Metodolac

Metodolac Uses, Dosage, Side Effects, Food Interaction and all others data.

Metodolac is a non-steroidal anti-inflammatory drug (NSAID). It inhibits the formation of prostaglandins. The inhibition of prostaglandin synthesis observed with Metodolac differs from that of other NSAIDs. Studies in human cell models have confirmed that Metodolac is selective for the inhibition of COX-2. Experiments have shown Metodolac to have marked anti-inflammatory activity, being more potent than several clinically established NSAIDs.

Metodolac is an anti-inflammatory agent with analgesic and antipyretic properties. It is used to treat osteoarthritis, rheumatoid arthritis and control acute pain. The therapeutic effects of etodolac are achieved via inhibition of the synthesis of prostaglandins involved in fever, pain, swelling and inflammation. Metodolac is administered as a racemate. As with other NSAIDs, the S-form has been shown to be active while the R-form is inactive. Both enantiomers are stable and there is no evidence of R- to S- conversion in vivo.

Trade Name Metodolac
Availability Prescription only
Generic Etodolac
Etodolac Other Names Etodolac, Étodolac, Etodolaco, Etodolacum, Etodolic acid, Etodolsäure
Related Drugs Humira, Buprenex, aspirin, prednisone, ibuprofen, acetaminophen, tramadol, meloxicam, naproxen, Tylenol
Weight 300mg
Type Capsule
Formula C17H21NO3
Weight Average: 287.3535
Monoisotopic: 287.152143543
Protein binding

> 99% bound, primarily to albumin

Groups Approved, Investigational, Vet approved
Therapeutic Class Drugs for Osteoarthritis, Drugs used for Rheumatoid Arthritis, Non-steroidal Anti-inflammatory Drugs (NSAIDs)
Manufacturer MedRx Life Science Ltd
Available Country Bangladesh
Last Updated: September 19, 2023 at 7:00 am
Metodolac
Metodolac

Uses

Carefully consider the potential benefits and risks of etodolac capsules and other treatment options before deciding to use etodolac capsules. Use the lowest effective dose for the shortest duration consistent with individual patient treatment goals.Metodolac are used:1. For acute and long-term use in the management of signs and symptoms of the following:

  • Osteoarthritis
  • Rheumatoid arthritis

2. For the management of acute pain

Metodolac is also used to associated treatment for these conditions: Chronic Back Pain, Extra-Articular Rheumatism, Juvenile Idiopathic Arthritis (JIA), Muscle Spasms, Nonspecific Pain Post Traumatic Injury, Osteoarthritis (OA), Pain, Acute, Postoperative pain, Rheumatoid Arthritis, Spinal Disorders

How Metodolac works

Similar to other NSAIDs, the anti-inflammatory effects of etodolac result from inhibition of the enzyme cycooxygenase (COX). This decreases the synthesis of peripheral prostaglandins involved in mediating inflammation. Metodolac binds to the upper portion of the COX enzyme active site and prevents its substrate, arachidonic acid, from entering the active site. Metodolac 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.

Dosage

Metodolac dosage

Carefully consider the potential benefits and risks of Metodolac and other treatment options before deciding to use Metodolac capsules. Use the lowest effective dose for the shortest duration consistent with individual patient treatment goals.

After observing the response to initial therapy with Metodolac capsules, the dose and frequency should be adjusted to suit an individual patient's needs.

Dosage adjustment of Metodolac is generally not required in patients with mild to moderate renal impairment. Metodolac should be used with caution in such patients, because, as with otherNSAIDs, they may further decrease renal function in some patients with impaired renal function.

Analgesia: The recommended total daily dose of Metodolac for acute pain is up to 1000 mg, given as 200 to 400 mg every 6 to 8 hours. Doses of Metodolac greater than 1000 mg/day have not been adequately evaluated in well-controlled clinical trials.

Osteoarthritis and Rheumatoid Arthritis: The recommended starting dose is 300 mg b.i.d., t.i.d., or 400 mg b.i.d., or 500 mgb.i.d.A lower dose of 600 mg/day may suffice for long-term administration. Physicians should be aware that doses above 1000 mg/day have not been adequately evaluated in well-controlled clinical trials.

In chronic conditions, a therapeutic response to therapy with Metodolac is sometimes seen within one week of therapy, but most often is observed by two weeks. After a satisfactory response has been achieved, the patient's dose should be reviewed and adjusted as required.

Side Effects

The common side effects of Metodolac involve the gastrointestinal system. It can cause abdominal pain, constipation, diarrhea, dyspepsia, flatulence, heartburn, nausea, GI ulcers, vomiting. Other events including abnormal renal function, anemia, dizziness, edema, elevated liver enzymes, headaches, increased bleeding time, pruritis, rashes, tinnitus etc.

