Tacrolimus (Intravenous)

Administered as an injection, Tacrolimus works by suppressing the immune system so that it does not reject a transplanted organ.

Overview

Tacrolimus is a medication that is prescribed to patients that have had an organ transplant, to prevent the body from rejecting the organ. It is typically administered to those that have received new organs such as kidneys, livers and hearts and works by controlling the body's immune system to stop it from attacking the organ.

Our bodies produce millions of white blood cells, which are essential to our health and our ability to fight off diseases and infections. However, after a transplant, the white blood cells can treat the new organ as an “invader” and try to destroy it in order to protect the body.

Tacrolimus works by suppressing the immune system so that it isn't strong enough to fight the organ, eventually leading to acceptance by the body.

It is part of a family of drugs called immunosuppressants and is often prescribed to the patient along with a number of other prescription-only steroids. Patients will be closely monitored while taking this medication and other that are prescribed along with it, as there is the potential for side effects. It is also important that the body's reaction to the transplanted organ is monitored regularly for success. If the body is still rejecting the organ, other treatments may be added.

This medication is also sold and marketed under the brand name Prograf in the United States.

Conditions Treated

  • Prevention of rejection of transplanted organ

Type of Medicine

  • Intravenous

Side Effects

Tacrolimus is an exceptionally strong medication and there is a strong likelihood that patients will experience some of the reported side effects. Patients that have just started a course of this medication will be more prone to various side effects as their bodies adapt to the drug being in their systems. Usually, mild side effects are nothing to worry about and don't affect everyone. However, patients should always be mindful of how their bodies react to this drug and, if symptoms persist, they should contact their doctors for advice. As Tacrolimus is administered by a doctor, the patient will be closely monitored for adverse reactions, with tests taken from the patient during each sitting. If the body does not respond well to this medication, a doctor may decide on an alternative treatment.

Common side effects include:

  • Nausea
  • Vomiting
  • Tiredness and exhaustion
  • Headache
  • Infection
  • Tremor
  • High blood pressure (hypertension)
  • Impaired renal function
  • Constipation
  • Diarrhea
  • Stomach cramps and pain
  • Interrupted sleep patterns (insomnia)
  • Urinary tract infections such as cystitis
  • Hypophosphatemia
  • Peripheral edema
  • Asthenia

Less common - and potentially serious - side effects include:

  • Lymphoma due to immunosuppression - this is particularly likely to happen to the skin
  • Vulnerability to bacterial, fungal, protozoal and viral infections
  • Diabetes – those of African American or Hispanic have been found to be particularly at risk from developing this condition
  • Hypertension

Side effects are not limited to the above and patients should always be aware of any other changes to the body or mental state while taking this drug. Other changes may occur.

Dosage

The dosage your doctor sets will usually depend on your individual medical history and a number of other factors, mainly your body weight. Before deciding on the most appropriate dosage, your doctor will discuss details of your medical history with you, including any conditions you may have, or have suffered from in the past. You will also need to be weighed in order to calculate your dosage.

The initial dose of injection should be given to patients is 0.03 to 0.05 mg per kilogram of body weight per day. This should be administered into a vein in the arm by a doctor.

Adult patients are usually given a lower dose of the drug.

Intravenous administration is usually only given to those that are unable to take the drug orally for whatever reason. A doctor will look to convert the patient from intravenous administration to oral tablets in as quick a timeframe as possible. This transfer is usually recommended to take place after 2 to 3 days.

Intravenous dosages are not intended for long-term use, as the drug enters the bloodstream quicker through this route and is therefore likely to increase the chances of developing side effects or health complications.

It is important that each dose of this medication is taken at the correct time. The intravenous administrations will be carried out by a trained healthcare or medical professional, so, therefore, it is very important that patients stick to their hospital appointments. The drug is most effective when it is taken at the times recommended by your doctor; leaving too long between doses can lead to side effects, withdrawal symptoms or cause the drug to be less effective at treating your condition.

