Drugs online research references
Am J Cardiol. 1989 Jul 1;64(1):50-5.
Changes in dyspnea-fatigue ratings as indicators of quality of life in the treatment of congestive heart failure.
Feinstein AR, Fisher MB, Pigeon JG.
Yale University School of Medicine, New Haven, Connecticut 06510.
A new clinical index of dyspnea and fatigue has been applied to rate the condition of patients with congestive heart failure. The index has 3 components, each rated on a scale from 0 to 4, for the magnitude of the task that evokes dyspnea or fatigue, the magnitude of the pace (or effort) with which the task is performed and the associated functional impairment in general activities. The ratings for each component are added to form an aggregated score, which can range from 0, for the worst condition, to 12, for the best. Because dyspnea and fatigue are prime symptoms and sources of clinical distress, the index helps reflect the quality of life in patients with congestive heart failure. In double-blind trials of therapy, changes in the index showed good correlations with patients' self-selected ratings of improvement. The posttherapeutic changes in the index ratings were significantly higher with a new active agent (lisinopril) than with placebo or another active agent (captopril).
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=2545092&dopt=Abstract
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Nippon Yakurigaku Zasshi. 1989 Apr;93(4):219-24.
[Inhibitory effect of N-alpha-[(S)-1-carboxy-3-phenylpropyl]-L-lysyl-L-proline (MK-0521) on angiotensin converting enzyme in vitro]
[Article in Japanese]
Ino Y, Oda M, Sato T, Iwaki M.
Research Laboratories, Torii & Co., Ltd., Chiba, Japan.
N-alpha-[(S)-1-carboxy-3-phenylpropyl]-L-lysyl-L-proline (MK-0521) is a new non-sulfhydryl-containing angiotensin converting enzyme (ACE) inhibitor. The present investigation describes its ACE and other enzymes inhibitory properties and compares it to those of captopril, MK-421 and MK-422 in vitro. MK-0521 inhibited rat pulmonary ACE by 50% (IC50) at a concentration of 3 nM and was 6.13 times more potent than captopril. The IC50 values of MK-421 and MK-422 against ACE were 2,000 nM and 3.5 nM, respectively. MK-0521 had practically no inhibitory activities against carboxypeptidase A, carboxypeptidase B, leucine aminopeptidase, papain, pepsin and trypsin. The kinetic study on the inhibitory activity of M-0521 against ACE using Lineweaver-Burk plots indicated that MK-0521 exerted competitive ACE inhibition. The dialysis study conducted on the ACE-MK-0521 complex revealed that the inhibitory effect of MK-0521 against ACE was reversible. In the guinea pig ileum, MK-0521 potentiated the contractile effect of bradykinin and depressed the contractile effect of angiotensin I. These effects on bradykinin and angiotensin I were 33.11 and 2.63 times more potent than that of captopril, respectively. The present results suggest that MK-0521 may show a potent hypotensive effect in vivo.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=2545578&dopt=Abstract
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Nippon Yakurigaku Zasshi. 1989 Apr;93(4):225-34.
[Angiotensin converting enzyme inhibitory activity of MK-0521 in vivo and antihypertensive effect of its single oral administration on blood pressure and effect on the renin-angiotensin system in 2-kidney Goldblatt hypertensive dogs]
[Article in Japanese]
Oda M, Ino Y, Suzuki K, Sato T, Iwamoto S, Iwaki M.
Research Laboratories, Torii & Co., Ltd., Chiba, Japan.
Angiotensin converting enzyme (ACE) inhibitory activity of MK-0521 in dogs and the effects of its single oral administration on blood pressure and the renin-angiotensin system in 2-kidney Goldblatt hypertensive dogs were compared with those of captopril and MK-421. MK-0521 at 0.001-0.1 mg/kg, i.v., or 0.01-1 mg/kg, p.o., attenuated the pressor effect of angiotensin I without affecting that of angiotensin II and augmented the depressor effect of bradykinin. The potency of MK-0521 to reduce the pressor effect of angiotensin I was 9.8 times that of captopril by intravenous administration, and by oral administration, it was 15.9-32.1 times that of captopril and approximately 3 times that of MK-421. When administered orally, the onset of action and the time to peak effectiveness were more rapid than those of MK-421, but slower than those of captopril. Duration of the action of MK-0521 was longer than that of captopril and equal or longer than that of MK-421. The inhibition of ACE was well correlated with serum MK-0521 levels. MK-0521 produced a dose-dependent antihypertensive effect in 2-kidney Goldblatt hypertensive dogs at over 0.3 mg/kg, p.o., without affecting the heart rate. The antihypertensive effect of MK-0521 was persistent and approximately 3 times more potent than that of captopril. MK-0521 inhibited the serum ACE activity and increased the plasma renin activity, while it had a tendency to decrease plasma aldosterone level. These changes were parallel to the time course of the antihypertensive effect. These results suggest that the main mechanism of the antihypertensive effect of MK-0521 is the suppression of angiotensin II production due to the inhibition of the ACE.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=2545579&dopt=Abstract
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