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 02/2014. 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
AHFS DI Essentials. © Copyright, 2004-2015, Selected Revisions September 16, 2011. American Society of Health-System Pharmacists, Inc., 7272 Wisconsin Avenue, Bethesda, Maryland 20814.
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