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Indomethacin

Generality

Indomethacin is a non-steroidal anti-inflammatory drug (NSAID) belonging to the family of acetic acid derivatives.

Indomethacin - in addition to anti-inflammatory activity - has a marked antipyretic activity (it is more powerful than both aspirin, paracetamol) and an equally strong analgesic activity.

Ibuprofen - Chemical Structure

It is available in different pharmaceutical formulations suitable for oral, rectal, ocular and parenteral administration.

Examples of medicinal specialties containing Indomethacin

  • Difmetre ® (in combination with caffeine and prochlorperazine).
  • Indom Collirio ®
  • Indoxen ®
  • Liometacen ®

Indications

For what it uses

The use of indomethacin is indicated for the symptomatic treatment of inflammation and pain caused by diseases such as:

  • Musculoskeletal system disorders;
  • Rheumatoid arthritis;
  • Osteoarthritis;
  • Gout.

Moreover, indomethacin administered via the eye is indicated in the treatment of painful and inflammatory states (on a non-infectious basis) of the anterior segment of the eye, in particular, following cataract surgery.

Warnings

When indomethacin therapy is started, headache, dizziness and lightheadedness could occur. The incidence of these side effects can be reduced by starting treatment with low doses of the drug which will then be gradually increased.

Indomethacin may cause gastrointestinal ulceration, perforation and / or bleeding. Therefore, should gastrointestinal symptoms of any kind appear, it is advisable to inform the doctor immediately. Elderly patients and those who have suffered from severe gastrointestinal disorders in the past have an increased risk of onset of the aforementioned side effects.

If the doctor considers it necessary, he can decide to prescribe a therapy based on gastroprotective drugs in conjunction with indomethacin treatment.

Indomethacin may increase the risk of heart attack or stroke, especially when used at high doses and for long periods. Therefore, it is very important to never exceed the recommended drug doses.

Since cases of retinal changes and corneal deposits have been reported, appropriate eye checks should be performed in patients undergoing long-term indomethacin therapy.

Should any type of allergic reaction occur during treatment with indomethacin, treatment with the drug should be stopped immediately and the doctor should be informed immediately.

Furthermore, before starting treatment with indomethacin, it is advisable to inform your doctor if you suffer - or have suffered in the past - from diseases such as asthma, ulcerative colitis, Crohn's disease, liver, kidney and / or heart disease.

Interactions

Indomethacin is able to counteract the natriuretic effect of furosemide (a diuretic).

Indomethacin - as well as other NSAIDs - increases the effect of anticoagulants and antiplatelet agents .

Concomitant administration of indomethacin and corticosteroids causes an increased risk of developing ulceration or gastrointestinal bleeding.

Indomethacin may reduce the therapeutic efficacy of antihypertensive drugs (such as, for example, ACE inhibitors and angiotensin II antagonists). Furthermore, the concomitant intake of indomethacin and these drugs in patients with pre-existing renal impairment may cause a further worsening of the aforementioned functionality.

Finally, before starting indomethacin treatment, you need to tell your doctor if you are already taking medications, such as:

  • Calcitonin ;
  • Probenecid ;
  • SSRIs (selective serotonin reuptake inhibitors);
  • Proglumide ;
  • Sulfonamides ;
  • Zidovudine ;
  • Pentoxifylline ;
  • Other NSAIDs .

In any case, it is a good idea to inform your doctor if you are taking - or have recently taken - any type of medication, including over-the-counter medicines and herbal and homeopathic products.

Side effects

Indomethacin can cause various side effects, although not all patients experience them.

The main side effects that may occur during treatment with indomethacin are listed below.

Gastrointestinal disorders

During indomethacin therapy, the following may occur:

  • Nausea;
  • He retched;
  • Diarrhea or constipation;
  • Flatulence;
  • Dyspepsia;
  • Abdominal pain;
  • Melena;
  • Hematemesis;
  • Gastrointestinal ulceration, perforation and / or bleeding;
  • Worsening of ulcerative colitis and Crohn's disease in patients suffering from it.

Allergic reactions

Indomethacin may cause allergic reactions, even serious ones, in sensitive individuals. These reactions can occur in the form of:

  • Angioedema;
  • Urticaria;
  • Itch;
  • rashes;
  • Stevens-Johnson syndrome;
  • Toxic epidermal necrolysis;
  • Hair loss;
  • Sudden dyspnea;
  • Asthma.

Blood and lymphatic system disorders

Indomethacin treatment can cause:

  • Leukopenia;
  • thrombocytopenia;
  • Aplastic anemia;
  • Hemolytic anemia;
  • Purple.

