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Journal articles on the topic 'Calcium Channel Blockers – pharmacokinetics'

Author: Grafiati

Published: 4 June 2021

Last updated: 9 February 2022

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1

Hunt, Bernard A., Michael B. Bottorff, Vanessa L. Herring, Timothy H. Self, and Richard L. Lalonde. "Effects of calcium channel blockers on the pharmacokinetics of propranolol stereoisomers." Clinical Pharmacology and Therapeutics 47, no. 5 (1990): 584–91. http://dx.doi.org/10.1038/clpt.1990.79.

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2

ENOMOTO, Nobuo, Mitsuhiro YOKOTA, Iwao SOTOBATA, Junki GOTO, Kazuya ANDO, and Itsuro SOBUE. "Effects of calcium channel blockers on the pharmacokinetics of oral .BETA.-methyldigoxin." Nihon Naika Gakkai Zasshi 77, no. 6 (1988): 781–87. http://dx.doi.org/10.2169/naika.77.781.

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3

Cachat, Francois, and Alda Tufro. "Phenytoin/Isradipine Interaction Causing Severe Neurologic Toxicity." Annals of Pharmacotherapy 36, no. 9 (2002): 1399–402. http://dx.doi.org/10.1345/aph.1c012.

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OBJECTIVE: To report a young man on phenytoin who developed acute neurologic symptoms after isradipine was introduced to his treatment regimen and discuss the possible causes of this drug interaction. CASE SUMMARY: A 21-year-old white man, with propionic acidemia and seizures treated with phenytoin and carbamazepine, was started on isradipine for essential hypertension. Soon thereafter, he developed acute and severe lethargy, ataxia, dysarthria, and weakness that resolved once isradipine was withheld. Phenytoin concentrations were within normal limits or elevated, despite sequential reductions

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4

Avdeeva, O. I., M. N. Makarova, I. E. Makarenko, P. V. Burenkov, M. G. Shubina, and V. A. Kashkin. "TTOXICOLOGICAL EVALUATION OF COMBINATION OF AMLODIPINE CALCIUM CHANNELS BLOCKER WITH ANGIOTENSIN RECEPTOR BLOCKERS." Toxicological Review, no. 1 (February 28, 2016): 13–17. http://dx.doi.org/10.36946/0869-7922-2016-1-13-17.

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The article summarizes experimental data on toxicological interactions of blocker of amplodipine slow calcium channels with angiotensin II (AT1 subtype) receptors blockers (valsartan and losartan). Toxicity studies were performed in outbred rats after a single intragastric administration in doses permitting to estimate lethal doses for the objects under investigation (amlodipine, valsartan, losartan, amlodipine+ losartan 1:10, amlodipine+ losartan 1:20, amlodipine + valsartan 1:16, amlodipine + valsartan 1:32). Based on the research outcome, the possibility of different types of toxicological

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5

GLESBY, M., J. ABERG, M. KENDALL, et al. "Pharmacokinetic interactions between indinavir plus ritonavir and calcium channel blockers." Clinical Pharmacology & Therapeutics 78, no. 2 (2005): 143–53. http://dx.doi.org/10.1016/j.clpt.2005.04.005.

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6

Azuma, Junichi, Isamu Yamamoto, Takahiro Watase, et al. "Effects of grapefruit juice on the pharmacokinetics of the calcium channel blockers nifedipine and nisoldipine." Current Therapeutic Research 59, no. 9 (1998): 619–34. http://dx.doi.org/10.1016/s0011-393x(98)85060-1.

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7

Deslandes, A., F. Camus, C. Lacroix, C. Carbon, and R. Farinotti. "Effects of nifedipine and diltiazem on pharmacokinetics of cefpodoxime following its oral administration." Antimicrobial Agents and Chemotherapy 40, no. 12 (1996): 2879–81. http://dx.doi.org/10.1128/aac.40.12.2879.

