Haemodynamic effects of lercanidipine in anaesthetized open-chest dogs. 1996

G Sironi, and E Montagna, and L Greto, and A Leonardi, and R Testa
Pharmaceutical R&D Division, Recordati S.p.A., Milan, Italy.

In this study, the haemodynamic effects of lercanidipine (CAS 132866-11-6, Rec 15/2375) in anaesthetized open-chest dogs were investigated in comparison with nitrendipine. Intravenously administered lercanidipine induced a dose-related, long-lasting reduction in systemic and coronary vascular resistances, with concomitant decrease in arterial blood pressure and increase in coronary blood flow. The hypotensive ED25 was 6.1 micrograms/kg and 4.2 micrograms/kg (decrease of mean blood pressure and of total peripheral resistances, respectively) and the ED50 on coronary vasodilation, 4.8 micrograms/kg 7.8 micrograms/kg (increase of coronary blood flow and decrease in coronary vascular resistances, respectively). The time-course of the haemodynamic effects was investigated after administration of 5 micrograms/kg. A slow onset of haemodynamic vasodilation and long-lasting activity were observed, since peak effects on mean blood pressure and coronary blood flow occurred at 20 and 30 min after the administration, respectively, and the effects on systemic and coronary resistances were still significant at 30 and 150 min after administration, respectively. A reflex, non-dose-dependent increase in heart rate was observed after the administration of 10 and 30 micrograms/kg, which was absent with the 5 micrograms/kg dose. As far as cardiac contractility was concerned, the contractile index dP/dtmax and dP/dt/P were analyzed. In the dose-response study, dP/dtmax was practically not affected. In the time-course study, dP/dtmax was not modified after administration of 5 micrograms/kg, and dP/dt/P showed a slight but long-lasting increase. Haemodynamic investigation confirmed in vivo the high vascular selectivity of lercanidipine and a lack of sympathetic reflex activation at vasodilating doses.

UI MeSH Term Description Entries
D007275 Injections, Intravenous Injections made into a vein for therapeutic or experimental purposes. Intravenous Injections,Injection, Intravenous,Intravenous Injection
D008297 Male Males
D009568 Nitrendipine A calcium channel blocker with marked vasodilator action. It is an effective antihypertensive agent and differs from other calcium channel blockers in that it does not reduce glomerular filtration rate and is mildly natriuretic, rather than sodium retentive. Balminil,Bay e 5009,Bayotensin,Baypresol,Baypress,Gericin,Jutapress,Nidrel,Niprina,Nitre AbZ,Nitre-Puren,Nitregamma,Nitren 1A Pharma,Nitren Lich,Nitren acis,Nitrend KSK,Nitrendepat,Nitrendi Biochemie,Nitrendidoc,Nitrendimerck,Nitrendipin AL,Nitrendipin Apogepha,Nitrendipin Atid,Nitrendipin Basics,Nitrendipin Heumann,Nitrendipin Jenapharm,Nitrendipin Lindo,Nitrendipin Stada,Nitrendipin beta,Nitrendipin-ratiopharm,Nitrendipino Bayvit,Nitrendipino Ratiopharm,Nitrensal,Nitrepress,Tensogradal,Trendinol,Vastensium,nitrendipin von ct,nitrendipin-corax,Nitre Puren,NitrePuren,Nitrendipin ratiopharm,Nitrendipinratiopharm,nitrendipin corax,nitrendipincorax
D002121 Calcium Channel Blockers A class of drugs that act by selective inhibition of calcium influx through cellular membranes. Calcium Antagonists, Exogenous,Calcium Blockaders, Exogenous,Calcium Channel Antagonist,Calcium Channel Blocker,Calcium Channel Blocking Drug,Calcium Inhibitors, Exogenous,Channel Blockers, Calcium,Exogenous Calcium Blockader,Exogenous Calcium Inhibitor,Calcium Channel Antagonists,Calcium Channel Blocking Drugs,Exogenous Calcium Antagonists,Exogenous Calcium Blockaders,Exogenous Calcium Inhibitors,Antagonist, Calcium Channel,Antagonists, Calcium Channel,Antagonists, Exogenous Calcium,Blockader, Exogenous Calcium,Blocker, Calcium Channel,Blockers, Calcium Channel,Calcium Blockader, Exogenous,Calcium Inhibitor, Exogenous,Channel Antagonist, Calcium,Channel Blocker, Calcium,Inhibitor, Exogenous Calcium
D004095 Dihydropyridines Pyridine moieties which are partially saturated by the addition of two hydrogen atoms in any position.
D004285 Dogs The domestic dog, Canis familiaris, comprising about 400 breeds, of the carnivore family CANIDAE. They are worldwide in distribution and live in association with people. (Walker's Mammals of the World, 5th ed, p1065) Canis familiaris,Dog
D004305 Dose-Response Relationship, Drug The relationship between the dose of an administered drug and the response of the organism to the drug. Dose Response Relationship, Drug,Dose-Response Relationships, Drug,Drug Dose-Response Relationship,Drug Dose-Response Relationships,Relationship, Drug Dose-Response,Relationships, Drug Dose-Response
D006439 Hemodynamics The movement and the forces involved in the movement of the blood through the CARDIOVASCULAR SYSTEM. Hemodynamic
D000758 Anesthesia A state characterized by loss of feeling or sensation. This depression of nerve function is usually the result of pharmacologic action and is induced to allow performance of surgery or other painful procedures.
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia

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