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1. |
ABSTRACTS |
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The Journal of Clinical Pharmacology,
Volume 22,
Issue 4,
1982,
Page 1-18
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ISSN:0091-2700
DOI:10.1002/j.1552-4604.1982.tb02155.x
出版商:Blackwell Publishing Ltd
年代:1982
数据来源: WILEY
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2. |
Captopril‐Induced Skin Eruptions |
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The Journal of Clinical Pharmacology,
Volume 22,
Issue 4,
1982,
Page 151-159
JOHN R. LUDERER,
DONALD P. LOOKINGBILL,
DENNIS W. SCHNECK,
LAWRENCE M. DEMERS,
CYNTHIA COHEN,
ARTHUR H. HAYES,
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摘要:
Abstract:Seven of 23 hypertensive patients treated with captopril (SQ 14,225), an orally active converting enzyme inhibitor, developed a pruritic, erythematous, macular, and papular eruption of the trunk, face, and proximal extremities. The eruption appeared one to 31 weeks after initiation of captopril therapy and was associated with diarrhea (three patients), fever (two patients), and generalized arthralgias (one patient). Six patients had an increased percentage of band cells (5 to 34 per cent) on peripheral smear without an associated leukocytosis. In one patient, the skin rash was associated with a peripheral eosinophilia (20 per cent), Coombs‐positive hemolytic anemia, and acute renal failure with eosinophiluria. There were no changes in BUN, creatinine, or urinalyses in the remaining patients. Four patients showed a transient rise in plasma PGE without concomitant changes in plasma PFG2αor 6‐keto PGF1α, and three patients had slight elevations in the erythrocyte sedimentation rate. Skin biopsies revealed a perivascular and perifollicular lymphocytic and histiocytic infiltrate with negative immunofluorescence to IgG, IgM, IgA, and β1C. The skin eruption and associated symptoms resolved in all patients, even though captopril administration was continued in six of the seven pa
ISSN:0091-2700
DOI:10.1002/j.1552-4604.1982.tb02156.x
出版商:Blackwell Publishing Ltd
年代:1982
数据来源: WILEY
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3. |
The Oral Analgesic Efficacy of Bicifadine Hydrochloride in Postoperative Pain |
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The Journal of Clinical Pharmacology,
Volume 22,
Issue 4,
1982,
Page 160-164
RICHARD I. H. WANG,
ROGER P. JOHNSON,
JOHN C. M. LEE,
ELIZABETH M. WAITE,
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摘要:
Abstract:The analgesic efficacy of 75 and 150 mg bicifadine hydrochloride was compared to 650 mg aspirin and placebo in a double‐blind, single‐dose study. Oral doses were administered to 100 patients suffering from moderate to severe postoperative pain. Significant analgesic activity was demonstrated with 650 mg aspirin and 150 mg bicifadine as compared to 75 mg bicifadine or placebo. No significant treatment difference was found between 75 mg bicifadine and placebo. Side effects were minor and did not interfere with the course of ther
ISSN:0091-2700
DOI:10.1002/j.1552-4604.1982.tb02157.x
出版商:Blackwell Publishing Ltd
年代:1982
数据来源: WILEY
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4. |
Buprenorphine and Morphine Efficacy in Postoperative Pain: A Double‐Blind Multiple‐Dose Study |
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The Journal of Clinical Pharmacology,
Volume 22,
Issue 4,
1982,
Page 165-172
ROBERT D. OUELLETTE,
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摘要:
Abstract:The analgesic activity of buprenorphine was monitored versus that of morphine in a double‐blind, randomized, multiple‐dose, parallel‐design study involving 97 postsurgical patients. Patients could receive intramuscular injections of either buprenorphine (0.3, 0.45, or 0.6 mg) or morphine (10, 15, or 20 mg) every 3 or more hours. Pain intensity, degree of sedation, vital signs, pain relief, and side effects were assessed prior to and at regular intervals after each drug injection. No statistically significant differences were found between the two drugs in total pain relief, sum of pain intensity difference by patient and over time, time to peak pain intensity difference, duration of pain, and side effects. It has been suggested that the addictive potential of buprenorphine may be less than that of morphine. Since both drugs seem to be effective analgesics, buprenorphine appears to offer an effective and safe alternative to morphine for patients with acute
ISSN:0091-2700
DOI:10.1002/j.1552-4604.1982.tb02158.x
出版商:Blackwell Publishing Ltd
年代:1982
数据来源: WILEY
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5. |
Gastrointestinal Blood Loss of Oxaprozin and Aspirin with Placebo Control |
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The Journal of Clinical Pharmacology,
Volume 22,
Issue 4,
1982,
Page 173-178
ANDRÉ LUSSIER,
