Toradol Information
Toradol (Ketorolac tromethamine) Description
Toradol (Ketorolac tromethamine) is a member of the pyrrolo-pyrrole group of nonsteroidal anti-inflammatory drugs (NSAIDs). The chemical name for ketorolac tromethamine is (±)-5-benzoyl-2,3-dihydro-1-pyrrolizine-1-carboxylic acid, compound with 2-amino-2-(hydroxymethyl)-1,3-propanediol (1:1), and the chemical structure is:
Ketorolac tromethamine is a racemic mixture of [-]S and [+]R ketorolac tromethamine. Ketorolac tromethamine may exist in three crystal forms. All forms are equally soluble in water. Ketorolac tromethamine has a pKa of 3.5 and an n-octanol/water partition coefficient of 0.26. The molecular weight of ketorolac tromethamine is 376.41. Its molecular formula is CHNO.
Toradol (Ketorolac tromethamine) is available as round, white, film-coated, red-printed tablets. Each tablet contains 10 mg ketorolac tromethamine, the active ingredient, with added lactose, magnesium stearate and microcrystalline cellulose. The white film-coating contains hydroxypropyl methylcellulose, polyethylene glycol and titanium dioxide.
Thetablets are printed with red ink that includes FD&C Red #40 Aluminum Lake as the colorant. There is a large T printed on both sides of the tablet, as well as the word Toradol (Ketorolac tromethamine) on one side, and the word ROCHE on the other.
Toradol (Ketorolac tromethamine) Clinical Pharmacology
Ketorolac tromethamine is a nonsteroidal anti-inflammatory drug (NSAID) that exhibits analgesic activity in animal models. The mechanism of action of ketorolac, like that of other NSAIDs, is not completely understood but may be related to prostaglandin synthetase inhibition. The biological activity of ketorolac tromethamine is associated with the S-form. Ketorolac tromethamine possesses no sedative or anxiolytic properties.
The peak analgesic effect of Toradol (Ketorolac tromethamine) occurs within 2 to 3 hours and is not statistically significantly different over the recommended dosage range of Toradol (Ketorolac tromethamine) . The greatest difference between large and small doses of Toradol (Ketorolac tromethamine) is in the duration of analgesia.
Toradol (Ketorolac tromethamine) Indications And Usage
Carefully consider the potential benefits and risks of Toradol (Ketorolac tromethamine) and other treatment options before deciding to use Toradol (Ketorolac tromethamine) . Use the lowest effective dose for the shortest duration consistent with individual patient treatment goals.
Toradol (Ketorolac tromethamine) Contraindications
Toradol (Ketorolac tromethamine) is contraindicated in patients with previously demonstrated hypersensitivity to ketorolac tromethamine.
Toradol (Ketorolac tromethamine) is contraindicated in patients with active peptic ulcer disease, in patients with recent gastrointestinal bleeding or perforation and in patients with a history of peptic ulcer disease or gastrointestinal bleeding.
Toradol (Ketorolac tromethamine) should not be given to patients who have experienced asthma, urticaria, or allergic-type reactions after taking aspirin or other NSAIDs. Severe, rarely fatal, anaphylactic-like reactions to NSAIDs have been reported in such patients (see , and ).
Toradol (Ketorolac tromethamine) is contraindicated as prophylactic analgesic before any major surgery.
Toradol (Ketorolac tromethamine) is contraindicated for the treatment of peri-operative pain in the setting of coronary artery bypass graft (CABG) surgery (see ).
Toradol (Ketorolac tromethamine) is contraindicated in patients with advanced renal impairment or in patients at risk for renal failure due to volume depletion (see for correction of volume depletion).
Toradol (Ketorolac tromethamine) is contraindicated in labor and delivery because, through its prostaglandin synthesis inhibitory effect, it may adversely affect fetal circulation and inhibit uterine contractions, thus increasing the risk of uterine hemorrhage.
The use of Toradol (Ketorolac tromethamine) is contraindicated in nursing mothers because of the potential adverse effects of prostaglandin-inhibiting drugs on neonates.
Toradol (Ketorolac tromethamine) inhibits platelet function and is, therefore, contraindicated in patients with suspected or confirmed cerebrovascular bleeding, hemorrhagic diathesis, incomplete hemostasis and those at high risk of bleeding (see and ).
Toradol (Ketorolac tromethamine) is contraindicated in patients currently receiving aspirin or NSAIDs because of the cumulative risks of inducing serious NSAID-related adverse events.
The concomitant use of Toradol (Ketorolac tromethamine) and probenecid is contraindicated.
The concomitant use of ketorolac tromethamine and pentoxifylline is contraindicated.
Toradol (Ketorolac tromethamine) Warnings
The total combined duration of use of Toradol (Ketorolac tromethamine) and IV or IM dosing of ketorolac tromethamine is not to exceed 5 days in adults. Toradol (Ketorolac tromethamine) is not indicated for use in pediatric patients.
