Download TACROLIMUS prepared by Turkeyah Al

TACROLIMUS
prepared by
Turkeyah Al-Backer
Tacrolimus is a potent macrolide
immunosuppressant derived from
streptomyces tsukubaensis,and has
similar actions to those of
cyclosporine.It is used to prevent or
reserve rejection in patients receiving
organ transplants.
Mechanism of Action:
*Tacrolimus binds to FK-binding
protein,inhibiting cacineurin, a
cytoplasmic phosphatase.
*Calineurin regulates the ability of
the nuclear factor of activated T
cells to translocate the nucleus and
increase the production of cytokines.
*By this way,tacrolimus inhibit
the synthesis of cytokines that
normaly occur in response to T
cell activation..
Pharmacokinetics:
*administrated orally or
intravenously.
*oral absorption is in complete
*absorption is decrease if drug is
taken with high fat or high
carbohydrate meals.
*highly bound to serum protein.
*highly concentrated in the
erythrocyte.
*metabolized in the liver by
CYTP3A4
*most of the drug and its
metabolites are found in the
feces
*renal excretion is very low
Clinical Uses:
*organ transplantation especially in
kidney and liver transplantation
*oral psoriasis
*atopic dermatitis
*glomerular kidney disease
*hepatitis
*inflammatory bowel disease
*mysthenia gravis
Adverse Effects:
*cacinogenicity
*sever anemia due to selective
depression of erythropiosis
*post transplant diaetes mellitus
*hypertrophic cardiomyopathy
*nephrotoxicity
*peripheral neuropathy
*lentigines(small pigmented
macules in the skin)
Drug-Drug Ineraction:
*anti-bacterial
drugs.e.g.erythromycin
*anti-viral drugs
*calcium channels
blockers.e.g.nifedipine
*danazole
*all these drugs increase the level
of tacrolimus
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