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Query: UMLS:C0085580 (essential hypertension)
 14,686 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

The antihypertensive effect of slow release nifedipine (CAS 21829-25-4) tablets (20 mg, Adalat) administered once or twice daily was studied in patients with essential hypertension of WHO stage I or II. Ambulatory blood pressure was monitored by a finger volume oscillometric device every 5 min for 24 h before and during the treatment with nifedipine. Whether administered once or twice daily, nifedipine tablets dit not change the pattern of circadian blood pressure variation; i.e. diurnal rise and nocturnal fall. Twice daily administration induced a significant downward shift in the blood pressure pattern. In other words, further hypotensive effect was observed during the night when the blood pressure was already low. On the other hand, administration once daily in the morning lowered daytime blood pressure without affecting blood pressure during the night. The duration of action of nifedipine tablets administered once daily was 12 h or more. In the acute experiment using 20 mg tablets of nifedipine, plasma concentration of nifedipine was well correlated with the percentage change in mean blood pressure. The minimal effective plasma concentration of nifedipine was estimated to be 13.4 ng/ml. However, in chronic treatment, nifedipine lowered blood pressure at the plasma concentration of 10 ng/ml. The results indicate that nifedipine tablets administered once daily provide an effective antihypertensive regimen for controlling daytime hypertension with minimal antihypertensive effect during the night.
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PMID:Effect of slow release nifedipine tablets in patients with essential hypertension. 128 7

Possible metabolic changes during chronic treatment is of specific importance for the development of antihypertensive drugs. The impact of a combination treatment with co-dergocrine mesilate/nifedipine (Pontuc; CAS 8067-24-1 resp. CAS 21829-25-4) on the lipid metabolism as well as hematological and biochemical values was evaluated in a group of hypertensive patients. HDL-cholesterol remained unchanged, whereas total cholesterol and LDL-cholesterol slightly decreased, apoprotein AI increased and apoprotein B decreased. In conclusion the results of this study indicate that co-dergocrine mesilate/nifedipine has no negative impact on the lipid metabolism in patients with essential hypertension.
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PMID:[Metabolic consequences of long-term antihypertensive treatment with co-dergocrine mesylate/nifedipine in high age groups]. 149 90

Clentiazem (TA-3090, CAS 96125-53-0), a new benzothiazepine Ca++ antagonist, was orally administered to inpatients with essential hypertension at a dose of 30 mg at 8:00 a.m. once (n = 5) or daily for 2 weeks (n = 22). After administration of the medication, the daily variations in blood pressure and pulse rate were monitored using a portable blood pressure recorder, and plasma concentrations of clentiazem were determined by HPLC. 1. In the single administration study, an antihypertensive effect was observed between 4 and 12 h with a peak approximately 8 h after administration. After the single dose, the diurnal pulse rate was higher than the pretreatment level, but it was not correlated with the antihypertensive effect. 2. In the repeated administration study, both the systolic and diastolic blood pressures showed significant decreases after administration throughout the day (p less than 0.01). The nocturnal antihypertensive effect was weaker than the diurnal effect, and the minimum decrease/maximum decrease ratio in a day was 0.52 for both systolic and diastolic pressures. The pulse rate decreased slightly during certain time intervals after administration (p less than 0.01 or p less than 0.05), but those were slight changes. 3. As to the pharmacokinetic profile clentiazem showed a long-lasting plasma level, the tmax was 6.8 +/- 1.1 h for the single treatment and 6.9 +/- 1.6 h for the repeated treatment; the Cmax was 16.9 +/- 6.1 ng/ml and 19.3 +/- 8.8 ng/ml, respectively; and the t1/2 was 6.6 +/- 1.5 h and 12.5 +/- 5.4 h, respectively. The plasma level profiles for single and repeated administrations were similar.(ABSTRACT TRUNCATED AT 250 WORDS)
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PMID:Analysis of the daily variation in blood pressure and pharmacokinetics after single or repeated administration of clentiazem to patients with essential hypertension. 164 78

Levcromakalim (BRL 38227, CAS 94535-50-9) is a new antihypertensive drug with vasodilator activity due to activation of potassium channels in vascular smooth muscle. In this study, we treated 14 patients with essential hypertension on an out-patient basis to investigate the antihypertensive effect of levcromakalim by 24-h blood pressure monitoring for a 12-weeks treatment period. Levcromakalim significantly lowered blood pressure for 24 h without affecting standard deviation, range of variation and pulse rate. When 24-h monitoring period was divided into daytime (6:00-22:00) and nighttime (22:30-5:30), there were no statistically significant differences in magnitude of fall in blood pressure at night between baseline and end of treatment values. Four patients (28.5%) reported 6 adverse events, including headache, facial hot flushes, oedema and floating feeling. All symptoms were mild or moderate. These data show that levcromakalim controls ambulatory blood pressure both in the daytime and nighttime without changing the circadian rhythm of blood pressure, and suggest that levcromakalim will be an efficacious and safe antihypertensive drug.
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PMID:Antihypertensive effect of levcromakalim in patients with essential hypertension. Study by 24-h ambulatory blood pressure monitoring. 757 47

