Intacept 25mg (Etanercept)

DESCRIPTION

Intacept containing an active ingredient Etanercept, which is composed by recombinant DNA technology having various activities like;

• Disease modifying Anti-rheumatoid arthritis
• Immuno suppressive activity
• Anti-inflammatory activity
• Tumor necrosis factor inhibitory activity

Intacept injection is used only by the patients having valid prescription, under the supervision of medical practitioner. Intacept injection is available in the strength of 50mg & 25mg containing 1.0ml & 0.5ml solution of Etanercept respectively.

INDICATION

Intacept is prefilled syringe available in two strengths like 50mg & 25mg. Intacept is used by administering subcutaneously as a single dose. The primary indication of Intacept ;

1. Rheumatoid arthritis; combining with methotrexate
2. Psoriasis arthritis; combined with MTX while in the patients non-effective to methotrexate alone
3. Ankylosing spondylitis
4. Plaque psoriasis
5. Polyarticular juvenile idiopathic arthritis; in pediatric with the age of 2 years or older

MECHANISM OF ACTION

Intacept performed by prohibiting the tumor necrosis factor, which is generally arising cytokine the factor which is significant for inflammatory response, occurs in rheumatoid arthritis, juvenile idiopathic arthritis, AS etc.

Rheumatoid arthritis causes aggregation of tumor necrosis factor in synovial fluid leads to cause joint eradication in RA, JIA, AS, PA, and PsO. Intacept inhibiting the binding of tumor necrosis factor with cell surface receptors like p55 & p75 and prohibition of activity occurs causes TNF biologically inactive

ADME PROPERTIES

ABSORPTION

The absorption of Intacept occurs moderately, after drug intake. The peak plasma concentration of Intacept reaches at 69 ± 34 hours, after taking 25mg of Intacept . The effect of Intacept occurs only after 2 to 3 weeks, since in RA patients an effect occurs in 1 to 2 weeks. Finally, the complete effect should be reached in 3 months

DISTRIBUTION

The volume of distribution of Etanercept is occurs 12L after single dose.

METABOLISM & ELIMINATION

Etanercept after binding with TNF-alpha receptor forms Etanercept-TNF complex which is apparently metabolized by undergoing proteolytic processes, before excretion. The clearance of Etanercept occurs in both adolescents and children are; 160±80ML/Hour in adult patients 46ML/Hr/m2 in children The terminal half life period of Intacept in; Adults with rheumatoid arthritis: 102 with the range of ±30 hours In children with juvenile idiopathic arthritis ≥ 4 years and adults with JIA: 70 to 94.8 hours with the range of 31.2 to 104.8 hours.

DOSAGE MANAGEMENT

IN ADULTS

In rheumatoid arthritis, psoriatic arthritis & Ankylosing spondylitis
The usual prescribed dosage of Intacept is 50mg should be administered once a week. Glucocorticoid, salicylates, Methotrexate, NSAIDS or analgesics may combine with Intacept if required conditions

In plague psoriasis
The usual recommended dosage of Intacept ; Starting dose of Intacept: The recommended dosage is 50mg of Intacept should be administered two times a week for 3 months, rather the initial dose of 25mg to 50mg should be given as a once a week. The maintenance dosage: The recommended dosage is 50mg of Intacept should be administered once a week

IN PEDIATRIC

Plaque psoriasis: 4 years or older
Less than 63kg: The recommended dosage is 0.8mg/kg of Intacept should be administered once a week 63kg or more: The recommended dosage is 50mg of Intacept should be taken as once a week The maximum dosage of Intacept is 50mg should be administered SC as a once a week

Juvenile idiopathic arthritis: 2 years or older
Depending up on the weight of patients, dosage should be recommended; 63kg or more: The recommended dosage of 50mg of Intacept should be taken as once a week Less than 63kg: The recommended dosage is 0.8mg/kg of Intacept should be taken as a once a week The maximum dosage of Intacept is 50mg should be taken as a once a week

