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  1. Choy YW, Cheong I
    Family Physician, 1989;1:19-22.
    This study was carried out on 30 patients to: i) determine the efficacy of low dose captopril as monotherapy (with or without a diuretic) in the treatment of various grades of hypertension. ii) assess the quality of life of these patients 12 weeks after commencement of therapy. Our results showed that there was a sustained and significant fall in both mean systolic and diastolic blood pressure from 171.9 ± 24 to 150.5 ± 25 mm Hg and 109.0 ± 14 to 93.6 ± 15mmHg respectively (p<0.001). Improvement in quality of life was however not statistically significant (p<0.05). We concluded that low dose captopril used alone or in combination with a diuretic can be considered for the initial therapy of mild to moderate hypertension. The optimal dosage and the longterm benefits on quality of life need further evaluation in a larger series.
    Matched MeSH terms: Captopril
  2. Nair RS, Nair S
    Curr Drug Deliv, 2015;12(5):517-23.
    PMID: 25675336
    Mortality rate due to heart diseases increases dramatically with age. Captopril is an angiotensin converting enzyme inhibitor (ACE) used effectively for the management of hypertension. Due to short elimination half-life of captopril the oral dose is very high. Captopril is prone to oxidation and it has been reported that the oxidation rate of captopril in skin tissues is considerably low when compared to intestinal tissues. All these factors make captopril an ideal drug candidate for transdermal delivery. In this research work an effort was made to formulate transdermal films of captopril by utilizing polyvinylpyrrolidone (PVP) and polyvinyl alcohol (PVA) as film formers and polyethylene glycol 400 (PEG400) as a plasticizer. Dimethyl sulfoxide (DMSO) and dimethylformamide (DMF) were used as permeation enhancers. Physicochemical parameters of the films such as appearance, thickness, weight variation and drug content were evaluated. The invitro permeation studies were carried out through excised human cadaver skin using Franz diffusion cells. The in-vitro permeation studies demonstrated that the film (P4) having the polymer ratio (PVP:PVA = 80:20) with DMSO (10%) resulted a promising drug release of 79.58% at 24 hours with a flux of 70.0 µg/cm(2)/hr. No signs of erythema or oedema were observed on the rabbit skin as a result of skin irritation study by Draize test. Based on the stability report it was confirmed that the films were physically and chemically stable, hence the prepared films are very well suited for transdermal application.
    Matched MeSH terms: Captopril/administration & dosage*; Captopril/pharmacokinetics*
  3. Elkafrawy N, Younes K, Naguib A, Badr H, Kamal Zewain S, Kamel M, et al.
    Phytother Res, 2020 Dec;34(12):3379-3387.
    PMID: 32725873 DOI: 10.1002/ptr.6792
    Hypertension is a public health concern that needs immediate attention upon diagnosis. The demand for natural alternatives is on the rise; Hibiscus sabdariffa and Olea europaea are traditionally used for hypertension management in Egypt. In this study, we aimed to investigate the antihypertensive efficacy and safety of two doses of an herbal product of Hibiscus sabdariffa calyxes and Olea europaea leaves (NW Roselle) in Egyptian patients with grade 1 essential hypertension. We equally randomized 134 patients to receive captopril 25 mg, low-dose NW Roselle, or high-dose NW Roselle BID for 8 weeks. No significant decrease was found in systolic blood pressure or diastolic blood pressure when we compared low-dose NW Roselle and high-dose NW Roselle to captopril (p > .05). In all groups, mean reduction in BP at 8 weeks was significant; 16.4/9.9 mmHg (p captopril, low-dose NW Roselle, and high-dose NW Roselle respectively. In addition, low-dose NW Roselle induced a significant reduction in the mean level of triglycerides (17.56 mg/dL; p = .038). In conclusion, NW Roselle had comparable antihypertensive efficacy and safety to captopril in Egyptian patients with grade 1 essential hypertension.
