AMLODIPINE PHARMACOKINETICS ine is a dihydropyridine calcium antagonist that was synthesized in an attempt to develop a compound with a typical dihydropyridine pharmacologic profile, which would also have the properties of increased oral bioavailability and low clearance in humans. The disposition of amlodipine, a new calciumchannel blocker with a slow onset and long duration of action, has been investigated in humans and in the animal species used in the evaluation of drug efficacy and safety. Pharmacokinetic studies were conducted with nonlabeled drug using specific high-pressure liquid chromatography or gas chromatographic. Myocardial dynamic effects and pharmacokinetics of amlodipine were studied in the isolated retrogradely perfused and spontaneously beating guinea-pig heart. Pharmacokinetic analysis of drug accumulation showed one-compartment characteristics with an half-life of 76 min The present study investigates the effects of diabetes mellitus on the pharmacokinetics and pharmacodynamics of amlodipine in hypertensive subjects with and without diabetes mellitus to determine whether the diabetic state alters these parameters
Background: Amlodipine is rarely used in the treatment of pregnant hypertensive women due to limited pharmacokinetic data during pregnancy and the postpartum period. Objective: To evaluate the pharmacokinetics of amlodipine besylate in the peri-partum period including quantities of placental passage, breast milk excretion and infant exposure Amlodipine, a third-generation dihydropyridine calcium antagonist, has a mode of action and pharmacodynamic profile which are comparable to those of conventional compounds in this series, such as nifedipine. Its physicochemical behavior, however, appears to be somewhat different. A pKa value of 8.7 The pharmacokinetics of amlodipine in healthy volunteers after single intravenous and oral doses and after 14 repeated oral doses given once daily Br J Clin Pharmacol. 1986 Jul;22(1):21-5. doi: 10.1111/j.1365-2125.1986.tb02874.x. Authors J K Faulkner, D. Amlodipine is a calcium channel blocker medication used to treat high blood pressure and coronary artery disease. While not typically recommended in heart failure, amlodipine may be used if other medications are not sufficient for treating high blood pressure or heart-related chest pain
Amlodipine pharmacokinetics The effect of sildenafil on arterial pressure has been tested in 16 hypertensive men taking amlodipine 5-10 mg/day (23). Sildenafil did not affect amlodipine pharmacokinetics, but caused a further additive fall in blood pressure. Adverse events with the combination of sildenafil and amlodipine, headache, dyspepsia, and nausea, did not require drug withdrawal Amlodipine is a low-clearance, dihydropylidine calcium antagonist. The slow rate of elimination (elimination half-life of 40-60 h) confers several pharmacokinetic characteristics that are not seen with other calcium-antagonist drugs. It has high oral bioavailability (60-80%) and accumulates to a steadystate with once-daily administration over a. Amlodipineoralandintravenouspharmacokinetics gas(1 mlmin-)anddetectormakeupgas(35ml minil) being nitrogen. The temperature was programmedfrom280to3200 Cat20°Cminr1, andthenkeptat3200Cfor9min.Theinjection portanddetectortemperaturesweremaintained at3200C. Undertheseconditions, theretention times of amlodipine and the internal standar Amlodipine is a dihydropyridine calcium antagonist and is widely used for the treatment of cardiovascular diseases. Amlodipine has two stereoisomers [R(+), S(-)], and only the S(-) isomer exerts vasodilating action. In this preliminary study, amlodipine (5 mg) was given to three elderly hypertensive
With chronic oral dosing of amlodipine once daily for 14 days, support was provided for the linearity of amlodipine's pharmacokinetics and absence of such with chronic oral dosing with verapamil, diltiazem, and nifedipine. In the elderly population, elimination half-life of 5 mg oral doses is significantly prolonged (48 vs 35 hours; p less than. The objective of this study was to compare the pharmacokinetic (PK) profiles of HCP1401, a fixed-dose combination of amlodipine 5 mg, losartan 100 mg, and chlorthalidone 25 mg, with the separate components (loose combination) of amlodipine/losartan 5/100 mg and chlorthalidone 25 mg Purpose: Because of the developing theoretical basis that diabetes mellitus (DM) and its complications may provoke important alterations of pharmacokinetics (PK) and pharmacodynamics (PD) of cardiovascular drugs [Diabetes Care 1999;22:982-8], we investigated the comparative PK and PD of amlodipine in hypertensive subjects with and without Type II DM The current study will evaluate the plasma pharmacokinetics of amlodipine in a cohort of 8 adult volunteers who are receiving regular hemodialysis treatment (HD) 3 days a week for 4 hours each day and have been taking a total daily dose of 5-10 mg of amlodipine besylate for >30 days as part of their usual care
