Amlodipine, a new 1,4-dihydropyridine calcium antagonist with a particularly strong antihypertensive profile

Fleckenstein, A.; Frey, M.; Zorn, J; Fleckenstein-Grün, G.

doi:10.1016/0002-9149(89)90957-0

Cited by 30 publications

(12 citation statements)

References 11 publications

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“…Amlodipine and TREK-1 in the Cardiovascular System. Amlodipine is one of the most effective Ca 2ϩ antagonists prescribed in the treatment of hypertension (Fleckenstein et al, 1989). It is not known whether any of the actions of amlodipine on the cardiovascular system could be due to inhibition of TREK-1 channels.…”

Section: Discussionmentioning

confidence: 99%

Potent Inhibition of Native TREK-1 K⁺Channels by Selected Dihydropyridine Ca²⁺Channel Antagonists

Liu¹,

Enyeart²,

Enyeart³

2007

J Pharmacol Exp Ther

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Bovine adrenal zona fasciculata (AZF) cells express bTREK-1 background K ϩ channels that set the resting membrane potential. Whole-cell and single-channel patch-clamp recording were used to compare five Ca 2ϩ channel antagonists with respect to their potency as inhibitors of native bTREK-1 K ϩ channels. The dihydropyridine (DHP) Ca 2ϩ channel antagonists amlodipine and niguldipine potently and specifically inhibited bTREK-1 with IC 50 values of 0.43 and 0.75 M, respectively. The other Ca 2ϩ channel antagonists, including the DHP nifedipine, the diphenyldiperazine flunarizine, and the cannabinoid anandamide were less potent, with IC 50 values of 8.18, 2.48, and 5.07 M, respectively. Additional studies with the highly prescribed antihypertensive amlodipine showed that inhibition of bTREK-1 by this agent was voltage-independent and specific. At concentrations that produced near complete block of bTREK-1, amlodipine inhibited voltage-gated K v 1.4 K ϩ and T-type Ca 2ϩ

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Section: Discussionmentioning

confidence: 99%

Potent Inhibition of Native TREK-1 K⁺Channels by Selected Dihydropyridine Ca²⁺Channel Antagonists

Liu¹,

Enyeart²,

Enyeart³

2007

J Pharmacol Exp Ther

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“…Some dihydropyridine CCBs preferentially dilate the preglomerular blood vessels (2). The preferential dilation of preglomerular afferent arterioles might induce the elevation lower the blood pressure in a RAS-independent manner (9,10). In recent years, combination therapy with different types of antihypertensive drugs has been increasingly used in an effort to improve on the clinical benefits of monotherapy.…”

Section: Introductionmentioning

confidence: 99%

Renoprotective Effects of Benidipine in Combination with Angiotensin II Type 1 Receptor Blocker in Hypertensive Dahl Rats

et al. 2003

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“…Amlodipineis a dihydropyridine calcium antagonist that inhibits the transmembrane influx of calcium ions into vascular smooth muscle and cardiac muscle [15,16].…”

Section: Amlodipine Besylate (Norvascmentioning

confidence: 55%

Simultaneous Determination of Dofetilide and Amlodipine in Plasma by HPLC

Kaddar¹,

Pilote²,

Wong³

et al. 2013

J Chromat Separation Techniq

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Dofetilide is a Class III antiarrhythmic drug useful in the management of atrial fibrillation but also known to prolong the QT interval on the ECG and to induce malignant ventricular tachyarrhythmias such as torsades de pointes (TDP). Drugs with calcium channel-blocking properties contribute to decrease the incidence of TDP. Amlodipine is a dihydropyridine calcium channel antagonist. Considering the potentially safe and useful combined use of dofetilide and amlodipine, we undertook drug biotransformation studies. To perform studies aiming to evaluate the possible pharmacokinetic interaction between these drugs, a unique sensitive HPLC assay able to quantify both drugs simultaneously was required. A sensitive and specific HPLC method using a tandem of UV/fluorescence detection was described for the analysis of amlodipine and dofetilide in plasma. The within-day and between-day precision studies showed good reproducibility with coefficients of variation less than 10% for all the analytes. The limits of detection were 0.5 ng/mL and 0.25 ng/mL and the limit of quantification were 1.7 ng/mL and 0.8 ng/mL for dofetilide and amlodipine respectively. This new method could be of great value in many applications such as in vitro and in vivo pharmacokinetic and drug-drug interactions studies, as well as therapeutic drug monitoring.

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Amlodipine, a new 1,4-dihydropyridine calcium antagonist with a particularly strong antihypertensive profile

Cited by 30 publications

References 11 publications

Potent Inhibition of Native TREK-1 K⁺Channels by Selected Dihydropyridine Ca²⁺Channel Antagonists

Potent Inhibition of Native TREK-1 K⁺Channels by Selected Dihydropyridine Ca²⁺Channel Antagonists

Renoprotective Effects of Benidipine in Combination with Angiotensin II Type 1 Receptor Blocker in Hypertensive Dahl Rats

Simultaneous Determination of Dofetilide and Amlodipine in Plasma by HPLC

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Amlodipine, a new 1,4-dihydropyridine calcium antagonist with a particularly strong antihypertensive profile

Cited by 30 publications

References 11 publications

Potent Inhibition of Native TREK-1 K+Channels by Selected Dihydropyridine Ca2+Channel Antagonists

Potent Inhibition of Native TREK-1 K+Channels by Selected Dihydropyridine Ca2+Channel Antagonists

Renoprotective Effects of Benidipine in Combination with Angiotensin II Type 1 Receptor Blocker in Hypertensive Dahl Rats

Simultaneous Determination of Dofetilide and Amlodipine in Plasma by HPLC

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Potent Inhibition of Native TREK-1 K⁺Channels by Selected Dihydropyridine Ca²⁺Channel Antagonists

Potent Inhibition of Native TREK-1 K⁺Channels by Selected Dihydropyridine Ca²⁺Channel Antagonists