Tacrograf 0.5mg (Tacrolimus)
Tacrograf 0.5mg is available in capsule form; it is calcineurin inhibitor immunosuppressant drug Tacrograf 0.5mg is classified as macrolide antibiotic Tacrograf 0.5mg is used in combination with other medicines to protect the body from rejecting a transplanted organ like kidney, liver or heart
Tacrograf is available in capsule form; it is calcineurin inhibitor immunosuppressant drug Tacrograf is classified as macrolide antibiotic Tacrograf is used in combination with other medicines to protect the body from rejecting a transplanted organ like kidney, liver or heart
Mostly Tacrograf is concomitant with steroids, azathioprine, basiliximab or Mycophenolate mofetil Tacrograf is used for preventing organ rejection in organ transplant patients.
Tacrograf 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, Tacrograf 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:
Tacrograf is used in the treatment of organ rejection in patients who are receiving kidney transplant In this condition, Tacrograf concomitant with azathioprine or Mycophenolate
PROPHYLAXIS OF ORGAN REJECTION IN LIVER TRANSPLANT:
Tacrograf is used in the treatment of organ rejection in patients who are receiving liver transplant Tacrograf with adrenal corticosteroids is taken in this condition
PROPHYLAXIS OF ORGAN REJECTION IN HEART TRANSPLANT:
Tacrograf is used in the treatment of organ rejection in patients who are receiving heart transplant Tacrograf with azathioprine or Mycophenolate and adrenal corticosteroid is used.
The absorption of Tacrograf 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: Tacrograf should be taken with or without food, because with food will decrease the bioavailability of Tacrograf 0.5mg
The human plasma protein binding of Tacrograf is approximately 99% Tacrograf highly bound to plasma protein like albumin and alpha-1-acid glycoprotein
Tacrograf is largely metabolized by mixed function oxidase system, by cytochrome P-450 enzyme The main metabolites of Tacrograf in human liver microsomes is 13-demethyl Tacrograf
The route of elimination of Tacrograf 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 AND ADMINISTRATION OF TACROGRAF 0.5MG
The usual dose of Tacrolimus for organ transplant-rejection therapy
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
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
The initial dose of Tacrolimus is 0.05 to 0.075mg/kg should be taken as orally for twice daily
The initial dose of Tacrolimus is 0.0375mg/kg orally as twice daily
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 Tacrograf administration
TACROGRAF 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
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 Tacrograf
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 Tacrograf QT prolongation
Tacrograf is metabolized by CYP3A enzymes, by inhibiting these cytochrome enzymes leads to increasing plasma concentration of Tacrograf CYP3A inducers: may decrease the concentration of Tacrograf Mycophenolic acid products: increase exposure to Mycophenolic acid Grape fruit/grape fruit juice: this will prohibit CYP3A enzymes, leads to increase the Tacrograf whole blood trough concentrations Protease inhibitors: increase the concentration of Tacrograf
Anti-fungal agents: depending on whole blood concentration of Tacrograf , anti-fungal drugs are used. While concomitant voriconazole or posaconazole with Tacrograf 0.5mg, the dose of Tacrograf decreased to one-third of initial dose Calcium channel blockers: inhibit CYP3A enzymes, increase the concentration of Tacrograf Anti-bacterial: erythromycin, clarithromycin, troleandomycin, chloramphenicol are inhibit CYP3A enzyme, leads to elevate concentration of Tacrograf
Anti-mycobacterial: are rifampin and rifabutin; induce CYP3A enzymes causes decrease the Tacrograf concentration Anti-convulsant: decrease the concentration of Tacrograf St. Johns wort: decrease the concentration of Tacrograf Gastric acid regulator and suppressor: increase the concentration of Tacrograf
Hypersensitivity reaction or anaphylactic reactions occurs
PREGNANCY & LACTATION
Pregnancy category: C Tacrograf is crosses the placenta, so there is possibilities of risk; Premature delivery risk, neonatal hyperkalemia, renal dysfunction Tacrograf should be safely use in pregnancy condition; there is a chance of getting fetus harm, malformations etc Breast feeding is not recommended
Tacrograf is stored at room temperature 25°C (77°F); excursions permitted to 15°C to 30°C (59°F to 86°F).
Tacrograf , if patient fail to take the dose of Tacrograf , must consult with medical practitioner To avoid the illness produced by Tacrograf , do not double the dose and the missed dose should be skipped and follow the regular schedule