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| Lacidipine Basic information |
| Product Name: | Lacidipine | | Synonyms: | 3,5-pyridinedicarboxylicacid,1,4-dihydro-2,6-dimethyl-4-(2-(3-(1,1-dimethylet;diethylester,(e)-hoxy)-3-oxo-1-propenyl)phenyl);MOTENS;3,5-Diethyl 4-{2-[(1E)-3-(tert-butoxy)-3-oxoprop-1-en-1-yl]phenyl}-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate;CID 5311217;Lacidipine，Lacipil;Lacidipine Solution, 100ppm;4-[2-[(1E)-3-(1,1-dimethylethoxy)-3-oxo-1-propen-1-yl]phenyl]-1,4-dihydro-2,6-dimethyl-3,5-pyridinedicarboxylic acid 3,5-diethyl ester | | CAS: | 103890-78-4 | | MF: | C26H33NO6 | | MW: | 455.54 | | EINECS: | 638-759-0 | | Product Categories: | Calcium channel;Dihydropyridine;Active Pharmaceutical Ingredients;Dihydropyridine Class Chemicals;Intermediates & Fine Chemicals;Pharmaceuticals;API;Lacipil, Motens | | Mol File: | 103890-78-4.mol |
| Lacidipine Chemical Properties |
| Melting point | 174-175°C | | Boiling point | 558.4±50.0 °C(Predicted) | | density | 1.127±0.06 g/cm3(Predicted) | | storage temp. | 2-8°C | | solubility | DMSO: soluble20mg/mL, clear | | form | powder | | pka | 3.00±0.70(Predicted) | | color | white to beige | | Merck | 14,5331 | | InChIKey | GKQPCPXONLDCMU-CCEZHUSRSA-N | | CAS DataBase Reference | 103890-78-4(CAS DataBase Reference) |
| Hazard Codes | Xn | | Risk Statements | 22 | | WGK Germany | 3 | | RTECS | US7970200 |
| Lacidipine Usage And Synthesis |
| Description | Lacidipine is a new second-generation dihydropyridine calcium antagonist introduced
as a once a day treatment for mild to moderate hypertension. It is reported to have high
selectivity for vascular smooth muscle and also a long duration of action. The use of
lacidipine as an antiatherosclerotic agent is currently under investigation. | | Description | Lacidipine is a dihydropyridine L-type calcium channel blocker. It induces relaxation of isolated rat aorta and inhibits calcium-induced contraction of rabbit ear artery (pA2 = 9.4). It also induces relaxation of calcium-induced contractions in isolated rat colon and bladder and guinea pig trachea (IC50s = 6.7, 6, and 7.8 nM, respectively). Lacidipine induces negative inotropy in isolated guinea pig ventricular strips (IC50 = 110 nM). It reduces mean blood pressure in spontaneously hypertensive rats (ED25 = 0.35 mg/kg) and in renal hypertensive dogs (ED25 = 0.22 mg/kg) with a transient increase in heart rate. Lacidipine inhibits copper-induced oxidation of isolated human LDL when used at concentrations of 1 and 5 μM. It reduces the extension of aortic atheromatous lesions and decreases renal injury in ApoE-/- mice in a model of Western diet-induced atherosclerosis. | | Chemical Properties | White-to-Off-White Crystalline Solid | | Originator | Glaxo (United Kingdom) | | Uses | A dihydropyridine calcium channel blocker. Antihypertensive. | | Uses | A dihydropyridine calcium channel blocker. Antihypertensive | | Uses | antihypertensive;dihydropyridinr calcium channel blocker | | Brand name | Lacipil; Lacirex; Viapres | | Biochem/physiol Actions | Lacidipine is a long-acting calcium antagonist that is used in the management of hypertension. Lacidipine is a L-type Ca(2+) channel blocker belonging to 1,4-dihydropyridine class. Also, Lacidipine inhibits ryanodine receptors on the ER membrane that enhances folding, trafficking and lysosomal activity of ERAD (ER-associated degradation) misfolded lysosomal glucocerebrosidase (GS). | | Clinical Use | #N/A | | Drug interactions | 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.
Antiepileptics: effect possibly reduced by
carbamazepine, barbiturates, phenytoin and
primidone.
Antifungals: metabolism possibly inhibited by
itraconazole and ketoconazole; negative inotropic
effect possibly increased with itraconazole.
Antihypertensives: enhanced hypotensive effect,
increased risk of first dose hypotensive effect of postsynaptic alpha-blockers.
Antivirals: concentration possibly increased by
ritonavir.
Ciclosporin: 10 kidney transplant patients on
ciclosporin, prednisone and azathioprine were given
4 mg lacidipine daily. A very small increase in the
trough serum levels (+6%) and AUC (+14%) of the
ciclosporin occurred.
Grapefruit juice: concentration increased - avoid
concomitant use | | Metabolism | Lacidipine undergoes extensive first-pass metabolism
in the liver. The drug is eliminated primarily by hepatic
metabolism (involving cytochrome P450 CYP3A4).
The principal metabolites possess little, if any,
pharmacodynamic activity.
Approximately 70% of the administered dose is
eliminated as metabolites in the faeces and the remainder
as metabolites in the urine. |
| Lacidipine Preparation Products And Raw materials |
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