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Blood pressure (BP) is one of the most important and common vascular risk factors but it is often poorly controlled. Inhibition of the renin-angiotensin-aldosterone system (RAAS) provides beneficial effects in hypertensives. The association of low-dosed diuretics in combination with RAAS blocking agents allows maximum benefit from potassium depleti...
Contexts in source publication
Context 1
... is an angiotensin II (AT1 receptor subtype) antagonist with lipophylic, non-peptide chemical structure. It is white, crystalline powder and is chemically described as 2- butyl-3-[p-(o-1H-tetrazol-5-ylphenyl) benzyl]-1,3-diazaspiro [4,4]non-1-en-4-one, with empirical formula C 25 H 28 N 6 O (Fig. 1). Irbesartan is slightly soluble in alcohol and methyl- ene chloride and practically insoluble in water [44]. HCTZ is a diuretic and antihypertensive drug. It is the 3,4-dihydro derivative of chlorothiazide. Its chemical name is 6-chloro-3,4-dihydro-2H-1,2,4- benzothiadiazine-7- sulfonamide 1, 1-dioxide, with empirical formula C 7 H 8 C ...
Context 2
... is the 3,4-dihydro derivative of chlorothiazide. Its chemical name is 6-chloro-3,4-dihydro-2H-1,2,4- benzothiadiazine-7- sulfonamide 1, 1-dioxide, with empirical formula C 7 H 8 C l N 3 O 4 S 2 (Figure 1). It is also a white crystalline pow- der, and slightly soluble in water, but freely soluble in so- dium hydroxide solution [45]. ...
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Citations
... It is a white crystalline powder, slightly soluble in water and freely soluble in sodium hydroxide solution. (15) Irbesartan is available in a fixed-dose combination formulation with hydrochlorothiazide, to achieve an additive antihypertensiveeffect. Irbesartan/hydrochlorothiaz ide combination preparations are marketed under various brand names. ...
Oro slippery tablets (OSTs) is a technique used to improve swallowing of tablets for patients with dysphagia. The aim of this study was to formulate irbesartan and hydrochlorothiazide as Oroslippery tablets (OST) containing 150 mg irbesartan and 25 mg hydrochlorothiazide for dysphagia patients. A simple and rapid method of analysis was developed and validated according to the ICH guideline using HPLC with UV detector. Tablets were prepared by direct compression and then coated with the slippery coat of three different concentrations of the slippering substance “xanthan gum’ (2%, 3% and 4%) in Opadry Colorcone® and evaluated according to USP. Slipperiness test was performed using Albino rabbits. Results showed that 2% xanthan gum gave the shortest swallowing time. Also, disintegration time was increased by the coat significantly with the increase of the gum’s concentration in the coat. The release kinetics study of the tested formulations (uncoated versus coated with 2% gum) gave the highest correlation for the "first-order release model" for both drugs in the absence and presence of the slippering agent which indicates that the coating did not interfere with the release kinetics of both drugs. In a conclusion, 2% xanthan gum as slippering agent the optimum concentration used to promote easy ingestion of this tablet.
... The combination of ARB and thiazide diuretic results in additive lowering of BP and was recommended for treatment of essential hypertension [2]. A fixed-dose combination of hydrochlorothiazide and irbesartan showed additive antihypertensive effect in a dosedependent manner up to hydrochlorothiazide (HCTZ) 25 mg and irbesartan 300 mg with high tolerability in diverse patient groups [7]. BP-lowering potential and safety profile of irbesartan/HCTZ combination were proved in clinical trials. ...
Background and objective: The combination antihypertensive therapy has shown greater blood pressure lowering potential as well as better adherence to the treatment. Therefore, a new generic fixed-dose combination containing irbesartan and hydrochlorothiazide was developed and rate and extend of absorption were compared with reference formulation to prove its bioequivalence in healthy volunteers.
... The combination of ARB and thiazide diuretic results in additive lowering of BP and was recommended for treatment of essential hypertension [2]. A xed-dose combination of hydrochlorothiazide and irbesartan showed additive antihypertensive effect in a dose-dependent manner up to hydrochlorothiazide (HCTZ) 25 mg and irbesartan 300 mg with high tolerability in diverse patient groups [7]. BP-lowering potential and safety pro le of irbesartan/HCTZ combination were proved in clinical trials. ...
