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)

Openers of adenosine triphosphate (ATP)-sensitive potassium channels relax vascular smooth muscle and protect ischemic myocardium. Cromakalim and BMS-180448 are examples of this class of compounds. They are equipotent in their cardioprotective activity, but cromakalim and related compounds are extremely hypotensive, an activity that limits their use. The effects of cumulative i.v. doses of BMS-180448 or cromakalim on hemodynamics and regional blood flow (radiolabeled microspheres) were evaluated in pentobarbital-anesthetized dogs and ferrets. Both compounds significantly reduced mean arterial blood pressure, cromakalim after 0.03-0.04 mg/kg in both species, and BMS-180448 only after 10 mg/kg in dogs and 30 mg/kg in ferrets. Neither drug affected cardiac output. BMS-180448, like cromakalim, increased blood flow in the heart, with augmented regional left ventricular blood flow occurring more in the subepicardium than in the subendocardium. The effect of BMS-180448 on myocardial blood flow, in both the dog and ferret, occurred at doses that were less hypotensive than those of cromakalim. The most striking difference between the actions of these agents was seen in the brain where cromakalim, but not BMS-180448, increased blood flow in all regions. The results of these studies further demonstrate the myocardium-specific vasodilator activity of BMS-180448. Moreover, the cerebral vasodilator effect of K(ATP) openers, which has been thought responsible for the occurrence of headache in clinical trials, has been found lacking in BMS-180448; this difference may represent a clear advantage in the pharmacologic profile of the agent.
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PMID:Selectivity of BMS-180448 on myocardial versus brain blood flow in dogs and ferrets. 926 22

In the paper we have described a case of acute, unintentional intoxication with clenbuterol, a selective beta 2-agonist. A 21-year-old bodybuilder to improve his physical fitness and to increase his muscle bulk was using clenbuterol in a dose of two tablets (20 mg) daily for a week before poisoning. On a day of acute intoxication he drank orange juice containing 48 tablets (4.8 g) of clenbuterol, which had been placed there by his friends. The patient was admitted to our clinic with tachycardia at rate 160 bpm, headache, dizziness, tremor, sweats, muscle weakness, agitation. Serum potassium concentration was 2.6 mmol/L, blood glucose level 18.7 mmol/L. All the symptoms and biochemical abnormalities disappeared after intravenous treatment with propranolol (1.0 mg) and potassium chloride (60 mmol) within five hour period. This case indicates that more attention should be paid to clenbuterol widely used as a stimulant by athletes, especially by bodybuilders.
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PMID:Acute poisoning with clenbuterol--a case report. 947 4

In this phase I study a novel potassium channel opener (YM934) was administered to young healthy male volunteers to identify a dose with minimal cardiovascular effects. The study was carried out using a double-blind, placebo-controlled rising dose design with oral YM934 in single doses of 20 micrograms, 60 micrograms, and 180 micrograms. During each study day frequent blood samples were obtained for drug assay, measurements of cardiovascular parameters, and parasympathetic activity. The drug was well tolerated, with headache being the only significant adverse event. No relationship could be detected between dose or plasma concentration of YM934 and headache. No significant changes in routine laboratory and pharmacodynamic parameters occurred between placebo and active drug treatment. The pharmacokinetics of YM934 were characterized by a rapid oral absorption, an elimination half-life of 30 hours, and an oral clearance of 1.7 L/h. The obtained data allow estimation of a YM934 dose regimen with minimal cardiovascular (side) effects to be used for future efficacy studies.
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PMID:A phase I double-blind, placebo-controlled, single rising dose study to determine the safety, tolerability, and pharmacokinetics of oral YM934 in healthy male volunteers. 959 59

Patients (16 women and 16 men) with brain tumors previously treated conservatively by surgery, radiation, and/or chemotherapy with typical symptoms of increased intracranial pressure were consecutively enrolled to test the effects of pharmacological dosages of sodium selenite (selenase) in conjunction with other supportive therapies (biological response modifiers, detoxification, chemotherapy, immunotherapy, oxygen therapy). The rationale for the use of sodium selenite was that the whole-blood selenium levels were subnormal in 70% of the patients on admission. Patients also frequently presented abnormal levels of other minerals, especially lowered sodium and elevated potassium levels, which appears to be characteristic of brain tumor patients. Sodium selenite was administered by infusion at dosages of 1000 microg Se in physiological saline/d for 4-8 wk. In 76% of the patients, a definite, and in 24% a slight improvement of the general condition and a decrease in symptoms, such as nausea, emesis, headache, vertigo, unsteady gait, speech disorders, and Jacksonian seizures, were observed. In all treated patients, improvements of erythrocyte, hemoglobin, and thrombocyte counts were observed. Additional beneficial effects were noted in the patients receiving the oxygen therapy. It is concluded that the sodium selenite can be employed with oxygen therapy and other supportive measures in the management of brain tumor patients.
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PMID:Symptomatic treatment of brain tumor patients with sodium selenite, oxygen, and other supportive measures. 963 Apr 18

