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Captopril hypertension treatment

Hydroxy-isobutyric acid 2 Captopril Treatment for hypertension Hydroxylation Candida rugosa Single-stage fermentation [4]... [Pg.230]

Autoantibodies to red blood cells and autoimmune hemolytic anemia have been observed in patients treated with numerous drugs, including procainamide, chlor-propaminde, captopril, cefalexin, penicillin, and methyldopa (Logue et al., 1970 Kleinman et al., 1984). Hydralazine- and procainamide-induced autoantibodies may also result in SLE. Approximately 20% of patients administered methyldopa for several weeks for the treatment of essential hypertension developed a dose-related titer and incidence of autoantibodies to erythrocytes, 1% of which presented with hemolytic anemia. Methlydopa does not appear to act as a hapten but appears to act by modifying erythrocyte surface antigens. IgG autoantibodies then develop against the modified erythrocytes. [Pg.558]

Peptidyl-dipeptidase A (angiotensin-I converting enzyme, ACE, EC 3.4.15.1) plays a pivotal role in the control of blood pressure [80]. It has been established that its active site contains an essential Zn-atom that functions like that of carboxypeptidase A [2], ACE is inhibited by peptides having a proline or aromatic amino acid at the C-terminal position. These observations as well as the similarities with the active site of carboxypeptidase A have allowed a rational design of effective inhibitors of ACE (e.g., captopril (3.4) and enalapril (3.5)) used in the treatment of hypertension [81]. [Pg.83]

Captopril (Capoten, Bristol-Myers Squibb) angiotensin converting enzyme (ACE) inhibitor for the treatment of hypertension... [Pg.35]

Captopril, as well as other ACE inhibitors, is indicated in the treatment of hypertension, congestive heart failure, left ventricular dysfunction after a myocardial infarction, and diabetic nephropathy. In the treatment of essential hypertension, captopril is considered first-choice therapy, either alone or in combination with a thiazide diuretic. Decreases in blood pressure are primarily attributed to decreased total peripheral resistance or afterload. An advantage of combining captopril therapy with a conventional thiazide diuretic is that the thiazide-induced hypokalemia is minimized in the presence of ACE inhibition, since there is a marked decrease in angiotensin Il-induced aldosterone release. [Pg.212]

An important class of orally active ACE inhibitors, directed against the active site of ACE, is now extensively used. Captopril and enalapril are examples of the many potent ACE inhibitors that are available. These drugs differ in their structure and pharmacokinetics, but in clinical use, they are interchangeable. ACE inhibitors decrease systemic vascular resistance without increasing heart rate, and they promote natriuresis. As described in Chapters 11 and 13, they are effective in the treatment of hypertension, decrease morbidity and mortality in heart failure and left ventricular dysfunction after myocardial infarction, and delay the progression of diabetic nephropathy. [Pg.378]

Peptides with C-terminal phosphonates, initially reported to have antibacterial properties, have also been found to possess inhibitory properties toward serine proteases)28 The synthesis of peptide phosphonates (Section 15.1.8) usually requires protection of the phos-phonic moiety as a diester, followed by selective deprotection in the final stage. The importance of peptide thiols (Section 15.1.9) is exemplified by captopril, an orally active angiotensin converting enzyme inhibitor used as a treatment for hypertension)29 These peptide thiols are prepared by the reaction of sulfanylalkanoyl amino acids with a-amino esters followed by deprotection of carboxy and sulfanyl groups. Other peptide thiols have been reported to be inhibitors of zinc metalloproteases, collagenases, and aminopeptidases. [Pg.3]

