VA Class: CV200
Chemical Name: 4-(4-Benzofurazanyl)-1,4-dihydro-2,6-dimethyl-3,5-pyridinedicarboxylic acid methyl 1-methylethyl ester
Molecular Formula: C19H21N3O5
CAS Number: 75695-93-1
Brands: DynaCirc, DynaCirc CR
Uses for Isradipine
One of several preferred initial therapies in hypertensive patients with a high risk of developing CAD, including those with diabetes mellitus;72 in geriatric patients with isolated systolic hypertension;50 54 and in patients with coexisting angina.5 50
Can be used as monotherapy for initial management of uncomplicated hypertension; however, thiazide diuretics are preferred by JNC 7.72
Isradipine Dosage and Administration
Extended-release Core Tablets
Swallow extended-release core tablets intact; do not chew, divide, or crush.59
Extended-release Core TabletsOral
Hypertensive Urgencies or Emergencies†
Rapid Reduction of BP†Oral Capsules, Extended-release Tablets, or Extemporaneous Suspension
Children and adolescents 1–17 years of age: 0.05–0.1 mg/kg per dose.76
Prepare extemporaneous isradipine suspension containing 1 mg/mL for those unable to swallow capsules or extended-release tablets.76 81 Open twenty-four 5-mg capsules and grind the contents to a fine powder with a mortar and pestle;76 levigate with a small amount of glycerin to form a paste.81 Add simple syrup in increasing amounts while mixing thoroughly; transfer the suspension to a graduated cylinder.81 Add any remaining drug in the mortar to the graduated container; the final volume of the suspension should be 120 mL.81 Transfer contents of the graduated cylinder into an appropriate size amber bottle.81 The isradipine suspension is stable for 35 days when refrigerated.81 Shake well before each use.81
Initially, 1.25–2.5 mg twice daily 1 2 3 4 5 7 14 15 16 50 as monotherapy or when added to thiazide diuretic therapy.1 However, a dosage form suitable for administering 1.25-mg doses currently is not commercially available in the US.1 22
Full hypotensive effect may not be seen for 2–4 weeks.1 If BP control is inadequate after this period, increase dosage in increments of 5 mg daily at intervals of 2–4 weeks, up to a maximum of 20 mg daily, according to patient’s BP response.1 4 5 50 59
Extended-release Core TabletsOral
Initially, 5 mg once daily as monotherapy or when added to thiazide diuretic therapy.59
Conventional capsules: Maximum 0.8 mg/kg (up to 20 mg) daily.76
Extended-release core tablets: Maximum 0.8 mg/kg (up to 20 mg) daily.76
Select dosage of isradipine extended-release core tablets with caution because of age-related decreases in hepatic, renal, and/or cardiac function and concomitant disease and drug therapy.59
Cautions for Isradipine
Possible mild to moderate peripheral edema associated with vasodilation of arterioles and other small blood vessels; appears to be dose related.59
Use extended-release core tablets with caution in patients with preexisting GI narrowing; obstruction may occur.59
Insufficient experience with use of isradipine extended-release core tablets in patients ≥65 years of age to determine whether geriatric patients respond differently than younger adults; select dosage with caution.59
Common Adverse Effects
Headache, dizziness, peripheral edema, palpitation, tachycardia, flushing, chest pain.1 2 3 4 5 10 11 13 14 15 16 17 18 19 20 21 22 23 24 25 26 27 28 29 30 31 32 33 34 35 36 37 38 39 40 41 42 43 44 45 46 47 48 49 50 51 52 53 54
Interactions for Isradipine
Increased peak plasma concentrations and AUC of isradipine1
Monitor carefully; reduction of isradipine dosage may be required1
Increased isradipine metabolism and clearance; reduction of isradipine concentrations to below detectable levels1
Isradipine concentrations and therapeutic effects will be markedly reduced or abolished with concomitant use1
Pharmacokinetic or pharmacodynamic interaction unlikely
90–95% absorbed following oral administration of conventional capsules, with peak plasma isradipine concentrations attained in about 1.5 hours.1
In patients with hepatic impairment, the peak plasma concentration and AUC of conventional capsules are increased by 32 and 52%, respectively.1
In patients with mild renal impairment (Clcr 30–80 mL/min), the AUC of conventional capsules is increased by 45%; however, in patients with severe renal failure (Clcr <10 mL/min) who have been on hemodialysis, AUC is decreased by 20–50%.1
It is not known whether isradipine is distributed into milk.1
Plasma Protein Binding
Tight, light-resistant containers at 20–25°C.82
Extended-release Core Tablets
Advice to Patients
Importance of swallowing extended-release tablets whole; do not divide, chew, or crush.59
Advise patients that empty tablet shell of extended-release core tablets may be noticeable in stool.59
Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.
