Amlodipine, a dihydropyridine calcium antagonist, was synthesized in an attempt to develop a compound with a pharmacokinetic profile characteristic of this class, which would also have an increased oral bioavailability and extended clearance time Amlodipine is a dihydropyridine calcium antagonist drug with distinctive pharmacokinetic characteristics which appear to be attributable to a high degree of ionisation. Following oral administration, bioavailability is 60 to 65% and plasma concentrations rise gradually to peak 6 to 8h after administration Author information: (1)Institute of Pharmacology, University of Aarhus, Denmark. 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.
Amlodipine besylate is the besylate salt of amlodipine, a long-acting calcium channel blocker ecific high-pressure liquid chromatography or gas chromatographic procedures. The metabolic fate of the drug was investigated in mice, rats, dogs, and humans using [4-14C]-amlodipine. After intravenous administration, the percentages of the dosed radioactivity recovered in urine were 62% in humans, 45% in dogs, 38% in rats, and 25% in mice. The remainder of the doses were recovered in the. Amlodipine is a dihydropyridine calcium antagonist (calcium ion antagonist or slow-channel blocker) that inhibits the transmembrane influx of calcium ions into vascular smooth muscle and cardiac muscle. Experimental data suggest that amlodipine binds to both dihydropyridine and nondihydropyridine binding sites
Amlodipine is a dihydropyridine calcium antagonist (calcium ion antagonist or slow-channel blocker) that inhibits the transmembrane influx of calcium ions into vascular smooth muscle and cardiac muscle. Experimental data suggest that Amlodipine binds to both dihydropyridine and nondihydropyridine binding sites Following oral administration of 10 mg amlodipine to 20 male volunteers, pharmacokinetics of amlodipine, geometric mean Cmax of amlodipine was 6.2 ng/mL when the drug was administered with grapefruit juice and 5.8 ng/mL when administered with water. Mean Tmax of amlodipine was 7.6 hours with grapefruit juice and 7.9 hours with water Amlodipine is a calcium-channel blocking agent; a dihydropyridine derivative with an intrinsically long duration of action The two amlodipine formulations showed similar pharmacokinetic and pharmacodynamic characteristics and the new amlodipine formulation, amlodipine nicotinate, was found to be equivalent for pharmacokinetics to the currently available amlodipine besylate with respect to the rate and extent of amlodipine absorption
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, a main series of L-type calcium channel blockers (CCBs), exerts potent antihypertensive effects. The aim of this trial was to explore the pharmacokinetics (PK) and safety with bioequivalence of orally administered Amlodipine provided by two sponsors in healthy volunteers (HVs). Method
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 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
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. Drug Metab Dispos. 2014;42(2):245-249. 32. Stangier J, Su CA Bioavailability File: Amlodipine Amlodipine (AML), a third-generation dihydropiridin, is a long-acting L-calcium channel blocker used in the treatment of hypertension and angina pectoris. It exerts.. 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- 60%, and a lower initial dose may. Learn More About the Potential Side Effects of Amlodipine. Includes. 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
T1 - Pharmacokinetics and pharmacodynamics of Amlodipine. AU - Abernethy, D. R. PY - 1992/1/1. Y1 - 1992/1/1. N2 - 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 An Overview of the Pharmacokinetics and Pharmacodynamics of Amlodipine in Elderly Persons with Systemic Hypertension Darrell R. Abernethy, MD, PhD Pharmacokinetic and pharmacodynamte data were compared between elderly and young pa- tients with hypertension who received single in- travenous doses of amlodipine, a dihydropyridine calcium antagonist, followed by oral administra- tion of.
