Cyclandelate - Indications, Dosage, and Adverse Drug Reactions

Introduction

Cyclandelate is a pharmaceutical agent categorized as a vasodilator, belonging to a class of drugs known for expanding the diameter of blood vessels. This results in widening the blood vessels and increased blood flow to certain body parts. The Food and Drug Administration (FDA) approved this drug under cyclospasmol in 1958 for intermittent claudication and cognitive dysfunction in Alzheimer’s disease.

However, it was withdrawn from the market due to its lack of effectiveness. The drug has been approved to treat various conditions that involve reduced blood flow to the limbs, such as peripheral vascular disease and Raynaud's disease. Peripheral vascular disease is a common condition affecting millions worldwide, particularly those over 50.

This condition occurs when plaque accumulates within the arteries, causing a reduction in blood flow to the limbs. Studies have demonstrated the efficacy of Cyclandelate in enhancing blood circulation to the affected regions, offering relief from symptoms, and enhancing the overall quality of life for individuals experiencing these conditions. It is available in the form of tablets and is taken orally.

Determining the appropriate dosage and duration of treatment for Cyclandelate will vary based on the particular condition being addressed, and it is essential to consult a healthcare professional for guidance in this regard. They will assess the individual's needs and prescribe the appropriate dosage and duration of treatment accordingly. As with all medications, Cyclandelate can cause side effects, and patients should be aware of the potential risks and benefits before starting treatment. This article will take a closer look at Cyclandelate, its mechanism of action, dosage, side effects, and precautions.

Mechanism of Action

Cyclandelate is classified as a vasodilator medication that operates by inhibiting the enzyme phosphodiesterase. This enzyme breaks down cyclic adenosine monophosphate (cAMP), ultimately leading to the relaxation of smooth muscles and the widening of blood vessels. As a result, blood flow to the affected areas increases. In simpler terms, Cyclandelate relaxes the walls of blood vessels, expanding their diameter and improving blood flow to the affected regions. This mechanism of action makes it an effective treatment for conditions characterized by reduced blood flow to the limbs, such as peripheral vascular disease and Raynaud's disease. It helps alleviate symptoms and enhance circulation in these conditions.

Clinical Drug Trials for Cyclandelate

Several clinical trials have been conducted to evaluate the effectiveness and safety of Cyclandelate in the treatment of various circulatory disorders.

Some of the notable clinical trials are

1. A placebo-controlled, double-blind, randomized study was undertaken to assess the efficacy and safety of Cyclandelate in patients diagnosed with cerebral insufficiency. The study found that Cyclandelate was well-tolerated and improved cognitive function in some patients.

2. A clinical trial was conducted to assess the effectiveness and safety of Cyclandelate in patients diagnosed with peripheral arterial disease. The study followed a double-blind, randomized, and placebo-controlled design, ensuring rigorous evaluation of the medication's efficacy and safety profile. The study found that Cyclandelate improved walking distance and reduced symptoms such as pain and numbness in the legs.

Indications of Cyclandelate

Cyclandelate is a medication used to treat various conditions involving reduced blood flow to the limbs.

Some of the most common uses of Cyclandelate include:

1. Peripheral Vascular Disease: Cyclandelate is prescribed for treating peripheral vascular disease, which pertains to impaired blood vessels outside the heart and brain. This condition arises from plaque accumulation within the arteries, reducing blood flow to the limbs. Consequently, individuals may experience pain, numbness, and tingling in their legs and feet. Cyclandelate can help improve blood flow to the affected areas and alleviate these symptoms.

2. Raynaud's Disease: Cyclandelate is also used to treat Raynaud's disease, a less common condition affecting the blood flow to the fingers and toes, causing them to turn white or blue and feel cold and numb. Cyclandelate can help improve blood flow to the affected areas and alleviate symptoms.

3. Cerebral Vascular Insufficiency: Cyclandelate is a medication that can treat cerebral vascular insufficiency, a condition characterized by insufficient blood flow to the brain. This condition can cause symptoms such as confusion, dizziness, and headaches. Cyclandelate can help improve blood flow to the brain and alleviate these symptoms.

4. Headaches: Cyclandelate can also be used to treat headaches caused by reduced blood flow to the head. Cyclandelate, by enhancing blood flow to the affected regions, can aid in alleviating these headaches.

Information About the Dosage

Cyclandelate is available in tablet form and is typically taken orally, with or without food.