ÉTIENNE LeBEL,
LÉON TÉTREAULT,
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摘要:
Abstract:The objective of this study was to compare the effects of oxaprozin (4,5‐diphenyl‐2‐oxazolepropionic acid), a nonsteroidal, antiinflammatory compound, and aspirin in a double‐blind, placebo‐controlled study to estimate gastrointestinal bleeding. The determination of fecal blood loss was made quantitatively by the use of the radioactive (51Cr) technique. During the first week, subjects were controlled with and without placebo. At the end of the second week, the subjects were divided and randomly assigned to one of three groups; 10 received 1200 mg oxaprozin (600 mg twice daily), 11 received 3900 mg aspirin (975 mg four times a day), and the remaining 8 subjects received placebo for two weeks. During the last two weeks, all received placebo again. A statistical analysis of variance showed that there were no statistical differences between the groups during the first and last two weeks of placebo therapy. During the active treatment period, weeks 3 and 4, there were statistically significant differences among the three groups. The mean blood loss during week 3 was significantly greater for the aspirin group, 8.8 ml/day, than the oxaprozin group, 3.3 ml/day (P<0.05), and the placebo group, 1.4 ml/day (P<0.001). The smaller difference between oxaprozin and placebo was also significant (P<0.05). During the fourth week, the mean daily blood loss among oxaprozin patients had decreased to 2.3 ml/day, and no statistically significant difference from placebo (1.1 ml/day)
ISSN:0091-2700
DOI:10.1002/j.1552-4604.1982.tb02159.x
出版商:Blackwell Publishing Ltd
年代:1982
数据来源: WILEY
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6. |
Differential Effects of Diuresis and Beta‐Adrenoreceptor Blockade During Angiotensin‐Converting Enzyme Inhibition in Patients with Severe Hypertension |
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The Journal of Clinical Pharmacology,
Volume 22,
Issue 4,
1982,
Page 179-186
JAN I. M. DRAYER,
MICHAEL A. WEBER,
JODI L. LIPSON,
BERNARD B. MEGAFFIN,
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摘要:
Abstract:The orally administered blocker of angiotensin‐converting enzyme, captopril, was given to 16 patients with moderate to severe hypertension in whom blood pressure could not adequately be controlled by combination treatment with a vasodilator (hydralazine 200 mg daily), a beta‐blocker (propranolol 320 mg daily), and a diuretic (hydrochlorothiazide 100 mg daily). Captopril (450 mg daily) alone maintained blood pressure at the same levels as during previous administration of the combination, although in the absence of the diuretic and the beta‐blocker there were increases in body weight of 1.8 ± 0.5 (S.E.) kg (P<0.01) and in supine heart rate of 10 ± 4 beats/min (P<0.01). After hydrochlorothiazide (100 mg daily) was added to the captopril, the supine mean blood pressure of 122 ± 5 mm Hg was significantly lower than during captopril alone (134 ± 4 mm Hg,P<0.01). Heart rate increased from 79 ± 3 to 90 ± 5 beats/min (P<0.05). In 13 of the 16 patients, in whom supine diastolic blood pressure still remained higher than 90 mm Hg, the addition of propranolol (120–360 mg daily) to the captopril‐hydrochlorothiazide combination decreased heart rate from 88 ± 5 to 65 ± 3 beats/min (P<0.01), but failed to produce a further blood pressure decrement. However, the supine mean blood pressure during the captopril‐hydrochlorothiazide‐propranolol combination of 120 ± 5 mm Hg was significantly lower (P<0.05) than that (132 ± 6 mm Hg) during the hydralazine‐hydrochlorothiazide‐propranolol combination. Despite similar diuretic doses in the two regimens, serum potassium concentration was significantly higher during treatment with the captopril combination (4.3 ± 0.2 vs. 3.6 ± 0.2 mEq/l.,P<0.01). It seems likely that converting enzyme inhibition by captopril increases the sensitivity of the blood pressure response to diuretic therapy, in part by blocking the countervailing effects of the reactive rise in renin release that is stimulated by sodium depletion. In these renin‐blocked patients, however, addition of propranolol does not appear to produce any
ISSN:0091-2700
DOI:10.1002/j.1552-4604.1982.tb02160.x
出版商:Blackwell Publishing Ltd
年代:1982
数据来源: WILEY
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7. |
Preserved Renal Perfusion During Treatment of Essential Hypertension with the Beta Blocker Nadolol |
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The Journal of Clinical Pharmacology,
Volume 22,
Issue 4,
1982,
Page 187-195
DANIEL T. O'CONNOR,
ANNA P. BARG,
KENNETH L. DUCHIN,
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摘要:
