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Urology
Published in David A Lisle, Imaging for Students, 2012
For other specific indications, modifications to renal scintigraphy may be used as follows: Diuresis renogram Renal scintigraphy with injection of furosemideIndication: differentiation of mechanical urinary tract obstruction from non-obstructive hydronephrosis (Fig. 5.1)Angiotensin-converting enzyme (ACE) inhibitor renogram Renal scintigraphy with injection of captoprilIndication: screening test for renal artery stenosis in suspected renovascular hypertension.
Drug-induced acute upper airway obstruction
Published in Philippe Camus, Edward C Rosenow, Drug-induced and Iatrogenic Respiratory Disease, 2010
Michael Lippmann, Ganesan Murali
The hypothesized mechanism of ACEI angioedema is the inhibition of bradykinin degradation by the drug, which acts as a kininase II inhibitor, as kininase II is identical to angiotensin-converting enzyme. The resulting increase in circulating bradykinin leads to a vasodilatory state, altering capillary permeability and leading to oedemagenesis, increased postcapillary venule pressure with the release of other vasoactive peptides.2,21 In addition there may be genetic factors such as a deficiency of other bradykinin-metabolizing enzymes such as carboxypeptidase-N and aminopeptidase-P.13 Nussberger et al. measured bradykinin levels in patients with hereditary angioedema, acquired angioedema, and one patient with angioedema due to captopril.37 Levels all rose during an acute attack of angioedema in all conditions, with the level rising 15-fold in the ACEI-induced cases, falling back to normal after drug withdrawal. In a subsequent paper the same authors described four additional patients with ACEI-induced angioedema, three of whom had elevated bradykinin levels during remission.16,38 Anderson and deShazo studied the cutaneous wheal and flare response to bradykinin, histamine and codeine in 10 normal subjects following the ingestion of the ACEI captopril.39 Five of the 10 patients developed flushing after the bradykinin skin test. They concluded that inhibition of bradykinin metabolism by ACEI is the cause of angioedema and not substance P where an expected increase in wheal and flare to histamine and codeine would have occurred. All these studies support the proposed mechanism of ACEI-induced angioedema outlined in Fig. 7.1.
Antihypertensive Drugs: Controlling Blood Pressure
Published in Richard J. Sundberg, The Chemical Century, 2017
The first group of ACE inhibitors was designed by taking advantage of deductions about the ACE active site. This was done prior to availability of any crystallographic information. A simple compound, N-succinoylproline, showed weak but specific inhibitory activity and was the starting point. Introduction of a thiol group at a point consistent with interaction of a Zn2+ ion at the active site led to a dramatic increase in activity. These studies at Squibb in Princeton, NJ, USA eventually led to captopril, the first clinically used ACE inhibitor.6 It was introduced in 1980.
Rhodium catalysis in the synthesis of fused five-membered N-heterocycles
Published in Inorganic and Nano-Metal Chemistry, 2020
Navjeet Kaur, Neha Ahlawat, Yamini Verma, Pranshu Bhardwaj, Pooja Grewal, Nirmala Kumari Jangid
The compounds from the heterocyclic family have their different applications biologically, chemically as well as industrially. These heterocycle structures are widely distributed in biologically-active products, serves as important pharmacophores for many therapeutic agents, and heterocycles are common fragments of most marketed drugs. This reflects the central role that heterocycles play in modern drug design. Heterocyclic compounds and majorly nitrogen containing heterocyclic compounds are very important concepts in the field of applied and pure chemistry. Advancements in new synthetic techniques, extraction from natural sources, exploring new applications of heterocyclic compounds in the field of pharmacy, chemistry, industry or medicine are the prime areas of research.[1–4] Other than the copiousness of heterocyclic compounds in organic chemistry, varied application of these in the field of biology, technology and chemistry make them extremely significant. Varied compounds like anti-biotics, alkaloids, vitamins, essential amino acids, hormones, hemoglobin, and many dyes and synthetic drugs contain heterocycles as their basic molecular framework. Because of their biological importance, the advancements in the synthetic methodologies for nitrogen bearing heterocyclic compounds and their fused scaffolds is considered to be the most emerging area in modern drug discovery and design.[5,6] Since many years, nitrogen containing heterocycles are used as medicinal compounds, and are the basis of many drugs like Captopril (hypertension), Morphine (analgesic), and Vincristine (cancer chemotherapy).[7–9]