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Key Features of Candesartan Cilexetil and a Comparison with Other Angiotensin II Receptor Antagonists
Journal of Human Hypertension (1999) 13, (Suppl 1), S3–S10 1999 Stockton Press. All rights reserved 0950-9240/99 $12.00 Key features of candesartan cilexetil and a comparison with other angiotensin II receptor antagonists PS Sever Imperial College of Science, Technology & Medicine at St Mary’s Hospital, London, UK Current research on angiotensin II AT1-receptor antag- in patients with essential hypertension. Candesartan onists (AIIRAs) and selected studies presented at the cilexetil has a rapid onset of action (approximately 80% recent symposium held in Amsterdam, The Netherlands, of total blood pressure reduction within the first 2 on 6 June 1998, titled ‘Angiotensin II Receptor Antagon- weeks) and dose-dependent effects on blood pressure, ists are NOT all the Same’ are reviewed. AIIRAs offer a is comparable in efficacy to a number of classes of anti- number of potential advantages over alternative antihy- hypertensives, and is effective in combination therapy pertensive agents acting via the renin-angiotensin-aldo- (eg, with hydrochlorothiazide and amlodipine). This sterone system. They combine blood pressure-lowering favourable profile may be due in part to the highly selec- effects at least equivalent to those of angiotensin-con- tive, tight binding to and slow dissociation of candesar- verting enzyme (ACE) inhibitors, coupled with placebo- tan from the AT1 receptor. Preliminary studies suggest like tolerability. Candesartan cilexetil is a novel AIIRA that candesartan cilexetil also protects end organs that has demonstrated clinical -
Effective Dose Range of Enalapril in Mild to Moderate Essential Hypertension
Br. J. clin. Pharmac. (1985), 19, 605-611 Effective dose range of enalapril in mild to moderate essential hypertension R. BERGSTRAND', H. HERLITZ2, SAGA JOHANSSON', G. BERGLUND2, A. VEDIN', C. WILHELMSSON', H. J. GOMEZ3, V. J. CIRILLO3 & J. A. BOLOGNESE4 'Department of Medicine, Ostra Hospital and 2Department of Medicine I, Sahlgrenska Hospital, Goteborg, Sweden and Department of 3Cardiovascular Clinical Research and 4Clinical Biostatistics, Merck Sharp & Dohme Research Laboratories, Rahway, New Jersey, USA 1 The dose-response relationship of enalapril was evaluated in a double-blind, balanced, two-period, incomplete-block study in 91 patients with mild to moderate essential hyper- tension. 2 Patients were randomly assigned to two of six treatments: placebo, 2.5, 5, 10, 20 and 40 mg/day of enalapril maleate. There were two 3-week treatment periods, each preceded by a 4-week, single-blind placebo washout. 3 Each dose of enalapril produced significant decreases in standing and supine systolic and diastolic blood pressure after 2 and 3 weeks of treatment. There were no significant changes on placebo. 4 There was a significant linear dose response relationship for both mean blood pressure and mean change from baseline in blood pressure (P < 0.01 for systolic and mean arterial pressure, and P < 0.05 for diastolic pressure). 5 Enalapril was associated with an increasing dose-response relationship across the 2.5- 40 mg/day range. The 2.5 mg/dose is effective in some patients; however, doses ¢ 10 mg/ day may be necessary to achieve satisfactory blood pressure control. Keywords enalapril angiotensin converting enzyme inhibitor dose-response relationship Introduction In recent years much interest has been focused with renal impairment treated with high doses of on angiotensin converting enzyme (ACE) in- captopril. -
A Comparison of the Tolerability of the Direct Renin Inhibitor Aliskiren and Lisinopril in Patients with Severe Hypertension
