Cilostazol

Cilostazol is a platelet aggregation inhibitor that alleviates the symptoms of intermittent claudication.

Generic Pletal

Cilostazol

Pletoz, Stozic, Cilodoc

10

Cipla, Intas Pharma, Lupin

Tablet

100 mg, 50 mg

India

Cilostazol

1. Introduction to Cilostazol

What is Cilostazol?

Cilostazol is classified as a phosphodiesterase three inhibitor medication. It is well known for its ability to dilate blood vessels, and as a result, it has garnered significant attention as an effective treatment for peripheral vascular disease, specifically intermittent claudication.

The Historical Development of Cilostazol

Cilostazol, which was developed by Otsuka Pharmaceutical Co. was initially authorized by the FDA in 1999. The approval was primarily granted due to the results of clinical trials that showed its effectiveness in enhancing walking distances for individuals with intermittent claudication. Since its approval, the drug has proven effective in alleviating symptoms for numerous patients making it a trusted option.

Current Standing in the Pharmaceutical Market

Today Cilostazol enjoys a respected status within the pharmaceutical industry. It is widely recognized as a preferred therapeutic agent for treating intermittent claudication in various regions across the globe. Furthermore, market reports indicate that Cilostazol is experiencing a positive trend owing to its well-established safety record and reliable effectiveness.

2. Composition and Characteristics of Cilostazol

Understanding the Chemical Composition of Cilostazol

Cilostazol, chemically known as 6-[4-(1 cyclohexyl 1H tetrazole 5-yl)butoxy]-3,4 dihydro 2(1H)-quinolinone is a crystalline powder that appears as white to off-white. This substance is slightly soluble in methanol and ethanol. But it does not dissolve well in water. Cilostazol has a molecular weight of 369.46.

Pharmaceutical Properties of Cilostazol

Cilostazols' exceptional pharmaceutical characteristics are crucial in its therapeutic effects. It functions as a selective inhibitor of phosphodiesterase 3 (PDE3), leading to a rise in cyclic adenosine monophosphate (cAMP) levels within cells. This increase, in turn, effectively hampers platelet aggregation and induces vasodilation.

3. Understanding How Cilostazol Works

Mechanism of Action of Cilostazol

Cilostazol operates by inhibiting PDE3, an essential enzyme in platelets and vascular smooth muscles, by inhibiting PDE3. The level of cAMP is heightened. This increase in cAMP effectively hinders platelet aggregation and directly causes blood vessels to dilate. These combined effects contribute to the alleviation of symptoms associated with intermittent claudication.

Effect of Cilostazol on the Body

The impact of Cilostazol on the body goes beyond just relieving symptoms. It has numerous effects that improve overall vascular health. These effects include enhancing blood flow by dilating arterial vessels and reducing the risk of blood clots by inhibiting platelet aggregation. Additionally, it improves the walking distance for individuals with peripheral vascular disease. These attributes make Cilostazol a valuable asset in treating peripheral vascular conditions.

4. Approved Uses of Cilostazol

List of FDA-approved Uses for Cilostazol

Cilostazol has been approved by the Food and Drug Administration (FDA) for treating intermittent claudication, a condition related to peripheral artery disease. This condition causes walking pain due to reduced blood flow—the drug functions by improving blood flow to the legs, thereby reducing symptoms and improving mobility.

Here are some references for you:

1. FDA

2. Mayo Clinic

Worldwide Variations in Approved Uses

Cilostazol's primary approved use remains consistent worldwide. However, certain countries have broadened its usage. In Japan, for example, it is also officially recommended for the secondary prevention of ischemic stroke. This endorsement is based on the findings of a large-scale multicenter clinical trial conducted within the country.

Here are some references for you:

1. Pubmed

Case Studies of Successful Treatments with Cilostazol

Various case studies have substantiated the impressive effectiveness of Cilostazol. A notable instance is highlighted in an influential publication, the Journal of Vascular Surgery, which reports substantial improvement in walking distance among patients with peripheral artery disease who received treatment with Cilostazol. Importantly. This study also affirms this medication's outstanding tolerability and commendable safety profile.

Here are some references for you:

1. Journal of Vascular Surgery

5. Off-label Uses of Cilostazol

Understanding Off-label Use in Medicine

Off-label use denotes the utilization of pharmaceutical drugs beyond their approved indication or prescribed parameters, such as age group, dosage level, or mode of administration. While off-label use may provoke contention at times, it can also demonstrate the drug's flexibility and potential effectiveness when used thoughtfully and substantiated by solid research.