Interactions

There are some other drugs that can interact with this one. This basically means that, when taken together, these drugs can cause a reaction inside the body, leading to worsened side effects and even danger to health. Interactions are grouped into three categories, depending on the severity of their reaction when mixed together - minor interactions, moderate interactions and major interactions. Drugs with minor interactions may still be suitable for taking at the same time. However, the doctor may recommend altering the dosage of either medication to lessen the impact of any reaction.

Those with major interactions should not be taken together as their intended effects may become nullified and conditions can become worse as a result. The risk of taking drugs with major interactions has been found to outweigh any potential health benefit in all but the most extreme of circumstances.

There are more than 500 drugs that have some form of interaction with tacrolimus, including those from mild to severe. Of these drugs, there are a large number of medicines, listed below, which have a major reaction with tacrolimus. If you are taking any of these medications, you must tell your doctor. Failure to do so may result in serious health complications and side effects that could turn out to be life-threatening.

  • Acetaminophen, aluminum hydroxide, aspirin, caffeine, magnesium hydroxide
  • Acetaminophen, aspirin
  • Acetaminophen, aspirin, caffeine
  • Acetaminophen, aspirin, caffeine, salicylamide
  • Acetaminophen, aspirin, diphenhydramine
  • Acetaminophen, aspirin, phenylpropanolamine
  • Acetaminophen, caffeine, magnesium salicylate
  • Acetaminophen, caffeine, magnesium salicylate, phenyltoloxamine
  • Acetaminophen, caffeine, phenylpropanolamine, salicylamide
  • Acetaminophen, caffeine, phenyltoloxamine, salicylamide
  • Acetaminophen, chlorpheniramine, phenylephrine, salicylamide
  • Acetaminophen, magnesium salicylate
  • Acetaminophen, magnesium salicylate, pamabrom
  • Acetaminophen, phenyltoloxamine, salicylamide
  • Acetaminophen, salicylamide
  • Acyclovir
  • Adalimumab
  • Adefovir
  • Aluminum hydroxide, aspirin, calcium carbonate, magnesium hydroxide
  • Amikacin
  • Amiloride
  • Amiloride, hydrochlorothiazide
  • Amiodarone
  • Amoxicillin, clarithromycin, lansoprazole
  • Amoxicillin, clarithromycin, omeprazole
  • Amphotericin b
  • Amphotericin b cholesteryl sulfate
  • Amphotericin b lipid complex
  • Amphotericin b liposomal
  • Anagrelide
  • Arsenic trioxide
  • Artemether, lumefantrine
  • Aspirin
  • Aspirin, brompheniramine, dextromethorphan, phenylpropanolamine
  • Aspirin, butalbital
  • Aspirin, butalbital, caffeine
  • Aspirin, butalbital, caffeine, codeine
  • Aspirin, caffeine
  • Aspirin, caffeine, dihydrocodeine
  • Aspirin, caffeine, orphenadrine
  • Aspirin, caffeine, propoxyphene
  • Aspirin, caffeine, salicylamide
  • Aspirin, calcium carbonate
  • Aspirin, carisoprodol
  • Aspirin, carisoprodol, codeine
  • Aspirin, chlorpheniramine, dextromethorphan
  • Aspirin, chlorpheniramine, dextromethorphan, phenylpropanolamine
  • Aspirin, chlorpheniramine, phenylephrine
  • Aspirin, chlorpheniramine, phenylpropanolamine
  • Aspirin, citric acid, sodium bicarbonate
  • Aspirin, codeine
  • Aspirin, diphenhydramine
  • Aspirin, diphenhydramine, phenylpropanolamine
  • Aspirin, dipyridamole
  • Aspirin, hydrocodone
  • Aspirin, meprobamate
  • Aspirin, methocarbamol
  • Aspirin, omeprazole
  • Aspirin, oxycodone
  • Aspirin, pentazocine
  • Aspirin, phenyltoloxamine
  • Aspirin, pravastatin
  • Aspirin, pseudoephedrine
  • Bacitracin
  • Baclofen, flurbiprofen, lidocaine topical
  • Balsalazide
  • BCG
  • Bedaquiline
  • Benzoic acid, hyoscyamine, methenamine, methylene blue, phenyl salicylate
  • Benzoic acid, methenamine, sodium salicylate
  • Bepridil
  • Betrixaban
  • Boceprevir
  • Botulism immune globulin
  • Bromfenac
  • Caffeine, magnesium salicylate
  • Caffeine, pheniramine, phenylephrine, sodium citrate, sodium salicylate
  • Capreomycin
  • Celecoxib
  • Ceritinib
  • Certolizumab
  • Chlorpheniramine, ibuprofen, pseudoephedrine
  • Choline salicylate
