beraprost

Action and Spectrum

Actions and Spectrum: 

beraprost is a medication used to treat various cardiovascular and circulatory conditions. It primarily belongs to the class of drugs known as prostacyclin analogs or prostaglandin I2 (PGI2) analogs.  

Action: 

beraprost is a synthetic analog of prostacyclin (PGI2), a naturally occurring prostaglandin in the body. 

Prostacyclin is a potent vasodilator and also inhibitor of platelet aggregation, making it essential for maintaining normal blood vessel function and preventing blood clots. 

beraprost mimics the effects of prostacyclin by binding to the same receptors (IP receptors) on blood vessel walls and platelets. 

Spectrum: 

Pulmonary Arterial Hypertension (PAH): beraprost primarily treats pulmonary arterial hypertension. PAH is a condition characterized by elevated blood pressure in the pulmonary arteries, leading to increased resistance to blood flow in the lungs. beraprost helps dilate pulmonary blood vessels, reducing this resistance and improving blood flow. 

Peripheral Vascular Diseases: beraprost can also treat peripheral vascular diseases like intermittent claudication. These conditions involve reduced blood flow to the extremities (e.g., legs) due to arterial narrowing or blockage. beraprost’s vasodilatory properties can help improve circulation in these areas. 

Drug Interaction

Adverse Reaction

Frequency not defined 

Headache 

Enhanced liver enzymes 

Hot flushes 

GI upset 

Dizziness 

Tendency 

Enhanced triglycerides  

Enhanced bilirubin 

Black Box Warning

Black Box Warning: 

None 

Contraindication / Caution

Contraindication/Caution: 

Contraindication 

• Hypersensitivity: beraprost should not be used in individuals with a known hypersensitivity or allergy to beraprost or its components. Allergic reactions can be severe and life-threatening. 
• Severe Bleeding Disorders: beraprost can inhibit platelet aggregation and increase the risk of bleeding. It should be used cautiously or avoided in individuals with severe bleeding disorders or a history of bleeding problems. 
• Active Gastric or Duodenal Ulcers: beraprost may increase the risk of gastrointestinal bleeding. Therefore, it should be used cautiously or avoided in individuals with active gastric or duodenal ulcers. 
• Severe Liver or Kidney Impairment: beraprost is metabolized in the liver, and its elimination may be impaired in individuals with severe liver impairment. Similarly, individuals with severe kidney impairment may also have altered drug metabolism. beraprost should be used cautiously and with dose adjustments in such cases. 
• Pregnancy and Breastfeeding: The safety of beraprost during pregnancy and breastfeeding is not well-established. It should only be used during pregnancy condition or breastfeeding if the potential benefits outweighs the potential risks. Healthcare providers should carefully evaluate the risks and benefits in these situations. 
• Children: beraprost’s safety and efficacy in pediatric patients are not well-established. It is generally not recommended for children unless a pediatric specialist prescribes it. 
• Interactions with Other Medications: beraprost may interact with other medications, potentially leading to adverse effects or reduced effectiveness. Healthcare providers should know the patient’s medication history to assess potential interactions. 
• Uncontrolled Hypertension: beraprost can cause vasodilation, which may lower blood pressure. It should be used cautiously in individuals with uncontrolled low blood pressure (hypotension). 