* available from one or more manufacturer, distributor, and/or repackager by generic (nonproprietary) name
Tablets, Extended-release core
This pricing information is subject to change at the sole discretion of DS Pharmacy. This pricing information was updated 02/2013. Actual costs to patients will vary depending on the use of specific retail or mail-order locations and health insurance copays.
DynaCirc CR 10MG 24-hr Tablets (GLAXO SMITH KLINE): 30/$129.99 or 90/$369.96
DynaCirc CR 5MG 24-hr Tablets (GLAXO SMITH KLINE): 30/$83.99 or 90/$232.51
Isradipine 2.5MG Capsules (WATSON LABS): 60/$79.99 or 180/$211.97
This report on medications is for your information only, and is not considered individual patient advice. Because of the changing nature of drug information, please consult your physician or pharmacist about specific clinical use.
The American Society of Health-System Pharmacists, Inc. and Drugs.com represent that the information provided hereunder was formulated with a reasonable standard of care, and in conformity with professional standards in the field. The American Society of Health-System Pharmacists, Inc. and Drugs.com make no representations or warranties, express or implied, including, but not limited to, any implied warranty of merchantability and/or fitness for a particular purpose, with respect to such information and specifically disclaims all such warranties. Users are advised that decisions regarding drug therapy are complex medical decisions requiring the independent, informed decision of an appropriate health care professional, and the information is provided for informational purposes only. The entire monograph for a drug should be reviewed for a thorough understanding of the drug's actions, uses and side effects. The American Society of Health-System Pharmacists, Inc. and Drugs.com do not endorse or recommend the use of any drug. The information is not a substitute for medical care.
AHFS Drug Information. © Copyright, 1959-2013, Selected Revisions September 16, 2011. American Society of Health-System Pharmacists, Inc., 7272 Wisconsin Avenue, Bethesda, Maryland 20814.
1. Reliant Pharmaceuticals. DynaCirc (isradipine) capsules prescribing information. Liberty Corner, NJ; 2003 Oct.
2. Lopez LM, Santiago TM. Isradipine—another calcium-channel blocker for the treatment of hypertension and angina. Ann Pharmacother. 1992; 26:789-99. [IDIS 298260] [PubMed 1535246]
3. Fitton A, Benfield P. Isradipine: a review of its pharmacodynamic and pharmacokinetic properties, and therapeutic use in cardiovascular disease. Drugs. 1990; 40:31-74. [PubMed 2143980]
4. Walton T, Symes LR. Felodipine and isradipine: new calcium-channel blocking agents for the treatment of hypertension. Clin Pharm. 1993; 12:261-75. [IDIS 311530] [PubMed 8458178]
5. Joint National Committee on Detection, Evaluation, and Treatment of High Blood Pressure. The fifth report of the Joint National Committee on Detection, Evaluation, and Treatment of High Blood Pressure (JNC V). Arch Intern Med. 1993; 153:154-83. [IDIS 309043] [PubMed 8422206]
6. Prisant LM, Carr AA, Nelson EB et al. Isradipine vs propranolol in hydrochlorothiazide-treated hypertensives: a multicenter evaluation. Arch Intern Med. 1989; 149:2453-7. [IDIS 260612] [PubMed 2530945]
7. Anon. Isradipine for hypertension. Med Lett Drugs Ther. 1991; 33:51-4. [PubMed 1827655]
8. Alderman MH. Which antihypertensive drugs first—and why! JAMA. 1992; 267:2786-7. Editorial.
9. Weber MA, Laragh JH. Hypertension: steps forward and steps backward: the Joint National Committee fifth report. Arch Intern Med. 1993; 153:149-52. [PubMed 8422205]
10. Dahlof B. Hemodynamic response, safety, and efficacy of isradipine in the treatment of essential hypertension. Am J Med. 1988; 86(Suppl 4A):19-26.
