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Formulas

Sirolimus 0.1% Topical Gel

The Sirolimus 0.1% Topical Gel is a specialized semisolid formulation designed for targeted treatment of specific skin conditions. This gel is dispensed through a pump mechanism, which ensures ease of use and precise dosing for the patient. The consistency of the gel allows for smooth application and optimal absorption of the active ingredient, sirolimus, into the skin.

Sirolimus, the active ingredient in this formulation, is primarily known for its immunosuppressive properties. In a topical gel form, it is used to treat various dermatological conditions. This includes the treatment of facial angiofibromas associated with tuberous sclerosis complex and the potential management of other skin diseases that may benefit from its immunomodulatory effects. The 0.1% concentration provides a therapeutic dose intended to minimize systemic absorption and focus treatment on the affected skin areas.

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Topical Gel
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Formula Information

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Sirolimus 0.1% Topical Gel is a specialized medication formulated by the compounding pharmacists at Bayview Pharmacy to address specific dermatological conditions. This semisolid formulation is designed to be dispensed through a pump mechanism, which ensures ease of use and precise dosing for patients. The gel base provides a suitable medium for the active ingredient, sirolimus, to be applied topically on the skin, allowing for targeted treatment and effective absorption.

Sirolimus, also known as rapamycin, is an immunosuppressant drug that has been found to have efficacy in treating various skin conditions due to its anti-proliferative and anti-inflammatory properties. It is particularly beneficial in the treatment of tuberous sclerosis complex (TSC)-associated angiofibromas, which are benign skin growths that can cause disfigurement and bleeding. Additionally, sirolimus has been used off-label for the treatment of psoriasis, atopic dermatitis, and certain rare skin diseases where overactive immune response plays a role in the pathology.

The 0.1% concentration of sirolimus in the gel formulation is carefully compounded to ensure therapeutic effectiveness while minimizing potential systemic absorption and side effects. The gel base is non-comedogenic and designed to be gentle on the skin, making it suitable for long-term use as directed by a healthcare provider. Patients should apply the gel as prescribed, typically to clean, dry skin, and they should be advised to avoid covering the treated area with occlusive dressings unless instructed otherwise by their physician.

Prescribers opting to use Sirolimus 0.1% Topical Gel should consider the patient's medical history, concurrent medications, and the potential for drug interactions. Monitoring for local skin reactions and systemic side effects is recommended, especially in patients with increased systemic absorption risk. As with all compounded medications, this formulation is prepared in a controlled environment to ensure quality and consistency in each batch.

For patients and prescribers interested in Sirolimus 0.1% Topical Gel or seeking more information about its use and potential benefits for specific dermatological conditions, please reach out to us at Bayview Pharmacy. Our team of knowledgeable compounding pharmacists is available to answer questions and provide guidance on the appropriate use of this customized medication.

Drug Interactions

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Sirolimus, also known as rapamycin, is an immunosuppressive agent that is primarily used to prevent organ transplant rejection and to treat certain rare lung diseases. When formulated as a 0.1% topical gel, sirolimus is used for its anti-proliferative and immunomodulatory effects on the skin, which can be beneficial in treating conditions such as psoriasis, atopic dermatitis, and cutaneous manifestations of tuberous sclerosis complex. However, due to its systemic absorption potential, sirolimus can interact with a variety of substances, and it is important to consider these interactions to ensure patient safety and efficacy of the treatment.

Sirolimus is metabolized by the cytochrome P450 3A4 (CYP3A4) enzyme system in the liver and intestines and is also a substrate of the P-glycoprotein (P-gp) efflux transporter. Therefore, concomitant use of drugs that inhibit or induce CYP3A4 or P-gp can significantly affect the concentration of sirolimus. Strong inhibitors of CYP3A4 such as ketoconazole, itraconazole, clarithromycin, and ritonavir may increase sirolimus levels, potentially leading to toxicity. Conversely, inducers of CYP3A4 like rifampin, phenytoin, and St. John's Wort may decrease sirolimus levels, reducing its efficacy.

Additionally, sirolimus has been shown to increase the serum concentrations of other drugs metabolized by CYP3A4, such as certain calcium channel blockers (e.g., verapamil, diltiazem), statins (e.g., atorvastatin, simvastatin), and protease inhibitors. This can enhance the effects and adverse reactions of these drugs. Patients should be monitored for signs of toxicity, and dosage adjustments may be necessary when sirolimus is used concurrently with these medications.

Grapefruit juice and other grapefruit products should be avoided as they contain compounds that inhibit CYP3A4, which can lead to increased systemic levels of sirolimus and potential toxicity. Similarly, patients should be advised to avoid consuming pomegranate or Seville oranges, as they can have similar effects.

