Sublingual Semaglutide and Tirzepatide are now available! Learn More

Tacrolimus 1.5 mg Rectal Suppository

The Tacrolimus 1.5 mg Rectal Suppository is a solid dosage form designed for insertion into the rectum. Upon administration, it dissolves or melts, facilitating the release of the active ingredient, tacrolimus, for local or systemic absorption. This formulation is specifically compounded to treat disease states such as inflammatory bowel disease, including ulcerative colitis and Crohn's disease, as well as for the prevention of organ rejection in patients who have undergone an allogeneic organ transplant. The rectal route of administration provides an alternative for patients who may not tolerate oral medications or require targeted delivery to the site of inflammation.

Want a different strength?
Click the Text Us button below.
To prescribe, you must be a verified prescriber.
To prescribe, you must be in a state where we hold an active out-of-state pharmacy license.
Starting at
Must be E-Prescribed
Get Started
Generate LeafletShow Leaflet
This medication requires a prescription from your doctor
Are you a prescriber? Sign Up
Trusted by 55,278 patients to date.
A group of faces of our past satisfied patients.
A svg symbol of a mortar and pestle with ingredients going in.
Custom made in our compounding labs.
Sliders that show the customization of ingredients.
Personalized treatment for better results.
User with a gear showing the personalization of the formulation.
All strengths and ingredients are tailored to your needs.
This medication is not available at retail pharmacies. It is compounded, and may be more effective at treating you or your patient.
Suppository
65d78108dc0fb489710dfafa
Thank you! Your submission has been received!
Oops! Something went wrong while submitting the form.
Loading icon rotating.
Thank you! Your submission has been received!
Oops! Something went wrong while submitting the form.

Dosing Calculator

Get general dosing information for a patient by using this calculator.
Thank you! Your submission has been received!
Oops! Something went wrong while submitting the form.
Loading icon rotating.
Thank you! Your submission has been received!
Oops! Something went wrong while submitting the form.

Formula Information

A small arrow pointing down

Tacrolimus is an immunosuppressive medication commonly used to prevent organ transplant rejection and to treat certain autoimmune conditions. The 1.5 mg Tacrolimus Rectal Suppository is a solid dosage form designed for rectal administration, where it dissolves or melts to release the active medication. This route of administration can be particularly beneficial for patients who are unable to take oral medications or for those who require targeted delivery to the rectal area.

When inserted into the rectum, the suppository allows the tacrolimus to be absorbed directly into the bloodstream or to exert its effects locally within the rectal tissue. This can be advantageous in minimizing systemic side effects while providing a high concentration of the drug to the affected area. The rectal route can also bypass the first-pass metabolism in the liver, which is particularly useful for drugs like tacrolimus that have a narrow therapeutic index and are extensively metabolized.

The 1.5 mg dose of Tacrolimus in the suppository form is carefully compounded to ensure uniformity and stability of the medication. This dosage form is used in the management of diseases where tacrolimus has shown efficacy, such as in inflammatory bowel diseases like ulcerative colitis, where local immunosuppression may be desired. It may also be used in patients with proctitis or other inflammatory conditions affecting the rectum. Additionally, systemic absorption through the rectal mucosa can provide therapeutic levels of tacrolimus for patients with conditions that are not limited to the rectal area.

It is important for both patients and prescribers to understand that the use of Tacrolimus Rectal Suppositories should be guided by careful consideration of the patient's overall health status, the indication for treatment, and the potential for systemic absorption. Monitoring of tacrolimus blood levels may be necessary to ensure therapeutic efficacy and to avoid toxicity. As with any medication, adherence to the prescribed regimen and awareness of potential side effects are crucial for optimal treatment outcomes.

At Bayview Pharmacy, our team of compounding pharmacists is dedicated to providing high-quality, customized medications to meet the unique needs of each patient. We are available to answer any questions and provide additional information to ensure the safe and effective use of Tacrolimus Rectal Suppositories. If you have any questions or require further assistance, please do not hesitate to reach out to us.

Drug Interactions

A small arrow pointing down

Tacrolimus is an immunosuppressive drug that is commonly used to prevent organ transplant rejection and to treat certain autoimmune conditions. When formulated as a 1.5 mg rectal suppository, tacrolimus is intended for local or systemic absorption through the rectal mucosa. It is important to consider potential drug interactions when prescribing or administering tacrolimus in any form, including rectal suppositories.

One of the major concerns with tacrolimus is its narrow therapeutic index and the potential for significant drug interactions that can either increase or decrease its blood levels, leading to toxicity or reduced efficacy, respectively. Drugs that inhibit the cytochrome P450 3A4 (CYP3A4) enzyme can increase tacrolimus blood concentrations. Examples of such inhibitors include, but are not limited to, ketoconazole, itraconazole, voriconazole, clarithromycin, erythromycin, and diltiazem. Patients and prescribers should be aware that co-administration of these drugs with tacrolimus may necessitate a reduction in the tacrolimus dose and careful monitoring of tacrolimus blood levels.