The goals of stable angina pectoris treatment are: (i) symptom relief and increase in angina-free walking time; and (ii) reduction of mortality and adverse outcome. Strategies used for plaque stabilisation resulting in a reduction in cardiovascular mortality and morbidity are: smoking cessation; aspirin (acetylsalicylic acid); blood pressure control; lipid lowering agents when low density lipoprotein cholesterol is elevated despite dietary therapy; coronary bypass surgery in patients with left main stem disease or triple vessel coronary disease and diminished left ventricular function; and use of estrogen in postmenopausal women. For symptom relief and to increase angina-free walking time, long acting nitrates, beta-blockers, calcium antagonists and potassium channel openers can be used. Drugs from these 3 classes are all effective when used optimally and choice of initial therapy should consider the presence of concomitant disease and underlying left ventricular function. However, none of the long acting nitrates provide continuous prophylaxis because nitrate tolerance develops during long term therapy. In patients with uncomplicated stable angina, nitrates, beta-blockers and calcium antagonists are all effective. Intermittent nitrate therapy is not associated with tolerance, but headache is a common adverse effect and the patient is unprotected at night and in the early hours of the morning. Concomitant treatment with a beta-blocker may be beneficial if the patient experiences withdrawal or early morning angina. For patients with stable angina and hypertension, therapy with a beta-blocker or a calcium antagonist rather than nitrate is indicated. beta-Blockers are preferred in patients who have had a myocardial infarction, or in those with a history of supraventricular tachyarrhythmias. beta-Blockers may produce excessive slowing of the heart rate, fatigue and bronchospasm in susceptible patients. Calcium antagonists are indicated as initial therapy when beta-blockers are either not tolerated or contraindicated. beta-Blockers and nondihydropyridine calcium antagonists should not be used in patients with sinus bradycardia and those with greater than first degree atrioventricular (AV) block because of the possibility of further slowing of heart rate and/or the development of high grade AV block. When monotherapy with one class is ineffective or associated with adverse effects, the patient should be switched to another class rather than given an additional drug. Optimal monotherapy is often as effective as combination therapy. If maximum monotherapy is only partially effective, a combination therapy which is not additive in terms of adverse effects should be chosen. Triple therapy may be deleterious and no more effective than dual therapy.
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PMID:Choosing the most appropriate treatment for stable angina. Safety considerations. 967 56

We describe a 28-year-old subject employed as a roofer in a construction company since the age of 19, who developed work-related symptoms of a cough, shortness of breath, wheezing, rhinitis and headaches. A description of a usual day at work suggested that the symptoms worsened while he was sawing corrugated fiber cement. Baseline spirometry was normal, and there was a mild bronchial hyperresponsiveness to carbachol. A skin patch test to chromium was negative. A specific inhalation challenge showed a boderline fall in forced expiratory volume in 1 s (FEV1) after exposure to fiber cement dust. Exposure to nebulization of potassium dichromate (K2Cr2O7), at 0.1 mg.ml-1 for 30 min, was followed by an immediate fall by 20% FEV1. Simultaneously, a significant increase in bronchial hyperresponsiveness was demonstrated.
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PMID:Occupational asthma due to chromium. 978 25

Renal artery stenosis or occlusion causing the hyponatremic-hypertensive syndrome has been rarely reported. Our impression, however, was that the disorder is not uncommon. Case records from patients in one city (population 350 000) presenting between 1980 and 1997 with hypertension, hyponatremia, and evidence of renal ischemia were scrutinized. Thirty-two patients fulfilling inclusion criteria were identified. Admission supine arterial pressures were high (mean 228/124 mm Hg), but there was a vigorous fall in pressure on standing (26/12.7 mm Hg recorded in 27 patients). Mean plasma concentrations of sodium (129.7 mmol/L) and potassium (2.7 mmol/L) were low, and 24-hour urine protein excretion was elevated in 19 of 26 patients. Twenty-two of the 32 patients were female, the majority were asthenic, and all but 5 were smokers. Symptoms precipitating hospitalization were headache, clouding of consciousness, confusion, weakness, weight loss, thirst, and polyuria. Plasma renin levels, measured in 20 patients, were elevated in most cases and correlated inversely (r=-0.63, P<0.01) with the plasma sodium concentration. The hyponatremic-hypertensive syndrome in patients with renal ischemia is not rare: Rather, it is underreported. It tends to affect elderly asthenic women who smoke heavily. Stimulation of renin release from the ischemic kidney is probably central to the pathophysiology. The syndrome deserves better recognition to ensure appropriate investigations and management.
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PMID:Hyponatremic-hypertensive syndrome with renal ischemia: an underrecognized disorder. 1020 41