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We compared the effects of nifedipine and diltiazem on the uptake of cefpodoxime proxetil (CP). The study was aimed at establishing the impact of increased mesenteric blood flow due to calcium channel blockers on passive transport. Twelve volunteers were given CP (200 mg) orally in a crossover design. The absorption, disposition, and elimination parameters of cefpodoxime were compared among the following three treatment groups: CP alone, CP following oral administration of diltiazem (60 mg), or CP following oral administration of nifedipine (20 mg). No statistically significant difference in p

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8

Sica, Domenic A., and Todd W. B. Gehr. "Calcium-channel blockers and end-stage renal disease: pharmacokinetic and pharmacodynamic considerations." Current Opinion in Nephrology and Hypertension 12, no. 2 (2003): 123–31. http://dx.doi.org/10.1097/00041552-200303000-00001.

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9

Sica, Domenic A. "Calcium Channel Blocker Class Heterogeneity: Select Aspects of Pharmacokinetics and Pharmacodynamics." Journal of Clinical Hypertension 7 (April 2005): 21–26. http://dx.doi.org/10.1111/j.1524-6175.2006.04482.x.

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10

Hanafy, S., N. J. Dagenais, W. F. Dryden, and F. Jamali. "Effects of angiotensin II blockade on inflammation-induced alterations of pharmacokinetics and pharmacodynamics of calcium channel blockers." British Journal of Pharmacology 153, no. 1 (2008): 90–99. http://dx.doi.org/10.1038/sj.bjp.0707538.

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11

Maezawa, Izumi, David Paul Jenkins, Benjamin E. Jin, and Heike Wulff. "Microglial KCa3.1 Channels as a Potential Therapeutic Target for Alzheimer’s Disease." International Journal of Alzheimer's Disease 2012 (2012): 1–8. http://dx.doi.org/10.1155/2012/868972.

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There exists an urgent need for new target discovery to treat Alzheimer’s disease (AD); however, recent clinical trials based on anti-Aβand anti-inflammatory strategies have yielded disappointing results. To expedite new drug discovery, we propose reposition targets which have been previously pursued by both industry and academia for indications other than AD. One such target is the calcium-activated potassium channel KCa3.1 (KCNN4), which in the brain is primarily expressed in microglia and is significantly upregulated when microglia are activated. We here review the existing evidence support

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12

Kim, Minsoo, Heebin Son, Keumhan Noh, Eunyoung Kim, Beom Shin, and Wonku Kang. "Effects of Verapamil and Diltiazem on the Pharmacokinetics and Pharmacodynamics of Rivaroxaban." Pharmaceutics 11, no. 3 (2019): 133. http://dx.doi.org/10.3390/pharmaceutics11030133.

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Concomitant use of rivaroxaban with non-dihydropyridine calcium channel blockers (non-DHPs) might lead to an increase of systemic rivaroxaban exposure and anticoagulant effects in relation to the inhibition of metabolic enzymes and/or transporters by non-DHPs. This study was designed to evaluate the effects of verapamil and diltiazem on the pharmacokinetics and the prolongation of prothrombin time of rivaroxaban in rats. The data were analyzed using a pharmacokinetic/pharmacodynamics (PK/PD) modeling approach to quantify the influence of verapamil. Verapamil increased the systemic exposure of

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13

Sketris, Ingrida S., Michelle E. Methot, David Nicol, Philip Belitsky, and Margot G. Knox. "Effect of Calcium-Channel Blockers on Cyclosporine Clearance and Use in Renal Transplant Patients." Annals of Pharmacotherapy 28, no. 11 (1994): 1227–31. http://dx.doi.org/10.1177/106002809402801101.

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OBJECTIVE: To determine the effect of calcium-channel blockers (CCBs) on cyclosporine dose, clearance, and cost, and their effect on kidney graft function and survival in patients who underwent kidney transplant. DESIGN: A total of 176 adults receiving 177 transplants were studied retrospectively. Patients were stratified as follows: no CCB (n=57), diltiazem (n=13), nifedipine (n=37), and verapamil (n=70). Patients received cyclosporine 3–4 mg/kg by continuous infusion for 5 days followed by cyclosporine 10 mg/kg/d po to maintain initial whole blood concentrations of 300–400 ng/mL. Clearance o

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14

Lopez, Larry M., and Tamara M. Santiago. "Isradipine—Another Calcium-Channel Blocker for the Treatment of Hypertension and Angina." Annals of Pharmacotherapy 26, no. 6 (1992): 789–99. http://dx.doi.org/10.1177/106002809202600610.

