Tacrolimus

Introduction

Tacrolimus is an immunosuppressive drug used to prevent rejection in organ transplantation, especially kidney transplantation. It is a calcineurin inhibitor that blocks the production of interleukin-2 (IL-2), a necessary component of the immune response, thereby preventing the immune system from attacking a transplanted organ.

Uses_for

Tacrolimus is used for the prevention of kidney, heart, and liver graft rejection. It is also used to treat severe rheumatoid arthritis and a certain skin disease (atopic dermatitis).

Brand Name	Tacrolimus
Type
Weight
Generic	Tacrolimus
Manufacturer
Available in	English বাংলা

Mechanism of Action

Tacrolimus inhibits the production of the interleukin-2 (IL-2) by blocking the calcineurin enzyme. By blocking this enzyme, tacrolimus prevents the production of interleukin-2, which the body needs to activate the T-cells of the immune system. This inhibits the immune system from attacking the transplanted organ and helps to prevent rejection of the organ.

How Long Does It Take to Work?

Tacrolimus may begin to take effect within 2-4 days of administration, but it may take several weeks for it to achieve its full effect. This time varies depending upon body weight, dosage, and the type of organ being transplanted.

Absorption

Tacrolimus is absorbed from the gastrointestinal tract and has a bioavailability of about 50%.

Route of Elimination

Tacrolimus is eliminated principally through the bile into the feces and to a lesser extent into the urine. It is metabolized by the liver through several pathways.

Dosage

The dosage of Tacrolimus required is dependent upon the type of organ being transplanted. The usual dose for a kidney transplant is 0.15-0.3mg/kg. For a heart transplant, it is 0.3-0.6mg/kg. For a liver transplant, it is 0.7-0.9mg/kg.

Administration

Tacrolimus is available in oral and intravenous formulations. It is usually taken twice daily. It can also be given once daily, depending on the patient's needs.

Side_Effect

Tacrolimus may cause side effects such as headache, diarrhoea, nausea, vomiting, constipation, dizziness, abdominal pain, fever, joint pain, cough, and rash. It may also cause high blood pressure, high cholesterol, hyperglycemia, tremors, edema, and liver toxicity.

Toxicity

Overdoses of Tacrolimus can cause symptoms such as nausea, abdominal pain, vomiting, diarrhoea, confusion, decreased urine output, and seizures. Treatment of overdose includes supportive care and may require the administration of activated charcoal.

Precautions

Tacrolimus should be used with caution in patients with kidney or liver disease, those with diabetes, and in geriatric patients. It should also be used with caution in patients taking other immunosuppressants, radiation therapy, or other medications.

Interactions

Tacrolimus may interact with antibiotics, antifungals, HIV medications, seizure medications, and other immunosuppressants, as well as with some supplements and vitamins.

Disease Interaction

Tacrolimus may interact with some diseases such as kidney or liver diseases, diabetes mellitus, HIV, and congestive heart failure.

Drug Interaction

Tacrolimus may interact with some drugs such as antibiotics, antifungals, HIV medications, seizure medications, and other immunosuppressants, as well as with some vitamins and supplements.

Food Interactions

Tacrolimus may interact with some foods, including grapefruit and grapefruit juice, as well as caffeine. Consult your doctor or pharmacist for additional information.

Pregnancy Use

Tacrolimus is not recommended for use during pregnancy. It may cause harm to an unborn baby if taken while pregnant.

Lactation Use

Tacrolimus is not recommended for use in nursing mothers. It may cause harm to a nursing infant.

Acute_overdose

Symptoms of an acute overdose may include nausea, abdominal pain, vomiting, diarrhoea, confusion, decreased urine output, and seizures. Treatment of overdose includes supportive care and may require the administration of activated charcoal.

Contraindication

Tacrolimus is contraindicated in patients with an allergy to macrolide antibiotics.

Use Direction

Tacrolimus should be taken exactly as prescribed by the doctor. The patient should not take more or less than the prescribed dose. The patient should also take the medication at the same time each day.

Storage Condition

Tacrolimus should be stored at room temperature, away from moisture and heat. Do not freeze the medication. Do not store it in the bathroom.

Volume of Distribution

Tacrolimus has a volume of distribution of 16-18 L/kg

Half Life

The half-life of tacrolimus is typically 12 to 24 hours, but may vary depending on body weight, drug interactions, and kidney function.

Clearance

Tacrolimus is mainly cleared by the kidneys, and its clearance rate is about 16-18ml/minute/kg.

See in details version Tacrolimus also Tacrolimus in bangla

Some Frequently Asked Questions About Tacrolimus