Live vaccines should be used with caution in patients receiving immunosuppressive doses of sirolimus, as the immunosuppressive effect may lead to reduced vaccine efficacy and increased risk of infection. Nonsteroidal anti-inflammatory drugs (NSAIDs) may increase the risk of nephrotoxicity when used with sirolimus, and monitoring of renal function is advised.

It is also important to consider the potential for additive immunosuppression when sirolimus is used with other immunosuppressants, which could increase the risk of infection and lymphoma. Patients should be monitored closely for signs of infection and new growths on the skin.

Given the complexity of potential drug interactions with sirolimus, prescribers should review the patient's current medication regimen in detail before initiating treatment with sirolimus 0.1% topical gel. Pharmacists should verify the patient's medication history and counsel patients on the importance of adhering to prescribed medications while avoiding contraindicated substances. If you have any questions or require further information regarding drug interactions with sirolimus 0.1% topical gel, please reach out to us at Bayview Pharmacy for assistance.

How Does it Work

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Sirolimus, also known as rapamycin, is an immunosuppressive drug that is commonly used to prevent organ transplant rejection. However, in a 0.1% topical gel formulation, sirolimus works by a different mechanism. When applied to the skin, sirolimus inhibits the mammalian target of rapamycin (mTOR) pathway, which is a key regulator of cell growth, proliferation, and survival. By inhibiting this pathway, sirolimus can reduce the proliferation of keratinocytes and other skin cells, which is beneficial in treating various dermatological conditions.

The 0.1% concentration in the gel ensures a low dose application, minimizing systemic absorption and potential side effects. This is particularly important for long-term treatments. The semisolid gel formulation is designed to enhance the delivery of sirolimus to the affected skin areas. The gel base allows for a controlled release of the active ingredient, ensuring a sustained action over the area of application. The pump mechanism of the container dispenses a consistent amount of gel with each use, which helps in maintaining dosing accuracy and ease of use for the patient.

Sirolimus 0.1% Topical Gel is used in the treatment of various skin conditions, such as psoriasis, atopic dermatitis, and tuberous sclerosis complex (TSC)-associated angiofibromas. In psoriasis, sirolimus helps to reduce the hyperproliferation of skin cells and the associated inflammation. For atopic dermatitis, it can help to modulate the immune response and decrease the inflammatory processes in the skin. In the case of TSC-associated angiofibromas, sirolimus can reduce the size and redness of these benign skin tumors by inhibiting the mTOR pathway, which is often overactive in TSC patients.

It is important for both patients and prescribers to understand that while sirolimus 0.1% Topical Gel is beneficial for these conditions, it should be used with caution. Patients should apply the gel as directed by their healthcare provider, and avoid contact with eyes, mouth, and mucous membranes. The area of application should be clean and dry before application. Patients should also be aware of potential side effects, which may include local irritation, redness, or itching at the site of application. If any severe reactions occur, they should discontinue use and consult their healthcare provider.

For prescribers, it is crucial to consider the patient's overall health status and any concomitant medications that may interact with sirolimus. Regular monitoring and follow-up are recommended to assess the efficacy and safety of the treatment. If you have any questions or require further information about Sirolimus 0.1% Topical Gel, please reach out to us at Bayview Pharmacy. Our team of compounding pharmacists is here to support you with the knowledge and expertise to ensure the best possible outcomes for your patients.

Other Uses

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Sirolimus 0.1% Topical Gel is a specialized formulation designed primarily for the treatment of various skin conditions. While its main indication is in the treatment of facial angiofibromas associated with tuberous sclerosis complex, its unique mechanism of action as a mTOR inhibitor makes it a potential candidate for off-label uses. It is important to note that these alternative uses are not FDA-approved and should only be considered after a thorough consultation with a healthcare provider.

Emerging research has suggested potential benefits of Sirolimus in the management of other dermatological conditions. For instance, Sirolimus has shown promise in treating psoriasis due to its immunosuppressive and antiproliferative properties. In addition, limited studies have indicated effectiveness in the treatment of certain rare skin disorders such as lymphangioleiomyomatosis and Kaposi's sarcoma, providing possible alternative therapeutic approaches for these complex diseases.

Its immunomodulatory effects make Sirolimus a subject of interest in the field of dermatology for wound healing and scar improvement, especially in individuals where excessive scarring occurs. Furthermore, its anti-fibrotic qualities may be useful for the management of scleroderma and hypertrophic scars, although this requires more in-depth research. Due to its ability to inhibit cell growth and proliferation, there has been interest in exploring the use of topical Sirolimus in other proliferative cutaneous disorders.

In the context of cosmeceuticals, Sirolimus may have utility in procedures where modulation of the immune response is beneficial, such as post-laser treatments and dermabrasion where it could potentially improve healing and reduce downtime. Lastly, because of its anti-angiogenic properties, there is a theoretical role for Sirolimus in conditions with a vascular component, such as rosacea or port-wine stains; however, studies to fully evaluate this potential are still required.

