Acular
(KETOROLAC TROMETHAMINE 0.5%)

Drug Effects

Synonyms(It is also Known As)


ketorolac tromethamine.

Chemical Structure


Chemical Formula


C15H13NO3 .

Iupac Name


(±)-5-benzoyl-2,3-dihydro-
1H-pyrrolizine-1-carboxylic acid,
2-amino-2-(hydroxymethyl)-1,3-propanediol.

Usage


Ketorolac is used to relieve moderately severe pain, usually after surgery. Ketorolac is in a class of medications called NSAIDs. It works by stopping the body's production of a substance that causes pain, fever, and inflammation.

Adverse Effect


  • Upset stomach, nausea, vomiting, constipation, diarrhea, gas, dizziness, or drowsiness may occur. If any of these effects persist or worsen, tell your doctor or pharmacist promptly.
  • Remember that your doctor has prescribed this medication because he or she has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.
  • Tell your doctor immediately if any of these unlikely but serious side effects occur:fainting, fast/pounding heartbeat, hearing changes (such as ringing in the ears), mental/mood changes (such as confusion, depression), persistent/severeheadache, stomach pain, sudden/unexplained weight gain, swelling of the hands orfeet, vision changes (such as blurred vision), unusual tiredness.
  • Tell your doctor immediately if any of these rare but serious side effects occur: easy bruising/bleeding, change in amount of urine, signs of infection (such as fever, chills, persistent sore throat), symptoms of meningitis (such as unexplained stiff neck, fever).
  • This drug may rarely cause serious (possibly fatal) liver disease. Seek immediate medical attention if you have any symptoms of liver damage, including: dark urine, stomach/abdominal pain, persistent nausea/vomiting, yellowing eyes/skin.
  • A very serious allergic reaction to this drug is rare. However, seek immediate medical attention if you notice any symptoms of a serious allergic reaction, including: rash,itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.

 

Mechanism Action


The primary mechanism of action responsible for ketorolac's anti-inflammatory, antipyretic and analgesic effects is the inhibition of prostaglandin synthesis by competitive blocking of the enzyme cyclooxygenase (COX). Ketorolac is a non selective COX inhibitor.

Precaution


  • Before taking ketorolac, tell your doctor or pharmacist if you are allergic to it; or to aspirin or other nonsteroidal anti-inflammatory drugs-NSAIDs (such as ibuprofen,naproxen, celecoxib); or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.
  • Before taking this medication, tell your doctor or pharmacist your medical history, especially of: asthma (including a history of worsening breathing after taking aspirin or other NSAIDs), bleeding or clotting problems, blood disorders (such as anemia), heart disease (such as previous heart attack), high blood pressure, liver disease, growths in the nose (nasal polyps), throat/stomach/intestinal problems (such as bleeding, heartburn, ulcers), stroke, swelling of the ankles/feet/hands.
  • Kidney problems can sometimes occur with the use of NSAID medications, including ketorolac. Problems are more likely to occur if you are dehydrated, have heart failure or kidney disease, are an older adult, or if you take certain medications (see also Drug Interactions section). Drink plenty of fluids as directed by your doctor to prevent dehydration and tell your doctor right away if you have any unusual change in the amount of urine.
  • This drug may make you dizzy or drowsy. Do not drive, use machinery, or do any activity that requires alertness until you are sure you can perform such activities safely. Avoid alcoholic beverages.
  • This medicine may cause stomach/intestinal bleeding. Daily use of alcohol and tobacco, especially when combined with this medicine, may increase your risk for stomach bleeding. Limit alcohol and stop smoking. Consult your doctor or pharmacist for more information.
  • This medication may infrequently make you more sensitive to the sun. Avoid prolonged sun exposure, tanning booths, and sunlamps. Use a sunscreen and wear protective clothing when outdoors.

 

Drug Interaction


  • The effects of some drugs can change if you take other drugs or herbal products at the same time. This can increase your risk for serious side effects or may cause your medications not to work correctly. These drug interactions are possible, but do not always occur. Your doctor or pharmacist can often prevent or manage interactions by changing how you use your medications or by close monitoring.
  • To help your doctor and pharmacist give you the best care, be sure to tell your doctor and pharmacist about all the products you use (including prescription drugs, nonprescription drugs, and herbal products) before starting treatment with this product. While using this product, do not start, stop, or change the dosage of any other medicines you are using without your doctor's approval.
  • Some products that may interact with this drug include: aliskiren, ACE inhibitors (such as captopril, lisinopril), angiotensin II receptor blockers (such as losartan, valsartan), methotrexate, probenecid, corticosteroids (such as prednisone), other medications that may affect the kidneys (including cidofovir, cyclosporine, tenofovir, "water pills"/diuretics such as furosemide, hydrochlorothiazide, triamterene).
  • This medication may increase the risk of bleeding when taken with other drugs that also may cause bleeding. Examples include anti-platelet drugs such as clopidogrel, "blood thinners" such as dabigatran/enoxaparin/warfarin, among others.
  • This medication can slow down the removal of other medications from your body, which may affect how they work. Examples of affected drugs include lithium, pemetrexed, among others.
  • Check all prescription and nonprescription medicine labels carefully since many medications contain pain relievers/fever reducers (aspirin, NSAIDs such as ibuprofen or naproxen). These drugs are similar to ketorolac and may increase your risk of side effects if taken together. However, if your doctor has directed you to take low-dose aspirin to prevent heart attack or stroke (usually at dosages of 81-325 milligrams a day), you should continue taking the aspirin unless your doctor instructs you otherwise. Ask your doctor or pharmacist for more details.

 

Pregnancy Category


Pregnancy Category C-  Animal reproduction studies have shown an adverse effect on the fetus and there are no adequate and well-controlled studies in humans, but potential benefits may warrant use of the drug in pregnant women despite potential risks.

Absorption


  • Bioavailability: 80-100%
  • Onset: IM: 10 min; PO: 30-60 min
  • Duration: 6-8 hr
  • Peak Plasma Time: IV: 1-3 min; IM: 30-60 min; PO: ~1 hr
  • Peak Plasma Concentration: varies with dose & route

 

Distribution


  • Protein Bound: >99%
  • Vd: 0.11-0.33 L/kg

 

Metabolism


Liver .p-hydroxyketorolac & unidentified polar metabolites

Elemination


Urine (91%); feces (6%).

References


  1. http://www.fundinguniverse.com/company-histories/roche-bioscience-history/
  2. http://www.drugs.com/mtm/ketorolac.html
  3. http://www.drugs.com/mtm/ketorolac-ophthalmic.html
  4.  http://www.drugs.com/sprix.html
  5. "Ketorolac-tromethamine". The American Society of Health-System Pharmacists. Retrieved 3 April 2011. .
  6. MHRA Drug Safety Update October 2007, Volume 1, Issue 3, pp 3-4.
  7. Committee on the Safety of Medicines, Medicines Control Agency: Ketorolac: new restrictions on dose and duration of treatment. Current Problems in Pharmacovigilance: June 1993; Volume 19 (pages 5-8).
  8. Strom BL et al. Parenteral Ketorolac and risk of gastrointestinal and operative site bleeding: a postmarketing surveillance study JAMA 1996; 275:376-82.
  9. Martindale, The Complete Drug Reference, 35th Edition, 2007