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Diltiazem 2% Rectal Gel

The Diltiazem 2% Rectal Gel is a semisolid formulation designed for rectal administration. This gel is dispensed through a pump mechanism, which ensures easy and precise application. The consistency of the gel allows for targeted treatment, optimizing the absorption of the active ingredient, diltiazem, directly at the site of action. This formulation is primarily used in the treatment of anal fissures, providing relief from pain and facilitating the healing process by promoting blood flow to the affected area. Additionally, it may be utilized in the management of chronic anal fissure-associated symptoms, contributing to an overall improvement in patient comfort and quality of life.

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Topical Gel
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Formula Information

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Diltiazem 2% Rectal Gel is a specially compounded medication designed to deliver the calcium channel blocker diltiazem through a rectal route, using a semisolid gel formulation. This preparation is intended for patients who require the therapeutic effects of diltiazem but may not be able to take the medication orally or require a localized effect. The gel is dispensed through a pump mechanism, which ensures ease of use and precise dosing. The consistency of the gel allows for smooth application and may improve patient compliance due to its user-friendly nature.

The active ingredient, diltiazem, is primarily known for its ability to relax the smooth muscles of the blood vessels, leading to vasodilation and a subsequent reduction in blood pressure. This makes it useful in the treatment of hypertension and angina. However, when formulated as a 2% rectal gel, diltiazem can be particularly effective in treating anal fissures. By promoting blood flow to the affected area and reducing the sphincter muscle spasm, diltiazem aids in the healing process of these painful tears in the lining of the anus. The localized application minimizes systemic absorption, which can be beneficial in reducing potential side effects associated with oral administration.

For prescribers considering this formulation for their patients, it is important to note that the rectal administration of diltiazem may offer a more direct therapeutic effect on anal fissures, with a lower risk of systemic side effects. The 2% concentration has been found to be effective in clinical studies, and the gel formulation provides a convenient alternative for patients who may have difficulty with oral medications or who require targeted delivery of the medication.

Patients prescribed with Diltiazem 2% Rectal Gel should be instructed on the proper administration technique to ensure optimal efficacy of the treatment. It is also crucial for patients to understand the importance of adhering to the prescribed dosing schedule and to report any adverse effects or lack of improvement to their healthcare provider. As with any medication, the use of diltiazem rectal gel should be part of a comprehensive treatment plan that may include lifestyle modifications and other medications as indicated.

If you have any questions regarding Diltiazem 2% Rectal Gel or its use in treating specific disease states, please do not hesitate to reach out to us at Bayview Pharmacy. Our team of compounding pharmacists is dedicated to providing in-depth information and support to both patients and healthcare providers to ensure the safe and effective use of compounded medications.

Drug Interactions

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Diltiazem is a calcium channel blocker that is commonly used to treat hypertension, angina, and certain heart rhythm disorders. When formulated as a 2% rectal gel, it is intended for local application and may be used for conditions such as anal fissures where it works by relaxing the smooth muscles and improving blood flow to the affected area. However, even when applied rectally, diltiazem can be absorbed systemically and may interact with other medications.

Patients should be aware that diltiazem can interact with a wide range of drugs, potentially leading to serious adverse effects. For example, concomitant use with beta-blockers or digoxin can lead to an increased risk of heart failure or bradycardia. When used with other antihypertensive agents or medications that lower blood pressure, there is an increased risk of hypotension. Additionally, diltiazem can raise the levels of certain drugs in the blood, such as statins (e.g., simvastatin, atorvastatin), increasing the risk of muscle toxicity, including rhabdomyolysis.

Patients taking diltiazem should also be cautious about using it with drugs that are metabolized by the liver enzyme CYP3A4, as diltiazem can inhibit this enzyme and increase the levels of these drugs. This includes certain immunosuppressants (e.g., cyclosporine, tacrolimus), benzodiazepines (e.g., midazolam, triazolam), and some antiviral medications used to treat HIV. Grapefruit juice, which can also inhibit CYP3A4, should be avoided as it can have a similar effect.

Moreover, diltiazem can interact with other drugs that prolong the QT interval, a measure of the time it takes for the heart's muscle to recharge between beats. This can lead to an increased risk of serious arrhythmias. Patients should inform their healthcare provider of all medications they are taking, including over-the-counter drugs, herbal supplements, and vitamins, to ensure that there are no potential interactions.

It is important for prescribers to review the patient's complete medication profile for potential drug interactions before prescribing diltiazem rectal gel. Monitoring for signs of drug interactions is crucial, and dose adjustments or alternative therapies may be necessary. If you have any questions or concerns regarding the use of diltiazem 2% rectal gel or its interactions with other medications, please reach out to us at Bayview Pharmacy for further assistance.

How Does it Work

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Diltiazem is a calcium channel blocker that works by relaxing the muscles of your heart and blood vessels. When formulated as a 2% rectal gel, it is designed to exert its effects locally within the rectal area. The mechanism of action of diltiazem involves the inhibition of the influx of calcium ions during membrane depolarization of cardiac and vascular smooth muscle. The reduction in intracellular calcium inhibits the contractile processes of the myocardial smooth muscle cells, leading to dilation of the coronary and systemic arteries, thereby reducing blood pressure and myocardial oxygen demand. This action can be particularly beneficial in treating conditions such as anal fissures, where the relaxation of the smooth muscle can help to reduce pain and facilitate healing.

The semisolid formulation of the Diltiazem 2% Rectal Gel allows for the medication to be dispensed through a pump mechanism. This delivery system is designed to provide a consistent dose with each application, which can be critical for ensuring therapeutic effectiveness and patient adherence. The gel-like consistency of the formulation is intended to make the application process more comfortable for the patient, as well as to provide a localized effect of the medication with minimal systemic absorption. This localized application can be advantageous in targeting the specific area of discomfort or disease, such as the rectal tissue affected by an anal fissure, without exerting widespread effects on the body.

