Careload Beraprost Sodium Sustained-release Tablets

1. Indications and Usage
Chronic Arterial Occlusive Disease: Indicated to improve symptoms such as ulcers, intermittent claudication, pain, and coldness associated with chronic arterial occlusive disease.
Primary Pulmonary Hypertension: Indicated to improve the exercise tolerance of patients with WHO functional class I-III pulmonary hypertension (PAH).
2. Dosage and Administration
Adults: The initial dose is typically 120 μg per day, administered orally in divided doses (e.g., after breakfast and dinner).
Dosage Adjustment: The dosage may be gradually increased depending on the patient’s symptoms and tolerability, but the maximum daily dose should not exceed 360 μg.
Administration Instructions: These are sustained-release tablets and must be swallowed whole. They should not be split, crushed, chewed, or powdered, as this would destroy the sustained-release structure and could lead to overdose.
3. Mechanism of Action
IP Receptor Activation: Beraprost sodium is a stable analogue of prostacyclin (PGI2) that binds to IP receptors on platelets and vascular smooth muscle cells.
Vasodilation: This binding activates adenylate cyclase, increasing intracellular cyclic AMP (cAMP), which leads to relaxation of vascular smooth muscle and significant vasodilation.
Antithrombotic Effects: It inhibits calcium influx and thromboxane A2 generation, thereby suppressing platelet aggregation and exerting dual antithrombotic and vasodilatory effects to improve blood flow.
4. Safety and Warnings
Bleeding Risk: This medication may increase the risk of bleeding (e.g., intracranial, gastrointestinal, retinal, or subcutaneous bleeding). Caution is required in patients with bleeding tendencies.
Hypotension and Syncope: May cause blood pressure drops, tachycardia, fainting, or syncope. Patients should be cautious when driving or operating heavy machinery.
Contraindications: Contraindicated in patients with active bleeding tendencies (e.g., hemophilia, upper gastrointestinal bleeding, retinal hemorrhage) and pregnant or potentially pregnant women.
Other Serious Risks: Interstitial pneumonia, liver function abnormalities (e.g., elevated ALT/AST), and myocardial infarction may occur.
5. Adverse Reactions and Clinical Research
Adverse Reactions: The most common adverse reactions include headache, facial flushing, and feelings of heat. Less common reactions include nausea, diarrhea, palpitations, abdominal pain, and fatigue.
Clinical Research: Clinical trials in patients with pulmonary hypertension have demonstrated that beraprost sodium significantly improves exercise tolerance and quality of life while delaying disease progression.
6. Drug Interactions
Anticoagulants and Antiplatelets: Concomitant use with agents such as warfarin, heparin, or aspirin may potentiate the risk of bleeding.
Thrombolytic Agents: Use with thrombolytic agents requires extreme caution due to the additive risk of hemorrhage.
Renal Impairment: Patients with renal dysfunction may exhibit increased maximum plasma concentration (Cmax) and area under the curve (AUC), necessitating careful dose titration.
7. Pharmaceutical Information
Composition: The active ingredient is beraprost sodium.
Appearance: White to slightly yellow tablets.
Storage: Store in a light-proof, tightly sealed container. Protect from moisture and store at a controlled room temperature not exceeding 25°C.