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Isradipine

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1 CEP/COS
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35 FDF Dossiers, 10 FDA Orange Book, 23 Europe, 2 South Africa

35 FDF Dossiers
10 FDA Orange Book
23 Europe
2 South Africa

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Synopsis

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Chemistry

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Also known as: 75695-93-1, Dynacirc, Isradipin, Lomir, Isrodipine, Prescal

Molecular Formula

C₁₉H₂₁N₃O₅

Molecular Weight

371.4 g/mol

InChI Key

HMJIYCCIJYRONP-UHFFFAOYSA-N

FDA UNII

YO1UK1S598

A potent antagonist of CALCIUM CHANNELS that is highly selective for VASCULAR SMOOTH MUSCLE. It is effective in the treatment of chronic stable angina pectoris, hypertension, and congestive cardiac failure.

Isradipine is a Dihydropyridine Calcium Channel Blocker. The mechanism of action of isradipine is as a Calcium Channel Antagonist.

1 2D Structure

Isradipine

2 Identification

2.1 Computed Descriptors

2.1.1 IUPAC Name

3-O-methyl 5-O-propan-2-yl 4-(2,1,3-benzoxadiazol-4-yl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate

2.1.2 InChI

InChI=1S/C19H21N3O5/c1-9(2)26-19(24)15-11(4)20-10(3)14(18(23)25-5)16(15)12-7-6-8-13-17(12)22-27-21-13/h6-9,16,20H,1-5H3

2.1.3 InChI Key

HMJIYCCIJYRONP-UHFFFAOYSA-N

2.1.4 Canonical SMILES

CC1=C(C(C(=C(N1)C)C(=O)OC(C)C)C2=CC=CC3=NON=C32)C(=O)OC

2.2 Other Identifiers

2.2.1 UNII

YO1UK1S598

2.3 Synonyms

2.3.1 MeSH Synonyms

1. Dynacirc

2. Isradipine, (+-)-isomer

3. Isradipine, (r)-isomer

4. Isradipine, (s)-isomer

5. Lomir

6. Pn 200-110

7. Pn 205 033

8. Pn 205 034

9. Pn 205-033

10. Pn 205-034

11. Pn 205033

12. Pn 205034

13. Pn-200-110

14. Pn-205-033

15. Pn-205-034

16. Pn205033

17. Pn205034

2.3.2 Depositor-Supplied Synonyms

1. 75695-93-1

2. Dynacirc

3. Isradipin

4. Lomir

5. Isrodipine

6. Prescal

7. Esradin

8. Dynacirc Cr

9. Clivoten

10. Pn 200-110

11. Dynacrine

12. Isradipinum [latin]

13. Isradipino [spanish]

14. Pn-200-110

15. Rebriden

16. Dynacire

17. Dynacire Cr

18. (+/-)-isradipine

19. Isradipine (dynacirc)

20. Pn 200

21. C19h21n3o5

22. (+-)-isradipine

23. 3-isopropyl 5-methyl 4-(benzo[c][1,2,5]oxadiazol-4-yl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate

24. 3-o-methyl 5-o-propan-2-yl 4-(2,1,3-benzoxadiazol-4-yl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate

25. 3,5-pyridinedicarboxylic Acid, 4-(4-benzofurazanyl)-1,4-dihydro-2,6-dimethyl-, Methyl 1-methylethyl Ester

26. Nsc-759892

27. Yo1uk1s598

28. 131970-21-3

29. 3,5-pyridinedicarboxylic Acid, 4-(2,1,3-benzoxadiazol-4-yl)-1,4-dihydro-2,6-dimethyl-, Methyl 1-methylethyl Ester

30. Isradipine D3

31. Isradipinum

32. Isradipino

33. Dsstox_cid_3179

34. Dsstox_rid_76907

35. Dsstox_gsid_23179

36. Icaz

37. 4-(2,1,3-benzoxadiazol-4-yl)-1,4-dihydro-2,6-dimethyl-3,5-pyridinecarboxylic Acid Methyl 1-methylethyl Ester