Here are some references for you:

1. PubMed

Evidence for Off-label Use of Cilostazol

Various studies and clinical trials have indicated potential off-label uses of Cilostazol. Specifically, it has been investigated for its ability to prevent restenosis. The re-narrowing of blood vessels. Following percutaneous coronary intervention. Additionally, recent research shows that it may offer advantages in managing heart failure and diabetic nephropathy.

Here are some references for you:

1. Stat Pearls

Case Studies and Patient Testimonials

Multiple case studies and patient testimonials provide evidence for the advantageous effects associated with Cilostazol beyond its officially approved usage. Specifically, patients suffering from coronary artery disease have reported significant symptom relief and overall enhancement in their quality of life through off-label consumption of Cilostazol. While these stories are based on personal experiences rather than scientific data, they contribute to a growing corpus emphasizing the necessity for broader utilization opportunities surrounding this medication.

Here are some references for you:

1. WebMD

 

6. Dosage and Administration of Cilostazol

To effectively treat intermittent claudication, taking Cilostazol at a dosage of 100 mg twice daily is recommended. Taking the medication at least thirty minutes before or two hours after breakfast and dinner is essential. However, the appropriate dosage may differ based on individual patient needs and should always be overseen by a healthcare professional.

Tips for Safe and Effective Administration

It is essential to adhere to specific administration protocols to optimize the therapeutic benefits of Cilostazol and minimize any potential side effects. These protocols include keeping a regular schedule for taking the medication and ensuring that it is consumed with a full glass of water, and it is refraining from crushing, chewing, or breaking the tablet.

Adjustments in Dosage and Administration for Specific Populations

Adjustments in the dosage and administration of Cilostazol may be necessary for specific populations. For instance, individuals with kidney or liver impairment might require dosage adjustment. Moreover, it is essential to exercise caution when monitoring the elderly population as they have an increased potential for drug sensitivity.

7. Administration Considerations for Specific Populations

Cilostazol and Elderly Patients: Precautions and Guidance

Elderly patients may experience changes in how Cilostazol is processed in their bodies, called pharmacokinetics. Due to age-related changes, It is essential to be cautious when administering Cilostazol to this population. As advised by a healthcare professional, regular monitoring and adjustments to the dosage can help effectively manage any potential risks.

Use of Cilostazol During Pregnancy and Lactation

Pregnancy calls for cautious intake of Cilostazol, as its benefits must override any potential harm that may affect the fetus. The uncertainty surrounding whether this drug is eliminated through human milk necessitates carefully administering Cilostazol for breastfeeding mothers.

Administration to Children: Safety, Dosage, and Benefits

Considering insufficient findings on the safety and effectiveness of Cilostazol among pediatric patients, exercise utmost care before prescribing it for children. The decision to use this medication must weigh its prospective advantages against any plausible risks, ultimately considering patient well-being. Consequently, diligent supervision by a healthcare professional becomes indispensable as part of responsible administration protocols.

8. Interactions of Cilostazol with Other Drugs

Common Drug Interactions and How to Manage Them

Cilostazol may have an impact on the effectiveness of various medications. This is particularly true for anticoagulants, antiplatelet drugs, and certain antidepressants. Hence, patients must communicate all the medications they are currently using to their healthcare provider to prevent potential complications.

Understanding the Effects of Food and Alcohol on Cilostazol

The ingestion of food can enhance the bioavailability of Cilostazol, ultimately increasing its concentration within the body. Conversely, alcohol consumption may amplify the drug's ability to induce headaches, a prevalent side effect experienced by many individuals. Therefore, patients must adhere to a consistent eating schedule and exercise moderation when consuming alcoholic beverages.

How to Safely Combine Cilostazol with Other Medications

Adhering to the fundamental precept of 'start low and go slow' is crucial when incorporating Cilostazol with other medications by initially administering the lowest feasible dose. Practitioners can prudently gauge its impact on the patient. Subsequently, if deemed necessary, they can gradually escalate the dosage while diligently evaluating how well their body reacts to this combination therapy.

9. Side Effects of Cilostazol

Commonly Observed Side Effects

Like other medications available on the market today, Cilostazol has its fair share of potential side effects that users should be aware of. These commonly reported adverse reactions include but are not limited to headache discomforts accompanied by episodes of diarrhea which may at times cause one's stool consistency to become irregular while also affecting heart rhythm resulting in vibrations being felt by some individuals consuming this pharmaceutical agent. Fortunately though, for most patients partaking in a prescribed course of treatment involving Cilostazol, such symptoms tend not to be severe, eventuating into more manageable levels as their bodily system begins accommodating said medication accordingly over time, albeit should anyone experience persistent occurrences or debilitating inconveniences immediate consultation with a healthcare professional should be sought.