Background and objective
The combination antihypertensive therapy has shown greater blood pressure lowering potential as well as better adherence to the treatment. Therefore, a new generic fixed-dose combination containing irbesartan and hydrochlorothiazide was developed and rate and extend of absorption were compared with reference formulation to prove its bioequivalence in healthy volunteers.
Methods
A single-center, open-label, randomized, two-period, crossover, single dose study under fasting conditions, including at least 7-days washout period, was performed in 30 healthy male and female volunteers. Twenty blood samples were collected in each study period: prior to dosing (0:00) and up to 72:00 hours after dosing and plasma concentrations of irbesartan and hydrochlorothiazide were analyzed using preliminary validated methods.
Results
The 90% CIs for the geometric mean ratios of test and reference of Cmax and AUC0 − t were 89.22–98.80% and 100.58–115.11%, respectively, for irbesartan and 91.80–122.96% and 94.88–117.56%, respectively. Thus, the corresponding ratios of Cmax and AUC0 − t for irbesartan and hydrochlorothiazide met the predetermined criteria for bioequivalence (90% confidence intervals of the geometric mean ratios of test and reference within the 80.00% − 125.00%). Both the test and reference products demonstrated good tolerability profile in this population, and no serious AEs were observed.
Conclusions
Therefore, the test product (Irbesartan/hydrochlorothiazide 300/25 mg film-coated tablets, manufactured by Tchaikapharma High Quality Medicines Inc., Bulgaria) and the reference product (CoAprovel 300/25 mg film-coated tablets, manufactured by Sanofi Clir SNC, France) are considered bioequivalent.
... Clinically the problem-related side effects may be solved by introducing low-dose combination drugs for first-line antihypertensive therapy. The combination of Irbesartan and Hydrochlorothiazide is one of the right combinations for antihypertensive and effective to reduce blood pressure and oedema in hypertensive patients who are usually accompanied by complications and minimal side effects, namely hyperkalemia [1]. The combined use of angiotensin receptor (AR) blockers and diuretics is better tolerated, but more costly, than generic ACE inhibitors and diuretics, mostly because of the absence of cough and much lower incidence of angioedema [2]. ...
... Finally, IRB-HCT combination brings positive effects of IRB on undesired effects of diuretic, provides advantages of AR blockade, decreases resistance because of activated RAAS, simplifies treatment regimen, besides providing better BP control. Moreover, HCT may increase protective organ benefits of the AR antagonist by providing better BP control in this combination [1], [2], [4], [5], [6], [7]. ...
... Therefore, it is possible to evaluate the clinical efficacy under 2 main titles: BP-lowering efficacy, and the end-organ protection. The combination are fixed-dose combinations achieved BP targets in 77% of patients with systolic, 83% for diastolic and 69% for both BP levels [1], [2], [4], [5], [6], [7] ...
BACKGROUND: Irbesartan and hydrochlorothiazide are a group of anti-hypertensive drugs that are very effective and safe to use to reduce blood pressure and oedema. The combination has a small active ingredient content so that if the treatment didn't meet the requirements for therapeutic doses, it not achieved to the maximum therapy.
AIM: The research aims to the simultaneous determination of irbesartan and hydrochlorothiazide in tablets by Ratio subtraction spectrophotometry method.
METHODS: The absorption spectra and sample measurement in the Ratio subtraction method performed on Irbesartan at a wavelength of 247.6 nm and 273.6 nm for the Hydrochlorothiazide (HCT) using 0.1 N NaOH as a solution. This method is validated with linearity, accuracy, and precision in intraday and interday, LOD and LOQ and applied in the determination of a mixture of irbesartan and hydrochlorothiazide in the dosage tablet.
RESULTS: The validation test for IRB is 101.03 for accuracy, with a precision of 0.57; with precision testing at intraday 0.34 and interday 1.34, and LOD is 0.70 and LOQ is 2.12. Meanwhile, validation for HCT that the accuracy 100.34%; precision 0.89 and precision on intraday 1.20 and interday 1.18, and LOD 0.78 and LOQ 2.37 with IRB levels are 101.03 ± 0.63% and HCT is 100.59 ± 0.91%.
CONCLUSION: The ultraviolet spectrophotometric method in subtraction ratio method was validated a method of linearity, accuracy, precision in intraday and interday, LOD, and LOQ and according to ICH guidelines and successfully applied for the determination simultaneous of irbesartan and hydrochlorothiazide in the tablet's dosage form.