In a randomised, placebo-controlled design 40 patients with moderately severe essential hypertension were treated with bunazosin (CAS 52712-76-2) retard in increasing doses ranging between 6 and 18 mg/day. In intervals of 14 days titration steps were made, the minimal period of treatment was 4 weeks. In 34 patients (80.6%) a blood pressure response could be achieved with Bunazosin retard alone, the rest of the patients needed the additional administration of 25 mg hydrochlorothiazide daily. In all actively treated patients diastolic blood pressure could be normalised (DBP < or = 90 mmHg). After 4 weeks the mean blood pressure was lowered in the Bunazosin group by 16.2 mmHg (diastolic) and 25 mmHg (systolic). The mean heart rate at rest remained almost constant. Bunazosin was generally well tolerated; only very few adverse events occurred, and no patient collapsed. Compared to placebo the orthostatic tolerance was not influenced by bunazosin retard. Only when changing from resting to standing position the rise in heart rate was slightly more pronounced under bunazosin. Also the physiological blood pressure profile under bunazosin remained unchanged during the orthostatic tests.
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PMID:[Treatment of essential hypertension with the alpha-1 antagonist bunazosin retard. A multicenter, double-blind, placebo-controlled study]. 790 71

Hypotensive and antihypertensive effects of S-312-d (S-(+)-methyl-4,7-dihydro-3-isobutyl-6-methyl-4-(3-nitrophenyl)thieno[2, 3- b]pyridine-5-carboxylate, CAS 120056-57-7) in Wistar Kyoto rat (WKY), spontaneously hypertensive rat (SHR), stroke-prone SHR (SHRSP), and DOCA-salt hypertensive rat (DOCA-HR) were compared with those of other representative calcium antagonists. The minimal effective hypotensive dose of S-312-d in WKY was 3 mg/kg p.o. and those in SHR, SHRSP, and DOCA-HR were 1 mg/kg p.o. in gum arabic suspension. The minimal antihypertensive dose of S-312-d in polyethylene glycol solution was 0.3 mg/kg p.o. in SHRSP. The antihypertensive effects of S-312-d was the most potent and long-lasting compared with the calcium antagonists, nifedipine, nicardipine, nimodipine, nilvadipine, and flunarizine. In conscious two-kidney Goldblatt-type hypertensive dogs, a significant antihypertensive effect and concomitant increases of heart rate with S-312-d at 1 mg/kg lasted for 4 to 6 h after oral administration. Determination of the plasma concentration of S-312-d by HPLC showed that more than 4.3 ng/ml of S-312-d is required for a significant antihypertensive effect. Subcutaneous administration of atenolol at 20 mg/kg 30 min before S-312-d significantly inhibited the tachycardia with S-312-d at 1 mg/kg p.o. but not its antihypertensive effect. S-312-d is considered useful for the treatment of essential hypertension and related organ disorders.
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PMID:Pharmacological studies on a new dihydrothienopyridine calcium antagonist. 3rd communication: antihypertensive effects of S-(+)-methyl-4,7-dihydro-3-isobutyl-6-methyl-4-(3-nitrophenyl)thieno[2, 3-b] pyridine-5-carboxylate in hypertensive rats and dogs. 814 15