38. Smr000466320

39. Smr002529690

40. Dynacirc (tn)

41. Isradipine (usp/inn)

42. Sr-01000597526

43. Mfcd00153820

44. Unii-yo1uk1s598

45. Isradipine [usan:usp:inn:ban]

46. Ncgc00016931-01

47. (-)-isradipine

48. (plusmn)-isradipine

49. Cas-75695-93-1

50. Pn200-110

51. Isopropyl Methyl (+-)-4-(4-benzofurazanyl)-1,4-dihydro-2,6-dimethyl-3,5-pyridinedicarboxylate

52. Spectrum_000218

53. Isradipine [mi]

54. Pn-200110

55. Isradipine [inn]

56. Prestwick0_001021

57. Prestwick1_001021

58. Prestwick2_001021

59. Prestwick3_001021

60. (.+/-.)-isradipine

61. Isradipine [usan]

62. Isradipine [vandf]

63. Isradipine [mart.]

64. Chembl1648

65. Isradipine [usp-rs]

66. Isradipine [who-dd]

67. Schembl34555

68. Bspbio_001201

69. Kbioss_000698

70. 4-(4-benzofurazanyl)-1,4-dihydro-2,6-dimethyl-3,5-pyridinedicarboxylic Acid Methyl 1-methylethyl Ester

71. Mls000759425

72. Mls001424076

73. Mls002154106

74. Mls003915633

75. Mls006010138

76. O5-methyl O3-propan-2-yl 4-(2,1,3-benzoxadiazol-7-yl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate

77. Spbio_003062

78. Bpbio1_001323

79. Chebi:6073

80. Chembl315436

81. Gtpl4488

82. Chembl3211306

83. Dtxsid4023179

84. Isradipine [orange Book]

85. Kbio2_000698

86. Kbio2_003266

87. Kbio2_005834

88. Isradipine [ep Monograph]

89. Hms1571m03

90. Hms2051j12

91. Hms2098m03

92. Hms2235o12

93. Hms3268d21

94. Hms3393j12

95. Hms3413a15

96. Hms3655c17

97. Hms3677a15

98. Hms3715m03

99. Hms3884e06

100. Isradipine [usp Monograph]

101. Pharmakon1600-02300234

102. (non-isotopelabelled)isradipine-d7

103. Act02697

104. Bcp06719

105. Hy-b0233

106. Benzo[1,2,5]oxadiazol-4-aldehyde

107. Tox21_110690

108. Bdbm50436176

109. Nsc759892

110. S1662

111. Akos015895129

112. Isradipine, >=98% (hplc), Solid

113. Tox21_110690_1

114. Ac-8539

115. Ccg-101027

116. Ccg-213711

117. Db00270

118. Hs-0085

119. Nc00277

120. Nsc 759892

121. Isopropyl Methyl 4-(4-benzofurazanyl)-1,4-dihydro-2,6-dimethyl-3,5-pyridinedicarboxylate

122. Ncgc00025341-01

123. Ncgc00025341-02

124. Ncgc00025341-03

125. Ncgc00025341-06

126. 3,5-pyridinedicarboxylic Acid, 4-(2,1,3-benzoxadiazol-4-yl)-1,4-dihydro-2,6-dimethyl-, Methyl 1-methylethyl Ester (9ci)

127. 3,5-pyridinedicarboxylic Acid, 4-(4-benzofurazanyl)-1,4-dihydro-2,6-dimethyl-, Methyl 1-methylethyl Ester, (+-)-

128. 4-(2,1,3-benzooxadiazol-4-yl)-2.6-dimethyl-1,4-dihydro-3-isopropyloxycarbonylpyridine-5-carboxylic Acid Methyl Ester

129. 4-(4-benzofurazanyl)-1,-4-dihydro-2,6-dimethyl-3,5-pyridinedicarboxylic Acid Methyl 1-methhylethyl Ester