    Matched MeSH terms: Captopril/pharmacology; Captopril/therapeutic use*
  4. Sharma JN, Stewart JM, Mohsin SS, Katori M, Vavrek R
    Agents Actions Suppl., 1992;38 ( Pt 3):258-69.
    PMID: 1334354
    We have evaluated the effects of a B2 receptor antagonist (B5630) of kinins on BK and captopril-induced acute hypotensive responses in anaesthetized SHR. Intravenous treatment of BK (1.0 microgram) and captopril (0.3 mg/kg) caused significant (p < 0.05) fall in the SBP and DBP. Whereas BK caused greater fall in the SBP (p < 0.05), DBP (p < 0.01) and duration of hypotension (p < 0.05) when administered after captopril (Fig 1 and 2). All the hypotensive effects of BK and captopril were significantly antagonised (p < 0.05) in the presence of B5630 (2.0 mg/kg). Further, the duration of hypotensive responses of BK and captopril were blocked (p < 0.05) by B5630. The agonists and BK-antagonist did not cause significant (p > 0.05) alterations in HR during the entire investigation. These findings provide evidence to support the suggestion that B2 receptor might be involved in the regulation of the hypotensive actions of BK and captopril. Kinins should also have valuable functions in the antihypertensive property of captopril-like drugs.
    Matched MeSH terms: Captopril/administration & dosage; Captopril/antagonists & inhibitors; Captopril/pharmacology*
  5. Quek DKL, Alfred E, Ong SBL
    Family Physician, 1991;3:34-38.
    Cough associated with angiotensin converting-enzyme (ACE) inhibitor therapy has been reported in Western communities, where its incidence is disputed. We, therefore, reviewed our patients who were treated with captopril primarily for congestive cardiac failure. 19 of 61 patients (31.1%) receiving an ACE inhibitor had volunteered cough as an important adverse effect, compared with only one of 59 patients who recieved other treatment. In 3 patients, the cough was intolerably severe to require discontinuation of treatment. Another 7 patients were withdrawn from ACE inhibitor treatment because of other adverse effects including deteriorating renal function, insomnia, dizzy spells, ageusia and proteinuria, and skin rash. We suggest that although ACE inhibitors are very beneficial in improving the clinical status of congestive heart failure, intolerable adverse effects are not uncommon and might mandate withdrawal in a sizeable minority (16.4%).
    Matched MeSH terms: Captopril
  6. Hoe SZ, Kamaruddin MY, Lam SK
    Med Princ Pract, 2007;16(3):203-8.
    PMID: 17409755
    To investigate the hypotensive and angiotensin-converting enzyme (ACE) inhibitory activities of a partially purified fraction (FA-I) of the leaves of Gynura procumbens and to qualitatively analyse the putative compounds present in the fraction.
    Matched MeSH terms: Captopril/pharmacology
  7. Mahadi, M., Eshak, Z., Teoh, Y.C., Ibrahim, A.H., Fauziah, O.
    MyJurnal
    K.alvarezii is a macro algae that claimed to have beneficial effect on reducing risk of cardiovascular disease. The present study investigated the effects of K. alvarezii on the histology of the heart in hypertensive and hypercholesterolemic induced rats. Thirty male Sprague-Dawley rats were divided into 5 groups: normal, negative control, positive control (Captopril 30mg/kg + Simvastatin 2 mg/kg), 5% and 10% K. alvarezii. All groups were fed with NaCl-high fat diet (NaCl-HFD) for 6 weeks except the normal group and treated for 4 weeks after the induction period. The body weight, blood pressure and total cholesterol were measured on week 0, 6 and 10. Body weight, blood pressure and total cholesterol was significantly increased after induction period compared to normal group (p
    Matched MeSH terms: Captopril
  8. You HW, Tajuddin NSA, Anwar YAS
    Malays J Med Sci, 2019 Sep;26(5):113-121.
    PMID: 31728123 MyJurnal DOI: 10.21315/mjms2019.26.5.10
    Background: This study is aimed to analyse the availability, prices and affordability of medicines for ischaemic heart disease (IHD) in Bangi, Selangor, Malaysia.