The prophylactic and therapeutic effects of S-312-d (S-(+)-methyl-4,7-dihydro-3-isobutyl-6-methyl-4-(3-nitrophenyl)thieno[2, 3- b]pyridine-5-carboxylate, CAS 120056-57-7) were compared with those of nimodipine or nicardipine using male stroke-prone spontaneously hypertensive rats (SHRSP). The survival rate of SHRSP was dose-dependently increased by once a day oral administration of S-312-d (0.3, 1, and 3 mg/kg) or nimodipine (10 mg/kg), while all non-treated SHRSP fed with high Na+ diet died within 40 days after the start of the experiment. All SHRSP treated with 3 mg/kg S-312-d survived during the 60-day experiment periods. Marked decreases of body weights and various neurological symptoms were also inhibited with S-312-d or nimodipine. Moderate diuretic effects were observed with S-312-d at doses of 1 and 3 mg/kg. The appearance of urinary occult blood in control SHRSP was markedly inhibited with S-312-d at 1 mg/kg and nimodipine at 10 mg/kg. Histological examination of the brain of SHRSP showed that cerebral stroke lesion including edema, hemorrhage, and/or softening was dose-dependently inhibited with S-312-d. Once a day oral administration of S-312-d (1, 3, or 10 mg/kg) dose-dependently increased the body weights and improved the neurological symptoms of diseased SHRSP. The appearance of proteinuria and of occult blood in the urine of SHRSP were also markedly inhibited with S-312-d or nicardipine. Histological examination of the brain of SHRSP showed that the arbitrary neurotoxic index (ANI) for stroke lesion dose-dependently decreased with S-312-d at 1, 3, and 10 mg/kg as follows: 4.8, 3.0, 2.3. The ANI for non-treated SHRSP was 7.6. The therapeutic effects of nicardipine (ANI 3.9) at 10 mg/kg corresponded to those of S-312-d at 3 mg/kg. Thus, S-312-d can be recommended for the treatment of cerebral insufficiency or vasospasm following stroke as well as in essential hypertension.
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PMID:Pharmacological studies on a new dihydrothienopyridine calcium antagonist. 4th communication: prophylactic and therapeutic effects of S-(+)-methyl-4,7-dihydro-3-isobutyl-6-methyl-4-(3-nitrophenyl)thieno[2, 3- b]pyridine-5-carboxylate in stroke-prone spontaneously hypertensive rats. 814 16

The effects of isradipine (Lomir, CAS 75695-93-1) and metoprolol (CAS 37350-58-6) on geometry and arterial compliance of the arteria brachialis of 14 patients each with essential hypertension were compared acutely and after three months of therapy by means of pulsed Doppler sonography and the determination of pulse wave velocity. A calculation model was used that allowed to determine the drug-specific effects on arterial diameter and compliance under isobaric conditions. Isradipine increased measured and isobaric diameter during short-term (p < 0.05) and long-term administration (p < 0.05) whereas metoprolol did not change it. Isradipine increased measured and isobaric compliance during short-term (p < 0.05) and long-term administration (p < 0.05). Metoprolol reduced measured compliance acutely (p < 0.01) and isobaric compliance acutely (p < 0.05) and long-term (p < 0.05). Drug-specific effects on compliance were different during short-term and long-term administration (p < 0.01); the diameter was influenced differently only during short-term administration (p < 0.05). These opposite drug effects on the A. brachialis are probably due to a vasoselective relaxation of smooth muscle in large arteries by isradipine and-in the case of metoprolol-arterial constriction. The increase of arterial compliance by isradipine reduces very effectively the load on the heart and could form the basis for the improvement in the prognosis of the hypertensive patient.
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PMID:[Vasoselective, substance-specific actions of isradipine on the great arteries of hypertensives in comparison to metoprolol]. 819 95

In this multicenter, placebo-controlled study, 16 patients with mild to moderate essential hypertension were treated with 10 mg/day isradipine retard (PN 200-110, Lomir SRO, CAS 75695-93-1) for 3 weeks. The study started with a 2 week placebo wash out phase. 13 patients were randomised to an exclusive placebo therapy. After the placebo wash out phase, following the 1st medication in active therapy and after the end of therapy, 24-h blood pressure profiles were recorded. The profile under placebo on the 1st medication was separated by a one-week intervening placebo therapy for all patients. On active therapy, the systolic as well as the diastolic blood pressure (day time, night time and 24-h mean values) were significantly reduced. The antihypertensive effect of the active therapy became already manifest after the 1st medication and was augmented after 3 weeks of therapy. In the placebo group no parameter of the 24-h profiles changed significantly. The tolerability of treatment was excellent in 14 (87.5%) of the isradipine patients and in 10 (76.9%) of the placebo group. In one of 16 patients in the active group, adverse events (flush and ankle oedema) were observed. However, therapy could be continued. In one patient of the placebo group, oedema of the fingers was noticed, in another headache was documented. In the placebo group two patients discontinued the study due to inefficacy, in the isradipine group one patient for the same reason; a second patient was excluded from this group due to a concomitant disease unrelated to the study drug.
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PMID:[Circadian antihypertensive effect of sustained-release isradipine in patients with essential hypertension in comparison to placebo]. 824 Apr 58

MPC-1304 ((+-)-methyl 2-oxopropyl 1,4-dihydro 2,6-dimethyl-4-(2-nitrophenyl)-3,5-pyridinedicarboxylate, CAS 86780-90-7), a new calcium antagonist, was orally administered to 10 outpatients with mild essential hypertension. It was observed that MPC-1304 inhibited elevations of blood pressure both at rest and under exercise loading without any adverse hemodynamic effects. The findings obtained indicated that MPC-1304 would be clinically useful in the treatment of hypertensive patients undergoing therapy while continuing normal everyday activities including physical exertion.
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PMID:Effect of a new calcium antagonist on hemodynamics at rest and exercise loading in patients with essential hypertension. 829 57


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