Etova-MR Actions

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Consists of etodolac, thiocolchicoside

Actions of Etodolac (Etova-MR) 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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Similar to other NSAIDs, the anti-inflammatory effects of Etodolac (Etova-MR) result from inhibition of the enzyme cycooxygenase (COX). This decreases the synthesis of peripheral prostaglandins involved in mediating inflammation. Etodolac (Etova-MR) binds to the upper portion of the COX enzyme active site and prevents its substrate, arachidonic acid, from entering the active site. Etodolac (Etova-MR) was previously thought to be a non-selective COX inhibitor, but it is now known to be 5 – 50 times more selective for COX-2 than COX-1. Antipyresis may occur by central action on the hypothalamus, resulting in peripheral dilation, increased cutaneous blood flow, and subsequent heat loss.

How should I take Etodolac (Etova-MR)?

For safe and effective use of Etodolac (Etova-MR), do not take more of it, do not take it more often, and do not take it for a longer time than ordered by your doctor. Taking too much of Etodolac (Etova-MR) may increase the chance of unwanted effects, especially in elderly patients.

When used for severe or continuing arthritis, Etodolac (Etova-MR) must be taken regularly as ordered by your doctor in order for it to help you. Etodolac (Etova-MR) usually begins to work within one week, but in severe cases up to two weeks or even longer may pass before you begin to feel better. Also, several weeks may pass before you feel the full effects of Etodolac (Etova-MR).

Swallow the extended-release tablet whole. Do not crush, break, or chew it.

Dosing

The dose of Etodolac (Etova-MR) 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 Etodolac (Etova-MR). 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.

Missed Dose

If you miss a dose of Etodolac (Etova-MR), 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. Keep from freezing.

Ask your healthcare professional how you should dispose of any medicine you do not use.

Keep out of the reach of children.

Do not keep outdated medicine or medicine no longer needed.

Etodolac (Etova-MR) 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.

Do not crush, chew, or break an extended-release tablet. Swallow the pill whole. It is specially made to release medicine slowly in the body. Breaking the pill would cause too much of the drug to be released at one time.

It may take up to 2 weeks of using this medicine before your symptoms improve. For best results, keep using the medication as directed. Talk with your doctor if your symptoms do not improve.

If you take Etodolac (Etova-MR) for a long period of time, your doctor may want to check you on a regular basis to make sure this medication is not causing harmful effects. Do not miss any scheduled visits to your doctor.

This medication can cause you to have unusual results with certain medical tests. Tell any doctor who treats you that you are using Etodolac (Etova-MR).

Store Etodolac (Etova-MR) at room temperature away from moisture and heat.

Etodolac (Etova-MR) 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.
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Pharmacodynamics

Etodolac (Etova-MR) Extended-Release Tablets are a nonsteroidal anti-inflammatory drug (NSAID) that exhibits anti-inflammatory, analgesic, and antipyretic activities in animal models. The mechanism of action of Etodolac (Etova-MR) Extended-Release Tablets, like that of other NSAIDs, is not completely understood, but may be related to prostaglandin synthetase inhibition.

Pharmacokinetics

Absorption

Etodolac (Etova-MR) Extended-Release Tablets and Etodolac (Etova-MR) tablets both contain Etodolac (Etova-MR), but differ in their release characteristics. The systemic availability of Etodolac (Etova-MR) from Etodolac (Etova-MR) Extended-Release Tablets is generally greater than 80%. Etodolac (Etova-MR) does not undergo significant first-pass metabolism following oral administration. After oral administration of Etodolac (Etova-MR) Extended-Release Tablets in doses up to 800 mg once daily, peak concentrations occur approximately 6 hours after dosing and are dose proportional for both total and free Etodolac (Etova-MR).

Table 1 shows the comparison of Etodolac (Etova-MR) pharmacokinetic parameters after the administration of Etodolac (Etova-MR) tablets and Etodolac (Etova-MR) Extended-Release Tablets.

Table 2 shows the Etodolac (Etova-MR) pharmacokinetic parameters in various populations. The data from patients with renal and hepatic impairment were obtained following administration of (immediate-release) Etodolac (Etova-MR) tablets.

