What Is Beraprost?

Derivatives of prostaglandin prostaglandin (PGI2). Among various humoral factors synthesized by the blood vessel wall, prostaglandin (PGI2) is the earliest listed substance that can regulate blood vessel tension and play an important role in maintaining blood flow in various tissues.

Chinese name: Beraprost
Foreign name: Beraprost

Main indications: Treatment of ulcers caused by chronic arterial occlusive disease
Drug type: Antiplatelet drugs

Basic information

Chinese name:

Chinese alias: 2,3,3A-8B-tetrahydro-2-hydroxy-1- (3-hydroxy-4-methyl-1-octene-6-alkynyl) -1H-cyclopenta [B] benzene Benzofuran-5-butanoic acid; 2,3,3A, 8B-tetrahydro-2-hydroxy-1- (3-hydroxy-4-methyl-1-octene-6-alkynyl) -1 H-ring Pentamyl [B] benzofuran-5-butanoic acid

English name: Beraprost

English alias: Unii-35E3njj4o6; 2-Hydroxy-1- (3-hydroxy-4-methyl-1-octen-6-ynyl) -2,3,3A, 8B-tetrahydro-1H-cyclopenta (B) benzofuran-5 -butanoic acid; Domer; Befaprost; ML 1229; Beraprostum

CAS number: 88430-50-6

Molecular formula: C ₂₄ H ₃₀ O ₅

Molecular weight: 398.49200

Exact mass: 398.20900

PSA: 86.99000

LogP: 3.28590

Physical and chemical properties

Density: 1.254 g / cm ³

Boiling point: 572.1ºC at 760 mmHg

Refractive index: 1.624 ^[1]

Beiprost Beleoprost related drug label information

Beraprost indication

Chronic arterial occlusive diseases such as Raynaud's disease, Raynaud's syndrome, chronic cerebral infarction and other chronic arterial occlusive diseases.

Beiprost usage and dosage

Oral administration: The total daily amount is 120 g, and it is taken in 3 times.

Beleprost pharmacological action

This is the final product of arachidonic acid chain reaction, which has a strong anti-platelet aggregation effect and vasodilation effect. It is mainly produced by the metabolism of arachidonic acid in the blood vessel wall. Not only vascular endothelial cells, but also vascular smooth muscle cells can also produce PGI2. It has a strong vasodilatory effect. It is now known that PGI2 is reduced in blood vessels in the site of arteriosclerosis. It has been reported that FGI2 stabilization factor apolipo-poteint A-I decreases in patients with ischemic heart disease and in patients with acute myocardial infarction and unstable angina associated with coronary spasm.

PGI2 has an exoenolether structure. Because of its extremely unstable chemical properties, PGI2 is rapidly decomposed in a neutral solution and the body, so it is only used for diseases that can be dripped intravenously. This product replaces the exenol structure with phenol and chemically modifies the side chain to make it more active and stable. This product is a prostacyclin derivative that can be taken orally. It has strong vasodilation and anti-platelet agglutination.

Pharmacokinetics

After oral administration of this drug, patients with diabetic autonomic neuropathy take effect in 1 to 3 months, patients with intermittent claudication take effect in 1 week, and patients with pulmonary hypertension take effect in 15 to 30 minutes. After taking 100mg of the drug in healthy subjects, the average peak plasma concentration was 0.4ng / ml. The peak time of this drug is 1.4h, and its half-life is 1h, 15% of which is excreted in its original form and 70% is excreted as metabolites.

Dosage form and specifications

Tablet: 20 g.

Bereprost adverse reactions

Occasionally after taking the medicine, headache, nausea, diarrhea, lack of appetite, flushing of the face, palpitations, allergic reactions, elevated liver enzymes and other adverse reactions.

Beprostil considerations

Use with caution: (1) those with a history of allergies or adverse reactions to prostacyclin derivatives; (2) hypotension: hypotension tends to worsen after taking medication; (3) during pregnancy and lactation; (4) renal function or Liver insufficiency: due to the lack of relevant pharmacokinetic and clinical data. 2. A large amount of medication may cause bleeding or exacerbate bleeding tendency.