Understanding Severe and Rare Side Effects

Severe side effects, although occurring less often, may take place. These may encompass chest pain, a fast or irregular heartbeat, and bleeding or bruising. It is important to seek medical attention if these symptoms become apparent promptly. Furthermore, a small percentage of individuals who use this product might encounter hypersensitivity reactions like rash, itching, or hives.

Tips to Manage and Mitigate Side Effects

If you experience headaches, over-the-counter pain relievers can provide some relief. Additionally, regular breaks from activities have effectively reduced headaches' frequency and intensity. In the case of diarrhea, it is advisable to maintain proper hydration and consider adopting a bland diet until the symptom subsides. Furthermore. If palpitations become an issue. Practicing relaxation techniques can prove beneficial. While simultaneously limiting one's intake of caffeine.

10. Warnings, Contraindications, and Precautions for Cilostazol Use

Important Warnings for Patients Using Cilostazol

It is advisable for individuals suffering from congestive heart failure to refrain from using Cilostazol as this may worsen their condition. Moreover, patients who are scheduled for surgery should inform their doctor about their usage of Cilostazol as there is a possibility that the medication could impact bleeding.

Contraindications: Who Should Not Take Cilostazol

Patients who have heart failure, regardless of its severity are advised not to take cilostazol. Furthermore, the drug should not be given to individuals who are known or suspected to have an allergic reaction to any of its ingredients.

Precautions to Take for Safe Usage of Cilostazol

Patients are kindly advised to inform their healthcare provider about any medical conditions they may have. Particularly kidney or liver diseases, bleeding disorders, and other heart conditions. It is further recommended that blood counts and liver function be regularly monitored in certain circumstances.

11. Dealing with Overdosage of Cilostazol

Signs and Symptoms of Cilostazol Overdose

Although uncommon. An overdose of Cilostazol has the potential to manifest in individuals with notable symptoms, including severe headaches, bloody stools, and low blood pressure levels accompanied by a rapid and irregular heartbeat. Notably, it is imperative to acknowledge that these symptoms correspond directly with the ingested dosage.

Immediate Steps to Take in Case of Overdose

If there are indications of a potential overdose, it becomes paramount to get the individual to the emergency department without delay quickly. While waiting for medical help upholding a tranquil and comfortable environment for them becomes vital. Notably, under no circumstances should forced emesis ever be attempted at home.

Recovery and Long-term Effects of Overdosage

The approach taken in treating an overdose usually revolves around providing necessary support to preserve vital bodily functions. Swift medical attention often results in complete patient recovery and minimal long-term implications. However, it is imperative to recognize that any potential lasting effects will hinge upon the extent of the overdose and an individual's general state of health.

12. Storage and Handling Precautions for Cilostazol

Best Practices for Storing Cilostazol

The stability and effectiveness of Cilostazol are greatly influenced by how it is stored. To ensure optimal storage conditions it is recommended to store the medication at room temperature specifically between 20 25°C (68 77°F). It is important to keep it away from moisture and light. As these can potentially impact the quality of the medication. Avoid storing Cilostazol in bathrooms or other damp areas. As the humidity present there could compromise its effectiveness. Additionally it is advisable to retain the medication in its original packaging until it is ready to be consumed.

Safety Measures While Handling Cilostazol

When handling Cilostazol, it is essential to take certain safety precautions. To ensure the medication's effectiveness. The tablets should be swallowed whole and not crushed or chewed. Additionally, washing your hands before and after handling the medication is crucial. If, by accident, the medication comes into contact with your eyes or mouth, make sure to rinse thoroughly with water. If any discomfort persists, seek medical advice promptly.

Disposal of Unused or Expired Cilostazol

Ensuring the proper disposal of unused or expired medication is imperative to avoid unintentional ingestion and environmental contamination. Therefore. It is strongly advised against disposing of cilostazol through regular household waste or flushing it down the toilet. Instead, the most suitable course of action is to return unused or expired medication to a pharmacy as they possess the necessary capabilities to dispose of it safely and efficiently. Alternatively, patients may seek guidance on drug disposal from the FDAs guidelines or their local waste disposal agency for further information.

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