Hypertension direct vasodilators

Prazosin is a selective aradrenergic receptor antagonist that, at therapeutic doses, has little activity at a2-adrenergic receptors and clinically insignificant direct vasodilating activity The drug does not cause the other effects attributed to phentolamine. Most important, it produces less tachycardia than does phentolamine and, therefore, is useful in the treatment of essential hypertension. 

Which of the following diuretics could be added to the therapeutic regimen of a patient who is receiving a direct vasodilator for the treatment of hypertension ... 

All patients taking these drugs for long-term hypertension therapy should first receive both a diuretic and a /1-blocker. The diuretic minimizes the side effect of sodium and water retention. Direct vasodilators can precipitate angina in patients with underlying coronary artery disease unless the baroreceptor reflex mechanism is completely blocked with a /3-blocker. Nondihydropyridine CCBs can be used as an alternative to /3-blockers in patients with contraindications to /3-blockers. 

Propranolol was the first blocker shown to be effective in hypertension and ischemic heart disease. Propranolol has now been largely replaced by cardioselective blockers such as metoprolol and atenolol. All B-adrenoceptor-blocking agents are useful for lowering blood pressure in mild to moderate hypertension. In severe hypertension, blockers are especially useful in preventing the reflex tachycardia that often results from treatment with direct vasodilators. Beta blockers have been shown to reduce mortality after a myocardial infarction and some also reduce mortality in patients with heart failure they are particularly advantageous for treating hypertension in patients with these conditions (see Chapter 13). 

Hypertension is an important risk factor for coronary heart disease and stroke. Since ancient times, hypertensive patients have been treated orally with plant extracts based on folk medicine. However, and despite their in vitro vasodilator effects, little information about the protective effects of flavonoids on hypertension is available in the literature. Flavonoids have been considered as active principles of several antihypertensive plant extracts (e.g. rhamnoglycoside of limocitrin isolated from Citrus limonum, kaempferol 4 -0-glucose and hyperin from Euphorbia maddeni, moracenins from Morus alba, procyanidin glycoside from Rhamnus lycioides) [150,151]. In all cases, only the acute antihypertensive effects after i.v. administration in anaesthetised normotensive and/or hypertensive animals have been described. In addition to the direct vasodilator effects discussed above, the inhibition of angiotensin-converting enzyme reported... 

Phentolamine is a nonselective a-adrenoceptor blocker. It is given i.v. for brief effect in adrenergic hypertensive crises, e.g. phaeochromocytoma or the MAOI-S5nnpathomimetic interaction. In addition to a-neceptor block it has direct vasodilator and cardiac inotropic actions. The dose for hypertensive crisis is 2-5 mg i.v. repeated as necessary (in minutes to hours). The use of phentolamine as a diagnostic test for phaeochromocytoma is appropriate only when biochemical measurements are impracticable, since it is less reliable. 

Careful monitoring of the heart and hemodynamic status should be performed. Hypertension and symptoms of CNS stimulation usually resolve spontaneously with only supportive measures. Antiarrhythmic and antihypertensive agents may be necessary in severe exposures. If treatment of hypertension is necessary, a direct vasodilator such as nitroprusside or nifedipine should be utilized. Treat agitation and seizures as necessary with benzodiazepines. Management of concurrently ingested drugs should be appropriate to the agent involved. 

Antihypertensive Vasodilators - A common characteristic of hypertensive patients, regardless of the etiology of their disease, is abnormally high peripheral vascular resistance. Drugs that act directly on peripheral vasculature to decrease resistance are, therefore, logical agents for the treatment of hypertension. Unfortunately, sympathetic reflex actions leading to cardiac stimulation, hyperreninemia and fluid retention limit the hypotensive action of vasodilators and they are used mainly in combination with 6-blockers and diuretics for the treatment of more severe hypertension. A vasodilator that may not cause undesirable reflex... 

Celiprolol is a potent beta -adrenergic receptor antagonist. It has intrinsic sympathomimetic action, possesses some alpha2-adrenoreceptor antagonistic properties, is a direct vasodilator, and a direct bronchodilator. Celiprolol is incompletely and variably absorbed, eliminated both in bile and urine, and has a half-life of 4 to 5 hours. Celiprolol (200 to 400 mg/day) has efficacy similar to atenolol or propranolol in reducing blood pressure and is useful in hypertensive patients with asthma or bronchitis. Furthermore, celiprolol is as effective as atenolol in treating patients with stable angina. 

Epoprostenol is a peripheral vasodilator, with a direct vasodilation of pulmonary and systemic arterial vascular beds and inhibition of platelet aggregation. It is indicated in long-term IV treatment of primary pulmonary hypertension. 

In the treatment of hypertension, a major use of beta-blockers is in combination with hydralazine. The direct vasodilators bring about reflex cardiac stimulation, and beta-blockers prevent these adverse effects (see also Figure 67). Beta-blockers also reduce blood pressure by exerting a central effect or a peripheral action, or both, which decreases renin activity. Metoprolol and atenolol are beta selective, and they are safer agents in patients with asthma, diabetes mellitus, or low-renin hypertension. Some beta-blocking agents such as pindolol have intrinsic sympathomimetic activity and may be used in the treatment of pronounced bradycardia (sick sinus syndrome). Unlike propranolol, metoprolol is not a very lipid-soluble... 

Prazosin, (1 mg t.i.d.) alone or in combination with other drugs such as a diuretic, is indicated in the management of moderate hypertension. It is a direct vasodilator and is nsed for long-term therapy. Its side effects are sedation, postural hypotension, and headache (due to vasodilation). As much as 91% of prazosin is bound to plasma protein. When used for the first time or in larger-than-recommended doses, prazosin may cause pronounced hypotension, faintness, dizziness, and palpitations. These effects, which have been labeled first-dose phenomena, are seen especially in salt-and water-depleted patients. Therefore, the initial dose of prazosin is small, and it is given at bedtime. 

Calcium channel blockers cause more pronounced lowering of blood pressure in hypertensive patients than in normotensive individuals. Generally, all calcium channel blockers cause an immediate increase in PRA during acute treatment in patients having hypertension but PRA is normalized during chronic treatment despite the sustained decrease in blood pressure. These agents also do not generally produce sodium and water retention, unlike the conventional vasodilators. This is because they produce diuretic effects by direct actions on the kidney. 

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