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Ketorolac

Generality

Ketorolac is a non-steroidal anti-inflammatory drug (NSAID) used to reduce inflammation and pain of a different nature.

It is available in different pharmaceutical formulations, suitable for oral, ocular and parenteral administration.

From the chemical point of view, ketorolac is a derivative of acetic acid.

Ketorolac - Chemical Structure

Examples of medicinal specialties containing Ketorolac

  • Acular ®
  • Lixidol ®
  • Toradol ®
  • Onidra ® (in association with phenylephrine).

Indications

For what it uses

The use of ketorolac is indicated for the short-term treatment of:

  • Moderate to severe post-surgical pain (oral and parenteral administration);
  • Prophylaxis and reduction of ocular inflammation following cataract surgery in adult patients (ocular administration).

Warnings

Ketorolac is a pain medication which should only be administered under strict medical supervision and should not be used to treat mild or chronic pain .

Before starting treatment with ketorolac orally or parenterally, you must inform your doctor if you are in one of the following situations:

  • If you suffer - or have suffered in the past - from gastrointestinal diseases, including ulcerative colitis and Crohn's disease;
  • If you are allergic to other NSAIDs;
  • If you have a history of angioedema, bronchospasm, asthma and / or nasal polyps;
  • If you suffer from cardiovascular diseases (hypertension, heart failure, peripheral arterial disease, chronic ischemic heart disease or cerebral vasculopathy);
  • If you have diabetes;
  • If you suffer from hypercholesterolemia or hypertriglyceridemia;
  • If you suffer from liver and / or kidney disease, as the drug should be used very carefully in this category of patients;
  • If you have a smoking habit;
  • If you are planning a pregnancy, as ketorolac may adversely affect female fertility.

Instead, before starting an ocular ketorolac therapy, you must inform your doctor if:

  • One suffers - or has suffered in the past - from eye infections;
  • You suffer - or have suffered in the past - from asthma after taking NSAIDs;
  • You suffer from rheumatoid arthritis;
  • You suffer from diabetes;
  • One suffers - or has suffered in the past - from dry eye syndrome;
  • If you have recently undergone eye surgery;
  • If the cornea is damaged.

Furthermore, ketorolac can cause undesirable effects that can alter the ability to drive and / or use machinery, so great care should be taken.

Finally, it should be remembered that fat-rich meals delay the absorption of orally administered ketorolac.

Interactions

The concomitant intake of oral or parenteral ketorolac and the following drugs should be avoided, as there is an increased risk of developing gastrointestinal bleeding and an increased risk of developing bleeding:

  • Acetylsalicylic acid and other NSAIDs ;
  • Corticosteroids ;
  • Anticoagulants, such as, for example, warfarin and heparin;
  • Antiplatelet agents ;
  • SSRIs (selective serotonin reuptake inhibitors);
  • Pentoxifylline .

The concomitant intake of oral or parenteral ketorolac and probenecid (a drug used in the treatment of gout) increases the plasma concentration of ketorolac itself, thus increasing the side effects.

Concomitant use of ketorolac by oral or parenteral route and methotrexate (an anticancer agent) or lithium salts (used to treat bipolar disorder) may cause an increase in blood levels of the latter, resulting in increased toxicity.

Oral or parenteral ketorolac should not be given concomitantly with antihypertensive drugs, as it may reduce the effect and may increase the risk of kidney damage in dehydrated or elderly patients with already impaired kidney function.

In any case, it is a good idea to inform your doctor if you are taking - or have recently been - any type of medication, including non-prescription medicines and herbal and homeopathic products.

Side effects

Ketorolac can cause different types of side effects, but not all patients experience them.

The type of adverse effects and the intensity with which they occur depend on the different sensitivity that each individual has towards the drug.

Listed below are some of the side effects that may occur during ketorolac therapy.

Gastrointestinal disorders

Treatment with ketorolac can cause:

  • Nausea and vomit;
  • Dyspepsia;
  • Diarrhea or constipation;
  • Melena;
  • Hematemesis;
  • Abdominal pain;
  • Flatulence;
  • Esophagitis;
  • Gastritis;
  • Gastrointestinal ulceration, perforation and / or bleeding;
  • Exacerbation of ulcerative colitis and Crohn's disease in patients suffering from it.

Cardiovascular disorders

Ketorolac therapy may cause vasodilation, hypotension or hypertension, palpitations, bradycardia and heart failure.

Kidney and urinary tract disorders

Treatment with ketorolac may favor the onset of:

  • polyuria;
  • oliguria;
  • Increased frequency of urination;
  • Acute renal failure;
  • Interstitial nephritis;
  • Nephrotic syndrome;
  • Urinary retention.

Skin and subcutaneous tissue disorders

Ketorolac therapy can cause:

  • Increased sweating;
  • Exfoliative dermatitis;
  • Maculopapular rash;
  • Urticaria;
  • Itch;
  • Purple;
  • Stevens-Johnson syndrome;
  • Toxic epidermal necrolysis.

Hepatobiliary disorders

Treatment with ketorolac may promote the onset of liver failure, hepatitis and cholestatic jaundice.