Toxicity

Selective COX-2 inhibitors have been associated with increased risk of serious cardiovascular events (e.g. myocardial infarction, stroke) in some patients. Current data is insufficient to assess the cardiovascular risk of etodolac. Metodolac may increase blood pressure and/or cause fluid retention and edema. Risk of GI toxicity including bleeding, ulceration and perforation. Risk of direct renal injury, including renal papillary necrosis. Anaphylactoid and serious skin reactions (e.g. exfoliative dermatitis, Stevens-Johnson syndrome, toxic epidermal necrolysis) have been reported. Common adverse events include abdominal pain, constipation, diarrhea, dyspepsia, flatulence, GI bleeding, GI perforation, nausea, peptic ulcer, vomiting, renal function abnormalities, anemia, dizziness, edema, liver function test abnormalities, headache, prolonged bleeding time, pruritus, rash, tinnitus. Symptoms of overdose include lethargy, drowsiness, nausea, vomiting, and epigastric pain.

Precaution

Metodolac should be given with caution in patients with severe hepatic reactions, pre-existing asthma, fluid retention, hypertension or heart failure. If clinical sings and symptoms consistent with liver disease develop, or if systemic manifestations occur (e.g. eosinophilia, rash etc.), it should be discontinued.

Interaction

Since Metodolac is extensively protein-bound, it may be necessary to modify the dosage of other highly protein-bound drugs. The concomitant administration of Warfarin and Metodolac should not require a dosage adjustment of either drug, however it has rarely led to prolonged prothrombin times, therefore caution should be exercised when Metodolac is administered with Warfarin. Concomitant use of Ciclosporin, Methotrexate, Digoxin, or Lithium with NSAIDs may cause an increase in serum levels of these compounds and associated toxicities. Care should also be taken in patients treated with any of the following drugs as interactions have been reported in some patients: Anti-hypertensives, Mifepristone, other Analgesics, Corticosteroids and Quinolone Antibiotics.

Food Interaction

  • Avoid alcohol.
  • Take with food. Food reduces irritation.

Metodolac Alcohol interaction

[Moderate] GENERALLY AVOID:

The concurrent use of aspirin or nonsteroidal anti-inflammatory drugs (NSAIDs) and ethanol may lead to gastrointestinal (GI) blood loss.

The mechanism may be due to a combined local effect as well as inhibition of prostaglandins leading to decreased integrity of the GI lining.



Patients should be counseled on this potential interaction and advised to refrain from alcohol consumption while taking aspirin or NSAIDs.

Metodolac Hypertension interaction

[Major] Fluid retention and edema have been reported in association with the use of nonsteroidal anti-inflammatory drugs (NSAIDs).

Therapy with NSAIDs should be administered cautiously in patients with preexisting fluid retention, hypertension, or a history of heart failure.

Blood pressure and cardiovascular status should be monitored closely during the initiation of NSAID treatment and throughout the course of therapy.

Hypertension interaction

[Moderate] Nonsteroidal anti-inflammatory drugs (NSAIDs), including topicals, can lead to new onset of hypertension or worsening of preexisting hypertension, either of which can contribute to the increased incidence of cardiovascular events.

NSAIDs should be used with caution in patients with hypertension.

Blood pressure should be monitored closely during the initiation of NSAID therapy and throughout the course of therapy.

Volume of Distribution

  • 390 mL/kg

Elimination Route

Based on mass balance studies, the systemic bioavailability of etodolac from either the tablet or capsule formulation is at least 80%.

Half Life

Terminal t1/2, 7.3 ± 4.0 hours. Distribution t1/2, 0.71 ± 0.50 hours

Clearance

  • Oral cl=49.1 mL/h/kg [Normal healthy adults]
  • Oral cl=49.4 mL/h/kg [Healthy males (18-65 years)]
  • Oral cl=35.7 mL/h/kg [Healthy females (27-65 years)]
  • Oral cl=45.7 mL/h/kg [Eldery (>65 years)]
  • Oral cl=58.3 mL/h/kg [Renal impairement (46-73 years)]
  • Oral cl=42.0 mL/h/kg [Hepatic impairement (34-60 years)]

Elimination Route

It is not known whether etodolac is excreted in human milk; however, based on its physical-chemical properties, excretion into breast milk is expected. Metodolac is extensively metabolized in the liver. The hydroxylated-etodolac metabolites undergo further glucuronidation followed by renal excretion and partial elimination in the feces (16% of dose). Approximately 1% of a etodolac dose is excreted unchanged in the urine with 72% of the dose excreted into urine as parent drug plus metabolite.

Pregnancy & Breastfeeding use

Pregnancy: There are no adequate and well-controlled studies in pregnant women. It should be use in pregnancy only if the potential benefit justifies the potential risk to the fetus.

Lactation: It is not known whether Metodolac is excreted in human milk. A decision should be made whether to discontinue nursing or to discontinue the drug taking into account the importance of the drug to the mother.

Contraindication

Metodolac is contraindicated in patients with known hypersensitivity to Metodolac. Metodolac should not be given to patients who have experienced asthma, urticaria or other allergic-type reactions after taking Aspirin or other NSAIDs.