Safety and Pharmacokinetics Study of Amlodipine 10mg and Candesartan 32mg The safety and scientific validity of this study is the responsibility of the study sponsor and investigators. Listing a study does not mean it has been evaluated by the U.S. Federal Government Abstract. Amlodipine is currently available as the besylate salt (Norvasc®, Pfizer Inc.). The pharmacokinetic similarities of amlodipine maleate (AmVaz ™, Reddy Pharmaceuticals Inc.) compared with the besylate salt (Norvasc) were demonstrated in two studies.Two open-label, single-dose, pharmacokinetic studies included healthy nonsmoking volunteers PURPOSE: To build a physiologically based pharmacokinetic (PBPK) model for fimasartan, amlodipine, and hydrochlorothiazide, and to investigate the drug-drug interaction (DDI) potentials. METHODS: The PBPK model of each drug was developed using Simcyp software (Version 15.0), based on the information obtained from literature sources and in vitro.
PHARMACOKINETICS AND DISPOSITION Population pharmacokinetic modelling to quantify the magnitude of drug-drug interactions between amlodipine and antiretroviral drugs Perrine Courlet 1 & Monia Guidi1,2,3 & Susana Alves Saldanha1 & Matthias Cavassini4 & Marcel Stoeckle5 & Thierry Buclin1 & Catia Marzolini5 & Laurent A. Decosterd 1 & Chantal. Amlodipine is a long-acting calcium antagonist of the dihydropyridine class which is of value in treating hypertension and the symptoms of angina pectoris .The clinical pharmacokinetics of amlodipine have previously been reviewed .There is as yet only a single study on the pharmacokinetics of amlodipine in patients with renal failure .In this study, 27 patients were separated into five. The pharmacokinetic parameters of amlodipine alone are in good agreement with reported values, still with a lower apparent clearance in our analysis [6,7,8,9]. Several studies used a 2-compartment model to describe amlodipine concentration-time profile [ 7 , 10 , 19 ] CONTEXT: Danshen tablets (DST), an effective traditional Chinese multi-herbal formula, are often combined with amlodipine (ALDP) for treating coronary heart disease. OBJECTIVE: This study investigated the effects of DST on the pharmacokinetics of ALDP and the potential mechanism Amlodipine was well tolerated. Renal impairment had little effect on the pharmacokinetics of amlodipine. The elimination half-life was of the order of 50 h, similar to previously reported values and did not vary with renal function. Steady-state pre-dose concentrations were observed after the ninth dose
Amlodipine is rarely used in the treatment of pregnant hypertensive women due to limited pharmacokinetic data during pregnancy and the postpartum period. Objective To evaluate the pharmacokinetics of amlodipine besylate in the peri-partum period including quantities of placental passage, breast milk excretion and infant exposure The pharmacokinetics of amlodipine are not significantly altered in elderly or renally impaired patients, but there is reduced clearance in patients with hepatic impairment. There are no pharmacokinetic interactions between amlodipine and cimetidine or digoxin. AB - Structural features of amlodipine give the molecule physicochemical and. Abernethy DR. The pharmacokinetic profile of amlodipine. Am Heart J. 1989;118(5 Pt 2):1100-1103. 30. Meredith PA, Elliott HL. Clinical pharmacokinetics of amlodipine. Clin Pharmacokinet. 1992;22(1):22-31. 31. Zhu Y, Wang F, Li Q, et al. Amlodipine metabolism in human liver microsomes and roles of CYP3A4/5 in the dihydropyridine dehydrogenation The pharmacokinetics of amlodipine and olmesartan in healthy volunteers after coadministration of amlodipine besylate and olmesartan medoxomil concomitantly as separate dosage forms and together in a fixed-dose combination tablet were characterized in 5 phase I, randomized, crossover studies. The mean steady-state pharmacokinetics of amlodipine.
