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Query: UMLS:C0016382 (flushing)
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A controlled multicentre trial was organised to compare the effects of 20 mg Nifedipine tablets (N) and 2,5 mg Indapamide tablets (I) during a 4 months' treatment period after a placebo period, in 59 patients with moderate essential hypertension (n = 59). The results of blood pressure measurements of 18 patients treated by nifedipine (1 tablet twice daily) and 22 patients treated by indapamide (1 tablet every morning) were compared. The systolic blood pressure, after 10 minutes recumbency, fell from 165 +/- 10 mmHg to 148 +/- 13 mmHg (p less than 0.01), and the diastolic pressure from 104 +/- 6 mmHg to 86 +/- 7 mmHg (p less than 0.01) in the patients treated with nifedipine. In the indapamide group, the SBP fell from 164 +/- 13 mmHg to 152 +/- 15 mmHg (p less than 0.01) and the DBP from 100 +/- 4 mmHg to 87 +/- 6 mmHg (p less than 0.01). There were no significant changes of heart rate with either drug; plasma creatinine, potassium and uric acid concentrations were also unchanged. There was a higher incidence of headaches and tiredness in the nifedipine group, whilst patients treated with indapamide complained more often of muscular cramps. Flushing was observed in nearly a quarter of the patients in both groups. These results confirm that both nifedipine and indapamide induce significant and persistant falls in systolic and diastolic blood pressure. Although the fall was greater with nifedipine than with indapamide, the difference was not statistically significant. The tolerance was satisfactory in both groups of patients.(ABSTRACT TRUNCATED AT 250 WORDS)
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PMID:[Comparative effects of nifedipine and indapamide in the treatment of arterial hypertension]. 393 9

The action of nifedipine tablets was examined in 17 patients with essential hypertension focusing particularly on the profile of blood pressure (BP) reduction over 24 hours resulting from both twice-daily and once-daily therapy (dose range 40 to 120 mg daily). This new formulation of nifedipine has a more prolonged and lower peak plasma level than an equivalent dose of nifedipine capsules. Our patients were fully ambulant and studied by continuous intraarterial recording techniques. BP responses during isometric and dynamic exercise testing were also observed. Within-patient comparisons of consecutive mean hourly systolic and diastolic BP showed a highly significant effect from twice-daily therapy (p less than 0.001) for nearly the entire day. Also, significantly lower BP was maintained during isometric and dynamic exercise. Mean hourly heart rates were not significantly altered. The profile of action of the single morning dose was initially similar, but its efficacy diminished from 6 P.M. to 8 A.M. on the following day. Side effects were not unduly troublesome and did not cause any patient withdrawals. Four patients developed mild ankle edema. Two others had facial flushing. Nifedipine given twice daily in tablet form, therefore, is an effective antihypertensive drug capable of lowering BP consistently over 24 hours in ambulant patients and during formal exercise testing. We suggest that this agent may be useful as initial therapy for systemic hypertension, although the tablets are not as yet widely available.
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PMID:Nifedipine tablets for systemic hypertension: a study using continuous ambulatory intraarterial recording. 684 59

Nifedipine kinetics have not been described in clinically relevant detail because of difficulties in formulating a stable preparation for intravenous use and lack of a specific and sensitive assay for plasma nifedipine. We recently developed a gas-chromatographic method and determined conditions in which nifedipine could be protected from photodegradation. Therefore, we evaluated the kinetics and bioavailability of nifedipine in 12 normal subjects after single intravenous (1 mg/5 min) and oral (10 mg) doses. After intravenous dosing, the drug was eliminated with a half-time of 1.77 +/- 0.25 hour, and total clearance was calculated at 0.62 +/- 0.09 liter/kg/hr. With oral drug administration, the elimination half-time was twice as long for the group; but within these subjects, marked variability in the rate of appearance of the drug in plasma was observed, giving profiles consistent with fast and slow absorption. In the latter group, peak plasma drug concentrations were only one third the level seen in those exhibiting a faster absorption profile, although the extent of drug absorption (as derived from areas under the plasma level-time curves) did not vary. Bioavailability was 0.45 +/- 0.08. Untoward effects resulting from the drug's pharmaco-subjects after intravenous administration (flushing).
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PMID:Nifedipine kinetics and bioavailability after single intravenous and oral doses in normal subjects. 686 80