  • Choline salicylate, magnesium salicylate
  • Cidofovir
  • Cisapride
  • Cisplatin
  • Citalopram
  • Clarithromycin
  • Clotrimazole
  • Clozapine
  • Colchicine
  • Colchicine, probenecid
  • Colistimethate
  • Crizotinib
  • Cyclosporine
  • Cytomegalovirus immune globulin
  • Dalfopristin, quinupristin
  • Dasabuvir, ombitasvir, paritaprevir, ritonavir
  • Deferasirox
  • Dextromethorphan, quinidine
  • Diatrizoate
  • Diatrizoate, iodipamide
  • Diclofenac
  • Diclofenac, misoprostol
  • Diflunisal
  • Diphenhydramine, ibuprofen
  • Diphenhydramine, magnesium salicylate
  • Diphenhydramine, naproxen
  • Disopyramide
  • Dofetilide
  • Dolasetron
  • Dronedarone
  • Droperidol
  • Droperidol, fentanyl
  • Edoxaban
  • Efavirenz
  • Efavirenz, emtricitabine, tenofovir
  • Emtricitabine, lopinavir, ritonavir, tenofovir
  • Emtricitabine, nelfinavir, tenofovir
  • Erythromycin
  • Erythromycin, sulfisoxazole
  • Escitalopram
  • Esomeprazole, naproxen
  • Etanercept
  • Etidronate
  • Etodolac
  • Famotidine, ibuprofen
  • Fenoprofen
  • Fingolimod
  • Fluconazole
  • Flurbiprofen
  • Foscarnet
  • Gallium nitrate
  • Gatifloxacin
  • Gentamicin
  • Golimumab
  • Grepafloxacin
  • Halofantrine
  • Haloperidol
  • Hydrochlorothiazide, spironolactone
  • Hydrochlorothiazide, triamterene
  • Hydrocodone, ibuprofen
  • Hyoscyamine, methenamine, methylene blue, phenyl salicylate
  • Hyoscyamine, methenamine, methylene blue, phenyl salicylate, sodium biphosphate
  • Ibandronate
  • Ibuprofen
  • Ibuprofen, oxycodone
  • Ibuprofen, phenylephrine
  • Ibuprofen, pseudoephedrine
  • Ibutilide
  • Iloperidone
  • Imune globulin intravenous
  • Immune globulin intravenous and subcutaneous
  • Indomethacin
  • Infliximab
  • Influenza virus vaccine, h1n1, live
  • Influenza virus vaccine, live, trivalent
  • Iodamide
  • Iodipamide
  • Iodixanol
  • Iohexol
  • Iopamidol
  • Iopromide
  • Iothalamate
  • Ioversol
  • Ioxaglate
  • Ioxilan
  • Isoniazid, pyrazinamide, rifampin
  • Isoniazid, rifampin
  • Itraconazole
  • Ivabradine
  • Ivacaftor, lumacaft
  • Kanamycin
  • Ketoconazole
  • Ketoprofen
  • Ketorolac
  • Lansoprazole, naproxen
  • Leflunomide
  • Letrozole, ribociclib
  • Levomethadyl acetate
  • Lithium
  • Loperamide
  • Loperamide, simethicone
  • Lopinavir, ritonavir
  • Magnesium salicylate
  • Magnesium salicylate, phenyltoloxamine
  • Measles virus vaccine
  • Measles virus vaccine, mumps virus vaccine, rubella virus vaccine
  • Measles virus vaccine, mumps virus vaccine, rubella virus vaccine, varicella virus vaccine
  • Measles virus vaccine, rubella virus vaccine
  • Meclofenamate
  • Mefenamic acid
  • Meloxicam
  • Mesalamine
  • Mesoridazine
  • Methadone
  • Methotrexate
  • Methoxyflurane
  • Metrizamide
  • Mifepristone
  • Moxifloxacin
  • Mumps virus vaccine
  • Mumps virus vaccine, rubella virus vaccine
  • Nabumetone
  • Naproxen
  • Naproxen, pseudoephedrine
  • Naproxen, sumatriptan
  • Natalizumab
  • Neomycin
  • Netilmicin
  • Nilotinib
  • Olsalazine
  • Ombitasvir, paritaprevir, ritonavir
  • Oxaprozin
  • Pamidronate
  • Panobinostat
  • Papaverine
  • Pasireotide
  • Pentamidine
  • Phenylbutazone
  • Pimozide
  • Piroxicam
  • Poliovirus vaccine, live, trivalent
  • Polymyxin b
  • Posaconazole
  • Procainamide
  • Quinidine
  • Respiratory syncytial virus immune globulin
  • Ribociclib
  • Rifabutin
  • Rifampin
  • Rifapentine
  • Ritonavir
  • Rofecoxib
  • Rotavirus vaccine
  • Rubella virus vaccine
  • Salsalate
  • Saquinavir
  • Smallpox vaccine
  • Sodium salicylate
  • Sodium thiosalicylate
  • Sotalol
  • Sparfloxacin
  • Spironolactone
  • St. John's Wort
  • Streptomycin
  • Sulfasalazine
  • Sulindas
  • Talimogene laherparepvec
  • Telaprevir
  • Telavancin
  • Telithromycin
  • Temsirolimus
  • Teriflunomide
  • Thioridazine
  • Tobramycin
  • Tofacitinib
  • Tolmetin
  • Toremifene
  • Triamterene
  • Troleandomycin
  • Typhoid vaccine, live
  • Valacyclovir
  • Valdecoxib
  • Vancomycin
  • Vandetanib
  • Varicella virus vaccine
  • Vemurafenib
  • Venetoclax
  • Voriconazole
  • Yellow fever vaccine
  • Ziprasidone
  • Zoledronic acid
  • Zoster vaccine live