11. Kirkendall WM. Comparative assessment of first-line agents for treatment of hypertension. Am J Med. 1988; 84(Suppl 3B):32-41. [IDIS 243146] [PubMed 3260071]
12. Rauramaa R, Taskinen E, Seppanen K et al. Effects of calcium antagonist treatment on blood pressure, lipoproteins and prostaglandins. Am J Med. 1988; 84(Suppl 3B):93-6.
13. Cocco G, Alfiero R, Boxho G et al. Multicenter evaluation of the safety and efficacy of isradipine in hypertension. The Italian-Belgian Isradipine Study Group. Am J Med. 1989; 86(Suppl 4A):94-7.
14. Sundstedt CD, Ruegg PC, Keller A et al. A multicenter evaluation of safety, tolerability, and efficacy of isradipine in the treatment of essential hypertension. Am J Med. 1989; 86(Suppl 4A):98-102. [IDIS 254264] [PubMed 2523665]
15. De Keyser P, Bouve J, Clement D et al. Isradipine in essential hypertension: the Belgian general practitioners’ study. Am J Med. 1989; 86(Suppl 4A):103-9. [PubMed 2565687]
16. Anderton JL, Adams RM, Chowdary KVG et al. Evaluation of the safety and efficacy of isradipine in elderly patients with essential hypertension. The British Isradipine Hypertension Group. Am J Med. 1989; 86(Suppl 4A):110-14.
17. O’Rourke MF, Balasubramaniam A, Anavekar S et al. A multicenter evaluation of the safety and efficacy of isradipine and atenolol in the treatment of hypertension. Isradipine in Hypertension Study Group. Am J Med. 1989; 86(Suppl 4A):119-23.
18. Ruegg PC, Nelson DJ. Safety and efficacy of isradipine, alone and in combination, in the treatment of angina pectoris. Am J Med. 1989; 86(Suppl 4A):70-4. [IDIS 254258] [PubMed 2565689]
19. McGrath BP, Newman R, Older P. Hemodynamic study of short- and long-term isradipine treatment in patients with chronic ischemic congestive heart failure. Am J Med. 1989; 86(Suppl 4A):75-80. [IDIS 254259] [PubMed 2523660]
20. Chellingsworth MC, Willis JV, Jack DB et al. Pharmacokinetics and pharmacodynamics of isradipine (PN 200-110) in young and elderly patients. Am J Med. 1988; 84(Suppl 3B):72-9.
21. Cotting J, Reichen J, Kutz K et al. Pharmacokinetics of isradipine in patients with chronic liver disease. Eur J Clin Pharmacol. 1990; 38:599-603. [IDIS 268333] [PubMed 2142648]
22. Sandoz Pharmaceuticals Corp, East Hanover, NJ: Personal communication.
23. Glasser SP, Clark PI, Lipicky RJ et al. Exposing patients with chronic, stable, exertional angina to placebo periods in drug trials. JAMA. 1991; 265:1550-4. [PubMed 1671885]
24. National Heart, Lung, and Blood Institute. NHLBI panel reviews safety of calcium channel blockers. Rockville, MD; 1995 Aug 31. Press release.
25. National Heart, Lung, and Blood Institute. New analysis regarding the safety of calcium-channel blockers: a statement for health professionals from the National Heart, Lung, and Blood Institute. Rockville, MD; 1995 Sep 1.
26. Anon. NHLBI panel stands by JNC V in response to Circulation CCB article; AIM report supports use of beta blockers for prevention of sudden cardiac death. F-D-C Rep. 1995; 57(Sep 4):3- 4.
