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Query: UMLS:C0020538 (hypertension)
 170,190 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

The physicochemical properties, pharmacology, pharmacokinetics, cardiovascular and metabolic effects, adverse effects, dosage, and administration of doxazosin are described, and comparative clinical studies of doxazosin therapy in patients with mild to moderate hypertension are reviewed. Doxazosin mesylate, an alpha 1-adrenoceptor antagonist, is rapidly absorbed after oral administration and undergoes extensive hepatic metabolism. The drug decreases blood pressure by reducing peripheral resistance. Maximum hypotensive effects occur four to eight hours after the dose. Doxazosin favorably affects serum lipids by increasing concentrations of high-density lipoprotein (HDL) cholesterol, increasing the HDL:total cholesterol ratio, and decreasing concentrations of low-density lipoprotein cholesterol, total cholesterol, and triglycerides. In comparative clinical trials, doxazosin lowered standing and supine systolic and diastolic blood pressures as effectively as other alpha-adrenoceptor antagonists, beta-adrenoceptor antagonists, diuretics, angiotensin-converting-enzyme inhibitors, and calcium-channel-blocking agents. The most frequently reported adverse effects are dizziness, headache, nausea, lethargy, and fatigue. Doxazosin may be used either alone or in combination with a beta-adrenoceptor inhibitor or a diuretic. Orthostatic hypotension after the first dose occurs infrequently and may be minimized by initiating therapy at a dosage of 1 mg/day. The dosage may be increased at two-week intervals as needed, and blood pressure should be closely monitored. Doxazosin has blood-pressure-lowering effects comparable to those of other alpha 1-adrenoceptor inhibitors and to those of antihypertensives in other drug classes.
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PMID:Doxazosin: a new alpha 1-adrenergic antagonist. 134 55

Conventional formulations of metoprolol have become well established in cardiovascular medicine and are particularly useful in the management of hypertension and ischaemic heart disease. Recently developed controlled release metoprolol delivery systems (metoprolol CR/ZOK and metoprolol OROS) were designed to overcome the drug delivery problems of matrix-based sustained release forms by releasing the drug at a relatively constant rate over a 24-hour period, and thus producing sustained and consistent metoprolol plasma concentrations and beta 1-blockade while retaining the convenience of once daily administration. Clinically and statistically significant reductions in blood pressure have been observed with metoprolol CR/ZOK and metoprolol OROS 24 hours after administration in mildly or moderately hypertensive patients. Studies in patients with mild to moderate hypertension have demonstrated that a similar or higher percentage of patients achieved a goal response with metoprolol CR/ZOK compared with matrix-based sustained release formulations of metoprolol, or conventional atenolol or bisoprolol, while metoprolol OROS achieved an equal or greater response rate compared with conventional or matrix-based sustained release metoprolol preparations. In patients with stable effort angina pectoris, once daily administration of metoprolol CR/ZOK provided at least equal antianginal efficacy as conventional metoprolol in divided doses, while metoprolol OROS reduced the mean number of anginal attacks by the same margin as atenolol. Controlled release metoprolol formulations have been well tolerated in clinical trials. Metoprolol CR/ZOK was associated with a similar or lesser degree of adverse effects related to the central nervous system compared with atenolol or long acting propranolol. Metoprolol CR/ZOK also demonstrated less pronounced beta 2-mediated bronchoconstrictor effects than atenolol in asthmatics, and less general fatigue and leg fatigue in healthy subjects. Metoprolol OROS produced less pronounced bronchoconstrictor effects than atenolol, matrix-based sustained release metoprolol or long acting propranolol in patients with asthma or obstructive airways disease, and healthy volunteers. These results are presumably due to the beta 1-selectivity of metoprolol in addition to the relatively low plasma concentrations maintained by metoprolol CR/ZOK and metoprolol OROS, and the avoidance of high peak plasma concentrations with these agents. Despite the relative safety of the controlled release forms of metoprolol, the use of all beta-adrenoceptor antagonists should be avoided in patients with a history of bronchospasm. Thus, controlled release metoprolol formulations offer the potential to maximise the confirmed benefits of this agent in the management of hypertension and angina, by maintaining clinically effective plasma concentrations within a narrow therapeutic range over a 24-hour dose interval.
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PMID:Controlled release metoprolol formulations. A review of their pharmacodynamic and pharmacokinetic properties, and therapeutic use in hypertension and ischaemic heart disease. 137 20

