Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0010200 (cough)
 23,843 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Benazepril (CGS 14824A HCl) is a new prodrug type angiotensin converting enzyme (ACE) inhibitor. The active form is considered to be benazeprilat, a diacid hydrolyzed compound. Benazepril and benazeprilat inhibited the contraction induced by exposure with angiotensin I, not angiotensin II, in the isolated rabbit aorta. The ACE inhibiting activity of benazeprilat was 1000 times more potent than that of benazepril in this experiment. Benazepril as well as benazeprilat and captopril exerted little influence on norepinephrine, serotonin and high K(+)-induced contraction or bradykinin-induced relaxation in isolated blood vessel preparations, thus angiotensin II synthesis inhibition seemed to be the main cause for its vasodilation. Benazepril, unlike benazeprilat or captopril showed considerable influence on prostaglandin (PG)-induced responses at higher concentrations. The vasocontraction induced by PGF2 alpha was competitively antagonized at 10(-5)-10(-4) mol/l, while vascular responses induced by PGE1, PGE2 or PGI2 was inhibited at 3 x 10(-4) mol/l of benazepril. Although these influences on PGs might not contribute much to its vasodilatory mechanism, the action seemed interesting in relation to cough induction, a known side effect of ACE inhibitors in the market. Benazepril has two asymmetric carbon atoms, thus four optical isomers are possible, SS (benazepril), SR (CGP 14'829A), RS (CGP 42'454A), RR (CGP 42'456A). The SS configuration was the most potent for antagonizing angiotensin I-induced vasocontraction, which seemed to be the best fitted for the ACE molecule.
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PMID:Antihypertensive mechanism of action of the novel angiotensin converting enzyme inhibitor benazepril. Effect on isolated vascular preparations. 208 Sep 46

In a multicenter study in general practice, the tolerability and safety of ramipril alone and in combination with a low dose of furosemide were assessed in moderate hypertension. After a placebo run-in period involving 770 patients, 661 were included in the active treatment period and received ramipril alone (2.5-5 mg/day). After 6 weeks, the nonresponders entered in a double-blind period and they received daily ramipril 10 mg or ramipril 5 mg in combination with furosemide 20 mg. In this hypertensive population, the adverse events more commonly reported were headache, cough, dizziness, asthenia, cramps diarrhea and nausea, but not all these events were related to ramipril. There was seemingly a relation between cough prevalence and rampiril dosage; an increased incidence was also observed during the outbreaks of flu-syndrome in our country. 38 patients discontinued the active treatment due to non-serious adverse events, mainly cough, dizziness or diarrhea. No serious adverse drug reaction was observed. Laboratory data (blood cells count, electrolytes, serum creatinine, fasting blood glucose, apolipoproteins AI and B) remained most commonly unaffected. In moderate hypertension in general practice, this study confirms that ramipril is well tolerated, especially with regard to the class effects of the angiotensin converting enzyme inhibitors.
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PMID:[Tolerance to Triatec in monotherapy and in combination with Lasilix in a French multicenter study]. 214 97

In order to determine the possible role of prostaglandins in the abnormal cough reflex in patients with dry cough, the effects of a cyclooxygenase inhibitor on cough symptoms were examined. This was measured by a cough symptom score and by the cough reflex sensitivity to inhaled capsaicin in a double blind, randomized, cross-over study comparing the effects of placebo with sulindac, 200 mg daily for 1 week. We studied six hypertensive patients with angiotensin converting enzyme inhibitor-associated cough and six patients with an idiopathic, dry, unproductive cough, all of whom had an increase in the sensitivity of the cough reflex. There was no change in blood pressure control in the hypertensive patients during sulindac therapy. The patients with the angiotensin converting enzyme-associated cough had a significant reduction in the cough symptom score and also a significant increase in the dose of capsaicin causing two or more coughs (threshold sensitivity) and that causing five or more coughs (near maximum response) during sulindac therapy as compared to placebo. In those patients with idiopathic, dry, unproductive cough, sulindac did not alter the symptom of cough or the cough reflex response to capsaicin. These results suggest that prostaglandins may be involved in cough associated with angiotensin converting enzyme inhibitor therapy, but are less likely to be important in the pathogenesis of more common dry coughs of unknown cause.
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PMID:The effect of sulindac on the abnormal cough reflex associated with dry cough. 221 52

