Actions of Rolacsin in details
Pharmacology: As a nonsteroidal anti-inflammatory drug (NSAID), Rolacsin possesses analgesic, anti-inflammatory and antipyretic activity. The major mechanism by which Rolacsin and other NSAIDs exert their pharmacological effects is inhibition of prostaglandin synthesis. NSAIDs are most active in the periphery but recent evidence suggests they may act centrally also.
Pharmacokinetics: Tablet: The oral bioavailability of Rolacsin is 80-100%. The peak plasma concentrations are reached within about 30-60 min after oral administration. The pharmacokinetics of Rolacsin is linear over the usual dosage range. Steady-state plasma levels achieved after 1 day of 4 times daily dosing.
As with other NSAIDs, Rolacsin is almost entirely bound to plasma proteins (>99%). It is extensively metabolised, primarily by conjugation with glucuronic acid and excreted via kidney. The metabolites have no significant analgesic activity. The mean terminal elimination half-life of Rolacsin in healthy volunteers is about 5 hrs.
Injection: The bioavailability of Rolacsin after oral administration is about 80-100%. The bioavailability is similar after IV/IM administration. The pharmacokinetics of Rolacsin is linear over the usual parenteral dosage range. Steady-state plasma drug concentration is about 50% higher than after single-dose administration.
As with other NSAIDs, Rolacsin is almost entirely bound to plasma proteins (>99%), which results in a small apparent volume of distribution (Vd) <0.3 L/kg. It is extensively metabolised, primarily by conjugation with glucuronic acid and excreted via kidney. The metabolites have no significant analgesic activity. The mean terminal half-life of Rolacsin in healthy volunteers is about 5 hrs.
How should I take Rolacsin?
For patients taking Rolacsin tablets:
- To lessen stomach upset, Rolacsin tablets should be taken with food (a meal or a snack) or with an antacid.
- Take Rolacsin 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 Rolacsin injection:
- Medicines given by injection are sometimes used at home. If you will be using Rolacsin 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 Rolacsin, 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 Rolacsin increases the chance of unwanted effects, especially in elderly patients.
Rolacsin 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 Rolacsin for use in the future, and do not share it with other people.
Dosing
The dose of Rolacsin 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 Rolacsin. 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 pain:
- 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.
- For pain:
Missed Dose
If you miss a dose of Rolacsin, 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.
Rolacsin administration
Intranasal: For intranasal use only; do not inhale Rolacsin nasal spray. Each nasal spray bottle contains medication for 1 day of therapy. Before first use of nasal spray, prime by holding the bottle upright and pressing pump 5 times. There is no need to prime again if more doses are administered during the next 24 hours using the same nasal spray bottle. Repeat priming each day prior to first use of each new nasal spray bottle. Blow nose to clear nostrils before using nasal spray.
Sit up straight or stand; tilt head slightly forward. Insert tip of container into nostril, keeping bottle upright, and point bottle toward the back and away from center of the nose. Hold breath and spray once, pressing down evenly on both sides of container. Immediately after administration, resume breathing through mouth to expel the product; pinch nose to help retain spray if dripping begins. Repeat in the opposite nostril if 2 sprays are prescribed per dose.
Discard bottle within 24 hours of priming even if there is unused medication.
Rolacsin pharmacology
Pharmacodynamics
Rolacsin Tromethamine is a nonsteroidal anti-inflammatory drug (NSAID) that exhibits analgesic activity in animal models. The mechanism of action of Rolacsin, like that of other NSAIDs, is not completely understood but may be related to prostaglandin synthetase inhibition.
The biological activity of Rolacsin Tromethamine is associated with the S-form. Rolacsin Tromethamine possesses no sedative or anxiolytic properties.
The peak analgesic effect of Rolacsin Tromethamine occurs within 2 to 3 hours and is not statistically significantly different over the recommended dosage range of Rolacsin Tromethamine. The greatest difference between large and small doses of Rolacsin Tromethamine by either route is in the duration of analgesia.
Pharmacokinetics
Rolacsin Tromethamine 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 Rolacsin Tromethamine, following IV, IM and oral doses of Rolacsin Tromethamine are compared in. In adults, the extent of bioavailability following administration of the ORAL and IM forms of Rolacsin Tromethamine was equal to that following an IV bolus.
Linear Kinetics
In adults, following administration of single ORAL, IM or IV doses of Rolacsin Tromethamine in the recommended dosage ranges, the clearance of the racemate does not change. This implies that the pharmacokinetics of Rolacsin Tromethamine in adults, following single or multiple IM, IV or recommended oral doses of Rolacsin Tromethamine, are linear. At the higher recommended doses, there is a proportional increase in the concentrations of free and bound racemate.
Distribution
The mean apparent volume (Vß) of Rolacsin Tromethamine following complete distribution was approximately 13 liters. This parameter was determined from single-dose data.
The Rolacsin Tromethamine racemate has been shown to be highly protein bound (99%). Nevertheless, plasma concentrations as high as 10 mcg/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.
Rolacsin Tromethamine is excreted in human milk.
Metabolism
Rolacsin Tromethamine 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 Rolacsin and its metabolites is renal. About 92% of a given dose is found in the urine, approximately 40% as metabolites and 60% as unchanged Rolacsin. Approximately 6% of a dose is excreted in the feces.
A single-dose study with 10 mg Rolacsin Tromethamine (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.
The half-life of the Rolacsin Tromethamine 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
Rolacsin Tromethamine 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 mcg/mL (SD ± 0.13) on Day 1 and 0.55 mcg/mL (SD ± 0.23) on Day 6. Steady state was approached after the fourth dose.
Accumulation of Rolacsin Tromethamine has not been studied in special populations (geriatric, pediatric, renal failure patients, or hepatic disease patients).
Kinetics in Special Populations
Geriatric Patients
Based on single-dose data only, the half-life of the Rolacsin Tromethamine 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 mcg/mL ± 0.77; young, 2.99 mcg/mL ± 1.03).
Pediatric Patients
Limited information is available regarding the pharmacokinetics of dosing of Rolacsin Tromethamine 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 Rolacsin in pediatric patients was higher than those observed in adult subjects. There are no pharmacokinetic data available for administration of Rolacsin Tromethamine by the IM route in pediatric patients.
Renal Insufficiency
Based on single-dose data only, the mean half-life of Rolacsin Tromethamine 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 Rolacsin Tromethamine 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 Rolacsin Tromethamine implies an increase in unbound fraction.
The AUC∞-ratio of the Rolacsin Tromethamine 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.
IV-Administration: In normal subjects (n=37), the total clearance of 30 mg IV-administered Rolacsin Tromethamine was 0.030 (0.017-0.051) L/h/kg. The terminal half-life was 5.6 (4.0-7.9) hours.
References
- 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).
Reviews
The results of a survey conducted on ndrugs.com for Rolacsin are given in detail below. The results of the survey conducted are based on the impressions and views of the website users and consumers taking Rolacsin. We implore you to kindly base your medical condition or therapeutic choices on the result or test conducted by a physician or licensed medical practitioners.User reports
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Information checked by Dr. Sachin Kumar, MD Pharmacology
