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

Isradipine (Lomir) a new dihydropyridine calcium antagonist was evaluated for its efficacy, tolerability and safety among mild to moderate Tanzanian hypertensives. Twenty nine patients (7 males and 22 females), mean age 42.7 +/- 8.5 years entered active treatment phase, of the 16 week open label therapeutic trial. A mean decrease from base line in supine systolic blood pressure (SBP) of 17.6 mmHg (p < 0.001) and diastolic blood pressure (DBP) of 13.5 mmHg (p < 0.001) were achieved at the end of the study period. The corresponding changes from base line in standing SBP and DBP were 18 mmHg (p < 0.001) and 13.5 mmHg (p < 0.001) respectively. The efficacy was excellent or good in 84% and fair or none in 16% of the study patients. The tolerability of the drugs was excellent or good in 88.8% of patients, fair in 7.4% and bad in 3.8%. The mild side effects included headache, palpitations, tiredness and nocturia. But these improved with continued treatment. Isradipine (Lomir) at a dose of 1.25mg to 2.5mg twice daily is effective, safe and tolerable in mild to moderate hypertension.
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PMID:Efficacy, tolerability and safety of isradipine (Lomir) in the treatment of mild to moderate Tanzanian hypertensives. 129 33

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

The antihypertensive efficacy and tolerability of the new calcium antagonist isradipine was assessed in 86 hypertensive patients who had pretreatment diastolic blood pressures (DBP) greater than or equal to 105 mm Hg and who were randomly allocated to a double-blind comparison of three different dosage regimens: 1.25 mg, 2.5 mg, and 5 mg b.i.d., and placebo. A 2-week run-in period was followed by a 4-week course of treatment. Isradipine reduced systolic and diastolic blood pressures dose-dependently; the normalization rate (DBP less than or equal to 90 mm Hg) was 5% with placebo and 29, 55, and 64% with isradipine 1.25, 2.5, and 5 mg b.i.d., respectively. The proportion of patients experiencing at least a 10 mm Hg reduction in sitting DBP was 29, 67, 86, and 91%, respectively. All three dosages proved to be significantly effective compared to placebo. Neither heart rate nor blood pressure regulation in orthostasis were influenced. The main side effects were headache, dizziness, and flushing; isradipine 1.25 and 2.5 mg b.i.d. were well tolerated (not significantly different from placebo). In conclusion, isradipine 2.5 mg b.i.d. appears to be the potential dose of first choice, exhibiting a favorable benefit-risk profile.
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PMID:Efficacy and tolerability of the new calcium antagonist isradipine in essential hypertension. 169 4

This multicenter trial compared the efficacy and safety of isradipine and enalapril in 160 patients with essential hypertension. Patients received isradipine or enalapril for 10 weeks after a placebo wash-out period of three to five weeks. Dosage was titrated for six weeks on the basis of blood pressure (BP) response and was then maintained for the remainder of the study. Isradipine reduced systolic and diastolic BP by 12 and 9 mm Hg, respectively, and enalapril by 10 and 7 mm Hg, respectively (between-treatment difference P less than .05 for diastolic BP). Overall, isradipine resulted in a higher responder rate, particularly among patients who had higher entry BPs. Fifteen enalapril-treated patients and four isradipine-treated patients discontinued treatment (four taking enalapril and none taking isradipine withdrew because of lack of efficacy). The most frequently reported adverse reactions were headache, dizziness, and edema in the isradipine group, and cough, headache, and chest pain in the enalapril group. Both drugs produced significant reductions in BP, but, in this study isradipine was more effective. The drugs were similarly well tolerated.
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PMID:A multicenter comparison of the safety and efficacy of isradipine and enalapril in the treatment of hypertension. 182 8

Isradipine is a new dihydropyridine calcium antagonist with a high degree of selectivity for the coronary, cerebral, and skeletal muscle vasculature. The drug has minimal depressant activity on sinoatrial node automaticity and negligible negative chronotropic, dromotropic, and inotropic actions. Isradipine reduces blood pressure and systemic vascular resistance without changes in cardiac output and stroke volume. Renal blood flow is maintained while renal vascular resistance is reduced; this is accompanied by both short- and long-term diuretic and natriuretic effects. Doses of 1.25 to 5 mg twice daily lowers blood pressure effectively over 24 h. In open as well as placebo-controlled trials, 2.5 to 10 mg isradipine twice daily was safe and well tolerated, and reduced systolic and diastolic values in up to 85% of patients with mild-to-moderate hypertension. Efficacy is similar to those of nifedipine and nitrendipine, and potentially superior to those of propranolol, atenolol, prazosin, hydrochlorothiazide, and diltiazem. The drug can be safely combined with beta-blockers, angiotensin-converting enzyme (ACE) inhibitors, and diuretics. Adverse effects are dose-dependent and secondary to arterial vasodilatation, such as headache, flushing, ankle edema, dizziness, palpitations, and tachycardia. At the recommended dose of 2.5 mg twice daily, the total incidence of side effects does not differ from that with placebo. The antiatherosclerotic, antitrophic, and cerebroprotective effects seen in experimental animal models are promising for the drug in the treatment of human hypertension. Isradipine may not only reduce blood pressure, but may also reduce the risk for the consequences of this peril, namely, cerebral stroke and myocardial infarction.
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PMID:The place of isradipine in the treatment of hypertension. 182 26

