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 56,091 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Urapidil is a postsynaptic alpha 1-adrenoceptor antagonist with a pharmacodynamic profile similar to prazosin. Unlike prazosin, however, urapidil also has some central activity which may explain the apparent improved tolerability of urapidil, including the absence of first-dose syncope. In clinical trials urapidil therapy resulted in significant reductions in blood pressure in patients with mild to severe essential hypertension, with little influence on heart rate. It is an effective antihypertensive when administered as monotherapy or in combination with beta-blockers and thiazide diuretics. In the few patients with cardiac dysfunction who have been studied to date, urapidil has improved myocardial oxygen consumption, systemic vascular resistance, left ventricular function, cardiac output and pulmonary capillary wedge pressure; however, further study is needed to assess the full therapeutic potential of urapidil in these patients. Urapidil has also been used successfully in the treatment of hypertensive emergencies, including eclampsia and pre-eclampsia, hypertensive crisis and hypertension occurring during general and cardiac surgery, rapidly lowering blood pressure without altering heart rate. Urapidil does not affect lipid or glucose metabolism, nor does it impair renal function. In addition, urapidil may be beneficial to patients with pulmonary hypertension, in whom it dilates pulmonary vascular beds to a greater extent than systemic vasculature, although therapeutic trials have not examined this effect. The most common adverse effects associated with urapidil therapy are dizziness, nausea, headache, fatigue and palpitations; however, these tend to be mild and transient and usually do not require discontinuation of treatment. Thus, urapidil offers a useful alternative to currently available drugs for the treatment of mild to severe hypertension, either as monotherapy or in combination with other antihypertensive drugs.
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PMID:Urapidil. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic potential in the treatment of hypertension. 269 46

Electronic data collection was used in this open study to survey the safety and efficacy of nifedipine when used in the treatment of 3972 patients with mild to moderate essential hypertension. The safety and efficacy results are presented and discussed as well as the advantages, disadvantages and reliability of electronic data collection. The validity of data collected electronically has not previously been tested, such data having been assumed to be reliable. The pattern of adverse events reported in this study is compared with the pattern of reports to the Committee on Safety of Medicine (CSM), to Bayer UK and in a large paper-based study of nifedipine, in order to test these assumptions. Reported adverse medical events pre-treatment, prior to entry to the study and noted at visit 1, were compared with reports during treatment in the study at visits 2 and 3. The expected incidence of flushing and headache was seen which diminished with continued treatment. Reductions were seen in dyspnoea and impotence. Ankle oedema was observed and was not reduced by time alone. After one month of treatment with nifedipine 20 mg tablets twice daily, 66.5% of patients had a sitting phase V diastolic blood pressure of 90 mmHg or below and 79% of 95 mmHg or below.
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PMID:Safety and efficacy of nifedipine 20 mg tablets in hypertension using electronic data collection in general practice. 275 81

The effectiveness of enalapril 10-40 mg/day as first choice treatment of mild (90-104 mmHg, n = 37), moderate (105-114 mmHg, n = 21), or severe (115-130 mmHg excluding accelerated hypertension, n = 16) essential hypertension was studied in an open multicentre trial. Enalapril alone controlled the hypertension (diastolic blood pressure 90 mmHg or less) in 25 patients (34%). Of these, 20 had mild and 5 had moderate hypertension. The remaining patients required either enalapril plus hydrochlorothiazide 12.5 or 25 mg/day (n = 30), or a third drug of the physician's choice (n = 9). A relationship was present between baseline blood pressure and the number of drugs required to achieve blood pressure control. Plasma creatinine increased beyond the limits of laboratory error in 3 patients, and from 100-108 mumol/l (p less than 0.05) on enalapril alone in a subgroup of patients who ultimately required a diuretic. Enalapril was well tolerated; 60 (73%) had no drug related side effects during active treatment. Tiredness (n = 5), headache (n = 4), dizziness (n = 4) and palpitations (n = 3) were the most frequent side effects. Cough was a feature in 3 patients and 1 patient had a rash. This study suggests that enalapril is an effective and well tolerated anti-hypertensive agent in mild, moderate or severe hypertension, but that caution may be required in patients with impaired renal function.
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PMID:Enalapril as first choice treatment of mild, moderate and severe essential hypertension: results of an open multicentre clinical trial. New Zealand Hypertension Study Group. 283 97

Multiclinic controlled studies have shown that enalapril alone 10 to 40 mg/day orally is effective in lowering blood pressure in patients with essential hypertension. Enalapril has been compared with thiazides and beta-blockers (propranolol, metoprolol and atenolol). The effect on systolic blood pressure has been greater with enalapril than with beta-blockers. The proportion of patients who respond to enalapril alone with a decrease in diastolic blood pressure (greater than or equal to 10mm Hg) is around 70%. When a thiazide is added to the treatment, the proportion is above 90%. Enalapril improves the signs and symptoms associated with congestive heart failure. Patients increased their exercise tolerance by an average of 148 sec and improved in their NYHA cardiac status and prognosis classification. The overall incidence of side effects is similar to that seen in the placebo control groups. Side effects such as agranulocytosis, taste loss, rash, proteinuria were not characteristic of enalapril. This supports the hypothesis that the improved safety profile of enalapril is the result of being a nonsulphydryl angiotensin-converting enzyme (ACE) inhibitor. The most common side effects reported were dizziness, headache and asthenia. Abnormalities in electrolytes, uric acid, glucose or in lipids have generally not been associated with enalapril.
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PMID:Enalapril in hypertension and congestive heart failure. Overall review of efficacy and safety. 286 29