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OBJECTIVE: To review the pharmacology, pharmacokinetic disposition, dose recommendations, adverse effects, drug interactions, and efficacy of isradipine in patients with hypertension or ischemic heart disease. DATA SOURCES: Data from scientific literature were extracted, evaluated, and summarized for presentation. A MEDLINE search was conducted using the following indexing terms: isradipine, calcium-channel blockers, hypertension, and angina pectoris. Experiences from studies evaluating isradipine reported in the form of articles, abstracts, or proceedings involving patients or healthy subject

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15

Siddiqi, Nida, and Ibrahim F. Shatat. "Antihypertensive agents: a long way to safe drug prescribing in children." Pediatric Nephrology 35, no. 11 (2019): 2049–65. http://dx.doi.org/10.1007/s00467-019-04314-7.

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Abstract Recently updated clinical guidelines have highlighted the gaps in our understanding and management of pediatric hypertension. With increased recognition and diagnosis of pediatric hypertension, the use of antihypertensive agents is also likely to increase. Drug selection to treat hypertension in the pediatric patient population remains challenging. This is primarily due to a lack of large, well-designed pediatric safety and efficacy trials, limited understanding of pharmacokinetics in children, and unknown risk of prolonged exposure to antihypertensive therapies. With newer legislatio

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16

Lefebvre, M., V. Villière, L. Dumont, D. Garceau, and G. Caillé. "Intravenous bolus pharmacokinetics of TA-3090, a new calcium channel blocker in anesthetized dogs." European Journal of Pharmacology 183, no. 5 (1990): 1855. http://dx.doi.org/10.1016/0014-2999(90)92186-m.

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17

Kumagai, Yuji, Akio Fujimura, Tsuyoshi Shiga, Ken-ichiro Sunaga, Kyo-ichi Ohashi, and Akio Ebihara. "PHARMACOKINETICS AND PHARMACODYNAMICS OF A NEW CALCIUM CHANNEL BLOCKER MPC-1304 IN HYPERTENSIVE SUBJECTS." American Journal of Therapeutics 3, no. 12 (1996): 807–10. http://dx.doi.org/10.1097/00045391-199612000-00004.

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18

SCHWARZWALD, C. C., R. A. SAMS, and J. D. BONAGURA. "Pharmacokinetics of the calcium-channel blocker diltiazem after a single intravenous dose in horses1." Journal of Veterinary Pharmacology and Therapeutics 29, no. 3 (2006): 165–71. http://dx.doi.org/10.1111/j.1365-2885.2006.00733.x.

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19

Siegrist, Romain, Davide Pozzi, Gaël Jacob, et al. "Structure–Activity Relationship, Drug Metabolism and Pharmacokinetics Properties Optimization, andin VivoStudies of New Brain Penetrant Triple T-Type Calcium Channel Blockers." Journal of Medicinal Chemistry 59, no. 23 (2016): 10661–75. http://dx.doi.org/10.1021/acs.jmedchem.6b01356.

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20

Dubovsky, Steven L. "Applications of calcium channel blockers in psychiatry: pharmacokinetic and pharmacodynamic aspects of treatment of bipolar disorder." Expert Opinion on Drug Metabolism & Toxicology 15, no. 1 (2018): 35–47. http://dx.doi.org/10.1080/17425255.2019.1558206.

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21

Bernard, Elodie, Sylvain Goutelle, Yves Bertrand, and Nathalie Bleyzac. "Pharmacokinetic Drug-Drug Interaction of Calcium Channel Blockers With Cyclosporine in Hematopoietic Stem Cell Transplant Children." Annals of Pharmacotherapy 48, no. 12 (2014): 1580–84. http://dx.doi.org/10.1177/1060028014550644.

