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Article: Cicaprost, an orally active prostacyclin analogue: Its effects on platelet aggregation and skin blood flow in normal volunteers

TitleCicaprost, an orally active prostacyclin analogue: Its effects on platelet aggregation and skin blood flow in normal volunteers
Authors
Issue Date1993
PublisherBlackwell Publishing Ltd. The Journal's web site is located at http://www.blackwellpublishing.com/journals/BJCP
Citation
British Journal Of Clinical Pharmacology, 1993, v. 35 n. 6, p. 643-647 How to Cite?
Abstract1. Prostacyclin (PGI2) and its analogues may be useful in peripheral vascular disease. However, most have to be given intravenously due to their metabolic instability. 2. We have investigated the pharmacological effects of cicaprost, a synthetic PGI2 analogue which is metabolically stable and bioavailable after oral administration, in eight healthy male volunteers. 3. This was a double-blind, placebo-controlled, cross-over study. The volunteers were given either placebo, 5 μg, 7.5 μg or 10 μg cicaprost (at 09.00 h, 14.00 h, 19.00 h and again at 09.00 h the following day) on four separate occasions each 14 days apart. 4. Platelet aggregation induced by collagen and ADP in platelet rich plasma (PRP) and whole blood were measured prior to and 1 h after the trial medication. Laser Doppler flowmetry measured skin blood flow on the face before and after medication. 5. There was a statistically significant dose relationship in the inhibition of platelet aggregation induced by 2 μM ADP and 0.4 μg ml-1 collagen in PRP and 2 μM ADP and 0.6 μg ml-1 collagen in whole blood by cicaprost (P = 0.008, P = 0.34, P = 0.011 and P = 0.036, respectively). The threshold dose was 7.5 μg. Attenuation of anti-platelet effects was seen with the 14.00 h and 19.00 h doses. This may be due to a decrease in absorption after meals or to the development of tachyphylaxis. 6. Similar dose dependent effects of cicaprost on skin blood flow were also found (P = 0.01 and P = 0.006 for maximum output signal and red blood cell flux, respectively). The threshold dose was 7.5 μg. 7. In conclusion, cicaprost has significant anti-platelet and vasodilatory effects when given in doses of 7.5 μg and 10 μg three times a day in healthy male volunteers.
Persistent Identifierhttp://hdl.handle.net/10722/161983
ISSN
2015 Impact Factor: 3.83
2015 SCImago Journal Rankings: 1.486
ISI Accession Number ID

 

DC FieldValueLanguage
dc.contributor.authorBelch, JJFen_US
dc.contributor.authorMclaren, Men_US
dc.contributor.authorLau, CSen_US
dc.contributor.authorMackay, IRen_US
dc.contributor.authorBancroft, Aen_US
dc.contributor.authorMcewen, Jen_US
dc.contributor.authorThompson, JMen_US
dc.date.accessioned2012-09-05T05:16:27Z-
dc.date.available2012-09-05T05:16:27Z-
dc.date.issued1993en_US
dc.identifier.citationBritish Journal Of Clinical Pharmacology, 1993, v. 35 n. 6, p. 643-647en_US
dc.identifier.issn0306-5251en_US
dc.identifier.urihttp://hdl.handle.net/10722/161983-
dc.description.abstract1. Prostacyclin (PGI2) and its analogues may be useful in peripheral vascular disease. However, most have to be given intravenously due to their metabolic instability. 2. We have investigated the pharmacological effects of cicaprost, a synthetic PGI2 analogue which is metabolically stable and bioavailable after oral administration, in eight healthy male volunteers. 3. This was a double-blind, placebo-controlled, cross-over study. The volunteers were given either placebo, 5 μg, 7.5 μg or 10 μg cicaprost (at 09.00 h, 14.00 h, 19.00 h and again at 09.00 h the following day) on four separate occasions each 14 days apart. 4. Platelet aggregation induced by collagen and ADP in platelet rich plasma (PRP) and whole blood were measured prior to and 1 h after the trial medication. Laser Doppler flowmetry measured skin blood flow on the face before and after medication. 5. There was a statistically significant dose relationship in the inhibition of platelet aggregation induced by 2 μM ADP and 0.4 μg ml-1 collagen in PRP and 2 μM ADP and 0.6 μg ml-1 collagen in whole blood by cicaprost (P = 0.008, P = 0.34, P = 0.011 and P = 0.036, respectively). The threshold dose was 7.5 μg. Attenuation of anti-platelet effects was seen with the 14.00 h and 19.00 h doses. This may be due to a decrease in absorption after meals or to the development of tachyphylaxis. 6. Similar dose dependent effects of cicaprost on skin blood flow were also found (P = 0.01 and P = 0.006 for maximum output signal and red blood cell flux, respectively). The threshold dose was 7.5 μg. 7. In conclusion, cicaprost has significant anti-platelet and vasodilatory effects when given in doses of 7.5 μg and 10 μg three times a day in healthy male volunteers.en_US
dc.languageengen_US
dc.publisherBlackwell Publishing Ltd. The Journal's web site is located at http://www.blackwellpublishing.com/journals/BJCPen_US
dc.relation.ispartofBritish Journal of Clinical Pharmacologyen_US
dc.subject.meshAdulten_US
dc.subject.meshBlood Platelets - Drug Effectsen_US
dc.subject.meshBlood Pressure - Drug Effectsen_US
dc.subject.meshDouble-Blind Methoden_US
dc.subject.meshEpoprostenol - Adverse Effects - Analogs & Derivatives - Pharmacologyen_US
dc.subject.meshFemaleen_US
dc.subject.meshHeart Rate - Drug Effectsen_US
dc.subject.meshHumansen_US
dc.subject.meshLaser-Doppler Flowmetryen_US
dc.subject.meshMaleen_US
dc.subject.meshPlatelet Aggregation - Drug Effectsen_US
dc.subject.meshPlatelet Aggregation Inhibitors - Pharmacologyen_US
dc.subject.meshRegional Blood Flow - Drug Effectsen_US
dc.subject.meshSkin - Blood Supplyen_US
dc.subject.meshVasodilator Agents - Pharmacologyen_US
dc.titleCicaprost, an orally active prostacyclin analogue: Its effects on platelet aggregation and skin blood flow in normal volunteersen_US
dc.typeArticleen_US
dc.identifier.emailLau, CS:cslau@hku.hken_US
dc.identifier.authorityLau, CS=rp01348en_US
dc.description.naturelink_to_subscribed_fulltexten_US
dc.identifier.doi10.1111/j.1365-2125.1993.tb04195.x-
dc.identifier.pmid8329292-
dc.identifier.scopuseid_2-s2.0-0027324953en_US
dc.identifier.volume35en_US
dc.identifier.issue6en_US
dc.identifier.spage643en_US
dc.identifier.epage647en_US
dc.identifier.isiWOS:A1993LG27200015-
dc.publisher.placeUnited Kingdomen_US
dc.identifier.scopusauthoridBelch, JJF=7101752870en_US
dc.identifier.scopusauthoridMcLaren, M=7005471705en_US
dc.identifier.scopusauthoridLau, CS=14035682100en_US
dc.identifier.scopusauthoridMackay, IR=7202234474en_US
dc.identifier.scopusauthoridBancroft, A=7004599092en_US
dc.identifier.scopusauthoridMcEwen, J=7102809775en_US
dc.identifier.scopusauthoridThompson, JM=7405817802en_US

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