After a brief review of the pathophysiological properties of calcium channel blockers on the ischaemic heart muscle the author deals with the therapeutic effect of blockers on coronary spasms and at the same time on vasodilatation of arteries in the systemic circulation. Their effect is manifested also by the favourable action on the arteriosclerotic process proper, the clinically significant retardation of atherogenesis, stabilization of atherosclerotic plaques. The author pays special attention to the new calcium channel blocker-amlodipine which as to its pharmacokinetic properties is superior to all hitherto used types of blockers.

• MeSH
• blokátory kalciových kanálů terapeutické užití   MeSH
• ischemická choroba srdeční farmakoterapie   MeSH
• lidé MeSH
• Check Tag
• lidé MeSH
• Publikační typ
• anglický abstrakt MeSH
• časopisecké články MeSH
• Názvy látek
• blokátory kalciových kanálů MeSH

The interactions between Ca(2+)-channel blockers (verapamil and gallopamil) and synaptic plasma membranes (SPM) from bovine brain or human lymphocyte and platelet plasma membranes were studied. Changes in binding parameters of [3H]imipramine, [3H]desmethylimipramine and [3H]gallopamil were determined after addition of unlabelled verapamil or imipramine and after addition of phosphatidylserine (PS) (PS-stimulation). Specific binding of [3H]imipramine to SPM was decreased and [3H]desmethylimipramine binding was increased by 1 microM verapamil. [3H]gallopamil binds specifically to SPM as well as to platelet and lymphocyte membranes. [3H]gallopamil binding to SPM or lymphocyte plasma membranes was PS-stimulated in contrast to platelet plasma membranes without PS effect on binding. Imipramine inhibited both [3H]gallopamil binding and PS-stimulated [3H]gallopamil binding to SPM or lymphocyte plasma membranes. Mutual effects of tricyclic antidepressants and Ca(2+)-channel blockers on their binding sites require relatively high drug concentrations. Mechanism of Ca(2+)-channel blockers action in the treatment of depression may be connected rather with changes in signal transduction through serotonin and catecholamine receptor systems than with direct interaction of drugs with binding sites for tricyclic antidepressants.

• MeSH
• antidepresiva tricyklická metabolismus   MeSH
• blokátory kalciových kanálů farmakologie   MeSH
• buněčná membrána metabolismus   MeSH
• desipramin metabolismus   MeSH
• fosfatidylseriny farmakologie   MeSH
• galopamil farmakologie   MeSH
• imipramin metabolismus   MeSH
• lidé MeSH
• lymfocyty metabolismus   MeSH
• skot MeSH
• synaptické membrány metabolismus   MeSH
• techniky in vitro MeSH
• trombocyty metabolismus   MeSH
• verapamil farmakologie   MeSH
• zvířata MeSH
• Check Tag
• lidé MeSH
• skot MeSH
• zvířata MeSH
• Publikační typ
• anglický abstrakt MeSH
• časopisecké články MeSH
• Názvy látek
• antidepresiva tricyklická MeSH
• blokátory kalciových kanálů MeSH
• desipramin MeSH
• fosfatidylseriny MeSH
• galopamil MeSH
• imipramin MeSH
• verapamil MeSH

Combination of drugs from different classes of antihypertensives provides an additional antihypertensive effect thus minimising the probability of adverse effects related to the dose of antihypertensive. Combination therapy is indicated for the following groups of hypertensive patients: (a) all hypertensive patients whose systolic blood pressure exceeds the target systolic blood pressure value by > 20 mm Hg, or whose diastolic blood pressure exceeds the target diastolic blood pressure value by > 10 mm Hg; (b) in patients with diabetes mellitus (because the target values are < 130/80 mm Hg); (c) patients with target organ damage; (d) patients with a kidney or cardiovascular disease (patients with IHD, patients after a cerebrovascular accident); (e) patients with overall cardiovascular risk according the SCORE > or = 5%. The advantage of fixed combinations resides in the fact that they increase compliance with treatment by reducing the number of pills taken by the patients. A fixed combination of the ACE inhibitor perindopril and the calcium channel blocker amlodipine proves optimal as has been shown by the results of the ASCOT-BPLA study. The launch of the above combination on this market should therefore be welcome. The fixed combination of perindopril and amlodipine will be indicated for hypertensive patients with uncontrolled hypertension or cardiovascular risk factors. This fixed combination will also be ideal for patients with a higher risk of diabetes mellitus, i.e. patients with a higher fasting glycaemia, in patients with impaired glucose tolerance and in patients with the metabolic syndrome. We strongly believe that it will improve the control of hypertension in our hypertensive patients, and improve the cardioprotective and nephroprotective effect of hypertension therapy.

