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Diltiazem HCl 10 mg Rectal Suppository

Diltiazem HCl 10 mg Rectal Suppository is a solid dosage form designed for insertion into the rectum. Upon administration, the suppository dissolves or melts, facilitating the release of the active ingredient, Diltiazem HCl, for local or systemic absorption. This formulation is specifically used to treat conditions such as anal fissures and chronic anal fissure-associated pain by promoting smooth muscle relaxation and increasing blood flow to the affected area. Additionally, it may be utilized for its off-label use in managing hypertension and certain types of angina when oral administration is not feasible.

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Formula Information

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Diltiazem HCl is a calcium channel blocker that is commonly used to treat hypertension (high blood pressure), angina (chest pain), and certain heart rhythm disorders. The 10 mg rectal suppository form of Diltiazem HCl is a solid dosage designed for insertion into the rectum, where it dissolves or melts to release the medication. This route of administration can be particularly useful for patients who are unable to take medications orally due to vomiting, surgery, or gastrointestinal issues. The rectal administration of Diltiazem allows for the medication to be absorbed directly into the bloodstream, bypassing the digestive system, which can lead to a more rapid onset of action compared to oral administration.

When inserted rectally, the suppository base, typically made of a substance like cocoa butter or a glycerinated gelatin, melts at body temperature and allows the active drug, Diltiazem HCl, to be released and absorbed through the rectal mucosa. Once absorbed, Diltiazem works by inhibiting the influx of calcium ions during membrane depolarization of cardiac and vascular smooth muscle. This action results in the dilation of coronary and systemic arteries, leading to decreased blood pressure, reduced heart rate, and a decrease in the workload on the heart, thereby alleviating symptoms of angina. Additionally, by affecting the electrical conduction within the heart, Diltiazem can help to restore normal heart rhythms.

For patients and prescribers considering the use of Diltiazem HCl 10 mg rectal suppository, it is important to note that this formulation provides an alternative for those who require the therapeutic benefits of Diltiazem but are not candidates for oral administration. The suppository form can be particularly beneficial in acute situations where a rapid response is desired or when maintaining consistent plasma levels of the medication is necessary. It is also a viable option for patients with difficulty swallowing pills or those who have restrictions on oral intake.

As with any medication, the use of Diltiazem HCl rectal suppositories should be under the guidance of a healthcare professional. It is essential to follow the prescribed dosing regimen and to be aware of potential side effects, which may include dizziness, headache, peripheral edema, and gastrointestinal discomfort. Patients with pre-existing conditions such as low blood pressure, heart failure, or liver disease should use this medication with caution. Monitoring of blood pressure and heart rate may be necessary to ensure the safe use of this medication.

If you have any questions or require further information about the Diltiazem HCl 10 mg rectal suppository formulation, please do not hesitate to reach out to us at Bayview Pharmacy. Our team of compounding pharmacists is dedicated to providing comprehensive support and guidance to both patients and prescribers to ensure the safe and effective use of this medication.

Drug Interactions

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Diltiazem HCl is a calcium channel blocker that is used to treat hypertension (high blood pressure), angina (chest pain), and certain heart rhythm disorders. When formulated as a 10 mg rectal suppository, diltiazem is absorbed through the rectal mucosa and enters the systemic circulation, exerting its effects by dilating blood vessels and reducing the workload on the heart. This can help to lower blood pressure, improve blood flow to the heart, and control heart rate.

When considering the use of diltiazem in any form, it is crucial to be aware of potential drug interactions that may alter its effectiveness or increase the risk of adverse effects. Diltiazem is metabolized by the liver enzyme CYP3A4, and thus, drugs that inhibit or induce this enzyme can affect diltiazem plasma concentrations. Strong CYP3A4 inhibitors, such as ketoconazole, itraconazole, and ritonavir, can increase diltiazem levels, potentially leading to toxicity. Conversely, CYP3A4 inducers like rifampin and St. John's Wort can decrease diltiazem levels, reducing its efficacy.

