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Lacidipine

Synopsis

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Chemistry

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Also known as: 103890-78-4, Lacipil, Motens, Gr-43659x, Trans lacidipine, Gr 43659x

Molecular Formula

C₂₆H₃₃NO₆

Molecular Weight

455.5 g/mol

InChI Key

GKQPCPXONLDCMU-CCEZHUSRSA-N

FDA UNII

260080034N

Lacidipine is a lipophilic dihydropyridine calcium antagonist with an intrinsically slow onset of activity. Due to its long duration of action, lacidipine does not lead to reflex tachycardia. It displays specificity in the vascular smooth muscle, where it acts as an antihypertensive agent to dilate peripheral arterioles and reduce blood pressure. Compared to other dihydropyridine calcium antagonists, lacidipine exhibits a greater antioxidant activity which may confer potentially beneficial antiatherosclerotic effects. Lacidipine is a highly lipophilic molecule that interacts with the biological membranes. Through radiotracer analysis, it was determined that lacidipine displays a high membrane partition coefficient leading to accumulation of the drug in the membrane and slow rate of membrane washout. When visualized by small-angle X-ray diffraction with angstrom resolution to examine its location within the membranes, lacidipine was found deep within the membrane's hydrocarbon core. These results may explain the long clinical half-life of lacidipine. In randomised, well-controlled trials, administration of daily single-dose lacidipine ranging from 2-6 mg demonstrated comparable antihypertensive efficacy similar to that of other long-acting dihydropyridine calcium antagonists, thiazide diuretics, atenolol (a beta-blocker) and enalapril (an ACE inhibitor). It is available as once-daily oral tablets containing 2 or 4 mg of the active compound commonly marketed as Lacipil or Motens. It is not currently FDA-approved.

1 2D Structure

Lacidipine

2 Identification

2.1 Computed Descriptors

2.1.1 IUPAC Name

diethyl 2,6-dimethyl-4-[2-[(E)-3-[(2-methylpropan-2-yl)oxy]-3-oxoprop-1-enyl]phenyl]-1,4-dihydropyridine-3,5-dicarboxylate

2.1.2 InChI

InChI=1S/C26H33NO6/c1-8-31-24(29)21-16(3)27-17(4)22(25(30)32-9-2)23(21)19-13-11-10-12-18(19)14-15-20(28)33-26(5,6)7/h10-15,23,27H,8-9H2,1-7H3/b15-14+

2.1.3 InChI Key

GKQPCPXONLDCMU-CCEZHUSRSA-N

2.1.4 Canonical SMILES

CCOC(=O)C1=C(NC(=C(C1C2=CC=CC=C2C=CC(=O)OC(C)(C)C)C(=O)OCC)C)C

2.1.5 Isomeric SMILES

CCOC(=O)C1=C(NC(=C(C1C2=CC=CC=C2/C=C/C(=O)OC(C)(C)C)C(=O)OCC)C)C

2.2 Other Identifiers

2.2.1 UNII

260080034N

2.3 Synonyms

2.3.1 MeSH Synonyms

1. Caldine

2. Gr 43659x

3. Gr-43659x

4. Lacimen

5. Lacipil

6. Motens

2.3.2 Depositor-Supplied Synonyms

1. 103890-78-4

2. Lacipil

3. Motens

4. Gr-43659x

5. Trans Lacidipine

6. Gr 43659x

7. Lacidipine (lacipil, Motens)

8. Diethyl 2,6-dimethyl-4-[2-[(e)-3-[(2-methylpropan-2-yl)oxy]-3-oxoprop-1-enyl]phenyl]-1,4-dihydropyridine-3,5-dicarboxylate

9. Gx-1048

10. Sn-305

11. 4-(o-((e)-2-carboxyvinyl)phenyl)-1,4-dihydro-2,6-dimethyl-3,5-pyridinedicarboxylic Acid, 4-tert-butyl Diethyl Ester

12. Lacimen

13. Dsstox_cid_26429

14. Dsstox_rid_81607

15. Dsstox_gsid_46429

16. 3,5-pyridinedicarboxylic Acid, 4-(2-(3-(1,1-dimethylethoxy)-3-oxo-1-propenyl)phenyl)-1,4-dihydro-2,6-dimethyl-, Diethyl Ester, (e)-

