Sulindaco: Formula, Presentation, Indications, Mechanism of Action, Dosage, Side Effects and Interactions

It is a non-steroidal antirheumatic drug that has analgesic, anti-inflammatory and antipyretic properties.

With good tolerance at the gastrointestinal level, it is of fast action and a prolonged half-life.

Sulindaco is native to sulfinilindene, which is transformed by the action of liver enzymes into a sulfinyl compound, with analgesic properties.

Chemical formula

  • C20H17FO3S.
  • 2 – [(3Z) -6-fluoro-2-methyl-3 – [(4-methylsulfinylphenyl) methylideno] inden-1-yl] acetic acid.

Presentation

  • The Sulindaco has its presentation in 150 and 200 mg tablets.

Indications

Sulindaco is used especially for the medication of osteoarthritis, rheumatoid arthritis , osteoporosis and ankylosing spondylitis .

It is also used in the treatment of patients with periarticular diseases such as acute gouty arthritis.

It is used in the treatment of inflammatory and traumatic disorders of the acute and soft tissues, in lumbosacral pain, as well as in dysmenorrhea, inflammatory and intestinal diseases and headaches.

The Sulindaco is sometimes administered to reduce the number of polyps in the colon and rectum.

Mechanism of action

The mechanism of action that has been established for sulindac is similar to that of some non-steroidal anti-inflammatories.

This is done by inhibiting the synthesis processes of prostaglandins ( cyclo-oxygenase) which results in a decrease in their concentration, reducing pain, inflammation and febrile symptoms.

Dose

  • The recommended dose is to administer 150 or 200 mg tablets twice a day accompanied by liquids or foods.
  • Preferably with meals.
  • The maximum dose should not exceed 400 mg per day.

Side effects

Sulindaco’s administration generally does not cause any side effects.

However, there may be some adverse effects that are of some severity and are usually related to high doses.

Among the most common side effects of Sulindaco, which involve the gastrointestinal system are:

  • It produces ulcerations in the stomach and small intestine.
  • Presence of gastrointestinal pain and cramps, nausea with or without vomiting, gastritis, diarrhea, constipation, flatulence and severe gastrointestinal bleeding.
  • Ulcers in the stomach and bleeding can occur without the occurrence of any abdominal pain.
  • The presence of black tarry stools, signs of weakness and dizziness upon incorporation ( orthostatic hypotension ) may be the only symptoms of the presence of an internal hemorrhage.

Other important side effects have been reported, including:

  • Eruptions, purito, edema.
  • Anorexia.
  • The advent of hepatic toxicities such as elevation of transaminases and other liver enzymes.
  • Renal insufficiency and dysuria , hematuria, crystalluria, interstitial nephritis.
  • Ringing in the ears or tinnitus.
  • Stunning and nervousness.
  • Heart failure, palpitations.
  • Allergies, Stevens-Johnson syndrome and severe anaphylaxis.

The administration of Sulindaco is a well-established cause, but a rare occurrence of idiosyncratic liver disease, which is apparently induced by drugs.

Warnings and contraindications

This drug should not be administered in patients with:

  • This drug is contraindicated in patients who have a history of hypersensitivity to Sulindac or any of its components. In the same way in patients who have had an allergic reaction to acetylsalicylic acid or any other non-steroidal anti-inflammatory.
  • In case the patient suffers from gastritis and active peptic ulcers, a history of gastrointestinal hemorrhages or ulcers.
  • Administration in children is not recommended.
  • Although its placental passage is little or almost null, it is not recommended in pregnant women.
  • It has been shown that it is found in breast milk, which is why it is restricted in nursing mothers.
  • In cases of asthmatic patients.
  • Fluid retention, blood clots, heart attacks, high blood pressure and heart failure have been associated with the use of sulindaco.
  • Special caution should be taken with oral anticoagulants or oral hypoglycaemic agents.

Interactions

Generally all drugs that bind to plasma proteins, as with sulindac. These are able to displace other drugs that also tend to bind to plasma proteins such as warfarin or in the case of oral hypoglycemic agents.

Sulindacum should not be administered with dimethylsulfoxide since there is a possibility of causing neuropathy.

Nor should it be taken together with methotrexate since toxicity can be increased and the same occurs when its administration is associated with ciclosporin .

The concomitant administration of sulindac with other non-steroidal anti-inflammatory drugs is not advisable given the possibility of side effects being added and competition at the level of plasma proteins.

The administration of antacids reduces their absorption. Sulindaco tends to increase blood levels of lithium by inducing its removal by the kidneys. This increase in lithium levels can lead to toxicity.

Sulindaco can reduce blood pressure, this can happen because prostaglandins have a role in regulating (reducing) blood pressure.

Combination of NSAIDs such as sulindac with angiotensin receptor blockers (eg, valsartan [Diovan], losartan [Cozaar], irbesartan [Avapro]) or angiotensin-converting enzyme (ACE) inhibitors.

For example, enalapril (Vasotec), captopril (Capoten) in patients who are elderly, with fluid loss (including those on diuretic therapy) or with impaired renal function may reduce renal function, including renal failure .

When sulindaco is used in combination with methotrexate (Rheumatrex, Trexall) or aminoglycoside antibiotics (eg, gentamicin), blood levels of methotrexate or aminoglycoside may increase. Presumably because the elimination of methotrexate or aminoglycosides from the body is reduced.

This can lead to more side effects related to methotrexate or aminoglycosides.

Sulindac has an increased risk of developing stomach ulcers in people who consume more than three alcoholic beverages per day.

Alterations of laboratory tests may occur when sulindaco is administered, detecting altered levels of agranulocytosis of liver enzymes, neutropenia, thrombocytopenia and aplastic anemia.