    Methods: A quantitative research was carried out using the methodology developed by the World Health Organization and Health Action International (WHO/HAI). The prices were compared with international reference prices (IRPs) to obtain a median price ratio. The daily wage of the lowest paid unskilled government worker was used as the standard of the affordability for the medicines. In this study, ten medicines of the IHD were included. The data were collected from 10 private medicine outlets for both originator brand (OB) and lowest-priced generic brand (LPG) in Bangi, Selangor.

    Results: From the results, the mean availability of OB and LPG were 30% and 42%, respectively. Final patient prices for LPG and OB were about 10.77 and 24.09 times their IRPs, respectively. Medicines that consumes more than a day's wage are considered unaffordable. Almost half of the IHD medications cost more than one day's wage. For example, the lowest paid unskilled government worker would need 1.4 days' wage for captopril, while 1.2 days' wage to purchase enalapril for LPG. Meanwhile, for OB, the costs rise to 3.4 days' wage for amlodipine and 3.3 days' wage for simvastatin.

    Conclusion: The findings of this study emphasise the need of focusing and financing, particularly in the private sector, on making chronic disease medicines accessible. This requires multi-faceted interventions, as well as the review of policies and regulations.

    Matched MeSH terms: Captopril
  9. Sharma JN, Amrah SS, Noor AR
    Pharmacology, 1995 Jun;50(6):363-9.
    PMID: 7568335
    The present investigation evaluated the effects of aprotinin, an inhibitor of kallikrein, on blood pressure responses, heart rate, and duration of hypotension induced by acute administration of captopril and enalapril (angiotensin-converting enzyme inhibitors) in anaesthetized spontaneously hypertensive rats. Captopril (20 mg/kg) and enalapril (20 mg/kg) administered intravenously caused a significant (p < 0.001) fall in systolic and diastolic blood pressures in the absence of aprotinin. In contrast, captopril (20 mg/kg) and enalapril (20 mg/kg) failed (p > 0.05) to cause a fall in systolic and diastolic blood pressures in the presence of aprotinin (2 mg/kg). Captopril and enalapril were able to significantly reduce the heart rate (p < 0.05 and p < 0.001) in the presence as well as in the absence of aprotinin. The duration of hypotension produced by captopril and enalapril was abolished significantly (p < 0.001) in the presence of aprotinin. These findings may suggest that captopril and enalapril caused hypotension via the kallikrein pathway, since the kallikrein inhibitor aprotinin can antagonize the hypotensive responses of these agents. Thus, kallikrein may be an independent mediator in the regulation of blood pressure.
    Matched MeSH terms: Captopril/pharmacology*
  10. Abu Hasan Z', Williams H, Ismail NM, Othman H, Cozier GE, Acharya KR, et al.
    Sci Rep, 2017 03 27;7:45409.
    PMID: 28345667 DOI: 10.1038/srep45409
    The control of mosquitoes is threatened by the appearance of insecticide resistance and therefore new control chemicals are urgently required. Here we show that inhibitors of mosquito peptidyl dipeptidase, a peptidase related to mammalian angiotensin-converting enzyme (ACE), are insecticidal to larvae of the mosquitoes, Aedes aegypti and Anopheles gambiae. ACE inhibitors (captopril, fosinopril and fosinoprilat) and two peptides (trypsin-modulating oostatic factor/TMOF and a bradykinin-potentiating peptide, BPP-12b) were all inhibitors of the larval ACE activity of both mosquitoes. Two inhibitors, captopril and fosinopril (a pro-drug ester of fosinoprilat), were tested for larvicidal activity. Within 24 h captopril had killed >90% of the early instars of both species with 3rd instars showing greater resistance. Mortality was also high within 24 h of exposure of 1st, 2nd and 3rd instars of An. gambiae to fosinopril. Fosinopril was also toxic to Ae. aegypti larvae, although the 1st instars appeared to be less susceptible to this pro-drug even after 72 h exposure. Homology models of the larval An. gambiae ACE proteins (AnoACE2 and AnoACE3) reveal structural differences compared to human ACE, suggesting that structure-based drug design offers a fruitful approach to the development of selective inhibitors of mosquito ACE enzymes as novel larvicides.
    Matched MeSH terms: Captopril/pharmacology
  11. Sasongko TH, Nagalla S, Ballas SK
    PMID: 26041152 DOI: 10.1002/14651858.CD009191.pub3
    BACKGROUND: Sickle cell disease is a group of disorders characterized by deformation of erythrocytes. Renal damage is a frequent complication in sickle cell disease as a result of long-standing anemia and disturbed circulation through the renal medullary capillaries. Due to the improvement in life expectancy of people with sickle cell disease, there has been a corresponding significant increase in the incidence of renal complications. Microalbuminuria and proteinuria are noted to be a strong predictor of subsequent renal failure. There is extensive experience and evidence with angiotensin-converting enzyme (ACE) inhibitors over many years in a variety of clinical situations for patients who do not have sickle cell disease, but their effect in people with this disease is unknown. It is common practice to administer ACE inhibitors for sickle nephropathy due to their renoprotective properties; however, little is known about their effectiveness and safety in this setting. This is an update of a Cochrane Review first published in 2013.