Eye disorders

Indomethacin therapy may cause:

  • Blurred vision;
  • Orbital and periorbital pain;
  • Corneal deposits;
  • Retinal changes.

Hepatobiliary disorders

Treatment with indomethacin may cause hepatitis and jaundice.

Cardiovascular disorders

Indomethacin therapy may favor the onset of:

  • Myocardial infarction;
  • Stroke;
  • Heart failure;
  • Hypertension.

Other side effects

Other side effects that may occur during treatment with indomethacin are:

  • Headache;
  • Dizziness;
  • Syncope;
  • Confusion and stunning;
  • Depression;
  • Epistaxis;
  • Kidney failure;
  • Hematuria and / or glycosuria;
  • Fatigue.

Side effects due to ocular administration of indomethacin

Following the use of indomethacin based eye drops, they can occur:

  • Eye burn;
  • Heat sensation;
  • Conjunctival redness;
  • Light sensitivity.

Overdose

At present, no cases of overdose are known following the use of indomethacin for ocular use.

On the other hand, when overdoses of indomethacin are taken orally, rectally or parenterally, gastrointestinal symptoms may occur. Treatment is only symptomatic and supportive.

In any case, should you suspect an indomethacin overdose, you must contact your doctor immediately or go to the nearest hospital.

Action mechanism

Indomethacin carries out its anti-inflammatory, analgesic and antipyretic activity by inhibiting the activity of cyclooxygenase (or COX).

Cyclooxygenase is an enzyme of which three different isoforms are known: COX-1, COX-2 and COX-3.

COX-1 is a constitutive isoform, normally present in cells and involved in the mechanisms of cellular homeostasis.

COX-2, on the other hand, is an inducible isoform that is produced by inflammatory cells (inflammatory cytokines) activated. The task of these enzymes is to convert arachidonic acid into prostaglandins, prostacyclines and thromboxanes.

Prostaglandins are involved in inflammatory and painful processes (in particular, PGG2 and PGH2) and induce an increase in body temperature, ie they induce fever (in particular, PGE).

Therefore, through the inhibition of COX-2, indomethacin hinders the formation of prostaglandins responsible for fever, inflammation and pain.

It should be remembered, however, that indomethacin is not selective for COX-2, therefore it is also able to inhibit COX-1. This latter inhibition is at the origin of some of the side effects typical of all non-selective NSAIDs.

Mode of Use - Posology

Indomethacin is available for:

  • Oral administration in the form of hard capsules.
  • Rectal administration in the form of suppositories.
  • Parenteral administration in the form of powder and solvent for solution for injection.
  • Ocular administration in the form of eye drops.

Below are some indications on the doses of indomethacin usually used in therapy. Notwithstanding that during the treatment with the drug, it is always necessary to follow the indications provided by the doctor, both as regards the amount of indomethacin to be taken, and as regards the duration of the treatment itself.

Oral and rectal administration

When indomethacin is administered orally or rectally, it is recommended to start treatment with a dose of 75 mg of drug per day. The dose can be gradually increased up to 100-200 mg of indomethacin per day.

Parenteral administration

Indomethacin parenterally can only be administered in the hospital by specialized personnel. The usual dose is 25-50 mg, to be administered intravenously.

Ocular administration

Indomethacin based eye drops are mainly used for the treatment of inflammation of the anterior segment of the eye following cataract surgeries. The dosage of the drug must be established by the doctor on an individual basis.

Pregnancy and breastfeeding

During the first and second trimester of pregnancy, indomethacin should only be used if the doctor considers it absolutely necessary.

In the third trimester of pregnancy, on the other hand, the use of the drug is contraindicated due to the potential damage it can cause to the fetus (cardiopulmonary toxicity, renal dysfunction and prolonged bleeding time) and to the mother (inhibition of uterine contractions with consequent delay or prolonged labor and increased bleeding time).

Since there are not enough data regarding the safe use of indomethacin by breast-feeding mothers, the use of the drug in this category of patients is not recommended.

Contraindications

The use of indomethacin is contraindicated in the following cases:

  • In patients with known hypersensitivity to indomethacin itself or to other NSAIDs;
  • In patients who have had allergic reactions after taking salicylates (such as acetylsalicylic acid);
  • In patients who suffer - or who have suffered - from a gastrointestinal ulcer;
  • In patients with severe heart failure;
  • In patients undergoing intensive diuretic therapy;
  • In patients predisposed to the development of bleeding;
  • In patients with epilepsy;
  • In patients suffering from parkinsonism;
  • Pregnant;
  • During breastfeeding.

Furthermore, the use of oral, rectal or parenteral indomethacin is contraindicated in children and adolescents less than 14 years of age, while the use of ocular indomethacin is contraindicated in children under 3 years of age. age.

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