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- Free chlorine reactions of angiotensin II receptor antagonists: Kinetics study, transformation products elucidation and in-silico ecotoxicity assessment. [Journal Article]
- STSci Total Environ 2018 Aug 07; 647:1000-1010
- Angiotensin II receptor antagonists (ARA II) are widely employed in the treatment of hypertension-related diseases. Because of their partial metabolization and limited biodegradability, these drugs h...
Angiotensin II receptor antagonists (ARA II) are widely employed in the treatment of hypertension-related diseases. Because of their partial metabolization and limited biodegradability, these drugs have become ubiquitous pollutants in the aquatic environment, including surface water. This research evaluated the reactivity of the ARA II drugs: irbesartan (IRB), losartan (LOS) telmisartan (TEL) and valsartan (VAL) with free chlorine. Responses of parent compounds and their transformation products (TPs) were followed by liquid chromatography (LC) with quadrupole (Q) time-of-flight (TOF) mass spectrometry. Degradation experiments were carried out using ultrapure and river water samples, adjusted at different pHs and, in some cases, adding a small amount (ng mL-1 level) of bromide salts. Whilst TEL and VAL remained stable in presence of relatively high concentrations of free chlorine (10 mg L-1), IRB and LOS were removed according to a pseudo-first order kinetics model. Considering an initial chlorine concentration of 10 mg L-1, their half-lives varied between 6 and 734 min, depending mostly on the water pH. IRB reacted with free chlorine through hydroxylation processes, with and without molecular cleavage and re-arrangements in the imidazolone ring. Its TPs showed a lower in-silico predicted toxicity than the parent drug. In case of LOS, two major competitive degradation routes were identified. They involved replacement of the methanol group attached to the imidazole cycle by chlorine or bromine, and the cleavage of this cycle with removal of the chlorinated carbon and the nitrogen in alpha position. The TPs generated following the first route are predicted to be more toxic than LOS.
- Carnosic acid improves diabetic nephropathy by activating Nrf2/ARE and inhibition of NF-κB pathway. [Journal Article]
- PPhytomedicine 2018 Aug 01; 47:161-173
- CONCLUSIONS: These findings suggest that CA is a safe compound which exerts the protective effects on diabetes-induced kidney complications.
- The Use of Dried Blood Spots for the Quantification of Antihypertensive Drugs. [Review]
- IJInt J Anal Chem 2018; 2018:3235072
- Hypertension or high blood pressure is a harbinger of cardiovascular diseases. There are several classes of drugs used to treat hypertension. This review discusses the use of dried blood spots (DBSs)...
Hypertension or high blood pressure is a harbinger of cardiovascular diseases. There are several classes of drugs used to treat hypertension. This review discusses the use of dried blood spots (DBSs) for the quantification by mass spectrometry (MS), tandem mass spectrometry (MS/MS), or, in some cases, by fluorescence detection methods the following antihypertensive medications: angiotensin-converting enzyme inhibitors (ramipril, ramiprilat, captopril, and lisinopril); angiotensin II receptor antagonists (valsartan, irbesartan, losartan, and losartan carboxylic acid); calcium channel blockers (verapamil, amlodipine, nifedipine, pregabalin, and diltiazem); α blockers (guanfacine, doxazosin, and prazosin); β blockers (propranolol, bisoprolol, atenolol, and metoprolol); endothelin receptor antagonists (bosentan and ambrisentan); and statins (simvastatin, atorvastatin, and rosuvastatin).
- Eco-Friendly Green Liquid Chromatographic Determination of Azelastine in the Presence of its Degradation Products: Applications to Degradation Kinetics. [Journal Article]
- JAJ AOAC Int 2018 Aug 10
- CONCLUSIONS: The proposed method could be used as a harmless alternative for quality control analysis of the mentioned drug, without interference from dosage form additives or decomposition products. Highlights: A highly sensitive stability-indicating eco-friendly green MELC method was developed for the separation of the antihistaminic drug AZL from its degradation products.
- Differential effects of angiotensin II type I receptor blockers on reducing intraocular pressure and TGFβ signaling in the mouse retina. [Journal Article]
- PlosPLoS One 2018; 13(8):e0201719
- CONCLUSIONS: Administration via chow is an effective delivery method for ARBs, as evidenced by lowered blood pressure. ARBs vary in their abilities to lower IOP or reduce TGFβ signaling. Considering the significant roles of IOP and TGFβ in glaucoma pathogenesis, specific ARBs with dual effects, such as telmisartan, may be more effective than other ARBs for treating glaucoma.
- The effects of nebivolol and irbesartan on postdialysis and ambulatory blood pressure in patients with intradialytic hypertension: a randomized cross-over study. [Journal Article]
- JHJ Hypertens 2018 Jul 30
- CONCLUSIONS: Both nebivolol and irbesartan reduced postdialysis and 24-h BP in patients with intradialytic hypertension. Weekly administration had greater effect and nebivolol was numerically slightly more potent than irbesartan.
- Determination of cardiovascular drugs in sewage sludge by matrix solid-phase dispersion and ultra-performance liquid chromatography tandem mass spectrometry. [Journal Article]
- ABAnal Bioanal Chem 2018 Jul 30
- The current study presents a single step sample preparation procedure for the simultaneous determination of five antihypertensive (propranolol, losartan, irbesartan, telmisartan, and valsartan), thre...