    OBJECTIVES: To determine the effectiveness of ACE inhibitor administration in people with sickle cell disease for decreasing intraglomerular pressure, microalbuminuria and proteinuria and to to assess the safety of ACE inhibitors as pertains to their adverse effects.

    SEARCH METHODS: The authors searched the Cochrane Cystic Fibrosis and Genetic Disorders Group's Hameoglobinopathies Trials Register comprising references identified from comprehensive electronic database searches and handsearches of relevant journals and abstract books of conference proceedings.Date of the most recent search: 03 June 2015.

    SELECTION CRITERIA: Randomized or quasi-randomized controlled trials of ACE inhibitors designed to reduce microalbuminuria and proteinuria in people with sickle cell disease compared to either placebo or standard treatment regimen.

    DATA COLLECTION AND ANALYSIS: Three authors independently applied the inclusion criteria in order to select studies for inclusion in the review. Two authors assessed the risk of bias of studies and extracted data and the third author verified these assessments.

    MAIN RESULTS: Five studies were identified through the searches, only one met our inclusion criteria. The included study randomized 22 participants (seven males and 15 females) having proteinuria or microalbuminuria with sickle cell disease and treated the participants for six months (median length of follow up of three months) with captopril or placebo. The overall quality of the outcomes reported was high, since most aspects that may contribute to bias were regarded to be of low risk, although allocation concealment was not reported. At six months, the study reported no significant difference in urinary albumin excretion between the captopril group and the placebo group, although the mean urinary albumin excretion in the captopril group was lower by a mean difference of -49.00 (95% confidence interval -124.10 to 26.10) compared to that of placebo. However, our analysis on the absolute change score showed significant changes between the two groups by a mean difference of -63.00 (95% confidence interval -93.78 to -32.22). At six months albumin excretion in the captopril group was noted to decrease from baseline by a mean of 45 ± 23 mg/day and the placebo group was noted to increase by 18 ± 45 mg/day. Serum creatinine and potassium levels were reported constant throughout the study. The potential for inducing hypotension should be highlighted; the study reported a decrease of 8 mmHg in systolic pressure and 5 mmHg in diastolic and mean blood pressure.

    AUTHORS' CONCLUSIONS: There is not enough evidence to show that the administration of ACE inhibitors is associated with a reduction of microalbuminuria and proteinuria in people with sickle cell disease, although a potential for this was seen. More long-term studies involving multiple centers and larger cohorts using a randomized-controlled design are warranted, especially among the pediatric age group. Detailed reporting of each outcome measure is necessary to allow a clear cut interpretation in a systematic review. One of the difficulties encountered in this review was the lack of detailed data reported in the included study.

