Calcium channel blockers properties

Other agents are also used for the treatment of manic-depressive disorders based on preliminary clinical results (177). The antiepileptic carbamazepine [298-46-4] has been reported in some clinical studies to be therapeutically beneficial in mild-to-moderate manic depression. Carbamazepine treatment is used especially in bipolar patients intolerant to lithium or nonresponders. A majority of Hthium-resistant, rapidly cycling manic-depressive patients were reported in one study to improve on carbamazepine (178). Carbamazepine blocks noradrenaline reuptake and inhibits noradrenaline exocytosis. The main adverse events are those found commonly with antiepileptics, ie, vigilance problems, nystagmus, ataxia, and anemia, in addition to nausea, diarrhea, or constipation. Carbamazepine can be used in combination with lithium. Several clinical studies report that the calcium channel blocker verapamil [52-53-9] registered for angina pectoris and supraventricular arrhythmias, may also be effective in the treatment of acute mania. Its use as a mood stabilizer may be unrelated to its calcium-blocking properties. Verapamil also decreases the activity of several neurotransmitters. Severe manic depression is often treated with antipsychotics or benzodiazepine anxiolytics. 

The electrophysiological effects of amiodarone may be a composite of several properties. In addition to prolonging action potential duration and refractory period in ad tissues of the heart, the compound is an effective sodium channel blocker (49), calcium channel blocker (50), and a weak noncompetitive -adrenoceptor blocking agent (51). Amiodarone slows the sinus rate, markedly prolongs the QT interval, and slightly prolongs the QRS duration (1,2). 

Gupta SP (2006) QSAR Studies on Calcium Channel Blockers. 4 249-287 Gupton JT (2006) Pyrrole Natm-al Products with Antitimior Properties. 2 53-92 Gute BD, see Basak SC (2006) 3 39-80... 

If a patient s blood pressure is greatly increased, pharmacological treatment should be instituted. Treatments for MAOI-induced hypertension include administration of the calcium channel blocker nifedipine and use of drugs with a-adrenergic-blocking properties, such as phentolamine (5 mg intravenous). Because treatment with phentolamine may be associated with cardiac arrhythmias or severe hypotension, this approach should be carried out only in an emergency department setting. 

Certain other drugs also having uterine relaxant property are calcium channel blockers, prostaglandin synthesis inhibitors, progesterone, nitrites, anticholinergics, ethyl alcohol etc. 

Cinnarizine is an H 1-receptor antagonist and a calcium channel blocker used for the treatment of vertigo and emetic symptoms due to Meniere s disease and related labyrinth disorders. It is also effective in motion sickness. It is used for peripheral and cerebral vascular disorders, because of its calcium channel blocking properties. 

The pharmacokinetic properties of these drugs are set forth in Table 12-5. The choice of a particular calcium channel-blocking agent should be made with knowledge of its specific potential adverse effects as well as its pharmacologic properties. Nifedipine does not decrease atrioventricular conduction and therefore can be used more safely than verapamil or diltiazem in the presence of atrioventricular conduction abnormalities. A combination of verapamil or diltiazem with 3 blockers may produce atrioventricular block and depression of ventricular function. In the presence of overt heart failure, all calcium channel blockers can cause further worsening of heart failure as a result of their negative inotropic effect. Amlodipine, however, does not increase the mortality of patients with heart failure due to nonischemic left ventricular systolic dysfunction and can be used safely in these patients. 

Clozel J-P, Ertel EA, Ertel SI (1997) Discovery and main pharmacological properties of mibefradil (Ro 40-5967), the first selective T-type calcium channel blocker. J Hypertension 15(5) S17-S25... 

The calcium channel blockers are divided into three chemical classes, each with different pharmacokinetic properties and clinical indications (Figures 19.11 and 19.12). 

The spasmolytic action of cyclandelate, an ester of man-delic acid, was described as early as 1959, but only in later years have its properties been more fully investigated. It appears to act as a calcium channel blocker in smooth muscle and platelets, this effect being partly dne to inhibition of phosphodiesterases. It also produces increased deformability of erythrocytes, the mechanism of which is so far unknown, although phosphodiesterase inhibition may again be responsible. Cyclandelate also rednces the activity of the rate-limiting enzyme in the biosynthesis of cholesterol (HMG-CoA), and its antidiabetic properties may be due to inhibition of aldose rednctase. 

Felodipine is a dihydropyridine derivative with diuretic properties (1). Its diuretic properties are not unique but are shared by other dihydropyridines. Its vasodilator-related adverse effects include flushing, headache, and tachycardia (2,3). Reduced arterial oxygen saturation has been seen in patients given intravenous felodipine for pulmonary hypertension (4,5). Along with amlodipine, but unlike other calcium channel blockers, felodipine may be safer in severe chronic heart failure accompanied by angina or hypertension. 

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 .)... 

NSC 77370 CP 10188) is an ENZYME INHIBITOR, a selective irreversible tryptophan hydroxylase inhibitor, thereby depleting 5-HT in the brain. As an indirect 5-HT antagonist, it has been given to patients with carcinoid syndrome to relieve some of the symptoms, fendiline [inn] is a methylbenzylamine, a CALCIUM-CHANNEL BLOCKER and calmodulin antagonist, with coronary VASODILATOR properties. 

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