In a 16 weeks open label therapeutic trial, studies were performed on isradipine (Lomir) to evaluate its haematological and biochemical safety and hypotensive capacity in the management of adult black hypertensive patients. The mean sitting diastolic blood pressure decreased from 105.5 +/- 9.66 mm hg at the end of the washout period to 92.1 +/- 7.59 mm hg at the end of the study, p less than 0.0001; while the mean standing diastolic blood pressure was 108.0 +/- 7.10 mm hg and 93.9 +/- 8.4 mm hg at the end of the washout phase and at the completion of the therapy respectively, p less than 0.0001. The corresponding mean sitting systolic blood pressures were 155.4 +/- 9.91 mm hg and 140.6 +/- 9.47 mm hg, p less than 0.001 while the corresponding mean standing systolic blood pressures were 156.6 +/- 12.50 mm hg and 142.6 +/- 9.15 mm hg, p less than 0.001. There were negligible changes in the mean heart rate; from 79.5 +/- 9.23 beats per minute (bpm) at the end of the placebo phase to 78.2 +/- 9.15 bpm at the end of the study in the sitting position, p greater than 0.1. The corresponding mean standing values of heart rate were 82.5 +/- 11.33 and 78.6 +/- 8.76, p greater than 0.5. The haematological, biochemical and electrocardiographic parameters remained within normal limits during the study. Side effects were mild, transitory, improved with therapy and consisted of dizziness, palpitations, headache, nocturia, tiredness and fainting attacks. The study achieved 96% good-to-excellent results with respect to both efficacy and tolerability. Isradipine (Lomir) is therefore an efficacious and safe antihypertensive agent in the management of black adult patients with mild to moderate primary arterial hypertension when administered in the dose of upto 2.5 mg twice daily alone or in combination with a beta-blocker.
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PMID:Clinical studies on isradipine in the management of adult hypertensive patients at Moi University Teaching Hospital, Eldoret, Kenya. 138 77

Two-hundred and fifty patients undergoing initial exploration for primary hyperparathyroidism were analyzed for differences in clinical presentation, biochemical status, pathology, and outcome of surgery. In patients less than 60 years of age (younger patients, n = 119) the most common preoperative symptoms and signs were fatigue (40.3%), bone pain (33.6%), renal stones (31.0%), hypertension (27.7%), and psychiatric illness (27.7%). In patients greater than or equal to 60 years of age (older patients, n = 131) the most frequent symptoms and signs were hypertension (46.6%), fatigue (35.1%), bone pain (30.5%), muscle weakness (28.2%), and joint pain (22.9%). Renal stones were 2.6 times more common (p less than 0.001, chi 2) in younger patients and hypertension 1.7 times more common (p less than 0.05, chi 2) in older patients. There was no significant difference in the preoperative and postoperative laboratory values typically associated with primary hyperparathyroidism. Double adenomas were more common in older (9.2%) than in younger patients (2.5%, p less than 0.05, chi 2). Surgical cure was obtained in 98.8% of patients, and after parathyroidectomy 83% of the younger and 82% of the older patients experienced substantial relief of pre-operative symptoms. Specific questioning revealed most patients to be symptomatic and older patients appear to receive the same clinical and metabolic benefits from parathyroidectomy as younger patients.
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PMID:Primary hyperparathyroidism in younger and older patients: symptoms and outcome of surgery. 141 50

The calcium antagonist, diltiazem is effective in the treatment of patients with various types of angina pectoris, as well as with essential and renovascular arterial hypertension. Sustained-release diltiazem in dose of 180 mg once daily is effective as sustained-release diltiazem in dose of 90 mg twice daily. Besides, in patients with stable angina pectoris and essential arterial hypertension the monotherapy with sustained-release diltiazem in dose of 180 mg is similarly effective as beta blockers and thiazide diuretics. However, monotherapy with sustained-release diltiazem is at least effective as monotherapy with sustained-release verapamil. Comparative clinical investigations showed that diltiazem is more effective than propranolol in decreasing ischemic attacks, whereas the risk of bradycardia is smaller. On the other hand, nifedipine (dihydropyridine calcium antagonist) is more effective than diltiazem in lowering ischemic electrocardiographic changes, incidence of attacks and improving working capability. The efficacy of diltiazem, nifedipine and verapamil is similar in the treatment of patients with spastic angina pectoris, whereas the least effective is propranolol. As far as the arterial hypertension is concerned, clinical investigations showed that the efficacy of diltiazem and nifedipine is similar. Side effects are relatively rare (1.8-9.6% patients) and depend on the dose (nausea, fatigue, dizziness, headache and itching).
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PMID:[Pharmacology--new therapy. Calcium channel blockers: new aspects of therapeutic use of diltiazem]. 146 75