Always make sure you tell your doctor about your medical history. Other drugs may cause an interaction with this one - and your doctor will be able to make an informed judgement about whether this prescription is right for you or whether you would be better suited to another injectable substance.

Warnings

Tacrolimus is only to be administered by or under the supervision of a qualified doctor. Patients must not attempt administration themselves. When giving patients each injection of tacrolimus, the administration should be carried out in a medical environment that is equipped with supportive laboratory and medical resources. At each appointment, the doctor should monitor the patients progress closely and extensively and carry out tests for any of the possible serious side effects.

Disease interactions

As with other drugs, you should always tell your doctor about any other conditions you are suffering from, or have suffered from in the past. Also, be sure to mention if you have a family history of any conditions, particularly those that have been suffered from by close relatives. Tacrolimus may not be suitable for people with various other conditions and may make them worse. Likewise, any other medications that you are taking to treat these conditions may interfere with the drug's ability to suppress the immune system and support your newly transplanted organ. These seven disease interactions are:

  • Diabetes Mellitus
  • Qt Interval Prolongation
  • Renal Dysfunction
  • Hyperkalemia
  • Hypertension
  • Hepatic Dysfunction
  • Infections

There may be other conditions that could impact the ability of tacrolimus to help the body accept a new organ. Always tell your doctor, whether your condition is listed above or not.

Pregnancy and breastfeeding

There have been various studies into the safety of tacrolimus in pregnancy and during breastfeeding. Although there have not been found to be any risks of causing abnormalities and birth defects in the unborn fetus, there is an increased risk of the baby being born underweight or prematurely, if the mother is taking this drug. Users should proceed with taking injections of tacrolimus with caution. However, it has also been found that these risks are also reported by patients taking other immune system suppressants. Your doctor will likely recommend that you continue ahead with taking this drug, as the risk to your health is usually greater than to your unborn baby.

