Etodolac; Uses, Dosage, Side effects, Interactions

Etodolac
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Etodolac is a nonsteroidal anti-inflammatory agent with potent analgesic and antiarthritic properties. It has been shown to be effective in the treatment of osteoarthritis; rheumatoid arthritis; ankylosing SPONDYLITIS; and in the alleviation of postoperative pain (PAIN, POSTOPERATIVE).
Etodolac is a pyranocarboxylic acid and non-steroidal anti-inflammatory drug (NSAID) with antipyretic and analgesic activities. Etodolac inhibits the activity of cyclooxygenase I and II, thereby preventing the formation of prostaglandin which is involved in the induction of pain, fever, and inflammation. It also inhibits platelet aggregation by blocking platelet cyclooxygenase and the subsequent formation of thromboxane A2.
Etodolac is a nonsteroidal anti-inflammatory drug (NSAID) that is available by prescription only and is used long-term for therapy of chronic arthritis and short-term for acute pain. Etodolac has been linked to rare instances of clinically apparent drug-induced liver disease.

Mechanism of Action of Etodolac 

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

Indications of Etodolac 

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

Contra-Indications of Etodolac 

  • Active peptic ulcer
  • Acute rhinitis
  • Allergic to thiocolchicoside
  • Asthma
  • Breastfeeding
  • Pregnant
  • Urticaria
  • Concurrent peptic ulcer, or history of ulcer disease
  • Allergy to indomethacin, aspirin, or other NSAIDs
  • Patients with nasal polyps reacting with angioedema to other NSAIDs
  • Children under 2 years of age (with the exception of neonates with patent ductus arteriosus)
  • Some painkillers, including opioid painkillers;
  • Hypnotic drugs;
  • Psychotropic drugs;
  • Used monoamine oxidase inhibitors (MAOIs) such as phenelzine or tranylcypromine
  • Epilepsy;
  • Addiction or are recovering from addiction to another medication.
  • History of peptic ulcer disease,
  • Gastrointestinal bleeding,
  • Severe pre-existing renal and liver damage
  • Caution: pre-existing bone marrow damage (frequent blood cell counts are indicated)
  • Caution: bleeding tendencies of unknown origin
  • Caution: Parkinson’s disease, epilepsy, psychotic disorders
  • Patients who have a patent ductus arteriosus dependent heart defect (such as transposition of the great vessels)
  • Significant hypertension (high blood pressure)
  • Concomitant administration of lithium salts (such as lithium carbonate)
  • History of gastric bypass surgery

Dosage of Etodolac 

Strengths: 200 mg; 300 mg; 400 mg; 500 mg; 600 mg

Osteoarthritis

Immediate Release

  • Initial dose: 300 mg orally 2 to 3 times a day or 400 mg to 500 mg orally twice a day
  • Maintenance dose: A lower dose of 600 mg/day may suffice for long-term use
  • Maximum dose: 1000 mg/day

Extended Release

  • 400 mg to 1000 mg orally once a days

Rheumatoid Arthritis

Immediate Release

  • Initial dose: 300 mg orally 2 to 3 times a day or 400 mg to 500 mg orally twice a da
  • Maintenance dose: A lower dose of 600 mg/day may suffice for long-term use
  • Maximum dose: 1000 mg/day

Extended Release

  • 400 mg to 1000 mg orally once a day

Pediatric Juvenile Rheumatoid Arthritis

Extended Release>6 to 16 years

  • 20 to 30 kg: 400 mg orally once a day
  • 31 to 45 kg: 600 mg orally once a day
  • 40 to 60 kg: 480 mg orally once a day
  • Greater than 60 kg: 1000 mg orally once a day
  • 17 to 18 years: 400 mg to 1000 mg orally once a day

Side Effects of Etodolac 

The most common

  • GI disorders (e.g. dyspepsia, abdominal pain, nausea, vomiting, diarrhea, flatulence, constipation,ulcerative stomatitis, ), indigestion,
  • Disturbances of the gut such as diarrhea, constipation, nausea, vomiting or abdominal pain.
  • Drowsiness and lightheadedness
  • Nausea and vomiting
  • joint pain
  • Nausea and vomiting
  • Severe stomach ache
  • Severe diarrhea
  • Vaginal thrush
  • Skin rash
  • Headache
  • Chest pain
  • Diarrhea or loose stools
  • Difficulty with breathing
  • Dizziness
  • Heartburn
  • Muscle pain

More common

  • Abdominal or stomach pain,
  • Chills or fever
  • A headache,
  • Joint or back pain
  • Muscle aching or cramping
  • Muscle pains or stiffness
  • Chest pressure or squeezing pain in the chest
  • Excessive sweating
  • feeling of heaviness, pain, warmth and/or swelling in a leg or in the pelvis
  • sudden tingling or coldness in an arm or leg
  • Constipation
  • Diarrhoea
  • Loss of muscle coordination
  • Sleepiness or unusual drowsiness
  • Clumsiness or unsteadiness
  • Drowsiness

