SIROLIMUS 1MG TABLET

Raparen 1mg is an immunosuppressive agent. Raparen 1mg is a macrocyclic lactone obtained from Streptomyces hygroscopicus which acts by selectively stopping the transcriptional activation of cytokines thereby preventing cytokine production.
It is bioactive only when linked to immunophilins. Raparen 1mg possesses both antifungal and antineoplastic properties.
Raparen 1mg is a prescription drug which is used under guidance of medical practioners.

Sirolimus

1mg

100 Tablets




Usage

Raparen 1mg tablets are used for the prophylaxis of organ rejection in patients aged 13 years or older getting renal transplants.

Mechanism of action

Raparen tablets prohibits T lymphocyte activation and multiplication which occurs in response to antigenic and cytokine (Interleukin IL-2, IL-4, and IL-15) provocation by a mechanism that is obvious from that of other immunosuppressants.
Raparenalso prohibits antibody production. In cells, Raparenjoints to the immunophilin, FK Binding Protein-12 (FKBP-12), to produce an immunosuppressive complex. The FKBP-12 complex (Raparen) on calcineurin activity has no effect. This complex link to and prevents the activation of the mammalian Target of Rapamycin (mTOR), a key regulatory kinase. This prohibition restrains cytokine-driven T-cell proliferation, prohibiting the progression from the G1 to the S phase of the cell cycle.



Pharmacokinetic

In healthy patients and renal transplant patients the peak plasma concentration is 1-2 hours and bioavailability are 27%.

Human plasma protein binding is 92%

Raparen is extensively 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 Raparen is 57-63 hours.



Blueberrypharma.com-img1

sirolimus-1mg

Ingredients Sirolimus
Strength 1mg
Pack 100 Tablets
Rating

RAPAREN IS USED FOR THE PROPHYLAXIS OF RENAL TRANSPLANT REJECTION :
Starting treatment combination with cyclosporine and corticosteroids
High immunologic risk :
The loading dose is <40 kg: 3 mg/m² ≥40 kg: 15 mg PO loading dose Maintenance dose of Raparen 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 adjusted to regulate trough concentrations within desired range based on clinical state and combination therapy; further dose adjustment should not be done sooner than 7-14 days following a dose adjustment
Concomitant therapy: For the first year, following transplantation, Raparen should be used in concomitant with cyclosporine and corticosteroids; cyclosporine may be started at 7 mg/kg/day in divided doses with the dose modify to achieve trough concentrations; prednisone should be given at a dose of 5 mg/day
Low-to-moderate immunologic risk :
The loading dose <40 kg: 3 mg/m² ≥40 kg: 6 mg PO loading dose Maintenance: 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 adjusted to regulate trough concentrations within desired range based on clinical state and combination therapy; further dose adjustment should not be done sooner than 7-14 days following a dose adjustment
Concomitant therapy: Following transplantation, Raparen should be used in concomitant with cyclosporine and corticosteroids; may stops cyclosporine gradually over 4-8 weeks two to four months after transplant in patients with low immunologic risk, &Raparen dose higher (serum concentrations of sirolimus may reduce following cyclosporine withdrawal)
LYMPHANGIOLEIOMYOMATOSIS :
Raparen used for treatment of lymphangioleiomyomatosis (LAM)
Starting dose: 2 mg/day PO given in 10-20 days and then check whole blood trough level
Over dosage :
If overdose occurs all should provide general supportive measures.

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.

Precautions

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

DRUG – DRUG INTERACTION

  • Raparen combination with cyclosporine will increases sirolimus concentration. Hence sirolimus should give 4 hours after administration of cyclosporine
  • Avoid combination use of Raparen with strong inducers and strong inhibitors will reduces interaction potential with sirolimus
  • Using with grapefruit juice will prohibits the CY3A4 – mediated metabolism of Raparen. Avoid during using with sirolimus

Contraindications

Raparen 1mg is contraindicated with patients having hypersensitivity to sirolimus




Pregnancy category is C
Raparen 1mg: There are no enough and well-tolerated studies in pregnant women. Efficient contraception must be started before sirolimus therapy, during sirolimus therapy, and for 12 weeks after Raparen therapy has been stopped.

Many drugs are excreted in human milk, and because of the possible undesirable effects in nursing infants from Raparen 1mg, a decision should be considered whether to stops for nursing or to discontinue the drug, considering the necessary of the drug to the mother.

Raparen 1mg Stored at 20 - 25°C
Avoid using if blister is torn or broken.

If dose is missed, have it soon before next dose reaches or skip the dose and follow normal timing
Please Consult with the doctor


Blueberrypharma.com-img2



Quick Contact




Prescription upload






PRESCRIPTION


Blueberrypharma.com , a fully licensed and regulated pharmacy medicine, takes all precautions to strictly abide by the laws and regulations set forth in the dispensing of prescription medications. By placing the order for your prescription medicines, you acknowledge and accept the following terms regarding the purchase of any prescription medicines.

Blueberrypharma.com will not dispense any prescription medication without a valid prescription from a licensed physician.

If you are ordering prescription medication(s), you hereby confirm that you will send us a scanned copy of your valid prescription(s) via email, fax, Whatsapp, or by post, and this prescription shall then be subject to the scrutiny of and approval by our qualified Pharmacists.

The drug information provided in the Blueberrypharma.com is for informative purposes only and this Website is not intended to provide diagnosis, treatment or medical advice. We are not liable for any adverse effects or harm to you as a result of your reliance on the information in the Website.

Blueberrypharma.com requires either the User or Customer or the Caregiver to confirm he/she is completely aware of the indications, side effects, drug interactions, effects of missed dose or overdose of the medicines he/she orders from us. It is imperative to seek professional advice from your physician before purchasing or consuming any medicine from Blueberrypharma.com

At Blueberrypharma.com , a Caregiver can order prescription medicines on your behalf.