Nifedipine Bayer

Adalat Retard (Nifedipine). Bayer pic. UK Summary of product characteristics, September 2006. 

Adalat CC (Nifedipine). Bayer HealdiCare. US Prescribing information, August 2005. 

Calcium antagonists (Figure 4.3) are agents which block the flow of calcium ions into cardiac and vascular smooth muscle when they are stimulated to contract. They have value as vasodilators for use in hypertension and also reduce blood flow resistance and cardiac workload in the treatment of angina. Verapamil (Knoll Pfizer, 1967) is also used as an antiarrhythmic because of its effects on ion channels in the heart s electrical conduction system. Nifedipine (Bayer, 1977) is among the world s top 25 drugs and is the forerunner of several agents of the dihydropyridine class. 

It is closely related to the Bayer compound nifedipine currently under investigation in Europe as an antianginal agent (40). 

USAN Nifedipine Trade name Adaialf Bayer... 

Generally, the dihydropyridine CCBs have evolved into three distinct subclasses based on their pharmacokinetics and pharmacodynamics. Early dihydropyridines such as nifedipine and nicardipine are characterized by a rapid onset of action and short duration of action due to limited half-life lives, thus requiring twice-daily dosing (Bayer, 2004). In addition, these short-acting compounds may have potential detrimental effects... 

As mentioned before, nifedipine was the first marketed dihydropyridine CCB. Initially, the drug indication was exclusively for angina, but the more recently developed extended release (ER) formulations are used off-label primarily for hypertension (Bayer, 2004). The extended-release tablets use a cellulose coat that extends their release time. The half-life of the ER formulation is reported as 7 h, whereas the immediate-release formulation has a half-life of 2 h (Bayer). 

The probably most striking example so far of solvent influence on enzyme selectivity has been found by Yoshihiko Hirose and co-workers at the Amano Corp. in Nagoya, Japan, studying nifedipines, which provide a befitting conclusion of this chapter and a transition to the next on use of enzyme catalysis in the pharma industry. Nifedipines, structurally 1-substituted dihydropyridine mono- or diesters, are used in cardiovascular therapy, where they are termed calcium antagonists (Goldmann, 1991) the most prominent representative is Adalat from Bayer (Leverkusen, Germany). While the simplest achiral dihydropyridines can be syn-... 

Meyer H, et al. Bayer-Symposium, 9th Cardiovascular Eff. Dihydropyridine-Type Calcium Antagonists Agonists, Rigid Calcium Agonists of the Nifedipine Type Geometric Requirements for the Dihydropyridine Receptor 1985 90-103. 

The l,4-dihydro-2,6-dimethyl-4-(2- or 3-nitrophenyl)-3,5-pyridine-dicarboxylate derivatives nifedipine (NF), nitrendipine (NT), and nimodipine (NM) were supplied by Bayer AG (Wuppertal, Germany). Analytical grade reagents were used at all times, toluene AR (Riedel-de-Haen AG, Seelze, Germany) was distilled over a 50 cm Vigreux column before use. Sodium hydroxide, 0.5 mol/L, was purchased from J.T. Baker Chemical Corp. (USA) and the amber screw-cap autosampler bottles (2 mL) were obtained from Pierce Biotechnology Inc. (Rockford IL USA) and rinsed with acetone before use. 

Nifedipine ( Adalat, Bayer 10A0)(20), used for the treatment of angina, 87 is a powerful peripheral vasodilator and has hypotensive properties in man.88 A dose of 30mg sublingually lowered blood pressure substantially in 1A essential hypertensives for more than k hrs. with a rise in heart rate and plasma renin activity. Nifedipine interferes with the transmembrane calcium flux causing a reduction in vascular smooth muscle tone.87)89 The conformational requirement for dopamine induced renal... 

Nifedipine Adalat Bayer U.K. (1) treatment and prophylaxis of angina pectoris (2) treatment of hypertension (3) treatment of Raynaud s phenomenon... 

Mannhold R, Rodenkirchen R and Bayer R, Haus W, The importance of drug ionization for the action of calcium antagonistsand related compounds, Arzneim.-Forsch., 34, 407-409 (1984). NB Tetrabutylammonium hydroxide used as base. Cited in Nifedipine, Ali SL, APDS, 18,231-288 (1989). 

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