SIDE EFFECTS

INTACEPT CAUSING ADVERSE EFFECTS
The most common adverse reaction of Intacept is severe infections associated with viral, bacterial or fungus
Rash, Diarrhea, Pruritus, Pyrexia, Urticaria, Injection site causes pain, swelling, redness, Immunogenicity, Auto antibodies, Upper respiratory tract infections, Hypersensitivity reactions, Varicella infections in pediatric patient, Aseptic meningitis in pediatric patients with JIA, Inflammatory bowel syndrome, Congestive heart failure, Elevation of transaminase, Angioedema, Chest pain, Autoimmune hepatitis, Lupus like syndrome, Interstitial lung disease,

Lab abnormalities
Pancytopenia, Anemia, Leucopenia, Neutropenia, Thrombocytopenia, Lymphadenopathy, Aplastic anemia,

PRECAUTION

INTACEPT WARNING & PRECAUTIONS
While taking Intacept tablets, care should be taken because various adverse effects may occur;

Serious infections:
Serious infection like tuberculosis active, viral infections, fungal infections and some other bacterial infections may occur Severe infection occurs due to concurrent use of Intacept with other Immuno suppressant agents such as methotrexate or glucocorticoid. To avoid this type of conditions, counsel the patients earlier about the adverse effects of Intacept . If adverse may occur, must provide supportive measures.

Before starting the therapy, some risk factor may take into consider;
1. If patient expose to active tuberculosis or not
2. History of any cosmopolitan infection occur already
3. Any viral or fungal infections occurs

Other adverse effects like;
Malignancies like Lymphoma, leukemia, non-melanoma skin cancer Neurological problems, if it occurs, discontinue the therapy and substitute with supportive measures Lymphoma is caused in pediatric patients easily during the treatment using Intacept . A severe cardiac problem like congestive heart failure has been reported in Intacept therapy. At the time of therapy with Intacept , there is a chance of getting reactivation of HBV infection. In Intacept therapy, severe hypersensitivity reactions may happens. Intacept should not be concurrently used with live vaccines, immunization. Lupus like syndrome occurs in the patients who are treating with Intacept , in that condition the Intacept therapy should be stopped as soon as possible. Due to inhibition of TNF, infection may occur easily in the patients because of suppression of immune response. Wegner’s granulomatosis patients are receiving Immuno suppressants; in this stage Intacept should not be used. Combination of Intacept with Anakinra or Abatacept should be avoided, because of increasing the adverse effects of Anakinra or Abatacept. In severe alcoholic hepatitis infected patients, Intacept used in caution

DRUG INTERACTION

Combination of Intacept with live vaccines should not be allowed, if patients have exposure to varicella virus Intacept treatment should be stopped for particular period of time. If Intacept is combined with Anakinra, there is a chance of getting bacterial pneumonia, cellulitis, pulmonary fibrosis leads to respiratory failure. Avoid this concomitant. Avoid concurrent use of Intacept with immune modulating biological product such as Abatacept or Anakinra because it may leads to increase the adverse effects of these drugs. If combination of Anakinra with Intacept , 2% of patients have chance to get neutropenia Avoid Intacept Cyclophosphamide combination therapy. Intacept concurrently used with sulfasalazine, leads to diminishing the neutrophils count.

CONTRAINDICATION

In Intacept therapy, no contraindication occurs An anaphylactic reactions occurs, if patients are contraindicated to the ingredient of Intacept Intacept is contraindicated to the patients with sepsis, tuberculosis or other infections.

PREGNANCY

In TGA pregnancy category of Intacept is D US FDA authorized pregnancy category of Intacept is B If Intacept is necessary, used cautiously in pregnancy condition under the knowledge of medical practitioner.

LACTATION

Breast feeding should not be recommended

STORAGE

Intacept prefilled syringe should be stored at 2°C to 8°C Protect from light Keep in cool and dry place

MISSED DOSE

If patients are missed the dose of Intacept , must consult with medical practitioner and follow the advice. On the other way, skip the missed dose and regular dosing schedule follows.