Ketolac Actions

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Actions of Ketolac in details

The action of the drug on the human body is called Pharmacodynamics in Medical terminology. To produce its effect and to change the pathological process that is happening the body and to reduce the symptom or cure the disease, the medicine has to function in a specific way. The changes it does to the body at cellular level gives the desired result of treating a disease. Drugs act by stimulating or inhibiting a receptor or an enzyme or a protein most of the times. Medications are produced in such a way that the ingredients target the specific site and bring about chemical changes in the body that can stop or reverse the chemical reaction which is causing the disease.
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Ketolac is a potent analgesic agent of the nonsteroidal anti-inflammatory class (NSAID). Its mode of action is to inhibit the cyclooxygenase enzyme system and hence prostaglandin synthesis, and it demonstrates a minimal anti-inflammatory effect at its analgesic dose.

Ketolac is not an anesthetic agent and possesses no sedative or anxiolytic properties; therefore it is not recommended as a preoperative medication for the support of anesthesia when these effects are required. It is not an opioid and has no known effects on opioid receptors.

Pharmacokinetics: Tablet: Ketolac trometamol was rapidly and completely absorbed following oral administration with a mean peak plasma concentration of 0.87 mcg/mL occurring in an average of 50 min after a single 10-mg dose. The terminal plasma half-life was on average 5.4 hrs in young adults and 6.2 hrs in elderly patients (mean age 72). The total clearance in elderly patients was slightly lower than that in young adults.

The pharmacokinetics of Ketolac trometamol in man following single or multiple doses are linear. Steady-state plasma levels are achieved after dosing every 6 hrs for 1 day. No changes in clearance occur with continued dosing. The primary route of excretion of Ketolac trometamol and its metabolites is renal: 91.4% (mean) of a given dose being found in the urine and 6.1% (mean) in the feces.

More than 99% of the Ketolac trometamol in plasma is protein-bound over a wide concentration range.

Ampoule: Following IM administration, Ketolac trometamol was rapidly and completely absorbed, a mean peak plasma concentration of 2.2 mcg/mL occurring in an average of 50 min after a single 30-mg dose. The influences of age, kidney and liver function on terminal plasma half-life and mean total clearance are outlined in the following table (estimated from a single 30-mg IM dose of Ketolac trometamol).

IV administration of a single 10-mg dose of Ketolac trometamol resulted in a mean peak plasma concentration of 2.4 mcg/mL occurring in an average of 5.4 min after dosing, with an average terminal plasma elimination half-life of 5.1 hrs, an average volume of distribution of 0.15 L/kg, and a total plasma clearance of 0.35 mL/min/kg.

Special Clinical Situations: Patients with impaired hepatic function from cirrhosis do not have any clinically important changes in Ketolac trometamol clearance or terminal half-life.

How should I take Ketolac?

For patients taking Ketolac tablets:

  • To lessen stomach upset, Ketolac tablets should be taken with food (a meal or a snack) or with an antacid.
  • Take Ketolac with a full glass of water. Also, do not lie down for about 15 to 30 minutes after taking it. This helps to prevent irritation that may lead to trouble in swallowing.

For patients using Ketolac injection:

  • Medicines given by injection are sometimes used at home. If you will be using Ketolac at home, your health care professional will teach you how the injections are to be given. You will also have a chance to practice giving injections. Be certain that you understand exactly how the medicine is to be injected.

For safe and effective use of Ketolac, do not use more of it, do not use it more often, and do not use it for more than 5 days. Using too much of Ketolac increases the chance of unwanted effects, especially in elderly patients.

Ketolac should be used only when it is ordered by your doctor for treating certain kinds of pain. Because of the risk of serious side effects, do not save any leftover Ketolac for use in the future, and do not share it with other people.

Dosing

The dose of Ketolac will be different for different patients. Follow your doctor's orders or the directions on the label. The following information includes only the average doses of Ketolac. If your dose is different, do not change it unless your doctor tells you to do so.

The amount of medicine that you take depends on the strength of the medicine. Also, the number of doses you take each day, the time allowed between doses, and the length of time you take the medicine depend on the medical problem for which you are using the medicine.

  • For oral dosage form (tablets):
    • For pain:
      • Adults (patients 16 years of age and older)—One 10-milligram (mg) tablet four times a day, four to six hours apart. Some people may be directed to take two tablets for the first dose only.
      • Children up to 16 years of age—Use and dose must be determined by your doctor.
  • For injection dosage form:
    • For pain:
      • Adults (patients 16 years of age and older)—15 or 30 mg, injected into a muscle or a vein four times a day, at least 6 hours apart. This amount of medicine may be contained in 1 mL or in one-half (0.5) mL of the injection, depending on the strength. Some people who do not need more than one injection may receive one dose of 60 mg, injected into a muscle.
      • Children up to 16 years of age—Use and dose must be determined by your doctor.