Clentiazem, 8-chloro diltiazem, is a calcium channel blocker currently undergoing evaluation for the treatment of stable angina and hypertension. As patients with ischaemic disorders often present some degree of heart failure, the aim of this study was to investigate the effect of congestive heart failure on clentiazem (200 micrograms kg-1, i.v. bolus) pharmacokinetics in a canine model. Congestive heart failure was induced in six dogs by rapid ventricular pacing (240 beats min-1) for 3-5 weeks. Clentiazem pharmacokinetics was studied in each dog under the control condition and after the development of clinical signs of heart failure (ascites, dyspnea, fatigue). Blood samples were collected up to 480 min post-dose. Clentiazem plasma concentrations were determined by high performance liquid chromatography. The area under the plasma concentration versus time curves (AUC0-infinity) was significantly increased in congestive heart failure dogs (8.8 +/- 1.6 vs 21.8 +/- 1.4 micrograms min ml-1) (mean +/- SEM). These changes were related to a reduction of the volume of distribution of the central compartment (0.9 +/- 0.1 vs 0.2 +/- 0.11 kg-1) and total body clearance (1.9 +/- 0.4 vs 0.7 +/- 0.21 h-1 kg-1). It is concluded that, in our model, congestive heart failure significantly modifies clentiazem disposition. These results suggest that caution should be exercised when clentiazem is given to patients with a low ejection fraction and a compromised cardiac function. Reduced loading and maintenance doses might be recommended in patients with severe congestive heart failure.
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PMID:Effect of congestive heart failure on clentiazem pharmacokinetics in a dog model. 148 42

This report describes a case of epinephrine predominant pheochromocytoma successfully managed intraoperatively with an infusion of diltiazem. A 50-yr-old woman with a 10-yr history of diabetes mellitus was admitted to the hospital because of thirst and general fatigue. A cystic left adrenal tumor was found on computed tomographic scan. Although resting plasma catecholamine levels were normal, plasma norepinephrine and epinephrine levels obtained from the left adrenal vein were 1.6 ng.ml-1 (normal, 0.04-0.35) and 6.2 ng.ml-1 (normal, less than 0.12), respectively. Diltiazem was administered i. v. at a rate of 3 micrograms.kg-1.min-1 before induction of anesthesia. Anesthesia was induced with enflurane 2-3% and nitrous oxide in oxygen, followed by tracheal intubation facilitated with vecuronium. Anesthesia was maintained with enflurane 1-3% and nitrous oxide in oxygen. Paralysis was maintained with vecuronium. Hypertension during the manipulation of the tumor was controlled by increasing the inspired concentration of enflurane or by increasing the infusion rate of diltiazem to 5 micrograms.kg-1.min-1. There was no tachyarrhythmia. The infusion of diltiazem was continued until the draining vein from the tumor had been ligated. Hypotension, after removal of the tumor, was treated by the rapid infusion of fluid. Plasma norepinephrine and epinephrine levels during tumor manipulation were 1.18 ng.ml-1 and 6.57 ng.ml-1, respectively.
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PMID:[Use of diltiazem in the anesthetic management of epinephrine predominant pheochromocytoma]. 149 89

