Apilac is a nonsteroidal anti-inflammatory drug (NSAID) chemically related to indomethacin and tolmetin. Apilac tromethamine is a racemic mixture of [-]S- and [+]R-enantiomeric forms, with the S-form having analgesic activity. Its antiinflammatory effects are believed to be due to inhibition of both cylooxygenase-1 (COX-1) and cylooxygenase-2 (COX-2) which leads to the inhibition of prostaglandin synthesis leading to decreased formation of precursors of prostaglandins and thromboxanes from arachidonic acid. The resultant reduction in prostaglandin synthesis and activity may be at least partially responsible for many of the adverse, as well as the therapeutic, effects of these medications. Analgesia is probably produced via a peripheral action in which blockade of pain impulse generation results from decreased prostaglandin activity. However, inhibition of the synthesis or actions of other substances that sensitize pain receptors to mechanical or chemical stimulation may also contribute to the analgesic effect. In terms of the ophthalmic applications of ketorolac - ocular administration of ketorolac reduces prostaglandin E2 levels in aqueous humor, secondary to inhibition of prostaglandin biosynthesis.
Apilac injections and tablets are used for the short-term management of moderate to severe acute post-operative pain.
Apilac is also used to associated treatment for these conditions: Acute Migraine, Cystoid Macular Edema, Eye Pain, Inflammation, Ocular Itching, Pseudophakic Cystoid Macular Edema, Acute Pericarditis, Acute, moderate Pain, Acute, severe Pain, Chronic aphakic cystoid macular edema, Intraoperative miosis, Postoperative ocular pain
|Other Names||Ketorolac, Kétorolac, Ketorolaco, Ketorolacum, rac-Ketorolac|
>99% of Ketorolac is plasma protein bound.
|Therapeutic Class||Drugs used for Rheumatoid Arthritis, Non-Opioid Analgesics|
|Manufacturer||APC Pharma Ltd|
|Last Updated:||June 23, 2021 at 11:22 am|
Table Of contents
Apilac Tablet is recommended for short-term use only (up to 7 days) and are not recommended for chronic use. 10 mg every 4 to 6 hours as required. Doses exceeding 40 mg/day are not recommended. For patients receiving parenteral Apilac tromethamine, and who are converted to Apilac tromethamine oral tablets, the total combined daily dose should not exceed 90 mg (60 mg for the elderly, renally impaired patients and patients less than 50 kg) and the oral component should not exceed 40 mg on the day the change of formulation is made. Patients should be converted to oral treatment as soon as possible.
Apilac injection may be used as a single or multiple doses, on a regular or when necessary schedule for the management of moderately severe, acute pain that requires analgesia at the opioid level, usually in a postoperative setting. When administering Apilac injection, the IV bolus must be given over no less than 15 seconds. The IM administration should be given slowly and deeply into the muscle. The analgesic effect begins within 30 minutes with maximum effect in 1 to 2 hours after dosing IV or IM. Duration of analgesic effect is usually 4 to 6 hours. Single-Dose Treatment: The following regimen should be limited to single administration use only.
IM Dosing (Adult):
- Patients <65 years of age: One dose of 60 mg.
- Patients >65 years of age, renally impaired and/or less than 50 kg of body weight: One dose of 30 mg.
IV Dosing (Adult):
- Patients <65 years of age: One dose of 30 mg.
- Patients >65 years of age, renally impaired and/or less than 50 kg of body weight: One dose of 15 mg.
IV or IM Dosing (2 to 16 years of age):
- IM Dosing: One dose of 1 mg/kg up to a maximum of 30 mg.
- IV Dosing: One dose of 0.5 mg/kg up to a maximum of 15 mg.
Multiple-Dose Treatment (IV or IM):
- Patients <65 years of age: The recommended dose is 30 mg Apilac injection every 6 hours. The maximum daily dose should not exceed 120 mg. Patients >65 years of age, renally impaired patients and patients less than 50 kg: The recommended dose is 15 mg Apilac injection every 6 hours. The maximum daily dose for these populations should not exceed 60 mg. For breakthrough pain, do not increase the dose or the frequency of Apilac Tromethamine.
