Amlodin/Norvasc/3-Ethyl 5-methyl 2-[(2-aminoethoxy)methyl]-4-(2-chlorophenyl)-6-methyl-1,4-dihydropyridine-3,5-dicarboxylate benzenesulfonate (1:1)/3-Ethyl 5-methyl 2-[(2-aminoethoxy)methyl]-4-(2-chlorophenyl)-6-methyl-1,4-dihydro-3,5-pyridinedicarboxylate benzenesulfonate (1:1)/3,5-Pyridinedicarboxylic acid, 2-[(2-aminoethoxy)methyl]-4-(2-chlorophenyl)-1,4-dihydro-6-methyl-, 3-ethyl 5-methyl ester, benzenesulfonate (1:1)/Benzolsulfonsaure--3-ethyl-5-methyl-2-[(2-aminoethoxy)methyl]-4-(2-chlorphenyl)-6-methyl-1,4-dihydropyridin-3,5-dicarboxylat(1:1)/acide benzenesulfonique - 2-[(2-aminoethoxy)methyl]-4-(2-chlorophenyl)-6-methyl-1,4-dihydropyridine-3,5-dicarboxylate de 3-ethyle et de 5-methyle (1:1)/3-ethyl 5-methyl 2-[(2-aminoethoxy)methyl]-4-(2-chlorophenyl)-6-methyl-1,4-dihydropyridine-3,5-dicarboxylate benzenesulfonate/3-Ethyl 5-methyl 2-[(2-aminoethoxy)methyl]-4-(2-chlorophenyl)-6-methyl-1,4-dihydro-3,5-pyridinedicarboxylate benzenesulfonate/Amlodipine Besilate/Amlodipine besylate/benzenesulfonic acid,3-O-ethyl 5-O-methyl 2-(2-aminoethoxymethyl)-4-(2-chlorophenyl)-6-methyl-1,4-dihydropyridine-3,5-dicarboxylate/AMLODIPINE BENZENESULFONATE/3-Ethyl 5-Methyl (±)-2-[(2-Aminoethoxy)methyl]-4-(2-chlorophenyl)-6-methyl-1,4-dihydro-3,5-pyridinedicarboxylate Monobenzenesulfonate
benzenesulfonic acid;3-O-ethyl 5-O-methyl 2-(2-aminoethoxymethyl)-4-(2-chlorophenyl)-6-methyl-1,4-dihydropyridine-3,5-dicarboxylate
Amlodipine besylate is a long-acting calcium channel blocker.Target: Calcium ChannelAmlodipine is a dihydropyridine calcium antagonist (calcium ion antagonist or slow-channel blocker) that inhibits the movement of calcium ions into vascular smooth muscle cells and cardiac muscle cells. Experimental data suggest amlodipine binds to both dihydropyridine and nondihydropyridine binding sites. The contractile processes of cardiac muscle and vascular smooth muscle are dependent upon the movement of extracellular calcium ions into these cells through specific ion channels. Amlodipine inhibits calcium ion influx across cell membranes selectively, with a greater effect on vascular smooth muscle cells than on cardiac muscle cells. Negative inotropic effects, or decreased heart muscle contractility, can be detected in vitro, but such effects have not been seen in intact animals at therapeutic doses. Serum calcium concentration is not affected by amlodipine. Within the physiologic pH range, amlodipine is an ionized compound (pKa = 8.6), and its interaction with the calcium channel receptor is characterized by a gradual rate of association and dissociation with the receptor binding site, resulting in a gradual onset of effect. Amlodipine is a peripheral arterial vasodilator that acts directly on vascular smooth muscle to cause a reduction in peripheral vascular resistance and reduction in blood pressure. From Wikipedia.
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Amlodipine is rarely used in the treatment of pregnant hypertensive women due to limited pharmacokinetic data during pregnancy and the postpartum period.
To evaluate the pharmacokinetics of amlodipine besylate in the peri-partum period including quantities of placental passage, breast milk excretion and infant exposure.
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. Cord and maternal blood samples were collected at delivery. On postpartum day 2, six paired maternal plasma and breast milk samples were obtained at 4, 6, 8, 12, 15 and 24 h following amlodipine dosing. Infant plasma samples were collected 24-48 h after delivery. All samples were analyzed for amlodipine concentration. A one compartment, first-order model was used to calculate pharmacokinetic estimates for maternal plasma.