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22

El-Masry, Soha Mahmoud, and Noha Mahmoud El-Khodary. "Pharmacokinetic and Tolerability Comparison of Sustained and Immediate Release Oral Formulations of Nifedipine Tablet Formulations: A Single-Dose, Randomized, Open-Label, Two-Period, Two-Way Crossover Study in Healthy, Fasting Egyptian Male Volunteers." Drug Research 70, no. 02/03 (2019): 91–96. http://dx.doi.org/10.1055/a-1035-9212.

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AbstractNifedipine is one of calcium channel blockers that commonly used clinically to treat hypertension and angina in Egyptian patients. A sustained-release (SR) formulation of nifedipine is available in the Egyptian community and administered twice daily. This study aimed to to compare the pharmacokinetics and safety profiles of a 20 mg SR and IR (immediate release) formulation of nifedipine after single-dose administration in healthy Egyptian subjects. Randomized, crossed open-label two- way clinical trial, in 16 healthy adult volunteers, of 24.75±5.20 years, with BMI 23.26±1.756 were asse

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23

Johnson, Brian F., John Wilson, Raj Marwaha, Kathleen Hoch, and Johanna Johnson. "The comparative effects of verapamil and a new dihydropyridine calcium channel blocker on digoxin pharmacokinetics." Clinical Pharmacology and Therapeutics 42, no. 1 (1987): 66–71. http://dx.doi.org/10.1038/clpt.1987.109.

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24

Billups, Sarah J., and Barry L. Carter. "Mibefradil: A New Class of Calcium-Channel Antagonists." Annals of Pharmacotherapy 32, no. 6 (1998): 659–71. http://dx.doi.org/10.1345/aph.17323.

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OBJECTIVE: To describe the pharmacology, pharmacokinetics, and clinical efficacy of mibefradil compared with other agents used for hypertension and angina. DATA SOURCES: A MEDLINE search was performed for the period of January 1980 through September 1997 using the key terms mibefradil or Ro 40–5967. All articles written in English were considered for review. STUDY SELECTION AND DATA EXTRACTION: All clinical studies involving mibefradil were evaluated. Preclinical data were included if these data were not adequately represented in clinical (human) studies. DATA SYNTHESIS: Mibefradil is the firs

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25

Lechleitner, Monika, and Friedrich Hoppichler. "Present and Prospective Clinical Therapeutic Options for the Elderly Patient with Hypertension." Clinical Medicine Insights: Therapeutics 2 (January 2010): CMT.S2110. http://dx.doi.org/10.4137/cmt.s2110.

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Purpose The purpose of this review was to summarize current treatment guidelines and recently published studies about the efficacy and safety of antihypertensive therapy in elderly patients. Methods A literature research (MEDLINE) was performed with respect to the prevalence of hypertension in the elderly, the underlying pathophysiological mechanisms and current treatment options. Results Hypertension affects up to 70% of the population aged 65 years and older and results in a significant increase of cardiovascular morbidity and mortality. Antihypertensive drug therapy reduces the risk of card

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26

Lee, Hyung, Soo-Yeon Jung, Hang-Ah Park, et al. "Multi-Functional 3,4-Dihydroquinazoline Derivative as T-Type Calcium Channel Blocker: Pharmacokinetics and Anti-Tremor Activity." Bulletin of the Korean Chemical Society 31, no. 9 (2010): 2451–52. http://dx.doi.org/10.5012/bkcs.2010.31.9.2451.

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27

Teramura, T., T. Watanabe, S. Higuchi, and K. Hashimoto. "Pharmacokinetics of barnidipine hydrochloride, a new dihydropyridine calcium channel blocker, in the rat, dog and human." Xenobiotica 25, no. 11 (1995): 1237–46. http://dx.doi.org/10.3109/00498259509046679.

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28

Mueller, Markus S., Kasra Shakeri-Nejad, Marcelo M. Gutierrez, et al. "Tolerability and Pharmacokinetics of ACT-280778, a Novel Nondihydropyridine Dual L/T-type Calcium Channel Blocker." Journal of Cardiovascular Pharmacology 63, no. 2 (2014): 120–31. http://dx.doi.org/10.1097/fjc.0000000000000030.