The effect of nifedipine, one of calcium antagonists, was studied on esophageal function of 10 patients with achalasia. Lower esophageal sphincter pressure (LESP) was measured with constantly perfused catheter before and after sublingual administration of 10 mg nifedipine. Nifedipine decreased LESP both in achalasia patients and normal controls except one patient. The fall of LESP by nifedipine seems to correlate with initial resting LESP. A clinical trial of nifedipine on patients with achalasia was carried out taking nifedipine sublingually in a daily dosage of 30 to 60 mg before meal. Nifedipine therapy gave good results in 8 patients, and poor response in one and no effects in one patient. Nifedipine improved symptoms of achalasia, but did not improve the degree of esophageal dilatation. Side effect was observed in only one patient, which was flushing of extremities caused by vasodilation, and it is not hazardous to continue nifedipine therapy. Sublingual administration of nifedipine in patients with achalasia is very useful way of medical treatment in two respects, 1) nifedipine decreases LESP, and 2) sublingual administration does not need to pass through the drug through esophagogastric junction which pressure is abnormally high in achalasia patients.
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PMID:[Clinical effect of nifedipine in patients with achalasia]. 714 40

The calcium antagonist nifedipine (Adalat) was administered to 60 patients with essential hypertension and investigations were performed on acute and chronic hypotensive effects. The following results were obtained: 1. Acute hypotensive effects: Nifedipine (20 mg) was either orally or sublingually administered. Following oral administration, significant hypotensive effect was attained 20 min after administration and the maximum hypotensive response was obtained 2-4 h after administration. In cases of sublingual administration, significant hypotensive effect was notable 5 min after administration and blood pressure reached the lowest level 2-3 h after administration. The hypotensive effects lasted for a relatively longer period and significantly lower blood pressure than the control level was observed even 3 h after administration. 2. Chronic hypotensive effects: Nifedipine (30-60 mg/d) was orally administered consecutively. Significant hypotensive effect was attained in and after the 4th week of administration. The yearly changes in the long-term administration cases over 3 years demonstrated significant hypotensive effects. The cases who did not respond to single administration of thiazides or beta-blockers exhibited significant hypotensive response by the combined use of nifedipine. 3. Change in heart rate: In the acute study, heart rate increased after nifedipine administration and lasted for several hours. In the long-term administration cases, the changes in heart rate were not significant. 4. Side effects attributable to nifedipine such as headache in 2 cases, facial flushing, palpitation, warm sensation and nausea in 1 case each were observed early after the administration but there were no cases in whom administration was discontinued due to these side effects.
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PMID:Antihypertensive effects of the calcium antagonistic agent nifedipine. 720 Jul 85

In 102 cases of severe hypertension (DBP > or = 115 mm Hg), with or without acute complications, efficacy and safety of SL Nifedipine 10 mg (NIF), SL Captopril 25 mg (CAP), IV Metoprolol 15 mg (MET) and SL NIF + IV MET were studied in an inpatient trial. Maximum mean percent reduction in SBP was 13.3, 9.7, 15.7 and 19.9 and in DBP was 21.2, 13.9, 12.5 and 20.4 with NIF, CAP, MET and NIF + MET respectively. A safe DBP of < or = 110 mm Hg (Kaplan) was achieved in 90, 61, 72.2 and 95.2 percent of patients. A statistically significant fall in DBP was observed at 5 minutes with all regimens except CAP which was at 15 minutes. Mild side effects observed were palpitations and flushing (NIF n = 4), taste disturbances (CAP n = 3), heaviness of head (CAP n = 1) and giddiness (MET n = 2, NIF + MET n = 2). The trial data suggest that hypertensive crisis can be managed, without intensive care facility, with all four regimens; this implies significant cost containment.
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PMID:Nifedipine, captopril, metoprolol and nifedipine with metoprolol in hypertensive crisis in non-intensive care setting. 928 10

Effects of a new calcium antagonist, CD-832, on intracranial pressure (ICP), vertebral blood flow (VBF) and common carotid blood flow (CCBF) were investigated in dogs and the results were compared with findings for nifedipine and diltiaem. Dogs were anesthetized with sodium pentobarbital and a 20-gauge needle was inserted into the cisterna magna for ICP determination. Mean arterial blood pressure (MBP), heart rate (HR), CP, VBF and CCBF were measured before and during the continuous intravenous infusion of CD-832 (0.3, 1 and 3 microg/kg/min), nifedipine (0.1, 0.3 and 1 microg/kg/min) or diltiazem (1, 3 and 10 microg/kg/min). Although the three drugs caused a comparable hypotension, differences were evident in effects of these agents on ICP, VBF and CCBF. Nifedipine and diltiazem but not CD-832 significantly increased ICP, VBF and CCBF. These results suggest that CD-832 is a unique calcium antagonist which does not increase ICP during hypotension. Because the most evident side effects of calcium antagonists are caused by vasodilation and include headache and flushing, CD-832 may possibly be useful to treat subjects with hypertension or angina pectoris.
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PMID:Effects of CD-832, a new calcium antagonist, on intracranial pressure in anesthetized dogs. 958 14