For patients and prescribers considering the use of Diltiazem 2% Rectal Gel, it is important to understand that this formulation is specifically designed for rectal administration and should not be used in any other manner. The gel is typically applied topically to the affected area, and the precise dosing facilitated by the pump mechanism helps to ensure that the correct amount of medication is administered each time. Patients should be instructed on how to use the pump and apply the gel properly to maximize the therapeutic benefits while minimizing potential side effects.

It is also important for patients to be aware that while Diltiazem 2% Rectal Gel can provide significant relief from symptoms associated with anal fissures, it is not a cure for the underlying condition. Patients should follow the full course of treatment prescribed by their healthcare provider and attend all scheduled follow-up appointments to monitor the progress of healing. Additionally, lifestyle changes and other medical interventions may be necessary to address the root causes of the anal fissure.

If you have any questions about the Diltiazem 2% Rectal Gel formulation or its use in treating specific disease states, please do not hesitate to reach out to us at Bayview Pharmacy. Our team of compounding pharmacists is here to provide you with the information and support you need to ensure safe and effective treatment for your patients.

Other Uses

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The primary indication for Diltiazem 2% Rectal Gel is for the treatment of anal fissures to promote healing and provide pain relief through its vasodilatory effects, which improve blood flow to the affected area. However, beyond its conventional use, the gel may have other potential applications. It is sometimes utilized off-label for the relief of chronic anal sphincter spasms, which can contribute to issues such as chronic proctalgia. Moreover, the calcium channel blocking properties of diltiazem may be beneficial for conditions where smooth muscle relaxation is desired in proximity to the application site.

Considering its formulation, this rectal gel might be investigated for localized treatment of hemorrhoids, especially when inflammation is accompanied by a significant amount of spasm and discomfort, although this use is not widely established. The gel's mode of delivery and pharmacological action might also theoretically assist in reducing the discomfort associated with other anorectal conditions such as pilonidal disease or after surgical procedures in the anorectal region, but further clinical evidence would be necessary to support these uses. Being a calcium channel blocker, diltiazem could theoretically have other vascular benefits, but the rectal mode of application limits systemic uptake, making significant systemic effects unlikely. Therefore, the use of Diltiazem 2% Rectal Gel is generally confined to the anorectal area.

Patients and prescribers should be aware that the use of any medication outside its approved indication should be based on a careful consideration of the potential risks and benefits. As with any medical intervention, consultation with a healthcare provider is essential before using this medication for an off-label purpose. As compounding pharmacists, we can provide additional information on the potential uses of this compound, and we can assist in tailoring therapies to meet specific patient needs. In any case where there is uncertainty or where additional advice is needed on the use of Diltiazem 2% Rectal Gel, please feel free to reach out to us for guidance and support.

Frequently Asked Questions

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What is Diltiazem 2% Rectal Gel used for?

Diltiazem 2% Rectal Gel is typically prescribed for the treatment of anal fissures or other conditions where a smooth muscle relaxant is needed to alleviate pain, discomfort, or to promote healing in the rectal area.

How do you apply Diltiazem 2% Rectal Gel?

The gel should be applied as directed by your healthcare provider. Generally, a measured amount of gel is applied to the tip of the finger and then gently inserted into the rectal area. Always wash your hands before and after applying the medication.

How often should Diltiazem 2% Rectal Gel be used?

The frequency of application will depend on your physician's prescription. Typically, the gel is applied two to four times daily, but follow your doctor's specific instructions for dosage and frequency.

Can Diltiazem 2% Rectal Gel cause any side effects?

As with any medication, Diltiazem 2% Rectal Gel may cause side effects. Mild discomfort, itching, or a burning sensation at the application site may occur. If you experience any severe reactions or signs of an allergic reaction, contact your healthcare provider immediately.

Is Diltiazem 2% Rectal Gel suitable for everyone?

Most adult patients can use Diltiazem 2% Rectal Gel if prescribed by a healthcare provider; however, it may not be suitable for everyone, including those with certain allergies or medical conditions. Always consult your doctor before beginning any new medication.

Should I continue using Diltiazem 2% Rectal Gel if my symptoms improve?

Do not discontinue use of the gel without consulting your healthcare provider, even if symptoms improve. It's important to complete the full course of treatment as prescribed to ensure proper healing.

Can I use Diltiazem 2% Rectal Gel if I am pregnant or breastfeeding?

Consult with your healthcare provider before using Diltiazem 2% Rectal Gel if you are pregnant, planning to become pregnant, or breastfeeding, as they will need to evaluate the benefits and risks associated with its use.

How should Diltiazem 2% Rectal Gel be stored?

Store the gel at room temperature, away from heat and direct light, and keep the pump mechanism clean to ensure hygiene. Make sure the cap is tightly closed when not in use. Do not freeze the medication.

What should I do if I miss a dose of Diltiazem 2% Rectal Gel?

If you miss a dose, apply it as soon as you remember. If it is almost time for your next dose, skip the missed dose and continue with your regular schedule. Do not apply extra gel to make up for a missed dose.

Can I use other medications alongside Diltiazem 2% Rectal Gel?

Some medications can interact with diltiazem, affecting its potency or causing side effects. Discuss with your healthcare provider all the medications, supplements, and herbal products you are taking before starting treatment with Diltiazem 2% Rectal Gel.

Is there anything else I need to know before starting treatment with Diltiazem 2% Rectal Gel?

It's critical to follow your healthcare provider’s instructions regarding the use of Diltiazem 2% Rectal Gel. Discuss any concerns or questions you have about this medication with your healthcare provider, including your medical history and current health conditions.

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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.