Etodolac

ATC CodeM01AB08
CAS number41340-25-4
PUB number3308
Drugbank IDDB00749
Empirical formulaC17H21NO3
Molar mass (g·mol−1)287,353
Physical statesolid
Density (g·cm−3)1,2
Melting point (°C)148
Boiling point (°C)507,9
PKS value4,73
Solubility0.0392 mg/mL

Basics

Etodolac is an active ingredient that is used to treat pain, fever and inflammation. It belongs to the group of NSAIDs - non-steroidal anti-inflammatory drugs - and is an arylacetic acid derivative. The active ingredient is usually in the form of a white crystalline powder and is insoluble in water. Etodolac is available as a film-coated tablet or as a prolonged-release film-coated tablet. The advantage of a prolonged-release film-coated tablet is that the active substance is released evenly in the body over a longer period of time. This extends the duration of action.

Etodolac is a racemate, whereby the S-enantiomer has a stronger effect. A racemate is an active substance that consists of 2 molecules that occur in a 1:1 ratio and behave like an image and mirror image. One speaks of the R- (dextrorotatory) enantiomer and S- (levorotatory) enantiomer. Enantiomers do NOT differ in their physical properties such as melting or boiling point. However, they can have the opposite effect. For example, (S)-carvone smells like caraway and (R)-carvone smells like mint. The amino acid (S)-valine tastes bitter, while (R)-valine tastes sweet. For these reasons, both enantiomers are always tested in today's approval procedures for new active ingredients. Sometimes one enantiomer can be converted into the other in the body.

Graphic structural formula of the active substance etodolac

Effect

Etodolac works by inhibiting the enzyme cyclooxygenase, or COX for short. This is often referred to as a COX inhibitor. By binding the active ingredient to the binding site, the actual substrate, namely arachidonic acid, cannot bind to the receptor. The inhibition of cyclooxygenase leads to a decrease in prostaglandin synthesis. Prostaglandins, in turn, are involved in inflammatory reactions. There are several cyclooxygenase enzymes and etodolac inhibits all of them, but COX-2 significantly more strongly than the other isoforms.

Etodolac is metabolized in the liver and excreted via the kidneys. The bioavailability, i.e. the percentage of the active substance available in the blood, is at least 80%. The half-life, i.e. the time the body needs to excrete half of the active substance, is approx. 7.3 hours.

Dosage

Always take Etodolac exactly as described in the package leaflet or as advised by your doctor.

The usual recommended dose for adults or adolescents weighing 60 kg or more is 400-1000 mg per day, depending on the diagnosis and the patient's response.

The maximum dose is 1000 mg per day.

The recommended dose for children and adolescents weighing 20-60 kg is 400-600 mg per day, depending on the diagnosis and the patient's response.

Side effects

The following side effects may occur:

Frequent:

Occasionally:

Rarely:

Very rare:

  • Disorders of kidney function
  • Intestinal inflammation
  • Pancreatitis

Frequency unknown:

  • DRESS syndrome

Interactions

Interactions may occur if the following medicines are taken at the same time:

Contraindications

Etodolac must NOT be taken in the following cases

  • in case of allergy to etodolac
  • in the last trimester of pregnancy
  • with active stomach or intestinal ulcers
  • gastrointestinal bleeding
  • Crohn's disease
  • ulcerative colitis
  • severe liver dysfunction
  • severe renal dysfunction
  • for severe cardiac insufficiency
  • for the treatment of pain after coronary bypass surgery on the heart

Age restriction

Etodolac can be used from 20 kg. However, you should consult your doctor if you are under 16 years of age.

Pregnancy & breastfeeding

During pregnancy, Etodolac should only be taken after consultation with your doctor.

The active substance can betaken before the 20th week of pregnancy, but should be taken in the lowest possible dose and for as short a time as possible.

From the 20th week of pregnancy onwards, etodolac can cause damage to the unborn child and should therefore NOT be taken .

Etodolac is absolutely contraindicated in the last trimester of pregnancy.

Etodolac should NOT be taken during breastfeeding.

Paracetamol can be taken as an alternative during pregnancy and breastfeeding.

Thomas Hofko

Thomas Hofko



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The presented content does not replace the original package insert of the medication, especially regarding the dosage and effects of individual products. We cannot assume liability for the accuracy of the data, as the data has been partially converted automatically. Always consult a doctor for diagnoses and other health-related questions.

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