130. 4-(4-benzofurazanyl)-1,4-dihydro-2,-6-dimethyl-3,5-pyridinedicarboxylic Acid Methyl 1-methylethyl Ester

131. Isopropyl 4-(2,1,3-benzoxadiazol-4-yl)-1,4-dihydro-5-methoxycarbonyl-2,6-dimethyl-3-pyridinecarboxylate

132. Methyl 1-methylethyl 4-(2,1,3-benzoxadiazol-4-yl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate

133. Db-055981

134. Ab00514007

135. Ft-0627542

136. I0876

137. Sw220017-1

138. D00349

139. Ab00514007_02

140. Ab00514007_03

141. 695i931

142. Q414873

143. J-513454

144. Sr-01000597526-1

145. Sr-01000597526-2

146. Sr-01000597526-8

147. Brd-a90799790-001-03-3

148. Brd-a90799790-001-10-8

149. Isradipine, European Pharmacopoeia (ep) Reference Standard

150. Isradipine, United States Pharmacopeia (usp) Reference Standard

151. Isopropyl Methyl 4-(2,1,3-benzoxadiazol-4-yl)-1,4-dihydro-2,6-dimet

152. 3,5-pyridinedicarboxylic Acid, 4-(4-benzofurazanyl)-1,4-dihydro-2,6-dimethyl-, Methyl 1-methylethyl Ester, (+/-)-

153. 3,5-pyridinedicarboxylic Acid, 4-(4-benzofurazanyl)-1,4-dihydro-2,6-dimethyl-, Methyl 1-methylethyl Ester, (.+/-.)-

154. 3-isopropyl 5-methyl 4-(2,1,3-benzoxadiazol-4-yl)-2,6-dimethyl-1,4-dihydro-3,5-pyridinedicarboxylate #

155. 3-methyl 5-propan-2-yl 4-(2,1,3-benzoxadiazol-4-yl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate

156. 4-(4-benzofurazanyl)-1,4-dihydro-2,6-dimethyl-3,5-pyridinedicarboxylic Acid Isopropyl Methyl Ester

157. Isopropyl Methyl (+/-)-4-(4-benzofurazanyl)-1,4-dihydro-2,6-dimethyl-3,5-pyridinedicarboxylate

158. Isopropyl Methyl (.+/-.)-4-(4-benzfurazanyl)-1,4-dihydro-2,6-dimethyl-3,5-pyridinedicarboxylate

159. Isopropyl Methyl (.+/-.)-4-(4-benzofurazanyl)-1,4-dihydro-2,6-dimethyl-3,5-pyridinedicarboxylate

2.4 Create Date

2005-03-25

3 Chemical and Physical Properties

Molecular Formula	C₁₉H₂₁N₃O₅
Molecular Weight	371.4 g/mol
XLogP3	4.3
Hydrogen Bond Donor Count	1
Hydrogen Bond Acceptor Count	8
Rotatable Bond Count	6
Exact Mass	371.14812078 g/mol
Monoisotopic Mass	371.14812078 g/mol
Topological Polar Surface Area	104 Å²
Heavy Atom Count	27
Formal Charge	0
Complexity	685
Isotope Atom Count	0
Defined Atom Stereocenter Count	0
Undefined Atom Stereocenter Count	1
Defined Bond Stereocenter Count	0
Undefined Bond Stereocenter Count	0
Covalently Bonded Unit Count	1

4 Drug and Medication Information

4.1 Drug Information

1 of 2
Drug Name	Isradipine
PubMed Health	Isradipine (By mouth)
Drug Classes	Antianginal, Antihypertensive, Cardiovascular Agent
Drug Label	Isradipine is a calcium antagonist available for oral administration in capsules containing 2.5 mg or 5 mg. The structural formula of isradipine is:Chemically, isradipine is 3,5-Pyridinedicarboxylic acid, 4-(4-benzofurazanyl)-1,4-dihydro-2,6-dimethyl...
Active Ingredient	Isradipine
Dosage Form	Capsule
Route	Oral
Strength	2.5mg; 5mg
Market Status	Prescription
Company	Watson Labs; Mikah Pharma

