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| Active: | ketorolac trometamol 5 mg/mL |
| Inactive: | benzalkonium chloride 0.01% (w/v), disodium edetate 0.1% (w/v), octoxinol 40, sodium chloride and water - purified. |
Chemical Name: (±)-5-benzoyl-2,3-dihydro-1H-pyrrolizine-1-carboxylic acid
compound with 2-amino-2-(hydroxymethyl)-1,3-propanediol (1:1)
Empirical Formula: C19 H24 N2 O6
Molecular Weight: 376.41
CAS No: 74103-07-4 pKa: 3.54
Ketorolac trometamol is a white to off-white crystalline substance, which is a racemic mixture. It may exist in three crystalline forms, all of which are equally soluble in water. Ketorolac trometamol 5mg/mL ophthalmic solution is a clear, colourless to pale yellow, sterile, isotonic aqueous solution.
Ketorolac trometamol is a member of the pyrrolo-pyrolle group of non-steroidal anti-inflammatory drugs for ophthalmic use.
Ketorolac trometamol is a nonsteroidal, anti-inflammatory agent demonstrating analgesic and anti-inflammatory activity. It is believed to inhibit the cyclo-oxygenase enzyme essential for prostaglandin biosynthesis. Ocular administration of ketorolac trometamol reduces prostaglandin E2 levels in the aqueous humour. Ketorolac trometamol given systemically does not cause pupil constriction. Results from clinical studies indicate that ACULAR® eye drops have no significant effect upon intraocular pressure.
Two drops (0.1 mL) of 0.5% ACULAR® eye drops instilled into the eyes of patients 12 hours and 1 hour prior to cataract extraction achieved measurable levels in 8 of 9 patients' eyes (mean ketorolac concentrations 95 nanograms/mL aqueous humour, range 40-170 nanograms/mL). One drop (0.05 mL) of 0.5% ketorolac trometamol solution was instilled into one eye and one drop of the vehicle into the other eye three times a day for 21 days in 26 normal subjects. Only 5 of 26 subjects had detectable amounts of ketorolac in their plasma (range 10.7 to 22.5 nanograms/mL) at Day 10 during topical ocular treatment. When ketorolac is given systemically to relieve pain, plasma levels following chronic systemic use average around 860 nanograms/mL.
ACULAR® eye drops are indicated for the short term (2 - 4 weeks) prophylaxis and reduction in inflammation in patients undergoing cataract extraction.
ACULAR eye drops are also indicated for the short term (2 - 4 weeks) relief of symptoms of seasonal allergic conjunctivitis.
ACULAR® eye drops are contraindicated in patients hypersensitive to any of the components of the medication.
The potential exists for cross sensitivity to acetylsalicylic acid and other nonsteroidal anti-inflammatory medicines. ACULAR® is contraindicated in patients who have previously exhibited sensitivities to these drugs.
ACULAR® eye drops are contraindicated in children.
Patients with bleeding tendencies:
With some nonsteroidal anti-inflammatory drugs a potential exists for
increased bleeding time due to interference with thrombocyte aggregation. There
have been reports that ocularly applied nonsteroidal anti-inflammatory drugs may
cause increased bleeding of ocular tissues (including hyphemas) in conjunction
with ocular surgery. ACULAR® eye drops should be used with care in
patients with known bleeding tendencies, or in patients who are receiving other
medications which may prolong bleeding time, or patients with a known history of
peptic ulceration.
Ability to drive:
As ACULAR® eye drops may cause transient blurring on
instillation, caution is required with the use of hazardous machinery or
driving, which are not recommended unless vision is clear.
Masking of infections:
In common with other anti-inflammatory drugs, ACULAR may mask the usual
signs of infections.
Soft (hydrophobic) contact lens:
ACULAR® eye drops contains benzalkonium chloride as a
preservative, and should not be used in patients continuing to wear soft
(hydrophobic) contact lens.
Use in Pregnancy and Lactation:
Ketorolac trometamol and its metabolites have been shown to pass into the
foetus and milk of animals, and have been detected in human breast milk. Safety
in human pregnancy has not been established. Not recommended in pregnancy or
lactation.
Carcinogenesis, Mutagenesis, Impairment of Fertility:
An 18-month study in mice at oral doses of ketorolac trometamol equal
to the parental Maximum Recommended Human Dose (MRHD) and a 24-month study in
rats at oral doses 2.5 times the parental MRHD showed no evidence of tumours.
Ketorolac trometamol was not mutagenic in the Ames test, unscheduled DNA
synthesis and repair, and in forward mutation assays. Ketorolac did not cause
chromosome breakage in the in vivo mouse micronucleus assay. At 1590
micrograms/mL approximately 1000 times the average human plasma levels, and at
higher concentrations, ketorolac trometamol 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 (53.1
mg/square m) and 16 mg/kg (94.9 mg/square m) respectively.
The most frequent adverse events reported with the use of ACULAR® eye drops are transient burning and stinging on instillation and other minor symptoms of ocular irritation. None of the typical adverse reactions reported with the systemic nonsteroidal anti-inflammatory agents (including systemic ketorolac trometamol) have been observed at the doses used in topical ophthalmic therapy.
ACULAR® eye drops have been safely administered with systemic and ophthalmic medications such as antibiotics, sedatives, beta blockers, carbonic anhydrase inhibitors, miotics, mydriatics, cycloplegics, local anaesthetics, and corticosteroids.
There is no experience of overdosage by the ophthalmic route. If accidentally ingested, fluids should be taken to dilute the effects, if any.
The recommended dose of ACULAR® eye drops for allergic conjunctivitis is one drop (0.25 mg) instilled in the eye four times daily. Treatment may be continued for up to four weeks.
The recommended dose of ACULAR® eye drops for the prophylaxis and treatment of post operative inflammation in patients who have undergone cataract extraction is 1-2 drops (0.25 to 0.5 mg) four times daily, starting 24 hours before surgery and continuing for 2 - 4 weeks.
Discard any unused contents 28 days after opening the bottle.
5, and 10 mL pack sizes in bottles with dropper applicators.
Store below 25 degrees C and protect from light.
Prescription Only Medicine
NAME AND ADDRESS
Allergan New Zealand Ltd
3 - 5 Westfield Place
PO Box 1873
Mt Wellington,
Auckland, New Zealand
DATE OF PREPARATION
December 2002