The safety of terazosin, an effective agent for the treatment of hypertension, was assessed by analyzing data from 1,006 hypertensive patients who were enrolled in short-term and/or long-term studies. The total experience with terazosin in this article represents 422.5 patient-years. Changes in pulse rate measurements from pretreatment to posttreatment were not significantly different between the terazosin- and placebo-treated patients (-1.0 beat per minute for the terazosin group and -1.0 beat per minute for the placebo group, in the supine position). Dizziness, headache, and asthenia were the most commonly reported adverse experiences among all terazosin-treated patients, although the incidence of headache in placebo-controlled trials was not significantly different between the terazosin and placebo groups. As a whole, patients receiving terazosin had a tendency to gain small amounts of weight (2 pounds). In addition, there was a trend for slight decreases in hemoglobin, hematocrit, white blood cell count, total protein, and albumin levels in those patients who received terazosin, suggesting hemodilution. Overall, terazosin was shown to be safe in patients with mild to moderate essential hypertension.
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PMID:Overall safety of terazosin as an antihypertensive agent. 287 12

Terazosin is a post-synaptic alpha 1-adrenoceptor antagonist with a similar pharmacodynamic profile to prazosin. It differs from prazosin in having a longer duration of action, with an elimination half-life some 2 to 3 times that of prazosin, allowing the convenience of once daily administration. Moreover, its absorption from the gastrointestinal tract is more complete and predictable than that of prazosin which may facilitate dose titration. Terazosin therapy results in a significant reduction in blood pressure in patients with mild to moderate essential hypertension, with little influence on heart rate. The drug is an effective antihypertensive when administered as monotherapy or in combination with a range of antihypertensive agents including beta-blockers, diuretics and combinations of the two. In the few patients with congestive heart failure studied, terazosin produced an increase in cardiac output with a reduction in ventricular filling pressure and systemic vascular resistance, but no studies have been performed to assess the therapeutic potential of terazosin in this indication. Reductions in total plasma cholesterol and low density plus very low density lipoprotein cholesterol fractions have been reported after terazosin therapy, while high density lipoprotein cholesterol concentrations have tended to increase. Should such beneficial changes be confirmed in long term clinical studies they would suggest a therapeutic advantage of terazosin over some other antihypertensive drugs, particularly diuretics, which have been reported to adversely affect the plasma lipid profile. The most common side effects associated with terazosin treatment are dizziness, headache, asthenia and nasal congestion, but these are usually mild and do not require treatment discontinuation. Terazosin is normally administered once daily, starting at a dose of 1 mg/day and gradually titrating upwards as the blood pressure stabilises at each new dose, until blood pressure is adequately controlled or to a maximum dose of 20mg daily. First-dose syncope occurs rarely after terazosin, and can largely be avoided by giving the first dose at bedtime. Thus, terazosin offers a useful alternative to the drugs currently available for the management of mild to moderate essential hypertension either as monotherapy or in combination with other antihypertensive drugs.
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PMID:Terazosin. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic efficacy in essential hypertension. 288 69

A randomised double blind parallel group study was performed to compare the efficacy and acceptability of slow release nifedipine (maximum dose 40 mg twice a day) with those of atenolol (maximum dose 100 mg once a day) as single agents for the treatment of essential hypertension. Of 410 patients recruited almost exclusively from general practices in 22 centres in the United Kingdom 210 received nifedipine and 200 atenolol. Both drugs significantly reduced blood pressure, and control--a reduction of the diastolic pressure to less than 95 mm Hg--was obtained in about 65% of patients. Those who received nifedipine had more pronounced reductions in systolic pressure than those who received atenolol. One hundred and forty nine patients who failed to respond adequately to either atenolol or nifedipine in low doses were given both drugs once daily for eight weeks in a fixed combination capsule that contained atenolol 50 mg and nifedipine 20 mg. All patients showed further reductions in blood pressure, although those who were taking beta atenolol before the combination capsule had more pronounced reductions in systolic pressures. Twenty six patients (12%) were withdrawn because of adverse effects while taking nifedipine compared with 19 (10%) taking atenolol. Flushing and oedema were more common after the calcium antagonist, whereas diarrhoea and dyspepsia were more common after atenolol. The frequencies of headaches, dizziness, fatigue, and dyspnoea were equally distributed between the two groups. When the fixed combination capsule was taken side effects such as flushing and oedema continued. Nifedipine was more effective than atenolol in lowering systolic blood pressure, although neither drug used alone controlled the pressure of more than two thirds of the patients studied. When used in a fixed combination slightly better control of blood pressure was achieved with a lower dose of each drug.
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PMID:Nifedipine and atenolol singly and combined for treatment of essential hypertension: comparative multicentre study in general practice in the United Kingdom. Nifedipine-Atenolol Study Review Committee. 289 83