Caution 

• Dosage and Titration: beraprost should be taken as prescribed by a healthcare provider. It may require careful dosage titration to achieve the desired therapeutic effect while diminishing side effects. Follow your healthcare provider’s instructions closely. 
• Monitoring: Regular monitoring by a healthcare provider is essential when using beraprost. This includes assessments of your blood pressure, heart rate, and symptoms to ensure that the medication is working effectively and not causing any of the adverse effects. 
• Drug Interactions: beraprost may interact with other medications you are taking. Inform the healthcare professional about all the prescription and over-the-counter drugs, supplements, and herbal products you use to check for potential interactions. 
• Bleeding Risk: beraprost can inhibit platelet aggregation and increase the risk of bleeding. If you take other anticoagulant or antiplatelet medications (e.g., aspirin or warfarin), your bleeding risk may increase.  
• Gastrointestinal Effects: beraprost may cause gastrointestinal side effects, such as nausea, vomiting, and diarrhea. If you experience severe or persistent gastrointestinal symptoms, contact your healthcare provider. 
• Blood Pressure: beraprost can lower blood pressure, which may lead to dizziness or fainting, significantly when changing positions (e.g., getting up from a seated or lying position). Be cautious when rising from a sitting or lying position and report any significant drops in blood pressure to your healthcare provider. 
• Liver and Kidney Function: If you have pre-existing liver or kidney conditions, your healthcare provider may need to adjust the dose of beraprost or closely monitor your liver and kidney function during treatment. 
• Pregnancy and Breastfeeding: If you are pregnant or planning to become pregnant condition or breastfeeding, discuss the risks and benefits of using beraprost with your healthcare provider. The safety of beraprost in these situations is not well-established. 
• Children and Adolescents: beraprost’s safety and effectiveness in children and adolescents have not been well-studied. Its use in pediatric populations should be carefully considered and prescribed by a specialist if necessary. 
• Allergic Reactions: If you experience any of the signs of an allergic reaction (e.g., rash, itching, swelling of the face/throat, severe dizziness, difficulty breathing), seek immediate medical attention. 

Pregnancy / Lactation

Pregnancy consideration:  

US FDA pregnancy category: Not assigned 

Lactation:   

Excreted into human milk: Not known. 

Pregnancy category: 

• Category A: well-controlled and Satisfactory studies show no risk to the fetus in the first or later trimester. 
• <b>Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women. 
• Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.    
• Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.    
• Category X: Drugs listed in this category outweigh the risks over benefits. Hence, these categories of drugs need to be avoided by pregnant women.    
• Category N: There is no data available for the drug under this category. 

Pharmacology

Pharmacology: 

beraprost is a synthetic prostacyclin (PGI2) analog that exerts the pharmacological effects by binding to and activating IP (prostacyclin) receptors. As a prostacyclin analog, beraprost primarily acts as a potent vasodilator, inhibits platelet aggregation, and exerts anti-inflammatory properties.

It relaxes vascular smooth muscle, dilating pulmonary and systemic arteries, reducing pulmonary vascular resistance and increasing cardiac output. This makes it particularly useful in treating pulmonary arterial hypertension (PAH) by improving blood flow in the pulmonary circulation and alleviating PAH-related symptoms. Additionally, beraprost’s antiplatelet effects reduce the risk of blood clot formation. 

Pharmacodynamics: 

Mechanism of action: The action of beraprost is closely related to its role as a synthetic analog of prostacyclin (also known as prostaglandin I2 or PGI2), a naturally occurring prostaglandin in the body. beraprost primarily acts by binding to and activating IP (prostacyclin) receptors.  

Activation of IP Receptors: 

beraprost exerts its primary pharmacological effects by selectively binding to and activating IP receptors located on the surface of cells, particularly endothelial cells in blood vessels and platelets. 

Vasodilation: 

Activation of IP receptors on endothelial cells leads to cyclic adenosine monophosphate (cAMP) within these cells. 

Elevated cAMP levels relax vascular smooth muscle cells in blood vessel walls, leading to vasodilation (widening of blood vessels). 

Vasodilation reduces peripheral vascular resistance, which lowers blood pressure and improves blood flow in the pulmonary and systemic circulation. 

Inhibition of Platelet Aggregation: 

beraprost’s activation of IP receptors on platelets inhibits platelet aggregation and adhesion. 

This antiplatelet effect reduces the risk of abnormal blood clot formation (thrombosis) within blood vessels, which is particularly important in conditions like pulmonary arterial hypertension (PAH), where blood clotting in the pulmonary arteries can be problematic. 

Anti-Inflammatory Properties: 

Prostacyclin analogs, including beraprost, have demonstrated anti-inflammatory properties in some studies. 