. A single intravenous dose of 10 mg resulted in an absolute bioavailability of 64% and a calculated. To investigate the effects of coadministration of esaxerenone with amlodipine on the pharmacokinetics (PK) of each drug, and of esaxerenone on the PK of digoxin. In three open-label, single-sequence, crossover studies, healthy Japanese males received single oral doses of esaxerenone 2.5 mg (Days 1, 15), with amlodipine 10 mg/day (Days 8-18) (Study 1, N = 24); single doses of amlodipine 2.5. The pharmacokinetics of amlodipine in healthy volunteers after single intravenous and oral doses and after 14 repeated oral doses given once daily. JK Faulkner, Search for more papers by this author. D McGibney, Search for more papers by this author. LF Chasseaud The pharmacokinetics of amlodipine are not significantly influenced by renal impairment. Patients with renal failure may therefore receive the usual initial dose. Elderly patients and patients with hepatic insufficiency have decreased clearance of amlodipine with
PHARMACOKINETICS AND DISPOSITION Population pharmacokinetic modelling to quantify the magnitude of drug-drug interactions between amlodipine and antiretrovira Description: Amlodipine, a dihydropyridine Ca-channel blocker, reduces peripheral vascular resistance and BP by relaxing coronary vascular smooth muscle and coronary vasodilation through inhibition of Ca ion transmembrane influx into cardiac and vascular smooth muscles. Onset: 24-48 hours. Duration: 24 hours. Pharmacokinetics: Absorption: Well absorbed from the gastrointestinal tract The aim of the present study was to explore the effects of common genetic polymorphisms of cytochrome P450 (CYP)3A4, CYP3A5, cytochrome P450 oxidoreductase (POR) and multidrug resistance protein 1 (MDR1) on the pharmacokinetics and pharmacodynamics of amlodipine in primary hypertensive patients. The mild‑to‑moderate essential hypertension patients were recruited to complete the genotyping. Amlodipine is a dihydropyridine calcium antagonist drug with distinctive pharmacokinetic characteristics which appear to be attributable to a high degree of ionisation
Introduction. Cardiovascular diseases (CVDs) are one of the most prevalent causes of fatality worldwide, contributing to 17.9 million deaths each year (approximately 31% of all global deaths). 1 CVDs are multifactorial disorders caused by multiple risk factors, including hypertension, dyslipidemia, and obesity. Various epidemiological studies have shown that hypertension and dyslipidemia are. Sildenafil: Amlodipine pharmacokinetics were not affected when amlodipine was co-administered with an individual sildenafil dose of 100 mg in patients with essential . 4 hypertension. Combination therapy of amlodipine and sildenafil, results in each drug individually utilising its own reducing effect on blood pressure.. Amlodipine, like other 1,4-dihydropyridine calcium channel antagonists is a substrate for CYP3A4 [12, 16]. However, unlike the other drugs in its class, grapefruit juice which inhibits CYP3A4 failed to alter the pharmacokinetics of amlodipine
Pharmacokinetic parameters of racemic amlodipine (AUC, C max, t max, and k el) were not markedly changed with grapefruit juice coadministration. Total plasma clearance and volume of distribution, calculated after intravenous amlodipine, were essentially unchanged by grapefruit juice (CL 6.65 ml min −1 kg −1 , juice vs 6.93 ml min −1 kg. The pharmacokinetic properties of each drug after coadministration of telmisartan and S-amlodipine were compared with those of each drug administered alone. Tolerability was assessed using measurements of vital signs, clinical chemistry tests, and interviews selectivity in amlodipine pharmacokinetics. For haemodynamic measures, area under the effect-time curves [AUEC(0,24 h)] were calculated for indivi-dual subjects using the linear trapezoidal method. Maximum changes in systolic blood pressure, diastolic blood pressure, and heart rate were also tabulated for individual subject
