- Tacrolimus, a calcineurin inhibitor, is a medication classified under the category of immunosuppressants.ṣ
- Its function is to decrease the body’s immunity.
- These drugs suppress the recipient’s immune system and prevent graft rejection, thus improving the prognosis of operations like kidney transplantation.
- Tacrolimus is used in several other medical conditions where the goal is to suppress the body’s immune system.
- Because it is an immunosuppressant, it is used as an anti-kidney rejection drug in kidney transplant patients. It has greatly improved the prognosis of kidney transplant cases.
- It is also used in post-transplant patients with other organs like the heart and liver.
- Tacrolimus is a powerful drug for treating a condition called nephrotic syndrome, especially steroid-resistant nephrotic syndrome, which is a very difficult disease to treat.
- It is used to treat Systemic lupus erythematosus, especially in pregnant females where the choice of drugs becomes very limited.
- It is used in the treatment of various other diseases like Psoriasis, where suppression of the immune system is a goal.
- The dose of Tacrolimus to be taken depends on the disease it is used for and the time for which the treatment has been going on.
- The duration of treatment depends on many factors, like the indication of use and the severity of the condition.
- For all the diseases, high Tacrolimus levels are given initially, but it is not exceeded 50 ng/ml blood level. A blood level above 50 ng/ml can have hazardous consequences. A blood level below 12 ng/ml is desirable.
- It is usually prescribed twice daily at 9 am and 9 pm or consistently 12 hours apart.
For kidney transplant patients:
- For the first three months post-kidney transplantation, 8-12 ng/ml of blood Tacrolimus level is targeted.
- Over the subsequent three to six months, the levels should be kept between 5-8 ng/ml. Before six months, it should be 3-5 ng/ml.
- As time passes, Tacrolimus levels are reduced from the initial high levels. This is done to prevent its side effects.
For the intravenous dosage forms:
- The ideal initiation intravenous dose of Tacrolimus for renal and liver transplant patients is 0.03-0.05 mg/kg/day.
- Tacrolimus is metabolised by the liver. So its dose needs to be reduced in cases of liver diseases where the liver functions are compromised. Your doctor will adjust the doses accordingly.
- The paediatric dose is higher than the adult dose.
Please note that the data provided here is purely for informative purposes. Please follow your doctor’s prescription for the dose of Tacrolimus to avoid side effects.
Guidelines for use:
- How to use Tacrolimus depends on the form of Tacrolimus your doctor has prescribed for you and the condition for which it has been prescribed. Given are some guidelines for the usage of Tacrolimus:
- If you use Tacrolimus in an ointment form, make sure your skin is dry and apply a thin layer. You should avoid contact with water for the first thirty minutes of application. After that, please wash your hands thoroughly with soap and water after applying the ointment, and ensure it does not touch your eyes or nose. If, however, it does happen accidentally, rinse it thoroughly with a lot of water.
- Tacrolimus can make your skin susceptible to sun damage. When using it in an ointment form, avoid sun exposure and make sure to use sunscreen with a good sun protection formula if you are stepping out into the sunlight.
- If you are using the capsules or tablets, make sure to swallow them with half a glass of water. Do not bite into them or break them, as it may interfere with their effectiveness.
- Capsules or tablets should be taken on an empty stomach, 1 hour before or 2 hours after a meal because this improves its effectiveness. However, some schools of thought state that Tacrolimus dosage does not depend on food intake.
- Consuming it every day at the same time will prevent you from forgetting to take the dose.
- Store the capsules or tablets at a temperature of 15-20 degrees celsius, away from sunlight and moisture.
- Should be stored out of reach of children
What if I miss a dose?
- Should you miss a dose, please contact your doctor for advice. Skipping a few doses of Tacrolimus can decrease its levels in the blood leading to treatment failure.
What if I don’t experience any improvement?
- If you do not experience any improvement for the first two weeks of its use, please don’t hesitate to get in touch with your doctor as he might prescribe some other medication that might be more suitable for you.
The blood concentration levels of Tacrolimus are strictly monitored at regular intervals while on Tacrolimus therapy. It helps prevent adverse events related to its overdose or toxicity and is also helpful for dose adjustment.
- Patients administered with an injectable form of Tacrolimus should be closely monitored for the first thirty minutes for adverse reactions. If any sign of an anaphylactic reaction occurs, it should be stopped immediately. It usually occurs with formulations containing castor oil as one of the ingredients.
- The intravenous dose should be discontinued, and the oral dose should be started as soon as the patient can tolerate it.
- You should take this drug only under the supervision of an expert doctor who has been using it for a long time.
- Do not consume grapefruit while on Tacrolimus, as it can increase its levels in the blood and increase the incidence of side effects.
- The safety of Tacrolimus usage is not clearly established in pregnancy. However, if prescribed, it should be monitored closely by an expert doctor.
It is not necessary that you will face these side-effects while on Tacrolimus. But staying vigilant is safer.
Short-term side effects:
- Headaches and tremors
- Insomnia (inability to fall asleep)
- Nausea (a feeling of impending vomiting) and diarrhoea
- Increased blood glucose levels
- Increased blood pressure or increased required for antihypertensives
- Increased cholesterol levels
- Neurological side effects such as neuropathies and PRES. The full form of PRES is Posterior Reversible Encephalopathy Syndrome. It is a neurological condition characterised by headaches, seizures, altered cognition, and diminished vision.
