Drugs online research references
Am J Physiol. 1992 Oct;263(4 Pt 1):G466-73.
Rat intestinal angiotensin-converting enzyme: purification, properties, expression, and function.
Erickson RH, Suzuki Y, Sedlmayer A, Song IS, Kim YS.
Gastrointestinal Research Laboratory, Department of Veterans Affairs Medical Center, San Francisco, California 94121.
Angiotensin-converting enzyme [ACE (peptidyl-dipeptidase A, EC 3.4.15.1)] was purified from a total cell membrane fraction of rat intestinal mucosa. A 4,500-fold purification was achieved after affinity chromatography with lisinopril-Sepharose and gel filtration. The final preparation was judged to be homogenous by sodium dodecyl sulfate-polyacrylamide gel electrophoresis with an apparent molecular weight of 160,000. The purified protein is a glycoenzyme containing 12% N-linked carbohydrate. Purified ACE had a specific activity of 65 U/mg protein with benzoyl-Gly-His-Leu as substrate. A kinetic analysis showed that the enzyme had the maximal velocity with substrates containing proline at the COOH-terminal end. Inhibitor studies indicated that the enzyme is a metalloprotein. Along the proximal-distal axis of the small intestine, ACE activity is most predominant in the proximal to middle portions, decreasing toward the distal end. This pattern was also observed for ACE mRNA and protein, suggesting that ACE expression is controlled at the level of mRNA. Perfusion of benzoyl-Gly-His-Leu in vivo through a segment of intestinal jejunum demonstrated that ACE is an important intestinal dipeptidyl carboxypeptidase, participating in the digestion and assimilation of dietary peptides.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=1329552&dopt=Abstract
J Hum Hypertens. 1989 Jun;3 Suppl 1:177-86.
Clinical experience with lisinopril. Observations on safety and tolerability.
Cameron HA, Higgins TJ.
Medical Research, ICI Pharmaceuticals, Macclesfield, UK.
The safety and tolerability of lisinopril (1.25-160 mg daily) were assessed in 3,270 patients (2,688 hypertensives and 582 patients with congestive heart failure (CHF] and 280 healthy subjects. The duration of therapy ranged from a single dose to 43 months; 438 patients received lisinopril for at least 12 months (mean 20 months). In the hypertensive population, the most frequent adverse events reported were headache, dizziness, cough, nausea, diarrhoea and fatigue, although not all of these events were thought to be related to lisinopril; 6.1% discontinued lisinopril due to adverse clinical events, most commonly cough and nausea. Twelve hypertensive patients died (0.45%), but most of these were not receiving lisinopril at the time of death and none was considered to be drug-related. In CHF patients, the most frequently reported adverse events were dizziness, dyspnoea, diarrhoea, hypotension and fatigue. Again, not all of these reports were considered to be drug-related. Therapy was withdrawn in 9.6% of patients--hypotension, dizziness, diarrhoea and rash being the most frequent reasons. Fifty-three CHF patients died (9.1%) and in three cases death was considered to be related to lisinopril therapy. Hypotension, orthostatic effects or dizziness following the initial dose of lisinopril occurred infrequently (in 1.3% of the hypertensive group, including those receiving hydrochlorothiazide, and in 4.8% of CHF patients). Changes in laboratory parameters were generally minor and seldom resulted in discontinuation of therapy. Long-term treatment of hypertension and CHF with lisinopril for at least 3 years confirms that the drug is well tolerated. Overall, the side-effect profile is very similar to that of other ACE inhibitors with regard to class-specific effects. However, taste disturbance was rarely observed.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=2550641&dopt=Abstract
Pol Tyg Lek. 1993 Jan 18-25;48(3-4):77-9.
[Effect of captopril and lisinopril on adrenergic receptor density and serum norepinephrine and epinephrine in patients with congestive heart disease]
[Article in Polish]
Halawa B.
Katedry i Kliniki Kardiologii AM, Wroclawiu.
Density of beta-adrenergic receptors in the lymphocytes, alpha 1- and alpha 2-adrenergic receptors in blood platelets, as well as blood serum norepinephrine levels have been assessed in 49 patients with congestive heart failure prior to, and 7 and 14 days of captopril and lisinopril administration. A decrease in beta-, alpha 1-, and alpha 2-adrenergic receptors density, an increase in blood serum norepinephrine, and normal epinephrine levels have been noted in these patients. A 7-day treatment with captopril, and a 14-day treatment with lisinopril have increased adrenergic receptors density, and decreased blood serum norepinephrine levels.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=8395686&dopt=Abstract
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