Acemetacin is a nonsteroidal anti-inflammatory drug (NSAID) commonly marketed under the trade names Emflex and Rheutrop. It is primarily used to manage
pain and
inflammation associated with a variety of conditions such as
osteoarthritis,
rheumatoid arthritis,
ankylosing spondylitis, and other musculoskeletal disorders. The drug has been studied extensively, with research and development efforts spearheaded by various pharmaceutical companies and academic institutions worldwide. Acemetacin has garnered significant attention for its efficacy and relatively favorable side effect profile compared to other NSAIDs.
Acemetacin works by inhibiting the activity of cyclooxygenase (COX) enzymes, specifically
COX-1 and
COX-2. These enzymes play a crucial role in the biosynthesis of prostaglandins, which are lipid compounds that contribute to inflammation, pain, and
fever. By blocking the production of prostaglandins, Acemetacin reduces inflammation and alleviates pain. Unlike some other NSAIDs, Acemetacin is a prodrug. This means that it is metabolized in the body to produce its active form,
indometacin. This conversion mainly occurs in the liver, where Acemetacin is hydrolyzed to release indometacin, which then exerts its therapeutic effects.
Acemetacin can be administered orally in the form of tablets or capsules, usually taken with food to minimize gastrointestinal discomfort. The standard adult dose typically ranges from 60 to 180 mg per day, divided into two or three doses. The onset of action for Acemetacin can vary, but patients generally begin to experience relief from symptoms within one to two hours after ingestion. For chronic conditions, such as
arthritis, it may take several days to weeks of consistent use before the full benefits are observed. It is crucial to adhere to the prescribed dosage and not to exceed the recommended amount to avoid adverse effects.
As with any medication, Acemetacin is not without its side effects. Common side effects include gastrointestinal issues such as
nausea,
vomiting,
diarrhea, and
abdominal pain. More serious gastrointestinal events, such as
ulcers and
bleeding, can occur, particularly with long-term use or at higher doses. Other potential side effects include
dizziness,
headache,
skin rash, and elevated liver enzymes. Due to the risk of cardiovascular events, such as
heart attack and
stroke, caution is advised when using Acemetacin in patients with pre-existing cardiovascular conditions. It is also contraindicated in patients with a known hypersensitivity to NSAIDs,
active gastrointestinal bleeding, or severe
renal or hepatic impairment. Pregnant women, particularly in the third trimester, should avoid using Acemetacin due to potential risks to the fetus.
Several drugs can interact with Acemetacin, potentially altering its efficacy or increasing the risk of adverse effects. Concomitant use of other NSAIDs, such as
aspirin or
ibuprofen, should be avoided to reduce the risk of
gastrointestinal bleeding and ulceration. Anticoagulants, such as
warfarin, may have an increased risk of bleeding when taken with Acemetacin, necessitating close monitoring of blood coagulation parameters. Diuretics and antihypertensive medications, such as
ACE inhibitors and
angiotensin II receptor blockers, may have reduced efficacy when used alongside Acemetacin, potentially leading to decreased control of blood pressure.
Lithium levels may also be elevated when taken with Acemetacin, increasing the risk of
lithium toxicity. Additionally, certain antidepressants, such as selective serotonin reuptake inhibitors (SSRIs), may increase the risk of bleeding when used in combination with Acemetacin. It is essential to inform healthcare providers of all medications being taken to manage potential drug interactions effectively.
Overall, Acemetacin remains a valuable therapeutic option for managing pain and inflammation associated with various musculoskeletal conditions. Its mechanism of action, as a prodrug converted to indometacin, offers unique benefits and considerations. By understanding the proper administration methods, potential side effects, and drug interactions, patients and healthcare providers can optimize the use of Acemetacin to achieve the best possible outcomes. As with any medication, ongoing research and clinical experience will continue to refine its use and enhance its safety profile.
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