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