calan drug classification
Atrial fibrillation (AF) is a progressive disease. Previously, clinical and animal experimental studies in AF revealed a variety of myocyte remodeling processes including L-type Ca(2+) channel reduction and structural changes, which finally result in electrical remodeling and contractile dysfunction. There are indications that myocyte remodeling is mediated by Ca(2+) overload induced calpain activation. To study in more detail the mechanisms underlying myocyte remodeling and to develop strategies for drug-interference, we utilised a paced cell model for AF.
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A 31-year-old white woman was admitted with an acute exacerbation of migraine with hemiplegia. A transcranial Doppler showed an increased flow velocity through the middle cerebral artery consistent with a migrainous process. The patient was treated with verapamil 5 mg iv and the hemiplegia gradually resolved. A transcranial Doppler indicated that the flow velocity through the middle cerebral artery was decreased after verapamil administration, indicating reversal of the vasospasm.
The magnitude of symptom distress or relief associated with symptoms in 2 patient populations correlated strongly with a shift in quality of life. The assessment of distress associated with symptoms provides valuable additional information on drug therapy.
It is not known whether tepal senescence in Iris flowers is regulated by hormones. We applied hormones and hormone inhibitors to cut flowers and isolated tepals of Iris × hollandica cv. Blue Magic. Treatments with ethylene or ethylene antagonists indicated lack of ethylene involvement. Auxins or auxin inhibitors also did not change the time to senescence. Abscisic acid (ABA) hastened senescence, but an inhibitor of ABA synthesis (norflurazon) had no effect. Gibberellic acid (GA3 ) slightly delayed senescence in some experiments, but in other experiments it was without effect, and gibberellin inhibitors [ancymidol or 4-hydroxy-5-isopropyl-2-methylphenyltrimethyl ammonium chloride-1-piperidine carboxylate (AMO-1618)] were ineffective as well. Salicylic acid (SA) also had no effect. Ethylene, auxins, GA3 and SA affected flower opening, therefore did reach the flower cells. Jasmonates delayed senescence by about 2.0 days. Similarly, cytokinins delayed senescence by about 1.5-2.0 days. Antagonists of the phosphatidylinositol signal transduction pathway (lithium), calcium channels (niguldipine and verapamil), calmodulin action [fluphenazine, trifluoroperazine, phenoxybenzamide and N-(6-aminohexyl)-5-chloro-1-naphtalenesulfonamide hydrochloride (W-7)] or protein kinase activity [1-(5-isoquinolinesulfonyl)-2-methylpiperazine hydrochloride (H-7), N-[2-(methylamino)ethyl]-5-isoquinolinesulfonamide hydrochloride (H-8) and N-(2-aminoethyl)-5-isoquinolinesulfonamide dihydrochloride (H-9)] had no effect on senescence, indicating no role of a few common signal transduction pathways relating to hormone effects on senescence. The results indicate that tepal senescence in Iris cv. Blue Magic is not regulated by endogenous ethylene, auxin, gibberellins or SA. A role of ABA can at present not be excluded. The data suggest the hypothesis that cytokinins and jasmonates are among the natural regulators.
calan 120 mg
To evaluate the effects of Verapamil and Metoprolol on improving heart rate variability(HRV) in patients with coronary heart disease (CHD).
It is now clear that different pathophysiologic mechanisms have a profound influence on the extent of the functional impairment in intermittent claudication. In particular, metabolic derangements, including impaired oxygen delivery and/or extraction, reduced nitric oxide synthesis, reduced glucose oxidation, accumulation of toxic metabolites and reduction in carnitine availability are correlated with disease severity. Therefore, metabolic interventions aimed at counteracting these alterations may represent a valid therapeutic approach to the treatment of this condition. To date, verapamil and L-arginine efficacy has been proven in few patients; a large scale clinical trial, conversely, reports that propionyl-L-carnitine appears to be an effective and well tolerated drug for the treatment of intermittent claudication.
calan eeze review
Oyster solution at 7 500 mg/mL inhibited noradrenaline-induced contraction in isolated aortic rings. Cardiac electrophysiology results showed that neither concentration of oyster solution was able to significantly reduce action potential duration at all phases of repolarisation in left ventricular papillary muscles from healthy animals.
