Gene/Protein Disease Symptom Drug Enzyme Compound
Pivot Concepts:   Target Concepts:
Query: UMLS:C0018681 (headache)
 56,091 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Beraprost sodium (BPS) is an orally stable analogue of prostacyclin that inhibits adenylate-cyclase-dependent platelet aggregation and is proposed for treatment of chronic arterial occlusion. To determine the duration and intensity of platelet antiaggregation with BPS, 12 healthy, nonsmoking, male white volunteers participated in a double-blind, dose-escalating design with randomized placebo, placebo-controlled, cross-over study. After overnight fasting, single (20, 40, 60 micrograms and placebo) and repeated [20, 40, 60 micrograms and placebo) and repeated [20, 40, 60 micrograms and placebo three times daily (t.i.d.) for 3 days] oral doses of BPS were administered. Mean percentage of inhibition of ADP-induced aggregation normalized to placebo was measured for 8 h after drug administration and related to plasma concentrations (Cp) of the active enantiomer (APS 314d). BPS 40 and 60 micrograms decreased platelet aggregation 1 h after single doses, and 0.5 h and 1 h after repeated doses. BPS 20 micrograms had no significant effect. APS 314d pharmacokinetics was linear, and its terminal half-life (t 1/2) ranged from 0.50 +/- 0.21 to 0.91 +/- 0.27 h (mean +/- SD) independently of BPS dose. Antiaggregating effects were poorly related to Cp of APS 314d (r2 < or = 0.2). Some subjects complained of moderate postdrug absorption headaches (7 of 12 after single and 8 of 12 after repeated doses) and flushes (6 of 12 and 7 of 12, respectively). These data indicate that orally active prostacyclin BPS (40 or 60 micrograms) exerts its maximal antiaggregating effects between 0.5 and 1 h.
 ...
PMID:Pharmacokinetics and platelet antiaggregating effects of beraprost, an oral stable prostacyclin analogue, in healthy volunteers. 750 23

The clinical usefulness of prostaglandin derivatives was reviewed for the treatment of peripheral vascular diseases such as arteriosclerosis obliterans, Buerger's disease, Raynaud's disease, and collagen disease etc. PGE1 was initially used for this purpose, however, it had to be infused intra-arterially or intravenously for hours. PGE1 incorporated in lipid microsphere (Lipo PGE1) was made for one-shot use and the targeting drug delivery because the lipid microsphere is easily taken up by some inflammatory cells. Lipo PGE1 was revealed to be effective to improvement of considerably large ischemic ulcer and pain. Beraprost sodium (PGI2 derivative) was produced for oral use, and has been widely used. The effectiveness was similar to Lipo PGE1, but the complications such as hypotension, headache, and numbness were more common in PGI2.
 ...
PMID:[Treatment of the peripheral vascular diseases with prostaglandin]. 793 9

The antiaggregation and hemodynamic effects of the new prostacyclin analogue beraprost sodium were investigated in a randomized, placebo-controlled, double-blind clinical trial of Latin-square design. Twelve healthy Caucasian males randomly received 8-day oral treatments of 20, 40, and 60 micrograms of beraprost sodium and a placebo. One-week washout periods followed each treatment. Pharmacokinetic and pharmacodynamic measurements were performed on days 1 and 8 for each period of treatment. All three doses of beraprost sodium significantly inhibited platelet aggregation on day 8 (compared with placebo) during the 1st h after drug intake. Incubation of the 60-micrograms beraprost sodium samples with ADP (2, 5, and 10 microM) and collagen (1.25 micrograms/mL) decreased platelet aggregation by 10, 19, 16, and 6 +/- 4% (mean +/- SE), respectively, compared with placebo. No significant hemodynamic effects on blood pressure, heart rate, and digital pulse were observed. The 60-micrograms dose of beraprost sodium did significantly decrease the IRZ index (which may reflect the left ventricular pre-ejection period) on days 1 and 8. Some subjects experienced headache and facial flushing, effects that were dose dependent and reversible. Beraprost sodium at 20- to 60-micrograms doses exerts platelet antiaggregation (day 8 of therapy) and slight hemodynamic (days 1 and 8 of treatment) effects in Caucasian males. Beraprost sodium hemodynamic effects and potential benefits in patients with cardiovascular disease should be explored further.
 ...
PMID:Platelet-aggregation inhibition and hemodynamic effects of beraprost sodium, a new oral prostacyclin derivative: a study in healthy male subjects. 896 Mar 77

The effects of the prostaglandin I2 derivative beraprost sodium (Dorner) on ankle pressure index (AP; ankle joint-to-upper extremity systolic pressure ratio), subjective symptoms, and intermittent claudication were investigated in diabetic patients with arteriosclerosis obliterans (ASO). Forty patients (25 men and 15 women), mean age 63.9 years, were enrolled in this study. ASO was grade I in 30 patients, grade II in seven, grade III in one, and grade IV in two according to the Fontaine classification. They were administered six tablets (20 microg/tablet) of beraprost sodium daily for 6 months. At 3 and 6 months, API had significantly increased and symptoms such as coldness, numbness, and lack of feeling in the lower extremities were significantly improved. Ten evaluable patients increased ambulatory distance by approximately threefold, suggesting an improvement in intermittent claudication. Adverse reactions were experienced by five (12.5%) of the 40 patients (one case each of headache, dull headache, pain in the posterior region of the neck, heartburn, stomach discomfort, and anemia), but all were mild and resolved without treatment. Beraprost sodium was shown to improve API and symptoms in the lower extremities in diabetic patients with ASO, suggesting that it is useful in treating peripheral circulatory disorders in such patients.
 ...
PMID:Effects of beraprost sodium (Dorner) in patients with diabetes mellitus complicated by chronic arterial obstruction. 1186 12

Beraprost sodium, an orally active prostaglandin I2 analog with vasodilatory, cytoprotective, antiplatelet, antithrombotic, and anti-inflammatory effects, 120 microg daily for 8 weeks, decreased plasma D-dimer, a marker of intravascular coagulation, and von Willebrand factor, a marker for endothelial injury, in 100 chronic peritoneal dialysis patients. Total cholesterol, triglycerides, high-density lipoprotein, apolipoprotein A1, apolipoprotein B, albumin, prealbumin, fibrinogen, troponin-T, and high-sensitivity C-reactive protein levels were not changed. Three patients complained of headache and 1 patient experienced facial flushing; however, no serious adverse effects were observed. These results suggest that beraprost sodium is effective in partially reversing the thrombogenic coagulation profile and endothelial injury in chronic peritoneal dialysis patients.
 ...
PMID:Effects of beraprost sodium, an oral prostaglandin i2 analog, on hemostatic factors and inflammation in chronic peritoneal dialysis patients. 1929 55