The following information provides a general guideline for the recommended dosages of Cyclandelate:

1. Peripheral Vascular Disease: The usual adult dose of Cyclandelate for treating peripheral vascular disease is 200 to 400 milligrams (mg) taken thrice daily. The total daily dose should be at most 1,200 mg.

2. Raynaud's Disease: The usual adult dose of cyclandelate for treating Raynaud's disease is 200 to 400 mg, taken three times a day. The total daily dose should be at most 1,200 mg.

3. Cerebral Vascular Insufficiency: The usual adult dose of cyclandelate for treating cerebral vascular insufficiency is 400 to 600 mg, taken thrice daily. The total daily dose should be at most 1,800 mg.

4. Headaches: The usual adult dose of Cyclandelate for headaches is 200 to 400 mg, taken thrice daily. The total daily dose should be at most 1,200 mg.

5. Pregnancy and Breastfeeding: There is limited information about the safety of Cyclandelate during pregnancy and breastfeeding. Therefore, it is important to consult a healthcare provider if you are pregnant or breastfeeding before using this medication. The use of Cyclandelate during pregnancy should be avoided unless the benefits outweigh the potential risks.

6. Renal Impairment: Patients with renal impairment may require a dosage adjustment of Cyclandelate. The dosage should be decreased in patients with moderate to severe renal impairment. In such cases, the medication should be used with caution and under the supervision of a healthcare provider. The usual dose is 200-400 mg two to three times a day for patients with mild to moderate renal impairment. The dose should be reduced to 100-200 mg two to three times daily in patients with severe renal impairment.

7. Hepatic Impairment: Patients with hepatic impairment may also require a dosage adjustment of Cyclandelate. The dosage should be decreased in patients with moderate to severe hepatic impairment. In such cases, the medication should be used with caution and under the supervision of a healthcare provider. The usual dose is 200-400 mg two to three times a day for patients with mild to moderate hepatic impairment. The dose should be reduced to 100-200 mg two to three times daily in patients with severe hepatic impairment.

8. Geriatric Patients: Geriatric patients may require a dosage adjustment of Cyclandelate. For elderly patients with impaired renal or hepatic function, as well as individuals who are sensitive to the effects of the medication, it is advisable to reduce the dosage of Cyclandelate. The drug should be used cautiously, as they may be more susceptible to the side effects of the medication. The recommended dose for elderly patients is 200-400 mg two to three times a day.

9. Pediatric Patients: The safety and effectiveness of Cyclandelate have not been established in pediatric patients.

Warnings and Precautions

Cyclandelate is a medication used to treat various conditions, including peripheral vascular disease and cerebral vascular insufficiency. However, like all medications, Cyclandelate has certain warnings and precautions that should be considered before use.

Some of the key warnings and precautions associated with Cyclandelate include:

1. Hypotension: Cyclandelate is a vasodilator that can lower blood pressure. Patients with hypotension or low blood pressure should use Cyclandelate cautiously, as the medication can further lower blood pressure and cause symptoms such as dizziness and lightheadedness.

2. Bleeding Disorders: Cyclandelate can increase the risk of bleeding, particularly in patients with bleeding disorders or those taking blood-thinning medications. Use caution in these patients, and closely monitor for any indications of bleeding, such as easy bruising or prolonged bleeding following an injury.

3. Pregnancy and Breastfeeding: The safety of Cyclandelate during pregnancy and breastfeeding has not been established, and the medication should only be used if the potential benefits outweigh the potential risks.

4. Hepatic and Renal Impairment: Patients with hepatic or renal impairment should exercise caution when using Cyclandelate, as these conditions can impact the metabolism and elimination of the medication. It may be necessary to administer a lower dosage of Cyclandelate to individuals with impaired liver or kidney function.

5. Elderly Patients: Elderly patients may be more susceptible to experiencing side effects of Cyclandelate, including dizziness and lightheadedness. Therefore, monitoring these individuals closely for such adverse effects is important. These patients may require a lower dosage of Cyclandelate and should be monitored closely for side effects.

6. Allergic Reactions: Patients with a history of allergic reactions to Cyclandelate or other vasodilators should avoid using this medication. Signs of an allergic reaction include a rash, hives, itching, swelling of the face, difficulty breathing, and swelling of the lips, tongue, or throat.

7. Alcohol Consumption: While using Cyclandelate, it is advisable to refrain from consuming alcohol as it can heighten the risk of side effects like dizziness and lightheadedness.

8. Driving and Operating Machinery: Cyclandelate can cause dizziness and drowsiness, impairing the ability to drive or operate machinery. Patients should use caution when performing these activities.