Osteopontin (OPN) is a multi-functional secreted glycoprotein that plays a crucial role in glucose metabolism and inflammatory process. Growing evidence suggests that there is a link between OPN and ovarian function. However, no such link has yet been found for OPN in polycystic ovary syndrome (PCOS). Our aim was to ascertain whether circulating OPN levels are altered in women with PCOS and to determine whether OPN levels differ between the follicular phase and mid-cycle of the menstrual cycle in eumenorrheic women.
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The decrease in phenylephrine-induced abrupt elevation in MAP (DeltaMAP(AE)) was significantly larger after verapamil than after SMF exposure. DeltaMAP(AE) inversely correlated with verapamil-induced significant increase in DeltaMPPG (r = 0.53, p < 0.000) and with SMF-induced significant increase in DeltaBRS (r = 0.47, p < 0.016).
calan 40 mg
A total of 9340 patients underwent randomization. The median follow-up was 3.8 years. The primary outcome occurred in significantly fewer patients in the liraglutide group (608 of 4668 patients [13.0%]) than in the placebo group (694 of 4672 [14.9%]) (hazard ratio, 0.87; 95% confidence interval [CI], 0.78 to 0.97; P<0.001 for noninferiority; P=0.01 for superiority). Fewer patients died from cardiovascular causes in the liraglutide group (219 patients [4.7%]) than in the placebo group (278 [6.0%]) (hazard ratio, 0.78; 95% CI, 0.66 to 0.93; P=0.007). The rate of death from any cause was lower in the liraglutide group (381 patients [8.2%]) than in the placebo group (447 [9.6%]) (hazard ratio, 0.85; 95% CI, 0.74 to 0.97; P=0.02). The rates of nonfatal myocardial infarction, nonfatal stroke, and hospitalization for heart failure were nonsignificantly lower in the liraglutide group than in the placebo group. The most common adverse events leading to the discontinuation of liraglutide were gastrointestinal events. The incidence of pancreatitis was nonsignificantly lower in the liraglutide group than in the placebo group.
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The human multidrug resistance P-glycoprotein (P-gp) pumps a wide variety of structurally diverse compounds out of the cell. It is an ATP-binding cassette transporter with two nucleotide-binding domains and two transmembrane (TM) domains. One class of compounds transported by P-gp is the rhodamine dyes. A P-gp deletion mutant (residues 1-379 plus 681-1025) with only the TM domains retained the ability to bind rhodamine. Therefore, to identify the residues involved in rhodamine binding, 252 mutants containing a cysteine in the predicted TM segments were generated and reacted with a thiol-reactive analog of rhodamine, methanethiosulfonate (MTS)-rhodamine. The activities of 28 mutants (in TMs 2-12) were inhibited by at least 50% after reaction with MTS-rhodamine. The activities of five mutants, I340C(TM6), A841C(TM9), L975C(TM12), V981C(TM12), and V982C(TM12), however, were significantly protected from inhibition by MTS-rhodamine by pretreatment with rhodamine B, indicating that residues in TMs 6, 9, and 12 contribute to the binding of rhodamine dyes. These results, together with those from previous labeling studies with other thiol-reactive compounds, dibromobimane, MTS-verapamil, and MTS-cross-linker substrates, indicate that common residues are involved in the binding of structurally different drug substrates and that P-gp has a common drug-binding site. The results support the "substrate-induced fit" hypothesis for drug binding.