The current study presents a single step sample preparation procedure for the simultaneous determination of five antihypertensive (propranolol, losartan, irbesartan, telmisartan, and valsartan), three antiarrhythmic drugs (flecainide, dronedarone, and amiodarone), and one of their metabolites (N-desethylamiodarone) in sludge from municipal sewage treatment plants (STPs). Matrix solid-phase dispersion (MSPD) and ultra-performance liquid chromatography (UPLC) with tandem mass spectrometry (MS/MS) detection were selected as sample preparation and determination techniques, respectively. Under optimal conditions, MSPD extractions were carried out with freeze-dried samples (0.5 g) dispersed on 2 g of C18. Exhaustive extraction of target compounds was achieved with 10 mL of a methanol/acetonitrile/formic acid (30:69:1) solution. The obtained extract was ready for UPLC-MS/MS analysis without any further treatment, except filtration. The overall recoveries of the method (calculated against solvent-based standards) varied from 82 to 124%, with standard deviations in the range from 2 to 16%. Thus, the method was free of matrix effects during electrospray ionization. The achieved limits of quantification stayed between 2 and 10 ng g-1, and the linear response range extended to 5000 ng g-1. The occurrence of target compounds was investigated in sludge from 14 different STPs. High detection frequencies were observed for all compounds, with average concentrations above 100 ng g-1 for six cardiovascular drugs.
- Effects of Sacubitril/Valsartan Versus Irbesartan in Patients with Chronic Kidney Disease: A Randomised Double-Blind Trial. [Journal Article]
- CircCirculation 2018 Jul 12
- Background -Sacubitril/valsartan reduces the risk of cardiovascular mortality among patients with heart failure with reduced ejection fraction, but its effects on kidney function and cardiac biomarke...
Background -Sacubitril/valsartan reduces the risk of cardiovascular mortality among patients with heart failure with reduced ejection fraction, but its effects on kidney function and cardiac biomarkers in people with moderate-to-severe chronic kidney disease are unknown. Methods -UK HARP-III was a randomised double-blind trial which included 414 participants with an estimated glomerular filtration rate (GFR) 20-60 mL/min/1.73m2 who were randomly assigned to sacubitril/valsartan 97/103 mg twice daily versus irbesartan 300 mg once daily. The primary outcome was measured GFR (mGFR) at 12 months using analysis of covariance with adjustment for each individual's baseline mGFR. All analyses were by intention to treat. This trial is registered at ISRCTN11958993 Results -207 participants were assigned to sacubitril/valsartan and 207 to irbesartan. Baseline mGFR was 34.0 (0.8) and 34.7 (0.8) mL/min/1.73m2 respectively. At 12 months there was no difference in measured GFR: 29.8 (SE 0.5) among those assigned sacubitril/valsartan versus 29.9 (0.5) mL/min/1.73m2 among those assigned irbesartan; difference -0.1 (0.7) mL/min/1.73m2 Effects were similar in all pre-specified subgroups. There was also no significant difference in estimated GFR at 3, 6, 9 or 12 months and no clear difference in urinary albumin:creatinine ratio between treatment arms (study average difference -9%, 95% CI -18% to 1%). However, compared to irbesartan, allocation to sacubitril/valsartan reduced study average systolic and diastolic blood pressure by 5.4 (95% CI 3.4-7.4) and 2.1 (95% CI 1.0-3.3) mmHg, and levels of troponin I and N-terminal of pro-hormone brain natriuretic peptide (tertiary endpoints) by 16% (95% CI 8-23) and 18% (95% CI 11-25), respectively. The incidence of serious adverse events (29.5% vs 28.5%; rate ratio [RR] 1.07, 95% CI 0.75-1.53), non-serious adverse reactions (36.7% vs 28.0%; RR 1.35, 95% CI 0.96-1.90) and potassium ≥ 5.5 mmol/L (32% vs 24%; p=0.10) were not significantly different between randomized groups. Conclusions -Over 12 months, sacubitril/valsartan has similar effects on kidney function and albuminuria to irbesartan, but has the additional effect of lowering blood pressure and cardiac biomarkers in people with chronic kidney disease. Clinical Trial Registration -URL: www.isrctn.com Unique Identifier: ISRCTN11958993.
- Drugs and Lactation Database (LactMed) [BOOK]
- BOOKNational Library of Medicine (US): Bethesda (MD)
- Because no information is available on the use of irbesartan during breastfeeding, an alternate drug may be preferred, especially while nursing a newborn or preterm infant.
Because no information is available on the use of irbesartan during breastfeeding, an alternate drug may be preferred, especially while nursing a newborn or preterm infant.
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- Effect of Home Blood Pressure Monitoring on Patient's Awareness and Goal Attainment Under Antihypertensive Therapy: The Factors Influencing Results in Anti-HypertenSive Treatment (FIRST) Study. [Journal Article]
- KBKidney Blood Press Res 2018; 43(3):979-986
- CONCLUSIONS: In a large Swiss cohort of patients with arterial hypertension, information and training on BP self-measurement and direct involvement of patients by using HBPM led to improvement in BP control. Treatment with irbesartan alone or in combination with hydrochlorothiazide was well tolerated and markedly reduced BP.