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