Journal of Human Hypertension (2007) 21, 780–787 & 2007 Nature Publishing Group All rights reserved 0950-9240/07 $30.00 www.nature.com/jhh ORIGINAL ARTICLE A comparison of the tolerability of the direct renin inhibitor aliskiren and lisinopril in patients with severe hypertension RH Strasser1, JG Puig2, C Farsang3, M Croket4,JLi5 and H van Ingen4 1Technical University Dresden, Heart Center, University Hospital, Dresden, Germany; 2Department of Internal Medicine, La Paz Hospital, Madrid, Spain; 31st Department of Internal Medicine, Semmelweis University, Budapest, Hungary; 4Novartis Pharma AG, Basel, Switzerland and 5Novartis Institutes for Biomedical Research, Cambridge, MA, USA Patients with severe hypertension (4180/110 mm Hg) LIS 3.4%). The most frequently reported AEs in both require large blood pressure (BP) reductions to reach groups were headache, nasopharyngitis and dizziness. recommended treatment goals (o140/90 mm Hg) and At end point, ALI showed similar mean reductions from usually require combination therapy to do so. This baseline to LIS in msDBP (ALI À18.5 mm Hg vs LIS 8-week, multicenter, randomized, double-blind, parallel- À20.1 mm Hg; mean treatment difference 1.7 mm Hg group study compared the tolerability and antihyperten- (95% confidence interval (CI) À1.0, 4.4)) and mean sitting sive efficacy of the novel direct renin inhibitor aliskiren systolic blood pressure (ALI À20.0 mm Hg vs LIS with the angiotensin converting enzyme inhibitor À22.3 mm Hg; mean treatment difference 2.8 mm Hg lisinopril in patients with severe hypertension (mean (95% CI À1.7, 7.4)). Responder rates (msDBPo90 mm Hg sitting diastolic blood pressure (msDBP)X105 mm Hg and/or reduction from baselineX10 mm Hg) were 81.5% and o120 mm Hg). -
Perindopril | Memorial Sloan Kettering Cancer Center
PATIENT & CAREGIVER EDUCATION Perindopril This information from Lexicomp® explains what you need to know about this medication, including what it’s used for, how to take it, its side effects, and when to call your healthcare provider. Brand Names: US Aceon [DSC] Brand Names: Canada AG-Perindopril; APO-Perindopril; Auro-Perindopril; BIO-Perindopril; Coversyl; JAMP-Perindopril; M-Perindopril Erbumine; MAR-Perindopril; MINT- Perindopril; NRA-Perindopril; PMS-Perindopril; Priva-Perindopril Erbumine; RIVA-Perindopril; SANDOZ Perindopril Erbumine; TEVA-Perindopril Warning Do not take if you are pregnant. Use during pregnancy may cause birth defects or loss of the unborn baby. If you get pregnant or plan on getting pregnant while taking this drug, call your doctor right away. What is this drug used for? It is used to treat high blood pressure. It is used to lower the risk of heart attack and death from heart disease in certain people. It may be given to you for other reasons. Talk with the doctor. Perindopril 1/7 What do I need to tell my doctor BEFORE I take this drug? If you are allergic to this drug; any part of this drug; or any other drugs, foods, or substances. Tell your doctor about the allergy and what signs you had. If you have ever had a very bad or life-threatening reaction called angioedema. Signs may be swelling of the hands, face, lips, eyes, tongue, or throat; trouble breathing; trouble swallowing; unusual hoarseness. If you have kidney disease. If you are taking a drug that has aliskiren in it and you also have diabetes or kidney problems. -
AVAPRO Rx Only (Irbesartan) Tablets
NDA 20-757/S-038 Page 3 ® AVAPRO Rx only (irbesartan) Tablets USE IN PREGNANCY When used in pregnancy during the second and third trimesters, drugs that act directly on the renin-angiotensin system can cause injury and even death to the developing fetus. When pregnancy is detected, AVAPRO should be discontinued as soon as possible. See WARNINGS: Fetal/Neonatal Morbidity and Mortality. DESCRIPTION ®* AVAPRO (irbesartan) is an angiotensin II receptor (AT1 subtype) antagonist. Irbesartan is a non-peptide compound, chemically described as a 2-butyl-3-[p-(o-1H-tetrazol-5- ylphenyl)benzyl]-1,3-diazaspiro[4.4]non-1-en-4-one. Its empirical formula is C25H28N6O, and the structural formula: Irbesartan is a white to off-white crystalline powder with a molecular weight of 428.5. It is a nonpolar compound with a partition coefficient (octanol/water) of 10.1 at pH of 7.4. Irbesartan is slightly soluble in alcohol and methylene chloride and practically insoluble in water. AVAPRO is available for oral administration in unscored tablets containing 75 mg, 150 mg, or 300 mg of irbesartan. Inactive ingredients include: lactose, microcrystalline cellulose, pregelatinized starch, croscarmellose sodium, poloxamer 188, silicon dioxide and magnesium stearate. CLINICAL PHARMACOLOGY Mechanism of Action Angiotensin II is a potent vasoconstrictor formed from angiotensin I in a reaction catalyzed by angiotensin-converting enzyme (ACE, kininase II). Angiotensin II is the principal pressor agent of the renin-angiotensin system (RAS) and also stimulates aldosterone synthesis and secretion by adrenal NDA 20-757/S-038 Page 4 cortex, cardiac contraction, renal resorption of sodium, activity of the sympathetic nervous system, and smooth muscle cell growth. -