... These drugs are very effective in the elderly and very elderly patients[10]. These combinations has an additive antihypertensive effect, reducing blood pressure to a greater degree than either component alone[11]. The association of low-dosed diuretics in combination with RAAS blocking agents allows maximum benefit from potassium depletion and control of compensatory increase in renin secretion, so increasing the efficacy and safety of RAAS blockers. ...
... The association of low-dosed diuretics in combination with RAAS blocking agents allows maximum benefit from potassium depletion and control of compensatory increase in renin secretion, so increasing the efficacy and safety of RAAS blockers. Irbesartan is a potent and selective angiotensin II subtype 1 receptor antagonist indicated for use in patients with hypertension, including those with type 2 diabetes mellitus and nephropathy[11]. The combination of the ARB irbesartan with the thiazide diuretic hydrochlorothiazide (HCTZ) has demonstrated efficacy and safety as initial therapy in patients with moderate and severe hypertension as well as in a broad range of patients who do not achieve BP goal on antihypertensive monotherapy[12,13]. ...
... FDC of renin-angiotensin-aldosterone system (RAAS) inhibitor and a diuretic in low-doses shows higher reduction of blood pressure and response to therapy than both APIs administered separately. It also compensates the increased plasma renin activity provoked by the diuretic [22,23,24,25]. During the observed period FDCs of sartan and diuretic performed steady increase in their dosage forms, trademarks and new international non-proprietary name (INN). ...
... For example irbesartan/HCT combination, proved to be safe, well tolerated and give better patients adherence. [28][29][30] The TALENT study, instead, suggested that nifedipine and telmisartan as monotherapy have a similar effect on blood pressure, but a synergistic effect when taken simultaneously, both on clinical and ambulatory blood pressure. 31,32 Given these positive results, recently fixed combination tablets containing both a calcium channel blocker and an ARB/ACE inhibitor have become available: one combination is enalapril/lercanidipine, this once-daily administration of a fixed-dose enalapril/lercanidipine, by bringing together two distinct and complementary mechanisms of action, reduces BP effectively and has the potential for improved target organ protection relative to either class agent alone. ...
Despite the availability of a wide range of antihypertensive medications, about 45.5% of treated patients in the US fail to achieve a blood pressure control target of <140/90 mmHg; for this reason, in the last two years, some emerging treatments have become available such as aliskiren, a renin inhibitor. A lot of trials showed that aliskiren proved to be safe and effective in monotherapy in reducing blood pressure, with a blood pressure-lowering effect similar, if not superior, to that of other first-line antihypertensive agents, and to be safe also in combination with various other antihypertensive medications. However, recently the European Medicines Agency decided to early terminate the ALTITUDE study, due to more cases of stroke, renal complications, hyperkalemia and hypotension in patients who received aliskiren compared with patients who received a placebo. Given these discrepancies, we conducted a review about the emerging pharmacotherapies for the management of hypertension focusing our attention on the latest class of antihypertensive drugs become available, such as renin inhibitor aliskiren. After an accurate review of all the most important studies conducted, we can conclude that aliskiren proved to be safe and well tolerated and to have some protective effects on heart and kidney, not observed with the other drugs. However, until further data will not be available, aliskiren should not be prescribed in combination with ACE inhibitors or ARBs. In combination with other anti-hypertensive drugs, instead, aliskiren should be considered for the treatment of hypertension in not well controlled hypertensive patients.
... I was very interested to read the recent review by Derosa et al. [1] in the journal Current Vascular Pharmacology (2009; 7(2): 120-136) entitled " Irbesartan and hydrochlorothiazide association in the treatment of hypertension " . There are many drugs available today to block the reninangiotensin system and often they are associated with di-uretic treatment. ...
Introduction: Current guidelines for pharmacotherapy briefly describe a role for combination antihypertensive therapy. However, guidance on whether combination therapy should be used at the time of initiating therapy or as add on, and the choice of combination therapy is scarce.
Areas covered: Current literature suggests that intensive blood pressure control is the key to managing cardiovascular risk. Along with lifestyle management, pharmacotherapy is an central component in the treatment of hypertension. Here, we aim to review the pathophysiology of hypertension, rationale for using combination therapy, and the different combinations of antihypertensive drug classes that are available in the market. Papers from 1967 through 2016 listed on PubMed on this topic were reviewed.
Expert Commentary: Based on the review of the literature, combination antihypertensive therapies are more effective than monotherapy and are also well tolerated, safe and cost effective for treatment of hypertension. Further research is needed to help guide the choice of combination antihypertensive therapy in different patient populations based on age, gender, race and comorbidities.
