Lefax
Lefax Uses, Dosage, Side Effects, Food Interaction and all others data.
Lefax is a prodrug which is metabolized to rhein. It is currently approved in France for the treatment of osteoarthritis although the use of diacerein is restricted due to the side effects including severe diarrhea . Lefax is under investigation for the treatment of Insulin Resistance, Diabetes Mellitus (Type 2), and Diabetes-Related Complications.
Decreases inflammation and cartilage destruction and also corrects altered osteoblast acitivity .
| Trade Name | Lefax |
| Generic | Diacerein |
| Diacerein Other Names | Diacerein, Diacereína |
| Weight | 50mg |
| Type | Capsule |
| Formula | C19H12O8 |
| Weight | Average: 368.297 Monoisotopic: 368.053217346 |
| Protein binding | 99% of rhein is bound to plasma proteins . |
| Groups | Approved, Investigational |
| Therapeutic Class | |
| Manufacturer | Adley Labs |
| Available Country | India |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Lefax is an slow-onset anthraquinone IL-1 inhibitor used in the treatment of degenerative joint diseases like osteoarthritis.
For the treatment of osteoarthritis affecting the hip or knee .
Lefax is also used to associated treatment for these conditions: Osteoarthritis in the Hip Joint, Osteoarthritis of the Knee
How Lefax works
Lefax's active metabolite rhein Rhein reduces cartilage destruction by decreasing expression of matrix metalloproteinase (MMP)-1 and -3 as well as upregulating tissue inhibitor of matrix metalloproteinases which serve to reduce the activity of several MMPs . The anti-inflammatory action of rhein reduces the level of interleukin-1beta activity which plays a large role in reduction of extracellular matrix production, MMP activity, and continued inflammation . Rhein reduces abnormal osteoblast synthetic activity through an unknown mechanism .
Toxicity
Rhein Rhein has an oral LD50 of >5000mg/kg in mice. This is equivalent to a diacerein dose of >6476mg/kg.
Volume of Distribution
15-60L .
Elimination Route
Bioavailability of 50-60% . Entirely converted to the active metabolite rhein Rhein before reaching systemic circulation.
Half Life
4-10h .
Clearance
Total CL is 1.5L/h and renal CL is 0.1L/h .
Elimination Route
37% excreted in urine and 53% in feces as estimated in rats .
Innovators Monograph
You find simplified version here Lefax
FAQ
What is Lefax used for?
Lefax is a slow-acting medicine of the class anthraquinone used to treat joint diseases such as osteoarthritis.
How safe is Lefax?
Lefax is safe, apart from a substantially higher risk of diarrhoea, especially with longer-term use.Lefax has an acceptable safety profile, particularly in comparison with that of NSAIDs and paracetamol. The ESCEO positions Lefax as a first-line pharmacological background treatment of osteoarthritis.
How does Lefax work?
Lefax works by blocking the actions of interleukin-1 beta, a protein involved in the inflammation and destruction of cartilage that plays a role in the development of symptoms of degenerative joint diseases such as osteoarthritis.
What are the common side effects of Lefax?
Common side effects of Lefax are include:
- Diarrhoea.
- Stomach discomfort and pain.
- Nausea.
- Vomiting.
- Yellowing of skin and eyes.
- Urine discoloration.
- Increase in liver enzyme levels.
- Allergic skin reaction.
Is Lefax safe during pregnancy?
Lefax should not be administered during pregnancy.
Is Lefax safe during breastfeeding?
Lefax should not be administered during lactation.
Can I drink alcohol with Lefax?
Patients should be advised to limit their alcohol intake while on treatment with Lefax.
Can I drive after taking Lefax?
Lefax may cause dizziness and drowsiness. So if you observe such symptoms, then do not drive.
When should be taken of Lefax?
The recommended starting dose is 50 mg once daily with evening meal for the first 2 to 4 weeks of treatment, after which the recommended daily dose is 50 mg twice daily.
Can I take Lefax on an empty stomach?
The Lefax should be taken with food, one with breakfast and the other with evening meal.
How often can I take Lefax?
The recommended dose is 50 mg to be taken twice daily.
How long does Lefax take to work ?
Lefax starts showing its action in 2-3 hours. The duration of action of Lefax is 27 hours
How long can Lefax be taken?
The duration of action of Lefax is 27 hours.
Who should not take Lefax?
Lefax should not be used in any patient with liver disease or a history of liver disease, and doctors should be monitoring their patients for early signs of liver problems.
Is Lefax an antibiotic?
Lefax is a novel antibacterial agent; the antibacterial breakpoint could not be found in the literature or in standards.
What happen If I missed a dose of Lefax?
If you forget to take a dose of Lefax, make sure that you remember to take your next dose when it is due. Do not take two doses together to make up for a missed dose.
What happen if I overdose on Lefax?
Never take more than the prescribed dose. Seek emergency medical treatment or contact the doctor if you suspect that you might have taken an overdose of Lefax.
Can Lefax causes diarrhoea?
Lefax may cause diarrhoea or loose stools in the first few days of treatment. Contact your doctor if the diarrhoea does not stop within 3-4 days.
Who should not take Lefax?
Avoid taking Lefax if you are allergic to it. Seek medical attention if you notice any allergic reactions such as skin rash, hives (painful, itchy eruptions that sting), swelling (face, lips, tongue, etc.), breathing difficulty, etc. Lefax is excreted through the kidneys.
If you have pre-existing kidney problems, this medicine may accumulate in your kidneys and further worsen your condition. Hence, this medicine is not recommended for use if you have kidney problems.
Can Lefax affects my heart ?
Lefax Improves Left Ventricular Remodeling and Cardiac Function by Reducing the Inflammatory Response after Myocardial Infarction.
Does Lefax cause kidney damage?
Lefax has shown to be safe and effective in patients with moderate to severe renal impairment, and dose adjustment is not required in these patients.
Can Lefax affects my liver?
Around 0.5% of patients on Lefax had some kind of liver reaction, with most cases being mild, reversible increases in serum transaminases.
