Topcerin
Topcerin Uses, Dosage, Side Effects, Food Interaction and all others data.
Topcerin 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 . Topcerin 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 | Topcerin |
| 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 | Lupin |
| Available Country | India |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Topcerin 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 .
Topcerin is also used to associated treatment for these conditions: Osteoarthritis in the Hip Joint, Osteoarthritis of the Knee
How Topcerin works
Topcerin'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 Topcerin
FAQ
What is Topcerin used for?
Topcerin is a slow-acting medicine of the class anthraquinone used to treat joint diseases such as osteoarthritis.
How safe is Topcerin?
Topcerin is safe, apart from a substantially higher risk of diarrhoea, especially with longer-term use.Topcerin has an acceptable safety profile, particularly in comparison with that of NSAIDs and paracetamol. The ESCEO positions Topcerin as a first-line pharmacological background treatment of osteoarthritis.
How does Topcerin work?
Topcerin 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 Topcerin?
Common side effects of Topcerin 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 Topcerin safe during pregnancy?
Topcerin should not be administered during pregnancy.
Is Topcerin safe during breastfeeding?
Topcerin should not be administered during lactation.
Can I drink alcohol with Topcerin?
Patients should be advised to limit their alcohol intake while on treatment with Topcerin.
Can I drive after taking Topcerin?
Topcerin may cause dizziness and drowsiness. So if you observe such symptoms, then do not drive.
When should be taken of Topcerin?
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 Topcerin on an empty stomach?
The Topcerin should be taken with food, one with breakfast and the other with evening meal.
How often can I take Topcerin?
The recommended dose is 50 mg to be taken twice daily.
How long does Topcerin take to work ?
Topcerin starts showing its action in 2-3 hours. The duration of action of Topcerin is 27 hours
How long can Topcerin be taken?
The duration of action of Topcerin is 27 hours.
Who should not take Topcerin?
Topcerin 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 Topcerin an antibiotic?
Topcerin 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 Topcerin?
If you forget to take a dose of Topcerin, 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 Topcerin?
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 Topcerin.
Can Topcerin causes diarrhoea?
Topcerin 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 Topcerin?
Avoid taking Topcerin 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. Topcerin 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 Topcerin affects my heart ?
Topcerin Improves Left Ventricular Remodeling and Cardiac Function by Reducing the Inflammatory Response after Myocardial Infarction.
Does Topcerin cause kidney damage?
Topcerin 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 Topcerin affects my liver?
Around 0.5% of patients on Topcerin had some kind of liver reaction, with most cases being mild, reversible increases in serum transaminases.