Acute Overdose

Symptoms following acute NSAID overdose are usually limited to lethargy, drowsiness, nausea, vomiting, and epigastric pain which are generally reversible with supportive care.

Storage Condition

Store at a cool and dry place protected from light & moisture. Keep out of reach of children.

Innovators Monograph

You find simplified version here Metodolac

Metodolac contains Etodolac see full prescribing information from innovator Metodolac Monograph, Metodolac MSDS, Metodolac FDA label

FAQ

What is Metodolac used for?

Metodolac is a nonsteroidal anti-inflammatory drug (NSAID) used to treat mild to moderate pain, and helps to relieve symptoms of arthritis (eg, osteoarthritis and rheumatoid arthritis), including inflammation, swelling, stiffness, and joint pain.

How safe is Metodolac?

Metodolac may also cause stomach or intestinal bleeding, which can be fatal. These conditions can occur without warning while you are using etodolac, especially in older adults.

How does Metodolac work?

Metodolac works by stopping the body's production of a substance that causes pain, fever, and inflammation.

What are the common side effects of Metodolac?

Common side effects of Metodolac are include:

  • Belching
  • bloody or black, tarry stools
  • blurred vision
  • body aches or pain
  • chest pain
  • cloudy urine
  • constipation
  • cough or hoarseness
  • decrease in urine output or decrease in urine-concentrating ability
  • diarrhea
  • dizziness
  • dryness or soreness of throat
  • feeling of indigestion
  • fever or chills
  • headache
  • increased bleeding time
  • itching, skin rash
  • loss of appetite
  • lower back or side pain
  • nausea and vomiting
  • nervousness
  • pain in the chest below the breastbone
  • painful or difficult urination
  • pale skin
  • pounding in the ears
  • runny nose
  • slow or fast heartbeat
  • stomach bloating, burning, cramping, or pain
  • swelling
  • tender, swollen glands in neck
  • trouble in swallowing
  • trouble breathing
  • unusual bleeding or bruising
  • unusual tiredness or weakness
  • voice changes
  • vomiting of blood or material that looks like coffee grounds
  • weight loss

Is Metodolac safe during pregnancy?

If you are pregnant, you should not take Metodolac unless your doctor tells you to.

Is Metodolac safe during breastfeeding?

Use should be avoided. The effects in the nursing infant are unknown. Since no information is available regarding use of this drug during breastfeeding, other agent may be preferred, especially while nursing a newborn or preterm infant.

Can I drink alcohol with Metodolac?

Do not drink alcohol while taking Metodolac. Alcohol can increase your risk of stomach bleeding caused by Metodolac. Call your doctor at once if you have symptoms of bleeding in your stomach or intestines.

Can I drink alcohol with Metodolac?

Do not drive, use machinery, or do anything that needs alertness until you can do it safely.

How many time can I take Metodolac daily?

To treat arthritis, the tablet and capsule are usually taken two to three times a day and the extended-release tablet is usually taken once a day. 

How often can I take Metodolac?

Adults, 200 to 400 milligrams (mg) every 6 to 8 hours.

How long does Metodolac take to work?

Peak plasma concentrations of etodolac are reached within 50 to 110 minutes after oral administration, and the peak analgesic effect occurs between one to two hours following a dose.

What is the half-life of Metodolac?

The effects of etodolac usually last six to eight hours. The elimination half-life of etodolac is between 6 and 8 hours in plasma, and is similar for both enantiomers.

How long can I take Metodolac?

For safe and effective use of this medicine, 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.

Who should not take Metodolac?

Do not take Metodolac around or after 20 weeks of pregnancy, unless you are told to do so by your doctor. talk to your doctor about the risks and benefits of taking etodolac if you are 75 years of age or older. Do not take this medication for a longer period of time or at a higher dose than recommended by your doctor.

What happens if I miss a dose?

Take the medicine as soon as you can, but skip the missed dose if it is almost time for your next dose. Do not take two doses at one time.

What happens if I overdose?

Seek emergency medical attention. Overdose symptoms may include drowsiness, vomiting, stomach pain, or stomach bleeding.

What happen If I stop taking Metodolac?

It comes with risks if you don't take it as prescribed by your doctor. If you stop or miss doses: If you stop taking this medication, miss doses, or don't take it on schedule, you may experience more pain caused by your condition.

Can Metodolac affect my liver?

Metodolac has been linked to rare instances of clinically apparent drug induced liver disease.

Can Metodolac affect my heart?

Metodolac can increase your risk of fatal heart attack or stroke, especially if you use it long term or take high doses, or if you have heart disease. Do not use this medicine just before or after heart bypass surgery (coronary artery bypass graft, or CABG).

Can Metodolac affect my kidneys?

The results suggest that Metodolac does not affect renal function in normal individuals, nor does it exacerbate underlying renal insufficiency when administered to patients with mild to moderate renal impairment.

*** Taking medicines without doctor's advice can cause long-term problems.
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