Clinical Pharmacology Details


Tacrolimus


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Indications & Dose:

Liver transplant:



PO 0.10-0.15 mg/kg/day in divided doses q 12h Kidney transplant:  



PO 0.2 mg/kg/day in divided doses q12h


RENAL OR HEPATIC IMPAIRMENT: Initiate doses at low end of range; further reductions in dose may be required 

Contraindications:

Hypersensitivity to HCO-60 polyoxyl 60 hydrogenated castor oil (used in vehicle for injection), concomitant use with cyclosporine (see Interactions, Drugs)

Side Effects:

CNS: Coma, delirium, neurotoxicity (tremor, headache, changes to motor function, mental status and sensory function), paresthesia, seizures
CV: Hypertensign peripheral edema GI: Abdominal pain anorexia. constipation, diarrhea, elevated liver function tests, nausea, vomiting
GU: Nephrotoxicity
HEME: Anemia, leukocytosis, thrombocytopenia
METAB: Hyperglycemia, hvperkalemia (10-44%), hyperuricemia, hypokalemia. hpomagnesemia
MS: Back pain
RESP: Atelectasis, dyspnea, pleural effusion
SKIN: Pruritus, rash
MISC: Anaphylaxis (with injection), asthenia, fever, lymphoma, pain 

Cautions:

Precautions:

Impaired renal and hepatic function, hypertension, myocardial hypertrophy, Netherton’s syndrome (increased systemic absorption of ointment), topical use in chicken pox, shingles, herpes simplex, eczema herpeticum

Interaction:

Drugs


• Azole antifungals, bromocriptine, calcium channel blockers, cimetidine, danazol, ethinyl estradiol, GI prokinetic agents, macrolide antibiotics, nefazodone, omeprazole, protease
inhibitors: Decreased metabolism or increased bioavailability of tacrolimus


• Carbamazepine, phenobarbital, phenytoin, rifamycins: Decreased tacrolimus blood levels


• Cyclosporine: Additive/synergistic nephrotoxicity, do not coadminister, discontinue tacrolimus or cyclosporine for 24 hr before starting the other


• Live vaccines: Avoid use of live vaccines, vaccinations may be less effective


• Nephrotoxic agents (aminoglycosides, amphotericin B, cisplatin, ganciclovir): Potential for additive or synergistic nephrotoxicity


• Potassium-sparing diuretics: Increased risk of hyperkalemia


• St. John’s wort (hypericum perforatum): Potential for decreased plasma tacrolimus concentrations

Warnings:

Adverse Effects:

Lactations:

Pregnancy category C; excreted in breast milk, avoid nursing

Special Precautions:

Counselling:

Side Effects Or Adverse Reactions:

Patient And Carer Advice: