Calcium channel blockers preparations

Benzothiazepines belong to the three classes of calcium channel blockers which are important cardiovascular drugs in the management of angina pectoris and hypertension. A diastereoselective one-pot synthesis of the trans-and ds-3-hydroxy-2-(4-methoxyphenyl)-2,3-dihydro-l,5-benzothiazepin-4-one nucleus, a key intermediate in the preparation of the calcium channel blocker Diltiazem, was carried out under microwave irradiation in an open vessel (Scheme 25). Control of the diastereoselectivity was achieved by vary-... 

A pharmacist asked a clinical pharmacist for information about Cartia . Because an electronic drug reference listed the active ingredient as aspirin, the pharmacist was prepared to substitute an aspirin product for Cartia . The clinical pharmacist recognized the new product as Cartia XT (Diltiazem, a calcium channel blocker) and prevented the error. 

Adalat is a proprietary preparation of nifedipine (a dihydropyridine calcium-channel blocker). 

Co-codamol is a combination of paracetamol (nonnapioid analgesic) and codeine (opioid analgesic). One of the side-effects of opioids is constipation. Naprosyn is a proprietary (trade name) preparation of the non-steroidal antiinflammatory drug naproxen Adalat is a proprietary preparation of the calcium-channel blocker nifedipine Amoxil is a proprietary preparation of the beta-lactam amoxicillin and Dulco-lax is the brand name of the stimulant laxative bisacodyl. 

Cytochrome P450 inhibition Coadministration of delavirdine tablets with certain nonsedating antihistamines, sedative hypnotics, antiarrhythmics, calcium channel blockers, ergot alkaloid preparations, amphetamines, and cisapride may result in potentially serious or life-threatening adverse events caused by possible effects of delavirdine on the hepatic metabolism of certain drugs metabolized by CYP3A and... 

Extensive stmcture activity relationship (SAR) studies in this series revealed that unsymmetrical substitution on the heterocyclic ring and hence the introduction of chirality on the central carbon atom led to increased potency. Such asymmetrical dihydro-pyridines can be prepared by stepwise variation of the Hantzsch synthesis, based on the hypothetical alternate route to nifedipine. Thus, aldol condensation of methyl acetoacetate with 2,3-dichlorobenzaldehyde (13-1) gives the cinnamyl ketone (13-2). Reaction of that with the enamine (13-3) from ethyl acetoacetate gives the calcium channel blocker felodipine (13-4) [14]. 

A benzoazathiazepine provides the nucleus for a stmcturally unusual calcium channel blocker. This was, incidentally, one of the first of the growing class of dmgs provided as the pure biologically active enantiomer. The key, and very carefully studied, reaction to the preparation of this compound consists of the opening of the racemic glycidic ester (27-2) with nitrothiophenol (27-1). The reaction proceeds to... 

Yuen, P.-W. (Warner-Lambert Co.), Substituted quinolines and isoquinolines as calcium channel blockers, their preparation and the use thereof, US5767129 (1998). 

Procardia XL, which is marketed by Pfizer, is a billion-dollar product employing Push-Pull technology. The preparation contains the calcium channel blocker nifedipine.40 A full list of marketed products developed by ALZA Corporation is shown in Table 7.4. 

Another example is the perturbing effect of eight calcium channel blockers on membranes prepared from two different lipids [68]. The authors used total lipids from rat brain and synaptosomal membranes. The spin probe was l-palmitoyl-2-stearoyl-phosphatidyl-choline labeled at the doxyl group at the carbon-16 position (16-PC). The apparent order parameter, S, is calculated from the apparent outer (Amax) and inner (Amin) splittings which were directly taken from the ESR spectra. It is used to describe the relative efficiency of the dmgs in perturbing the lipid membrane. 

The two isosteric diastereomers of the calcium channel blocker UK-74,756 have been prepared based on the resolution of the isosteric enantiomers of the 6,11-dihydrodibenzo[6,e]thiepin-l l-ol precursor [01TA975],... 

A focused SP library LIO of pools of 1,4-dihydropyridines (DHP) was reported by Gordeev et al. (45) and tested as a source of calcium channel blockers. The library consisted of 10 x 3 x 10 = 300 members prepared as 30 pools of 10 compounds (Fig. 4.11) whose deconvolution produced several new compounds of interest. The mono-... 

The pharmacodynamically active molecular structure of the calcium channel blocker, nifedipine, is photodecomposed by UV-VIS radiation (8). This effect is manifested by a change in color (from yellow to colorless) or the fading of colored preparations, formation of precipitation and alteration of the taste of the product. Such changes during storage may give patients the sense of uneasiness, confusion, and doubt as to the safety and efficacy of the product. 

One of the most widely used calcium channel blockers is verapamil. Verapamil hydrochloride was assayed from pharmaceutical preparations by ElGhany et al. [133]. The separations were performed on 200 x 100 mm and 100 x 100 mm silica gel 60 F254 plates using an ethyl acetate/methanol/water mobile phase and scanning the plates at 278 nm. The accuracy and precision data for the assay of spiked verapamil samples and the recovery data of verapamil from commercial preparations are shown in Tables 10.20 and 10.21. 

Unlike the situation with ephedra, in many cases we simply have no idea what the components do. The constituents of some herbal drugs seem to work synergistically and cannot be separated without loss of activity of the preparation. Herbal preparations are most often used as crude mixtures and are not standardized or analyzed for the content of the active principlc(s). Hence, the chemistry of medicinal herbs cannot be treated in the same way as that of. say. a pure antibiotic or a calcium channel blocker. The medicinal chemistry of the actions, interactions, and side effects of herbal products is complex and difficult to assess clinically and chemically. Frequently, some of the compounds present... 

Feldene piroxicam. felodipine [ban, inn, usan] (Plendil etc.) is a dihydropyridine calcium-channel blocker with VASODILATOR properties, which can be used in ANTIHYPERTENSIVE therapy and antianginal prophylaxis, felypressin [ban, inn, usan] ([Phe Lys ]vasopressin phelypressin PLV2 Octapressin Octopressin ) is a synthetic analogue of vasopressin. It is a VASOCONSTRICTOR and is incorporated into LOCAL ANAESTHETIC preparations to prolong their duration of action. (It is a constituent with prilocaine of Citanest with Octapressin .)... 

The nurse is preparing to administer a calcium channel blocker, a loop diuretic, and a beta blocker to a client diagnosed with arterial hypertension. Which action should the nurse implement ... 

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