Abstract:Several beta‐adrenergic antagonists impair renal perfusion during treatment of hypertension in man. The acute and chronic effects of a new noncardioselective beta blocker, nadolol, on renal hemodynamics, intravascular volume, and renal electrolyte excretion were studied in 10 men with essential hypertension. Oral nadolol normalized systemic blood pressure without impairment of glomerular filtration rate or renal blood flow, indicating preserved renal blood flow and glomerular filtration rate autoregulation. Intravascular volume and renal excretion of electrolytes were similarly unaltered. Once‐daily nadolol lowers blood pressure without renal hemodynamic or functional embarrassm
ISSN:0091-2700
DOI:10.1002/j.1552-4604.1982.tb02161.x
出版商:Blackwell Publishing Ltd
年代:1982
数据来源: WILEY
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8. |
Effect of Food on the Bioavailability and Pattern of Release of a Sustained‐Release Theophylline Tablet |
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The Journal of Clinical Pharmacology,
Volume 22,
Issue 4,
1982,
Page 196-200
NORMAN H. LEEDS,
PETER GAL,
ANAL A. PUROHIT,
JONNE B. WALTER,
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摘要:
Abstract:The effect of food on the bioavailability, time to peak level, and pattern of release of a sustained‐release theophylline preparation was examined in six normal volunteers. The average bioavailability for the 100‐ and 300‐mg tablets was 98 ± 0.03% (S.E.M.). This is consistent with previously published data. Food decreased measured theophylline concentration during the first 4 hours for the 100‐mg tablets and at the fourth‐hour sample following the 300‐mg tablets. The decreased rate of absorption resulted in a shift of the absorption curve to the right with a delay in the time to peak level. Peak serum concentrations for tablets given with a meal occurred 6 hours after the 100‐mg tablets and 8 hours after the 300‐mg tablets, as opposed to 4 and 6 hours, respectively, for tablets in the fasting state. The release pattern of the theophylline preparation approximated zero‐order kinetics for all fasting a
ISSN:0091-2700
DOI:10.1002/j.1552-4604.1982.tb02162.x
出版商:Blackwell Publishing Ltd
年代:1982
数据来源: WILEY
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9. |
Serum Binding of Diltiazem in Humans |
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The Journal of Clinical Pharmacology,
Volume 22,
Issue 4,
1982,
Page 201-205
D. C. BLOEDOW,
R. W. PIEPHO,
A. S. NIES,
J. GAL,
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摘要:
Abstract:Diltiazem binding was measured by equilibrium dialysis in the serum of five healthy male subjects, aged 22 to 34 years, at seven serum diltiazem concentrations ranging from 0.03 to 2.06 μg/ml. The percentage of unbound diltiazem ranged from 19.6 ± 3.1 to 22.6 ± 4.1 (mean ± S.D.) and was independent of serum diltiazem concentration. Serum diltiazem binding was also examined in the presence of six drugs that might be used concurrently with diltiazem in patients being treated for cardiac disease. The percentage of unbound diltiazem was not influenced by digoxin, hydrochlorothiazide, phenylbutazone, propranolol, salicylic acid, or warfarin at therapeutic concentrations of these drugs over the therapeutic range of diltia
ISSN:0091-2700
DOI:10.1002/j.1552-4604.1982.tb02163.x
出版商:Blackwell Publishing Ltd
年代:1982
数据来源: WILEY
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10. |
Pharmacokinetics of Hydroxyethyl Starch in Normal Subjects |
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The Journal of Clinical Pharmacology,
Volume 22,
Issue 4,
1982,
Page 206-212
AVRAHAM YACOBI,
ROGER G. STOLL,
CHECK Y. SUM,
CHII‐MING LAI,
SURINDER D. GUPTA,
JAMES D. HULSE,
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摘要:
Abstract:To determine the elimination of high‐molecular‐weight hydroxyethyl starch (HES,Mw450,000) in normal subjects, ten volunteers were given 500 ml 6% HES solution by intravenous infusion, and serial blood and urine samples were collected for nonglucose total carbohydrate determination. On the average, 46 and 64 per cent of the dose was excreted in the urine within two and eight days, respectively. The plasma concentration declined rapidly during the first week after infusion. The average terminal half‐life was 17 days during the first 42 days, which accounted for elimination of about 90 per cent of the dose. The remainder was eliminated with a terminal half‐life of 48 days determined between days 42 and 83 of the study. As expected, the infusion of HES resulted in plasma volume expansion over a 48‐hour period during which time levels of nonglucose carbohydrates were above 3.5 mg/ml. HES is metabolized by α‐amylase in the body. During the first 48 hours after infusion of HES, plasma α‐amylase activity was significantly increased over control. Concomitantly, α‐amylase activity in urine was also elevated but no
ISSN:0091-2700
DOI:10.1002/j.1552-4604.1982.tb02164.x
出版商:Blackwell Publishing Ltd
年代:1982
数据来源: WILEY
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