27. American Heart Association. Public advisory statement on calcium channel blocker drugs. Dallas, TX; 1995 Aug 28.
28. Psaty BM, Heckbert SR, Koepsell TD et al. The risk of myocardial infarction associated with antihypertensive drug therapies. JAMA. 1995; 274:620-5. [IDIS 352203] [PubMed 7637142]
29. Psaty BM, Heckbert SR, Koepsell TD et al. The risk of incident myocardial infarction associated with anti-hypertensive drug therapies. Circulation. 1995; 91:925.
30. Buring JE, Glynn RJ, Hennekens CH. Calcium channel blockers and myocardial infarction: a hypothesis formulated but not yet tested. JAMA. 1995; 274:654- 5. [IDIS 352205] [PubMed 7637148]
31. Furberg CD, Psaty BM, Meyer JV. Nifedipine: dose-related increase in mortality in patients with coronary heart disease. Circulation. 1995; 92:1326-31. [IDIS 353358] [PubMed 7648682]
32. Opie LH, Messerli FH. Nifedipine and mortality: grave defects in the dossier. Circulation. 1995; 92:1068-73. [IDIS 353353] [PubMed 7648646]
33. Kloner RA. Nifedipine in ischemic heart disease. Circulation. 1995; 92:1074-8. [IDIS 353354] [PubMed 7648647]
34. Yusuf S. Calcium antagonists in coronary artery disease and hypertension: time for reevaluation? Circulation. 1995; 92:1079-82. Editorial.
35. Lenfant C. The calcium channel blocker scare: lessons for the future. Circulation. 1995; 91:2855-6. [PubMed 7796490]
36. Habib GB. Are calcium antagonists harmful in hypertensive patients? Distinguishing hype from reality. Chest. 1995; 108:3-5. [IDIS 351406] [PubMed 7606987]
37. Horton R. Spinning the risks and benefits of calcium antagonists. Lancet. 1995; 346:586- 7. [IDIS 353102] [PubMed 7650997]
38. Yusuf S, Held P, Furberg C. Update of effects of calcium antagonists in myocardial infarction or angina in light of the Second Danish Verapamil Infarction Trial (DAVIT-II) and other recent studies. Am J Cardiol. 1991; 67:1295-7. [IDIS 284079] [PubMed 2035457]
39. Egstrup K, Andersen PE Jr. Transient myocardial ischemia during nifedipine therapy in stable angina pectoris, and its relation to coronary collateral flow and comparison with metoprolol. Am J Cardiol. 1993; 71:177- 83. [IDIS 308552] [PubMed 8421980]
40. Wagenknecht LE, Furberg CD, Hammon JW et al. Surgical bleeding: unexpected effect of a calcium antagonist. BMJ. 1995; 310:776-7. [IDIS 345035] [PubMed 7711582]
41. Miles Inc. American Heart Association, Dr. Psalty and Miles Inc. release statements qualifying possible risks of calcium channel blockers. West Haven, CT; 1995 Mar 15. Press release.
42. Dear healthcare professional letter regarding calcium-channel blockers and increased risk of heart attack. Chicago:Searle. 1995 Mar 17.
43. McClellan K. Unexpected results from MIDAS in atherosclerosis. Inpharma Wkly. 1994; Apr 9:4.
44. Anon. Groups act to dispel concerns about calcium-channel blockers. Am J Health-Syst Pharm. 1995; 52:1154, 1158. [PubMed 7656105]
45. Waters D. Proischemic complications of dihydropyridine calcium channel blockers. Circulation. 1991; 84:2598-600. [IDIS 295953] [PubMed 1959210]
46. Messerli FH. Case-control study, meta-analysis, and bouillabaisse: putting the calcium antagonist scare into context. Ann Intern Med. 1995; 123:888-9. [IDIS 356631] [PubMed 7486476]
47. Reviewers’ comments (personal observations).
48. Pratt Pharmacueticals. Procardia (nifedipine) capsules prescribing information (dated 1993 Feb). In: Physicians’ desk reference. 49th ed. Montvale, NJ: Medical Economics Company Inc; 1995:1906-7.