Nervous system disorders

During ketorolac therapy may occur:

  • Headache;
  • dizziness;
  • paresthesia;
  • hyperkinesia;
  • Alterations in the sense of taste;
  • Aseptic meningitis.

Psychiatric disorders

Treatment with ketorolac can cause depression, insomnia and sleep disorders, irritability, nervousness, hallucinations, euphoria, psychotic reactions, confusion and reduced concentration.

Other side effects

Other side effects that may occur during ketorolac therapy are:

  • Allergic reactions, even serious, in sensitive individuals;
  • Angioedema;
  • Stomatitis;
  • Tinnitus;
  • Changes in vision;
  • Pulmonary edema;
  • Dyspnoea;
  • Asthma;
  • Myalgia;
  • Epistaxis;
  • Asthenia;
  • Temperature;
  • Edema;
  • Chest pain;
  • hyperkalemia;
  • Hyponatremia.

Side effects due to ocular administration of ketorolac

Following ocular administration of ketorolac, undesirable effects such as:

  • Irritation, burning and / or eye pain;
  • Ocular inflammation;
  • Swelling of the eye and / or eyelid;
  • Retinal bleeding or swelling;
  • Headache;
  • Decreased or blurred vision;
  • Increased eye pressure.

Overdose

In case of excessive doses of ketorolac taken orally or parenterally, the following may occur:

  • Nausea and vomit;
  • Abdominal pain;
  • hyperventilation;
  • Gastrointestinal ulceration, perforation and / or bleeding;
  • Renal dysfunction;
  • Anaphylactoid reactions;
  • Hypertension;
  • Respiratory depression;
  • Coma.

If you suspect a ketorolac overdose, you must contact your doctor immediately and go to the nearest hospital.

Action mechanism

Ketorolac performs its analgesic and anti-inflammatory action by inhibiting the activity of cyclooxygenase (or COX).

Cyclooxygenase is an enzyme of which three different isoforms are known: COX-1, COX-2 and COX-3.

COX-1 is a constitutive isoform, normally present in cells and involved in the mechanisms of cellular homeostasis.

COX-2, on the other hand, is an inducible isoform that is produced by inflammatory cells (inflammatory cytokines) activated. These enzymes convert arachidonic acid into prostaglandins, prostacyclines and thromboxanes. Prostaglandins - in particular, prostaglandins G2 and H2 - are involved in inflammatory processes and mediate pain responses.

By inhibiting COX-2, ketorolac therefore prevents the synthesis of prostaglandins responsible for pain and inflammation.

Ketorolac, however, is not a selective COX-2 inhibitor, therefore it also inhibits COX-1. This latter inhibition is at the origin of some of the side effects typical of all non-selective NSAIDs.

Mode of Use - Posology

The ketorolac is available for the:

  • Oral administration in the form of tablets or oral drops.
  • Parenteral administration in the form of a solution for injection.
  • Ocular administration in the form of eye drops.

To avoid the occurrence of dangerous side effects, during treatment with the drug, it is very important to follow the instructions provided by the doctor, both as regards the amount of ketorolac to be taken, and as regards the duration of the same treatment.

Below are some indications on the doses of ketorolac usually used in therapy.

Elderly patients may need a reduction in the doses of ketorolac usually used.

Oral administration

The dose of ketorolac usually administered orally is 10 mg of drug every 4-6 hours as needed, up to a maximum of 40 mg a day.

Parenteral administration

When using the ketorolac based solution for injection, it is recommended to start with a dose of 10 mg, followed by 10-30 mg every 4-6 hours as needed, to be administered intramuscularly or intravenously (this last type of administration, however, can only be performed in hospitals and nursing homes).

In any case, the maximum daily dose of 90 mg of drug should never be exceeded. Therapy should not last more than two days.

Ocular administration

When using ketorolac based eye drops, it is advised to instill a drop in the affected eye three times a day for a period of 3-4 weeks. Usually, the treatment should start 24 hours before the cataract surgery.

Pregnancy and breastfeeding

Oral or parenteral ketorolac can be taken in the first and second trimester of pregnancy only if the doctor considers it absolutely necessary.

Because of the serious damage it can cause to the fetus and mother, the use of the drug in the third trimester of gestation is, instead, contraindicated.

The use of ketorolac orally or parenterally is also contraindicated in breastfeeding mothers.

With regard to ketorolac for ocular use, pregnant or breastfeeding women must seek medical advice before using it.

Contraindications

The use of ketorolac by oral and parenteral route is contraindicated in the following cases:

  • In patients with known hypersensitivity to the same ketorolac (even when the drug is administered via the eye);
  • In patients with chronic pain;
  • In patients who have had allergic and sudden reactions to acetylsalicylic acid and / or other NSAIDs;
  • In patients suffering from nasal polyposis;
  • In patients with asthma, bronchospasm or angioedema;
  • In patients with a history of gastrointestinal ulceration, perforation and / or bleeding;
  • In patients with severe heart failure;
  • In patients suffering from severe liver and / or renal diseases;
  • In patients already on anticoagulant therapy, other NSAIDs, acetylsalicylic acid, lithium salts, diuretics, probenecid or pentoxifylline;
  • In children and adolescents under 16 years of age;
  • In the last trimester of pregnancy;
  • During breastfeeding.

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