| Identification | More | [Name]
Lacidipine | [CAS]
103890-78-4 | [Synonyms]
CALDINE
(E)-4-[2-[3-(1,1-DIMETHYLETHOXY)-3-OXO-1-PROPENYL]PHENYL]-1,4-DIHYDRO-2,6-DIMETHYL-3,5-PYRIDINEDICARBOXYLIC ACID DIETHYL ESTER
GR-43659X
GX-1048
LACIDIPINE
LACIDIPINE-D9
LACIPIL
LACIREX
MOTENS
3,5-pyridinedicarboxylicacid,1,4-dihydro-2,6-dimethyl-4-(2-(3-(1,1-dimethylet
diethylester,(e)-hoxy)-3-oxo-1-propenyl)phenyl)
Lacidipin
LACIDIPINE, IMPURITY STANDARD BP STANDARD
LACIDIPINE, BP STANDARD
LACIDIPINE ASSAY STANDARD BP(CRM STANDARD)
LACIDIPINE BP STANDARD(CRM STANDARD)
LACIDIPINE IMPURITY STANDARD BP STANDARD(CRM STANDARD)
LACIDIPINE IMPURITY STANDARD BP(CRM STANDARD)
LacidipineC26H33N06
(E)-4-[2-[3-(1,1-Dimethylethoxy)-3-oxo-1-propenyl]phenyl]-1,4-dihydro-2,6-dimethyl-3,5-pyridinedicarboxylic Acid Diethyl Ester, GR-43659X, GX-1048, Caldine, Lacipil, Lacirex, Motens | [EINECS(EC#)]
638-759-0 | [Molecular Formula]
C26H33NO6 | [MDL Number]
MFCD00865936 | [Molecular Weight]
455.54 | [MOL File]
103890-78-4.mol |
| Chemical Properties | Back Directory | [Appearance]
White-to-Off-White Crystalline Solid | [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 | [Usage]
A dihydropyridine calcium channel blocker. Antihypertensive | [Merck ]
14,5331 | [InChIKey]
GKQPCPXONLDCMU-CCEZHUSRSA-N | [CAS DataBase Reference]
103890-78-4(CAS DataBase Reference) |
| Safety Data | Back Directory | [Hazard Codes ]
Xn | [Risk Statements ]
22 | [WGK Germany ]
3 | [RTECS ]
US7970200 | [Toxicity]
mouse,LD50,intraperitoneal,80200ug/kg (80.2mg/kg),SKIN AND APPENDAGES (SKIN): HAIR: OTHERSENSE ORGANS AND SPECIAL SENSES: PTOSIS: EYEBEHAVIORAL: SOMNOLENCE (GENERAL DEPRESSED ACTIVITY),Yakuri to Chiryo. Pharmacology and Therapeutics. Vol. 22, Pg. 335, 1994. |
| Hazard Information | Back Directory | [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. | [Chemical Properties]
White-to-Off-White Crystalline Solid | [Originator]
Glaxo (United Kingdom) | [Uses]
A dihydropyridine calcium channel blocker. Antihypertensive | [Uses]
antihypertensive;dihydropyridinr calcium channel blocker | [Definition]
ChEBI: Lacidipine is a cinnamate ester and a tert-butyl ester. | [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. |
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