49. Held PH, Yusuf S, Furberg CD. Calcium channel blockers in acute myocardial infarction and unstable angina: an overview. BMJ. 1989; 299:1187-92. [IDIS 260789] [PubMed 2513047]
50. National Heart, Lung, and Blood Institute National High Blood Pressure Education Program. The sixth report of the Joint National Committee on Prevention, Detection, Evaluation, and Treatment of High Blood Pressure (JNC VI). Bethesda, MD: National Institutes of Health; 1997 Nov. (NIH publication No. 98-4080.)
51. Kaplan NM. Choice of initial therapy for hypertension. JAMA. 1996; 275:1577-80. [IDIS 365188] [PubMed 8622249]
52. Psaty BM, Smith NL, Siscovich DS et al. Health outcomes associated with antihypertensive therapies used as first-line agents: a systematic review and meta-analysis. JAMA. 1997; 277:739-45. [IDIS 380501] [PubMed 9042847]
53. American College of Cardiology and American Heart Association. ACC/AHA guidelines for the management of patients with acute myocardial infarction: a report of the American College of Cardiology/American Heart Association Task Force on Practice Guidelines (Committee on Management of Acute Myocardial Infarction). J Am Coll Cardiol. 1996; 28:1328-428. [IDIS 376249] [PubMed 8890834]
54. Staessen JA, Fagard R, Thijs L et al. for the Systolic Hypertension-Europe (Syst-Eur) Trial Investigators. Morbidity and mortality in the placebo-controlled European Trial on Isolated Systolic Hypertension in the Elderly. Lancet. 1997; 350:757-64. [IDIS 392056] [PubMed 9297994]
55. Izzo JL, Levy D, Black HR. Importance of systolic blood pressure in older Americans. Hypertension. 2000; 35:1021-4. [PubMed 10818056]
56. Frohlich ED. Recognition of systolic hypertension for hypertension. Hypertension. 2000; 35:1019-20. [PubMed 10818055]
57. Bakris GL, Williams M, Dworkin L et al. Preserving renal function in adults with hypertension and diabetes: a consensus approach. Am J Kidney Dis. 2000; 36:646-61. [IDIS 452007] [PubMed 10977801]
58. Associated Press (American Diabetes Association). Diabetics urged: drop blood pressure. Chicago, IL; 2000 Aug 29. Press Release from web site.
59. Reliant Pharmaceuticals, LLC. DynaCirc CR (isradipine) controlled release tablets prescribing information. Liberty Corner, NJ; 2005 Aug.
60. Appel LJ. The verdict from ALLHAT—thiazide diuretics are the preferred initial therapy for hypertension. JAMA. 2002; 288:3039-60. [IDIS 490723] [PubMed 12479770]
61. The ALLHAT Officers and Coordinators for the ALLHAT Collaborative Research Group. Major outcomes in high-riskhypertensive patients randomized to angiotensin-converting enzyme inhibitor or calcium channel blocker vs diuretic: the Antihypertensive and Lipid-Lowering Treatment to Prevent Heart Attack Trial (ALLHAT). JAMA. 2002; 288:2981-97. [IDIS 490721] [PubMed 12479763]
62. Velussi M, Brocco E, Frigato F et al. Effects of cilazapril and amlodipine on kidney function in hypertensive NIDDM patients. Diabetes. 1996; 45:216-22. [IDIS 362953] [PubMed 8549868]
63. Estacio RO, Jeffers BW, Hiatt WR et al. The effect of nisoldipine as compared with enalapril on cardiovascular outcomes in patients with non-insulin-dependent diabetes and hypertension. N Engl J Med. 1998; 338:645-52. [IDIS 400553] [PubMed 9486993]
64. Pahor M, Psaty BM, Furberg CD. Treatment of hypertensive patients with diabetes. Lancet. 1998; 351:689-90. [IDIS 409001] [PubMed 9504510]
65. Tatti P, Pahor M, Byington RP et al. Outcome results of the Fosinopril versus Amlodipine Cardiovascular Events randomized Trial (FACET) in patients
66. Byington RP, Craven TE, Furberg CD et al. Isradipine, raised glycosylated haemoglobin, and risk of cardiovascular events. Lancet. 1997; 350:1075-6. [IDIS 393279] [PubMed 10213554]
67. Alderman M, Madhavan S, Cohen H. Calcium antagonists and cardiovascular events in patients with hypertension and diabetes. Lancet. 1998; 351:216-7. [IDIS 398935] [PubMed 9449897]