Table 1.
Mean (CV)%*
Pharmacokinetic Parameters Etodolac (Etova-MR) Tablets Etodolac (Etova-MR) Extended-Release Tablets
*
% Coefficient of variation
Extent of

Oral Absorption (Bioavailability) [F]

≥ 80% ≥ 80%
Time to Peak Concentration (Tmax), h 1.4 (61%) 6.7 (47%)

Oral Clearance (CL/F), mL/h/kg

49.1 (33%) 46.8 (37%)
Apparent Volume of Distribution (Vd/F), mL/kg 393 (29%) 566 (26%)
Terminal Half-Life (t½), h 6.4 (22%) 8.4 (30%)
Table 2. Mean (CV%)* Pharmacokinetic Parameters of Etodolac (Etova-MR) in Normal Healthy Adults and Various Special Populations
Etodolac (Etova-MR) Extended-Release Tablets Etodolac (Etova-MR) Tablets
PK Parameters Normal Healthy Adults (18 to 44)†

(n=116)

Healthy Males (18 to 43)

(n=102)

Healthy Females (25 to 44)

(n=14)

Elderly (>65 yr) (66 to 88)

(n=24)

Hemodialysis‡ (24 to 65)

(n=9)

Renal Impairment‡ (46 to 73)

(n=10)

Hepatic Impairment‡(34 to 60)

(n=9)

Dialysis On Dialysis Off
NA = not available
*
% Coefficient
Age range (years)
Pharmacokinetic parameters obtained following administration of Etodolac (Etova-MR) tablets
Tmax, h 6.7

(47%)*

6.8

(45%)

4.5

(56%)

6.2

(51%)

1.7

(88%)

0.9

(67%)

2.1

(46%)

1.1

(15%)

Oral Clearance, mL/h/kg (CL/F)

46.8

(37%)

46.8

(37%)

47.2

(38%)

51.6

(40%)

NA NA 58.3

(19%)

42.0

(43%)

Apparent Volume of Distribution, mL/kg (Vd/F) 566

(26%)

580

(26%)

459

(28%)

552

(34%)

NA NA NA NA
Terminal Half-Life, h 8.4

(30%)

8.4

(29%)

7.6

(45%)

7.8

(26%)

5.1

(22%)

7.5

(34%)

NA 5.7

(24%)

Food/Antacid Effects

Food has no significant effect on the extent of Etodolac (Etova-MR) Extended-Release Tablets absorption, however, food significantly increased Cmax (54%) following a 600 mg dose.

The extent of absorption of Etodolac (Etova-MR) is not affected when Etodolac (Etova-MR) is administered with antacid. Coadministration, with an antacid, decreases the peak concentration reached by about 15 to 20% with no measurable effect on time-to-peak.

Distribution

The mean apparent volume of distribution (Vd/F) of Etodolac (Etova-MR) following administration of Etodolac (Etova-MR) Extended-Release Tablets is 566 mL/kg. Etodolac (Etova-MR) is more than 99% bound to plasma proteins, primarily to albumin, and is independent of Etodolac (Etova-MR) concentration over the dose range studied. It is not known whether Etodolac (Etova-MR) is excreted in human milk. However, based on its physical-chemical properties, excretion into breast milk is expected.

Metabolism

Etodolac (Etova-MR) metabolites do not contribute significantly to the pharmacological activity of Etodolac (Etova-MR) Extended-Release Tablets.

Following administration of immediate-release Etodolac (Etova-MR), several metabolites have been identified in human plasma and urine. Other metabolites remain to be identified. The metabolites include 6-, 7-, and 8- hydroxylated Etodolac (Etova-MR) and Etodolac (Etova-MR) glucuronide. After a single dose of 14C-Etodolac (Etova-MR), hydroxylated metabolites accounted for less than 10% of total drug in serum. On chronic dosing, hydroxylated-Etodolac (Etova-MR) metabolites do not accumulate in the plasma of patients with normal renal function. The extent of accumulation of hydroxylated-Etodolac (Etova-MR) metabolites in patients with renal dysfunction has not been studied. The role, if any, of a specific cytochrome P450 system in the metabolism of Etodolac (Etova-MR) is unknown. The hydroxylated-Etodolac (Etova-MR) metabolites undergo further glucuronidation followed by renal excretion and partial elimination in the feces.

Excretion

The mean oral clearance of Etodolac (Etova-MR) following oral Etodolac (Etova-MR) Extended-Release Tablets dosing is 47 (±17) mL/h/kg. The terminal half-life (t½) of Etodolac (Etova-MR) after Etodolac (Etova-MR) Extended-Release Tablets administration is 8.4 hours compared to 6.4 hours for Etodolac (Etova-MR) tablets. Approximately 1% of an Etodolac (Etova-MR) tablet dose is excreted unchanged in the urine, with 72% of the dose excreted into the urine as parent drug plus metabolites:

-Etodolac (Etova-MR), unchanged 1%
-Etodolac (Etova-MR) glucuronide 13%
-hydroxylated metabolites (6-, 7-, and 8-OH) 5%
-hydroxylated metabolite glucuronides 20%
-unidentified metabolites 33%

Fecal excretion accounted for 16% of the dose.