The most serious risks associated with Toradol (Ketorolac tromethamine) are:
Toradol (Ketorolac tromethamine) Precautions
Toradol (Ketorolac tromethamine) cannot be expected to substitute for corticosteroids or to treat corticosteroid insufficiency. Abrupt discontinuation of corticosteroids may lead to disease exacerbation. Patients on prolonged corticosteroid therapy should have their therapy tapered slowly if a decision is made to discontinue corticosteroids.
The pharmacological activity of Toradol (Ketorolac tromethamine) in reducing inflammation may diminish the utility of this diagnostic sign in detecting complications of presumed noninfectious, painful conditions.
Toradol (Ketorolac tromethamine) is a potent NSAID and may cause serious side effects such as gastrointestinal bleeding or kidney failure, which may result in hospitalization and even fatal outcome.
Physicians, when prescribing Toradol (Ketorolac tromethamine) , should inform their patients or their guardians of the potential risks of Toradol (Ketorolac tromethamine) treatment (see , , , and sections), instruct patients to seek medical advice if they develop treatment-related adverse events, and
Remember that the total combined duration of use of Toradol (Ketorolac tromethamine) and IV or IM dosing of ketorolac tromethamine is not to exceed 5 days in adults. Toradol (Ketorolac tromethamine) is not indicated for use in pediatric patients.
Patients should be informed of the following information before initiating therapy with an NSAID and periodically during the course of ongoing therapy. Patients should also be encouraged to read the NSAID Medication Guide that accompanies each prescription dispensed.
An 18-month study in mice with oral doses of ketorolac tromethamine at 2 mg/kg/day (0.9 times the human systemic exposure at the recommended IM or IV dose of 30 mg qid, based on area-under-the-plasma-concentration curve [AUC]), and a 24-month study in rats at 5 mg/kg/day (0.5 times the human AUC) showed no evidence of tumorigenicity.
Ketorolac tromethamine was not mutagenic in the Ames test, unscheduled DNA synthesis and repair, and in forward mutation assays. Ketorolac tromethamine did not cause chromosome breakage in the in vivo mouse micronucleus assay. At 1590 µg/mL and at higher concentrations, ketorolac tromethamine increased the incidence of chromosomal aberrations in Chinese hamster ovarian cells.
Impairment of fertility did not occur in male or female rats at oral doses of 9 mg/kg (0.9 times the human AUC) and 16 mg/kg (1.6 times the human AUC) of ketorolac tromethamine, respectively.
Because ketorolac tromethamine may be cleared more slowly by the elderly (see ) who are also more sensitive to the dose-related adverse effects of NSAIDs (see ), extreme caution, reduced dosages (see ), and careful clinical monitoring must be used when treating the elderly with Toradol (Ketorolac tromethamine) .
Toradol (Ketorolac tromethamine) Adverse Reactions
Adverse reaction rates increase with higher doses of Toradol (Ketorolac tromethamine) . Practitioners should be alert for the severe complications of treatment with Toradol (Ketorolac tromethamine) , such as GI ulceration, bleeding and perforation, postoperative bleeding, acute renal failure, anaphylactic and anaphylactoid reactions and liver failure (see , , , and ). These NSAID-related complications can be serious in certain patients for whom Toradol (Ketorolac tromethamine) is indicated, especially when the drug is used inappropriately.
In patients taking Toradol (Ketorolac tromethamine) or other NSAIDs in clinical trials, the most frequently reported adverse experiences in approximately 1% to 10% of patients are:
Additional adverse experiences reported occasionally (
Other rarely observed reactions (reported from postmarketing experience in patients taking Toradol (Ketorolac tromethamine) or other NSAIDs) are:
Toradol (Ketorolac tromethamine) Symptoms And Signs
Symptoms following acute NSAID overdoses are usually limited to lethargy, drowsiness, nausea, vomiting, and epigastric pain, which are generally reversible with supportive care. Gastrointestinal bleeding can occur. Hypertension, acute renal failure, respiratory depression and coma may occur, but are rare. Anaphylactoid reactions have been reported with therapeutic ingestion of NSAIDs, and may occur following an overdose.
Toradol (Ketorolac tromethamine) Treatment
Patients should be managed by symptomatic and supportive care following a NSAIDs overdose. There are no specific antidotes. Emesis and/or activated charcoal (60 g to 100 g in adults, 1 g/kg to 2 g/kg in children) and/or osmotic cathartic may be indicated in patients seen within 4 hours of ingestion with symptoms or following a large oral overdose (5 to 10 times the usual dose). Forced diuresis, alkalization of urine, hemodialysis or hemoperfusion may not be useful due to high protein binding.
Single overdoses of Toradol (Ketorolac tromethamine) have been variously associated with abdominal pain, nausea, vomiting, hyperventilation, peptic ulcers and/or erosive gastritis and renal dysfunction which have resolved after discontinuation of dosing.
Toradol (Ketorolac tromethamine) Dosage And Administration
Patients age 17 to 64: 20 mg PO once followed by 10 mg q4-6 hours prn
Patients age ≥65, renally impaired, and/or weight
Do of 4 to 6 hours
The following table summarizes Toradol (Ketorolac tromethamine) dosing instructions in terms of age group:
Toradol (Ketorolac tromethamine) How Supplied
Toradol (Ketorolac tromethamine)
