Acemetacin: Chemical Formula, Presentation, Indications, Mechanism of Action, Dosage, Side Effects, Warnings and Contraindications

It is the generic name of a drug, it is the glycolic acid ester of indomethacin and it is a non-steroidal anti-inflammatory drug.

Chemical formula of acemetacin

  • C21H18NClO6.

Presentation

  • In 60 mg capsules.

Acemetacin indications

Acemetacin is used in cases of:

  • The wear and tear of the joint ( osteoarthritis ).
  • The back pain .
  • La ankylosing spondylitis .
  • The drop.
  • Inflammation of the tendon sheaths or bursa.
  • After suffering from blunt injuries or after surgery.
  • Inflammatory rheumatic diseases.

The drug is used to relieve mild to moderate pain and inhibit inflammation. This greatly improves the mobility of diseased joints and the spine.

After surgery and blunt injuries it also uses its antipyretic and decongestant effect.

Mechanism of action

The mechanism of action of acemetacin is not yet very clear but it is believed to be closely related to the drug’s ability to inhibit the synthesis of postaglandins .

Acemetacin is rebuilt in the body with the active ingredient indomethacin and works by blocking the effect of natural substances called cyclooxygenase enzymes, COX-1 and COX-2.

These enzymes help make other chemicals in the body, called prostaglandins and thromboxane B2. Some prostaglandins are produced at sites of injury or damage and cause pain and inflammation.

In this way, by blocking cyclooxygenase enzymes, it also inhibits the production of prostaglandins, which means that pain and inflammation are relieved.

Prostaglandins are messenger substances released during the onset of pain that irritate nerve endings and send pain signals to the brain, where pain perception and processing occurs.

Acemetacin relieves pain and inflammation. It has an anti-inflammatory, decongestant and analgesic effect.

By influencing the temperature control center in the brain, it has a fever reducing effect.

It also has an inhibitory effect on platelet aggregation and therefore on blood clotting.

Acemetacin dosage

The usual dose for adults is one 60 mg capsule taken orally, twice a day, preferably morning and evening.

If necessary, your doctor may increase the dose to one capsule three times a day.

Side effects

The frequency of possible side effects that occur with the administration of acemetacin listed below are classified into the following categories:

Very common side effects

Gastrointestinal symptoms, nausea, vomiting, abdominal pain, diarrhea, and gastrointestinal blood loss.

Common side effects

Indigestion, bloating, abdominal cramps, loss of appetite, stomach or intestinal ulcers (with bleeding and perforation), loss of appetite, headache and agitation,

Also irritability, fatigue, drowsiness, dizziness, hypersensitivity reactions (rash, itching) and high levels of liver enzymes in the blood.

Uncommon side effects

Vomiting blood, bloody stools, bloody diarrhea, hives , hair loss, liver damage, hepatitis with and without jaundice,  and blood disorder such as anemia.

Also lack or absence of certain blood cells, water retention in the tissues, especially with the presence of high blood pressure or kidney failure.

Rare side effects

Temporary loss of consciousness, even to a coma.

Very rare side effects

  • Stomatitis, glossitis, esophageal damage, colitis, Crohn’s disease , ulcerative colitis , constipation , sensory disturbances, muscle weakness, sweating, altered taste sensation, blurred vision, double vision, color spotting, tinnitus.
  • (Temporary) hearing loss, memory impairment, disorientation, cramps, anxiety, irritability, nightmares, tremors, psychosis, delusions, depression , rash blistering, eczema, mucosal eruptions, skin redness, sensitivity to the light.
  • Bleeding, including allergic conditions, small and large areas, severe skin reactions, such as Stevens-Johnson syndrome, Lyell syndrome, increased blood urea, acute kidney failure, protein in the urine, blood in the urine, damage kidney, vaginal bleeding.
  • Pancreatitis , high blood sugar, sugar in the urine, hemolytic anemia, inflammation of the blood vessels, heart palpitations, angina pectoris , pain, high blood pressure .
  • Heart failure, inflammatory exacerbation, digestive canal restrictions.

When the treatment is long-term

  • Change in iris color, corneal opacities.

Special features

In rare cases, blood loss in the gastrointestinal tract can lead to anemia in all patients.

Acemetacin causes more frequent side effects in the digestive tract of elderly patients, especially bleeding and advancement, which can also be fatal.

In isolated cases, aseptic meningitis can occur with symptoms of headache, nausea, vomiting, fever, stiff neck, or loss of consciousness.

Acemetacin use may be associated with a slightly increased risk of heart attack or stroke. This risk increases the higher the dose and the longer the treatment lasts.

The recommended dose or duration of treatment should not be exceeded. All side effects decrease when the lowest effective dose is used for the shortest possible time.

Acemetacin warnings and contraindications

Some drugs are not suitable for people with certain conditions, and sometimes a drug can only be used if special precautions are taken.

For these reasons, before you start taking acemetacin, it is important to tell your doctor:

  • If you have ever had an allergic reaction to any other non-steroidal anti-inflammatory drugs such as aspirin, naproxen , diclofenac, and indomethacin or any other medicine.
  • If you have ever had a problem with bleeding from the stomach or intestines, such as a peptic or duodenal ulcer.
  • If you have asthma or any other allergic disorder.
  • If you have a heart condition or a problem with your blood vessels or circulation.
  • If you are pregnant, trying for a baby, or breastfeeding.
  • If you have ever had blood clotting problems.
  • If you have an inflammatory bowel disorder such as Crohn’s disease or ulcerative colitis.
  • If you have a connective tissue disorder, such as systemic lupus erythematosus. This is an inflammatory condition that is also called lupus.
  • If you have any of the following conditions: high blood pressure, epilepsy, Parkinsonism, a mental health problem.
  • If you have any problems with your liver or kidney function.
  • It is contraindicated in children and during lactation.

Interactions

Lithium (for depression), phenytoin (antiepileptic), and digoxin (for heart muscle weakness) levels increase with concomitant use. Therefore, its effects and side effects are amplified.

The risk of bleeding increases when combined with blood thinning medications.

Its use in combination with other non-steroidal anti-inflammatory drugs, including so-called coxibs or selective cyclooxygenase-2 inhibitors, should be avoided due to the increased risk of bleeding in the digestive tract.

The effect of oral antidiabetics increases, which is diminished by dehydrating agents and antihypertensive agents.

Simultaneous intake of potassium-sparing dehydrating agents can lead to increased potassium levels and thus cardiac arrhythmias.

Renal failure has been reported with concomitant treatment with the dehydrator triamterene and indomethacin.

Since acemetacin is converted to indomethacin in the body, the concomitant use of acemetacin and triamterene should be avoided. For geriatric patients, this interaction is especially dangerous.

In addition, the intake of anti-inflammatories such as diflunisal along with acemetacin should be avoided.

In this combination, the active ingredient of acemetacin would increase and because of that the risk of side effects would increase.

When taken with hormones like glucocorticoids and other anti-inflammatory drugs, gastric ulcers are more common.

The intake of acetylsalicylic acid and phenobarbital, an antiepileptic, reduces the effectiveness of acemetacin, while sulfinpyrazone, for the treatment of gout, strengthens it.

Methotrexate used for rheumatoid arthritis increases when taken concomitantly.

Acemetacin inhibits the excretion of penicillins (antibiotics), which can increase their effects and promote side effects.

Special care should be taken to monitor acemetacin treatment while taking medications for the treatment of brain metabolism such as benzodiazepines (sedatives and sleeping pills) or with the intake of alcohol.