tolmetin

Action and Spectrum

Actions and Spectrum: 

tolmetin is a non-steroidal anti-inflammatory medicine (NSAID) that is used to treat pain and inflammation in several illnesses, including menstrual cramps, arthritis, and gout. It functions by preventing the body from producing prostaglandins, which are chemicals that induce pain and inflammation.  

tolmetin has both analgesic (pain-relieving) and anti-inflammatory properties. It belongs to the same family of NSAIDs as ibuprofen and naproxen and works similarly to other medications in this group called propionic acids. 

When used orally, the medication is quickly absorbed and reaches peak plasma concentrations in 1-2 hours. It is broken down in the liver and eliminated through the urine. Its activity lasts for around 6 to 8 hours. 

Drug Interaction

Adverse Reaction

Frequency Defined  

<1% 

Stevens-Johnson syndrome 

Toxic epidermal necrolysis 

Gastrointestinal hemorrhage 

Thrombotic tendency observations 

Erythema multiforme 

Scaling eczema 

Gastrointestinal perforation 

Inflammatory disorder of digestive tract 

Neutropenia 

Thrombocytopenia 

Jaundice 

Agranulocytosis 

Anemia 

Liver failure 

Hematuria 

Proteinuria 

Bronchospasm 

Anaphylactoid reaction 

Cerebrovascular accident 

Acute renal failure 

>10% 

liver function test increased (up to 15%) 

1-10% 

Edema 

Weight gain, Weight loss 

Abdominal pain 

Diarrhea 

Nausea (10%) 

Hypertension (3-9%) 

Myocardial infarction (<2%) 

Asthenia 

Dizziness 

Headache 

Flatulence 

Indigestion 

Nausea, Vomiting 

Black Box Warning

Black Box Warning 

The elevated risk of potentially deadly cardiovascular events, including heart attack and stroke, is highlighted in the black box warning for tolmetin. Those who take tolmetin at greater dosages or for longer periods of time than advised, as well as those who have pre-existing cardiovascular disease or risk factors for it, may be at higher risk. 

tolmetin is among the NSAIDs that the warning indicates can result in gastrointestinal bleeding, perforation and ulceration all of which can be deadly. Those having a history of gastrointestinal bleeding or ulcers and elderly people are at increased risk for these side effects. 

Contraindication / Caution

Contraindication/Caution: 

Contraindication: 

• allergy to tolmetin or any of its ingredients 
• history of urticaria, asthma, or any allergic reaction brought on by aspirin 
• responses to NSAIDs, such as aspirin 
• gastrointestinal haemorrhage or active peptic ulcer illness 
• serious liver impairment 

Caution: 

• cardiovascular illness or cardiovascular disease risk factors 
• renal dysfunction 
• gastrointestinal bleeding, ulcers, or perforations in the past 
• patients who experience allergic reactions or asthma 
• geriatric patients 
• breastfeeding and becoming pregnant 

Pregnancy / Lactation

Pregnancy warnings:     

Pregnancy category: C 

Lactation: Excreted into human milk and safety in infants not known. 

Pregnancy Categories:         

Category A: Studies that were well-controlled and met expectations revealed no risk to the fetus in either the first or second trimester. 

Category B: There were lack of studies on pregnant women and no evidence of risk to the foetus in animal experiments.   

Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.    

Category D: adequate data available with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.   

Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.    

Category N: There is no data available for the drug under this category

Pharmacology

Pharmacology:  

tolmetin is a non-steroidal anti-inflammatory medication (NSAID) with analgesic, antipyretic, and anti-inflammatory effects that can help with pain and inflammation. It functions by preventing the prostaglandin-producing enzyme cyclooxygenase (COX) from producing any new prostaglandins. Chemical mediators called prostaglandins encourage heat, discomfort, and inflammation. 

Ibuprofen, naproxen, and tolmetin are all NSAIDs that belong to the propionic acid class. When administered orally, it is quickly absorbed and reaches peak plasma concentrations in one to two hours. The medication undergoes substantial liver metabolization and is eliminated in the urine. 

Pharmacodynamics:  

tolmetin inhibits both COX-1 and COX-2 enzymes since it is a non-selective COX inhibitor. A constitutive enzyme called COX-1 is involved in the synthesis of prostaglandins, which support the maintenance of regular physiological processes including maintaining the stomach lining and controlling blood flow to the kidneys. 

Chemical mediators called prostaglandins have a role in the development of fever, discomfort, and inflammation. It further relieves pain, fever, and inflammation by inhibiting COX and lowering prostaglandin synthesis. 

Pharmacokinetics:  

Absorption   

Peak plasma concentrations of tolmetin are obtained within 1-2 hours of oral treatment and are quickly absorbed. The medication has a high absolute bioavailability, with a 95% absorption from the gastrointestinal system. 

Distribution 

tolmetin has a very narrow volume of distribution and is well bound to plasma proteins, particularly albumin. The medication is absorbed into many tissues, including the synovial fluid, where it may build up to larger amounts than in the plasma. 

Metabolism   

tolmetin undergoes substantial oxidative and glucuronidation metabolization in the liver. Tolmetin’s principal metabolite, 5-hydroxytolmetin, is a potent COX inhibitor. 

Elimination and excretion  

tolmetin and its metabolites are largely excreted in the urine, and after 24 hours of dosing, 80–90% of the medication has been removed. Tolmetin has a relatively short elimination half-life of 2-3 hours, meaning that it leaves the body relatively fast. 

Adminstartion

Administration:  

To lower the risk of gastrointestinal upset, tolmetin is normally taken orally with meals and is available as tablets. Depending on the patient’s reaction to the medication and the seriousness of the disease being treated, the dose may need to be changed. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: tolmetin 

Why do we use tolmetin? 

tolmetin is a non-steroidal anti-inflammatory medicine (NSAID) that is primarily used to treat the pain, swelling, and fever brought on by a number of illnesses, such as osteoarthritis, rheumatoid arthritis, dysmenorrhea, acute gout, ankylosing spondylitis