Additionally, diltiazem can interact with other cardiovascular drugs. Concurrent use with beta-blockers or digoxin can lead to an additive effect on heart rate, increasing the risk of bradycardia (slow heart rate). When used with other antihypertensive agents or vasodilators, there is a risk of excessive blood pressure lowering, which could result in symptoms like dizziness or fainting. Patients taking diltiazem should also avoid consuming grapefruit juice, as it contains compounds that inhibit CYP3A4, potentially leading to increased diltiazem concentrations and side effects.

Other potential interactions include an increased risk of bleeding when combined with anticoagulants such as warfarin, due to the potential for diltiazem to affect platelet function and coagulation pathways. Diltiazem may also increase the plasma concentrations of drugs such as statins (e.g., simvastatin, atorvastatin), which could increase the risk of muscle-related side effects, including rhabdomyolysis.

It is important for patients and prescribers to be aware of all medications, supplements, and over-the-counter drugs that are being taken concurrently with diltiazem to avoid potential interactions. Monitoring for signs of toxicity, therapeutic efficacy, and side effects is recommended when initiating diltiazem therapy or when changes are made to the medication regimen that includes diltiazem. If you have any questions or concerns regarding the use of diltiazem rectal suppositories or potential drug interactions, please reach out to us at Bayview Pharmacy for personalized advice and support.

How Does it Work

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Diltiazem HCl, the active ingredient in this formulation, is a calcium channel blocker that works by inhibiting the influx of calcium ions into cardiac and smooth muscle cells. This action results in the dilation of the coronary and systemic arteries, leading to a decrease in blood pressure and an improvement in blood flow. When formulated as a 10 mg rectal suppository, diltiazem is designed to be inserted into the rectum where it can dissolve or melt, allowing the medication to be absorbed directly into the bloodstream through the rich vascular supply of the rectal mucosa.

This route of administration can be particularly beneficial for patients who are unable to take medications orally due to nausea, vomiting, or difficulty swallowing. Additionally, rectal administration can provide a more rapid onset of action compared to oral administration, which can be crucial in acute situations. The rectal suppository form bypasses the first-pass metabolism in the liver, potentially reducing the dose needed to achieve therapeutic effects and minimizing systemic side effects.

Diltiazem is commonly used to treat conditions such as hypertension (high blood pressure), angina pectoris (chest pain due to coronary artery disease), and certain types of arrhythmias (irregular heartbeats). By relaxing blood vessels and reducing the workload on the heart, diltiazem helps to lower blood pressure, increase oxygen delivery to the heart, and stabilize heart rhythms. This can lead to a reduction in the frequency and severity of angina attacks and help control abnormal heart rhythms.

For patients and prescribers considering the use of diltiazem HCl 10 mg rectal suppository, it is important to understand that while this formulation provides the benefits of localized delivery and potentially faster systemic absorption, it should be used with caution in patients with rectal disorders or those who have undergone recent rectal surgery. Additionally, the suppository should be stored in a cool place to prevent melting before use and should be handled with clean hands to prevent contamination.

If you have any questions about this formulation or its appropriateness for a specific patient or condition, please reach out to us at Bayview Pharmacy. Our team of compounding pharmacists is here to provide guidance and support to ensure safe and effective treatment outcomes.

Other Uses

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Diltiazem hydrochloride is typically known to be a calcium channel blocker that is most commonly used for the treatment of hypertension, angina, and certain heart arrhythmias. However, in the form of a 10 mg rectal suppository, diltiazem HCl can be used for other medical conditions. One notable use is for the management of chronic anal fissures. The rectal suppository formulation promotes local vasodilation, which can help to alleviate the spasm of the anal sphincter and improve blood flow to the area, allowing for healing of the fissure and reducing pain and discomfort during bowel movements. This mode of delivery ensures direct and localized action, ideally reducing systemic side effects.

