Orcerin

Orcerin Uses, Dosage, Side Effects, Food Interaction and all others data.

Orcerin 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 . Orcerin 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 Orcerin
Generic Diacerein
Diacerein Other Names Diacerein, DiacereĆ­na
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 Macleods Pharmaceuticals
Available Country India
Last Updated: September 19, 2023 at 7:00 am
Orcerin
Orcerin

Uses

Orcerin 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 .

Orcerin is also used to associated treatment for these conditions: Osteoarthritis in the Hip Joint, Osteoarthritis of the Knee

How Orcerin works

Orcerin'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 Orcerin

FAQ

What is Orcerin used for?

Orcerin is a slow-acting medicine of the class anthraquinone used to treat joint diseases such as osteoarthritis.

How safe is Orcerin?

Orcerin is safe, apart from a substantially higher risk of diarrhoea, especially with longer-term use.Orcerin has an acceptable safety profile, particularly in comparison with that of NSAIDs and paracetamol. The ESCEO positions Orcerin as a first-line pharmacological background treatment of osteoarthritis.

How does Orcerin work?

Orcerin 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 Orcerin?

Common side effects of Orcerin 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 Orcerin safe during pregnancy?

Orcerin should not be administered during pregnancy.

Is Orcerin safe during breastfeeding?

Orcerin should not be administered during lactation.

Can I drink alcohol with Orcerin?

Patients should be advised to limit their alcohol intake while on treatment with Orcerin. 

Can I drive after taking Orcerin?

Orcerin may cause dizziness and drowsiness. So if you observe such symptoms, then do not drive.

When should be taken of Orcerin?

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 Orcerin on an empty stomach?

The Orcerin should be taken with food, one with breakfast and the other with evening meal.

How often can I take Orcerin?

The recommended dose is 50 mg to be taken twice daily.

How long does Orcerin take to work ?

Orcerin starts showing its action in 2-3 hours. The duration of action of Orcerin is 27 hours

How long can Orcerin be taken?

The duration of action of Orcerin is 27 hours.

Who should not take Orcerin?

Orcerin 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 Orcerin an antibiotic?

Orcerin 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 Orcerin?

If you forget to take a dose of Orcerin, 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 Orcerin?

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 Orcerin.

Can Orcerin causes diarrhoea?

Orcerin 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 Orcerin?

Avoid taking Orcerin 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. Orcerin 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 Orcerin affects my heart ?

Orcerin Improves Left Ventricular Remodeling and Cardiac Function by Reducing the Inflammatory Response after Myocardial Infarction.

Does Orcerin cause kidney damage?

Orcerin 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 Orcerin affects my liver?

Around 0.5% of patients on Orcerin had some kind of liver reaction, with most cases being mild, reversible increases in serum transaminases.

*** Taking medicines without doctor's advice can cause long-term problems.
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