The efficacy and safety of a fixed-combination homeopathic medication (Sinusitis PMD) consisting of Lobaria pulmonaria, Luffa operculata, and potassium dichromate were investigated in an open-label practice-based study of 119 male and female patients, 12 to 57 years of age, with clinical signs of acute sinusitis not previously treated. At the first visit, after a mean of 4.1 days of treatment, secretolysis had increased significantly and typical sinusitis symptoms, such as headache, pressure pain at nerve exit points, and irritating cough, were reduced. Ninety-nine patients received only the test medication. Twenty patients were able to discontinue concomitant medication at the first visit. Only one patient needed an antibiotic. The average treatment duration was 2 weeks. At the end of treatment, 81.5% of patients described themselves as symptom free or significantly improved. Adverse drug effects were not reported.
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PMID:Efficacy and safety of a fixed-combination homeopathic therapy for sinusitis. 1053 78

Azimilide is a potassium channel antagonist that, in contrast to existing class III antiarrhythmic agents, blocks both the rapidly (I(Kr)) and slowly (I(Ks)) activating components of the delayed rectifier potassium current. In animal and clinical studies, azimilide prolonged repolarisation by increasing the action potential duration and effective refractory period. In animal models, azimilide was effective in terminating both atrial and ventricular arrhythmias. Azimilide also demonstrated antifibrillatory efficacy in a canine model of sudden cardiac death. In patients with a history of atrial fibrillation/flutter, oral azimilide controlled arrhythmias more effectively than placebo in a 6-month randomised double-blind study. At a dosage of 125 mg once daily, azimilide significantly increased the time to first symptomatic recurrence of atrial fibrillation/flutter. However, no significant difference between placebo and azimilide was found in another study. Oral azimilide 100 mg once daily demonstrated clinically significant treatment effects in patients with paroxysmal supraventricular tachycardia. In clinical trials, azimilide was generally well tolerated and headache was the most commonly occurring adverse event. Azimilide is associated with a low incidence of proarrhythmic events, such as torsades de pointes, and few serious adverse events have been reported.
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PMID:Azimilide. 1073 May 50

The mechanism of action, pharmacokinetics, pharmacodynamics, clinical efficacy, and adverse effects of candesartan cilexetil are reviewed. Candesartan is an angiotensin II-receptor blocker (ARB). It is administered as a pro-drug that undergoes activation during gastrointestinal absorption. The agent is excreted mostly unchanged and has a terminal half-life of about nine hours (slightly longer in the elderly). Candesartan differs from other agents in its class in that it is tightly bound to angiotensin II type 1 receptors, allowing prolonged activity. In clinical trials, candesartan cilexetil has produced a dose-dependent effect when given in dosages of 2-32 mg/day. Observed trough-to-peak blood pressure ratios support a once-daily dosage regimen. The antihypertensive effect of candesartan cilexetil 4-16 mg/day was as great as that of enalapril 10-20 mg/day and amlodipine 5 mg/day and larger than that of losartan potassium 50 mg/day. Adding candesartan cilexetil to hydrochlorothiazide 12.5-25 mg/day and amlodipine 5 mg/day led to enhanced blood-pressure reductions and was well tolerated. It appears that candesartan can decrease renal perfusion without adversely affecting renal blood flow and may mediate a decrease in albuminuria in hypertensive patients with type 2 diabetes. No clinically important drug interactions have been reported. Adverse effects include headache, dizziness, nausea, diarrhea, and transient elevations in liver transaminases. The frequency of cough is similar to that seen with placebo. Candesartan cilexetil is an effective antihypertensive agent that can be used alone or in combination with other antihypertensive drugs. It is generally well tolerated and may be an option for patients who cannot tolerate angiotensin-converting-enzyme inhibitors because of cough.
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PMID:Candesartan cilexetil: an angiotensin II-receptor blocker. 1078 59


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