Hypertension and angina

Bevantolol hydrochloride is a moderately lipophilic, long-acting, cardioselective -adrenoceptor blocker. It has no ISA but has membrane-stabilizing activity. The dmg is in use in Europe for the treatment of hypertension and angina. It is rapidly absorbed from the GI tract. Peak plasma levels occur in 1—2 h. It is metabolized extensively in the Hver to a metaboHte that has some ISA. It is excreted by the Hver and the kidneys and excretion is delayed in patients having kidney failure. 

Carvedilol — This drug is a non-cardioselective p blocker used to manage hypertension and angina pectoris. Several methods have been developed to measure carvedilol in biological fluids.28 30 Zarghi et al developed a simple, rapid, and sensitive HPLC method to analyze carvedilol in human plasma... 

Amlodipine and nifedipine are dihydropyridine calcium-channel blockers. Amlodipine differs from nifedipine in that it has a longer duration of action and can therefore be given once daily, unlike nifedipine. Both are indicated in hypertension and angina and tend to cause ankle oedema that does not respond to diuretic therapy. Neither amlodipine nor nifedipine are available as spray formulations. 

Calcium-channel blockers such as amlodipine can be used in patients receiving angiotensin-receptor blockers such as valsartan for the treatment of hypertension and angina. Side-effects common to both drugs include dizziness and hypotension. 

Amlodipine is a calcium channel blocker used to treat hypertension and angina pectoris. Calcium channel blockers block the passage of calcium, an essential factor in muscle contraction, into the heart and smooth muscles. Such blockage interferes with the contraction of these muscles, which in turn dilates the veins that supply blood to them. This reduces blood pressure. 

Another cardioselective beta, blocking agent devoid of intrinsic sympathomimetic activity given once daily in the treatment of hypertension and angina pectoris. 

It is beta selective blocker with a modest capacity to activate beta receptors also. It is used in treating hypertension and angina pectoris. 

It is indicated in the treatment of essential hypertension and angina pectoris. 

Nifedipine is a dihydropyridine calcium channel modulator, often used in the treatment of hypertension and angina. CYP3A4, with a minor contribution from CYP3A5, is the principal enzyme involved in the metabolism of nifedipine (81). Smith et al. examined the effect of St. John s wort (900mg/day... 

Lancaster SG, Sorkin EM. Bisoprolol. A preliminary review of its pharmacodynamic and pharmacokinetic properties, and therapeutic efficacy in hypertension and angina pectoris. Drugs 1988 36(3) 256-85. 

Membrane bioreactors have been reported for the production of diltiazem chiral intermediate with a multiphase/extractive enzyme membrane reactor [15, 16]. The reaction was carried out in a two-separate phase reactor. Here, the membrane had the double role of confining the enzyme and keeping the two phases in contact while maintaining them in two different compartments. This is the case of the multiphase/ extractive membrane reactor developed on a productive scale for the production of a chiral intermediate of diltiazem ((2R,3S)-methylmethoxyphenylglycidate), a drug used in the treatment of hypertension and angina [15]. The principle is illustrated in... 

Lercanidipine (Fig. 7.10) is one of the last dihydropyridines introduced into the market. Its high lipophilicity explains its long duration of action. Lercanidipine is extensively metabolized in the liver after oral administration, and is then retained by vascular cells to achieve a sustained duration of action. It is used in the treatment of hypertension and angina. like lacidipine, its smooth onset of action... 

In conclusion, all dihydropyridines show a potent calcium channel antagonist activity, which is in turn translated into direct arteriolar spasmolytic effect that results in a beneficial vasodilatory activity. This is useful in some cardiovascular diseases, such as hypertension and angina, in which the peripheral resistances are raised due to increased calcium entry into the cells. Many analogues of nifedipine have been synthesized and introduced into the market, and each of these presents some common features and some peculiar differences. In particular ... 

Two groups of drugs, p-adrenergic blockers and calcium channel blockers, are used in both hypertension and angina. Several drugs for hypertension are used also in the treatment of heart failure. 

The therapeutic benefit of the calcium blockers in hypertension and angina is due mainly to their action as vasodilators. Their action on the heart gives non-dihydropyridines an additional role as Class 4 antiarrhythmics. 

The treatment of both hypertension and angina requires drugs that reduce the work of the heart cither directly or by lowering peripheral vascular resistance. 

The therapeutic advantages of p-adrenoceptor antagonists in the treatment of hypertension and angina are ascribed mainly to their S enantiomers. The R enantiomers, however, are not totally devoid of cardiovascular activities as properties like antiarrhythmias have been attributed to them. Hence, single enantiomers of these compounds may offer p-adrenoceptor blockers vrith different overall therapeutic profiles. The risk benefit ratio of using a single enantiomer of p-blockers, therefore, remains to be explored. 

A 43-year-old male non-smoker, with a history of asthma, hypertension, and angina pectoris, was admitted to an intensive care unit for mechanical ventilation for acute severe asthma (50). He was given an inhaled bronchodilator, aminophylline, and prednisolone. His condition improved slowly but he became hypovolemic. Within 60 seconds of a fluid challenge with pentastarch 200 ml he had a severe anaphylactoid reaction. 

The ability of certain nitrates, especially glycerol trinitrate, to lower the blood pressure has been used clinically in the treatment of hypertension and angina pectoris. A correlation was established between the rate of alkaline hydrolysis and the effectiveness of the nitrate in lowering the blood pressure D-mannitol hexanitrate, hydrolyzed more rapidly than glycerol... 

Use PO Treatment of angina due to Half-life Onset Peaks Duration coronary artery spasm (Prinzmetal s 3-8 hours PO 30-60 6-12 h 24 hours variant angina), chronic stable minutes angina (effort-associated angina). IV Immediate Extended release Treatment of essential hypertension and angina. Parenteral Temporary control of rapid ventricular rate in atrial fibrillation/flutter. Rapid conversion of PSVT to normal sinus rhythm. 

Pfizer s Procardia XL is a once daily calcium channel blocker (CCB) for hypertension and angina. It delivers nifedipine via Alza s osmotic pump, a patented high-tech sustained-release (SR) formulation. Several generic companies are currently seeking FDA approval for an A/B substitute using low-tech SR formulations. The generic companies claim that they are not infringing Pfizer s patent estate, which includes ... 

A more recent example of a drug discovered by chance observation is sildenafil (Viagra). This compound was developed as an inhibitor of phosphodiesterase 5, an enzyme that catalyzes the hydrolysis of cCiMP to GMP (Figure 35.16). The compound was intended as a treatment for hypertension and angina because cGMP plays a central role in the relaxation of... 

Covera-HS (verapamil) a controlled-onset, extended-release (COER-24) system for the management of hypertension and angina pectoris. 

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