Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0018681 (headache)
 56,091 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Nifedipine antagonises influx of calcium through cell membrane slow channels, and sustained release formulations of the calcium channel blocker have been shown to be effective in the treatment of mild to moderate hypertension and both stable and variant angina pectoris. Preliminary findings also indicate that these formulations are effective in the treatment of Raynaud's phenomenon and hypertension in pregnancy, and that they reduce the frequency of ischaemic episodes in some patients with silent myocardial ischaemia. The exact mechanism of action of nifedipine in all of these disorders has not been defined. However, its potent peripheral and coronary arterial dilator properties, together with improvements in oxygen supply/demand, are of particular importance. A major goal of sustained release therapy is to permit reductions in the frequency of nifedipine administration, preferably to once daily, and thus improve patient compliance. Two new once-daily formulations--the nifedipine gastrointestinal therapeutic system (GITS) and a fixed combination capsule comprising sustained release nifedipine 20 mg and atenolol 50 mg--have exhibited marked antihypertensive efficacy. The GITS preparation has also been used effectively in the treatment of stable angina pectoris, and both formulations appear to be well tolerated. Sustained release nifedipine formulations are generally better tolerated than their conventionally formulated counterparts, particularly with regard to reflex tachycardia. Adverse effects seem to be dose related, are mainly associated with the drug's potent vasodilatory action, and include headache, flushing and dizziness. Generally, these effects are mild to moderate in severity and transient, usually diminishing with continued treatment. Thus, sustained release nifedipine formulations are useful and established cardiovascular therapeutic agents which have demonstrable efficacy in various forms of angina, mild to moderate hypertension and Raynaud's phenomenon. Further, promising results shown by the nifedipine GITS formulation, with its advantage of once daily administration suggest that it is likely to become one of the preferred nifedipine formulations for the treatment of hypertension and the various forms of angina.
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PMID:Sustained release nifedipine formulations. An appraisal of their current uses and prospective roles in the treatment of hypertension, ischaemic heart disease and peripheral vascular disorders. 171 8

Improved measurement of the plasma concentration of nitrendipine demonstrated a plasma half-life of 17-21 h, allowing once-daily (o.d.) instead of currently twice-daily (b.i.d.) dosing. To determine the effectiveness of nitrendipine given o.d. vs. b.i.d., 78 hypertensive patients, [supine diastolic blood pressure (DBP) of 95-114 mm Hg] were randomized in a double-blind fashion to 12 weeks of treatment with either nitrendipine 10 mg b.i.d. (n = 39) or nitrendipine 20 mg o.d. (n = 39) after a 2-week placebo baseline period. Blood pressures (BPs) were measured in the morning at the end of the dosing interval. Mean +/- SD reduction in supine systolic BP (SBP) and DBP in patients evaluable for efficacy (greater than or equal to 14 days treatment) were 7.2 +/- 16.5 and 7.7 +/- 10.3 mm Hg, respectively, after nitrendipine b.i.d. (n = 38) and 9.4 +/- 15.1 and 9.5 +/- 7.0 mm Hg, respectively, after nitrendipine o.d. (n = 36). Similar falls in BP were found for both regimens in patients completing the full 12 weeks of treatment period (n: o.d. = 28, b.i.d. = 32). Discontinuation due to adverse experiences (AEs) occurred in three patients on b.i.d. and eight patients on o.d., the latter mostly in the first 2 weeks of therapy. Overall, AEs were higher in the o.d. group (% AEs at least possibly related to study medication: o.d. = 44%, b.i.d. = 33%). Most frequent AEs were headache and flushing.(ABSTRACT TRUNCATED AT 250 WORDS)
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PMID:Once- vs. twice-daily nitrendipine in the treatment of mild to moderate hypertension, Canadian Nitrendipine Study Group. 171 78

In this study of the efficacy and safety of isradipine as first-line therapy in hypertension, 1,647 patients enrolled; 1,472 completed the 4-week placebo run-in period and began treatment with isradipine at 2.5 mg twice daily for 4 weeks. During placebo, 11% (n = 175) of the 1,647 patients withdrew because of normalization of blood pressure, side effects, noncompliance, violation of the study protocol, side effects from concomitant therapy, or other reasons. During isradipine therapy (n = 1,376), blood pressure decreased from 168 +/- 18/102 +/- 8 mm Hg at the end of the placebo period to 155 +/- 17/94 +/- 9 mm Hg after 2 weeks (p less than 0.001) and 151 +/- 16/92 +/- 9 mm Hg after 4 weeks (p less than 0.001). During active treatment, 6.4% (n = 94) were withdrawn because of flushing, headache, edema, palpitations, gastrointestinal side effects, skin rashes, or other side effects, and two patients because of lack of efficacy. The side effect score in the remaining patients worsened for flushing, remained unchanged for edema, but significantly improved for palpitations, fatigue, dizziness, headache, and nervousness. After 4 weeks, 60% of patients had diastolic blood pressures of less than or equal to 90 mm Hg. Thus, isradipine is effective and safe as first-line therapy in patients with primary hypertension as seen in general practice.
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PMID:Calcium antagonists as first-line therapy in hypertension: results of the Swiss Isradipine Study. Swiss Hypertension Society. 172 Apr 76

The efficacy and safety of isradipine and nifedipine retard were compared in 51 patients with mild-to-moderate essential hypertension. A 4-week placebo run-in period was followed by an 8-week course of treatment. Patients were randomly allocated to either isradipine 1.25 mg twice daily (n = 24) or nifedipine 20 mg twice daily (n = 826); dosages were doubled if blood pressure was not normalized [diastolic blood pressure greater than or equal to 90 mm Hg) after 4 weeks of active treatment. Systolic/diastolic blood pressures were significantly reduced (p less than 0.01/p less than 0.01) by isradipine from 162/103 to 145/89 mm Hg, and by nifedipine from 162/104 to 143/88 mm Hg. Normalization rates were 79% with isradipine and 67% with nifedipine. It was necessary to double the dosage in seven of the patients taking isradipine and in three of those taking nifedipine; the mean final dosages were 1.63 mg and 22.4 mg twice daily, respectively. Heart rate did not change significantly with either treatment. There were drug-related adverse events in five patients (21%) taking isradipine (2 edema, 2 headache, 2 palpitations, 1 flushing) and in eight (30%) of those taking nifedipine (5 edema, 2 headache, 1 palpitations). Therapy was withdrawn in one patient in the isradipine group (1 headache) and two patients in the nifedipine group (1 edema, 1 headache). We conclude that isradipine is a highly effective and well tolerated antihypertensive agent.
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PMID:First clinical experience with isradipine in the treatment of hypertension in Portugal. 172 Apr 85

The antihypertensive effect of nitrendipine was examined in 29 outpatients with a mild or moderate hypertension and type II diabetes or a dyslipidemic condition. The drug was administered for 90 days at a daily dose of 10 to 40 mg. Following a washout period, the blood pressure (measured by a Dinamap device) was 181/99 mm Hg supine and 172/104 mm Hg standing. Nitrendipine caused a reduction in both pressures and after 90 days their values were 148/74 and 143/80 mm Hg, respectively. Heart rate was not affected by the drug, which also caused no variation in blood pressure, total and HDL cholesterol, and triglycerides. In more than 20% of the cases, treatment was associated with headache and flushing, which did not necessitate discontinuation of treatment. Thus, nitrendipine is an effective antihypertensive agent and causes no untoward metabolic effects.
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PMID:Nitrendipine efficacy and safety in patients with mild and moderate essential hypertension. 172 54

Efficacy and tolerability of antihypertensive monotherapy with the calcium antagonist nitrendipine were investigated in a 6-month open trial in 495 patients with mild to moderate essential hypertension from 101 practicing internists and general practitioners. Previous antihypertensive therapy (57.4%) was stopped for 1 week and therapy then started with nitrendipine, 20 mg once daily. Sixty-one patients discontinued therapy prematurely because of unwanted effects, mostly characteristic with dihydropyridines (headaches, flushing, and ankle edema), and 23 patients because of insufficient efficacy. In 75% of the remaining 411 patients, the goal blood pressure was achieved by nitrendipine monotherapy (10 mg in 17.6%, 20 mg in 73.3%, and 20 mg b.i.d. in 8%) and diastolic blood pressure was between 90 and 95 mm Hg in another 6%. The reduction in blood pressure did not result in changes of heart rate or weight. Nitrendipine was effective in patients of all age groups but patients older than 60 years of age showed a significantly greater fall in systolic pressure than middle-aged or young patients. At the end of the study, 15 patients still reported side effects. Nitrendipine appears to be well suited for first-line therapy of mild to moderate essential hypertension.
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PMID:Antihypertensive monotherapy with nitrendipine in general practice. 172 58

Twelve patients with critical ischaemia of the lower limbs were treated with iloprost. The purpose of this study was to investigate for a possible iloprost-digoxin interaction and to evaluate the clinical benefit provided by short- or long-term iloprost therapy. The pharmacokinetics of digoxin were studied before and during iloprost treatment. Under iloprost the absorption of digoxin was delayed by about one hour, but the area under the plasma digoxin concentration curve remained unmodified. In 11 of our 12 patients the clinical effect of iloprost was satisfactory both immediately and after 6 months. Pain vanished in 6 patients and diminished in 6 patients. All skin ulcers were healed. In most cases this improvement persisted beyond the study period: 2 patients treated at the beginning of the study and who are still followed up have remained improved after 2 1/2 years. Two patients with pain relapse received iloprost in repeated 10 days' courses with successful results. The treatment was relatively well tolerated (headaches, flushing, abdominal pain). Thus, iloprost can avoid amputation in severe arteritis unsuitable for revascularization and for which there is no effective treatment. Patients under digoxin may continue to take this drug in the same doses during treatment with iloprost.
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PMID:[Treatment with iloprost of critical ischemia of the lower limbs associated with cardiac insufficiency. Study of the interaction with pharmacokinetics of digoxin]. 172 24

We have treated with intravenous iloprost twelve patients suffering from cardiac insufficiency compensated under oral digoxin (NYHA class II) associated with severe limb ischaemia due to arterial insufficiency. Our aim was to study its possible interaction on digoxin levels and to evaluate the long-term efficacy of iloprost. Although iloprost slowed the digoxin absorption by approximately one hour, we found no clinically significant difference between the digoxin pharmacokinetic data before and during treatment by iloprost. Moreover, 11 out of the 12 patients had a good clinical fate after the treatment, which persisted at 6 months. The pain disappeared in 4 and diminished in 7; and all skin ulcers healed. This improvement has lasted up to two and a half years in two patients. The clinical tolerance of iloprost was acceptable despite frequent headache and flushing associated with hypotension and nausea. We conclude that iloprost seems to be a very promising treatment of severe limb ischaemia when no intervention on the proximal arteries is possible. The patients on digoxin can continue their treatment without dose alteration while starting on iloprost.
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PMID:[Treatment with iloprost of critical ischemia of the lower limbs associated with cardiac insufficiency. Study of interaction with the pharmacokinetics of digoxin]. 172 27

The safety and tolerability of lacidipine was assessed in a volunteer population, and its pharmacodynamic and pharmacokinetic profiles evaluated. In normotensive subjects, single oral doses of 3-5 mg of lacidipine produced a dose-related fall in peripheral vascular resistance. This was accompanied by reflex-mediated increases in heart rate and cardiac output to maintain blood pressure. Adverse events were those typically related to the vasodilatory action of lacidipine, such as flushing and headache. A 4-mg dose of lacidipine elicited a cardiovascular response equivalent to that with 10 mg of nifedipine, given as a single oral dose. Lacidipine did not affect sinoatrial or atrioventricular conduction in the healthy subjects studied. Two specialized electrophysiologic studies in patients confirmed that lacidipine does not affect pacemaker tissue and that it exhibits relative selectivity for the vascular smooth muscle. Lacidipine is eliminated primarily by hepatic metabolism, and extensive first-pass loss occurs after oral dosing. Absolute bioavailability is less than 10%. The systemic availability of lacidipine was increased in healthy elderly subjects and in patients with impaired hepatic function, but not in patients with impaired renal function.
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PMID:Clinical pharmacology of lacidipine. 172 14

Felodipine, a dihydropyridine calcium-channel antagonist, significantly reduces systolic and diastolic blood pressure (BP) in patients with hypertension and has been associated with beneficial hemodynamic effects in patients with chronic stable angina pectoris or congestive heart failure (CHF). In hypertensive patients, felodipine does not appear to significantly affect glomerular filtration rate, creatinine clearance, glucose tolerance, or plasma lipoprotein concentrations. Studies comparing felodipine with other agents as monotherapy in mild to moderate hypertension have demonstrated felodipine to be at least as efficacious as hydrochlorothiazide (HCTZ) and HCTZ plus amiloride hydrochloride in combination. Comparisons of felodipine with other agents as adjuncts to beta-blocker or diuretic therapy have shown felodipine to be at least as effective as HCTZ, propranolol hydrochloride, prazosin hydrochloride, and nifedipine. Evaluations of patients with chronic stable angina are limited, and additional studies are needed before felodipine can be recommended for the routine management of angina pectoris. Similarly, additional studies are essential to delineate the role of felodipine, if any, in the management of CHF. In the management of hypertension, felodipine 5-40 mg/d significantly reduces systolic and diastolic BP. Although some patients may be controlled throughout the entire dosing interval when felodipine is administered bid, many patients will require more frequent dosing to obtain adequate BP control. Adverse effects associated with felodipine are similar to those of other dihydropyridine calcium-channel antagonists and include peripheral edema, headache, dizziness, flushing, and fatigue. A potentially clinically important drug interaction was observed when felodipine was administered concomitantly with theophylline aminopropanol; significant decreases in theophylline concentrations were noted. In summary, felodipine appears to be safe and effective for the management of hypertension when used alone or in combination with other antihypertensive agents. The efficacy of felodipine in the management of chronic stable angina pectoris and CHF requires further investigation.
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PMID:Felodipine: a new dihydropyridine calcium-channel antagonist. 176 37


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