Of the 16 patients enrolled in the study, 11 had cord blood and maternal serum collected at delivery, of which only 6 produced sufficient breast milk for sampling. Amlodipine was detected in infant cord blood plasma with a mean concentration of 0.49 ± 0.29 ng/mL compared to mean maternal serum level of 1.27 ± 0.84 ng/mL. Amlodipine concentrations in both in breast milk and infant plasma were undetectable at the lower limit of assay detection (<0.1 ng/mL). In the immediate postpartum period, the amlodipine elimination half-life was 13.7 ± 4.9 h, the area under the curve was 53.4 ± 19.8 ng*h/mL and the peak concentration was 2.0 ± 1.0 ng/mL. CONCLUSIONS: Amlodipine does cross the placenta in measurable quantities, but is not detected in breast milk or infant plasma at 24-48 h of life indicating that it is likely safe to use during the peripartum period. Copyright © 2018 International Society for the Study of Hypertension in Pregnancy. Published by Elsevier B.V. All rights reserved.
Amlodipine; Breast milk; Chronic hypertension; Pharmacokinetics
Pharmacokinetics of amlodipine besylate at delivery and during lactation.
Morgan JL1, Kogutt BK2, Meek C3, Stehel EK4, McIntire DD2, Sheffield JS5, Roberts SW2.
Controlling blood pressure is a global health priority; single-pill antihypertensive combinations may improve adherence, persistence, and outcomes. Areas covered: A novel combination of perindopril arginine and amlodipine besylate was recently approved. A systematic review of the literature revealed its most common adverse effects as: peripheral edema (depending on the dose of amlodipine, but attenuated by perindopril), cough, dizziness and hypotension. Dose-dependent hyperkalemia, impairment of renal function (especially in renovascular hypertension), angioedema, and teratogenicity were derived from experience with other ACE-inhibitors. Expert opinion: Substantial clinical trial experience with amlodipine or perindopril suggests that these two agents effectively lower blood pressure, and can reduce the risk of major adverse cardiovascular events, as in the Anglo-Scandinavian Cardiac Outcomes Trial. The incidence of adverse effects reported in clinical trials is lower than expected, likely due to exclusion of subjects previously exposed to its components; the nature of open-label, uncontrolled observational studies; and difficulty in recognizing and measuring cough and pedal edema. This new formulation of perindopril arginine protects its ethyl ester, without requiring physical separation from amlodipine in a single tablet, and is less hygroscopic than perindopril erbumine. These and other attributes may make this combination an attractive addition to the antihypertensive armamentarium.
Angiotensin converting-enzyme inhibitor; calcium antagonist; clinical trials
Perindopril arginine and amlodipine besylate for hypertension: a safety evaluation.
Elliott WJ1, Bistrika EA1,2.
Fast Orally Dissolving Film preparation can be used for patients with problems in ingesting solid dosage forms, such as mentally ill, elderly, geriatric and patients who are reducing fluid intake or nausea.
This study aimed to formulate and evaluate the rapid dissolution of amlodipine besylate.
Amlodipine besylate film was prepared by solvent casting method by using hydroxypropyl methylcellulose (HPMC) as film formers, crospovidone as superdisintegrant with Varian concentration F1 (2%), F2 (4%), F3 (6%) and F4 (8%), PEG 400 as plasticizer, sucralose and sorbitol as sweetener, citric acid as saliva stimulation, and grape essence as flavoring and coloring agent. Characteristics of films include organoleptic, weight uniformity, film thickness, surface pH, swelling, uniformity of content, time of disintegration, and dissolution.
All formulated films produced a good film, smooth, transparent and uniform physical properties. F2 with polymer HPMC and the 4% concentration of crospovidone was the best formula with 31.50 seconds of disintegration time, the index expanding at the 15 second by 242.29% and the cumulative percent of the drug at 80 seconds by 98.08%.
Amlodipine besylate can be formulated into fast orally dissolving film preparations using HPMC and crospovidone polymers so that they may be considered for use in the treatment of hypertension for patients with drug-induced problems in tablet or capsule form.
Copyright: © 2019 Sumaiyah Sumaiyah, Julia Mentari, Suryanto Suryanto.
Amlodipine besylate; Crospovidone; Fast orally dissolving film; Solvent casting
The Effect of Crospovidone on the Dissolution Profile of Amlodipine Besylate from Fast Orally Dissolving Film.
Sumaiyah S1, Mentari J1, Suryanto S1.
2019 Nov 14