Amlodipine

Bezeichnung:Amlodipine

CAS-Nr88150-42-9

Englisch Name:Amlodipine

CBNumberCB9366505

SummenformelC20H25ClN2O5

Molgewicht408.88

MOL-Datei88150-42-9.mol

Amlodipine physikalisch-chemischer Eigenschaften

Schmelzpunkt	178-179°C
Siedepunkt	527.2±50.0 °C(Predicted)
Dichte	1.227±0.06 g/cm3(Predicted)
RTECS-Nr.	US7968329
storage temp.	Keep in dark place,Inert atmosphere,Store in freezer, under -20°C
Löslichkeit	Soluble in DMSO (up to 25 mg/ml), in DMF (up to 25 mg/ml) or in Ethanol (up to 25 mg/ml).
pka	pKa 8.6 (Uncertain)
Aggregatzustand	Almost white crystal powder
Farbe	White
Wasserlöslichkeit	75.3 mg/L
BCS Class	1
Stabilität	Stable for 1 year from date of purchase as supplied. Solutions in DMSO, DMF, or ethanol may be stored at -20°C for up to 3 months.
CAS Datenbank	88150-42-9(CAS DataBase Reference)
EPA chemische Informationen	3,5-Pyridinedicarboxylic acid, 2-[(2-aminoethoxy)methyl]-4-(2-chlorophenyl)-1,4-dihydro-6-methyl-, 3-ethyl 5-methyl ester (88150-42-9)

Sicherheit

HazardClass	IRRITANT
HazardClass	6.1
Giftige Stoffe Daten	88150-42-9(Hazardous Substances Data)
Toxizität	TDLo orl-chd: 400 mg/kg:BPR AJEMEN 18,581,2000

Gefahreninformationscode (GHS)

Amlodipine Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung
Amlodipine is a dihydropyridine L-type calcium channel blocker that selectively inhibits calcium influx in cardiac and vascular smooth muscle. Acting as a vasodilator, amlodipine reduces blood pressure by relaxing the smooth muscle in the arterial wall, decreasing total peripheral resistance. It inhibits calcium-induced contractions in depolarized rat aorta with an IC₅₀ value of 1.9 nM, displaying a slow rate of association and dissociation in isolated vascular and cardiac tissues. Amlodipine also demonstrates actions independent of L-type calcium channel blockade by regulating membrane fluidity and cholesterol deposition, stimulating nitric oxide production, acting as an antioxidant, and regulating matrix deposition in vitro and in vivo. Formulations containing amlodipine have been used in the treatment of hypertension.
Chemische Eigenschaften
Yellow Solid
Verwenden
A dihydropyridine calcium channel blocker; activity resides mainly in the (-)-isomer.
Verwenden
anti-hypertensive;calcium channel blocker
Verwenden
A deuterated dihydropyridine calcium channel blocker.;Application of Labeled APIs: Labeled Amlodipine, intended for use as an internal standard for the quantification of Amlodipine by GC- or LC-mass spectrometry.
Definition
ChEBI: 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.
Trademarks
Norvasc (Pfizer).
Allgemeine Beschreibung
Amlodipine, 2-[, for the treatment of hypertension. Amlodipineis also marketed as a combination therapy with atorvastatinunder the tradename Norvasc for the management of highcholesterol and high blood pressure.
Hazard
Human systemic effects.
Clinical Use
Calcium-channel blocker:
Hypertension
Angina prophylaxis
Sicherheitsprofil
Human systemic effects. Whenheated to decomposition it emits toxic vapors of NOx andCl^-.
Arzneimittelwechselwirkung
Potentially hazardous interactions with other drugs
Aminophylline and theophylline: possibly increased aminophylline and theophylline concentration.
Anaesthetics: enhanced hypotensive effect.
Antibacterials: metabolism possibly inhibited by clarithromycin, erythromycin and telithromycin.
Antidepressants: enhanced hypotensive effect with MAOIs, concentration possibly reduced by St John’s wort.
Antiepileptics: effects probably reduced by phenobarbital and primidone.
Antifungals: negative inotropic effect possibly increased with itraconazole.
Antihypertensives: enhanced hypotensive effect; increased risk of first dose hypotensive effect of postsynaptic alpha-blockers.
Antivirals: concentration increased by telaprevir and possibly by ritonavir - reduce dose of amlodipine.
Ciclosporin: ciclosporin concentration may be increased by up to 40%.
Lipid lowering agents: possibly increased risk of myopathy - do not exceed 20 mg of simvastatin.1 Tacrolimus: possibly increased tacrolimus levels.
Stoffwechsel
Amlodipine is extensively metabolised by the liver to inactive metabolites with 10% of the parent compound and 60% of metabolites excreted in the urine.
Einzelnachweise
1) Mason et al. (2003), Novel vascular biology of third-generation L-type calcium channel antagonists: ancillary actions of amlodipine; Arterioscler. Thromb. Vasc. Biol., 23 2155 2) Asano et al. (2003), A calcium channel blocker activates both ecto-5(‘)-nucleotidase and NO synthase in HUVEC; Biochem. Biophys. Res. Commun., 311 625 3) Yu et al. (2003), Amlodipine modulates THP-1 cell adhesion to vascular endothelium via inhibition of protein kinase C signal transduction; Hypertension, 42 329 4) Zhou et al. (2004), Inhibition of oxidative stress and improvement of endothelial function by amlodipine in angiotensin II-infused rats; Am. J. Hypertension, 17 167 5) Ueda et al. (1993), A comparative assessment of the duration of action of amlodipine and nifedipine GITS in normotensive subjects; Br. J. Clin. Pharmacol., 36 561

Amlodipine Upstream-Materialien And Downstream Produkte

Amlodipine Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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