The long-term treatment of essential hypertension with terazosin, a new once-a-day alpha 1-adrenergic blocking agent, was evaluated in 364 hypertensive patients who received total daily doses of 1 to 40 mg for 3 weeks to 56 months. Consistent mean decreases in supine and standing systolic and diastolic blood pressures were observed throughout the study for patients treated with terazosin as monotherapy (supine, 9 to 12/10 to 13 mm Hg; and standing, 12 to 18/11 to 14 mm Hg) or in combination with other antihypertensive agents (supine, 12 to 16/12 to 15 mm Hg; and standing, 16 to 22/13 to 19 mm Hg). The most commonly reported adverse experiences were dizziness, headache, asthenia, cold symptoms, and nasal congestion. Adverse effects and metabolic disorders often associated with diuretics and beta blockers such as sexual dysfunction, hyperglycemia, hyperuricemia, hypokalemia, or adverse lipid effects were seen infrequently during long-term treatment with terazosin as monotherapy. Overall, terazosin was shown to be effective, safe, and well tolerated by most patients.
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PMID:Terazosin, a new selective alpha 1-adrenergic blocking agent. Results of long-term treatment in patients with essential hypertension. 290 Dec 67

The author found that the onset of hypertension or hypotension is relatively often associated with infections or development of so-called "sneezing due to allergy to pollen or dust," with or without headache, or due to trauma to the occipital area of the head. Using the "Bi-Digital O-ring Test," it was possible to demonstrate that, among bacterial and viral infections, the most common cause of infection associated with the appearance of hypertension is chlamydia, herpes simplex virus, cytomegalovirus, or Epstein-Barr virus. Particularly chlamydia and/or herpes simplex virus, with or without coexistence of other microbes, is usually present at the heart representation area of the medulla oblongata, especially at the left ventricular representation area, often accompanied by upper respiratory infection, cephalic, cervical or facial pain, with or without coexisting genito-urinary infection. The left ventricular representation area of the medulla oblongata is usually located at the right side. In most hypertensive patients, the left ventricular representation area of the medulla oblongata is enlarged up to 3 or 4 times normal size. Sufficient antibiotic treatment of chlamydia with erythromycin sometimes eliminated severe hypertension which appeared after chlamydia infection. In the presence of viral infections, such as herpes simplex, which is also causing severe pain in the head or neck, oral administration of acyclovir, erythromycin, or EPA (Eicosa Pentaenoic acid)-DHA (docosa hexaenoic acid) Omega 3 fish oil often reduced associated intractable pain and hypertension toward the normal level. Thus, the author is proposing new possible mechanisms as among the causes of so-called essential hypertension as a result of microbial infection or trauma of the cardiovascular representation area, particularly that of the left ventricular representation area at the right side of the medulla oblongata.
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PMID:Microbial infection or trauma at cardiovascular representation area of medulla oblongata as some of the possible causes of hypertension or hypotension. 290 10

Doxazosin is a new quinazoline derivative that, like prazosin, has selectivity for alpha 1-receptors. A three-way crossover, randomized, open study in 18 patients with essential hypertension was conducted to investigate the clinical pharmacokinetics of 2, 4, and 8 mg doxazosin at steady state. The pharmacokinetics of the initial 2 mg dose was also studied. Doxazosin showed linear pharmacokinetics. Increases in doses from 2 to 8 mg (steady state) produced proportional increases in doxazosin serum levels (maximum plasma drug concentration [Cmax] minimum plasma drug concentration [C min], and O-24-hour area under the curve [AUC(p-24)], whereas half-life (t1/2) (19.4, 18.7, and 19.7 hours, respectively), volume of distribution (3.4, 3.4, and 3.6 L/kg, respectively), clearance from serum (2.2, 2.2, and 2.1 ml/min/kg, respectively), and degree of protein binding (1.2%, 1.0%, and 1.0% unbound, respectively) were dose independent. Similar t1/2 and time to reach peak concentration (tmax) were obtained with 2 mg initial dose and 2 mg steady state. alpha 1-Acid glycoprotein levels were unchanged during doxazosin treatment. Doxazosin lowered supine and standing systolic and diastolic blood pressure. The blood pressure reduction was associated with an increase in heart rate. Peak hypotensive and tachycardic effects occurred 5.7 +/- 0.1 hours after administration, whereas Cmax was achieved at 2.4 +/- 0.7 hours (tmax). Greater decreases in systolic blood pressure and increases in heart rate were seen in standing than in supine position. The reduction in standing systolic and diastolic blood pressure with 8 mg was greater than with 2 mg (P less than 0.05); however, the increases in heart rate were not different. Dizziness, headaches, and dry mouth were the most frequent side effects. This study indicates that doxazosin shows linear pharmacokinetics between 2 and 8 mg and that because of its long t1/2, once-a-day administration should be adequate for the treatment of hypertension.
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PMID:Clinical pharmacology of doxazosin in patients with essential hypertension. 295 Oct 51


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