Tacrolimus

A potent macrolide immunosuppressant derived from Streptom yces tsukubaensis. It prevents or reverses rejection in patients receiving organ transplants. On weight basis tacrolimus is 10-100 times more potent than cyclosporine in inhibiting immune responses. Nephrotoxicity, neurotoxicity, and gastrointestinal complaints are its common side effects.


Adult Dose
Dose: 100 to 200 mcg/kg
Single Dose: 150 (150)
Frequency: 6 hourly
Route: PO/IV-Inf
Instructions: In liver transplant starting 6 hrs after transplantation.
Neonatal
Paedriatic
Characteristics
. It is of Synthetic origin. . The Molecular Weight of Tacrolimus is 821.00.
Contraindications
Tacrolimus is contraindicated in conditions like Hypersensitivity,Pregnancy.
Effects
The severe or irreversible adverse effects of Tacrolimus, which give rise to further complications include Hallucinations, Tachycardia, Confusion, Anxiety, Leucopenia, Renal failure, Hyperglycemia, Hypertension, Angina, Leucocytosis, Tremors, Oliguria, Renal insufficiency, Anuria, Tublar necrosis.Tacrolimus produces potentially life-threatening effects which include Coma, Convulsions, Anaphylactic shock, Renal failure, Neurotoxicity, Psychosis, Speech disorder, Tubular necrosis. which are responsible for the discontinuation of Tacrolimus therapy.The symptomatic adverse reactions produced by Tacrolimus are more or less tolerable and if they become severe, they can be treated symptomatically, these include Headache, Nausea, Diarrhea, Constipation.
Indications
Tacrolimus is primarily indicated in conditions like Atopic dermatitis, Kidney transplantation, Liver transplantation, and can also be given in adjunctive therapy as an alternative drug of choice in Graft versus host disease, Immune disorders, Liver transplant, Organ grafts, Renal transplant.
Interactions
Tacrolimus is known to interact with other drugs, the details of drug interactions is as follows:DrugDetailsSeverityOnsetManagementAmiloride (HCl)Amphotericin BIncreased risk of nephrotoxicity when amphotericin given with Tacrolimus.MajorClose monitorinrg required.AzapropazoneCarbamazepineCisplatinCladribineClarithromycinClarithromycin increases the serum concentration of tacrolimus by inhibiting CYP450 3A4-mediated hepatic metabolism results in increased toxicity.ModerateClosely monitor the plasma concentration of tacrolimus and renal function.Reduce the dose of tacrolimus if necessary. Azithromycin and dirithromycin is considered safer alternatives of clarithromycin.DanazolErgotamine (Tartrate)ergotamine may inhibit the metabolism of tacrolimus ErythromycinGanciclovir (Na)IsoniazidKetoconazoleMethylprednisoloneMumps VaccineConcurrent use may weaken the immune system.OxaliplatinYou should inform your doctor before using this combination.Do not start or stop any medicine without doctor or pharmacist approval.PhenobarbitonePhenytoin (Na)RifampicinRitonavirSevelamer HClreduced level of Tacrolimus is observed when co administered wth sevelamer HClclose monitoring of blood concentration is requiredSpironolactoneTriamtereneVORICONAZOLEVoriconazole may increase the serum concentration of tacrolimus by decreasing its metabolism. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects These interactions are sometimes beneficial and sometimes may pose threats to life. Always consult your physician for the change of dose regimen or an alternative drug of choice that may strictly be required.
Interfrence
Abnormal LFTs Increased level of Blood urea nitrogen (BUN) concentrationsIncreased concentration of creatinine kinase
Risks
Drug should not be given to Pregnant Mothers, and Neonates.If prescribing authority justifies the benefits of the drug against the possible damages he/she should reevaluate them and consult the reference material and previous studies.
Storage
Caps Store at room temperature. Protect from Moisture. Inj Store at room temperature, Below 25°C. Refrigeration and Freezing is not recommended. Protect from Sunlight.
Warnings
Care is required in patients with pre-existing renal impairment. Dosage should be adjusted according to whole blood or plasma trough concentrations in individual patients. Dosage reduction may be necessary in patients with hepatic impairment. Monitoring of blood concentrations of tacrolimus is recommended in all patients. Renal and hepatic function, blood pressure and hematological and cardiac function a s well as visual function should be monitored regularly
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