These properties may help reduce inflammation and vascular remodeling associated with certain cardiovascular conditions. 

Pharmacokinetics: 

Absorption 

beraprost is typically administered orally in the form of tablets or capsules. 

After oral administration, beraprost is absorbed from the gastrointestinal tract, primarily in the small intestine. 

Its absorption may be influenced by factors such as food, which can slow down the absorption rate. 

Distribution 

Once absorbed into the bloodstream, beraprost is distributed throughout the body. 

It has a relatively short half-life, quickly metabolized and eliminated from the body. 

beraprost binds to plasma proteins, which can affect its distribution and availability for action. 

Metabolism 

beraprost undergoes metabolism in the liver through various enzymatic pathways. 

One of the primary metabolic pathways involves the conversion of beraprost to its active metabolite, beraprost-315. 

Cytochrome P450 enzymes, specifically CYP2C9 and CYP2C8, are involved in the metabolism of beraprost. 

Elimination and Excretion 

beraprost and its metabolites are primarily eliminated from the body through renal excretion. 

After metabolism, the resulting metabolites are excreted in the urine, allowing for their elimination from the body. 

Adminstartion

Administration: 

beraprost is typically administered orally in the form of tablets or capsules. The specific dosage and dosing schedule may vary depending on your medical condition, the formulation of the medication, and your healthcare provider’s recommendations.  

• Dosage: Your healthcare provider will determine The dosage of beraprost based on your medical condition and individual response to the medication. The usual starting dose for adults with pulmonary arterial hypertension (PAH) is often 20 micrograms (mcg) taken thrice daily. However, dosing can vary, and your healthcare provider may adjust the dosage. 
• Take with or without Food: beraprost can be taken with or without food. However, taking it with food may help reduce the likelihood of experiencing gastrointestinal side effects such as nausea. 
• Swallow Whole: Swallow the beraprost tablets or capsules whole with a glass of water.  
• Adherence to Schedule: It’s essential to take beraprost precisely as prescribed, at the exact times each day. This helps maintain a consistent level of the medication in your bloodstream, which is essential for its effectiveness. 
• Missed Dose: If a dose is missed, taking it as soon as possible is generally recommended. However, if the next scheduled dose is missed, it should be skipped and the following dose should be taken at the appropriate time. It is key to avoid taking a double dose of the drug in order to compensate for the missed dose. 
• Duration of Treatment: Continue taking beraprost for the entire duration prescribed by your healthcare provider, even if you start to feel better. Stopping the medication abruptly can have adverse effects. 
• Monitoring: Healthcare provider will likely to monitor your progress and may adjust your beraprost dosage based on your response to treatment and any potential side effects. Be prepared for regular check-ups and follow-up appointments. 
• Medication Interactions: Inform your healthcare provider of all the drugs, supplements, and also herbal products you are taking, as beraprost may interact with certain drugs. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: beraprost 

Why do we use beraprost? 

beraprost is a medication primarily used to treat certain cardiovascular and circulatory conditions. Its primary therapeutic use is in managing pulmonary arterial hypertension (PAH), but it may also have applications in other related conditions.  

• Pulmonary Arterial Hypertension (PAH): beraprost is approved for treating pulmonary arterial hypertension (PAH). PAH is a infrequent and severe condition characterized by elevated BP in the pulmonary arteries, which can lead to enhanced resistance to blood flow in the lungs. beraprost helps to relax and dilate the blood vessels in the lungs, reducing this resistance and improving blood flow. This can relieve symptoms such as shortness of breath and fatigue and improve exercise tolerance in PAH patients. 
• Peripheral Vascular Diseases: beraprost may also treat peripheral vascular diseases. These conditions involve reduced blood flow to the extremities (typically the legs) due to arterial narrowing or blockage. By dilating blood vessels, beraprost can help improve limb circulation, reducing symptoms like intermittent claudication (pain and cramping during physical activity).