By Dr. Winifred G. Nayler (auth.)
"Those who decide to bring up their wisdom nonetheless additional by way of examining ... will become aware of a thrilling new international. " NOEL WHITTAKER, in "Making funds Made uncomplicated" 1989. the advance of calcium antagonists has lately been defined as representing "one of the most important advances in cardiovascular thera peutics of the latter half the 20 th century" (Braunwald, 1990). even if, even supposing the improvement of those medications all started within the mid nineteen sixties it is just lately that their genuine strength has started to be preferred. Even now the calcium antagonist saga isn't entire, for the reason that new compounds proceed to seem and new healing applica tions emerge. in keeping with the event won within the clinics during which those medicinal drugs were used acceptance is being given now to the necessity to increase upon the prototypes of the crowd. Such development is leading to the advance and construction not just of long-acting formulations of the prototypes (nifedipine, verapamil and diltiazem) but in addition of latest calcium antagonists with more advantageous tissue selectivity, efficiency and period of motion. to these folks who're attracted to this box any such improvement is either intriguing and lucrative. so far as the clinicians who prescribe those medicinal drugs are involved the long-acting nature of a few of the more recent calcium antagonists may still make the passable administration in their sufferers an available goal.
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1), is light insensitive (in contrast to other dihydropyridine-based antagonists), is potent (daily dose of only 5-10 mg for control of hypertension (Chapter 14», and evokes minimal sideeffects (Chapter 18) - possibly because it has a slow onset of action (Chapter 6). The fascinating thing is that the slow onset of action of amlodipine is not due to its inclusion in a slow release capsule or some other slow release or slow absorbance device (as in the G ITS formulation of nifedipine). Instead it is an inherent property of the molecule and the way it associates with and dissociates from the dihydropyridine binding sites in the calcium channel complex.
2. 6. Some properties of second generation dihydropyridine-based calcium antagonists Compound Plasma half life Vascular selectivity Amlodipine Felodipine Isradipine Nicardipine Nimodipine Nisoldipine Nitrendipine 36 hr 10 hr 7 hr 4-5 hr 5 hr 8-12 hr 8 hr +++ +++ +++ +++ + + + (cerebral) + + + (coronary) +++ + denotes vascular selectivity. Vascular beds mentioned for nimodipine and nisoldipine indicate vascular beds which are particularly sensitive. Note the prolonged half-life of amlodipine, a property which must contribute to its prolonged duration of action (see Chapter 6).
Its chemical formula is as follows: (+)( -2S-3S)-3-acetoxy-8-chloro-5-(2-dimethylamino)ethyl)-2,3-dihydro-2-( 4-methoxyphenyl)-1,s-benzothiazepine-4 (5 H)-one maleate. , 1991). , 1988). Another benzothiazepine-based second generation calcium antagonist which does merit a mention here is still only known by its code number, SD3211. This compound is (+ )-(R)-3,4-dihydro-2-[5-methoxy-2-[3-[N-methylN -[2-[ (3,4-methylenedioxy)phenoxy]ethyl]amino]propoxy]phenyl] -4-methyl3-oxo-2H -l,4-benzothiazine hydrogen fumarate.
Amlodipine by Dr. Winifred G. Nayler (auth.)