Comparative pharmacokinetics of a fixed-dose combination vs concomitant administration of telmisartan and S-amlodipine in healthy adult volunteers Minkyung Oh,1,2,* Sung-Eun Park,3,* Jong-Lyul Ghim,1-3 Young-Kyung Choi,1 Eon-Jeong Shim,1-3 Jae-Gook Shin,1-3 Eun-Young Kim1-3 1Department of Pharmacology, 2PharmacoGenomics Research Center, Inje University College of Medicine, Busan. Background. The aim of this study was to investigate the effects of P450 oxidoreductase (POR) genetic polymorphisms on the pharmacokinetic parameters of amlodipine.Methods. After a single 10-mg dose of amlodipine administration, 25 healthy male subjects completed genotyping for 12 single nucleotide polymorphisms (SNPs) of the POR genes, cytochrome P450 (CYP)3A4 g.25343G>A (CYP3A4*1G), and. Also this finding may be attributable to the pharmacodynamic profile of amlodipine with a slow onset of action, a lower plasma peak, and a longer duration of action. 16, 17 A superior relation between response rate and side effects of amlodipine in comparison with felodipine was reported by van der Krogt et al. 18 Also Hoegholm et al 19.
Pharmacokinetics of Amlodipine Thus, although structurally related to other dihydropyridine derivatives, amlodipine displays significantly different pharmacokinetic characteristics and is suitable for administration in a single daily dose. Amlodipine is a recently developed member of the 1,4-dihydropyridine class of calcium antagonist drugs. Amlodipine is slowly and almost completely absorbed from the gastrointestinal tract. Peak plasma concentrations are reached 6-12 hour following oral administration. Its estimated bioavailability is 64-90%. Absorption is not affected by food. Volume of distribution: Not Available: Protein binding: 97.5%: Metabolis Background Amlodipine is rarely used in the treatment of pregnant hypertensive women due to limited pharmacokinetic data during pregnancy and the postpartum period
Since only amlodipine was entered without any further substances, no pharmacokinetic interaction can be detected.. Rating: The pharmacokinetic parameters of the average population are used as the starting point for calculating the individual changes in exposure due to the interactions. Amlodipine has a mean oral bioavailability [F ] of 64%, which is why the maximum plasma levels [Cmax] tend to. Pharmacokinetics of amlodipine are not significantly affected by renal impairment; therefore no dosage adjustment necessary; Hepatic impairment. Lower initial dose may be required for patients with hepatic impairment; Consider starting with 2.5 mg/day P The pharmacokinetics of amlodipine have not been studied in severe hepatic impairment. Amlodipine should be initiated at the lowest dose and titrated slowly in patients with severe hepatic impairment. Method of administration . Tablet for oral administration. 4.3 Contraindications
. Amlodipine should be initiated at the lowest dose and titrated slowly in patients with severe hepatic impairment. Method of administration. Tablets for oral administration. The tablets should be taken with a glass of water independently from meals Pharmacokinetics of Amlodipine Besylate at Delivery and During Lactation The safety and scientific validity of this study is the responsibility of the study sponsor and investigators. Listing a study does not mean it has been evaluated by the U.S. Federal Government
Amlodipine is a dihydropyridine calcium channel blocker (CCB) and is usually well tolerated up to 10 mg daily dose. It is one of the most widely prescribed anti-hypertensive agents. The reported chronic gastrointestinal side effects from amlodipine include constipation, dyspepsia, dysphagia, diarrhea, flatulence and pancreatitis Amlodipine is currently available as the besylate salt (Norvasc®, Pfizer Inc.). The pharmacokinetic similarities of amlodipine maleate (AmVaz™, Reddy Pharmaceuticals Inc.) compared with the. Amlodipine. The pharmacokinetics of amlodipine are not significantly influenced by renal impairment. Patients with renal failure may therefore receive the usual initial dose. Olmesartan medoxomil. In patients with renal insufficiency, serum concentrations of olmesartan were elevated compared to subjects with normal renal function
