Mylimus 1mg (Tacrolimus )

DESCRIPTION

Mylimus is available in capsule form; it is calcineurin inhibitor immunosuppressant drug Mylimus is classified as macrolide antibiotic Mylimus is used in combination with other medicines to protect the body from rejecting a transplanted organ like kidney, liver or heart

Mostly Mylimus is concomitant with steroids, azathioprine, basiliximab or Mycophenolate mofetil Mylimus is used for preventing organ rejection in organ transplant patients The usual availability of strength of  0.5mg, 1mg, 2mg

INDICATION

Mylimus is used in organ transplantation condition, in some patients who are attain organ transplant, their body white blood cells are trying to reject the transplanted organ. In this condition, Mylimus is helps to accept the transplanted organ by the patient’s body, through weakening the body’s immune system. This leads the body to acquire the new organ which is transplanted

PROPHYLAXIS OF ORGAN REJECTION IN KIDNEY TRANSPLANT:

Mylimus is used in the treatment of organ rejection in patients who are receiving kidney transplant In this condition, Mylimus concomitant with azathioprine or Mycophenolate

PROPHYLAXIS OF ORGAN REJECTION IN LIVER TRANSPLANT:

Mylimus is used in the treatment of organ rejection in patients who are receiving liver transplant Mylimus with adrenal corticosteroids is taken in this condition

PROPHYLAXIS OF ORGAN REJECTION IN HEART TRANSPLANT:

Mylimus is used in the treatment of organ rejection in patients who are receiving heart transplant Mylimus with azathioprine or Mycophenolate and adrenal corticosteroid is used.

ADME PROPERTIES

ABSORPTION

The absorption of Mylimus is incomplete and irregular. The bioavailability of the drug in; Kidney transplant: 17±10%; liver transplant: 22±6; heart transplant: 23±9% Effect of food: Mylimus should be taken with or without food, because with food will decrease the bioavailability of Mylimus 0.5mg

DISTRIBUTION

The human plasma protein binding of Mylimus is approximately 99% Mylimus highly bound to plasma protein like albumin and alpha-1-acid glycoprotein

METABOLISM

Mylimus is largely metabolized by mixed function oxidase system, by cytochrome P-450 enzyme The main metabolites of Mylimus in human liver microsomes is 13-demethyl Mylimus 0.5mg

ELIMINATION

The route of elimination of Mylimus metabolites Feces 92.6% urine 2.3% The terminal half-life of the drug in; Kidney transplant: 19 hours Liver transplant: 12 hours Heart transplant: 24 hours In pediatric liver transplant: 11.5±3.8 hours In pediatric kidney transplant: 10.2±5.0 hours

DOSAGE MANAGEMENT

DOSAGE AND ADMINISTRATION OF MYLIMUS 0.5MG

The usual dose of Tacrolimus for organ transplant-rejection therapy

KIDNEY TRANSPLANT
IMMEDIATE RELEASE

While combining with azathioprine, the initial dose of Tacrolimusis 0.1mg/kg taken orally for every 12 hours, initiate within 24 hours of surgery While combining with Mycophenolate mofetil or interleukin 2 receptor antagonist, initial dose is 0.05mg/kg for every 12 weeks

EXTENDED DOSE

Co administration of Tacrolimus with MMF, basiliximab and corticosteroid, starting dose is 0.15mg/kg/day orally as once daily Co administration of Tacrolimus with MMF, corticosteroids without basiliximab: Pre-operative dose: 0.1mg/kg/day within 12 hours before reperfusion Post-operative dose: 0.2mg/kg/day

LIVER TRANSPLANT

The initial dose of Tacrolimus is 0.05 to 0.075mg/kg should be taken as orally for twice daily

HEART TRANSPLANT

The initial dose of Tacrolimus is 0.0375mg/kg orally as twice daily

IN PEDIATRIC
LIVER TRANSPLANT

The initial dose is 0.075 to 0.1mg/kg as twice daily In immediate release, Tacrolimusshould be taken as twice daily, whereas in case of extended release the dose should be taken as once a time Tacrolimus should be taken on an empty stomach. Grape juice must be avoided during Mylimus administration

SIDE EFFECTS
MYLIMUS CAUSES SIDE EFFECTS

IN KIDNEY TRANSPLANT
Nervous system: tremor, headache, insomnia, paresthesia, dizziness. Gastrointestinal: diarrhea, nausea, constipation, vomiting, dyspepsia. Cardio vascular: hypertension, chest pain. Urogenital: creatinine increased, urinary tract infection. Metabolic and nutritional: hypophosphatemia, hypomagnesemia, hyperlipemia, hypo/hyperkalemia, diabetes mellitus, hyperglycemia, edema. Blood: anemia, leucopenia. Miscellaneous: infection, peripheral edema, asthenia, abdominal pain, fever, back pain. Pulmonary: dyspnea, cough. Muscle: arthralgia. Skin: rash, Pruritus. Injury: post-procedural pain, incision site complication, graft dysfunction.