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29

Shimizu, Norifumi, Shiroh Kishioka, Takehiko Maeda, et al. "Role of Pharmacokinetic Effects in the Potentiation of Morphine Analgesia by L-Type Calcium Channel Blockers in Mice." Journal of Pharmacological Sciences 94, no. 3 (2004): 240–45. http://dx.doi.org/10.1254/jphs.94.240.

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30

ORIBE, Hisatoshi, Hajime NAKASHIMA, Tetsuo SHITOU, et al. "Effect of Food and Gastric Acidity on the Pharmacokinetics of MPC-1304, a New Calcium Channel Blocker." Rinsho yakuri/Japanese Journal of Clinical Pharmacology and Therapeutics 22, no. 4 (1991): 757–66. http://dx.doi.org/10.3999/jscpt.22.757.

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31

Siegrist, Romain, Davide Pozzi, Gaël Jacob, et al. "Correction to Structure–Activity Relationship, Drug Metabolism and Pharmacokinetics Properties Optimization, and in Vivo Studies of New Brain Penetrant Triple T-Type Calcium Channel Blockers." Journal of Medicinal Chemistry 60, no. 5 (2017): 2163. http://dx.doi.org/10.1021/acs.jmedchem.7b00219.

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32

Yan, Aixia, Zhi Wang, Jiaxuan Li, and Meng Meng. "Human Oral Bioavailability Prediction of Four Kinds of Drugs." International Journal of Computational Models and Algorithms in Medicine 3, no. 4 (2012): 29–42. http://dx.doi.org/10.4018/ijcmam.2012100104.

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In the development of drugs intended for oral use, good drug absorption and appropriate drug delivery are very important. Now the predictions for drug absorption and oral bioavailability follow similar approach: calculate molecular descriptors for molecules and build the prediction models. This approach works well for the prediction of compounds which cross a cell membrane from a region of high concentration to one of low concentration, but it does not work very well for the prediction of oral bioavailability, which represents the percentage of an oral dose which is able to produce a pharmacol

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33

Leonova, M. V. "Drug-induced arrhythmias." Meditsinskiy sovet = Medical Council, no. 21 (January 17, 2021): 26–40. http://dx.doi.org/10.21518/2079-701x-2020-21-26-40.

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The article provides a scientific review based on the proceedings of the 2020 American Heart Association consensus on drugs that may cause arrhythmias on a risk-sensitive basis and a guidance on strategies for monitoring, prevention methods and therapeutic approaches.The risk factors for drug-induced arrhythmias are divided into modifiable and non-modifiable. Among the non-modifiable risk factors are congenital anomalies (changes in the conduction system, ion channel polymorphism) and heart diseases (cavity dilatation, myocardial ischemia). Among the modifiable risk factors are various electro

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34

TERAMURA*, T., T. WATANABE, S. HIGUCHI, and K. HASHIMOTO. "Metabolism and pharmacokinetics of barnidipine hydrochloride, a calcium channel blocker, in man following oral administration of its sustained release formulation." Xenobiotica 27, no. 2 (1997): 203–16. http://dx.doi.org/10.1080/004982597240695.

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35

Hanke, Nina, Denise Türk, Dominik Selzer, et al. "A Mechanistic, Enantioselective, Physiologically Based Pharmacokinetic Model of Verapamil and Norverapamil, Built and Evaluated for Drug–Drug Interaction Studies." Pharmaceutics 12, no. 6 (2020): 556. http://dx.doi.org/10.3390/pharmaceutics12060556.

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The calcium channel blocker and antiarrhythmic agent verapamil is recommended by the FDA for drug–drug interaction (DDI) studies as a moderate clinical CYP3A4 index inhibitor and as a clinical Pgp inhibitor. The purpose of the presented work was to develop a mechanistic whole-body physiologically based pharmacokinetic (PBPK) model to investigate and predict DDIs with verapamil. The model was established in PK-Sim®, using 45 clinical studies (dosing range 0.1–250 mg), including literature as well as unpublished Boehringer Ingelheim data. The verapamil R- and S-enantiomers and their main metabol

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36

Dubey, Rupal, Umadoss Pothuvan, Pankaj Bhamare, Alka Singh, and Neeraj Upmanyu. "A Review on Drug of Pediatric Pulmonary Arterial Hypertension (PAH), their Chemistry and Pharmaceutical Dosage Forms." Journal of Drug Delivery and Therapeutics 10, no. 2-s (2020): 156–70. http://dx.doi.org/10.22270/jddt.v10i2-s.3947.