may cause gingival hyperplasia. grapefruit juice may increase drug level. monitor blood pressure and pulse prior to and during therapy. monitor intake and output. assess for signs of CHF. assess characteristics of angina. instruct patient of interventions for hypertension and how to take blood pressure Amlodipine is a dihydropyridine calcium antagonist drug with distinctive pharmacokinetic characteristics which appear to be attributable to a high degree of ionisation. Following oral administration, bioavailability is 60 to 65% and plasma concentrations rise gradually to peak 6 to 8h after administration. Amlodipine is extensively metabolised. Summary: 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 procedures 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. See section 4.4 Special warnings and special precautions for use. Patients with renal impairmen . Study design This was a prospective study of pregnant women who were prescribed 5 mg of amlodipine daily for treatment of chronic hypertension and delivered at term
12 CLINICAL PHARMACOLOGY 12.1 Mechanism of Action CADUET is a combination of two drugs, a dihydropyridine calcium channel blocker (amlodipine) and an HMG-CoA reductase inhibitor (atorvastatin). The amlodipine component of CADUET inhibits the transmembran Currently approved calcium-channel blockers (CCBs) bind to L-type calcium channels located on the vascular smooth muscle, cardiac myocytes, and cardiac nodal tissue (sinoatrial and atrioventricular nodes). These channels are responsible for regulating the influx of calcium into muscle cells, which in turn stimulates smooth muscle contraction. Pharmacokinetics. Amlodipine is well absorbed following oral administration with peak blood concentrations occurring after 6-12 hours. The bioavailability varies but is usually about 60-65%. Amlodipine is reported to be about 97.5% bound to plasma proteins
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 Amlodipine: The pharmacokinetics of amlodipine is not significantly influenced by renal impairment [see Dosing and Administration (2.2) and Use in Specific Populations (8.6)]. Hepatic Impairment: Perindopril: The bioavailability of perindoprilat is increased in patients with impaired hepatic function
Development of separate enantiomers improves pharmacokinetics (PK) and avoids undesirable AEs . From R- and S-isomers of amlodipine, S-enantiomer has nearly 1000 times greater affinity for the receptor site. Further, S-amlodipine (S-AM) has less variable PK, lower intrasubject variation, and longer half-life Amlodipine besylate (Norvasc) is a calcium channel-blocker that is usually indicated for patients with angina pectoris due to coronary artery spasms. Generic Names & Brand Names amlodipine besylate (am loe' di peen) Norvasc Pregnancy Category C Drug classes Calcium channel-blocker Antianginal drug Antihypertensive Therapeutic actions Inhibits the movement of calcium ions across the membranes.
The geometric means of the primary pharmacokinetic parameters at steady state (day 9) for amlodipine when given alone were the following: maximum plasma concentration (C max) 17.7 ng/mL, area under the plasma concentration-time curve (AUC) 331 ng•h/mL, and renal clearance 39.5 mL/min, with 8% of the total amlodipine dose being excreted To evaluate the impact of age on the pharmacokinetics and blood pressure (BP) responses of a dihydropyridine (DHP) with large versus small first-pass metabolism in hypertensive subjects, younger (n = 28) and older (n = 35) patients with hypertension were randomized to placebo, felodipine-ER 5 mg/d, or amlodipine 5 mg/d Objective To evaluate the pharmacokinetics of amlodipine besylate in the peri-partum period including quantities of placental passage, breast milk excretion and infant exposure. Study design This. Amlodipine is currently available as the besylate salt (Norvasc®, Pfizer Inc.). The pharmacokinetic similarities of amlodipine maleate (AmVaz™, Reddy Pharmaceuticals Inc.) compared with the.
[see Clinical Pharmacology (12.4), Clinical Studies (14.1)]. 3 DOSAGE FORMS AND STRENGTHS . 2.5, 5, and 10 mg Tablets . 4 CONTRAINDICATIONS . NORVASC is contraindicated in patients with known sensitivity to amlodipine. 5 WARNINGS AND PRECAUTIONS . 5.1 Hypotension . Symptomatic hypotension is possible, particularly in patients with severe aortic. Amlodipine also known as amlodipine besylate, is a man-made long-acting dihydropyridine calcium channel blocker. Amlodipine is used alone or in combination with other medications to treat high blood pressure (hypertension) and chest pain (angina pectoris). Amlodipine lowers blood pressure by relaxing the blood vessels so the heart does not have. 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 Pharmacokinetics of CCBs • Absorption - typically oral form, but verapamil & diltiazem - also have IV formulation. nifedipine, verapamil & diltiazem - all possess significant first pass metabolism. • Metabolism & excretion - nifedipine & verapamil - excreted by kidney. verapamil - excreted by liver. 19. Amlodipine or nifedipine
The pharmacokinetics of amlodipine and olmesartan medoxomil from Azor are equivalent to the pharmacokinetics of amlodipine and olmesartan medoxomil when administered separately. The bioavailability of both components is well below 100%, but neither component is affected by food. The effective half-lives of amlodipine (45±11 hours) and. The pharmacokinetics of amlodipine and olmesartan medoxomil from Amlodipine and Olmesartan Medoxomil Tablets are equivalent to the pharmacokinetics of amlodipine and olmesartan medoxomil when administered separately. The bioavailability of both components is well below 100%, but neither component is affected by food Effect of CYP3A5*3 genotype on the pharmacokinetics and pharmacodynamics of amlodipine in healthy Korean subjects Kyoung-Ah Kim PhD , Departments of Clinical Pharmacology and Toxicology and Pharmacology, Anam Hospital, Korea University College of Medicine, Seou