Calcium channel blockers classes

Sica DA. Calcium channel blocker class heterogeneity select aspects of pharmacokinetics and pharmacodynamics, j Clin Hypertens. 2005 7(suppl l) 21-26. 

Other concerns related to side effects are fairly minor. Hypotension may occur with some agents, especially with bretylium (class III) and calcium channel blockers (class IV). Therapists should be aware that patients may become dizzy, especially after sudden changes in posture. 

Verapamil. Verapamil hydrochloride is a pbenyl alkyl amine and is considered the prototype of the Class I calcium channel blockers. Verapamil is also a potent inhibitor of coronary artery spasm and is useful in Prinzmetal s angina and in unstable angina at rest. Verapamil produces negative chronotropic and inotropic effects. These two actions reduce myocardial oxygen consumption and probably account for the effectiveness of verapamil in chronic stable effort angina (98,99). Moreover, verapamil is an effective antihypertensive agent. 

ACE inhibitors can be administered with diuretics (qv), cardiac glycosides, -adrenoceptor blockers, and calcium channel blockers. Clinical trials indicate they are generally free from serious side effects. The effectiveness of enalapril, another ACE inhibitor, in preventing patient mortaUty in severe (Class IV) heart failure was investigated. In combination with conventional dmgs such as vasodilators and diuretics, a 40% reduction in mortaUty was observed after six months of treatment using 2.5—40 mg/d of enalapril (141). However, patients complain of cough, and occasionally rash and taste disturbances can occur. 

The so-called calcium channel blockers constitute a class of cardiovascular agents that have gained prominence in the past few years. These drugs, which obtund contraction of arterial vessels by preventing the movement of calcium ions needed for those contractions, have proved especially useful in the treatment of angina and hypertension. Dihydropyridines such as nifedipine (30) are par-... 

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-... 

Many different drug classes have shown to cause hypotension and orthostatic reactions and drugs for cardiovascular conditions, psychoactive medicines and polypharmacy, can all have this side effect (Box 5.15). Among the most frequently used drugs in the elderly are diuretics, ACE-inhibitors, angiotensin II antagonists, calcium channel blockers and antidepressants. 

These drugs were developed as coronary vasodilating agents and were used for that purpose for some time, until it was discovered that they inhibit the contractile effect of calcium on smooth musculature and cardiac muscle, and that they affect calcium channels on the cell surface that permit calcium ions to enter. At first, they were called calcium antagonists however, later on this class of compounds was given the preferred name of calcium channel blockers. 

Chemically, calcium channel blockers are synthesized up of a fairly diverse group of compounds, which testifies of the diverse receptive regions both on the cell membrane surface as well as within the cell. Verapamil, which can be viewed as a benzylcyanide derivative, is one of the oldest and most actively used compounds of this class up to the present day. Diltiazem is a thiodiazepine, while nifedipin and nicardipine are derivatives of dihydropyridine. 

Antihypertensive drugs can be divided into eight classes based on the mechanism of action diuretics, )3-adrenoblockers, centrally acting sympatholytics, peripherally acting sympatholytics, calcium channel blockers, myotropic hypotensive drugs, angiotensin-con-verting enzyme inhibitors, and calcium channel activators. 

The following drug classes may have a potential drug interaction with nevirapine Antiarrhythmics, anticonvulsants, antifungals, calcium channel blockers, cancer chemotherapy (cyclophosphamide), ergot alkaloids, immunosuppressants, motility agents, opiate agonists. 

The six main drug classes used, worldwide, for blood pressure lowering treatment are diuretics, jS-blockers, calcium channel blockers (CCB), ACE inhibitors, angiotensin II (All) receptor blockers and a-adrenergic blockers. In some parts of the world, reserpine and methyldopa are also frequently used. 

The effects of the prototypical calcium channel blockers are seen most prominently in the cardiovascular system (Table 19.1), although calcium channels are widely distributed among excitable cells. The following calcium channel-blocking drugs are clinically the most widely used compounds in this very extensive class of pharmacological agents amlodipine, diltiazem, isradipine, nifedipine, nicardipine, nimodipine, and verapamil. 

The other major class of medications examined systematically is the calcium channel blockers. The more... 

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... 

This class of drugs includes the oral vasodilators, hydralazine and minoxidil, which are used for long-term outpatient therapy of hypertension the parenteral vasodilators, nitroprusside, diazoxide, and fenoldopam, which are used to treat hypertensive emergencies the calcium channel blockers, which are used in both circumstances and the nitrates, which are used mainly in angina (Table 11-3). 

Sodium and potassium are not the only ions which can participate in pumps and channels. Calcium is also pumped, channeled, exhanged,and stored. See Figure 23. Calcium concentration within the cell cytoplasm is very low. This allows the calcium to play a pivotal role in cellular activity. The cytoplasmic protein calmodulin binds and stores calcium ion. Various intracellular structures and organelles such as the mitochondria and sarcoplasmic reticulum also store calcium. Calcium is vital to such functions as the release of neurotransmitters from nerve cells. There are at least seven known modes of biochemical action for this ion, one of the most important of which involves stimulation of cardiac muscle protein (actin-myosin). Certain types of angina (heart pain) are believed to be caused by abnormal stimulation of cardiac arteries and muscle (coronary spasm) A relatively new class of drugs, known as the calcium channel blockers, has brought relief from pain and arrhythmias (irregular heart beats). 

STEP 1 In patients with mild hypertension, drug therapy is usually initiated with a single agent (monotherapy) from one of the following classes a diuretic, a beta blocker, an angiotensin converting enzyme (ACE) inhibitor, or a calcium channel blocker. 

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