Adverse Reaction of Cyclendelate Drug

Cyclandelate is a medication that is generally well-tolerated by most patients. However, like all medications, Cyclandelate can cause side effects in some individuals.

Some of the most common adverse reactions associated with Cyclandelate include:

• Gastrointestinal Disturbances: Gastrointestinal disturbances such as nausea, vomiting, and diarrhea are among Cyclandelate's most common side effects.

• Headache: Headache is another common side effect of Cyclandelate.

• Dizziness and Lightheadedness: Cyclandelate, as a vasodilator, dilates blood vessels and lowers blood pressure. Consequently, it can induce symptoms like dizziness and lightheadedness.

• Flushing: Cyclandelate can cause flushing or redness of the skin, particularly in the face and neck.

• Tachycardia: Tachycardia, or a rapid heart rate, may occur in some patients taking cyclandelate.

• Allergic Reactions: While rare, allergic reactions to cyclandelate can occur. Signs of an allergic reaction are rash, hives, rash itching, swelling of the face, difficulty breathing, and difficulty breathing on the lips, tongue, or throat.

• Bleeding Disorders: Cyclandelate can increase the risk of bleeding, particularly in patients with bleeding disorders or those taking blood-thinning medications.

• Hypotension: Cyclandelate can lower blood pressure, particularly in patients with pre-existing hypotension or low blood pressure.

• Other Side Effects: Other potential side effects of Cyclandelate include palpitations, sweating, dry mouth, and fatigue.

Drug Interaction for Cyclandelate

Cyclandelate may interact with other medications, including prescription, over-the-counter, and herbal supplements. Patients must disclose all medications they are taking to their healthcare provider before initiating Cyclandelate treatment.

Some of the medications that may interact with Cyclandelate include:

• Antihypertensive medications: Cyclandelate can lower blood pressure, and when used in combination with other antihypertensive medications, Cyclandelate can lower blood pressure, and when used in combination with other antihypertensive medication. It can result in a significant drop in blood pressure. Patients taking other antihypertensive medications should use Cyclandelate with caution. Patients taking other antihypertensive medications should use Cyclandelate with caution.

• Blood-thinning Medications: Cyclandelate can increase the risk of bleeding, particularly in patients taking blood-thinning medications such as warfarin, heparin, or aspirin. Patients taking these medications should use Cyclandelate with caution.

• Caffeine: Caffeine can increase the effects of Cyclandelate and may lead to jitteriness, nervousness, and difficulty sleeping. Patients should limit their caffeine intake while taking Cyclandelate.

• Alcohol: Alcohol can increase the effects of Cyclandelate and may lead to dizziness, lightheadedness, and fainting. Patients should avoid alcohol while taking Cyclandelate.

• Other Vasodilators: Cyclandelate is a vasodilator, and when used in combination with other vasodilators, it can result in a significant drop in blood pressure. Patients taking other vasodilators should use Cyclandelate with caution.

• Herbal Supplements: Some herbal supplements, such as ginkgo biloba and garlic, may increase the risk of bleeding when combined with Cyclandelate.

Information for the Doctor's

Description of Cyclendelate Tablet Composition

Cyclandelate is available in several forms, including tablets, capsules, and injections.

• The tablet form of Cyclandelate is usually available in strengths of 200 mg or 400 mg. It is typically taken two to four times daily, depending on the treated condition.

• The capsule form of Cyclandelate is usually available in strengths of 200 mg or 400 mg. It is typically taken two to four times daily, depending on the treated condition.

• A healthcare provider typically administers the injectable form of Cyclandelate within a hospital or clinic setting. The dosage and frequency of injections will vary depending on the treatment condition. The dosage and frequency of injections will vary depending on the treatment condition.

• Each Cyclandelate tablet contains 200 mg of the active ingredient Cyclandelate and several inactive ingredients such as microcrystalline cellulose, magnesium stearate, and colloidal silicon dioxide.

Pharmacodynamics

Cyclandelate acts on the vascular smooth muscle by increasing cyclic adenosine monophosphate (cAMP) and cyclic guanosine monophosphate (cGMP), both important secondary messenger molecules involved in smooth muscle relaxation. This leads to vasodilation and improved blood flow to the affected areas.

Pharmacokinetics

Absorption

Cyclandelate is well absorbed after oral administration, with an estimated bioavailability of 80 %. It is rapidly absorbed from the gastrointestinal tract, with peak plasma concentrations achieved within 2-3 hours after administration. The absorption of Cyclandelate is not significantly affected by food, so it can be taken with or without meals.