- Conversion from Parenteral to Oral Therapy: Apilac tablets may be used either as monotherapy or as follow-on therapy to parenteral Apilac. When Apilac tablets are used as a follow-on therapy to parenteral Apilac, the total combined daily dose of ketorolac (oral + parenteral) should not exceed 120 mg in younger adult patients or 60 mg in elderly patients on the day the change of formulation is made. On subsequent days, oral dosing should not exceed the recommended daily maximum of 40 mg. Apilac IM should be replaced by Apilac tablet as soon as feasible. The total duration of combined parenteral and oral treatment should not exceed 5 days.
Apilac Nasal spray-
- Adults weighing 50 kg or more: 31.5 mg or 2 spray in each nostril every 6 to 8 hours. Your doctor may adjust your dose if needed. However, the dose is not more than 126 mg (a total of 8 sprays) per day.
- Older adults and adults weighing less than 50 kg: 15.75 mg or 1 spray in only one nostril every 6 to 8 hours. However, the dose is usually not more than 63 mg (a total of 4 sprays) per day.
- Children: Use and dose must be determined by your doctor.
Commonly occurring side-effects are nausea, vomiting, gastro intestinal bleeding,melaena, peptic ulcer, pancreatitis, anxiety, drowsiness, dizziness, headache, hallucinations,excessive thirst, inability to concentrate, insomnia, malaise, fatigue, pruritus, urticaria, skin photosensitivity, Lyell's syndrome, Stevens-Johnson syndrome, flushing, bradycardia, hypertension, palpitations, chest pain, infertility in female, dyspnoea, asthma, pulmonary oedema, fever, injection site pain.
Patients over the age of 65 years may be at a greater risk of experiencing adverse events than younger patients. Apilac tromethamine can cause gastro-intestinal irritation, ulcers or bleeding in patients with or without a history of previous symptoms. Bronchospasm may be precipitated in patients with a history of asthma. Since ketorolac tromethamine and its metabolites are excreted primarily by the kidney, patients with moderate to severe impairment of renal function (serum creatinine greater than 160 micromol/l) should not receive. Fluid retention and oedema have been reported with the use of Apilac tromethamine.
Apilac tromethamine should not be used with other NSAIDs or in patients receiving aspirin because of the potential for additive side effects. Care should be taken when administering Apilac tromethamine with anti-coag ulants since co-administration may cause an enhanced anti-coagulant effect. Apilac tromethamine and other non-steroidal anti-inflammatory drugs can reduce the anti hypertensive effect of beta-blockers and may increase the risk of renal impairment when administered concurrently with ACE inhibitors, particularly in volume depleted patients. Caution is advised when methotrexate is administered concurrently, since some prostaglandin synthesis inhibiting drugs have been reported to reduce the clearance of methotrexate, and thus possibly enhance its toxicity. Probenecid should not be administered concurrently with ketorolac tromethamine because of increases in ketorolac plasma level and half-life.
- Take with food. Food reduces GI irritation.
Volume of Distribution
The apparent volume of distribution of ketorolac in healthy human subjects is 0.25 L/kg or less.
Apilac tromethamine is administered as a racemic mixture, therefore the half-life of each enantiomer must be considered. The half life of the S-enantiomer is ~2.5 hours, while the half life of the R-enantiomer is ~5 hours. Based on this data, the S enantiomer is cleared about twice as fast as the R enantiomer.
The plasma clearance of ketorolac is 0.021 to 0.037 L/h/kg. Further, studies have illustrated that clearance of oral, IM and IV doses of ketorolac are comparable which suggests linear kinetics. It should also be noted that clearance in children is about double the clearance found in adults.
Pregnancy & Breastfeeding use
Safety in human pregnancy has not been established. Apilac has been detected in human milk at low levels. Apilac is therefore contraindicated during pregnancy, labour or delivery, or in mothers who are breast feeding.
Apilac Tromethamine is contraindicated in patients with known hypersensitivity to NSAIDs and any of the components of Apilac Tromethamine. Moreover, the patient with the history of asthma, nasal polyp, angioedema, peptic ulcer and bleeding, bleeding disorders are contraindicated for this drug.
Symptoms: Abdominal pain, nausea, vomiting, hyperventilation, peptic ulceration, erosive gastritis and renal dysfunction.
Management: Symptomatic and supportive treatment. Consider gastric lavage or admin of activated charcoal within 1 hr of ingestion.
Tablet & injection should be store in a cool & dry place, protect from light & moisture.