The efficacy and acceptability of 5 mg nebivolol once daily, a long-acting, vasodilating cardioselective beta blocker that additionally facilitates the L-arginine/nitric oxide system, was assessed in a double-blind, randomized trial in comparison with 20 mg nifedipine retard twice daily in patients with essential hypertension. At 2 weeks of treatment, nebivolol was significantly more effective. Thereafter, both drugs effectively and similarly lowered systolic and diastolic pressures without orthostatic effect. Nebivolol had a trough-to-peak antihypertensive effect ratio of 90%. Nifedipine gave the expected side effects of headache, flushing, and edema. Nebivolol was well tolerated. Nebivolol slightly but significantly lowered heart rate. Neither drug adversely affected plasma levels of lipids.
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PMID:Nebivolol versus nifedipine in the treatment of essential hypertension: a double-blind, randomized, comparative trial. 1009 65

Ninety patients, 50 males and 40 females, and their ages ranged between 42 and 70 years, with severe hypertension were treated by either sublingual verapamil tablets 40 mg (30 patients) or 80 mg (30 patients) or sublingual nifedipine capsules 10 mg (30 patients). Blood pressure and heart rate were measured before and 15, 30, 60, 90 and 120 mins after administration of the drugs. - Results showed that sublingual verapamil 40 mg caused significant drop of blood pressure after 60 min (200 +/- 11.6 / 127 +/- 8.7 to 177 +/- 13.8 / 95.4 +/- 11.8, P <0.05) and in 10/30 patients blood pressure was less than 150/90 mmHg. Verapamil 40 mg decreased heart rate in 16 patients, elevated in 5 patients and unchanged heart rate in 9 patients. Verapamil 80 mg caused significant reduction of blood pressure after 30 min (201 +/- 16 / 129 +/- 7.5 to 182 +/- 13 / 105 +/- 10.7, P <0.05) and the blood pressure was dropped to less than 150/90 mmHg in 18/30 patients. Sublingual verapamil 80 mg caused significant decrease in heart rate in 21/30 patients and peak decrease was recorded at 90 min (92.6 +/- 7.2 beats/min to 82 +/- 9, P <0.05). It alleviated headache in 8 patients including 2 patients with migraine. Sublingual nifedipine caused significant drop of elevated blood pressure at each time intervals and the peak drop was at 60 min (from 199 +/- 13.8 / 126 +/- 13.2 to 142.8 +/- 15 / 80. 9 +/- 9, P <0.05). In 22/30 patients blood pressure dropped to less than 150/90 mmHg after 60 min. Nifedipine elevated heart rate in 22/30 patients and peak elevation was at 30 min (from 91.6 +/- 7.8 to 105.6 +/- 6.1 beats/min, P <0.05). It caused headache in 8 patients and flushing in other 2 patients. Therefore, as compared to sublingual verapamil, sublingual nifedipine caused rapid lowering of elevated blood pressure and elevation of heart rate in most of the patients treated. The differences in proportions of patients whom blood pressure was dropped to less than 150/90 mmHg between nifedipine group and verapamil 40 mg group and between verapamil 80 mg and verapamil 40 mg groups were significant (P <0.05). - It might be concluded that sublingual verapamil caused significant lowering of blood pressure in hypertensive patients, decreased heart rate in most of the treated patients and alleviated headache in symptomatic hypertensive patients.
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PMID:Efficacy of sublingual verapamil in patients with severe essential hypertension: comparison with sublingual nifedipine. 1033 9

Sublingual nifedipine is commonly used in hypertensive crisis, however, it may result in several adverse effects such as reflex tachycardia, headache, and flushing. Research is continuing to find a new drug that has the same efficiency and fewer side effects. Sublingual captopril, a new preparation of angiotensin-converting enzyme inhibitor, lowers blood pressure. It is not known whether it is effective in these emergent clinical settings. Therefore we designed a randomized, double-blind study to compare the efficacy and safety of those two drugs in hypertensive crisis. Eighty patients (32 male and 48 female) with hypertensive crisis were included in the study; their mean age was 43.4 +/- 7.9 years. Nifedipine 10 mg was given sublingually to 34 and captopril 25 mg to 46 patients randomly. There was no difference between the two drugs with respect to their antihypertensive effect. Heart rate significantly dropped (p < 0.01 and p < 0.001) in the patients taking captopril, but no changes were observed in the patients taking nifedipine. Twenty-three of 34 patients taking nifedipine encountered adverse effects. Adverse effects were observed in only three patients taking captopril (p < 0.001). Sublingual captopril is as effective as and has less side effects than sublingual nifedipine. Because sublingual captopril has fewer side effects, it may be safer than nifedipine in the treatment of hypertensive crisis.http://link.springer-ny.com/link/service/journals/00547/bibs/8n3p147.html
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PMID:A Comparison of Safety and Efficacy of Sublingual Captopril with Sublingual Nifedipine in Hypertensive Crisis. 1038 21


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