Angiotensin converting enzyme inhibitors: Comparative structure, pharmacokinetics, and pharmacodynamics

Thind, Gurdarshan S.

doi:10.1007/bf01857634

Cited by 43 publications

(19 citation statements)

References 45 publications

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“…However, some studies have sub-grouped these drugs for analytical purposes according to their penetrance of the blood brain barrier (BBB) which would be expected to be important for diseases such as AD, but there are conflicting reports on the penetration of some ACE-Is (Jackson et al 1987;Gohlke et al 1989;Cushman et al 1989;Tan et al 2005), questioning the validity of this manner of sub-grouping ). Instead, in the present study, we opted to subgroup drugs according to their chemical structures, which offers less ambiguity in some respects, although the potential for differential pharmacological profiles remains (Thind 1990;Ranadive et al 1992). Our rationale is supported by evidence that the sulfhydryl containing molecules (e.g., captopril) have beneficial antioxidant properties (Westlin and Mullane 1988), but that sulfhydryl containing drugs tend to have similar clinical adverse reactions (Jaffe 1986) which bias prescription rates in some groups.…”

Section: Introductionmentioning

confidence: 99%

Angiotensin-converting enzyme inhibitors and incidence of mild cognitive impairment. The Italian Longitudinal Study on Aging

Solfrizzi

Scafato

Frisardi

et al. 2011

AGE

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Midlife elevated blood pressure and hypertension contribute to the development of Alzheimer's disease (AD) and overall dementia. We sought to estimate whether angiotensin-converting enzyme AGE (2013) inhibitors (ACE-Is) reduced the risk of developing mild cognitive impairment (MCI) in cognitively normal individuals. In the Italian Longitudinal Study on Aging, we evaluated 1,445 cognitively normal individuals treated for hypertension but without congestive heart failure from a population-based sample from eight Italian municipalities with a 3.5-year follow-up. MCI was diagnosed with current clinical criteria. Dementia, AD, and vascular dementia were diagnosed based on DSM-IIIR criteria, NINCDS-ADRDA criteria, and ICD-10 codes. Among 873 hypertensiontreated cognitively normal subjects, there was no significant association between continuous exposure to all ACE-Is and risk of incident MCI compared with other antihypertensive drugs [hazard ratio (HR), 0.45, 95% confidence interval (CI), 0.16-1.28]. Captopril exposure alone did not significantly modify the risk of incident MCI (HR, 1.80, 95% CI,). However, the enalapril sub-group alone (HR, 0.17, 95% CI, 0.04 -0.84) or combined with the lisinopril sub-group (HR, 0.27, 95% CI, 0.08-0.96), another ACE-I structurally related to enalapril and with similar potency, were associated with a reduced risk of incident MCI. Study duration exposure to ACE-Is as a "class" was not associated with incident MCI in older hypertensive adults. However, within-class differences linked to different chemical structures and/or drug potencies may exist, with a possible effect of the enalapril and lisinopril sub-groups in reducing the risk of incident MCI.

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Section: Introductionmentioning

confidence: 99%

Angiotensin-converting enzyme inhibitors and incidence of mild cognitive impairment. The Italian Longitudinal Study on Aging

Solfrizzi

Scafato

Frisardi

et al. 2011

AGE

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“…The handout for this lesson and all lessons in the chemical basis of drug action course sequence is based on a thorough literature search of major medicinal chemistry textbooks, [15][16][17] therapeutics textbooks 18,19 and primary literature. [20][21][22][23][24] Students are also referred regularly to review their notes and textbooks in anatomy, physiology, biochemistry, microbiology, and pharmacology. Introduction.…”

Section: Designmentioning

confidence: 99%

Medicinal Chemistry and Therapeutic Relevance of Angiotensin-Converting Enzyme Inhibitors

Alsharif¹

2007

Am J Pharm Educ

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Chemical Basis of Drug Action (PHA337 and PHA447) is a required 2-semester course sequence taught to second-professional year pharmacy students at Creighton University in both the campus and distance-education pathways. The course emphasizes integration of previous content, critical thinking, and therapeutic relevance. The content and learning experiences are organized to transition the students' thinking through a constructive process that provides ample opportunities to recall and integrate previous knowledge, learn and apply new knowledge, establish a logical connection between the science and its therapeutic relevance, and finally to apply the science knowledge to predict clinical activity and clinical outcomes as can be expected in a patient. This manuscript is based on the angiotensin converting enzyme inhibitors as an illustration of how our course objectives are accomplished.