However, each of these possible applications should be considered experimental until more conclusive evidence is available. Dosing, efficacy, and safety for these off-label uses need careful and individualized evaluation. Any prescriber considering Sirolimus Topical Gel for an indication outside the established use should closely monitor the patient and adjust the treatment regimen based on therapeutic response and side effects. Furthermore, patients should be counseled on the investigational nature of these applications and the necessity for close follow-up.

This semisolid formulation through a pump mechanism is an advantageous dosage form that allows for controlled dosing and targeted application. Such precision can be critical, especially in cases of off-label use where the therapeutic window may be narrow. Patients and prescribers considering this formulation for other potential uses are encouraged to engage in an open dialogue to weigh the benefits against risks and to ensure that any treatment plan is tailored to the patient's specific needs.

If you have any questions regarding the potential off-label uses of Sirolimus 0.1% Topical Gel or require more information about its applications, please do not hesitate to reach out to us at Bayview Pharmacy. Our team of expert compounding pharmacists is here to provide support and guidance.

Frequently Asked Questions

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What is Sirolimus 0.1% Topical Gel used for?

Sirolimus 0.1% Topical Gel is used to treat various skin conditions that may respond to the anti-inflammatory and immunosuppressant properties of Sirolimus. It can be indicated for conditions such as psoriasis, atopic dermatitis, or to decrease the appearance and texture of skin lesions or scars, among other uses as directed by a healthcare professional.

How should I apply Sirolimus 0.1% Topical Gel?

Apply the Sirolimus 0.1% Topical Gel as directed by your healthcare provider. Usually, this involves pumping a small amount of the gel onto clean fingers or directly onto the affected area of the skin and gently spreading it to form a thin layer. It should be used strictly according to the prescribed regimen. Avoid contact with the eyes and mouth.

How does the pump mechanism work for dispensing the gel?

The pump mechanism is designed to dispense a controlled amount of Sirolimus 0.1% Topical Gel with each press. To use, hold the container upright, and press down the top of the pump to dispense the product. If using for the first time, you may need to prime the pump by pressing it several times until the gel is released.

Can I use other skincare products along with Sirolimus 0.1% Topical Gel?

It’s best to discuss the use of other skincare products with your healthcare provider. They can advise on appropriate complementary products or those that should be avoided due to potential interactions. In general, allow proper absorption of the Sirolimus gel before applying other products to the same area.

Should Sirolimus 0.1% Topical Gel only be applied to a particular area of the body?

Sirolimus 0.1% Topical Gel should be applied only to the areas of the skin that have been prescribed by your healthcare provider. Avoid applying the gel to mucous membranes or areas of the skin with open wounds, unless directed by your doctor.

What should I do if I miss a dose of Sirolimus 0.1% Topical Gel?

If you miss a dose of Sirolimus 0.1% Topical Gel, apply it as soon as you remember. However, if it is almost time for the next scheduled dose, skip the missed dose and proceed with your regular dosing schedule. Do not apply extra gel to make up for the missed dose.

Are there any side effects associated with Sirolimus 0.1% Topical Gel?

Like all medications, Sirolimus 0.1% Topical Gel can cause side effects, although not everybody gets them. Possible side effects include irritation at the application site, redness, itching, or rash. If you experience any severe or persistent side effects, contact your healthcare provider immediately.

How long does it take to see results from using Sirolimus 0.1% Topical Gel?

The time required to see results can vary depending on the condition being treated and individual factors. Some patients may notice improvements within a few weeks, while for others it may take longer. It is important to continue using the gel as directed by your healthcare provider and regularly follow up on your progress.

Can Sirolimus 0.1% Topical Gel be used by pregnant or breastfeeding women?

The safety of Sirolimus 0.1% Topical Gel for use during pregnancy or breastfeeding has not been fully established. If you are pregnant or breastfeeding, it is essential to discuss the potential risks and benefits with your healthcare provider before using this medication.

How should I store Sirolimus 0.1% Topical Gel?

Store Sirolimus 0.1% Topical Gel at room temperature, away from direct sunlight and heat. Keep the container tightly closed when not in use. Make sure to keep it out of reach of children and pets. Consult your pharmacist regarding the disposal of expired or unused gel.

Will Sirolimus 0.1% Topical Gel cure my skin condition?

While Sirolimus 0.1% Topical Gel can effectively manage symptoms and improve the appearance of certain skin conditions, it may not be a cure. Chronic skin conditions often require long-term management. It is important to follow your healthcare provider’s instructions and attend all scheduled appointments to monitor your condition.

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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.

No compounded medications are reviewed by the FDA for safety or efficacy.