Effect of telmisartan 80 mg once daily on 24-h blood pressure profile in patients with mild-to-moderate hypertension failing to respond to prior antihypertensive therapy

Carrillo, José Z Parra; Fernández, M; Barrera, Manuel; Bahena, Judith Huerta; Estrella, Michelle M.; Ruiz, R; Lepe, Luis; Arriaga, R.; Bonilla, Carlos A.; Fonseca, Salvador; Miranda, Sandra Marina Ribeiro de; Segovia, Carmen Rondon; Viesca, M.D.C. García Luna

doi:10.1111/j.1742-1241.2004.00404.x

Cited by 4 publications

(4 citation statements)

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“…10 Specifically, one randomised, double-blind multicentre study evaluated long-term telmisartan administration in patients with isolated systolic hypertension, showing in more than 50% of the treated hypertensives a target reduction in SBP, defined as a systolic value < 140 mmHg or a decrease of > 20 mmHg. 11 These figures have been confirmed by a number of studies performed by employing 24-hour ABPM, [12][13][14][15][16][17][18] which additionally documented both in uncomplicated and complicated hypertension (renal insufficiency, renal failure, diabetes mellitus, obesity as well as metabolic syndrome) that 1) the drug effectively reduces BP values throughout the 24-hour average interval, 2) the antihypertensive effect follows the circadian rhythm of BP, allowing protection of the cardiovascular system against the early morning BP rise and its adverse effects on the heart and vital organs. [12][13][14][15][16][17][18][19] Two other main issues, referring to the results of the studies published so far aimed at fully characterising the antihypertensive efficacy of telmisartan, should be worthy of mention.…”

Section: O P Y R I G H T J R a A S L I M I T E D R E P R O D U C T I O N P R O H I B I T E Dmentioning

confidence: 81%

“…11 These figures have been confirmed by a number of studies performed by employing 24-hour ABPM, [12][13][14][15][16][17][18] which additionally documented both in uncomplicated and complicated hypertension (renal insufficiency, renal failure, diabetes mellitus, obesity as well as metabolic syndrome) that 1) the drug effectively reduces BP values throughout the 24-hour average interval, 2) the antihypertensive effect follows the circadian rhythm of BP, allowing protection of the cardiovascular system against the early morning BP rise and its adverse effects on the heart and vital organs. [12][13][14][15][16][17][18][19] Two other main issues, referring to the results of the studies published so far aimed at fully characterising the antihypertensive efficacy of telmisartan, should be worthy of mention. The first one refers to the evidence collected in comparative studies (many of them based on home or ABPM) that the drug displays BPlowering effects similar for magnitude to those of amlodipine, atenolol, enalapril, lisinopril 16,17,[20][21][22][23][24][25] but greater than those of nifedipine gastrointestinal therapeutic system (GITS), ramipril, perindopril, losartan, valsartan, eprosartan and hydrochlorothiazide.…”

Section: O P Y R I G H T J R a A S L I M I T E D R E P R O D U C T I O N P R O H I B I T E Dmentioning

confidence: 81%

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Review: Cardioprotective effects of telmisartan in uncomplicated and complicated hypertension

Quartı-Trevano

Mancia

2008

J Renin Angiotensin Aldosterone Syst

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The development of angiotensin II receptor blockers (ARB) as a new class of drugs for the management of hypertension has elicited the attention of many clinicians worldwide with the aim of improving blood pressure (BP) control as well as cardiovascular protection.AmongARB telmisartan has been shown to be characterised by an antihypertensive efficacy fully covering the 24-hour period, thereby allowing to antagonise the adverse effects of early morning BP rise on cardiovascular risk. Other specific effects of the drug are represented by its favourable metabolic profile (particularly on insulin sensitivity) and neutral effects on sympathetic cardiovascular function.These properties are coupled with cardioprotective effects, documented by the evidence that the drug: 1) is effective in favouring the regression of cardiac and vascular organ damage, 2) reduces arterial stiffness and improves vascular distensibility and 3) reverses the endothelial dysfunction typical of the hypertensive state particularly when complicated by renal failure, diabetes, obesity or metabolic syndrome. Several of these properties can account for the results of the ONgoing Telmisartan Alone and in combination with Ramipril Global Endpoint Trial (ONTARGET), documenting the beneficial effects on the drug on cardiovascular morbidity and mortality.