2 of 2
Drug Name	Isradipine
PubMed Health	Isradipine (By mouth)
Drug Classes	Antianginal, Antihypertensive, Cardiovascular Agent
Drug Label	Isradipine is a calcium antagonist available for oral administration in capsules containing 2.5 mg or 5 mg. The structural formula of isradipine is:Chemically, isradipine is 3,5-Pyridinedicarboxylic acid, 4-(4-benzofurazanyl)-1,4-dihydro-2,6-dimethyl...
Active Ingredient	Isradipine
Dosage Form	Capsule
Route	Oral
Strength	2.5mg; 5mg
Market Status	Prescription
Company	Watson Labs; Mikah Pharma

4.2 Drug Indication

For the management of mild to moderate essential hypertension. It may be used alone or concurrently with thiazide-type diuretics.

5 Pharmacology and Biochemistry

5.1 Pharmacology

Isradipine decreases arterial smooth muscle contractility and subsequent vasoconstriction by inhibiting the influx of calcium ions through L-type calcium channels. Calcium ions entering the cell through these channels bind to calmodulin. Calcium-bound calmodulin then binds to and activates myosin light chain kinase (MLCK). Activated MLCK catalyzes the phosphorylation of the regulatory light chain subunit of myosin, a key step in muscle contraction. Signal amplification is achieved by calcium-induced calcium release from the sarcoplasmic reticulum through ryanodine receptors. Inhibition of the initial influx of calcium decreases the contractile activity of arterial smooth muscle cells and results in vasodilation. The vasodilatory effects of isradipine result in an overall decrease in blood pressure.

5.2 MeSH Pharmacological Classification

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.)

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.)

Vasodilator Agents

Drugs used to cause dilation of the blood vessels. (See all compounds classified as Vasodilator Agents.)

5.3 FDA Pharmacological Classification

5.3.1 Active Moiety

ISRADIPINE

5.3.2 FDA UNII

YO1UK1S598

5.3.3 Pharmacological Classes

Dihydropyridine Calcium Channel Blocker [EPC]; Dihydropyridines [CS]; Calcium Channel Antagonists [MoA]

5.4 ATC Code

C - Cardiovascular system

C08 - Calcium channel blockers

C08C - Selective calcium channel blockers with mainly vascular effects

C08CA - Dihydropyridine derivatives

C08CA03 - Isradipine

5.5 Absorption, Distribution and Excretion

Absorption

Isradipine is 90%-95% absorbed and is subject to extensive first-pass metabolism, resulting in a bioavailability of about 15%-24%.

Route of Elimination

Approximately 60% to 65% of an administered dose is excreted in the urine and 25% to 30% in the feces.

5.6 Metabolism/Metabolites

Hepatic. Completely metabolized prior to excretion and no unchanged drug is detected in the urine.

5.7 Biological Half-Life

8 hours

5.8 Mechanism of Action

Isradipine belongs to the dihydropyridine (DHP) class of calcium channel blockers (CCBs), the most widely used class of CCBs. There are at least five different types of calcium channels in Homo sapiens: L-, N-, P/Q-, R- and T-type. CCBs target L-type calcium channels, the major channel in muscle cells that mediates contraction. Similar to other DHP CCBs, isradipine binds directly to inactive calcium channels stabilizing their inactive conformation. Since arterial smooth muscle depolarizations are longer in duration than cardiac muscle depolarizations, inactive channels are more prevalent in smooth muscle cells. Alternative splicing of the alpha-1 subunit of the channel gives isradipine additional arterial selectivity. At therapeutic sub-toxic concentrations, isradipine has little effect on cardiac myocytes and conduction cells.

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