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Hypertension, specifically pulmonary hypertension, is a syndromethat can affect pediatric patients as well as adults. Pulmonary arterial hypertension (PAH) in pediatric patients, while rare, can be a lifethreateningcondition. There is no cure for PAH, only treatment options forchildren that are largely based on the results of adult studies. These therapies, however, can improve quality of life and survival. Treatment can be challenging because of the less approved medications and tolerable dosage forms for pediatric patients. Pediatric pulmonary arterial hypertension (PAH) shares common featur

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37

An, Guohua, Wei Liu, W. Rachel Duan, Wolfram Nothaft, Walid Awni, and Sandeep Dutta. "Population Pharmacokinetics and Exposure-Uric Acid Analyses After Single and Multiple Doses of ABT-639, a Calcium Channel Blocker, in Healthy Volunteers." AAPS Journal 17, no. 2 (2015): 416–26. http://dx.doi.org/10.1208/s12248-014-9709-1.

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38

Zhang, Hong, Min Wu, Yue Hu та ін. "Pharmacokinetics and pharmacodynamics of MT-1207, a novel multitarget blocker of α1 receptor, 5-HT2A receptor, and calcium channel, in healthy subjects". Expert Opinion on Investigational Drugs 30, № 3 (2021): 271–78. http://dx.doi.org/10.1080/13543784.2021.1887137.

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39

Iurlo, Alessandra, Roberto Latagliata, Cristina Bucelli, et al. "Very Elderly Patients with Chronic Phase-Chronic Myeloid Leukemia on Imatinib: No Impact of Concomitant Drugs on Complete Cytogenetic Response." Blood 126, no. 23 (2015): 1582. http://dx.doi.org/10.1182/blood.v126.23.1582.1582.

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Abstract Tyrosine-kinase inhibitors (TKIs)have completely changed the expected survival of chronic myeloid leukemia (CML) patients which is now approaching that of the general population: a relevant proportion of CML patients are currently elderly or very elderly. Very elderly patients represent generally a small proportion in published experiences. Older CML patients imatinib treated, as it happens in the general population, receive other drug treatments for associated chronic illnesses. Our aim is to assess if and which classes of concomitant drugs have an impact on cytogenetic response in c

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40

Sоkоvа, E. A., R. A. Chilova, O. A. Demidova, and K. O. Akopov. "Clinical Pharmacology Aspects of Some Tocolytic Drugs Used in Pregnant Women at Risk of Preterm Birth." Bulletin of the Scientific Centre for Expert Evaluation of Medicinal Products 9, no. 3 (2019): 162–66. http://dx.doi.org/10.30895/1991-2919-2019-9-3-162-166.

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Spontaneous preterm birth is one of the most pressing issues in obstetrics, as it remains one of the leading causes of newborn morbidity and mortality. Pending issues of aetiology, pathogenesis, and absence of medicinal products indicated for the treatment of spontaneous preterm labour pose a challenge for rational pharmacotherapy. The paper presents the results of a scientific literature review on the problem of rational pharmacotherapy of spontaneous preterm labour using tocolytic drugs — calcium channel blockers, cyclooxygenase inhibitors. The paper summarises specific pharmacokinetic param

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41

An, Guohua, Wei Liu, W. Rachel Duan, Wolfram Nothaft, Walid Awni, and Sandeep Dutta. "Erratum to: Population Pharmacokinetics and Exposure-Uric Acid Analyses After Single and Multiple Doses of ABT-639, a Calcium Channel Blocker, in Healthy Volunteers." AAPS Journal 17, no. 2 (2015): 481–92. http://dx.doi.org/10.1208/s12248-015-9725-9.

