Pepcart D

Uses

Diacerein 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 .

Sodium Hyaluronate is used for the treatment of pain in osteoarthritis (OA) of the knee in patients who have failed to respond adequately to conservative nonpharmacologic therapy, and to simple analgesics, e.g., acetaminophen.

Sodium Hyaluronate is a viscous solution consisting of a high molecular weight fraction of purified natural sodium hyaluronate in buffered physiological sodium phosphate. It has a pH of 5.5-7.0. Hyaluronic acid is an important component of the body's extracellular matrix and is present in a particularly high concentration in cartilage and synovial fluid. Endogenous hyaluronic acid provides viscosity and elasticity to synovial fluid, which is fundamental for its lubricating and shock absorbing properties. It is essential for the correct structure of proteoglycans in articular cartilage. In osteoarthritis there is an insufficient amount of and a chance in the quality of hyaluronic acid in synovial fluid and cartilage. The intra-articular administration of hyaluronic acid into arthritic joints with degenerating cartilage surfaces and pathologically altered synovial fluid improved functions.

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

How Pepcart D works

Diacerein'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 .

Dosage

Pepcart D dosage

Sodium Hyaluronate is administered by intra-articular injection. A treatment cycle consists of five injections given at weekly intervals. Some patients may experience benefit with three injections given at weekly intervals. Inject the full 2 ml in one knee only. If treatment is bilateral, a separate injection should be used for each knee.

Side Effects

The common side-effects include gastrointestinal complaints, injection site pain, knee swelling/effusion, local skin reactions (rash, ecchymosis), pruritus, and headache.

Toxicity

Rhein Rhein has an oral LD50 of >5000mg/kg in mice. This is equivalent to a diacerein dose of >6476mg/kg.

Precaution

Use caution when injecting Sodium Hyaluronate into patients who are allergic to avian proteins, feathers, and egg products. Strict aseptic administration technique must be followed. Remove joint effusion, if present, before injecting Sodium Hyaluronate. Do not use the same syringe for removing joint effusion and for injecting Sodium Hyaluronate. It is recommended that the patient avoid any strenuous activities or prolonged (i.e., more than 1 hour) weight-bearing activities such as jogging or tennis within 48 hours following the intra-articular injection.

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 .

Pregnancy & Breastfeeding use

The safety and effectiveness of Sodium Hyaluronate have not been established in pregnant women. It is not known if Sodium Hyaluronate is excreted in human milk. The safety and effectiveness of Sodium Hyaluronate have not been established in lactating mother. The safety and effectiveness of Sodium Hyaluronate have not been demonstrated in children.

Contraindication

The drug is contraindicated in patients with known hypersensitivity to hyaluronate preparations. Intra-articular injections are contraindicated in cases of past and present infections or skin diseases in the area of the injection site.

Acute Overdose

No case of over dosage has been reported to date.

Storage Condition

Hyronate injection should be stored in a cool (below 25° C) and dry place and protected from light. Protect from freezing.

Innovators Monograph

You find simplified version here Pepcart D