Conversely, drugs that induce CYP3A4 can decrease the blood levels of tacrolimus, potentially leading to graft rejection in transplant patients or treatment failure in patients with autoimmune conditions. CYP3A4 inducers include rifampin, rifabutin, carbamazepine, phenytoin, phenobarbital, and St. John's Wort. If a patient is taking any of these medications, an increase in the tacrolimus dose may be required, along with close monitoring of drug levels and patient response.

Additionally, tacrolimus can increase the risk of nephrotoxicity when used concurrently with other nephrotoxic drugs such as NSAIDs, aminoglycosides, and amphotericin B. Blood levels of tacrolimus should be monitored, and renal function should be assessed regularly when these drugs are used concomitantly. Patients should also be advised to maintain adequate hydration and report any signs of renal impairment.

Calcium channel blockers, such as verapamil and nifedipine, can also interact with tacrolimus, leading to increased tacrolimus levels and the potential for toxicity. Blood pressure and tacrolimus levels should be monitored when these drugs are used together. Grapefruit juice is known to inhibit CYP3A4 and should be avoided during tacrolimus therapy, as it can lead to unpredictable increases in tacrolimus blood levels.

It is also important to note that tacrolimus can affect the metabolism of other drugs. For example, it can increase the plasma concentrations of drugs metabolized by CYP3A4, such as certain statins, leading to an increased risk of myopathy or rhabdomyolysis. Patients should be monitored for signs and symptoms of these conditions if they are taking statins concomitantly with tacrolimus.

Given the complexity of potential drug interactions with tacrolimus, it is crucial for prescribers to review a patient's complete medication list, including over-the-counter drugs and herbal supplements, before initiating therapy with tacrolimus rectal suppositories. Pharmacists can play a key role in identifying and managing drug interactions to ensure safe and effective use of tacrolimus. If you have any questions or require further information regarding drug interactions with tacrolimus, please reach out to us at Bayview Pharmacy.

How Does it Work

A small arrow pointing down

The Tacrolimus 1.5 mg Rectal Suppository is a solid dosage form designed to be inserted into the rectum, where it dissolves or melts at body temperature. Upon administration, the suppository base, typically composed of a substance like cocoa butter or a synthetic substitute, begins to melt due to the warmth of the human body. As the base melts, the active ingredient, tacrolimus, is released into the rectal tissues.

Tacrolimus is a potent immunosuppressive medication that works by inhibiting the activity of T-lymphocytes, a type of white blood cell involved in the immune response. By doing so, tacrolimus reduces inflammation and modulates the body's immune system. This mechanism of action makes it particularly effective in treating conditions where the immune system is overactive, such as in the prevention of organ transplant rejection, and in certain autoimmune diseases like inflammatory bowel disease (IBD) when administered rectally.

In the context of rectal administration, tacrolimus suppositories are used primarily for their local effect. This route of administration can be especially beneficial for patients with IBD affecting the rectum and lower colon, as it allows for high concentrations of the medication to be delivered directly to the site of inflammation with minimal systemic absorption. This can lead to a reduction in the severity of symptoms such as pain, bleeding, and inflammation associated with conditions like ulcerative colitis or Crohn's disease. Additionally, the rectal route can be an alternative for patients who are unable to take oral medications or for those who require targeted therapy with fewer systemic side effects.

It is important for both patients and prescribers to understand that while tacrolimus suppositories can be effective for local treatment, they should be used with caution due to the potential for systemic absorption, which could lead to side effects typically associated with oral or intravenous tacrolimus. Monitoring of blood levels may be necessary to ensure that the drug remains within the therapeutic range, especially in patients who are also receiving systemic immunosuppressants.

For optimal results, patients should follow the specific instructions provided by their healthcare provider regarding the use of tacrolimus suppositories. This includes proper insertion techniques, frequency of administration, and storage conditions for the medication. As with any medication, adherence to the prescribed regimen is crucial for the effectiveness of the treatment.

If you have any questions or require further information about the Tacrolimus 1.5 mg Rectal Suppository, please do not hesitate to reach out to us at Bayview Pharmacy. Our team of compounding pharmacists is here to provide support and guidance to ensure the safe and effective use of this medication.

Other Uses

A small arrow pointing down

Tacrolimus, an immunomodulating medication commonly employed in transplantation medicine to prevent organ rejection, has various other potential uses when compounded into a 1.5 mg rectal suppository. This form of delivery is particularly advantageous for patients who may be unable to take oral medications or for those seeking targeted local therapy. Besides its primary use in the management of recipient transplant rejection, rectally administered tacrolimus has been investigated for treating inflammatory and autoimmune conditions affecting the gastrointestinal tract, such as ulcerative colitis and Crohn's disease. The theory here is that the local delivery allows for high concentrations of the drug at the site of inflammation without producing the systemic levels that accompany oral administration, potentially reducing the risk of side effects.

The rectal route of administration can also be useful when managing conditions like proctitis or pouchitis, often accompanying inflammatory bowel diseases. Furthermore, some studies suggest that tacrolimus suppositories may have a role in treating perianal fistulas in Crohn's disease, providing localized immunosuppression and promoting fistula healing. Fewer systemic effects are noted with rectal administration compared to oral or intravenous routes, since the rectal mucosa directly absorbs the medication into the bloodstream, bypassing the first-pass metabolism in the liver.