For nursing mothers, it is not known whether this drug causes harm to breastfeeding babies. It has been found to show traces in the breast milk, but no harm has yet been reported.

Food and lifestyle interactions

There are two known food and lifestyle interactions with tacrolimus. The first one is any products containing grapefruit. Patients should avoid eating or drinking grapefruit, grapefruit juice, and other grapefruit products, as they can cause an increase in the levels of tacrolimus in the body. This can be potentially dangerous for the patient, resulting in the same impact as taking an overdose of the drug. Side effects can also increase in severity if the patient consumes grapefruit while on this medication.

Patients who suffer from high blood pressure or hypertension should also not usually be put on a course of tacrolimus. This is because the drug can lead to an increased blood pressure so those that already suffer from the condition risk their condition becoming even more damaging to their health. Patients with high blood pressure that do get put on a course of tacrolimus should be very closely monitored by their doctors throughout the treatment, with blood pressure levels taken regularly.

Hispanic and African American patients

There has been found to be an increased risk of developing diabetes in patients of these descents, by recent medical studies. An alternative medication may be sought if you are thought to be at a higher risk of developing the disease.

Storage

The powder solution should be stored at room temperature, at no warmer than 25 degrees centigrade. It should also be kept in its original packaging until it is ready for use. Upon dilution of the powder, the solution should be used immediately. However, it can be stored at room temperature for up to 24 hours once the solution is diluted.

Disposal

As the medication will be kept by a trained doctor, it is usually only healthcare professionals that will need to dispose of this drug. It must be disposed of safely and responsibly at all times. There are various take back schemes that are available to people throughout the United States, which are the quickest and safest way to dispose of unwanted or expired medications. You can visit the website of the FFA to see what schemes are available in your areas. If there are no such schemes available, there are various other steps you can take to make sure your medication is disposed of in the safest and most responsible way.

First, you should not attempt to ground or dissolve your medical solution. As a general rule, you should take the medication out of its packet and mix it with something else that cannot be consumed, like cat litter or used coffee beans. Or even soil or dirt from the garden. Once you have mixed the substances together, you then need to put them in a plastic bag that can be tightly sealed. Seal it up, and then put it in the trash can with other garbage. You can then put it out with regular trash collections.

Store away from direct light and heat sources at all times - heat and light can seriously impair your medication's effectiveness.

Summary

Tacrolimus has been found to be a highly effective treatment for those that have just received an organ transplant. In most cases, the injectable solution helps to suppress the immune system and prevent the body's white blood cells from attacking a new organ. As long as healthcare professionals and patients follow all usage and aftercare instructions, the risk of severe side effects is low, and most people can take the course of medications without too much discomfort.

However, tacrolimus is a very strong substance, so the risks of developing some form of side effect is heightened for those patients that are vulnerable to developing conditions such as diabetes and high blood pressure. Therefore, close and strict monitoring of a patient throughout his or her course of treatment is highly recommended.

Patients can help to reduce their risks of contracting serious side effects by always telling their doctor about their medical histories before starting the prescription. This is because there are a large number of other drugs and conditions that have been found to cause a major reaction when mixed with tacrolimus, leading to unwanted and unknown side effects.

There are also various studies that suggest tacrolimus should not be used by expectant mothers or those that are trying to become pregnant. Although no birth defects have been found to be caused by the drug, there is an increased risk of premature birth or underweight babies within mothers that have taken the medication. However, in many cases, a doctor may judge that the risk to an unborn baby is less than that of the mother opting for a different medication.

Overall, tacrolimus is a fairly safe drug that can help patients successfully adapt to their new organs. Before starting a course of treatment, there will be lengthy consultations between patient and doctor to help determine the right dosage, and what other steroids it is to be administered with in order to maximise the treatment's chances of success.

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Last Reviewed:
January 30, 2018
Last Updated:
January 27, 2018
Content Source: