Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0016382 (flushing)
 6,387 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

The long acting angiotensin-converting enzyme inhibitor enalapril was compared with the calcium channel blocker nifedipine as sustained-release formulation in 136 patients with mild to moderate hypertension. This multicentre study was carried out in a double-blind, double-dummy fashion by 28 cardiologists in private practice. After a 2-week placebo period, patients were randomly allocated to 2 treatment groups; the first group received enalapril 20 mg daily (n = 68), and the second group received sustained-release nifedipine 20 mg twice daily (n = 68). The duration of treatment was 12 weeks. In both groups, hydrochlorothiazide 25 mg was added at week 4 if diastolic blood pressure remained greater than 90 mm Hg. At week 8, if the target diastolic pressure of less than 90 mm Hg was not achieved, the dosage of hydrochlorothiazide was increased to 50mg. The clinical characteristics of the patients in each group were comparable. After 4 weeks of treatment, the reduction in supine diastolic blood pressure was similar in both groups (12.1 mm Hg in the enalapril group vs 10.3 mm Hg in the nifedipine group). Moreover, although the difference between the groups was more noticeable after 12 weeks of treatment (16.3 vs 13.9 mm Hg, respectively), it did not reach significance. The number of patients experiencing clinical adverse effects was significantly greater in the nifedipine group than in the enalapril group [33 (48.5%) vs 18 (26.5%), respectively]. The most common complaints of patients administered nifedipine included swollen ankles, flushing and headaches, whereas complaints in the enalapril group included cough, asthenia, and epigastralgia. Three patients were withdrawn from the study because of side effects in the enalapril group and 10 were withdrawn from the nifedipine group. These results indicate that enalapril and sustained-release nifedipine are equally effective in controlling mild to moderate hypertension. However, enalapril was much better tolerated in this study.
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PMID:Comparative efficacy and safety of enalapril and sustained-release nifedipine in patients with mild to moderate hypertension. The Enalapril vs Nifedipine French Study Group. 218 26

Nicardipine and nifedipine are structurally similar dihydropyridine calcium channel blockers with demonstrated efficacy in the treatment of stable angina pectoris. The present study was a prospective randomized trial designed to evaluate the relative incidence of dizziness, flushing, headache, pedal edema, and palpitations during use of these drugs in patients with angina pectoris. Of 250 patients who entered into the comparative treatment part of the study, 140 patients were susceptible to developing symptoms to nifedipine as identified during a 1-month open-label treatment with nifedipine. These patients were compared with a parallel cohort of 110 patients, who were identified during the same open-label period, but remained mostly asymptomatic. After a 1-week washout of nifedipine, equal numbers of patients in each cohort began an 8-week period of randomized, double-blind treatment with nifedipine (20 mg three times daily) or nicardipine (30 mg three times daily). Patients who experienced these symptoms during the open-label nifedipine treatment had a higher incidence of the same symptoms during the blinded treatment regimen. Nicardipine-treated patients had a lower incidence of each of the symptoms than did the nifedipine-treated patients. Statistically significant differences were reported for dizziness, the most common of the side effects. Patients who were free of these symptoms in the open-label period usually remained free of them in the blinded comparison. However, even among those free of dizziness during the open-label nifedipine treatment, more patients reported experiencing dizziness in the blinded phase from nifedipine than from nicardipine (18% vs 6%; p = 0.02).
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PMID:Randomized double-blind comparison of side effects of nicardipine and nifedipine in angina pectoris. The Nicardipine Investigators Group. 240 16

Lisinopril, a long-acting angiotensin converting enzyme inhibitor, and the calcium channel blocker nifedipine in its retard formulation, were compared as monotherapy in a group of 45 patients with essential hypertension. Lisinopril in single daily doses (range 20-80 mg, median dose 40 mg) and nifedipine retard in twice daily doses (total daily dose range 40-80 mg, median dose 60 mg) were equally effective in controlling hypertension. The lisinopril group (n = 30), at baseline supine blood pressure 178/109 +/- 23/9 mm Hg (mean +/- 1 SD), after 12 weeks' therapy measured 148/88 +/- 27/14 mm Hg; the nifedipine group (n = 15), at baseline 185/110 +/- 23/11 mm Hg, after 12 weeks' therapy measured 151/89 +/- 14/10 mm Hg. The number of patients who experienced clinical adverse effects was significantly greater in the nifedipine group: 8 of 15 (53%) compared to 4 of 30 (13%) in the lisinopril group. The commonest adverse effects of patients on nifedipine were swollen ankles, flushing, and headache. Two patients on nifedipine were withdrawn from the study because of their adverse experiences. Of the patients on lisinopril there were single reports of flushing, ankle swelling, tiredness, and chest pain. No patient withdrew from lisinopril because of an adverse experience. No adverse laboratory experiences were recorded in either group. In conclusion, lisinopril and nifedipine retard were equally effective in controlling essential hypertension. Lisinopril was, however, better tolerated during this study.
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PMID:Comparative efficacy of lisinopril and nifedipine retard in essential hypertension: a double-blind, placebo-controlled trial. 245 54

Throughout the developed world, populations are growing older. Blood pressure, especially systolic blood pressure, increases with aging, and this increase leads to increased risks of cardiovascular morbidity and mortality. Clinical trials demonstrate that treatment of hypertension in the elderly reduces overall cardiovascular mortality, cardiac mortality, nonfatal cardiovascular events, congestive heart failure, progression to severe hypertension, and strokes. Drug treatment has been well tolerated, but diuretic therapy has been known to increase plasma glucose, uric acid, and creatinine. Therapeutic trials of nonpharmacologic treatment may be indicated in those with mild elevation in blood pressure and no serious end organ disease. However, most people up to age 80 will require drug treatment. Many drugs are effective in the elderly, but, some like beta-blockers, may not be as effective as in younger patients. Controlled clinical trials demonstrate that nitrendipine, a calcium channel blocking drug, significantly reduced mean systolic and diastolic blood pressure in older hypertensive patients, (successfully controlling pressure in a high percentage) and was well tolerated. Drug effects persist for 12 h or more. The drug decreased the exercise-induced rise in the rate-pressure product. Although there is a temporary increase in heart rate, this returns to baseline after a short time. Side effects include headache, flushing, dizziness, edema, and palpitations. Therefore, nitrendipine offers a reasonable and useful alternative to many other drugs in the treatment of combined systolic and diastolic hypertension in the elderly.
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PMID:Epidemiologic aspects of elderly hypertensive patients and the results of treatment with nitrendipine. 248 68

Nicardipine is an investigational dihydropyridine calcium channel blocking agent. One hundred fifty-one patients with hypertension received either 30 mg nicardipine t.i.d. or 25 mg hydrochlorothiazide b.i.d. in a double-blind, randomized, multicenter trial. After 4 weeks of therapy and at the end of the dosing interval, nicardipine reduced arterial pressure by 10/6 mm Hg and 12/6 mm Hg in the supine and standing positions, respectively (all p less than 0.01). In the hydrochlorothiazide group, the reductions were 12/6 mm Hg and 14/6 mm Hg, respectively (all p less than 0.01). The maximum reduction in blood pressure of 16/14 mm Hg supine and 20/15 mm Hg standing occurred within 1 hour after administration of nicardipine. The mean reduction in the hydrochlorothiazide group after 1 hour was 14/11 mm Hg supine and 16/12 mm Hg standing. Neither drug affected autonomic reflexes associated with maximum exercise. Nicardipine increased urinary sodium excretion during the 4-hour period after the first dose. Adverse effects of nicardipine were primarily extensions of its vasodilator effect and included flushing, headache, and edema.
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PMID:Nicardipine and hydrochlorothiazide in essential hypertension. 264

1. The antihypertensive efficacy of a long acting formulation of the calcium channel blocking drug, nicardipine, was assessed using clinic and ambulatory (Remler M2,000) blood pressure measurements. 2. Eleven patients with essential hypertension (mean +/- s.e. mean; 173 +/- 6.6/103 +/- 1.9 mmHg) completed a randomised double-blind, placebo-controlled, cross-over study. The dose of nicardipine used was 60 mg twice daily for 4 weeks. 3. Mean ambulatory blood pressure was reduced from 164 +/- 5.3/97 +/- 2.9 to 151 +/- 5.2/88 +/- 2.4 mmHg (P less than 0.01); this effect was shown to be sustained for 8 h after the morning dose. Mean ambulatory heart rate was not significantly affected by treatment. 4. Clinic lying systolic blood pressure was reduced on treatment from 169 +/- 7.1 to 157 +/- 5.9 mmHg (P less than 0.2) and diastolic blood pressure from 99 +/- 3.6 to 89 +/- 3.9 mmHg (P less than 0.05). 5. One patient was withdrawn because of dizziness and flushing while on nicardipine; vasodilatory side effects such as headache, palpitations and flushing on nicardipine were noted by three patients. 6. We conclude that the long acting formulation of nicardipine studied in a dose of 60 mg twice daily is effective as monotherapy and is relatively well tolerated in mild hypertension. 7. This study highlights the importance of ambulatory blood pressure measurement in detecting significant changes in blood pressure, thereby permitting the study of small numbers of patients.
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PMID:The effect of slow-release nicardipine on ambulatory and clinic blood pressure in mild hypertension. 267 16

Most side-effects of calcium channel blockers are related to their pharmacological properties. This is best illustrated by the most common cardiovascular side-effects, which reflect the differences between the drugs of such a heterogeneous group. Side-effects related to excessive vasodilating activity (headache, dizziness, flushing, peripheral edema, and palpitations) are most likely with drugs such as nifedipine and other dihydropyridines, which are most active on vascular smooth muscle. Those related to depressed cardiac contraction and conduction are more likely with verapamil, whereas diltiazem is intermediate between the other two drugs. In the event of the occurrence of these adverse reactions, factors such as pharmacokinetics, galenic form, and the administration mode play a role. The pathological status of the patient also comes into play. Other less common reactions such as neuropsychic, gastrointestinal and endocrine effects and gingival hyperplasia appear as a consequence of the numerous sites of action of these molecules. Hepatic, haematological and cutaneous reactions appear to be relevant to immunological mechanisms. Therefore, most of the adverse effects of calcium channel blockers originate in the common mechanism of action of these drugs.
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PMID:[Side-effects of calcium inhibitors]. 267 81

The adverse reactions seen following administration of neuromuscular blocking agents are mainly cardiovascular. Due to the lack of specificity for the nicotinic receptor at the neuromuscular junction, these agents may interact with receptors in autonomic ganglia and muscarinic receptors in the heart. Furthermore, muscle relaxants may have histamine-releasing properties. The cardiovascular effects vary with potency and specificity of the drug, depending mainly on the chemical structure. Pancuronium, fazadinium and especially gallamonium block cardiac muscarinic receptors, and tachycardia may be seen. Atracurium, metocurine and in particular d-tubocurarine have histamine-releasing properties and may cause flushing, hypotension and tachycardia. Vecuronium has no effect on the cardiovascular system. The effect of succinylcholine on heart rate differs between children, where bradycardia is seen, and adults in whom tachycardia may follow. However, bradycardia may occur in adults following a single dose. Succinylcholine increases plasma potassium, especially in patients with nerve damage, and arrhythmias may be observed. The neuromuscular adverse effects of succinylcholine, such as fasciculations and increased gastric and intraocular pressure, may be prevented by precurarisation. Many drugs interact with neuromuscular blocking agents and there is often a potentiation of the neuromuscular effect. This is of clinical importance in the case of antibiotics, inhalational anaesthetics, lithium and cyclosporin. Difficulty in reversing the block may occur with calcium channel blockers and polymyxin. However, some drugs, such as phenytoin, carbamazepine and lithium, may cause resistance to neuromuscular blocking agents. Furthermore, clinically important interactions exist between individual neuromuscular blocking drugs. Precurarisation with a non-depolarising drug prolongs the onset of succinylcholine, and conversely a prolonged effect of non-depolarising drugs is seen following succinylcholine. The effect of succinylcholine is markedly prolonged if the drug is administered during recovery from pancuronium blockade or following neostigmine for reversal. Succinylcholine is hydrolysed by plasma cholinesterase, and drugs which decrease the activity of this enzyme may produce a prolonged block, i.e. contraceptive pills, cyclophosphamide, echothiopate and organophosphate.
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PMID:Adverse reactions and interactions of the neuromuscular blocking drugs. 268 31

Calcium channel blocking drugs are a chemically heterogenous group, so it might be expected that their effects on vascular smooth muscle, cardiac contractility, and conduction tissue may differ. However, the majority of adverse reactions are predictable from their pharmacological actions and may be conveniently grouped in the following categories: 1) vasodilatation, 2) negative inotropic effects, 3) conduction disturbances, 4) gastrointestinal effects, 5) metabolic effects, and 6) drug interactions. Vasodilatory symptoms, namely, dizziness, headaches, flushing sensation, and palpitation, are more likely with nifedipine. Peripheral edema is also common with nifedipine, but the mechanism is uncertain. For a given degree of vasodilation, the greatest negative inotropic effect is seen with verapamil first, diltiazem second, and nifedipine last. Calcium channel blocking drugs are contraindicated in hypertensive patients with second and third degree heart block, sick sinus syndrome, and severe heart failure. Verapamil and diltiazem have a significant effect on cardiac conduction, whereas nifedipine, in therapeutic doses, does not. Local gastrointestinal symptoms, such as nausea and constipation, are common with verapamil. None of the calcium channel blocking drugs have been reported to adversely affect lipid or protein metabolism. However, nifedipine, verapamil, and diltiazem in high doses may inhibit liberation of insulin. The significance of this finding needs to be explored further in hypertensive diabetics. Serum digoxin levels have been shown to increase after administration of verapamil and nifedipine, but there is no evidence that this change has any clinical relevance.(ABSTRACT TRUNCATED AT 250 WORDS)
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PMID:Side effects of calcium channel blockers. 328 Apr 92


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