We tested the hypothesis that the primary cilium of renal epithelia is mechanically sensitive and serves as a flow sensor in MDCK cells using differential interference contrast and fluorescence microscopy. Bending the cilium, either by suction with a micropipette or by increasing the flow rate of perfusate, causes intracellular calcium to substantially increase as indicated by the fluorescent indicator, Fluo-4. This calcium signal is initiated by Ca2+-influx through mechanically sensitive channels that probably reside in the cilium or its base. The influx is followed by calcium release from IP3-sensitive stores. The calcium signal then spreads as a wave from the perturbed cell to its neighbors by diffusion of a second messenger through gap junctions. This spreading of the calcium wave points to flow sensing as a coordinated event within the tissue, rather than an isolated phenomenon in a single cell. Measurement of the membrane potential difference by microelectrode during perfusate flow reveals a profound hyperpolarization during the period of elevated intracellular calcium. We conclude that the primary cilium in MDCK cells is mechanically sensitive and responds to flow by greatly increasing intracellular calcium.
Paclitaxel (PCT) is a cytotoxic agent with a broad antineoplastic activity. IV formulation of PCT causes hypersensitivity reactions in some patients and oral administration is an alternative to decrease the side effects. PCT is not orally available because of low solubility, lack of intestinal permeability, and efflux by pumps in intestinal wall. PCT solution in cremophor EL: ethanol (100 mg/kg) was administered orally to rats after pre-treatment by mefenamic acid, ibuprofen, verapamil, cyclosporine, and verapamil+ibuprofen in individual groups. Ibuprofen presented positive effect on intestinal permeation of PCT. C(max) and area under the serum concentration versus time curve (AUC) after pre-treatment by ibuprofen was decreased when the oral dose of PCT was decreased to 50 and 25 mg/kg, while dose-blood concentration relationship was nonlinear. Rise in oral bioavailability of PCT after pre-treatment by cyclosporine was lower than ibuprofen. It seems that by using ibuprofen in concomitant with potent P-gp inhibitors before PCT solution, oral delivery of PCT could be promising.
calan 80 mg
The therapeutic potential of berberine has been well documented in various neurological problems. However, the neurological mechanism of berberine remains untapped in the light of its P-glycoprotein (P-gp)-mediated gut efflux properties responsible for reduced bioavailability. Verapamil, a well known L-type calcium channel blocker, has additional inhibitory activity against P-gp efflux pump. Thus, there is a strong scientific rationale to explore the interaction of berberine with verapamil as a possible neuroprotective strategy.
Due to its high sensitivity, reproducibility and reliability, fura-2 is one of the most preferred tools to quantify Ca2+ levels. Recently, using fura-2/AM, some calcium channel blockers (CCBs) have been reported to have inhibitory effects on intracellular Ca2+ signaling even in nonexcitable cells that do not possess voltage-dependent Ca2+ channels (VDCC). Some CCBs are known to be photosensitive. Since photosensitive chemicals often have autofluorescent property, it is likely that CCBs with autofluorescence interfere with the fluorescent dye probes for Ca2+, which may cause misinterpretation of the results. The aim of this study was to clarify the characteristics of various CCBs on Ca2+ fluorescent probes and to identify proper fluorescent probes for each CCB to allow reliable Ca2+ measurement using endothelial cells (ECs), which possess no VDCC. Thapsigargin (TG, Ca2+-ATPase inhibitor on endoplasmic reticulum) increased fura-2 F340/F380 ratio from 0.75+/-0.06 to 4.28+/-0.32, suggesting the increase in cytosolic Ca2+ concentrations in ECs. Verapamil, nifedipine and nicardipine did not affect TG-induced increase in fura-2 F340/F380 ratio; however, amlodipine dose dependently inhibited the rise of fura-2 ratio by 24% at 100 nM, by 55% at 1 microM and by 82% at 10 microM, respectively, in ECs. In ex vivo experiments without cells, due to the autofluorescence of amlodipine excited by ultraviolet (UV light), amlodipine itself boosted the intensity of F380 much more than it did that of F340, which results in a decrease in F340/F380 ratio of fura-2 fluorescence. Rhod-2/AM, a fluorescent probe of which the excitation wavelength is out of the excitation spectrum of amlodipine, showed that amlodipine did not affect TG-induced intracellular Ca2+ increase in ECs. When the effect of amlodipine on intracellular Ca2+ concentration is assessed, fura-2 fluorospectrometry should not be used due to fluorescent interaction between amlodipine and fura-2, and using rhod-2 is strongly recommended.