Recently there has been extensive development of orally active angiotensin converting enzyme (ACE) inhibitors in addition to those already marketed, for example, captopril, enalapril, lisinopril and ramipril. It was initially thought that ACE inhibitors were likely to be most useful as antihypertensive agents in conditions in which circulating renin and angiotensin II were elevated. However, it is now clear that they can also lower arterial pressure when plasma renin is not high. In addition, they have beneficial effects in cardiac failure. Thus, captopril, enalapril, lisinopril and ramipril can be used in the treatment of mild to moderate hypertension either alone or in conjunction with diuretics or calcium antagonists. Broadly speaking, efficacy appears to be similar to that of beta-blockers or diuretics. Unfortunately, however, there are no long term studies comparing one ACE inhibitor with another or with other classes of antihypertensive agents. Furthermore, there are no prognostic studies which show that use of ACE inhibitors reduces morbidity or mortality in hypertension. Many new ACE inhibitors are undergoing clinical assessment, including alacepril, cilazapril, fosenopril, perindopril, quinapril and ramipril. The drugs vary, in that some exist in the active form whereas others are prodrugs which are converted to the active agent following absorption. In addition they each possess one of several ligands, for example, carboxyl, phosphinyl or sulfhydryl groups, and so vary in their affinity for ACE. Although many of these agents are renally excreted, a small number are metabolised via the liver (e.g. quinapril and spirapril) and this may prove advantageous in the presence of renal impairment. In common with captopril and enalapril, the new ACE inhibitors inhibit the renin-angiotensin system and initial results suggest that they are effective in lowering blood pressure in essential hypertension. Furthermore, they reduce systemic vascular resistance in the absence of a reflex tachycardia. There are a number of adverse effects which are attributable to the pharmacological mechanism of the ACE inhibitors as a group; these include hypotension, particularly in patients with high renin levels, prior diuretic use, renal impairment or in the elderly. Additional adverse effects may relate to chemical structure. The high incidence of adverse effects noted in early studies related to excess dosage and to the presence of a sulfhydryl group, which the more recently developed ACE inhibitors lack. The adverse effects most commonly reported with established and new ACE inhibitors include headache and fatigue, cough, skin rashes, hypotension and diarrhoea. As a group, ACE inhibitors have an acceptable but not negligible adverse effect burden.(ABSTRACT TRUNCATED AT 400 WORDS)
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PMID:Angiotensin converting enzyme inhibitors and moderate hypertension. 222 19

The ACE-inhibiting drugs enalapril and captopril may result in a chronic and sometimes severe cough for which no pathologic cause can be found. Drug-induced cough should therefore be considered in any symptomatic patient taking these medications. In such cases, prompt withdrawal of the drug and substitution of a non-ACE inhibitor is curative and conserves the time and resources of the patient and the physician by avoiding unnecessary diagnostic and therapeutic measures.
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PMID:Chronic cough due to angiotensin-converting enzyme inhibitors. 224 93

Quinapril hydrochloride is a nonsulfhydryl angiotensin converting enzyme (ACE) inhibitor that has been extensively tested and found effective when administered once-a-day to hypertensive patients of both sexes and all degrees of hypertension and cardiac compromise, including those with left ventricular hypertrophy, with and without congestive heart failure. Observations with earlier ACE inhibitors led to reports that this class of drugs was relatively ineffective in older hypertensive patients. To ascertain the role of quinapril (greater than or equal to 10 mg/day) in older patients, its blood pressure-lowering effects in 1,175 hypertensive patients less than or equal to 65 years of age were compared with those in 304 patients greater than 65 years of age. An excellent response was observed in patients greater than 65 years of age with mild to moderate hypertension (diastolic BP, 95 to 105 mm Hg) and moderate to severe hypertension (diastolic BP, 106 to 115 mm Hg). The reductions in blood pressure achieved with quinapril were at least comparable to those obtained in the younger hypertensives, and were numerically (but not statistically) greater in the mild to moderate group (-14 mm Hg v-12 mm Hg). In addition, the percentage of patients who experienced adverse experiences was lower in the greater than 65 group than in the less than or equal to 65 group (15% v 19%). The main adverse experiences reported included dizziness, headache, cough, fatigue, and hypotension. These findings indicate that quinapril is at least as safe and effective in older hypertensives as in younger patients.
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PMID:Use of quinapril in the elderly patient. 226 Nov 46