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42

Nikulina, N. N., S. V. Seleznev, M. B. Chernysheva, and S. S. Yаkushin. "Drug-induced bradycardia as a medical and social problem: data from the Cardiac Drug Overdoses Hospital Registry (STORM)." Russian Journal of Cardiology 25, no. 7 (2020): 3918. http://dx.doi.org/10.15829/1560-4071-2020-3918.

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Aim. To analyze hospitalizations due to drug-induced bradyarrhythmia (DIB) over a 5-year period (2014-2018), its clinical characteristics, causes and outcomes.Material and methods. The analysis included all hospitalizations due to DIB at the Ryazan Regional Vascular Center in 2017 and 2018 and retrospectively in 2014.Results. A total of 325 cases of DIB were included in the analysis (age 76,0 [68.0; 82.0] years; men — 26,1%). The proportion of DIB as a hospitalization cause in 2017 increased by 4,3 times compared to 2014 (p<0,001), in 2018 compared to 2014 — by 6,3 times (p<0,001) and co

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43

Lin, Brian Leei, Damian Matera, Julia F. Doerner, et al. "In vivo selective inhibition of TRPC6 by antagonist BI 749327 ameliorates fibrosis and dysfunction in cardiac and renal disease." Proceedings of the National Academy of Sciences 116, no. 20 (2019): 10156–61. http://dx.doi.org/10.1073/pnas.1815354116.

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Transient receptor potential canonical type 6 (TRPC6) is a nonselective receptor-operated cation channel that regulates reactive fibrosis and growth signaling. Increased TRPC6 activity from enhanced gene expression or gain-of-function mutations contribute to cardiac and/or renal disease. Despite evidence supporting a pathophysiological role, no orally bioavailable selective TRPC6 inhibitor has yet been developed and tested in vivo in disease models. Here, we report an orally bioavailable TRPC6 antagonist (BI 749327; IC50 13 nM against mouse TRPC6, t1/2 8.5–13.5 hours) with 85- and 42-fold sele

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44

Kochar, Mahendr S., and M. Ismail Qurashi. "Calcium channel blockers." Postgraduate Medicine 102, no. 6 (1997): 127–36. http://dx.doi.org/10.3810/pgm.1997.12.385.

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45

Abe, Masanori. "Calcium Channel Blockers." Journal of Nihon University Medical Association 73, no. 1 (2014): 12–13. http://dx.doi.org/10.4264/numa.73.12.

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46

White, Pamela. "Calcium Channel Blockers." AACN Advanced Critical Care 3, no. 2 (1992): 437–46. http://dx.doi.org/10.4037/15597768-1992-2015.

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Calcium channel blockers are widely used in the treatment of ischemic heart disease, hypertension, and supraventricular tachycardia. The prototype agents, verapamil, nifedipine, and diltiazem, represent three classes of calcium channel blockers, each of which has different pharmacologic effects. Nifedipine and the other dihydropyridines primarily are vasodilators and have no clinical effects on cardiac conduction or contractility. Diltiazem and verapamil also are vasodilators, but they possess, to varying degrees, negative inotropic, chronotropic, and dromotropic effects. Side effects of these

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47

Buckley, Nick, Andrew Dawson, and Ian Whyte. "Calcium channel blockers." Medicine 35, no. 11 (2007): 599–602. http://dx.doi.org/10.1016/j.mpmed.2007.08.025.

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Whyte, Ian, Nick Buckley, and Andrew Dawson. "Calcium channel blockers." Medicine 40, no. 3 (2012): 112–14. http://dx.doi.org/10.1016/j.mpmed.2011.12.022.

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Whyte, Ian, Nick Buckley, and Andrew Dawson. "Calcium channel blockers." Medicine 44, no. 3 (2016): 148–50. http://dx.doi.org/10.1016/j.mpmed.2015.12.029.

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Weiner, Donald A. "Calcium Channel Blockers." Medical Clinics of North America 72, no. 1 (1988): 83–115. http://dx.doi.org/10.1016/s0025-7125(16)30787-8.

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