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Although therapeutically beneficial in the treatment of certain diseases, L-type calcium channel antagonism can result in unwanted off-target pharmacology leading to adverse drug reactions and to the termination of the development of otherwise promising compounds. In the present study three marketed calcium channel inhibitors, nifedipine, verapamil and diltiazem were profiled in a series of in vitro and ex-vivo assays in an effort to determine the ability of these assays to discriminate, between dihydropyridine versus non-dihydropyridine-like compounds, and how well they can predict the cardiovascular effects observed in a conscious telemetered rat model.
calan 180 mg
Functional parameters of cardiac preload, including the RSVT, allow prediction of fluid responsiveness in an experimental model of acutely impaired cardiac function.
A stereospecific capillary zone electrophoresis (CZE) method was developed for the determination of verapamil (VER) and its main metabolite norverapamil (NOR) in human plasma. Optimal temperature, cyclodextrin selectors (CDs), pH of background electrolyte (BGE) and voltage were established to obtain complete separation of the chiral analytes and clopidogrel internal standard (I.S.) during one analytical run. Successful resolution of analytes was obtained in silica capillary filled with BGE consisting of heptakis 2,3,6-tri-O-methyl-beta-CD in phosphate buffer, pH 2.5 at 15 degrees C of capillary temperature. The calculated electrophoretic parameters of the analytes were as follows: apparent electrophoretic mobility, for VER enantiomers: micro(ap(+)-R) = 1.1 x 10(-4), micro(ap(-)s) = 1.06 x 10(-4) cm2/Vs and for NOR enantiomers: micro(ap(+)-R) = 1.09 x 10(-4), micro(ap(-)s) = 1.04 x 10(-4) cm2/Vs, resolution factors, R(s) = 5.4-6.6. Liquid extraction was applied for isolation of the analytes. The calibration curves ware linear in the range 0.25-10 microg/mL for VER and NOR enantiomer concentrations. The validation parameters were also established. The precision and accuracy of intra- and inter-day analysis were less than 15%. The lower limit of detection and limit of quantification for single enantiomers were 0.1 and 0.2 microg/mL, respectively. Recovery of the enantiomers from plasma was in the 91-103% range. To evaluate analytical applicability of the proposed method, plasma sample from patient suffering from arterial hypertension treated with 80 mg of commercial tablets was analyzed.
calan 240 mg
For assessment of the independent renoprotective effect of BP control and angiotensin-converting enzyme inhibitor (ACEi) therapy, the relationships of baseline BP, BP reduction, and follow-up BP with the incidence of persistent microalbuminuria were evaluated in 1204 hypertensive patients who had type 2 diabetes and normoalbuminuria and were included in the BErgamo Nephrologic Diabetic Complications Trial (BENEDICT) study and were randomly assigned to 3.6 yr of treatment with the ACEi trandolapril (2 mg/d), the nondihydropyridine calcium channel blocker (ndCCB) verapamil SR (240 mg/d), their fixed combination Veratran (trandolapril 2 mg/d plus verapamil SR 180 mg/d), or placebo, plus other antihypertensive medications targeted at systolic/diastolic BP <130/80 mmHg. Follow-up (from month 3 to study end) systolic, diastolic, mean, and pulse BP and their reductions versus baseline--but not baseline BP--independently predicted (P < 0.001) the risk for microalbuminuria. In patients with follow-up BP above medians, ACEi significantly reduced the risk for microalbuminuria to levels that were observed among patients with BP below medians, regardless of ACEi treatment. The same trend was observed among patients with BP reductions below medians. ndCCB therapy did not independently affect microalbuminuria. Patients who were on Veratran had lower BP and less frequently received diuretics, beta blockers, or dihydropyridine dCCB. In hypertensive, normoalbuminuric patients with type 2 diabetes, BP reduction and ACEi therapy both independently may prevent microalbuminuria. ACEi therapy is particularly effective when BP is poorly controlled, whereas ndCCB therapy is ineffective at any level of achieved BP. As compared with trandolapril, Veratran may help with achievement of target BP with less need for concomitant antihypertensive medications.