Fig. 1.3 Effect of captopril and losartan treatment on blood pressure and the expression of Gia proteins in different models of hypertensive rats (HR). Twelve-week-old SHR and age-matched WKY rats, 1 kidney 1 clip hypertensive rats (1K-1C HR) were treated with captopril (150mg/kg body wt/day) as described earlier (Pandey and Anand-Srivastava 1996 Ge et al. 1999), whereas L-NAME-induced hypertensive rats were treated with losartan (lOmg/kg body wt/day) as described earlier (Hashim and Anand-Srivastava 2004). The blood pressure was monitored by the tail cuff method. The expression of Gia-2 and Gia-3 protein in heart from SHR and L-NAME HR and aorta from 1K-1C HR were determined by Western blotting using antidodies AS/7 and EC/1 against Gia-2 and Gia-3 protein, respectively. The blots are representative of three or four separate experiments. P < 0.01, P < 0.001 versus control/WKY, tt/> < 0.01, mP < 0.001 versus SHR/1K-1C/L-NAME. Fig. 1.3 Effect of captopril and losartan treatment on blood pressure and the expression of Gia proteins in different models of hypertensive rats (HR). Twelve-week-old SHR and age-matched WKY rats, 1 kidney 1 clip hypertensive rats (1K-1C HR) were treated with captopril (150mg/kg body wt/day) as described earlier (Pandey and Anand-Srivastava 1996 Ge et al. 1999), whereas L-NAME-induced hypertensive rats were treated with losartan (lOmg/kg body wt/day) as described earlier (Hashim and Anand-Srivastava 2004). The blood pressure was monitored by the tail cuff method. The expression of Gia-2 and Gia-3 protein in heart from SHR and L-NAME HR and aorta from 1K-1C HR were determined by Western blotting using antidodies AS/7 and EC/1 against Gia-2 and Gia-3 protein, respectively. The blots are representative of three or four separate experiments. P < 0.01, P < 0.001 versus control/WKY, tt/> < 0.01, mP < 0.001 versus SHR/1K-1C/L-NAME.
Converting enzyme (ACE) inhibitors 176) likewise prevent the formation of angiotensin II and are used in the treatment of renal and essential hypertension. Examples of orally active ACE-inhibitors are (2)-l-[(2S)-3-[N-(S)-mercapto-2-methylpro-panoyl]proline170) (captopril 77), l-[N-(S)-l-carboxy-3-phenylpropyl]-L-alanyl-L-proline-1 -ethyl ester177 (enalapril 78), and 2-[N-[(S)-l-ethoxycarbonyl-3-phenyl-propyl]-L-alanyl]-(lS,3S,5S)-2-azabicyclo[3.3.0]octane-3-carboxylic acid178) (Hoe 498 79). [Pg.136]

Today, captopril (Capoten ) ranks among the most frequently used drugs in the treatment of hypertension. Enalapril (Xanef ) has been commercially available since 1985 as a second ACE inhibitor. The discovery of captopril started an avalanche of research into the synthesis of angiotensin-converting enzyme inhibitors. Some new developments should be mentioned at this point ... [Pg.137]

The discovery of teprotide led to a search for new, specific, orally active ACE inhibitors. Ondetti et al. (172) proposed a hypothetical model of the active site of ACE, based on analogy with pancreatic carboxypeptidase A, and used it to predict and design compounds that would occupy the carboxy-terminal binding site of the enzyme. Carboxyalkanoyland mer-captoalkanoyl derivatives of proline were found to act as potent, specific inhibitors of ACE and 2-D-methyl-3-mercaptopropanoyl-L-proline (131) (captopril) was developed and launched in 1981 as an orally active treatment for patients with severe or advanced hypertension. Captopril, modeled on the biologically active peptides found in the venom of the pit viper, made an important contribution to the understanding of hypertension and paved the... [Pg.881]

One of the most successful drugs of recent years is captopril [l-(3-mercapto-2-(S)-methyl-l-oxopropyl)-(S)-proIine] [6]. It is an inhibitor of the angiotensin-converting enzyme and is widely used for the treatment of hypertension and congestive heart failure. The stereochemical purity of captopril was investigated after esterification and acylation by enantio-selective gas chromatography using a XE-60-L-val-(S)-a-phenylethyI-amide column (43). [Pg.120]

Perlman JM, Volpe JJ. Neurologic complications of captopril treatment of neonatal hypertension. Pediatrics 1989 83(l) 47-52. [Pg.235]

An 86-year-old man, who was taking captopril 25 mg bd and bendroflumethiazide 25 mg/day for hypertension, had a transurethral resection of the prostate under spinal anesthesia, and developed profound bradycardia and hypotension with disturbances of consciousness during transfer to the recovery room (18). Initial treatment with atropine produced rapid improvement in cardiovascular and cerebral function. A further hypotensive episode, without bradycardia, occurred about 1 hour later, but responded rapidly to methoxamine. He made a full recovery overnight. [Pg.626]

Ortega G, Molina Boix M, Vidal JB, de Paco M, del Bano MD, Ruiz F. Tratamiento con captopril de la hipertension arterial en la nefropatia lupica. [Treatment of arterial hypertension with captopril in lupus nephropathy.] An Med Interna 1992 9(2) 72-5. [Pg.627]


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See also in sourсe #XX -- [ Pg.5 , Pg.26 , Pg.43 ]




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