Download Leaflet View the Patient Leaflet in PDF Format
Package leaflet: Information for the patient Fosinopril Sodium 10 mg Tablets Fosinopril Sodium 20 mg Tablets Fosinopril sodium Read all of this leaflet carefully before you start taking this medicine because it contains important information for you. - Keep this leaflet. You may need to read it again. - If you have any further questions, ask your doctor or pharmacist. - This medicine has been prescribed for you only. Do not pass it on to others. It may harm them, even if their signs of illness are the same as yours. - If you get any side effects, talk to your doctor or pharmacist. This includes any possible side effects not listed in this leaflet. See section 4. What is in this leaflet 1. What Fosinopril is and what it is used for 2. What you need to know before you take Fosinopril 3. How to take Fosinopril 4. Possible side effects 5. How to store Fosinopril 6. Contents of the pack and other information. 1. What Fosinopril is and what is it used for Fosinopril belongs to the class of medicines called Angiotensin Converting Enzyme (ACE) inhibitors that act on the heart and blood vessels. You may have been given Fosinopril to: • lower your blood pressure if it is too high (a condition called hypertension) • help your heart pump blood around your body if you have a condition known as heart failure and are also being treated with diuretics (medicines which help to remove excess fluid from the body). 2. What you need to know before you take Fosinopril Do not take Fosinopril: • if you are allergic to fosinopril or any other ACE inhibitor, or any of the other ingredients of this medicine (listed in section 6). -
Cough Induced by Enalapril but Not by Captopril
Eur Respir J 1989, 2, 289-291 CASE REPORT Cough induced by enalapril but not by captopril H. Puolijoki*, M. Nieminen*, E. Moilanen**, L. Siitonen*, A. Lahdensuo*, P. Reinikainen*, H. Vapaatalo** Cough iruluced by enalapril but 1101 by capropril. H. Puolijoki, M Nieminen, •Tampere University Central Hospital. E. Moilanen, L. Siironen, A. Lahdensuo, P. Reinikainen, If. VapaaJalo. •• Dept of Biomedical Sciences, University of ABSTRACT: We report a 68 yr old woman with hypertension wbo Tampcre. Finland. developed a dry cough on enalaprll but not on captopril therapy. Pul monary function te!its, methacholine in halation challenges, total blood Correspondence: H. Puolijoki, Dept of Pulmonary Diseases, Turlcu University Central Hospital, SF- eoslnophiJ counts, and changes In plasma concentrations or prostaglandin 207 40 Preitila, Finland. E2 and tllromboxane 81 did not explain the difference in the adverse reaction between tbese two angiotensin converting enzyme inhibitors. Keywords: ACE inhibitors; captopril; cough; Eur Respir J., 1989, 2, 289- 291. enalapril. Received: March, 1988; accepted after revision August 9, 1988. Angiotensin converting enzyme (ACE) inhibiLors like Case History capropril and ena1april are usually well tolerated. How ever, in some patientS they may cause cough as an A 68 yr old non-smoking woman with diabetes, adverse reaction [1]. We report a female patiem who hypertension and compensated heart failure, but with developed a cough on enalapril but not on captopril no respiratory disease or abnormalities on chest X-ray, therapy. We evaluated her lung function, bronchial re developed a dry cough but no dyspnoea or posrnasal activity to methacholine, LolaJ blood eosinophi l count as drip during Lreatmem with ena1april (Renitcc®, MSD, E 20 mg·day·1) for hypertension. -
Ace Inhibitors (Angiotensin-Converting Enzyme)
Medication Instructions Ace Inhibitors (Angiotensin-Converting Enzyme) Generic Brand Benazepril Lotensin Captopril Capoten Enalapril Vasotec Fosinopril Monopril Lisinopril Prinivil, Zestril Do not Moexipril Univasc Quinapril Accupril stop taking Ramipril Altace this medicine Trandolapril Mavik About this Medicine unless told ACE inhibitors are used to treat both high blood pressure (hypertension) and heart failure (HF). They block an enzyme that causes blood vessels to constrict. This to do so allows the blood vessels to relax and dilate. Untreated, high blood pressure can damage to your heart, kidneys and may lead to stroke or heart failure. In HF, using by your an ACE inhibitor can: • Protect your