Furthermore, diltiazem HCl suppositories might have applications in the off-label management of proctalgia fugax, a condition characterized by episodes of severe rectal pain. In this setting, the relaxing effect on smooth muscle could provide symptomatic relief. Additionally, research might explore the potentiality of this formulation in treating other conditions associated with smooth muscle spasms or dysfunction within the gastrointestinal tract.

While diltiazem is mostly used for its cardiovascular effects, patients and prescribers should be aware that its use as a suppository for non-cardiovascular issues is relatively less common and may lack extensive clinical trial backing. As such, utilizing the medication in this manner should be done under the guidance of a healthcare professional proficient in compounding pharmacy practices and familiar with the patient's overall health situation.

Patients should note that this route of administration does bypass the liver's first-pass effect, which can lead to differing systemic absorption and effect compared to oral routes. Monitoring by a healthcare provider is essential to ensure therapeutic efficacy and manage any potential adverse reactions and interactions with other medications the patient might be taking. If you have any questions regarding the use of diltiazem HCl 10 mg rectal suppository or would like to consider this formulation for other therapeutic uses, please feel free to reach out to us at Bayview Pharmacy. Our team of compounding pharmacists is here to provide the necessary guidance and support to optimize patient care.

Frequently Asked Questions

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What is Diltiazem HCl 10 mg Rectal Suppository used for?

Diltiazem HCl 10 mg Rectal Suppository is typically used to treat anal fissures and relieve symptoms like pain or discomfort. It can also be prescribed for conditions that require the muscle-relaxing properties of diltiazem, which may include managing certain types of heart conditions or blood pressure when rectal administration is preferred.

How does a rectal suppository work?

A rectal suppository is designed to be inserted into the rectum where it dissolves or melts, releasing the medication it contains. This allows the drug to either be absorbed into the local rectal tissue or into the bloodstream for systemic effects, depending on the drug's intended purpose and properties.

How should I store Diltiazem HCl Rectal Suppositories?

Diltiazem HCl Rectal Suppositories should be stored at room temperature away from moisture and heat. Keep the suppositories in their original packaging until ready to use, and do not expose them to direct light. Always check the specific storage instructions provided by the pharmacy or manufacturer as these can vary.

Can Diltiazem HCl Rectal Suppositories be used for conditions other than anal fissures?

While the primary use is to treat anal fissures and associated pain, it might be prescribed for other conditions at the discretion of a healthcare provider. Always use this medication for the condition for which it was prescribed and consult your doctor if you have questions regarding its use for other conditions.

What are the possible side effects of using Diltiazem HCl Rectal Suppositories?

The side effects can include local irritation or itching, a burning sensation, dizziness, headaches, or changes in heart rate or blood pressure. Systemic side effects are possible but less common due to the lower absorption rates. If you experience any severe or persistent side effects, contact your healthcare provider.

How often should I use Diltiazem HCl Rectal Suppositories?

The frequency of use should be as prescribed by your healthcare provider, often twice daily. It's essential to follow the dosage instructions provided by your doctor to ensure effectiveness and reduce the risk of side effects.

Can I use Diltiazem HCl Rectal Suppositories if I am pregnant or breastfeeding?

You should consult your healthcare provider before using Diltiazem HCl Rectal Suppositories if you are pregnant or breastfeeding. While rectal administration reduces systemic absorption, it is essential to weigh the benefits against the potential risks to the fetus or infant.

How do I insert a rectal suppository properly?

To insert a rectal suppository, wash your hands thoroughly, lie on your side with one leg bent up toward your chest, and gently push the suppository, pointed end first, into the rectum. Hold it in place for a few moments to ensure it stays put. Wash your hands again after insertion.

Can I use a laxative while using Diltiazem HCl Rectal Suppositories?

You should consult with your healthcare provider before combining treatments. Using a laxative may affect the absorption or retention time of the suppository, potentially altering its effectiveness.

Will using Diltiazem HCl Rectal Suppositories affect my daily activities?

Most people can continue with their everyday activities while using these suppositories. However, if you experience dizziness or other systemic effects, you should be cautious about driving or operating machinery until you know how the medication affects you.

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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.
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