calan 5 mg
The effects of calcium channel blockers (CCBs) verapamil and diltiazem on the toxicity of rubratoxin B in HL60 cells were investigated. Treatment of rubratoxin B caused a considerable rate of blebbing, fragmentation and condensation of cells. The rate of this morphological change was much lower in the concomitant rubratoxin B and CCBs-treated cells than in the cells treated only with rubratoxin B. Cell viability was determined by measuring mitochondrial succinic dehydrogenase activity and the rate of cell proliferation. The results of these assays were of the same tendency as that of the morphological study. CCBs attenuated rubratoxin B's toxicity on cell viability because of their protective action. Rubratoxin B induced apoptosis in the presence of internucleosomal fragmentation. In contrast, concomitant rubratoxin B and CCBs treatment did not. Taken together, the above results indicated that CCBs impaired the toxicity including morphological change, cell viability and apoptosis caused by rubratoxin B.
calan drug classification
This study investigated the effect on the uterus of the aqueous fraction of the partitioned methanol crude extract of the leaves of Anthocleista djalonensis (AD) and the possible mechanism of AD activity. AD inhibited the concentration-response curves induced by oxytocin and CaCl2 on the rat uterus in vitro and significantly reduced the EC50 in a concentration-dependent manner (p < 0.05). A similar effect was observed with salbutamol and verapamil on the concentration-response curves obtained for oxytocin and CaCl2. The inhibitory effect of AD was not attenuated in the presence of propranolol. AD, salbutamol, and verapamil also produced a concentration-dependent relaxation on K+-induced sustained uterine contraction. In Ca2+-free medium, AD and salbutamol similarly inhibited oxytocin-induced contraction, but verapamil failed to produce this effect. The present results suggest that AD, being a mixture of phytochemicals, probably exerts inhibitory activity on in vitro uterine contractions of the nonpregnant, diethylstilboestrol-treated rat by multiple mechanisms that do not involve interaction with β-adrenergic receptors and do not solely depend on inhibition of calcium influx.
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To eliminate the noncardiac toxicities associated with Adriamycin (Pharmacia Upjohn, Kalamazoo, MI) and to avoid the need for surgical implantation of a coronary artery catheter, we proposed serial intracoronary infusions of Adriamycin (Pharmacia Upjohn) with a Judkins catheter to develop a nonsurgical but selective model of dilated cardiomyopathy in dogs.
We have attempted to determine whether muscarinic stimulation induces RhoA/ROCK-mediated Ca2+ sensitization of contractions in chicken gizzard smooth muscles. rhoA is a small GTP-binding protein, and ROCK is a rhoA-associated coiled coil-forming serine/threonine kinase. The relationship between the cytosolic Ca2+ level ([Ca2+]i) and muscle force in the presence of a high K+ concentration was not different from that in the presence of carbachol. Verapamil inhibited muscle force in proportion to the decrease in [Ca2+]i in both the muscle stimulated with high K+ and that stimulated with carbachol. In addition, Y-27632 (10 microM), a ROCKs inhibitor, had no effect on the contractions. In the alpha-toxin-permeabilized muscles, Ca2+ induced a greater contraction in the presence of guanosine 5'-O-(3-thiotriphosphapte) (GTP[gamma-S]), whereas carbachol with GTP was not effective. The GTP[gamma-S]-induced Ca2+ sensitization was completely inhibited by Clostridium botulinum exoenzyme C3. Western blot analysis revealed both rhoA and ROCKII in the muscle extract. In addition, reverse transcriptase polymerase chain reaction (RT-PCR) analysis revealed the expression of both ROCKI and ROCKII mRNAs. These results suggest that Ca2+ sensitization in the chicken gizzard is elicited via a rhoA/ROCKs pathway, and that this pathway may be responsible for the augmentation of contraction by GTP[gamma-S] in the permeabilized muscles. If such a pathway does exist, however, carbachol-induced contraction may not be coupled to it, which explains the absence of Ca2+ sensitization in the intact chicken gizzard stimulated by carbachol.