heart from further injury doctor. • Improve your health • Reduce your symptoms • Can prevent heart failure. Generic forms of ACE Inhibitors (benazepril, captopril, enalapril, fosinopril, and lisinopril) may be purchased at a lower price. There are no “generics” for Accupril, Altace Mavik, and of Univasc. Thus their prices are higher. Ask your doctor if one of the generic ACE Inhibitors would work for you. How to Take Use this drug as directed by your doctor. It is best to take these drugs, especially captopril, on an empty stomach one hour before or two hours after meals (unless otherwise instructed by your doctor). Side Effects Along with needed effects, a drug may cause some unwanted effects. Many people will not have any side effects. Most of these side effects are mild and short-lived. Check with your doctor if any of the following side effects occur: • Fever and chills • Hoarseness • Swelling of face, mouth, hands or feet or any trouble in swallowing or breathing • Dizziness or lightheadedness (often a problem with the first dose) Report these side effects if they persist: • Cough – dry or continuing • Loss of taste, diarrhea, nausea, headache or unusual fatigue • Fast or irregular heartbeat, dizziness, lightheadedness • Skin rash Special Guidelines • Sodium in the diet may cause you to retain fluid and increase your blood pressure. -
Download Leaflet View the Patient Leaflet in PDF Format
Package leaflet: Information for the user Candesartan cilexetil 2 mg tablets Candesartan cilexetil 4 mg tablets Candesartan cilexetil 8 mg tablets Candesartan cilexetil 16 mg tablets Candesartan cilexetil 32 mg tablets candesartan cilexetil Read all of this leaflet carefully If you are going to have an operation, before you start taking this tell your doctor or dentist that you are medicine because it contains taking Candesartan cilexetil. This is important information for you. because Candesartan cilexetil, when - Keep this leaflet. You may need combined with some anaesthetics, to read it again. may cause an excessive drop in - If you have any further questions, blood pressure. ask your doctor or pharmacist. - This medicine has been Children and adolescents prescribed for you only. Do not Candesartan Cilexetil has been pass it on to others. It may harm studied in children. For more them, even if their signs of illness information, talk to your doctor. are the same as yours. Candesartan Cilexetil must not be - If you get any side effects, talk to given to children under 1 year of your doctor or pharmacist. This age due to the potential risk to the includes any possible side effects developing kidneys. not listed in this leaflet. See Other medicines and Candesartan section 4. cilexetil What is in this leaflet Tell your doctor or pharmacist if you 1. What Candesartan cilexetil is and are taking, have recently taken or what it is used for might take any other medicines. 2. What you need to know before you take Candesartan cilexetil Candesartan cilexetil can affect the 3. -
BENICAR HCT Tablets
® BENICAR HCT Tablets (OLMESARTAN MEDOXOMIL-HYDROCHLOROTHIAZIDE) WARNING: FETAL TOXICITY When pregnancy is detected, discontinue Benicar HCT as soon as possible. Drugs that act directly on the renin-angiotensin system can cause injury and death to the developing fetus. See Warnings: Fetal Toxicity DESCRIPTION BENICAR HCT® (olmesartan medoxomil-hydrochlorothiazide) is a combination of an angiotensin II receptor antagonist (AT1 subtype), olmesartan medoxomil, and a thiazide diuretic, hydrochlorothiazide (HCTZ). Olmesartan medoxomil, a prodrug, is hydrolyzed to olmesartan during absorption from the gastrointestinal tract. Olmesartan medoxomil is 2,3-dihydroxy-2-butenyl 4-(1-hydroxy-1-methylethyl)-2 propyl-1-[p-(o-1H-tetrazol-5-ylphenyl)benzyl]imidazole-5-carboxylate, cyclic 2,3 carbonate. Its empirical formula is C29H30N6O6 and its structural formula is: Olmesartan medoxomil is a white to light yellowish-white powder or crystalline powder with a molecular weight of 558.6. It is practically insoluble in water and sparingly soluble in methanol. Hydrochlorothiazide is 6-chloro-3,4-dihydro-2H-1,2,4-benzo-thiadiazine-7-sulfonamide 1,1-dioxide. Its empirical formula is C7H8ClN3O4S2 and its structural formula is: 1 Reference ID: 3227549 Hydrochlorothiazide is a white, or practically white, crystalline powder with a molecular weight of 297.7. Hydrochlorothiazide is slightly soluble in water but freely soluble in sodium hydroxide solution. BENICAR HCT® is available for oral administration in tablets containing 20 mg or 40 mg of olmesartan medoxomil combined with 12.5 mg of hydrochlorothiazide, or 40 mg of olmesartan medoxomil combined with 25 mg of hydrochlorothiazide. Inactive ingredients include: hydroxypropylcellulose, hypromellose, lactose, low-substituted hydroxypropylcellulose, magnesium stearate, microcrystalline cellulose, red iron oxide, talc, titanium dioxide and yellow iron oxide. -