Bariatric Surgery and Pharmacokinetics of Amlodipine The safety and scientific validity of this study is the responsibility of the study sponsor and investigators. Listing a study does not mean it has been evaluated by the U.S. Federal Government Pharmacokinetics of amlodipine in dogs with or without vagotomy The mean venous plasma concentrationâ time profiles of amlodipine following oral administration of an amlodipine orotate tablet in dogs with and without vagotomy are shown in Figure 1, and some relevant pharmacokinetic parameters are listed in Table 1
The of the combined administration of amlodipine pharmacokinetic parameters of amlodipine were and atorvastatin as separate tablets (section not significantly altered during coadministration 4.1.1) or as a fixed-dose, single-tablet formula-  with antacid, cimetidine or sildenafil. In clin- tion (section 4.1.2) in patients with hypertension. Amlodipine pharmacokinetics was affected by the genetic polymorphisms of the ABCB1 gene in humans. These ﬁndings may provide a plausible explanation for interindividual variation in the disposition of amlodipine, although our study could not explain the exact mechanism(s) by which the polymorphic ABCB1 gene paradox The pharmacokinetics of amlodipine are not significantly influenced by renal impairment. Patients with renal failure may therefore receive the usual initial dose. Elderly patients and patients with hepatic insufficiency have decreased clearance of amlodipine with a resulting increase in AUC of approximately 40 to 60%, and a lower initial dose.
Translations in context of pharmacokinetics of simvastatin, amlodipine in English-Portuguese from Reverso Context: In addition there was no clinically significant effect of ivabradine on the pharmacokinetics of simvastatin, amlodipine, lacidipine, on the pharmacokinetics and pharmacodynamics of digoxin, warfarin and on the pharmacodynamics of aspirin CHEBI:2668 - amlodipine. A fully substituted dialkyl 1,4-dihydropyridine-3,5-dicarboxylate derivative, which is used for the treatment of hypertension, chronic stable angina and confirmed or suspected vasospastic angina. This entity has been manually annotated by the ChEBI Team. We are unable to retrieve the vendor information for this entry at.
Amlodipine is a calcium channel blocking agent that selectively blocks calcium ion reflux across cell membranes of cardiac and vascular smooth muscle without changing serum calcium concentrations. It predominantly acts on the peripheral circulation, decreasing peripheral vascular resistance, and increases cardiac output The pharmacokinetics of the coadministration of fimasartan and amlodipine were compared with that of each drug alone. Results: The geometric mean ratio and 90% confidence intervals for C max,ss and area under the plasma concentration-time curve (AUC)τ ,ss of fimasartan (with/without amlodipine) were 1.096 (0.746-1.610) and 1.163 (1.001-1.351. Amlodipine is a medicine used to treat high blood pressure (hypertension).. If you have high blood pressure, taking amlodipine helps prevent future heart disease, heart attacks and strokes.. Amlodipine is also used to prevent chest pain caused by heart disease. This medicine is only available on prescription
Amlodipine, losartan and combined amlodipine and losartan were administered to 24 healthy male participants during periods 1, 2 and 3, respectively, for 9 days each. The pharmacokinetics of amlodipine, losartan and EXP‐3174, an active metabolite of losartan, were assessed at steady‐state The pharmacokinetics of amlodipine are not significantly influenced by renal impairment. Patients with renal failure may therefore receive the usual initial dose. Elderly patients and patients with hepatic insufficiency have decreased clearanceof amlodipine with a resulting increase in AUC of approximately 40-60%, and a lower initial dose may. Nebivolol Hydrochloride Pharmacokinetics Absorption Bioavailability. Absolute bioavailability not determined. Following oral administration, mean peak plasma concentrations occur within approximately 1.5-4 hours. Food. Food does not alter pharmacokinetics; however, may slightly reduce nebivolol glucuronides. Distribution Exten Results The maximum blood concentration (Cmax) of amlodipine in carriers of g.57332T>C and g.56551G>A SNPs of the POR gene was statistically significantly different. In addition, T‐allele carriers of g.57332T>C had a 21% higher Cmax than those with the CC genotype (p = .007)