- Tiredness and fatigue
- Itching, burning sensation, irritation, and rash can occur when using Tacrolimus ointment.
- Signs of infections like fever, chills, or sore throat. If you notice any of these symptoms, consult your doctor.
Long term side effects:
- Tacrolimus is a nephrotoxic drug. If Tacrolimus therapy is continued for a long time or its levels are not supervised, it leads to kidney damage
- Some patients have developed cancers, especially skin cancers, because of long-term exposure to high doses of Tacrolimus.
Certain drugs interact with Tacrolimus, causing its levels to increase. Such drugs should be avoided or used with caution if a patient is on Tacrolimus therapy.
- Antibiotics like Azithromycin and Clarithromycin, if taken simultaneously with Tacrolimus, increase its levels.
- There is a drug called Diltiazem that is used to treat heart diseases. This drug, if taken simultaneously with Tacrolimus, increases its levels significantly.
- Anticonvulsant drugs like Phenytoin, Valproic acid, and Carbamazepine lower Tacrolimus levels if taken while on Tacrolimus therapy.
- An anti-tubercular drug called Rifampicin should be used with caution while on Tacrolimus therapy because it reduces Tacrolimus levels
- Antifungal medications like Ketoconazole and Fluconazole cause a dramatic increase in Tacrolimus levels
- It is not recommended to use Tacrolimus simultaneously with Cyclosporine, another immunosuppressive medication. Cyclosporine intake should be stopped 24 hours before initiating Tacrolimus therapy
- If you are taking any of the medications mentioned above, please let your doctor know about it when he prescribes you Tacrolimus.
Why does Tacrolimus therapy need monitoring?
- Tacrolimus is one of the drugs that have a narrow therapeutic index.
- The therapeutic index is an indicator of drug safety. The wider the therapeutic index, the safer the drug.
- Drugs with a narrow therapeutic index need close monitoring as even a slight increase in dose can lead to adverse reactions and toxicity. This is because the difference between therapeutic level and toxic level is very less.
- The therapeutic level is the level below which the drug will not be effective, while the toxic level is the level above which the drug causes side effects or toxicity.
Brands of Tacrolimus available in India
- Generic Tacrolimus is manufactured by many pharmaceutical companies and sold under many brand names in India.
- It is advisable to always use the same generic product to avoid changes in Tacrolimus levels, so make sure that Tacrolimus looks exactly the same when you refill your prescription.
- It is made available by many pharmaceutical companies in India in tablet, capsule, suspension, injection, and ointment forms.
- Acroli and Acroli Forte by Psyco Remedies
- Cromus Forte by Segment Care
- Mustopic ointment by Systopic Laboratories Pvt. Ltd.
- Olmis and Olmis Forte by Unichem Laboratories Ltd.
- Tacrel and Tacrel-F by Zydus Cadila Healthcare Limited
- Tacroderm by Abbott Healthcare Pvt. Ltd.
- Tacro Kid by Elder Pharmaceuticals Pvt. Ltd
- Tacrotor by Torrent Laboratories Pvt. Ltd.
- Tacrovate Forte by Ochoa Laboratories Pvt. Ltd.
- Tacroz by Glenmark Pharmaceuticals Ltd.
- Tacus Forte by Canbro Healthcare
- Tacrolimus by Ajanta Pharma Ltd.
- Crolim by Ranbaxy Laboratories Ltd.
- Seegraf by Micro Labs Ltd.
- Brand names for capsule form of Tacrolimus:
- Olmis Cap by Unichem Laboratories Ltd.
- Pangraf by Panacea Biotec Ltd.
- Tacloran by Wockhardt Limited
- Tacrograf by Biocon Limited
- Tacromus by Zydus Cadila Healthcare Ltd.
- Tested by Steadfast Medishield Pvt. Ltd.
- Vingraf by Emcure Pharmaceuticals Ltd.
Frequently asked questions (FAQs)
Q: Why is Tacrolimus prescribed?
- You might have always heard that we need to increase our body’s immunity to get stronger.
- However, there are instances where we need to decrease the body’s immunity to protect it, like in the case of kidney transplantation.
- When a kidney is grafted from a donor to a recipient (whose kidneys have lost their function), the recipient’s body recognises it as a foreign substance and activates its immune system against it.
- This situation can prove detrimental and is one of the major reasons for the failure of kidney transplantation operation.
- In such a situation, immunosuppressant drugs like Tacrolimus are prescribed.
Q: Why is Tacrolimus called Superdrug?
- Tacrolimus is also called Superdrug, as it is one of the most potent immunosuppressants.
- Since it was discovered, it has been used to treat a wide variety of diseases.
- It is ten times more potent than Cyclosporine, another immunosuppressive drug.
Q: Why is Tacrolimus used for nephrotic syndrome?
- Nephrotic syndrome is a common kidney disease where immune system is involved
- It occurs in young children (newborn to 18 years of age), where the filtering pores of the kidney increase in size, leading to the passage of protein into the urine.
- Tacrolimus decreases the immune response and acts as a powerful drug to treat cases resistant to treatment with steroids
Q: Why is Tacrolimus used to treat SLE?
- SLE is an autoimmune disease that manifests as the patient’s immune system attacking its own organs.
- Tacrolimus suppresses the immune system in SLE patients, preventing it from attacking its own tissues.