Angiotensin-Converting Enzyme Inhibition but Not Angiotensin II Receptor Blockade Regulates Matrix Metalloproteinase Activity in Patients with Glomerulonephritis
J Am Soc Nephrol 14: 2861–2872, 2003 Angiotensin-Converting Enzyme Inhibition but not Angiotensin II Receptor Blockade Regulates Matrix Metalloproteinase Activity in Patients with Glomerulonephritis NADE` GE LODS,* PAOLO FERRARI,* FELIX J. FREY,* ANDREAS KAPPELER,† CELINE BERTHIER,* BRUNO VOGT,* and HANS-PETER MARTI* *Division of Nephrology and Hypertension, Inselspital Bern, Bern, Switzerland; and †Institute of Pathology, University of Bern, Bern, Switzerland Abstract. Equivalent long-term effects on the kidney are attrib- periods of 4 wk each without therapy. Untreated patients with uted to angiotensin-converting enzyme inhibitors (ACEI) and glomerulonephritis displayed distinctively higher serum levels angiotensin II type 1 receptor blockers (ARB). Nevertheless, it of MMP-2 but much lower MMP-1/-8/-9 concentrations com- is unknown to which degree effects of these compounds on pared with healthy control subjects. Immunohistology of individual inflammatory mediators, including matrix metallo- MMP-2 and MMP-9 in kidney biopsy specimen was accord- proteinases (MMP), are comparable. On the basis of structural ingly. However, these patients excreted higher amounts of and functional differences, it was hypothesized that ACEI and MMP-2 and MMP-9 in urine than healthy control subjects, ARB differentially regulate MMP activity. In a randomized, possibly reflecting ongoing glomerular inflammation. In pa- prospective crossover trial, the effect of an ACEI (fosinopril; tients with glomerulonephritis, ACEI significantly reduced 20 mg/d) and of an ARB (irbesartan; 150 mg/d) on MMP overall MMP serum activity to 25%, whereas ARB did not activity was evaluated. Ten hypertensive patients with glomer- show any effect. Activities of MMP-1/-2/-8/-9 were also sig- ulonephritis and normal or mildly reduced creatinine clearance nificantly inhibited by fosinopril but not by irbesartan. -
Effects of Olmesartan Vs Irbesartan on Metabolic Parameters and Visfatin in Hypertensive Obese Women
European Review for Medical and Pharmacological Sciences 2010; 14: 759-763 Effects of olmesartan vs irbesartan on metabolic parameters and visfatin in hypertensive obese women D.A. DE LUIS, R. CONDE, M. GONZALEZ SAGRADO, R. ALLER, O. IZAOLA, J.L. PEREZ CASTRILLON, E. ROMERO, M.J. CASTRO Institute of Endocrinology and Nutrition, Medicine School and Unit of Investigation. Hospital Rio Hortega. RD-056/0013 RETICEF. University of Valladolid. Valladolid (Spain) Abstract. – Background: Angiotensin II reg- dence of this rising tide of obesity and associated ulates the production of adipokines. The objective pathologies has led, in the last years, to a dramat- was to study the effect of treatment with irbesartan versus olmesartan in obese hypertensive women. ic increase of researches on the role of adipose Subjects: A sample of 34 obese hypertensive tissue as an active participant in controlling the women was analyzed in a prospective way with a body’s physiology2. randomized trial. Patients were randomized to irbe- Visfatin was recently identified as a protein sartan (300 mg/day) or olmesartan (40 mg/day) for preferentially expressed in visceral adipose tis- 3 months. Weight, body mass index, blood pres- sue, compared with subcutaneous adipose tis- sure, basal glucose, insulin, total cholesterol, LDL- sue3. It can be found in skeletal muscle, liver, cholesterol, HDL-cholesterol, triglycerides, HOMA and visfatin were determined at basal time and af- bone marrow and lymphocytes, where it was ter 3 months of treatment. initially identified as pre-B-cell colony-enhanc- Results: Thirty four patients gave informed con- ing factor (PBEF). Fukuhara et al4 clearly sug- sent and were enrolled in the study.