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Section: O P Y R I G H T J R a A S L I M I T E D R E P R O D U C T I O N P R O H I B I T E Dmentioning

confidence: 81%

Section: O P Y R I G H T J R a A S L I M I T E D R E P R O D U C T I O N P R O H I B I T E Dmentioning

confidence: 81%

Review: Cardioprotective effects of telmisartan in uncomplicated and complicated hypertension

Quartı-Trevano

Mancia

2008

J Renin Angiotensin Aldosterone Syst

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“…Each drug was administered once daily for 6 days either alone or in combination in a crossover fashion. Blood samples for concentration measurements were taken before the first dose and the fifth dose and at 0, 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3,4,5,6,8,12,16,24,48 and 72 hr after the last dose. Cardiovascular observations consisting of systolic and diastolic blood pressure and HR were measured using digital blood pressure cuffs before dosing from the first to the fifth dose and at 0, 2, 4, 8, 12, 24, 48 and 72 hr after the last dose.…”

Section: Methodsmentioning

confidence: 99%

“…It is well known that cardiovascular variables are subject to a 24-hr diurnal rhythm [16]. For example, three harmonic oscillators of periods 8, 12 and 24 hr have been identified [17].…”

Section: Pd Modelsmentioning

confidence: 99%

Mechanistic Model for Blood Pressure and Heart Rate Changes Produced by Telmisartan in Human Beings

Chae

Son

Kim

et al. 2017

Basic Clin Pharma Tox

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Telmisartan, an angiotensin receptor blocker (ARB), is indicated for the treatment of essential hypertension. This study aimed to develop a mechanistic model of telmisartan drug effect in human beings using non-invasive markers. Data were acquired from a previous study where telmisartan 80 mg was given once daily for 6 days. Systolic (SBP) and diastolic blood pressure (DBP) and heart rate (HR) were measured before dosing for days 1-5 and serially after the last dose. Mean arterial pressure (MAP) and pulse pressure (PP) were calculated from SBP and DBP. Relationships between MAP, PP, HR and total peripheral resistance (TPR) were developed. Circadian variation was incorporated into PP and HR, and TPR was assumed to adjust itself in response to changes in PP and HR based on baroreflex mechanism. Drug effects were then described as lowering the set point of MAP through TPR with a physiological feedback effect stimulating HR and PP. Drug concentrations were described by a two-compartment disposition model with first-order absorption and lag time, and first-order elimination. Circadian variation was described by cosine functions, having periods of 12 and 24 hr. A log-linear model was used to describe drug effect, with estimated drug effect parameter of 0.051/hr. Estimated fractional turnover rate of PP, HR and TPR was 11.2 hr. The model successfully described the time courses of these cardiovascular variables. This work demonstrated the feasibility of using non-invasive cardiovascular measurements to derive a mechanistic model for telmisartan in human beings. The model may be suitable for other ARBs.Telmisartan is an antagonist of the angiotensin II type 1 (AT1) receptor that is used for the treatment of hypertension. It selectively inhibits stimulation of the AT1 receptor by angiotensin II. It has a high volume of distribution and is eliminated mainly by the kidneys which results in a long terminal elimination half-life. The compound is not metabolized by cytochrome P450 isoenzymes and has a low risk for P450-based drug interactions [1,2].The action of telmisartan is known to lead to inhibition of aldosterone secretion and reduced vasoconstriction. The time course of its effect involves both rapid and slow responses. The rapid response is mainly due to antagonizing angiotensin II vasoconstriction. The slow response is due to antagonizing angiotensin-mediated aldosterone secretion which leads to a natriuretic effect, followed by decreased plasma volume and consequent decrease in cardiac stroke volume. Both the rapid and slow effects contribute to lowering of blood pressure [1].A population pharmacokinetic (PK) model for telmisartan was first published in 2003 [3] and reported that a two-compartment disposition model with first-order absorption and elimination described the data. A PKPD model of telmisartan has been published [4] in spontaneously hypertensive rats. To the authors' knowledge, no PKPD model of telmisartan has been published in human beings. Previous PKPD models used either an empirical modelli...

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Antihypertensive activity of angiotensin II AT1 receptor antagonists: a systematic review of studies with 24 h ambulatory blood pressure monitoring

Fabiá

Abdilla

Oltra

et al. 2007

Journal of Hypertension

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Effect of telmisartan 80 mg once daily on 24-h blood pressure profile in patients with mild-to-moderate hypertension failing to respond to prior antihypertensive therapy

Cited by 4 publications

References 29 publications

Review: Cardioprotective effects of telmisartan in uncomplicated and complicated hypertension

Review: Cardioprotective effects of telmisartan in uncomplicated and complicated hypertension

Mechanistic Model for Blood Pressure and Heart Rate Changes Produced by Telmisartan in Human Beings

Antihypertensive activity of angiotensin II AT1 receptor antagonists: a systematic review of studies with 24 h ambulatory blood pressure monitoring

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