• MeSH
• amlodipin aplikace a dávkování   MeSH
• antihypertenziva aplikace a dávkování   MeSH
• blokátory kalciových kanálů aplikace a dávkování   MeSH
• fixní kombinace léků MeSH
• hypertenze farmakoterapie   MeSH
• inhibitory ACE aplikace a dávkování   MeSH
• kardiovaskulární nemoci prevence a kontrola   MeSH
• lidé MeSH
• perindopril aplikace a dávkování   MeSH
• Check Tag
• lidé MeSH
• Publikační typ
• anglický abstrakt MeSH
• časopisecké články MeSH
• přehledy MeSH
• Názvy látek
• amlodipin MeSH
• antihypertenziva MeSH
• blokátory kalciových kanálů MeSH
• fixní kombinace léků MeSH
• inhibitory ACE MeSH
• perindopril MeSH

The author presents a review of the chemically heterogeneous group of calcium antagonists, focused on their pharmacodynamic properties. He includes in the older generation of calcium antagonists drugs like verapamil, dihydropyridines (nifedipine) and dilthiazem (Diacordin, Blocalcin). The newer generation of dihydropyridines comprises substances with a higher vascular selectivity at a concentration of lower order. The latter include felodipine (Plendil), isradipine (Lomir) and nitrendipine (Baypress). The third generation includes drugs like amlodipine (Norvasc) and lacidipine. The slow onset of action of amlodipine is associated with a decline of undesirable side effects, such as flush, tachycardia, headache, oedema of the ankles. An advantage is also the prolonged effect when a single dose per day is administered.

• MeSH
• blokátory kalciových kanálů farmakokinetika   farmakologie   MeSH
• lidé MeSH
• Check Tag
• lidé MeSH
• Publikační typ
• anglický abstrakt MeSH
• časopisecké články MeSH
• přehledy MeSH
• Názvy látek
• blokátory kalciových kanálů MeSH

Besides condoms and vasectomy with their own limitations, no other reliable methods of contraception are available to men. Ion channels play a key role in maturation, capacitation and acrosome reaction of sperms. Blockade of calcium channels with pharmacological inhibitors or compounds isolated from plant extracts might be suggested as one of promising mechanisms of future male contraceptives.

• MeSH
• antikoncepce metody   MeSH
• blokátory kalciových kanálů * MeSH
• lidé MeSH
• rostlinné extrakty MeSH
• Check Tag
• lidé MeSH
• mužské pohlaví MeSH
• Publikační typ
• časopisecké články MeSH
• Názvy látek
• blokátory kalciových kanálů * MeSH
• rostlinné extrakty MeSH

The effect of the blockers of calcium channels on the development of myocardial ischaemia in rats with an occlusion of the coronary artery was examined. An occlusion of the coronary artery was carried out in rats anaesthetized with pentobarbital by tightening the ends of the ligature freely placed under the left coronary artery - ramus interventricularis seven days prior to ligation. The ischaemia-induced changes in the R-wave and ST-segment were recorded using ECG. The occlusion of the coronary artery produced arrhythmias, a significant elevation of the ST-segment and a slight increase in the heart rate. The blockers of calcium channels with different pharmacological properties - verapamil, nifedipine and diltiazem influenced the ischaemia-induced changes with different intensity. Nifedipine (0.02 mg.kg-1, i.v., 30 min prior to occlusion), verapamil (0.2 mg.kg-1, i.v., 10 mins prior to ischaemia), and diltiazem (0.3 mg.kg-1, i.v., 10 mins prior to ischemia) significantly reduced the increased elevation of the ST-segment. The highest effect on the above-mentioned model was shown by verapamil.

