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