Drugs online research references
Scand J Urol Nephrol Suppl. 1984;79:125-7.
Acute hemodynamic and hormonal effects of MK-521 in congestive heart failure.
Dickstein K, Aarsland T, Woie L, Kremer D, Abrahamsen AM.
The acute hemodynamic and hormonal effects of the oral angiotensin converting enzyme (ACE) inhibitor MK-521 were assessed over a period of 96 hours in 6 patients with heart failure. This compound is the lysine analogue of enalapril diacid (MK-422) and is biologically active following absorption. Dosages ranging from 1.25 mg to 5.0 mg were administered on days 1 and 3, followed by 48 hours intensive hemodynamic observation. Marked reduction in mean arterial pressure (25.2%), pulmonary capillary wedge pressure (47.3%), and systemic vascular resistance (34.5%) was observed. Arterial blood was sampled at frequent intervals for angiotensin I (AI), angiotensin II (AII), plasma renin activity, renin substrate, plasma aldosterone, urinary aldosterone, ACE activity, and serum drug levels. Right atrial blood was sampled simultaneously for AI and AII thus permitting reliable assessment of the degree of pulmonary conversion to angiotensin II. Prolonged inhibition of the renin-angiotensin-aldosterone system was confirmed and corresponded to drug concentration. The results indicate hemodynamic efficacy and potent ACE inhibition over a period exceeding 24 hours.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=6089311&dopt=Abstract
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J Hypertens Suppl. 1984 Dec;2(2):S37-42.
Kinetic and metabolic aspects of enalapril action.
Lant AF, McNabb RW, Noormohamed FH.
Enalapril is a long-acting, sulphydryl-free, ACE inhibitor whose humoral and hypotensive effects are maximal at 4-8 h and remain detectable at 24 h after a single dose. Serum profiles after chronic dosing of enalapril show little accumulation of the active diacid metabolite, enalaprilat. Comparison between the observed and predicted steady-state urinary recoveries of enalaprilat yields an effective accumulation half-life of approximately 11 h. In normotensive subjects, enalapril increases renal blood flow whilst leaving glomerular filtration unchanged irrespective of the state of sodium balance. Similarly under conditions of salt loading and salt depletion, a biphasic saluretic response is seen which parallels the excretory maxima for unchanged enalapril (1-2 h) and enalaprilat (4-8 h) suggesting direct interference by the drug moieties with tubular NaCl reabsorption. During the period of maximal enalapril action, uricosuria and phosphaturia are seen, supporting a direct action of enalaprilat on proximal tubular handling of these anions. Detailed documentation of the chronic metabolic effects of enalapril remains incomplete. A small rise in plasma potassium concentrations can occur but overt hyperkalaemia is unlikely in the absence of gross renal failure. Continued dosing is associated with a fall in plasma uric acid concentrations; plasma prolactin concentrations remain unaltered.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=6100875&dopt=Abstract
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Br J Clin Pharmacol. 1982 Sep;14(3):357-62.
Enalapril maleate and a lysine analogue (MK-521): disposition in man.
Ulm EH, Hichens M, Gomez HJ, Till AE, Hand E, Vassil TC, Biollaz J, Brunner HR, Schelling JL.
1 The disposition of two angiotensin converting-enzyme inhibitor drugs was studied in normal volunteers. One drug was enalapril maleate (MK-421), which requires in vivo esterolysis to yield active inhibitor (MK-422). The other was a lysine analogue of MK-422 (MK-521), which requires no bioactivation. 2 Absorption of enalapril maleate (10 mg, p.o.) was rapid, with peak serum concentrations of enalapril observed 0.5-1.5 h after administration. Based upon urinary recovery of total drug (enalapril plus MK-422), absorption was at least 61%. Bioactivation appeared to be largely post-absorptive. From the ratio of MK-422 to total drug in urine, the minimum extent of bioactivation was estimated at 0.7. 3 A similar dose of MK-521 was absorbed more slowly, reaching peak serum concentrations 6-8 h following drug administration. Minimum absorption, based upon urinary recovery, was 29%. 4 Serum concentration v time profiles for both drugs were polyphasic and exhibited prolonged terminal phases. 5 Recovery in urine and faeces of administered enalapril maleate (intact and as MK-422) was 94%. Recovery of MK-521 was 97%. These results indicate lack of significant metabolism of these agents, apart from the bioactivation of enalapril.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=6289858&dopt=Abstract
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