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“…Hence, drugs with high lipophilicity may facilitate increased inhibition of tissue ACE. In addition, most ACE inhibitors are prodrugs that exist in an esterified form to improve absorption 50,51 . Harrigan et al compared the in vitro effects of prodrug concentration on the potency of ACE inhibitor metabolites 52 .…”

Section: Specific Differences Between Ace Inhibitorsmentioning

confidence: 99%

Heart Failure and First Dose Hypotension After Angiotensin Converting Enzyme Inhibitors

Vítovec¹,

Špinar²

2004

Biomed Pap Med Fac Univ Palacky Olomouc Czech Repub

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The first-dose induced decrease in blood pressure in some patients following the administration of ACE inhibitors is a fact causing some concern among clinicians prescribing these drugs. However, an overview of clinical trials and the authors' own experience clearly point to the possibility of reducing the incidence and/or severity of first-dose hypotension. Apart from appropriate clinical measures to be taken, the choice of the ACE inhibitor seems to be of crucial importance as some (fosinopril, perindopril) produce less hypotension than others. Thus, with due circumspection, ACE inhibitors can safely retain their position as the cornerstone of the treatment of chronic heart failure.First-dose hypotension has been recognized as a potential limiting factor in the use of ACE inhibitors in the treatment of chronic heart failure (CHF) and after acute myocardial infarction (AMI). Concerns regarding firstdose hypotension may increase the risk of renal, myocardial, or cerebral hypoperfusion that may result. The incidence of first-dose hypotension after ACE inhibitors reported in large clinical trials is small, varying from 0.7 % in the SAVE trial to 13.3 % in the OPTIMAAL trial 1,2 . This variation reflects differences in study design, in patient selection, in the definition of first-dose hypotension, and in drug selection. The major reason for the low number of these events reported is a very infrequent use of ambulatory blood pressure monitoring, and thus the incidence of less than 10 % reflects only symptomatic or casually measured hypotension. A number of smaller trials have reported a much higher incidence of first-dose hypotension, affecting as many as one third of the patients. SYMPTOMS OF FIRST-DOSE HYPOTENSIONThe most frequently reported symptoms of drug-induced hypotension are those related to cerebral hypoperfusion. These include light headiness, dizziness, headache, general weakness and visual disturbances 3 . In elderly patients, drug-induced hypotension has also been associated with falling. Several studies conducted in the community and in long-term residential care facilities have found drug-induced hypotension to be the primary cause of falling in both fit and frail elderly patients [4][5][6] . The clinical consequences of first-dose hypotension assume particular relevance in this patient population because the compensatory circulatory response to hypotensive stimuli, pre-existing vascular disease or both declines with age 7,34 . With more severe first-dose hypotension, the subsequent drop in cerebral blood flow can lead to a sudden brief loss of consciousness (syncope), often accompanied by bradycardia 8 . This may be especially dangerous in patients with heart failure. The incidence of syncope following initiation of an ACE inhibitor appears to have decreased dramatically over the last decade to between 0.5 and 2.2 %, although this may reflect changes in reporting practices 9,10 . Many clinicians continue to monitor closely the response to the first dose of an ACE inhibitor in patients with grade 3 ...

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Angiotensin converting enzyme inhibitors: Comparative structure, pharmacokinetics, and pharmacodynamics

Cited by 43 publications

References 45 publications

Angiotensin-converting enzyme inhibitors and incidence of mild cognitive impairment. The Italian Longitudinal Study on Aging

Angiotensin-converting enzyme inhibitors and incidence of mild cognitive impairment. The Italian Longitudinal Study on Aging

Medicinal Chemistry and Therapeutic Relevance of Angiotensin-Converting Enzyme Inhibitors

Heart Failure and First Dose Hypotension After Angiotensin Converting Enzyme Inhibitors

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