IN LIVER TRANSPLANT
Nervous system: tremor, headache, insomnia, paresthesia, dizziness. Metabolic and nutritional: hypophosphatemia, hypomagnesemia, hyperlipemia, hypo/hyperkalemia, diabetes mellitus, hyperglycemia, edema. Blood: anemia, leucopenia, thrombocytopenia. Miscellaneous: infection, peripheral edema, asthenia, abdominal pain, fever, back pain, ascites. Pulmonary: dyspnea, cough, pleural effusion, atelectasis. Gastrointestinal: diarrhea, nausea, constipation, vomiting, dyspepsia, LFT abnormal. Cardio vascular: hypertension, chest pain. Urogenital: creatinine increased, urinary tract infection, kidney abnormal, BUN increased, oliguria Incision site complication, graft dysfunction, post-procedural pain. Musculoskeletal: arthralgia. Skin: rash, Pruritus.

IN HEART TRANSPLANT
CVS: hypertension, pericardial effusion. Whole body: CMV infection. Metabolic disorders: diabetic mellitus, hyperglycemia, hyperlipemia. Hemic and lymphatic system: anemia and leucopenia. Urogenital: kidney function abnormal and urinary tract infection. Respiratory: bronchitis. Nerve system: tremor.

SOME ADVERSE REACTIONS
Lymphoma, serious infections, polyoma virus infections, CMV infections, new onset of diabetes, nephrotoxicity, neurotoxicity, hyperkalemia, hypertension, anaphylactic reactions, myocardial hypertrophy, pure red cell aplasia, gastrointestinal perforation

PRECAUTION

PRECAUTIONS AND WARNING

Elevate the risk of infection and lymphoma, latent virus activation Risk of post-transplant diabetes mellitus Discontinue cyclosporine 24 hours before taking Mylimus 2mg

Hypertension occurs Caution with use, in concomitant with nephrotoxicity or calcium channel blockers Myocardial hypertrophy Care should be taken while using CYP3A inhibitors and inducers Monitor blood glucose level Nephrotoxicity and neurotoxicity Risk of viral, fungal, bacterial infection due to immunosuppressant activity of Mylimus QT prolongation

DRUG INTERACTION

Mylimus is metabolized by CYP3A enzymes, by inhibiting these cytochrome enzymes leads to increasing plasma concentration of Mylimus CYP3A inducers: may decrease the concentration of Mylimus Mycophenolic acid products: increase exposure to Mycophenolic acid Grape fruit/grape fruit juice: this will prohibit CYP3A enzymes, leads to increase the Mylimus whole blood trough concentrations Protease inhibitors: increase the concentration of Mylimus 1mg

Anti-fungal agents: depending on whole blood concentration of Mylimus , anti-fungal drugs are used. While concomitant voriconazole or posaconazole with Mylimus 0.5mg, the dose of Mylimus decreased to one-third of initial dose Calcium channel blockers: inhibit CYP3A enzymes, increase the concentration of Mylimus Anti-bacterial: erythromycin, clarithromycin, troleandomycin, chloramphenicol are inhibit CYP3A enzyme, leads to elevate concentration of Mylimus 2mg

Anti-mycobacterial: are rifampin and rifabutin; induce CYP3A enzymes causes decrease the Mylimus concentration Anti-convulsant: decrease the concentration of Mylimus St. Johns wort: decrease the concentration of Mylimus Gastric acid regulator and suppressor: increase the concentration of Mylimus 2mg

CONTRAINDICATION

Hypersensitivity reaction or anaphylactic reactions occurs

PREGNANCY  & LACTATION

Pregnancy category: C Mylimus is crosses the placenta, so there is possibilities of risk; Premature delivery risk, neonatal hyperkalemia, renal dysfunction Mylimus should be safely use in pregnancy condition; there is a chance of getting fetus harm, malformations etc Breast feeding is not recommended

STORAGE

Mylimus is stored at room temperature 25°C (77°F); excursions permitted to 15°C to 30°C (59°F to 86°F).

MISSED DOSE

Mylimus , if patient fail to take the dose of Mylimus 2mg, must consult with medical practitioner To avoid the illness produced by Mylimus , do not double the dose and the missed dose should be skipped and follow the regular schedule