17. Diethyl (e)-4-(2-(3-(tert-butoxy)-3-oxoprop-1-en-1-yl)phenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate

18. 260080034n

19. Lacidipinum [latin]

20. Lacidipino [spanish]

21. Lacidipino

22. Lacidipinum

23. Lacirex

24. (e)-diethyl 4-(2-(3-(tert-butoxy)-3-oxoprop-1-en-1-yl)phenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate

25. Smr000466342

26. Cas-103890-78-4

27. Sr-05000001445

28. Gr 43659 X

29. Viapres

30. Molap

31. Lacidipine [usan:inn:ban]

32. Lacidipine,(s)

33. Ncgc00164545-01

34. (e)-diethyl 4-(2-(3-tert-butoxy-3-oxoprop-1-enyl)phenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate

35. Lacidipine- Bio-x

36. Motens (tn)

37. Unii-260080034n

38. Lacidipine [mi]

39. Lacidipine [inn]

40. Lacidipine [jan]

41. Lacidipine (usan/inn)

42. Lacidipine [usan]

43. Lacidipine [vandf]

44. Lacidipine [mart.]

45. Lacidipine [who-dd]

46. Lacipil, Motens, Lacidipine

47. Schembl49277

48. Schembl49278

49. Mls000759454

50. Mls001424282

51. Chembl460291

52. Chembl1728809

53. Dtxsid1046429

54. Schembl13287288

55. Chebi:94480

56. Gtpl11740

57. Chebi:135737

58. Hms2052f03

59. Hms2089k22

60. Hms3713d20

61. Hms3884i18

62. (non-isotopelabelled)lacidipine-d9

63. Bcp02933

64. Gr43659x

65. Hy-b0347

66. Tox21_112174

67. Gx1048

68. S1994

69. Stl454986

70. Akos005066844

71. Tox21_112174_1

72. Zinc100015470

73. Bcp9000831

74. Ccg-101153

75. Ccg-220579

76. Db09236

77. Gx 1048

78. Hs-0086

79. Nc00403

80. Ncgc00263529-01

81. 3,5-pyridinedicarboxylic Acid, 1,4-dihydro-2,6-dimethyl-4-(2-(3-(1,1-dimethylethoxy)-3-oxo-1-propenyl)phenyl)-, Diethyl Ester, (e)-

82. Ac-11008

83. Ac-33195

84. Bl164603

85. Cpd000466342

86. Bcp0726000285

87. L0276

88. Sw219840-1

89. C71162

90. D04657

91. Ab00698350-05

92. Ab01275445-01

93. Ab01275445_02

94. Gx-1048,gr-43659x,sn-305

95. 890l784

96. A800840

97. J-001058

98. Q1163827

99. Sr-05000001445-1

100. Sr-05000001445-2

101. Brd-k05851096-001-01-9

102. 2,6-dimethyl-4-[2-[(e)-3-[(2-methylpropan-2-yl)oxy]-3-oxoprop-1-enyl]phenyl]-1,4-dihydropyridine-3,5-dicarboxylic Acid Diethyl Ester

103. Diethyl 2,6-dimethyl-4-[2-[(e)-3-[(2-methylpropan-2-yl)oxy]-3-oxidanylidene-prop-1-enyl]phenyl]-1,4-dihydropyridine-3,5-dicarboxylate

104. Diethyl 4-{2-[(1e)-3-tert-butoxy-3-oxoprop-1-en-1-yl]phenyl}-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate

2.4 Create Date

2005-09-13

3 Chemical and Physical Properties

Molecular Formula	C₂₆H₃₃NO₆
Molecular Weight	455.5 g/mol
XLogP3	4.5
Hydrogen Bond Donor Count	1
Hydrogen Bond Acceptor Count	7
Rotatable Bond Count	11
Exact Mass	455.23078777 g/mol
Monoisotopic Mass	455.23078777 g/mol
Topological Polar Surface Area	90.9 Å²
Heavy Atom Count	33
Formal Charge	0
Complexity	805
Isotope Atom Count	0
Defined Atom Stereocenter Count	0
Undefined Atom Stereocenter Count	0
Defined Bond Stereocenter Count	1
Undefined Bond Stereocenter Count	0
Covalently Bonded Unit Count	1

4 Drug and Medication Information

4.1 Drug Indication

Indicated for the treatment of hypertension either alone or in combination with other antihypertensive agents, including -adrenoceptor antagonists, diuretics, and ACE-inhibitors.

