Tacrolimus Pharmacology


About Tacrolimus
Calcineurin Inhibitor, a macrolide, Immunosuppressant for prevention of graft rejection.
Mechanism of Action of Tacrolimus
It binds to specific receptors on T cells. It reduces peptidyl-prolyl isomerase activity by forming a complex with immunophilin FKBP-12 (FK506 binding protein).This leads to an increase in intracellular calcium that, in turn, causes a series of reactions inhibiting the transcription of several genes, mainly the cytokines (IL-2, IL-4, and IL-5). It also decreases the production of IL-8 receptor genes and inhibits the production of receptors for IgE molecules.
Pharmacokinets of Tacrolimus
Absorption- Moderately absorbed after oral administration.
Distribution- 75 to 99% bound to the plasma proteins.
Metabolism- Metabolized in the liver to its metabolites by demethylation and hydroxylation.
Excretion- Excreted via bile.
Onset of Action for Tacrolimus
Duration of Action for Tacrolimus
Half Life of Tacrolimus
Side Effects of Tacrolimus
1. Blurred vision
2. Liver problems
3. Kidney problems
4. Seizures
5. Tremors
6. Hypertension
7. Hypomagnesemia
8. Diabetes mellitus
9. Hyperkalemia
10. Itching
11. Insomnia
12. Confusion
13. Loss of appetite
14. Hyperglycemia
15. Weakness
16. Depression
17. Cramps
18. Neuropathy
19. Herpes zoster infections
20. Polyoma viral infections
Contra-indications of Tacrolimus
1. Hypersensitivity to the drug or any components of it
Special Precautions while taking Tacrolimus
1. Heart disease
2. Kidney disease
3. Diabetes
Pregnancy Related Information
Old Age Related Information
Use with caution
Breast Feeding Related Information
Children Related Information
Use with caution
Indications for Tacrolimus
1. Prophylaxis of organ rejection in patients receiving allogenic liver or kidney transplants
Interactions for Tacrolimus
Increased nephrotoxicity may result if tacrolimus is given with other potentially nephrotoxic drugs like cyclosporin.
Avoid concomitant use of potassium-sparing diuretics. Concomitant use of drugs which inhibit the cytochrome P450 (CYP3A) potentiate the effects of tacrolimus.
Typical Dosage for Tacrolimus
Kidney transplantation- 0.2mg/kg/day in adults as two divided doses.
Liver transplantation- 0.10-0.15mg/kg/day in two divided doses.
Maintenance dosage should be individualized so as to maintain whole blood concentration between 5-20 ng/ml.
Children- Generally need doses 1.5 to 2 times greater than those in adults.
Schedule of Tacrolimus
Storage Requirements for Tacrolimus
Store it at room temperature and away from excess heat and moisture. Keep out of reach of children.
Effects of Missed Dosage of Tacrolimus
Take the missed dose as soon as noticed and if it is the time for next dose then skip the missed dose. Continue the regular schedule. Do not double the dose.
Effects of Overdose of Tacrolimus
Give symptomatic and supportive treatment.

Home Delivery for Tacrolimus in Your City

Medicine India is just a publishing medium for medicine related information and does not provide services or sales of medicines including tacrolimus.

However, we do publish a comprehensive directory of Pharmacies, Chemists and Druggists in cities all over India. You can use this directory to find the medicine stores in your city (or area) that provide home delivery services for tacrolimus and other medicines and health products. Home delivery services for tacrolimus may be free or they may cost you depending on the pharmacy and the minimum order requirements. It would be best to get this clarified while placing the order.

Please be aware that you should take tacrolimus only if a doctor has recommended or prescribed it. Some or all pharmacies who provide a home delivery service for medicines might insist on a prescription for tacrolimus before they complete the sale. You can get this information while placing the order for tacrolimus with the pharmacy.

Tacrolimus is a generic medicine name and there are several brands available for it. Some of the brands for tacrolimus might be better known than tacrolimus itself. If the pharmacy that's willing to deliver medicines to your home doesn't have tacrolimus in stock, you can ask for one of the branded alternatives for tacrolimus.