Drug Discovery

Maxwell, Robert A.; Eckhardt, Shohreh B.

doi:10.1007/978-1-4612-0469-5

Cited by 40 publications

(8 citation statements)

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“…He proposed a hypothetical model of the active site of ACE and used it to predict and design compounds that would occupy the carboxy-terminal binding site of the enzyme captopril, a specific potent inhibitor of ACE. Clinical trials showed excellent anti-hypertensive properties and these results had a major impact on the treatment of cardiovascular disease [11]. The first demonstration of an orally active ACE inhibitor was made on 31 March 1975, when the succinyl group was replaced with a derivative of cysteine, increasing inhibitory potency about 2,000-fold because sulphhydryl of cysteine bound with zinc more tightly than the carboxyl of succinyl.…”

Section: Historymentioning

confidence: 99%

Interaction Studies of ACE Inhibitors with Statins

Sattar¹

2015

Hypercholesterolemia

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Hypercholesterolemia 204 tissue distribution. All ACE inhibitors have a similar antihypertensive efficacy -they effectively block the conversion of angiotensin 1 to angiotensin II -and all have similar therapeutic indications, adverse effect profiles and contraindications. Mechanism of actionThese inhibitors block the converting enzyme of angiotensin, which is responsible for cleavage from angiotensin I, which is decapeptide, to angiotensin II, which is octapeptide [17,18], and lower the BP by reducing PVR (peripheral vascular resistance). They also decrease aldosterone secretion and the resulting sodium and water retention. PharmacokineticsThe oral bioavailability of ACE inhibitors ranges from 13% to 95% [19,20]. Most ACE inhibitors are administered as pro-drugs that remain inactive until esterified in the liver [21]. Pharmakokinetic characteristics of different ACE inhibitors are given in Therapeutic useACE inhibitors are effective in patients with mild to moderately severe hypertension, normal or low plasma renin activity, collagen vascular disease and cardiovascular disease [22,23]. They are also used in the prevention and treatment of myocardial infarction [24,25] and in the management of cardiac arrhythmias [26]. They can decrease the progression of atherosclerosis, microalbuminuria and diabetic retinopathy, and produce a beneficial effect in patients with Bartter's syndrome [27]. Adverse effectsACE inhibitors have a relatively low incidence of side effects and are well tolerated; however, dry cough is common, appearing in 10-30% of patients. This appears to be related to the elevation in bradykinin [28][29][30]. Hypotension is seen especially in patients with heart failure [31], angiooedema (life-threatening airway swelling and obstruction; 0.1-0.2% of patients) and hyperkalaemia. ACE inhibitors are contraindicated in pregnancy, in the first trimester associated with a risk of major congenital malformations, particularly affecting the cardiovascular and central nervous systems [32]. The most common (≥1% of patients) adverse effects HMG-CoA reductase inhibitors (statins)3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase inhibitors (statins) are the most effective among all hypolipidaemic agents [50]. These lipid-lowering drugs are increasingly used for primary and secondary hindrance of cardiovascular disease [51]; they have only been recognized for treatment of hyperlipidaemia. In clinical studies, statins are highly effective in enhancing HDL levels while reducing total cholesterol, LDL cholesterol, apolipoprotein B and triglyceride levels.The normal treatment regimen for these drugs involves daily exposure over a period of many years [52,53]. They have also been examined in combination with cures of multiple sclerosis, osteoporosis, Alzheimer's disease and dropping the superfluous increased occurrence in CHD in women on HRT treatment [54]. They have anti-thrombogenic, anti-inflammatory and anticoagulant properties [55,56]. These therapeutic properties are independent of lipid lowering [57], an...

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Section: Historymentioning

confidence: 99%

Interaction Studies of ACE Inhibitors with Statins

Sattar¹

2015

Hypercholesterolemia

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“…13 Visher, Schneider, Wathington, and Collado (2010); ; ; . 14 Scrivener et al (2008); Weissman et al (2011). ic achievement. Popular strategies include tutoring --which can be provided by faculty, staff, or student peers or through computer-assisted instruction with tutorial software packages -and supplemental instruction, a more structured tutoring model that is connected directly with a particular course.…”

Section: Student Supportsmentioning

confidence: 99%

“…However, early data showed that the college grade point averages (GPAs) of College Now students were comparable to those of a national sample of freshmen. 18 More recently, comparison studies of CUNY's College Now program found that it had small but statistically significant benefits for students who matriculated at a CUNY 14 Kleiman (2001). 15 Golann and Hughes (2008).…”

Section: Research Evidence Supporting Dual Enrollment Programsmentioning

confidence: 99%

“…While different versions of mainstreaming exist, common practices include offering a college-level course with a modified curriculum over a lengthier period of time (usually two semesters) or 14 Epper and Baker (2009). 15 Bassett (2009).…”

Section: Mainstreaming Into College-level Coursesmentioning

confidence: 99%

“…13 Experimental studies have also found positive impacts on students' achievement and persistence in school; learning communities programs that link a developmental math or developmental English class with a college-level course have resulted in improvements in the number of credits earned and in students' progression through developmental education. 14 However, these effects tended to diminish after the programs ended. These results should be considered a more definitive characterization of learning communities, given the strong research models used to document these effects.…”

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confidence: 99%

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