The pharmacokinetics of quinapril, a novel angiotensin converting enzyme (ACE) inhibitor, and its active metabolite, quinaprilat, were determined following a single 20-mg oral dose of quinapril in six patients with chronic renal failure maintained on continuous ambulatory peritoneal dialysis (CAPD). Overall, quinapril was well tolerated by these CAPD patients, with mild and transient side effects, not unexpected in this clinical setting, which included pruritus, headache, nausea, and cough. Blood pressure reduction was observed in four of six patients, with onset reliably two to four hours after dosing and duration up to 48 hours, associated with quinaprilat concentrations in plasma above 90 ng/mL for at least 33 hours postdose. Two patients experienced significant hypotension, systolic blood pressure below 90 mm Hg, which responded promptly to oral fluid administration and/or reduction in dialysate tonicity. The pharmacokinetic profile of quinapril in these CAPD patients was not significantly different from that previously observed in healthy subjects with normal renal function and in patients with moderate to severe renal dysfunction not yet requiring dialysis (RDND). The apparent elimination half-life of quinapril was approximately one hour, with negligible dialysate excretion. The pharmacokinetic profile of quinaprilat in these CAPD patients was similar to that previously observed in patients with RDND. The elimination half-life of quinaprilat was markedly prolonged when compared to that in healthy subjects and averaged 20 hours, with only a small amount of quinaprilat excreted in dialysate (mean = 2.6% of total dose).(ABSTRACT TRUNCATED AT 250 WORDS)
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PMID:Pharmacokinetics of quinapril and its active metabolite quinaprilat during continuous ambulatory peritoneal dialysis. 227 86

ACE inhibitors have antihypertensive efficacy similar to that of thiazides, beta-blockers and calcium antagonists. They are simple to prescribe and to take, and are relatively free from subjective side-effects apart from persistent dry cough. There are few specific concerns about safety, but experience of long-term use is still relatively limited. They are valuable additional or alternative antihypertensive drugs when standard therapy is contraindicated or fails to control blood pressure.
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PMID:The role of ACE inhibitors in the management of hypertension. 228 49

It has been reported that angiotensin converting enzyme inhibitor (ACE-I) elicits dry cough more frequently in women than in men. This study was designed to evaluate whether airway cough receptors are more sensitive in women than in men. Cough threshold to inhaled tartaric acid was measured in 33 men and 29 women. In non-atopic and non-smoking subjects, geometric mean value of cough threshold in women was 10.0 (GSEM, 1.29) %, which was significantly (p less than 0.02) lower than that in men, 22.5 (GSEM, 1.30) %. In non-atopic men, the cough threshold was significantly (p less than 0.05) lower in smokers (9.3 (GSEM, 1.57) %) than in non-smokers. In non-smoking women, the cough threshold was significantly (p less than 0.02) lower in atopic subjects (4.2 (GSEM, 1.33) %) than in non-atopic subjects. These results demonstrated that airway cough receptors may be more sensitive in women, smoking men and atopic women.
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PMID:[Relationship between cough threshold to inhaled tartaric acid and sex, smoking and atopy in humans]. 229 Feb 33

Physicians should suspect ACE inhibitors as the cause of cough in patients whose symptom begins soon after the institution of therapy with this class of drugs. This is particularly important in patients without a personal or family history of atopy, with normal physical findings, chest radiographs, and lung function tests. Rather than subjecting the patient to an extensive workup, substitution of a different antihypertensive agent is an inexpensive way to show whether the ACE inhibitor is the cause of the chronic cough.
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PMID:Chronic cough caused by angiotensin converting enzyme inhibitors. 229 44


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