Rapacan 1mg

Rapacan 1mg belongs to immunosuppressant agent required to prevent organ refusal in renal transplants, in concomitant use with corticosteroids and cyclosporine.
It is also needed to inhibit rejection in heart transplant and for immunosuppression for stem cell/bone marrow transplants.
Rapacan 1mg which is prescribed as prescription drug under supervision of medical practioners.

INDICATION

Indicated for the prophylaxis of organ refusal in patients aged 13 years or older diagnosed renal transplants.

DOSAGE

RAPACAN IS USED FOR THE PROPHYLAXIS OF RENAL TRANSPLANT REJECTION :
Initiating treatment concomitant use with cyclosporine and corticosteroids
High immunologic risk
The usual loading dose is <40 kg: 3 mg/m² ≥40 kg: 15 mg PO loading dose Sustenance dose of Rapacan is 5 mg/day PO if >40 kg and 1 mg/m²/day if <40 kg on day 2 and after that; produce trough levels between days 5 and 7.
Dose should be adapting to control trough concentrations within desired range based on clinical state and concomitant therapy; further dose adjustment should not be done sooner than 7-14 days following a dose adjustment
Combination therapy: For the first year, continuing transplantation, Rapacan should be used in interaction with cyclosporine and corticosteroids; cyclosporine may be initiated at 7 mg/kg/day in double doses with the dose modify to get trough concentrations; prednisone should be taken at a dose of 5 mg/day
Low-to-moderate immunologic risk
The usual loading dose <40 kg: 3 mg/m² ≥40 kg: 6 mg PO loading dose Sustenance: 2 mg/day PO if ≥ 40 k g and 1 mg/m²/day if <40 kg on day 2 and thereafter; obtain trough levels between days 5 and 7
Dose should be adapting to control trough concentrations within desired range based on clinical state and concomitant therapy; further dose adjustment should not be done sooner than 7-14 days following a dose adjustment
Combination therapy: continuing transplantation, Rapacan should be used in interaction with cyclosporine and corticosteroids; may stops cyclosporine gradually over 4-8 weeks two to four months after transplant in patients with low immunologic risk, & Rapacan dose higher (serum concentrations of sirolimus may reduce following cyclosporine withdrawal)
LYMPHANGIOLEIOMYOMATOSIS :
Rapacan prescribed for therapy of lymphangioleiomyomatosis (LAM)
Initial prescribed dose: 2 mg/day PO given in 10-20 days and then monitor whole blood trough level
Over dosage :
If overdose occurs all should provide general supportive measures.

MECHANISM

Sirolimus blocks the T-lymphocytes activation and multiplication which occurs in response to antigenic and cytokinin (Interleukin [IL]-2, IL-4, and IL-15) activated by a mechanism which is distinct from that of other immunosuppressants. Sirolimus also prevents antibody production. In cells, sirolimus joints to the immunophilin, FK Binding Protein-12 (FKBP-12), to produce an immunosuppressive complex. Sirolimus consist of FKBP-12 complex has no effect on calcineurin activity. This complex link to and prevents the activation of the mammalian target of rapamycin (mTOR), a key regulatory kinase. This prevention suppresses cytokine-driven T-cell replication, preventing the progression from the G1 to the S phase of the cell cycle.

ADME

The high plasma concentration is 1-2 hours in healthy patients and renal transplant patients and bioavailability are 27%.
The drug has serum protein binding is 92%
Rapacan is widely metabolized in the intestinal wall and liver. It is substrate for both CYP3A4 and P-gp
Most of radioactivity was recovered from the faces is 91% and only little amount was excreted in urine is 2.2%. Half-life of Rapacan is 57-63 hours.

PRECAUTION

Rapacan 1mg should be prescribed only by physicians who have experience with immunosuppression in organ transplant recipients and can supply necessary follow-up and appropriate checking
Usage in liver or lung transplantation as safety and efficacy is not established.
In liver transplant recipients have been noticed having high mortality, loss in graft, and hepatic artery thrombosis
In lung transplant recipients has been noticed Bronchial anastomotic dehiscence
Rapacan 1mg will have high risk of infection, lymphoma, and other malignancies due to raise immunosuppression
Greatest enhance sun exposure due to increased skin cancer risk
Patients generally presents with hemiparesis, apathy, confusion, cognitive deficiencies, and ataxia will have resulted Progressive multifocal leukoencephalopathy (PML), sometimes fatal

DRUG INTERACTION

Rapacan co administration with cyclosporine will increases sirolimus concentration. Hence sirolimus should give 4 hours after administration of cyclosporine
Avoid co administration of Rapacan with strong inducers and strong inhibitors will decrease interaction potential with sirolimus
Using with grapefruit juice will blocks the CY3A4 – mediated metabolism of Rapacan. Avoid during using with sirolimus

CONTRAINDICATION

hypersensitivity to sirolimus

MISSED DOSE

If dose is missed to take, have immediately before next dose reaches or skip the dose and follow normal timing.
Please Consult with the doctor.

STORAGE

Rapacan 1mg Stored at 20℃-25℃
Avoid using if blister is torn or broken.

SIDE EFFECTS

Common side effects :
Fever, cold and cough
Mouth sores;
Nausea, stomach pain, diarrhoea;
Headache, muscle aches;
Chest pain;
Dizziness; or
Acne.
Other side effects, if it occurs then immediately call doctor :
Slow healing of a skin wound;
A new skin lesion,
Unusual bleeding
Sudden discomfort in chest, cough, feeling short of breath;
Pain around the transplanted kidney;
Infection like--fever, chills, painful mouth sores, skin sores, cold or flu symptoms, pain or burning when you urinate; or
Anemia- skin in pale, unusual weakness, feeling light-headed or Dyspnea cold hands and feet.