Drugs online research references
Eur J Clin Pharmacol. 1987;32(1):11-6.
Lisinopril in hypertensive patients with and without renal failure.
van Schaik BA, Geyskes GG, Boer P.
Lisinopril (MK521), a lysine analogue of enalaprilic acid, the bioactive metabolite of enalapril, has a longer half-life than enalaprilic acid, and is excreted unchanged in the urine. Its kinetic profile and antihypertensive and hormonal effects have been investigated in an open study in 3 groups each of 6 hypertensive patients, with normal, moderate and severe impairment of renal function. Serum drug level, blood pressure, converting enzyme activity (CEA), plasma renin activity (PRA), aldosterone concentration (PAC), and serum potassium and creatinine were measured during 1 week following a single oral dose and subsequently following 8 daily doses of 5 mg lisinopril. Accumulation of lisinopril was found in the severe renal failure group. CEA was suppressed to less than 10% of its initial value from 4 to 24 h after the initial dose in all three groups, and the suppression was more marked and lasted longer in patients with severe renal failure. An inverse correlation was found in all patients between log serum lisinopril concentration and log CEA. Lisinopril lowered blood pressure in all three groups over 24 h. PRA rose and PAC fell similarly in the groups. Serum potassium increased in the renal failure groups and creatinine remained unchanged in all groups. Thus, when lisinopril 5 mg is given daily to patients with severe renal failure it may accumulate. The high serum lisinopril concentration does not cause an excessive antihypertensive effect. In patients with severe renal failure, adjustment of the dose or the dosing frequency to the degree of renal failure is recommended to avoid administration of doses in excess of those required to achieve adequate inhibition of converting enzyme.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=3034622&dopt=Abstract
word match zestril online literature
Biochem Pharmacol. 1987 Apr 15;36(8):1357-60.
Measurement of angiotensin converting enzyme inhibitors in serum by radioinhibitor binding displacement assay.
Jackson B, Cubela R, Johnston CI.
The principle of enzyme radioinhibitor binding displacement was developed to measure the concentration of angiotensin converting enzyme (ACE) inhibitors in rat serum. 125I MK351A, a tyrosyl derivative of enalaprilic acid, and a potent ACE inhibitor, bound in a concentration and time dependent manner to ACE. Binding of 125I MK351A to rat serum ACE was reduced in a concentration dependent manner in vitro by the ACE inhibitors MK521 (lisinopril), S9780, and Ro 31-3113-000 (Cilazapril diacid). This relationship was used to measure MK521 and S9780 in rat serum four hours after oral gavage with MK521, S9490-3 the prodrug ester of S9780, at 1, 2 and 4 mg/kg, or 1/2 hour after intraperitoneal injection of Ro 31-3113-000 (0.0125-0.7 mg/kg). Serum MK521 concentrations, estimated by radio inhibitor binding displacement, and radioimmunoassay, correlated well (r = 0.94, N = 9, P less than 0.001). Serum MK521, S9780 and Ro 31-3113-000 concentrations measured by radioinhibitor binding displacement assay were dose related, and inversely related to serum ACE enzymatic activity. The radioinhibitor binding displacement assay method using 125I MK351A as a ligand for ACE has application to the measurement of any competitive inhibitor of ACE.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=3036166&dopt=Abstract
word match zestril online literature
Clin Exp Hypertens A. 1987;9(2-3):307-21.
Angiotensin converting enzyme inhibition in plasma and tissues.
Johnston CI, Cubela R, Sakaguchi K, Jackson B.
Angiotensin converting enzyme (ACE) and the ACE inhibitor lisinopril were measured in patients with renal impairment, by both radioinhibitor 125I MK351A binding studies, and by radioimmunoassay. Plasma concentration of lisinopril estimated by radioinhibitor binding displacement correlated closely with that measured by radioimmunoassay. Plateau lisinopril concentration in 8 patients with varying degrees of renal failure treated with 5 mg lisinopril per day for 1 week, was inversely related to renal function. Plasma lisinopril concentrations of 30-70 ng/ml were required for 50% inhibition of plasma ACE activity in vivo. Acute studies in the rat showed inhibition of ACE in different tissues had different time courses. These observations suggest that 125I MK351A binding studies in tissues will be useful in establishing the pharmacokinetic and pharmacodynamic profiles of newer ACE inhibitors, and may help delineate the contribution of ACE in different tissues to cardiovascular homeostasis.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=3038391&dopt=Abstract
word match zestril online literature
Herbs and Pharmaceuticals Online ||
Hair Million herbal formula for hair loss and hair growth ||
Antibiotics and prescription medications online literature ||