Missed Dose

If you miss a dose of Ketolac, take it as soon as possible. However, if it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule. Do not double doses.

Storage

Store the medicine in a closed container at room temperature, away from heat, moisture, and direct light. Do not refrigerate. Keep from freezing.

Keep out of the reach of children.

Do not keep outdated medicine or medicine no longer needed.

Ketolac administration

Administration of drug is important to know because the drug absorption and action varies depending on the route and time of administration of the drug. A medicine is prescribed before meals or after meals or along with meals. The specific timing of the drug intake about food is to increase its absorption and thus its efficacy. Few work well when taken in empty stomach and few medications need to be taken 1 or 2 hrs after the meal. A drug can be in the form of a tablet, a capsule which is the oral route of administration and the same can be in IV form which is used in specific cases. Other forms of drug administration can be a suppository in anal route or an inhalation route.
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Take this medication exactly as it was prescribed for you. Do not take the medication in larger amounts, or take it for longer than recommended by your doctor. Follow the directions on your prescription label. Ketolac is not for treating minor aches and pains.

Ketolac is usually given first as an injection, and then as an oral (by mouth) medicine. Ketolac injection is given through a needle into a muscle or a vein. Your doctor, nurse, or other healthcare provider will give you this injection.

The Ketolac tablet should be taken with a full glass of water.

Ketolac is normally given for 5 days or less, including both the injection and oral forms combined. Long-term use of Ketolac can damage your kidneys or cause bleeding.

If you need to have any type of surgery, tell the surgeon ahead of time if you have recently used Ketolac.

Store Ketolac tablets at room temperature away from moisture and heat.

Ketolac pharmacology

Pharmacokinetics of a drug can be defined as what body does to the drug after it is taken. The therapeutic result of the medicine depends upon the Pharmacokinetics of the drug. It deals with the time taken for the drug to be absorbed, metabolized, the process and chemical reactions involved in metabolism and about the excretion of the drug. All these factors are essential to deciding on the efficacy of the drug. Based on these pharmacokinetic principles, the ingredients, the Pharmaceutical company decides dose and route of administration. The concentration of the drug at the site of action which is proportional to therapeutic result inside the body depends on various pharmacokinetic reactions that occur in the body.

Pharmacodynamics

Ketolac is a nonsteroidal anti-inflammatory drug (NSAID) that exhibits analgesic activity in animal models. The mechanism of action of Ketolac, like that of other NSAIDs, is not completely understood but may be related to prostaglandin synthetase inhibition. The biological activity of Ketolac is associated with the S-form. Ketolac possesses no sedative or anxiolytic properties.

The peak analgesic effect of Ketolac (Ketolac) occurs within 2 to 3 hours and is not statistically significantly different over the recommended dosage range of Ketolac (Ketolac). The greatest difference between large and small doses of Ketolac (Ketolac) is in the duration of analgesia.

Pharmacokinetics

Ketolac is a racemic mixture of [-]S- and [+]R-enantiomeric forms, with the S-form having analgesic activity.

Comparison of IV, IM and

Oral Pharmacokinetics

The pharmacokinetics of Ketolac, following IV and IM doses of Ketolac and oral doses of Ketolac (Ketolac), are compared in Table 1. In adults, the extent of bioavailability following administration of the ORAL form of Ketolac and the IM form of Ketolac was equal to that following an IV bolus.

Linear Kinetics

In adults, following administration of single ORAL doses of Ketolac or IM or IV doses of Ketolac in the recommended dosage ranges, the clearance of the racemate does not change. This implies that the pharmacokinetics of Ketolac in adults, following single or multiple IM or IV doses of Ketolac or recommended oral doses of Ketolac (Ketolac), are linear. At the higher recommended doses, there is a proportional increase in the concentrations of free and bound racemate.

Absorption

Ketolac (Ketolac) is 100% absorbed after oral administration.

Oral administration of Ketolac (Ketolac) after a high-fat meal resulted in decreased peak and delayed time-to-peak concentrations of Ketolac by about 1 hour. Antacids did not affect the extent of absorption.

Distribution

The mean apparent volume (Vβ) of Ketolac following complete distribution was approximately 13 liters. This parameter was determined from single-dose data. The Ketolac racemate has been shown to be highly protein bound (99%). Nevertheless, plasma concentrations as high as 10 μg/mL will only occupy approximately 5% of the albumin binding sites. Thus, the unbound fraction for each enantiomer will be constant over the therapeutic range. A decrease in serum albumin, however, will result in increased free drug concentrations.