Nonetheless, it is essential to understand that the therapeutic efficacy and safety profile of tacrolimus rectal suppositories for uses beyond transplant medicine remain under investigation. Clinicians should weigh the potential benefits against the risks, considering the individual patient's medical history and concurrent medications. Patients should be aware that monitoring of tacrolimus blood levels might be necessary, as systemic absorption can still occur. Also, patients should be counseled on the proper administration of the suppository to maximize its efficacy and minimize adverse effects.

Patient suitability for tacrolimus suppository therapy should be decided on a case-by-case basis, and it's crucial for healthcare providers to provide a thorough explanation of the potential off-label uses and benefits. Prescribers and patients are encouraged to reach out to our team at Bayview Pharmacy with any questions regarding tacrolimus rectal suppositories or other compounding options. We are dedicated to providing comprehensive information to ensure optimal medication therapy outcomes.

Frequently Asked Questions

A small arrow pointing down

What is a Tacrolimus 1.5 mg Rectal Suppository?

A Tacrolimus 1.5 mg Rectal Suppository is a solid dosage form containing 1.5 milligrams of the medication Tacrolimus. It is designed to be inserted into the rectum, where it will dissolve or melt to release the medication either for a local effect or for absorption into the bloodstream for systemic therapy.

How do you use a Tacrolimus Rectal Suppository?

To use the suppository, first, ensure cleanliness by washing your hands and the application area. Unwrap the suppository, lie on your side, and gently insert it into the rectum, pointed end first. Remain still for a few minutes to ensure the suppository stays in place and is able to dissolve fully.

Why is Tacrolimus prescribed in a suppository form?

Tacrolimus is prescribed in a suppository form when a localized or systemic effect is desired without the variability of absorption that can occur with oral medications. It is also used when the patient may not be able to take medications orally.

How does a Tacrolimus suppository work?

Tacrolimus suppositories work by melting at body temperature when inserted into the rectum, releasing the Tacrolimus medication which is then absorbed through the rectal mucosa. This can provide a local anti-inflammatory effect as well as systemic immunosuppression if absorbed into the bloodstream.

What conditions are treated with Tacrolimus Rectal Suppositories?

Conditions treated with Tacrolimus Rectal Suppositories often include inflammatory bowel diseases such as ulcerative colitis or Crohn’s disease, and sometimes for systemic conditions where immunosuppression may be beneficial and rectal delivery is appropriate.

Can Tacrolimus Rectal Suppositories cause side effects?

Yes, side effects are possible with Tacrolimus Rectal Suppositories. These may include local irritation, rectal discomfort, or systemic effects similar to oral Tacrolimus such as increased risk of infection, headaches, nausea, or kidney issues.

How often should I use Tacrolimus Rectal Suppositories?

The frequency of use for Tacrolimus Rectal Suppositories is determined by your healthcare provider based on your condition and response to treatment. Follow the prescribed regimen closely, and do not alter the frequency without consulting your doctor.

Should I use Tacrolimus Suppositories if I have a rectal irritation or injury?

If you have rectal irritation or an injury, you should consult with your healthcare provider before using Tacrolimus Suppositories as they may exacerbate certain conditions or not be appropriate for use.

How should I store Tacrolimus Rectal Suppositories?

Store Tacrolimus Rectal Suppositories in a cool, dry place as directed by the packaging or your pharmacist. Keep them away from direct heat or light and out of the reach of children and pets. Do not use if the suppository has melted or changed shape.

What should I do if I miss a dose of Tacrolimus Rectal Suppository?

If you miss a dose of your Tacrolimus Rectal Suppository, insert it as soon as you remember. However, if it's almost time for your next dose, skip the missed one and resume your usual dosing schedule. Do not double-dose to make up for the missed suppository.

Are there any interactions between Tacrolimus Suppositories and other medications?

Tacrolimus may interact with other medications, including prescription and over-the-counter drugs, vitamins, and herbal products. It's important to disclose all medications you are taking to your healthcare provider to avoid potential interactions.

Can I drink alcohol while using Tacrolimus Rectal Suppositories?

Alcohol consumption can affect the absorption and effectiveness of Tacrolimus. It is advisable to consult your healthcare provider regarding alcohol use while being treated with Tacrolimus Rectal Suppositories.

Related Formulas

Related Products
Formulas and/or material listed are not to be interpreted as a promise, guarantee or claim of therapeutic efficacy or safety. The information contained herein is not intended to replace or substitute for conventional medical care, or encourage its abandonment. Every patient is unique, and formulas should be adjusted to meet their individual needs.
NEW PRESCRIPTION ORDER FORM
1
Circle for steps.
Patient Information
2
Circle for steps.
Prescriber and Prescription Information
3
Circle for steps.
Fax order form to Bayview Pharmacy at 401-284-4506.
Thank you! Your submission has been received!
Oops! Something went wrong while submitting the form.