The effects of isradipine (a new calcium antagonist of the dihydropyridine type) on maternal blood pressure and heart rate, fetal heart rate, and uterine activity in labour were measured. Uterine activity was recorded by an intrauterine microtip transducer catheter connected to a fetal monitor. Isradipine was given as a slow injection in doses of 0.5 mg (10 women), 1 mg (11 women), and 1.5 mg (6 women). A reduction of systolic (6-16%) and diastolic (19-22%) blood pressure was seen, and concomitantly there was an increase in maternal (29-34%) and fetal (3-10%) heart rates. Reduction in uterine activity was not dose-related (maximum reduction 17%). Side effects (headache, palpitations) were minor and well tolerated. One women in the high-dose group had a shortlasting episode of hypotension. The results suggest that isradipine given as a bolus dose decreases blood pressure in pregnant women with little effects on uterine activity and fetal heart rate.
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PMID:Effects of isradipine, a new calcium antagonist, on maternal cardiovascular system and uterine activity in labour. 214 69

Isradipine is a dihydropyridine calcium-entry blocking agent with pronounced vasodilator activity and no significant cardiac effects at clinical doses, a desirable profile for an antihypertensive drug. Prazosin, a post-junctional alpha-adrenoceptor blocking agent, may produce a similar hemodynamic pattern. Therefore, we compared the effects of isradipine (2.5-10 mg bid) with those of prazosin (2-8 mg bid) in 83 patients with established essential hypertension, using a randomized, double-blind, parallel-group design. Patients received a placebo for 3-5 weeks, then either isradipine or prazosin over a 6-week titration period, followed by a 4-week plateau phase. During the plateau period, isradipine therapy lowered sitting blood pressure more effectively than did the administration of prazosin: Mean systolic BP fell 16.7 versus 8.1 mmHg (p less than 0.001) and mean diastolic BP was reduced 15.6 versus 12.6 mmHg (p less than 0.01). In the dosing range used (while also noting that prazosin is occasionally titrated up to doses of 30 mg qd), 83% of isradipine-treated patients had at least a 10 mmHg reduction in diastolic BP, compared with 64% of prazosin-treated patients (p = 0.05, FET). Tachyphylaxis did not occur with either drug. The rate of occurrence of side effects was similar in both treatment groups; the most common adverse event seen with isradipine was headache (20%) and with prazosin, dizziness (19%).
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PMID:A multicenter comparison of isradipine and prazosin for treatment of essential hypertension. 214 12

The calcium antagonists of the dihydropyridine group, isradipine and nifedipine, were compared in 64 patients with mild to moderate hypertension (diastolic blood pressure 95 to 110mm Hg). A 2-week placebo run-in phase was followed by a double-blind crossover trial comprising two 3-week treatment periods with either calcium antagonist. The (fixed) dosages were isradipine 2.5mg twice daily and nifedipine retard 20mg twice daily. Blood pressure (systolic/diastolic) at baseline was 155/101mm Hg and decreased significantly by 14%/15% on isradipine and by 11%/12% on nifedipine (difference between treatments not significant). The drugs differed significantly with regard to incidence of adverse effects (mostly flushing and headache); the total rates were 16% on isradipine and 36% on nifedipine. At the end of the trial, patients were asked which drug or treatment phase they preferred. Isradipine was preferred by 50% of patients; only 20% preferred nifedipine. Thus, it is concluded that isradipine, administered in an equally effective antihypertensive dosage regimen is superior to nifedipine with regard to the incidence of adverse effects, resulting in greater patient satisfaction with treatment.
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PMID:The calcium antagonist isradipine in the therapy of hypertension. A double-blind crossover comparison with nifedipine. 215 Jun 44

Six hundred outpatients aged between 22 and 84 years with essential hypertension (diastolic blood pressure of at least 95 mm Hg) entered a multinational, multicenter, single-blind trial with dose titration to assess the safety, tolerability, and efficacy of isradipine in doses of 1.25, 2.5, and 5.0 mg twice daily over 12 weeks, following a two-week placebo run-in period. Isradipine alone was taken by 321 patients, the remainder receiving, in addition, other antihypertensive drugs. In valid patients receiving monotherapy, the mean final isradipine dose was 3.4 mg (median, 2.5 mg) twice daily, which normalized supine diastolic blood pressure in 85 percent and 64 percent of patients two to four hours and 10 to 14 hours post-dose, respectively. Overall, 242 patients (40 percent) reported adverse events, 39 (7 percent) of whom withdrew from the study for this reason. The most common side effects were flushing (11 percent), headache (10 percent), and localized edema (4 percent). None of the pathologic changes in hematologic or biochemical values was attributable to isradipine. It is concluded that a slow titration of isradipine by increments at three-week intervals results in an effective and well-tolerated treatment for essential hypertension, both in mono- and combination therapy.
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PMID:A multicenter evaluation of the safety, tolerability, and efficacy of isradipine in the treatment of essential hypertension. 252 65

The author presents a review of the chemically heterogeneous group of calcium antagonists, focused on their pharmacodynamic properties. He includes in the older generation of calcium antagonists drugs like verapamil, dihydropyridines (nifedipine) and dilthiazem (Diacordin, Blocalcin). The newer generation of dihydropyridines comprises substances with a higher vascular selectivity at a concentration of lower order. The latter include felodipine (Plendil), isradipine (Lomir) and nitrendipine (Baypress). The third generation includes drugs like amlodipine (Norvasc) and lacidipine. The slow onset of action of amlodipine is associated with a decline of undesirable side effects, such as flush, tachycardia, headache, oedema of the ankles. An advantage is also the prolonged effect when a single dose per day is administered.
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PMID:[Pharmacokinetics and pharmacodynamics of calcium channel blockers]. 776 70


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