Rare

  • Anxiety
  • change in vision
  • seizures
  • abnormal or fast heart rate
  • weight loss
  • chest pain or tightness
  • confusion
  • a cough
  • Agitation
  • arm, back, or jaw pain
  • blurred vision
  • chest pain or discomfort
  • convulsions
  • extra heartbeats, fainting
  • blurred vision
  • chest pain or discomfort
  • convulsions
  • extra heartbeats
  • hallucinations
  • a headache
  • irritability
  • lightheadedness
  • mood or mental changes
  • muscle pain or cramps
  • muscle spasm or jerking of all extremities
  • muscle pains or stiffness
  • chest pressure or squeezing pain in the chest
  • discomfort in arms, shoulders, neck or upper back
  • pain or discomfort in the chest, upper stomach, or throat
  • pale or blue lips, fingernails, or skin
  • puffiness or swelling of the eyelids or around the eyes, face, lips, or tongue
  • unusual drowsiness, dullness, or feeling of sluggishness

Drug Interactions of Etodolac 

Etodolac may interact with following drugs, supplements & may change the efficacy of drugs

  • antacids (e.g., aluminum hydroxide, calcium carbonate, magnesium hydroxide)
  • bisphosphonates (e.g., alendronate, etidronate,  risedronate, zoledronic acid)
  • antipsychotics (e.g., chlorpromazine, clozapine, haloperidol, olanzapine, quetiapine, risperidone)
  • angiotensin-converting enzyme inhibitors (ACEIs; e.g., captopril, enalapril, ramipril)
  • angiotensin receptor blockers (ARBs; e.g., candesartan, irbesartan, losartan)
  • beta-adrenergic blockers (e.g., metoprolol, atenolol)
  • baclofen
  • barbiturates (e.g., butalbital, phenobarbital)
  • benzodiazepines (e.g., alprazolam, diazepam, lorazepam)
  • calcium channel blockers (e.g., amlodipine, diltiazem, nifedipine, verapamil)
  • celecoxib
  • cilostazol
  • “azole” antifungals (e.g., itraconazole, ketoconazole, voriconazole)
  • clopidogrel
  • corticosteroids (e.g., dexamethasone, hydrocortisone, prednisone)
  • cyclosporine
  • diuretics (water pills; e.g., furosemide, hydrochlorothiazide, triamterene)
  • 5-ASA medications (e.g, sulfasalazine)
  • glucosamine
  • haloperidol
  • heparin
  • methotrexate
  • multivitamins
  • other non-steroidal anti-inflammatory medications (NSAIDs;e.g., diclofenac, ibuprofen, ketorolac, naproxen)
  • Omega-3 fatty acids
  • phenytoin
  • phenobarbital
  • pentoxifylline
  • quinolone antibiotics (e.g., ciprofloxacin, ofloxacin)
  • selective serotonin reuptake inhibitors (SSRIs; e.g., citalopram, duloxetine,fluoxetine, paroxetine, sertraline)
  • serotonin/norepinephrine reuptake inhibitors (SNRIs; e.g., duloxetine, venlafaxine)
  • tricyclic antidepressants (e.g., amitriptyline, clomipramine, desipramine, trimipramine)
  • warferin

Other NSAIDs: Concomitant therapy with aspirin or other NSAIDs may increase the frequency of adverse reactions, including the risk of GI bleeding.

Pregnancy & Lactation of Etodolac 

FDA Pregnancy Category C

Pregnancy

It is unknown whether etodolac is excreted into breast milk. According to the manufacturer, because many drugs are excreted in human milk and because of the potential for serious adverse reactions in nursing babies from etodolac. The safety of using this medication during pregnancy has not been established. Using this medication during pregnancy is not recommended. If you become pregnant while taking this medication, contact your doctor immediately

Lactation

It is not known if etodolac passes into breast milk. If you are a breastfeeding mother and are taking this medication, it may affect your baby. Talk to your doctor about whether you should continue breastfeeding.

Important information

Etodolac 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). Etodolac 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.

Do not use any other over-the-counter cold, allergy, or pain medication without first asking your doctor or pharmacist. Many medicines available over the counter contain aspirin or other medicines similar to etodolac (such as ibuprofen, ketoprofen, or naproxen). If you take certain products together you may accidentally take too much of this type of medication. Read the label of any other medicine you are using to see if it contains aspirin, ibuprofen, ketoprofen, or naproxen. Do not drink alcohol while taking this medicine. Alcohol can increase the risk of stomach bleeding caused by etodolac. Avoid exposure to sunlight or artificial UV rays (sunlamps or tanning beds). This medicine can make your skin more sensitive to sunlight and sunburn may result.

References

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