68. Josefson D. Infarction risk found with calcium channel blocker. BMJ. 1998; 316:797.
69. Cutler JA. Calcium-channel blockers for hypertension—uncertainty continues. N Engl J Med. 1998; 338:679-81. [IDIS 400554] [PubMed 9486999]
70. Bayer, West Haven, CT: Personal communication on amlodipine.
71. Bakris GL, Copley JB, Vicknair N et al. Calcium channel blockers versus other antihypertensive therapies on progression of NIDDM associated nephropathy. Kidney Int. 1996; 50:1641-50. [PubMed 8914031]
72. National Heart, Lung, and Blood Institute National High Blood Pressure Education Program. The seventh report of the Joint National Committee on Prevention, Detection, Evaluation, and Treatment of High Blood Pressure (JNC VII) Express. Bethesda, MD: May 14 2003. From NIH website. (Also published in JAMA. 2003; 289.
73. American Diabetes Association. Position statements: treatment of hypertension in adults with diabetes. Diabetes Care. 2003; 26(Suppl 1):S80-S82.
74. Kaplan NM. The meaning of ALLHAT. J Hypertens. 2003; 21:233-4. [PubMed 12569243]
75. Guidelines Committee. 2003 European Society of Hypertension–European Society of Cardiology guidelines for the management of arterial hypertension. J Hypertension. 2003; 21:1011-53.
76. National High Blood Pressure Education Program Working Group on Hypertension Control in Children and Adolescents. The fourth report on the diagnosis, evaluation, and treatment of high blood pressure in children and adolescents. Pediatrics. 2004; 114(Suppl 2):555-76. [PubMed 15286277]
77. Wright JT, Dunn JK, Cutler JA et al. Outcomes in hypertensive black and nonblack patients treated with chlorthalidone, amlodipine, and lisinopril. JAMA. 2005; 293:1595-607. [IDIS 531054] [PubMed 15811979]
78. Neaton JD, Kuller LH. Diuretics are color blind. JAMA. 2005; 293:1663-6. [IDIS 531056] [PubMed 15811986]
79. Leenen FHH, Nwachuku CE, Black HR et al. Clinical events in high-risk hypertensive patients randomly assigned to calcium-channel blocker versus angiotensin-converting enzyme inhibitor in the Antihypertensive and Lipid-Lowering treatment to prevent Heart Attack Trial. Hypertension. 2006; 48:374-84. [PubMed 16864749]
80. Messerli FH, Staessen JA. Amlodipine better than lisinopril: how one randomized clinical trial ended fallacies from observational studies? Hypertension. 2006; 48:359-61. Editorial.
81. (Isradipine Suspension 1 mg/mL) In: Jew RK, Mullen RJ, Soo-Hoo W. Extemporaneous formulations. Bethesda, MD; American Society of Health-System Pharmacists, Inc: 2003:(page 32).
82. Cobalt Laboratories. Isradipine capsules prescribing information. Bonita Springs, FL; 2008 May.
More Isradipine resources
- Isradipine Prescribing Information (FDA)
- Isradipine Professional Patient Advice (Wolters Kluwer)
- isradipine Concise Consumer Information (Cerner Multum)
- isradipine Advanced Consumer (Micromedex) - Includes Dosage Information
- isradipine MedFacts Consumer Leaflet (Wolters Kluwer)
- DynaCirc Prescribing Information (FDA)
- DynaCirc CR extended-release tablets MedFacts Consumer Leaflet (Wolters Kluwer)
- DynaCirc CR Prescribing Information (FDA)