Special Populations

Geriatric

In clinical studies, age was not shown to have any effect on half-life or protein binding, and demonstrated no change in expected drug accumulation. No dosage adjustment is generally necessary in the elderly on the basis of pharmacokinetics. The elderly may need dosage adjustment, however, as they may be more sensitive to antiprostaglandin effects than younger patients.

Pediatric

The pharmacokinetics of Etodolac (Etova-MR) Extended-Release Tablets were assessed in an open-label, 12-week clinical trial which included plasma sampling for population pharmacokinetics. Seventy-two (72) patients, 6 to 16 years of age, with juvenile rheumatoid arthritis, received Etodolac (Etova-MR) Extended-Release Tablets in doses of 13.3 to 21.3 mg/kg given as 400 to 1000 mg once daily. The results from a population pharmacokinetic analysis based on the 59 subjects who completed the trial are as follows:

Table 3. Pharmacokinetic Parameter Estimates for Etodolac (Etova-MR) Extended-Release Tablets in Patients with Juvenile Rheumatoid Arthritis
Parameter JRA* (Age: 6 to 16)†

n = 59

*
Mean (CV) of parameter estimates predicted from population pharmacokinetics
Age range (years)

Oral Clearance (CL/F), mL/h/kg

47.8 (38%)
Apparent Volume of Distribution (Vd/F), mL/kg 78.9 (61%)
Half-life (t½), h 12.1 (75%)

While similar, the pharmacokinetic parameters for children with juvenile rheumatoid arthritis did not directly correlate with adult pharmacokinetic data in rheumatoid arthritis. In the population pharmacokinetic analysis, body weights below 50 kg were found to correlate with CL/F.

Race

Pharmacokinetic differences due to race have not been identified. Clinical studies included patients of many races, all of whom responded in a similar fashion.

Hepatic Insufficiency

The pharmacokinetics of Etodolac (Etova-MR) following administration of Etodolac (Etova-MR) Extended-Release Tablets have not been investigated in subjects with hepatic insufficiency. Following administration of Etodolac (Etova-MR) tablets, the plasma protein binding and disposition of total and free Etodolac (Etova-MR) were unchanged in the presence of compensated hepatic cirrhosis. Although no dosage adjustment is generally required in patients with chronic hepatic diseases, Etodolac (Etova-MR) clearance is dependent on liver function and could be reduced in patients with severe hepatic failure.

Renal Insufficiency

The pharmacokinetics of Etodolac (Etova-MR) following administration of Etodolac (Etova-MR) Extended-Release Tablets have not been investigated in subjects with renal insufficiency. Etodolac (Etova-MR) renal clearance following administration of Etodolac (Etova-MR) tablets was unchanged in the presence of mild-to-moderate renal failure (creatinine clearance, 37 to 88 mL/min). Although renal elimination is a significant pathway of excretion for Etodolac (Etova-MR) metabolites, no dosing adjustment in patients with mild-to-moderate renal dysfunction is generally necessary. Etodolac (Etova-MR) plasma protein binding decreases in patients with severe renal deficiency. Etodolac (Etova-MR) should be used with caution in such patients because, as with other NSAIDs, it may further decrease renal function in some patients. Etodolac (Etova-MR) is not significantly removed from the blood in patients undergoing hemodialysis.

Actions of Thiocolchicoside (Etova-MR) 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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Thiocolchicoside (Etova-MR) belongs to group of medicines called muscle relaxant. It is semi-synthetic derivative of naturally occurring compound colchicoside. It acts against chemical called gamma amino-butyric acid (GABA). It reduces the swelling (anti-inflammatory) and pain (analgesic), and relaxes the muscles.

References

  1. DailyMed. "ETODOLAC: DailyMed provides trustworthy information about marketed drugs in the United States. DailyMed is the official provider of FDA label information (package inserts).". https://dailymed.nlm.nih.gov/dailyme... (accessed September 17, 2018).
  2. EPA DSStox. "Etodolac: DSSTox provides a high quality public chemistry resource for supporting improved predictive toxicology.". https://comptox.epa.gov/dashboard/ds... (accessed September 17, 2018).
  3. EPA DSStox. "Thiocolchicoside: 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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