5 Pharmacology and Biochemistry

5.1 Pharmacology

acidipine is a specific and potent calcium antagonist with a predominant selectivity for calcium channels in the vascular smooth muscle. Its main action is to dilate predominantly peripheral and coronary arteries, reducing peripheral vascular resistance and lowering blood pressure. Following the oral administration of 4 mg lacidipine to volunteer subjects, a minimal prolongation of QTc interval has been observed (mean QTcF increase between 3.44 and 9.60 ms in young and elderly volunteers).

5.2 MeSH Pharmacological Classification

Antihypertensive Agents

Drugs used in the treatment of acute or chronic vascular HYPERTENSION regardless of pharmacological mechanism. Among the antihypertensive agents are DIURETICS; (especially DIURETICS, THIAZIDE); ADRENERGIC BETA-ANTAGONISTS; ADRENERGIC ALPHA-ANTAGONISTS; ANGIOTENSIN-CONVERTING ENZYME INHIBITORS; CALCIUM CHANNEL BLOCKERS; GANGLIONIC BLOCKERS; and VASODILATOR AGENTS. (See all compounds classified as Antihypertensive Agents.)

Calcium Channel Blockers

A class of drugs that act by selective inhibition of calcium influx through cellular membranes. (See all compounds classified as Calcium Channel Blockers.)

5.3 ATC Code

C - Cardiovascular system

C08 - Calcium channel blockers

C08C - Selective calcium channel blockers with mainly vascular effects

C08CA - Dihydropyridine derivatives

C08CA09 - Lacidipine

5.4 Absorption, Distribution and Excretion

Absorption

Since it is a highly lipophilic compound, lacidpine is rapidly absorbed from the gastrointestinal tract following oral administration with the peak plasma concentrations reached between 30 and 150 minutes of dosing. The peak plasma concentrations display large interindividual variability, with the values ranging from 1.6 to 5.7 g/L following single-dose oral administration of lacidipine 4mg in healthy young volunteers. Absolute bioavailability is less than 10% due to extensive first-pass metabolism in the liver.

Route of Elimination

Approximately 70% of the administered dose is eliminated as metabolites in the faeces and the remainder as metabolites in the urine.

5.5 Metabolism/Metabolites

Lacidipine undergoes complete CYP3A4-mediated hepatic metabolism, with no parent drug detected in the urine or faeces. The 2 main metabolites have no pharmacological activity.

5.6 Biological Half-Life

The average terminal half-life of lacidipine ranges from between 13 and 19 hours at steady state.

5.7 Mechanism of Action

By blocking the voltage-dependent L-type calcium channels, it prevents the transmembrane calcium influx. Normally, calcium ions serve as intracellular messengers or activators in exictable cells including vascular smooth muscles. The influx of calcium ultimately causes the excitation and depolarization of the tissues. Lacidipine inhibits the contractile function in the vascular smooth muscle and reduce blood pressure. Due to its high membrane partition coefficient, some studies suggest that lacidipine may reach the receptor via a two-step process; it first binds and accumulates in the membrane lipid bilayer and then diffuses within the membrane to the calcium channel receptor. It is proposed that lacidipine preferentially blocks the inactivated state of the calcium channel. Through its antioxidant properties shared amongst other dihydropyridine calcium channel blockers, lacidipine demonstrates an additional clinical benefit. Its antiatherosclerotic effects are mediated by suppressing the formation of reactive oxygen species (ROS) and subsequent inflammatory actions by chemokines, cytokines and adhesion molecules, thus reducing atherosclerotic lesion formation. Lacidipine may also suppress cell proliferation and migration in smooth muscle cells and suppress the expression of matrix metalloproteinases, which affects the stability of atheromatous plaques.

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