• MeSH
• blokátory kalciových kanálů farmakologie   MeSH
• elektrokardiografie účinky léků   MeSH
• infarkt myokardu patofyziologie   MeSH
• krysa rodu Rattus MeSH
• potkani Wistar MeSH
• zvířata MeSH
• Check Tag
• krysa rodu Rattus MeSH
• mužské pohlaví MeSH
• zvířata MeSH
• Publikační typ
• anglický abstrakt MeSH
• časopisecké články MeSH
• Názvy látek
• blokátory kalciových kanálů MeSH

• MeSH
• blokátory kalciových kanálů terapeutické užití   MeSH
• dysmenorea farmakoterapie   patofyziologie   MeSH
• leukotrien B4 fyziologie   MeSH
• lidé MeSH
• Check Tag
• lidé MeSH
• ženské pohlaví MeSH
• Publikační typ
• časopisecké články MeSH
• Názvy látek
• blokátory kalciových kanálů MeSH
• leukotrien B4 MeSH

Target blood pressure levels are not being achieved with the current hypertension treatment. Monotherapy that normalizes BP in about 20% of patients does not provide sufficient control to reach this goal and thus combination therapy is required. Results from recent clinical studies showed that a combination of an angiotenzin-converting enzyme inhibitor (ACEi) with a calcium channel blocker (CCB) provide better results and reduced incidence of cardiovascular events than a combination of a diuretic with an ACE inhibitor. Combination therapy based on rennin-angiotenzin system blockade: ACEi with a CCB, ACEi with a diuretic or angiotenzin receptor blocker (AT1) with a diuretic as a first-line treatment of the stage 2 hypertension might lead to significantly better control of blood pressure than monotherapy.

• MeSH
• antihypertenziva terapeutické užití   MeSH
• blokátory kalciových kanálů aplikace a dávkování   MeSH
• hypertenze farmakoterapie   patofyziologie   MeSH
• inhibitory ACE aplikace a dávkování   MeSH
• kombinovaná farmakoterapie MeSH
• lidé MeSH
• renin-angiotensin systém účinky léků   MeSH
• Check Tag
• lidé MeSH
• Publikační typ
• anglický abstrakt MeSH
• časopisecké články MeSH
• přehledy MeSH
• Názvy látek
• antihypertenziva MeSH
• blokátory kalciových kanálů MeSH
• inhibitory ACE MeSH

Calcium channel blockers represent a pharmacologically non homogenic group. Verapamil and diltiazem have myocardial component of their effect, which acts against activated sympathicus. Short acting dihydropyridines (nifedipin) appear to be harmful by patients after myocardial infarction which is caused by the reflex sympathetic response to the predominant vasodilation. In the treatment of cardiovascular disease (e.g. hypertension, coronary vascular disease) are short acting dihydropyridines not recommended. Dihydropyridines of the new generation (amlodipin, felodipin, isradipin, lacidipin, nicardipin, nimodipin, nisoldipin, nitrendipin) induce less tachycardia due to their favorable kinetic features. If the slow movement in blood or at the receptor site is not a result of molecule features there is necessary to use retarded preparations of active substance. Nevertheless, commonly used retarded preparations fulfil this requirement only incompletely. The desirable quality is provided by modern form of retardation. (e.g. GITS) only.

• MeSH
• blokátory kalciových kanálů škodlivé účinky   terapeutické užití   MeSH
• hypertenze farmakoterapie   MeSH
• infarkt myokardu prevence a kontrola   MeSH
• koronární nemoc farmakoterapie   MeSH
• lidé MeSH
• Check Tag
• lidé MeSH
• Publikační typ
• anglický abstrakt MeSH
• časopisecké články MeSH
• Názvy látek
• blokátory kalciových kanálů MeSH

Angiotensin receptor antagonists (AT(1)-blockers) are considered as one of the major classes of antihypertensive drugs suitable for monotherapy as well as for combination treatment. AT(1)-blockers have comparable antihypertensive efficacy with other major classes of antihypertensive drugs. AT(1)-blockers are considered by current guidelines of Czech society of hypertension altogether with ACE-inhibitors and calcium channel blockers as universal antihypertensive drug class. AT(1)-blockers has the lowest profile of side-effects among all antihypertensive drug classes and thus very high persistence to therapy. Mechanisms of antihypertensive effects of AT(1)-blockers are discussed altogether with the results of large clinical trials and indications in the treatment of hypertension.

• MeSH
• antagonisté receptorů pro angiotenzin terapeutické užití   MeSH
• antihypertenziva terapeutické užití   MeSH
• blokátory kalciových kanálů terapeutické užití   MeSH
• hypertenze farmakoterapie   MeSH
• inhibitory ACE terapeutické užití   MeSH
• kombinovaná farmakoterapie MeSH
• lidé MeSH
• Check Tag
• lidé MeSH
• Publikační typ
• časopisecké články MeSH
• přehledy MeSH
• Názvy látek
• antagonisté receptorů pro angiotenzin MeSH
• antihypertenziva MeSH
• blokátory kalciových kanálů MeSH
• inhibitory ACE MeSH