Metabolism

Cyclandelate is extensively metabolized in the liver via hydrolysis and oxidation. The primary metabolites of Cyclandelate are the monohydroxy derivative (M1) and the dihydroxy derivative (M2). M1 is formed by hydrolysis of the ester bond in Cyclandelate, while M2 is formed by further oxidation of M1. Both metabolites are pharmacologically active, although they are less potent than Cyclandelate.

Elimination

Cyclandelate and its metabolites are eliminated primarily via the kidneys. The elimination half-life of Cyclandelate is approximately 2.5 to 3 hours, while the half-life of M1 and M2 is longer, approximately four to six hours. The major route of elimination is renal excretion, with approximately 70 to 80 % of a dose excreted in the urine, mainly as the glucuronide conjugates of Cyclandelate and its metabolites. The remainder of the dose is excreted in the feces.

Pharmacokinetic Variability

The pharmacokinetics of Cyclandelate can be affected by various factors, including age, gender, and hepatic or renal impairment. In elderly patients, the elimination half-life of Cyclandelate may be prolonged due to decreased hepatic and renal function. In patients with hepatic or renal impairment, the clearance of Cyclandelate may be reduced, leading to higher plasma concentrations and a higher risk of adverse effects. Gender differences in the pharmacokinetics of Cyclandelate have also been observed, with women having a lower clearance than men.

Drug Interactions

Cyclandelate is metabolized by cytochrome P450 enzymes in the liver, primarily by CYP3A4 and CYP2C9. Therefore, drugs that inhibit or induce these enzymes may affect the pharmacokinetics of Cyclandelate. For example, drugs that inhibit CYP3A4, such as Ketoconazole or Erythromycin, may increase plasma concentrations of Cyclandelate.

For Patients

What Is Cyclandelate Used For?

Cyclandelate is a medication utilized to enhance blood flow to specific body areas. It achieves this by relaxing the muscles in the walls of blood vessels, thereby facilitating increased blood circulation. Cyclandelate is often used to treat conditions such as peripheral vascular disease, Raynaud's phenomenon, and other circulation disorders.

Peripheral vascular disease is a medical condition characterized by the narrowing or blockage of blood vessels responsible for supplying blood to the arms and legs. This restriction in blood flow can lead to various symptoms and complications. This can lead to pain, cramping, and difficulty walking. Raynaud's phenomenon is a medical condition where the blood vessels in the fingers and toes experience episodes of constriction, causing symptoms like numbness, tingling, and pain.

Cyclandelate helps to improve blood flow to these areas, which can help to alleviate symptoms and improve the quality of life for patients. It can also be used to treat other conditions, such as cerebral insufficiency, which is a condition in which there is not enough blood flow to the brain.

What Are the Side Effects of Cyclandelate?

Like all medications, Cyclandelate can cause side effects. Common side effects of Cyclandelate include headaches, dizziness, nausea, vomiting, diarrhea, and stomach upset. Some patients may also experience flushing, sweating, or changes in their heart rate. If someone experiences these side effects, they should speak with their doctor.

How Does Cyclandelate Interact With Other Drugs?

Cyclandelate may interact with other drugs, including blood thinners, aspirin, and other medications that affect blood clotting. It is important to inform the doctor about all the medications, including over-the-counter drugs and supplements. The doctor may need to adjust the dosage or monitor more closely if taking other medications that can interact with Cyclandelate.

How Should Cyclandelate Be Taken?

• Follow the doctor's instructions carefully.

• Take two to four times daily, before meals and bedtime, with a full glass of water.

• Store Cyclandelate at room temperature, away from moisture and heat.

• For missed doses, skipping and continuing with the regular dosing schedule is advised to avoid double dosing.

What Precautions Should Be Taken While Using Cyclandelate Tablets?

It is important to take precautions while using Cyclandelate. For example, avoid alcohol, as it can increase the risk of side effects such as dizziness and flushing. It is important to refrain from engaging in activities that demand mental alertness, such as driving or operating heavy machinery while using Cyclandelate. If someone has a history of bleeding disorders, liver or kidney disease, pregnancy, or breastfeeding, the doctor should be informed before taking Cyclandelate. It is important to take Cyclandelate precisely as the doctor prescribes and consult them before changing the dosage.

Conclusion

Cyclandelate is a medication utilized to enhance blood flow to specific body areas. It can effectively treat peripheral vascular disease and Raynaud's phenomenon. However, it can cause side effects and may interact with other medications. Therefore, patients should take precautions while using Cyclandelate and inform their doctor about medical conditions or if taking any other medications.