The negative effects of noise on sleep and behaviour have been related to three mechanisms: a physiological arousal (above a certain threshold of noise), an aversive reaction and an interference with non auditive neurophysiological and mental processes. The perturbation of verbal communication and the effects of sleep are the directly observable consequences. The negative effects of noise above a certain threshold on sleep have been demonstrated both in experimental conditions and in real life. They concern length, EEG pattern, and subjective quality and produce an increase of irritability and tiredness. There is no habituation. In all populations studied, strong discomfort is expressed by 50% of the subjects living in an area with an Ldn of 75 dB in the case of air traffic noise, the same results being obtained with ground traffic for a 5-15 dB higher level. Objective expressions of discomfort: use of aural protections, closing the windows, staying indoor, changing residence, increase linearly with the intensity of noise. Noise influences the incidence of stress-related disorders: hypertension, related cardio-vascular diseases, psychosomatic and psychological disorders. It has been shown by the use of different techniques (epidemiological studies based on the frequency of medical contacts, on the diagnoses made by general practitioners, on the use of specific drugs, and on the examination of the whole population) that the prevalence increases in relation with the level of noise in the vicinity of airports.(ABSTRACT TRUNCATED AT 250 WORDS)
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PMID:[Noise, sleep and behavior]. 150 64

Cilazapril is a new once-daily angiotensin-converting (ACE) enzyme inhibitor which has been administered to 4,500 patients with mainly mild to moderate essential hypertension in a multinational clinical research program. Sitting diastolic blood pressure was reduced by about 9 mm Hg from baseline (p less than 0.01) after 4 weeks of treatment with cilazapril 1.25-10 mg/day in double-blind placebo-controlled studies. Total responder rates to cilazapril were usually 50-60% compared with 30% to placebo. Adding hydrochlorothiazide 12.5 mg/day to cilazapril 5.0 mg/day increased the total responder rate from 52 to 71%. Double-blind dose titration studies for 8 weeks showed that cilazapril 2.5-5 mg/day possessed equivalent efficacy to usual therapeutic regimens of sustained release propranolol, captopril, hydrochlorothiazide, atenolol and enalapril, Cilazapril did not affect heart rate. During long-term open administration for 52 weeks, or longer, cilazapril, either alone or in combination with hydrochlorothiazide, effectively maintained control of blood pressure. Treatment of patients with severe hypertension with cilazapril plus hydrochlorothiazide achieved a total responder rate of 73%. Adverse events were mostly observed within the first 8-16 weeks of treatment, with headache, dizziness, fatigue, nausea, cough and chest pain being the most frequent. Non-life-threatening angioedema, facial edema and mild hypotension occurred in less than or equal to 0.2% of patients, and orthostatic hypotension was reported in 2%. Abnormal laboratory test values were rarely found with cilazapril treatment. Of the 2.3% of patients with elevated serum creatinine, at any time point during the study and irrespective of outcome on continuation with cilazapril therapy, about two thirds had prior renal impairment.(ABSTRACT TRUNCATED AT 250 WORDS)
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PMID:Cilazapril: an overview of its efficacy and safety in hypertension. 153 34

We compared the safety of a new dihydropyridine calcium entry blocker, isradipine, with an equipotent dose of diltiazem in 174 mild hypertensives (diastolic blood pressure [DBP] 95 to 105 mm Hg). After appropriate washout and placebo periods, patients were randomly assigned to receive either 1.25 mg isradipine twice daily (Group I) or 40 mg diltiazem thrice daily (Group D). If DBP remained above 90 mm Hg, doses were increased to a maximum of 5 mg isradipine twice daily or 120 mg diltiazem thrice daily. Active therapy was given for a total of 12 weeks. Only 18 patients (nine from each group) did not complete the protocol. The patients were well-matched at baseline with a mean BP of 149/100 mm Hg for those who were randomized to isradipine and completed the protocol and 153/99 mm Hg for the diltiazem group. The responses to each drug were excellent with 72% of the isradipine patients and 73% of the diltiazem group having DBP less than 90 mm Hg at the completion of the study. Of the 156 patients who completed the protocol, only 18 patients (ten in Group I and eight in Group D) failed to respond. Both drugs were well-tolerated. No adverse reactions were reported by 68 percent of the patients in Group I and 65% of those in Group D. The most common side effect was headache (9.0% in Group I and 7.8% in Group D) followed by fatigue (5.2% in Group I and 3.9% in Group D). Age and race did not predict response to either agent but men responded slightly better to diltiazem than women. We conclude that isradipine and diltiazem are equally well tolerated and can be used successfully as a monotherapy to treat hypertension in a wide variety of patients.
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PMID:A comparison of the safety of therapeutically equivalent doses of isradipine and diltiazem for treatment of essential hypertension. 153 28


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