    Matched MeSH terms: Captopril/therapeutic use*
  12. Azis NA, Agarwal R, Ismail NM, Ismail NH, Kamal MSA, Radjeni Z, et al.
    Mol Biol Rep, 2019 Jun;46(3):2841-2849.
    PMID: 30977084 DOI: 10.1007/s11033-019-04730-w
    This study investigated the effects of a standardised ethanol and water extract of Ficus deltoidea var. Kunstleri (FDK) on blood pressure, renin-angiotensin-aldosterone system (RAAS), endothelial function and antioxidant system in spontaneously hypertensive rats (SHR). Seven groups of male SHR were administered orally in volumes of 0.5 mL of either FDK at doses of 500, 800, 1000 and 1300 mg kg- 1, or captopril at 50 mg kg- 1 or losartan at 10 mg kg- 1 body weight once daily for 4 weeks or 0.5 mL distilled water. Body weight, systolic blood pressures (SBP) and heart rate (HR) were measured every week. 24-hour urine samples were collected at weeks 0 and 4 for electrolyte analysis. At week 4, sera from rats in the control and 1000 mg kg- 1 of FDK treated groups were analyzed for electrolytes and components of RAAS, endothelial function and anti-oxidant capacity. SBP at week 4 was significantly lower in all treatment groups, including captopril and losartan, when compared to that of the controls. Compared to the controls, ACE activity and concentrations of angiotensin I, angiotensin II and aldosterone were lower whereas concentrations of angiotensinogen and angiotensin converting enzyme 2 were higher in FDK treated rats. Concentration of eNOS and total anti-oxidant capacity were higher in FDK treated rats. Urine calcium excretion was higher in FDK treated rats. In conclusion, it appears that ethanol and water extract of FDK decreases blood pressure in SHR, which might involve mechanisms that include RAAS, anti-oxidant and endothelial system.
    Matched MeSH terms: Captopril/pharmacology
  13. Sharma JN, Kesavarao U
    Pharmacology, 2002 Apr;64(4):196-200.
    PMID: 11893900 DOI: 10.1159/000056171
    We investigated the total urinary kallikrein levels, left-ventricular wall thickness and mean arterial blood pressure of nontreated and captopril-treated diabetic and nondiabetic spontaneously hypertensive rats. The mean arterial blood pressure was significantly elevated in diabetic spontaneously hypertensive rats as compared to nondiabetic spontaneously hypertensive rats. Captopril treatment caused a significant reduction in the arterial blood pressure of both nondiabetic and diabetic spontaneously hypertensive rats. The left-ventricular wall thickness was also significantly reduced in diabetic and nondiabetic spontaneously hypertensive treated with captopril as compared to nontreated diabetic and nondiabetic spontaneously hypertensive rats. The total urinary kallikrein levels were significantly raised in captopril-treated diabetic and nondiabetic spontaneously hypertensive rats against the values obtained from nontreated diabetic and nondiabetic spontaneously hypertensive rats. These results indicate that blood pressure reduction and left ventricular wall regression with captopril treatment might be due to enhanced renal kallikrein formation. The significance of these findings is discussed.
    Matched MeSH terms: Captopril/pharmacology*
  14. Ismail NM, Ibrahim IA, Hashim NB, Jaarin K
    Arch Med Sci, 2013 Dec 30;9(6):1132-7.
    PMID: 24482662 DOI: 10.5114/aoms.2012.31252
    INTRODUCTION: Captopril is an angiotensin-converting enzyme inhibitor, which is used as an antihypertensive agent and has shown antioxidant properties. This study aims at determining the effects of captopril on factors affecting gastric mucosal integrity in aspirin-induced gastric lesions.
    MATERIAL AND METHODS: Eighteen male Sprague-Dawley (200-250 g) rats that were given aspirin (40 mg/100 g body weight) were divided into three groups: the control, captopril (1 mg/100 g body weight daily) and ranitidine (2.5 mg/100 g body weight twice daily) groups. Ranitidine and captopril were given orally for 28 days. Rats in all groups were sacrificed and the parameters measured.
    RESULTS: Captopril reduced gastric acidity, and increased gastric glutathione (GSH) and prostaglandin E2 (PGE2) significantly in comparison to the control group. Captopril also reduced malondialdehyde (MDA) and gastric lesions insignificantly compared to the control group. Ranitidine healed the lesions significantly compared to the control group. There was no difference between ranitidine and captopril on the severity of lesions, gastric acidity, MDA and GSH. Captopril increased PGE2 compared to ranitidine (p < 0.05).
    CONCLUSIONS: Captopril has desirable effects on the factors affecting gastric mucosal integrity (acidity, PGE2 and GSH) and is comparable to ranitidine in ulcer healing.
    KEYWORDS: aspirin; captopril; gastric lesions; ranitidine
    Matched MeSH terms: Captopril
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