Ketolac is excreted in human milk.

Metabolism

Ketolac is largely metabolized in the liver. The metabolic products are hydroxylated and conjugated forms of the parent drug. The products of metabolism, and some unchanged drug, are excreted in the urine.

Excretion

The principal route of elimination of Ketolac and its metabolites is renal. About 92% of a given dose is found in the urine, approximately 40% as metabolites and 60% as unchanged Ketolac. Approximately 6% of a dose is excreted in the feces. A single-dose study with 10 mg Ketolac (Ketolac) (n=9) demonstrated that the S-enantiomer is cleared approximately two times faster than the R-enantiomer and that the clearance was independent of the route of administration. This means that the ratio of S/R plasma concentrations decreases with time after each dose. There is little or no inversion of the R- to S- form in humans. The clearance of the racemate in normal subjects, elderly individuals and in hepatically and renally impaired patients is outlined in Table 2.

The half-life of the Ketolac S-enantiomer was approximately 2.5 hours (SD ± 0.4) compared with 5 hours (SD ± 1.7) for the R-enantiomer. In other studies, the half-life for the racemate has been reported to lie within the range of 5 to 6 hours.

Accumulation

Ketolac administered as an IV bolus every 6 hours for 5 days to healthy subjects (n=13), showed no significant difference in Cmax on Day 1 and Day 5. Trough levels averaged 0.29 μg/mL (SD ± 0.13) on Day 1 and 0.55 μg/mL (SD ± 0.23) on Day 6. Steady state was approached after the fourth dose. Accumulation of Ketolac has not been studied in special populations (geriatric, pediatric, renal failure or hepatic disease patients).

Kinetics in Special Populations

Geriatric Patients

Based on single-dose data only, the half-life of the Ketolac racemate increased from 5 to 7 hours in the elderly (65 to 78 years) compared with young healthy volunteers (24 to 35 years). There was little difference in the Cmax for the two groups (elderly, 2.52 μg/mL ± 0.77; young, 2.99 μg/mL ± 1.03).

Pediatric Patients

Limited information is available regarding the pharmacokinetics of dosing of Ketolac in the pediatric population. Following a single intravenous bolus dose of 0.5 mg/kg in 10 children 4 to 8 years old, the half-life was 5.8 ± 1.6 hours, the average clearance was 0.042 ± 0.01 L/hr/kg, the volume of distribution during the terminal phase (Vβ) was 0.34 ± 0.12 L/kg and the volume of distribution at steady state (Vss) was 0.26 ± 0.08 L/kg. The volume of distribution and clearance of Ketolac in pediatric patients was higher than those observed in adult subjects. There are no pharmacokinetic data available for administration of Ketolac by the IM route in pediatric patients.

Renal Insufficiency

Based on single-dose data only, the mean half-life of Ketolac in renally impaired patients is between 6 and 19 hours and is dependent on the extent of the impairment. There is poor correlation between creatinine clearance and total Ketolac clearance in the elderly and populations with renal impairment (r=0.5).

In patients with renal disease, the AUC∞ of each enantiomer increased by approximately 100% compared with healthy volunteers. The volume of distribution doubles for the S-enantiomer and increases by 1/5th for the R-enantiomer. The increase in volume of distribution of Ketolac implies an increase in unbound fraction.

The AUC∞ -ratio of the Ketolac enantiomers in healthy subjects and patients remained similar, indicating there was no selective excretion of either enantiomer in patients compared to healthy subjects.

Hepatic Insufficiency

There was no significant difference in estimates of half-life, AUC∞ and Cmax in 7 patients with liver disease compared to healthy volunteers.

Race

Pharmacokinetic differences due to race have not been identified.

Table 1 - Table of Approximate Average Pharmacokinetic Parameters (Mean ± SD) Following

Oral,

Intramuscular and

Intravenous Doses of Ketolac

Pharmacokinetic Parameters (units)

Oral*

Intramuscular†

Intravenous Bolus‡

10 mg 15 mg 30 mg 60 mg 15 mg 30 mg
Bioavailability (extent) 100%
Tmax in pediatric patients.


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References

  1. EPA DSStox. "Ketorolac: DSSTox provides a high quality public chemistry resource for supporting improved predictive toxicology.". https://comptox.epa.gov/dashboard/ds... (accessed September 17, 2018).

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Information checked by Dr. Sachin Kumar, MD Pharmacology

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