to clear nostrils. Sit up straight or stand. Tilt head slightly forward. Insert tip of container into nostril. Point container away from center of nose. Push down to spray. Bottles are for 24 hr use; discard bottle no more than 24 hr after taking first dose, even if the bottle still contains some liquid.

IV Administration:

Administer undiluted. Concentration: 15–30 mg/mL.
Rate: Administer over at least 15 sec.

Patient/Family Teaching ⬆ ⬇

Instruct patient on how and when to ask for and take pain medication. Advise patient to read Medication Guide and Instructions for Use before starting and with each Rx refill in case of changes.
Instruct patient to take medication exactly as directed. Take missed doses as soon as remembered if not almost time for next dose. Do not double doses. Do not take more than prescribed or for longer than 5 days.
- May cause drowsiness or dizziness. Advise patient to avoid driving or other activities requiring alertness until response to the medication is known.
- Instruct patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and consult health care professional before taking any new medications.
- Caution patient to avoid the concurrent use of alcohol, aspirin, NSAIDs, acetaminophen, or other OTC medications without consulting health care professional.
- 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.
- May cause fetal harm. Advise females of reproductive potential to notify health care professional if pregnancy is planned or suspected or if breastfeeding. Advise women to avoid ketorolac in the 3rd trimester of pregnancy (after 29 wk), may cause premature closure of the fetal ductus arteriosus. Use of ketorolac after 20 wk may cause fetal renal dysfunction leading to oligohydramnios. Avoid use of ketorolac in labor and delivery; may adversely affect fetal circulation and inhibit uterine contractions. The risk of uterine hemorrhage may be increased. May cause reversible infertility in women attempting to conceive; may consider discontinuing ketorolac.
Instruct patient on correct technique for administration, need to open a new bottle every 24 hr, and the 5-day limit for use.

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Pronunciation ⬇

Classifications ⬆ ⬇

Indications ⬆ ⬇

Action ⬆ ⬇

Pharmacokinetics ⬆ ⬇